Auxiliary binding substance and drop-shaped tablet prepared on its base

FIELD: medicine.

SUBSTANCE: claimed invention relates to chemical-pharmaceutical industry and concerns auxiliary binding substances for manufacturing drop-shaped tablets and to preparation of drop-shaped tablets. Auxiliary binding substances according to claimed invention are selected from group which consists of monosaccharide, oligosaccharide, polysaccharide, sugar ester, sugar of alcohol structure, alpha-hydroxy acid, higher fatty acid derivative, higher aliphatic alcohol, polyol, urea and poly(ethyleneoxide) derivative.

EFFECT: claimed invention reduces toxicity caused by polyethylene glycol, improves drop-shaped tablet quality and accelerates development of drop-shaped tablets.

20 cl, 68 ex, 2 tbl

 

The technical field to which the invention relates.

This invention relates to a pharmaceutical formulation. More specifically, this invention relates to a binder auxiliary substances for the manufacture of tablets in the form of drops and prepared on the basis of their tablets in the form of drops.

Background of the invention

Tablets in the form of drops produced by dripping, namely solid or liquid drug is suspended or emuleret in a binder substance, the mixture is then infused into insoluble in the binder substance chilling environment for the formation of droplets in the form of a flattened sphere or spheroid after hardening. The latter can be administered orally or in the body cavity or can be used for preparation of solutions, etc. In comparison with other pharmaceutical formulations of tablets in the form of drops have many advantages, such as easy control of the device to dripping, small fluctuations in the weight of the tablets, the exact content of the pharmaceutically active ingredient, low loss medicines in the production process, stable quality and the ability to make the drug is highly effective, with long-term efficiency or fast action, etc. Formulation of tablets in the form of drops is particularly suitable for poorly soluble in water Lech of the public funds, which is hardly absorbed, and herbs containing volatile oils as effective components. Development of formulations of tablets in the form of a droplet meets the basic requirements of modern pharmaceutical formulation, such as "less than three", i.e. fewer injections, less toxicity and fewer side effects; "the three components of efficiency, i.e. high efficiency, long-lasting effect and a rapid onset of effect, and ease of administration, handling and storage, so they are promising with huge market potential.

Despite recent progress in the field of production equipment and a large number of drugs for the preparation of tablets in the form of drops of research on the creation and use of new binder excipients for tablets in the form of drops still moving slowly. Thus, as a binder excipient for most tablets in the form of drops is widely used polyethylene glycol (PEG) and sometimes used of polyoxyethylene the monostearate, gluten, poloxamer, sleeper and similar substances. From the point of view of the origin of the polyethylene glycol, polyoxyethylene the monostearate, poloxamer, polyester and similar substances are produced by artificial synthesis. Gluten get is from natural materials, mainly from the skin and bones of animals. From a security perspective, the materials obtained by chemical synthesis, such as polyethylene glycol, polyoxyethylene the monostearate, poloxamer, polyester and the like, are pharmaceutically acceptable, but they can cause some hemolysis. In addition, some chemical components, such as ethylene oxide, epoxypropan and the like, which have toxic side effects in humans, inevitably added to the above materials in the process of chemical synthesis. In addition, these chemically synthesized materials may be incompatible with many drugs, such as salicylic acid, diphenhydramine, potassium penicillin G, tetracycline, etc. that reduces therapeutic effect of these drugs. As gluten, its use is limited, as auxiliary materials of animal origin is prohibited to avoid infection, zoonotic diseases, such as mad cow disease, disease of the mouth and foot" (foot-and-mouth), etc.

In addition, long-term study showed that the tablets in the form of drops polyethyleneglycol were unstable due to various problems, for example, they tended to aging, cracking, etc. and Thus are urgent and require solving the problems is the creation of new binders for tablets in the form of drops and expand the scope of their application, adapting them to the extracts of Chinese medicine with different properties (hydrophilicity or lipophilicity) to create formulations of tablets in the form of drops and increase the content of active ingredient in the recipe.

Thus, the research and development of some new safe and non-toxic binder excipients for tablets in the form of drops are essential to improve the quality of tablets in the form of drops, expand the scope of tablets in the form of drops, the development of formulations of tablets in the form of drops and encouraging the internationalization of the formulation of tablets in the form of drops. However, the requirements of the manufacturing process of tablets in the form of drops, glue auxiliary substances are very hard, and after replacing the binder excipients usually difficult to manufacture tablets in the form of drops, which would satisfy the quality requirements. Thus, at present there are no substitutes of polyethylene glycol, which would be more suitable for use as a binder auxiliary substances.

Summary of invention

The purpose of this invention is the change in the situation, when chemically synthesized materials, such as polyethylene glycol, and further used as a binder auxiliary substances, croweded to the toxic and side effects, and at the same time there is a shortage of auxiliary substances of animal origin; reducing the use of chemically synthesized materials and materials of animal origin; providing natural, safe and non-toxic materials derived from plants, for use as a binder auxiliaries or main component of the binder excipients in tablets in the form of drops; stimulating the development of the formulation of tablets in the form of drops; the acceleration of the internationalization of tablets in the form of drops.

Another purpose of this invention is a method for preparing tablets in the form of drops with or mainly using natural binder auxiliary substances of plant origin.

Particularly this invention relates to the following:

1. The tablet is in the form of drops, which contains a pharmaceutically active ingredient and at least one pharmaceutically acceptable binding of auxiliary substances selected from the group consisting of a monosaccharide, oligosaccharide, polysaccharide, ether, sugar, sugar alcohol structure, alpha-hydroxy acid, a derivative of the higher fatty acids, higher aliphatic alcohol, polyol, urea, and derived poly(ethylene oxide).

2. The tablet is in the form of a droplet according to claim 1, which is while in the, that mentioned pharmaceutically active ingredient is an extract of the crude drug.

3. The tablet is in the form of a droplet according to claim 1, which is characterized in that the said pharmaceutically active ingredient is a chemically synthesized drug, antibiotic drug or biochemical means.

4. The tablet is in the form of a droplet according to claims 1-3, which is characterized by the fact that named as a binder excipient monosaccharide is a D-ribose, fructose, glucose, xylose; named as a binder excipient oligosaccharide represents trehalose, raffinose, maltose; named as a binder excipient polysaccharide is geloso; named as a binder excipients sugar ester is a sucrose esters,γ-lactone D-ribnovo acid; named as a binder excipients sugar alcohol structure is erythritol, sorbitol, xylitol, arabitol, isomaltitol, lactitol; named as a binder excipient alpha hydroxycitrate represents malic acid, citric acid; named as a binder excipient derivative of the higher fatty acids Ave is dstanley a sodium stearate, glycerol stearate, glycerol palmitate, shellac; named as a binder excipient aliphatic alcohol is cetyl alcohol, stearyl alcohol; named as a binder excipient polyol is phenylethyl; named as a binder excipient derived poly(ethylene oxide) is a polyoxyethylene the monostearate, polyoxyethyleneglycol ether; and the above-mentioned compounds containing crystal water.

5. The tablet is in the form of a droplet according to claims 1-3, which is characterized by the fact that these binder excipient is at least one of the auxiliary natural substances of vegetable origin selected from the group consisting of the following: sorbitol, xylitol, lactitol, maltose, sucrose esters, and the above-mentioned compounds containing crystal water.

6. The tablet is in the form of a droplet according to claims 1-5, which is characterized by the fact that these tablet in the form of droplets further comprises at least one plasticizer selected from the group consisting of the following: starch and its derivatives, cellulose and its derivatives, Arabian gum, dextran, chitin, sesbania (sesbania) gum, karragenana (carrageen) gum, Indian gum, Danish and the ar tragakant, carrageenan, tamarind gum, pectin, xanthan gum, alginic acid and its salt, dextrin, cyclodextrin, agar, lactose, polyvinylpyrrolidone, polyvinylpyrrolidone cross, carbomer, polyvinyl alcohol, acrylic resin acids, poloxamer, silicon dioxide, gluten, glycerol monostearate, polyoxyethylene the monostearate.

7. The tablet is in the form of a droplet according to claim 6, which differs in that the plasticizing component is one or more substances selected from the group which consists of the following: pregelatinized starch, carboximetilkrahmal, methylcellulose, sodium carboxymethyl cellulose, hypromellose, Arabian gum, alginic acid, dextrin, cyclodextrin, agar, lactose, glycerol monostearate, polyoxyethylene the monostearate, sodium carboxymethylcellulose cross, silicon dioxide.

8. The tablet is in the form of drops on PP and 7, which is characterized by the fact that these binder excipient contains lactitol and starch.

9. The tablet is in the form of drops on PP and 7, which is characterized by the fact that these binder excipient contains xylitol and Arabian gum.

10. The tablet is in the form of drops on PP and 7, which is characterized by the fact that these binder excipient contains EF the R sucrose and glycerol monostearate or polyoxyethylene the monostearate.

11. The tablet is in the form of drops on PP and 7, which is characterized by the fact that these binder excipient contains sucrose esters, polyoxyethylene the monostearate and sodium carboxymethylcellulose cross.

12. The tablet is in the form of drops on PP and 7, which is characterized by the fact that these binder excipient contains sucrose esters, polyoxyethylene the monostearate, sodium carboxymethylcellulose cross and silicon dioxide.

13. The tablet is in the form of a droplet according to claim 1, which differs in that the weight ratio of the binder excipients and pharmaceutically active ingredient is in the range of 1:0.1 to~1:1.

14. The tablet is in the form of a droplet according to claim 1, which differs in that the weight ratio of the binder excipients and pharmaceutically active ingredient is in the range 1:0,1~1:0,6.

15. Binder and excipients for tablets in the form of drops, which differs in that it includes xylitol and starch in a weight ratio of 1:0,2~1:0,3.

16. Binder and excipients for tablets in the form of drops, which differs in that it includes lactitol and starch in a weight ratio of 1:0,2~1:0,3.

17. Binder and excipients for tablets in the form of drops, which differs in that it contains xylitol and Arabian gum in a weight with the relation 1:0,2~1:0,4.

18. Binder and excipients for tablets in the form of drops, which differs in that it contains sucrose esters and glycerol monostearate or polyoxyethylene the monostearate in a weight ratio of 1:0.1 to~1:1.

19. Binder and excipients for tablets in the form of drops, which differs in that it contains sucrose esters, polyoxyethylene the monostearate and sodium carboxymethylcellulose cross in a weight ratio of 1:(0,1~1):(0,1~1).

20. Binder and excipients for tablets in the form of drops, which differs in that it contains sucrose esters, a plasticizing component, including polyoxyethylene the monostearate, sodium carboxymethylcellulose cross and silicon dioxide in a weight ratio of 15:(7~15):(0,1~2):(0,1~2).

Detailed description of the invention

The tablet is in the form of drops according to the present invention consists of drugs and natural binder excipients for tablets in the form of drops, mainly of plant origin. These medicines include extract of the crude(CSOs) drug(CSOs) means(a)chemically synthesized drug, antibiotic, and biological drug.

Extract from the raw(CSOs) drug(CSOs) means(a) in the present invention refers to extracts of all plant species, animal is x, mushrooms or mineral, and the like, which are commonly used traditional Chinese medicine in China or in the quality of medicines of natural origin in other countries, including the extract of one or more kinds of crude drugs or mixture of extracts. These extracts, namely the effective fraction of medical materials, such as extracting solution, extract and liquid extract, etc. that include hydrophilic and lipophilic components, and components of volatile oils and the like, are obtained by methods commonly used in the prior art, for example, carry out the immersion extraction or getting a decoction of the crude drug with water or organic solvents, such as methanol, ethanol, ethyl ether, petroleum ether, acetone, chloroform, etc., optionally in the presence of acid or alkali. The above components may be used after further purification by means well known in the prior art methods, such as ion exchange resin, macroporous absorption resin, membrane ultrafiltration, chromatography on a column of silica gel or aluminum column high-performance liquid chromatography and the like of the Above-mentioned mixture of the extracts can be obtained by extracting the above-mentioned mixtures of crude drug medium is in or mixing extracts of crude drugs or a combination of these two methods. These extracts of crude drugs usually include, but are not limited to, all kinds of well-known natural organic compounds, such as sugar, protein, nucleic acid, alkaloid, glycoside, coumarin and lignin, essential oil, including monoterpenoid and diterpenoids, triterpenoids and triterpenoid saponins, cardiac glycosides and steroid saponins, flavones, quinones, polyphenols, etc. Called the extracts of the present invention typically do not include Monomeric medicines used as chemical drugs extracted from plants and animals, such as morphine, paclitaxel, tetrodotoxin, reserpine, berberine, artemisin etc. Mentioned extracts of crude drugs of the present invention can be prepared using well known methods from the prior art or can be produced on an industrial scale.

Named chemically synthesized medicines, antibiotics or biochemical medicines according to the present invention represent Monomeric or low molecular weight chemotherapeutic drugs, antibiotics, proteins, nucleic acids and the like, with an established structure and/or unitary characteristics obtained by chemical synthesis or ekstragirovannye fermented material. Monomeric medicines extracted from plants and animals, is used as the actual Monomeric drug or further transformed into other substances, which can be used as medicines. Named chemically synthesized drugs, antibiotics or biochemical medicines according to the present invention include, but are not limited to, sedatives and sleeping pills, such as barbiturates, benzodiazepines etc.; analgesics, such as morphine, pethidine, methadone, etc.; anticholinergic agents such as atropine, anisodamine etc., blockers, α - and β-receptors; antagonists of H1-, H2-histamine receptors; an inhibitor of HMG coenzyme A; medicines for the treatment of diseases of the hepatobiliary system, such as schisandrin B, schisandrin C, bifendate, silymarin, ursodeoxycholic acid etc.; antipyretic analgesics and nonsteroidal anti-inflammatory drugs; anticancer drugs such as alkylating agents, natural and synthetic alkaloids, taxanes, anticancer antibiotics, natural, semisynthetic and synthetic antibiotics such as β-lactams, macrolides, aminoglycosides, chloramphenicol etc.; synthetic antibacterial agents, such as quinolones, sulfanilate the s etc.; antifungal drugs such as azoles, etc.; antiviral medicines such as agents, nucleoside and non-nucleoside nature; antiparasitic drugs; hormones, such as prostaglandins, peptides, steroids, vitamins, immune nucleic acids, bacteria, etc. They also include, but are not limited to, Monomeric medicines extracted from plants and animals used in chemotherapy. These chemically synthesized drugs, antibiotics or biochemical medicines may be used alone or as a complex of several of the above-mentioned chemically synthesized drugs, antibiotics or biochemical medicines.

Named binder excipient of the present invention include excipients, mainly obtained from natural materials, especially from plants. Binder excipients may optionally include a plasticizer component.

More particularly, named binder excipient of the present invention represents at least one of the excipients, selected from the group which consists of the following: a pharmaceutically acceptable monosaccharide, Oli is saharid, the polysaccharide ether sugar, sugar alcohol structure, alpha hydroxycitrate (fruit acid), a derivative of the higher fatty acids, higher aliphatic alcohol, a polyol, urea, a derivative of poly(ethylene oxide).

For the above-mentioned substances examples, not limiting the scope of the invention, include for these monosaccharide is D-ribose, fructose, glucose, xylose; for these oligosaccharide is trehalose, raffinose, maltose; for the above-mentioned polysaccharide - geloso; for the above-mentioned sugar ester - ether of sucrose, γ-lactone D-ribnovo acid; called sugar alcohol structure - erythritol, sorbitol, xylitol, arabitol, isomaltitol, lactitol; called alpha-hydroxy acid is malic acid, citric acid; named for the derivative of the higher fatty acids such as sodium stearate, glycerol stearate, glycerol palmitate, shellac; named for higher aromatic alcohol is cetyl alcohol, stearyl alcohol; for these polyol - phenylethyl; for a named derived poly(ethylene oxide) - polyoxyethylene the monostearate, polyoxyethylene alkilany ether; and the above-mentioned compounds containing crystal water.

For the above-mentioned substances named materials derived from plants include erythritol, sorbitol, fructose, γ-lactone D-ribnovo acid, arabitol, tre is also, D-ribose, geloso with a low melting point, shellac, xylitol, raffinose, glucose, malic acid, citric acid, isomaltitol, lactitol, maltose, xylose, sucrose esters, etc. and the above-mentioned compounds containing crystal water; examples mentioned chemically synthesized excipients or auxiliary substances derived from animals include phenylethyl, polyethylene glycol, cetyl alcohol, stearyl alcohol, sodium stearate, glycerol stearate, glycerol palmitate, urea, polyoxyethylene the monostearate, polyoxyethylene alkilany ether.

For the above-mentioned compounds, the most preferred one or more excipients selected from sorbitol, lactitol, maltose, sucrose esters and the above-mentioned compounds containing crystal water.

Connecting auxiliary substances are natural excipients, mostly derived from plants, this means that the binder auxiliary substances the contents of the auxiliary substances of plant origin is equal to or exceeds 50% by weight and a content of chemically synthesized auxiliary substances and auxiliary substances of animal origin is less than or equal to the contents of the auxiliary substances of plant origin. Preferably only the auxiliary substances of plant origin used in the binder auxiliary substances for tablets in the form of drops, or auxiliary substance of vegetable origin is a major component and apply only small amounts of chemically synthesized excipients or excipients of animal origin. The content of chemically synthesized auxiliary substances and auxiliary substances of animal origin was less than 50% by weight, preferably less than 40% by weight and more preferably less than 30% by weight. These natural auxiliary substances of vegetable origin indicate the following: auxiliary substance itself extracted from cells or tissues of plants, or products obtained by modification of plant extracts, such as derivation, etc. Called chemically synthesized excipients represent artificially synthesized low molecular weight compounds or polymers obtained by chemical synthesis from simple molecules of small size. These natural excipients of animal origin indicates the following: auxiliary substance itself extracted from cells or tissues from animals or products obtained by modification of animal extracts, such as derivation, etc.

Named binder auxiliary substances of plant origin may have or the Udut to have artificial synthetic products in the future. If artificial synthetic products have properties identical or similar to the natural properties of the binder auxiliary substances of vegetable origin, for example they have such characteristics as the safety and toxicity, they can be used as substitutes for the natural binding of auxiliary substances of vegetable origin, like the use of natural binders auxiliary substances of plant origin.

To improve the ability of the tablets in the form of drops to keep in shape, preferably the binder further comprises a plasticizing components. Named plasticizing components can be one or more components selected from the group consisting of the following: natural auxiliary substances of vegetable origin, such as starch and its derivatives, cellulose and its derivatives, Arabian gum, dextran, chitin, sesbania (sesbania) gum, karragenana (carrageen) gum, Indian gum, Danish agar, tragakant, carrageenan, tamarind gum, pectin, xanthan gum, alginic acid and its salt, dextrin, cyclodextrin, agar, lactose; chemically synthesized auxiliary substances and excipients of animal origin, such as polyvinylpyrrolidone polyvinyl religon cross, carbomer, polyvinyl alcohol, acrylic resin acids, poloxamer, silicon dioxide, gluten etc.

Examples of the above mentioned starch and its derivatives, not limiting the scope of the invention include pregelatinized starch, modified starch, hydroxypropylmethyl, carboximetilkrahmal etc. Examples mentioned cellulose and its derivatives, not limiting the scope of the invention include methylcellulose, microcrystalline cellulose, sodium carboxymethylcellulose, hypromellose, sodium carboxymethylcellulose cross, hydroxyethylmethylcellulose, hydroxyethyl cellulose, hydroxypropylcellulose.

Preferably named plasticizing components may represent one or more components selected from the group consisting of the following: pregelatinized starch, carboximetilkrahmal, methylcellulose, sodium carboxymethyl cellulose, hypromellose, Arabian gum, alginic acid, dextrin, cyclodextrin, agar and lactose. In addition, as a plasticizer in conjunction with other binders auxiliary substances may be used glycerol monostearate and polyoxyethylene the monostearate.

The named components of plant origin indicate the following: the subsidiary in the society, itself extracted from cells or tissues of a plant or obtained by modification of plant extracts, such as derivation, etc. Called chemically synthesized excipients represent artificially synthesized low molecular weight compounds or polymers obtained by chemical synthesis from simple molecules of small size. These natural excipients of animal origin indicates the following: auxiliary substance itself extracted from cells or tissues of animals or obtained by the modification of animal extracts, such as derivation, etc.

Possibly named plasticizing components of plant origin had or will have in the future, artificial synthetic products. If artificial synthetic products have properties identical or similar to the plasticizing properties of natural components of vegetable origin, for example they have such characteristics as the safety and toxicity, they can be used as substitutes for natural plasticizing components of plant origin, like the use of natural binders auxiliary substances of plant origin.

Named binder excipient selected from monosugar is Yes, oligosaccharide, polysaccharide, ether, sugar, sugar alcohol structure, alpha-hydroxy acid, a derivative of the higher fatty acids, higher aliphatic alcohol, polyol, urea, a derivative of poly(ethylene oxide), etc., preferably the binder auxiliary agents of vegetable origin, selectively combined with the mentioned plasticizing components in accordance with the characteristics of the medicinal product. Preferred combinations include, but are not limited to, the following: xylitol and starch, lactitol and starch, xylitol and the Arabian gum; sugar ester and glycerol monostearate; sugar ester and polyoxyethylene the monostearate; sugar ester, polyoxyethylene the monostearate and sodium carboxymethylcellulose cross; sucrose esters, polyoxyethylene the monostearate, sodium carboxymethylcellulose cross and silicon dioxide. The weight ratio of these binders excipients and plasticizing component is 1:0~1:1.5 and preferably 1:0.1 to~1:0,9; most preferably 1:0,1~1:0,5.

For the above mentioned binder excipient preferred weight ratio of xylitol and starch is 1:0,2~1:0,3.

For the above mentioned binder excipient preferred weight ratio of lactitol and starch SOS is to place 1:0,2~1:0,3.

For the above mentioned binder excipient preferred weight ratio of xylitol and Arabian gum is 1:0,2~1:0,4.

For the above mentioned binder excipient preferred weight ratio of sugar ester and glycerol monostearate is 1:0.1 to~1:1, most preferably 1:0.5 in.

For the above mentioned binder excipient preferred weight ratio of sugar ester and polyoxyethylene monostearate of is 1:0.1 to~1:1, most preferably 1:0.5 in.

For the above mentioned binder excipient preferred weight ratio of sugar ester, of polyoxyethylene monostearate and sodium carboxymethylcellulose cross is 1:(0,1~1): (0,1~1), most preferably 1:0,4:0,6.

For the above mentioned binder excipient preferred weight ratio of sugar ester, of polyoxyethylene monostearate, sodium carboxymethylcellulose cross and silicon dioxide is 15:(7~15):(0,1-2):(0,1~2), most preferably 15:11:1:1.

The weight ratio of the binder excipient in tablets in the form of drops and the active ingredient is 1:0.1 to~1:1; preferably 1:0.1 to~1:0,6; most preferably 1:0,2~1:0,4.

One or more named binder excipients used the tablets in the form of drops according to the present invention, the weight ratio of the binder excipient and active ingredient complies with the above requirements, and the weight ratio of the binder excipient and plasticizing component also complies with the above requirements.

The process of making tablets in the form of drops can use the traditional way, such as tablets in the form of drops can be produced in accordance with the following procedures:

A. Choose one or more binders excipients listed above or select at least one binder and excipients, and one or more named plasticizer and mixing them until a homogeneous state.

b. Transfer the above(s) homogenized(s) binder(s) support(s) substance(s) or binder mixture of excipients in the car for dripping, add the active ingredients and mix named a mixture of a binder(it) support(CSOs) substances(a) and the active ingredient prior to homogenization.

C. Heat the mixture obtained in step b, to melt, drip molten mixture in the cooling fluid, and after curing is filtered tablets in the form of drops.

d. Remove the cooling fluid from the surface of the tablets in the form of drops of zentrifugenbau the M.

that is, After removal of the cooling medium is dried tablets in the form of drops at low temperature and get these tablets in the form of drops.

Set forth in the preparation of tablets in the form of drops the weight ratio of the binder excipient and plasticizing component is 1:0~1:5; preferably 1:0.1 to~1:0,9; most preferably 1:0.1 to~1:0,5. The purpose of adding a plasticizing component is to improve internal cohesion and plasticity of tablets in the form of drops. Added named plasticizing component or not, mainly depends on the properties of the active ingredient. If the active ingredient itself has good ductility and property internal clutch in the plasticizing component is not necessary or required in much smaller quantities. If the active ingredient has no such properties, you need a certain amount of plasticizing component.

Set forth in the preparation of tablets in the form of drops the weight ratio of the binder excipients and the active ingredient is 1:0.1 to~1:1; more preferably 1:0.1 to~1:0,6; most preferably 1:0,2~1:0,4.

Set forth in the preparation of tablets in drops while stirring the mixture of active ingredients with a binder sun is magatelli substances is 10-30 minutes. After homogenization, the temperature to which it is necessary to heat the mixture to melt and drop is 45-95°C., more preferably 60-95°C. Examples of the cooling medium include liquid paraffin, methanesiliconic or vegetable oil, including oil from the beans, castor oil and the like; preferred are liquid paraffin, methanesiliconic oil. Coolant temperature is from -20°C to 30°C, preferably 0~18°C. the Internal diameter of the drops is 1.0~4.0 mm, preferably of 1.2~2.5 mm is Preferred a smaller difference between the outer diameter and the inner diameter of the device to drop.

It should be noted that the invention will be better understood if the above information is illustrated by the examples which do not limit the variations of the process of preparation of tablets in the form of drops.

In addition to such advantages of traditional tablets in the form of drops, such as ease of preparation, stable quality, the introduction of liquid active ingredient in solid form, the traditional way of introduction, as well as high efficacy and rapid onset of effect, the greatest advantage of tablets in the form of drops, prepared according to the present invention, is the following: a binder excipient used in the present invention,are of vegetable origin or mainly include auxiliary binder substance of plant origin. Connecting auxiliary substances derived from natural plants, not only are pharmaceutically acceptable, but are widely used as additives in the food industry. As mentioned binder excipient is not only absolutely safe without any toxic and side effects, but are also very cheap and affordable, it has a great value for the application and popularization, thus creating a solid Foundation for the internationalization of these tablets in the form of drops.

Further, the present invention is more explained by using examples, but is not limited to them.

Except where otherwise indicated medical materials, extracts from medical materials and chemical medicines indicated in the following examples are products produced on an industrial scale, or get them using traditional methods of the prior art, and all reagents for their production are produced on an industrial scale.

Examples

Example 1

Radix Puerariae daidzein 20 g trehalose 35 g, dextrin 20,

Trehalose and dextrin fully mixed and transferred to the car to drop where add Radix Puerariae daidzein. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at a temperature of 90°Crespellano mixture drip at a temperature of 80°C in a cooling medium (liquid paraffin), having a temperature of 4°C, with a speed of 35 drops per minute. After giving drops form liquid paraffin on the surface of tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve on average for 5,14 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 2

The extract obtained from Radix Ginseng, Radix Ophiopogonis, Fructus Schisandrae in a weight ratio of 1:2:1.

Named extract 15 g, arabitol 35 g, hypromellose 12 g, xanthan gum 6,

Arabitol, hypromellose and xanthan gum fully mixed and transferred into a machine for drop where add named extract. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at a temperature of 90°C. the Melted mixture to drip at a temperature of 80°C in a cooling medium (liquid paraffin)having a temperature of 8°C, with a rate of 40 drops per minute. After giving drops parmigiani wax from the surface of the tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve on average for 2,98 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 3

The extract of Radix Salviae Miltiorrhizae 13 g of the extract of Radix Notoginseng (WO 02/058625 A2) 5 g, borneol 1.2 g, lactitol 45 g, pregelatinized starch, 12,

Lactitol and pregelatinized starch is fully mixed and transferred into a machine for drop where add the extract of Radix Salviae Miltiorrhizaer extract, Radix Notoginseng and borneol. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at a temperature of 83°C. the Melted mixture to drip at a temperature of 70°C in the cooling fluid (methanesiliconic oil)having a temperature of 0°C, with a speed of 35 drops per minute. After giving drops form methanesiliconic oil from the surface of the tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same razmara is, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve in an average of 3.96 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 4

Radix Paeoniae Alba, Herba Ephedrae and Radix Glycyrrhizae extracted with water; Rhizoma Pinelliae Preparata, Rhizoma Zingiberis and Fructus Schisansrae Chinensis extracted with ethanol. The above two extractive solution combine and concentrate to the condition of the extract; essential oil obtained by distillation of Herba Asari, Ramulus Cinnamomi, respectively.

These extracts 16 g, arabitol 20 g, carboximetilkrahmal 16 year

Lactitol and carboximetilkrahmal fully mixed and transferred into a machine for drop where add the extracts and essential oil. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at a temperature of 80°C. the Melted mixture to drip at a temperature of 70°C in a cooling medium (liquid paraffin)having a temperature of 4°C, with a rate of 40 drops per minute. After giving drops form liquid paraffin on the surface of tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tabla is key in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve in an average of 3.10 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 5

Rhizoma Coptidis, Cortex Phellodendri, Fructus Gardeniae and Radix Scutellariae with weight ratio of 1.6:1,1:1,1:2,2 extracted with water, precipitating with ethanol, then concentrate to obtain the extract.

Named extract 12 g, xylitol 30 g, methylcellulose 18 g, starch 5 g

Xylitol and methylcellulose fully mixed and transferred into a machine for drop where add the extract and essential oil. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at a temperature of 90°C. the Melted mixture to drip at a temperature of 85°C in a cooling medium (liquid paraffin)having a temperature of 10°C, with a rate of 30 drops per minute. After giving drops form liquid paraffin on the surface of tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination in the time of collapse, according to the way the Chinese Pharmacopoeia (2000) show that tablet in the form of drops completely and easily pass through a wire sieve on average for 3,76 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 6

Extract of leeches (Whitmania pigra Whitman) 20 g sorbitol 40 g, methylcellulose 15,

Sorbitol and methylcellulose fully mixed and transferred into a machine for drop where add extract of leeches. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at a temperature of 85°C. the Melted mixture to drip at a temperature of 80°C in a cooling medium (liquid paraffin)having a temperature of 8°C, with a speed of 35 drops per minute. After giving drops form liquid paraffin on the surface of tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve in an average of 4.10 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 7

Radix Bupleuri is extracted with hot water, precipitated with alcohol, then it will centerour to extract.

Named extract 18 g, xylitol 35 g, starch 12 year

Sorbitol and starch is fully mixed and transferred into a machine for drop where add extract. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at a temperature of 85°C. the Melted mixture to drip at a temperature of 75°C in the cooling fluid (methanesiliconic oil)having a temperature of 4°C, with a speed of 35 drops per minute. After giving drops form methanesiliconic oil from the surface of the tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve on average 3.25 per min, which meets the requirements of the Chinese Pharmacopoeia.

Example 8

Essential oil of Radix Bupleuri get in the way supercritical extraction, the residue is extracted to obtain saikosaponin as an effective component, and then the extract.

Named extract 20 g maltose 40 g, carboxymethylcellulose 10,

Maltose and carboxymethylcellulose fully mixed and transferred into a machine for drop where add the extract and essential oil. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at a temperature of 85°C. the Melted mixture to drip at a temperature of 70°C in a cooling medium (liquid paraffin)having a temperature of 5°C, with a speed of 35 drops per minute. After giving drops form liquid paraffin on the surface of tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve in an average 4,15 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 9

Oil of Blumea poplar (L.) DC 14 grams borneol 1 g, lactitol 35 g, Arabian gum 20g

Lactitol and Arabian gum fully mixed and transferred into a machine for drop where add oil of Blumea poplar (L.) DC and borneol. The mixture is stirred until homogenization, and then heated to melting the use of a water bath at 70°C. The melted mixture to drip at 60°C in a cooling medium (liquid paraffin)having a temperature of 0°C, with a speed of 35 drops per minute. After giving drops form liquid paraffin on the surface of tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve in an average of 3.43 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 10

The extract of Radix Salviae Miltiorrhizae and Radix Notoginseng (Chinese patent number CN 1348815 A) 12 g, borneol 1.2 g, xylitol 40 g starch 8,

Xylitol and the starch is fully mixed and transferred into a machine for drop where add the extract of Radix Salviae Miltiorrhizaer extract, Radix Notoginseng and borneol. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at a temperature of 80°C. the Melted mixture to drip at a temperature of 64°C in the cooling fluid (methanesiliconic oil)having a temperature of 0°C, with a rate of 40 drops per minute. After giving to ply form methanesiliconic oil from the surface of the tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve on average for 3,63 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 11

The extract of Radix Puerariae (the content of Pueraria flavones more than 80%) 15 g, lactitol 25 g, karragenana (carrageen) gum 20 g starch 6,

Lactitol, carragenin (carrageen) gum and starch is fully mixed and transferred into a machine for drop where add the extract of Radix Puerariae. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at a temperature of 90°C. the Melted mixture to drip at a temperature of 85°C in the cooling fluid (methanesiliconic oil)having a temperature of 10°C, with a rate of 40 drops per minute. After giving drops form methanesiliconic oil from the surface of the tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and without Schlei the project. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve in an average of 3.64 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 12

The extract of Radix Puerariae (the content of Pueraria flavones more than 40% and the content of puerarin more than 28%) 15 g, 25 g fructose, karragenana (carrageen) gum 20 g starch 6,

Fructose, carragenin (carrageen) gum and starch is fully mixed and transferred into a machine for drop where add the extract of Radix Puerariae. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at a temperature of 90°C. the Melted mixture to drip at a temperature of 85°C in a cooling medium (liquid paraffin)having a temperature of 10°C, with a speed of 35 drops per minute. After giving drops form liquid paraffin on the surface of tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops on the ability and without difficulty pass through a wire sieve in an average of 3.15 min, that meets the requirements of Chinese Pharmacopoeia.

Example 13

Oleum Rhododendri Daurici 13 g, isomaltitol 20 g of alginic acid 15 g

Isomaltitol and alginic acid are fully mixed and transferred into a machine for drop where add Oleum Rhododendri Daurici. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at a temperature of 80°C. the Melted mixture to drip at a temperature of 70°C in a cooling medium (liquid paraffin)having a temperature of 4°C, with a speed of 35 drops per minute. After giving drops form liquid paraffin on the surface of tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve in an average of 3.78 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 14

Oleum Viticis Maple 12 g, isomaltitol 35 g, karragenana (carrageen) gum 12 year

Isomaltitol and carragenine (carrageen) gum fully mixed and transferred into a machine for the drop is obrazovaniya, where add Oleum Viticis Maple. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at a temperature of 80°C. the Melted mixture to drip at a temperature of 65°C in a cooling medium (liquid paraffin)having a temperature of 0°C, with a speed of 35 drops per minute. After giving drops form liquid paraffin on the surface of tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve on average for 3,55 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 15

The extract of Radix Salviae Miltiorrhizae and Radix Notoginseng (Chinese patent number CN 1348815 A) 22 g, borneol 1.5 g, lactitol 40 g, Arabian gum 15,

Lactitol and Arabian gum in the recipe fully mixed and transferred into a machine for drop where add the extract of Radix Salviae Miltiorrhizae extract, Radix Notoginseng and borneol. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at the same time is the temperature value of 85°C. The melted mixture to drip at a temperature of 64°C in the cooling fluid (methanesiliconic oil)having a temperature of 4°C, with a rate of 40 drops per minute. After giving drops form methanesiliconic oil from the surface of the tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve in an average of 4.25 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 16

Extracts of Flos Lonicerae, Radix Scutellariae, Fructus Forsythiae with weight ratio of 1:1:2.

These extracts 20 g, arabitol 35 g, cyclodextrin 15,

Arabitol and cyclodextrin fully mixed and transferred into a machine for drop where add extract. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at 95°C. the Melted mixture to drip at a temperature of 80°C in a cooling medium (liquid paraffin)having a temperature of 10°C, with a speed of 35 drops per minute. After giving cap the holes form of liquid wax from the surface of the tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve on average for 3,68 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 17

Starlily ether 12 g, borneol 0.5 g, xylitol 40 g, hypromellose 10,

Xylitol and hypromellose fully mixed and transferred into a machine for drop where add starlily ether and borneol. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at a temperature of 75°C. the Melted mixture to drip at 60°C in a cooling medium (liquid paraffin)having a temperature of 0°C, with a speed of 35 drops per minute. After giving drops form liquid paraffin on the surface of tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the decay time with the public the way the Chinese Pharmacopoeia (2000) show that tablet in the form of drops completely and easily pass through a wire sieve in an average of 3.10 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 18

Essential oil of Rhizoma Chuanxiong get in the way supercritical extraction, the residue is extracted with ethanol low concentration, and concentrate to obtain the extract.

Named extract 12 g, borneol 0.5 g, lactitol 35 g, alginic acid 15 g

Lactitol and alginic acid are fully mixed and transferred into a machine for drop where add essential oil of Rhizoma Chuanxiong and borneol. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at a temperature of 85°C. the Melted mixture to drip at a temperature of 65°C in a cooling medium (liquid paraffin)having a temperature of 0°C, with a speed of 35 drops per minute. After giving drops form liquid paraffin on the surface of tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops t is firm and easily pass through a wire sieve on average for 3,22 min, that meets the requirements of Chinese Pharmacopoeia.

Example 19

Extract of Erigeron brevsicapus (Vant) Hand-Mazz, Folium Ginkgo, Radix Salviae Miltiorrhizae and natural borneol is prepared according to the method of preparation of tablets in the form of drops wendsankma (yinzhanxinmai) (National Assembly Specifications Preparation of Proprietary Traditional Chinese Medicine, part of the Internal medicine and Heart).

Named extract 15 g, arabitol 40 g, dextrin 12 g, xanthan gum 5,

Arabitol, dextrin, xanthan gum fully mixed and transferred into a machine for drop where add extract and borneol. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at a temperature of 90°C. the Melted mixture to drip at a temperature of 75°C in the cooling fluid (methanesiliconic oil)having a temperature of 8°C, with a speed of 35 drops per minute. After giving drops form methanesiliconic oil from the surface of the tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tabletki in the form of drops completely and easily pass through a wire sieve in an average of 4.16 min, that meets the requirements of Chinese Pharmacopoeia.

Example 20

Extract of Rhizoma Chuanxiong ethyl ester, 7.5 g; extract of Radix Angelicae Sinensis ethyl ether 13.5 g; γ-lactone D-ribnovo acid 30 g; karragenana (carrageen) gum 12 year

γ-lactone D-ribnovo acid and carragenine (carrageen) gum fully mixed and transferred into a machine for drop where add Rhizoma extract Chuanxlong and Radix Angelicae Sinensis ethyl ether. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at a temperature of 85°C. the Melted mixture to drip at a temperature of 75°C in a cooling medium (liquid paraffin)having a temperature of 4°C, with a speed of 35 drops per minute. After giving drops form liquid paraffin on the surface of tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve on average for at 3.35 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 21

Sonqi tofal in saponins std. 12 g of xylitol 35 g, lactose 12 g, Arabian gum 5,

Xylitol, lactose and Arabian gum fully mixed and transferred into a machine for drop where add Sonqi tofal in saponins std. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at a temperature of 85°C. the Melted mixture to drip at a temperature of 75°C in a cooling medium (liquid paraffin)having a temperature of 10°C, with a speed of 35 drops per minute. After giving drops form liquid paraffin on the surface of tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve on average for the 4.65 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 22

Essential oil Cinnamomum migao H.W.Li extracted evaporative distillation with water, 5 g; ethanol extract of Bulbus Alli Macrostemi 4 g; natural borneol 2 g; sorbitol 30 g; alginic acid 15 g

Sorbitol and alginic acid fully stirred and perenosyat machine for drop where add essential oil Cinnamomum migao H.W.Li extract of Bulbus Alli Macrostemi and natural borneol. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at a temperature of 80°C. the Melted mixture to drip at a temperature of 75°C in a cooling medium (liquid paraffin)having a temperature of 0°C, with a speed of 35 drops per minute. After giving drops form liquid paraffin on the surface of tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve in an average of 3.78 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 23

Andrographolide 15 grams of xylitol 40 g, hypromellose 13 g, starch 8,

Xylitol, hypromellose and the starch is fully mixed and transferred into a machine for drop where add Andrographolide. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath with temperature is round 90°C. The melted mixture to drip at a temperature of 80°C in a cooling medium (liquid paraffin)having a temperature of 4°C, with a speed of 35 drops per minute. After giving drops form liquid paraffin on the surface of tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve on average for 4,96 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 24

Cyclovirobuxine D 12 g, lactitol 30 g tragakant 15,

Lactitol and tragakant fully mixed and transferred into a machine for drop where add cyclovirobuxine D. the Mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at a temperature of 90°C. the Melted mixture to drip at a temperature of 85°C in a cooling medium (liquid paraffin)having a temperature of 10°C, with a speed of 35 drops per minute. After giving drops form liquid paraffin on the surface of tablets in the form of drops absorb with absorber the soup of paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve in an average to 4.23 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 25

Tinidazole 8 g sorbitol 30 g, polyvinylpyrrolidone 10,

Sorbitol and polyvinylpyrrolidone fully mixed and transferred into a machine for drop where add tinidazole. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at a temperature of 90°C. the Melted mixture to drip at a temperature of 80°C in a cooling medium (liquid paraffin)having a temperature of 8°C, with a speed of 35 drops per minute. After giving drops form liquid paraffin on the surface of tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that tab is ETCI in the form of drops completely and easily pass through a wire sieve on average for 5,62 min, that meets the requirements of Chinese Pharmacopoeia.

Example 26

Flavones Scabisa Comosa Fisch, extracted with 60% ethanol 15 g; lactitol 40 g; chitin 12 g; xanthan gum 5,

Lactitol, chitin and xanthan gum fully mixed and transferred into a machine for drop where add flavones Scabisa Comosa Fisch. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at a temperature of 90°C. the Melted mixture to drip at a temperature of 75°C in a cooling medium (liquid paraffin)having a temperature of 4°C, with a speed of 35 drops per minute. After giving drops form liquid paraffin on the surface of tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve on average for 4,72 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 27

Rutin 10 g, shellac 35 g, hypromellose 15,

Shellac and hypromellose fully mixed and transferred into a machine for drop where add rutin. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at a temperature of 90°C. the Melted mixture to drip at a temperature of 85°C in the cooling fluid (methanesiliconic oil)having a temperature of 8°C, with a rate of 40 drops per minute. After giving drops form methanesiliconic oil from the surface of the tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve on average for 5,43 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 28

Extract of Polygala tenuifolia Wild; prepared according to the method of obtaining the tincture polygala (polygala), described in the Chinese Pharmacopoeia 2000 (1st addition).

Named extract 12 g, raffinose 30 g; tragakant 12 year

The raffinose and tragakant fully mixed and transferred into a machine for drop where add extract. The mixture is stirred until homogenization, and then heated to melting with COI is whether the water bath at a temperature of 90°C. The melted mixture to drip at a temperature of 75°C in a cooling medium (liquid paraffin)having a temperature of 4°C, with a speed of 35 drops per minute. After giving drops form liquid paraffin on the surface of tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve in an average of 4.38 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 29

Extract of Cortex Moutan and a rhizome Chuanxiong, prepared according to the method of preparation of tablets in the form of drops axiorsontor (suxiaoxintong), described in the National Assembly Specifications Preparation of Proprietary Traditional Chinese Medicine, vol 19.

Named extract 15 g, sorbitol 35 g, starch 20 g

Sorbitol and starch is fully mixed and transferred into a machine for drop where add extract and borneol. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at a temperature of 90°C. Raspravleny the second mixture drip at a temperature of 80°C in a cooling medium (liquid paraffin), having a temperature of 5°C, with a speed of 35 drops per minute. After giving drops form liquid paraffin on the surface of tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve in an average of 3.42 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 30

The distillate was obtained by distillation or by distillation of Radix Bupleuri, then the distillate was loaded into a column of macroporous absorption resin, further suirable the column with ethanol and the eluate was concentrated to obtain essential oil of Radix Bupleuri.

Essential oil of Radix Bupleuri 15 g, lactitol 35 g, karragenana (carrageen) gum 20g

Lactitol and carragenine (carrageen) gum fully mixed and transferred into a machine for drop where add essential oil of Radix Bupleuri. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at a temperature of 80°C. the Melted mixture to drip at a temperature of 65°C in cooling the th environment (liquid paraffin), having a temperature of 4°C, with a speed of 35 drops per minute. After giving drops form liquid paraffin on the surface of tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve on average for 2,98 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 31

The extract of Radix Platycodi, polygala ternifolia Willd., Flos Farfarae, Radix Glycyrrhizae, prepared according to the method of Table powder connections Platycodon of the National Assembly Specifications Preparation of Proprietary Traditional Chinese Medicines of Ministry of health, volume 4.

Named extract 18 g, maltose 40 g, carboximetilkrahmal 12 g of polyoxyethylene alkilany ether 6,

Maltose, carboximetilkrahmal and polyoxyethylene alkilany ether fully mixed and transferred into a machine for drop where add extract. The mixture is stirred until homogenization, and then heated to melting with the use of the water bath when the tempo is the atur 90°C. The melted mixture to drip at a temperature of 82°C in the cooling fluid (methanesiliconic oil)having a temperature of 6°C, with a speed of 35 drops per minute. After giving drops form methanesiliconic oil from the surface of the tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve on average for 5,32 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 32

Thymol 14 g, oil of cloves 2.25 g, sorbitol 45 g, methylcellulose 15,

Sorbitol and methylcellulose fully mixed and transferred into a machine for drop where add thymol and clove oil. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at 70°C. the Melted mixture to drip at 60°C in a cooling medium (liquid paraffin)having a temperature of 0°C, with a speed of 35 drops per minute. After giving drops form liquid paraffin with the surface tablets forms the droplets absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve on average for 3,74 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 33

The weight ratio of Radix Aconiti Lateralis Preparata, Radix Glycyrrhizae and Rhizoma Zingiberis is 1:1:9. Radix Aconiti Lateralis Preparata was extracted with an acidic aqueous solution, precipitated with ethanol and then concentrated to a state of extract and dried under vacuum. Radix Glycyrrhizae was extracted with aqueous ammonia solution, the extract was concentrated, precipitated with acid, centrifuged to obtain a precipitate, the precipitate was ground and sifted; the mixture was obtained by mixing the above two extracts. Essential oil of Rhizoma Zingiberis received evaporative distillation with water.

Named a blend of extracts of 14 g D-ribose 35 g, agar 15 g, Arabian gum 5,

D-Ribose, agar and the Arabian gum fully mixed and transferred into a machine to drop, which add a mixture of extracts and essential oil of Rhizoma Zingiberis. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at a temperature of 85°C. Races is Lavandou mixture drip at a temperature of 75°C in a cooling medium (liquid paraffin), having a temperature of 3°C, with a speed of 35 drops per minute. After giving drops form liquid paraffin on the surface of tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve on average for 5,22 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 34

Extract of Cortex Cinnamomi, Rhizoma Chuanxiong, Rhizoma Cyperi was obtained by the method of preparation of tablets in the form of drops of xinchangdong (xintongning), described in the National Assembly Specifications Preparation of Proprietary Traditional Chinese Medicines of Ministry of health, volume 15.

Named extract 12 g, erythritol 14 g, starch 15 g, polyvinylpyrrolidone 5,

Erythritol, starch and polyvinylpyrrolidone fully mixed and transferred into a machine for drop where add extract. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at a temperature of 85°C. the Melted mixture to drip PR is a temperature of 75°C in a cooling medium (liquid paraffin), having a temperature of 4°C, with a speed of 35 drops per minute. After giving drops form liquid paraffin on the surface of tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve in an average 4,15 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 35

Extract of Boswellia carteri, Lignum Santali Albun, Radix Aristolochiae was obtained by the method of preparation of tablets in the form of drops guanxixue (guanxinsuhe), described in the National Assembly Specifications Preparation of Proprietary Traditional Chinese Medicines of Ministry of health, volume 12.

Named extract 10 g sorbitol 32 g, karragenana (carrageen) gum 18 g, starch 5 g

Sorbitol, carragenin (carrageen) gum and starch is fully mixed and transferred into a machine for drop where add extract, styrax and borneol. The mixture is stirred until homogenization, and then heated to melting with the use of the water bath when the temperature is e 80°C. The melted mixture to drip at a temperature of 65°C in a cooling medium (liquid paraffin)having a temperature of 0°C, with a speed of 35 drops per minute. After giving drops form liquid paraffin on the surface of tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve in an average of 2.68 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 36

The essential oil of Artemisia subdigitata Mattf., obtained by the method of evaporative distillation with water, 18 g, xylitol 40 g, alginic acid 13 year

Xylitol and alginic acid are fully mixed and transferred into a machine for drop where add the essential oil of Artemisia subdigitata Mattf. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at a temperature of 80°C. the Melted mixture to drip at a temperature of 65°C in a cooling medium (liquid paraffin)having a temperature of 4°C, with a speed of 35 drops per minute. After pridani the drops form a liquid wax from the surface of the tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve in an average of 3.16 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 37

12 g of essential oil Rododendron Lutescens Franch., obtained by the method of evaporative distillation with water, citric acid 35 g, Indian gum 10 g of polyoxyethylene the monostearate 10,

Citric acid, Indian gum and polyoxyethylene the monostearate fully mixed and transferred into a machine for drop where add essential oil Rododendron Lutescens Franch. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at a temperature of 80°C. the Melted mixture to drip at a temperature of 65°C in a cooling medium (liquid paraffin)having a temperature of 0°C, with a speed of 35 drops per minute. After giving drops form liquid paraffin on the surface of tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of drops have sferica what kind of shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve in an average of 3.75 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 38

The extract of Radix Sophorae Tonkinensis, Cortex Phellodendri, Radix Trichosanthis, Radix Aristolochiae, Radix Angelicae Dahuricae and Herba Asari was obtained by the method of preparation of tablets in the form of drops of aligning (yatongning), described in the National Assembly Specifications Preparation of Proprietary Traditional Chinese Medicine, part of the Internal medicine and Dentistry.

Named extract 12 g, lactitol 35 g, dextrin 10,

Lactitol and dextrin fully mixed and transferred into a machine for drop where add extract, camphor and natural borneol. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at a temperature of 90°C. the Melted mixture to drip at a temperature of 80°C in the cooling fluid (methanesiliconic oil)having a temperature of 8°C, with a speed of 35 drops per minute. After giving drops form methanesiliconic oil from the surface of the tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The result of the show the resulting tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve in an average of 3.10 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 39

The extract of Folium Ginkgo, Radix Salviae Miltiorrizae, Gynostemma pentaphyllum was obtained by the method of preparation of tablets in the form of drops windycity (yindanxintai), described in the National Assembly Specifications Preparation of Proprietary Traditional Chinese Medicine, part of the Internal medicine and Heart.

Named extract 13 g, alginic alcohol 40 g, hypromellose 15 g, xanthan gum 5,

Alginic alcohol, hydroxymethylcellulose and xanthan gum fully mixed and transferred into a machine for drop where add extract and natural borneol. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at a temperature of 90°C. the Melted mixture to drip at a temperature of 75°C in a cooling medium (liquid paraffin)having a temperature of 10°C, with a speed of 35 drops per minute. After giving drops form liquid paraffin on the surface of tablets in the form of drops absorbers by using absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve average is 4.93 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 40

Chlorphenamine maleate 8 g, isomaltose 45 g, alginic acid 25 g

Isomaltose and alginic acid are fully mixed and transferred into a machine to drop, which add chlorphenamine maleate. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at a temperature of 90°C. the Melted mixture to drip at a temperature of 82°C in a cooling medium (liquid paraffin)having a temperature of 10°C, with a speed of 35 drops per minute. After giving drops form liquid paraffin on the surface of tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the way the Chinese Pharmacopea the (2000) show that tablet in the form of drops completely and easily pass through a wire sieve on average for 5,14 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 41

Befindet 4 g, isomaltitol 30 g, xanthan gum 3 g, poloxamer 6,

Isomaltitol, xanthan gum, poloxamer fully mixed and transferred into a machine to drop befindet dissolved in a suitable amount of 95% ethanol and added to the above mixture. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at 95°C. the Melted mixture to drip at a temperature of 90°C in a cooling medium (liquid paraffin)having a temperature of 5°C, with a speed of 35 drops per minute. After giving drops form liquid paraffin on the surface of tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve on average for 5,33 min, which meets the requirements of the Chinese Pharmacopoeia

Example 42

Salvia miltiorrhiza Bunge was extracted with hot water extracted solution was loaded into the column with the resin, was suirable alcohol and the eluate was concentrated to obtain an extract of Salvia miltiorrhiza Bunge.

The extract of Salvia miltiorrhiza Bunge 15 grams of xylitol 35 g, tragakant 15,

Xylitol and tragakant fully mixed and transferred into a machine for drop where add the extract of Salvia miltiorrhiza Bunge. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at a temperature of 90°C. the Melted mixture to drip at a temperature of 75°C in a cooling medium (liquid paraffin)having a temperature of 8°C, with a speed of 35 drops per minute. After giving drops form liquid paraffin on the surface of tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve in an average of 3.65 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 43

Phenobarbital 6 grams of xylitol 30 g lactose 15 is, xanthan gum 5,

Xylitol, lactose, and xanthan gum is fully mixed and transferred into a machine for drop where add phenobarbital. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at a temperature of 90°C. the Melted mixture to drip at a temperature of 85°C in a cooling medium (liquid paraffin)having a temperature of 10°C, with a speed of 35 drops per minute. After giving drops form liquid paraffin on the surface of tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve on average for a 4.53 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 44

The corresponding extract was obtained according to the method of preparation of liquid huoxiangzhengqi (huoxiangzhengqi), described in the Chinese Pharmacopoeia.

Named extract 12 g, lactitol 30 g starch 20 g, Arabian gum 5,

Lactitol, starch and Arabian gum completely paramesh who live and move in the car to drop where to add the extract, essential oil Herba Pogostemonis and Perilla leaf (perylla). The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at a temperature of 80°C. the Melted mixture to drip at a temperature of 65°C in a cooling medium (liquid paraffin)having a temperature of 4°C, with a speed of 35 drops per minute. After giving drops form liquid paraffin on the surface of tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve on average per 3,79 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 45

Griseofulvin 5 g, 20 g fructose, sorbitol, 10 g, sodium alginate 20,

Fructose, sorbitol and sodium alginate fully mixed and transferred into a machine for drop where add griseofulvin. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at a temperature of 89°C. the Melted mixture to drip when temperature is round 82°C in a cooling medium (liquid paraffin), having a temperature of 3°C, with a speed of 35 drops per minute. After giving drops form liquid paraffin on the surface of tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve in an average to 3.58 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 46

Chloramphenicol 6 g, lactitol 30 g, karragenana (carrageen) gum 3 g, dextrin 5,

Lactitol, carragenin (carrageen) gum and dextrin fully mixed and transferred into a machine for drop where add chloramphenicol. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at 95°C. the Melted mixture to drip at a temperature of 90°C in a cooling medium (liquid paraffin)having a temperature of 5°C, with a rate of 40 drops per minute. After giving drops form liquid paraffin on the surface of tablets in the form of drops absorb with absorbent paper and then get the tab is ETCI in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve in an average of 4.13 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 47

Connection norgestrel 6 g, lactitol 26 g, isomaltitol 10 g, tragakant 5,

Lactitol, isomaltitol and tragakant fully mixed and transferred into a machine for drop where add connection norgestrel. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at a temperature of 89°C. the Melted mixture to drip at a temperature of 80°C in a cooling medium (liquid paraffin)having a temperature of 4°C, with a speed of 35 drops per minute. After giving drops form liquid paraffin on the surface of tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the way the Chinese who farmacopea (2000) show that tablet in the form of drops completely and easily pass through a wire sieve on average for 5,67 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 48

Spironolactone 5 g, lactitol 35 g, isomaltitol 25 g starch 8,

Lactitol, isomaltitol and the starch is fully mixed and transferred into a machine for drop spironolactone dissolved in 95% ethanol and added to the above mixture. The mixture is stirred until homogenization, and then heated to the melting temperature using a water bath at a temperature of 85°C. the Melted mixture to drip at a temperature of 80°C in a cooling medium (liquid paraffin)having a temperature of 4°C, with a rate of 40 drops per minute. After giving drops form liquid paraffin on the surface of tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve on average for 4,55 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 49

Radix Ginseng, Radix Ophiopogonis and ructus Schisandrae was mixed with a weight ratio of 1:2:1 and was prepared mixture to obtain an extract.

Named extract 15 g, xylitol 35 g, hypromellose 12 g, starch 6,

Xylitol is added to the extract, fully stirred and heated to the melting temperature using a water bath at 90°C. Then the mixture is transferred into the car to drop. The hypromellose and starch are mixed, heated, stirred to homogenize and transfer into the car to drop. The melted mixture to drip at a temperature of 80°C in the cooling fluid (dimethylsilicone oil)having a temperature of 10°C, with a rate of 40 drops per minute. After giving drops form dimethylsilicone oil from the surface of the tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve on average for 2,98 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 50

Rhizoma Coptidis, Cortex Phellodendri, Fructus Gardeniae and Radix Scutellariae were mixed with the weight ratio of 1.6:1,1:1,1:2,2 and the mixture was extracted with water is, precipitated with ethanol and then concentrated to obtain an extract.

Named extract 12 g, ether of sucrose 30 g of polyoxyethylene the monostearate 12 g, sodium carboxymethylcellulose cross 18,

Ether of sucrose added to the extract, fully stirred and heated to the melting temperature using a water bath at 90°C. of Polyoxyethylene the monostearate melted separately and mixed with the above mixture. Then the mixture is transferred into the car to drop where add sodium carboxymethylcellulose cross. The melted mixture to drip at a temperature of 85°C in the cooling fluid (dimethylsilicone oil)having a temperature of 15°C, with a rate of 30 drops per minute. After giving drops form dimethylsilicone oil from the surface of the tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve on average for 3,76 min, which meets the requirements of the Chinese f is makopi.

Example 51

Extract of leeches (Whitmania pigra Whitman) 20 g of the ether of sucrose 40 g of polyoxyethylene the monostearate 20,

Ether of sucrose added to the extract, fully stirred and heated to the melting temperature using a water bath at 85°C. of Polyoxyethylene the monostearate melted separately and mixed with the above mixture. Then the mixture is transferred into the car to drop. The melted mixture to drip at a temperature of 80°C in the cooling fluid (dimethylsilicone oil)having a temperature of 18°C, with a speed of 35 drops per minute. After giving drops form dimethylsilicone oil from the surface of the tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve in an average of 4.10 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 52

Radix Bupleuri were extracted with hot water, precipitated with ethanol and then concentrated to obtain an extract.

Named extract 20 g, sugar ester is PS 20 g glycerol monostearate 10,

Ether of sucrose added to the extract, fully stirred and heated to the melting temperature using a water bath at a temperature of 85°C. Glycerol monostearate is melted and mixed with the above mixture. Then the mixture is transferred into the car to drop. The melted mixture to drip at a temperature of 75°C in the cooling fluid (dimethylsilicone oil)having a temperature of 24°C, with a speed of 35 drops per minute. After giving drops form dimethylsilicone oil from the surface of the tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve on average 3.25 per min, which meets the requirements of the Chinese Pharmacopoeia.

Example 53

Essential oil of Radix Bupleuri received by way supercritical extraction, the residue was extracted to obtain saikosaponin as effective fraction and then got an extract.

Named extract 20 g of the ether of sucrose 20 g glycerine m is netearth 14 year

Ether of sucrose added to the extract, fully stirred and heated to the melting temperature using a water bath at a temperature of 85°C. Glycerol monostearate is melted and mixed with the above mixture. Then the mixture is transferred into the car to drop. The melted mixture to drip at a temperature of 75°C in the cooling fluid (dimethylsilicone oil)having a temperature of 28°C, with a speed of 35 drops per minute. After giving drops form dimethylsilicone oil from the surface of the tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve on average 3.25 per min, which meets the requirements of the Chinese Pharmacopoeia.

Example 54

Oil of Blumea poplar (L.) DC 14 grams borneol 1 g, ether of sucrose 40 g of polyoxyethylene the monostearate 21,

The sucrose esters and borneol add in the oil Blumea poplar (L.) DC, fully stirred and heated to the melting temperature using a water bath at a temperature of 85°C. Polyoxide the Jena monostearate melted separately and mixed with the above mixture. Then the mixture is transferred into the car to drop. The melted mixture to drip at a temperature of 80°C in the cooling fluid (dimethylsilicone oil)having a temperature of 26°C, with a speed of 35 drops per minute. After giving drops form dimethylsilicone oil from the surface of the tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve in an average of 3.43 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 55

The extract of Radix Salviae Miltiorrhizae and Radix Notoginseng (Chinese patent number CN 1348815 A) 12 g, borneol 1.2 g, sucrose esters of 28 g of polyoxyethylene the monostearate 14 year

The sucrose esters and borneol added to the extract, fully stirred and heated to the melting temperature using a water bath at 85°C. of Polyoxyethylene the monostearate melted separately and mixed with the above mixture. Then the mixture is transferred into the car to drop. The melted mixture to drip at a temperature of 64°C in holidayshow environment (dimethylsilicone oil), having a temperature of 30°C, with a rate of 40 drops per minute. After giving drops form dimethylsilicone oil from the surface of the tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve on average for 3,63 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 56

The extract of Radix Puerariae (the content of Pueraria flavones more than 80%) 15 g, ether of sucrose 30 g of polyoxyethylene the monostearate 9 g, sodium carboxymethylcellulose cross 15 year

Ether of sucrose added to the extract, fully stirred and heated to the melting temperature using a water bath at 90°C. of Polyoxyethylene the monostearate melted separately and mixed with the above mixture. Then the mixture is transferred into the car to drop where add sodium carboxymethylcellulose cross. The melted mixture to drip at a temperature of 85°C in the cooling fluid (dimethylsilicone oil), have th temperature of 23°C, with a speed of 40 drops per minute. After giving drops form dimethylsilicone oil from the surface of the tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve in an average of 3.64 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 57

The extract of Radix Puerariae (the content of Pueraria flavones more than 40% and the content of puerarin more than 28%) 12 g, ether of sucrose 30 g of polyoxyethylene the monostearate 6 g, sodium carboxymethylcellulose cross 18,

Ether of sucrose added to the extract, fully stirred and heated to the melting temperature using a water bath at 90°C. of Polyoxyethylene the monostearate melted separately and mixed with the above mixture. Then the mixture is transferred into the car to drop where add sodium carboxymethylcellulose cross. The melted mixture to drip at a temperature of 85°C in the cooling fluid (dimethylsilicone oil, having a temperature of 19°C, with a speed of 35 drops per minute. After giving drops form dimethylsilicone oil from the surface of the tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve in an average of 3.15 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 58

Oleum Rhododendri Daurici 12 g, borneol 1.2 g, sucrose esters of 28 g of polyoxyethylene the monostearate 25,2,

The sucrose esters and borneol added to Oleum Rhododendri Daurici, fully stirred and heated to the melting temperature using a water bath at 85°C. of Polyoxyethylene the monostearate melted separately and mixed with the above mixture. Then the mixture is transferred into the car to drop. The melted mixture to drip at a temperature of 70°C in the cooling fluid (dimethylsilicone oil)having a temperature of 25°C, with a speed of 35 drops per minute. After giving drops form dimethylsilicone oil from the surface of the tablets in the form of Capel who absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve on average for 3,63 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 59

Oleum Viticis Maple 12 g, sucrose esters 35 g of polyoxyethylene the monostearate 12 year

Ether of sucrose added to Oleum Viticis Maple, fully stirred and heated to the melting temperature using a water bath at a temperature of 80°C. of Polyoxyethylene the monostearate melted separately and mixed with the above mixture. Then the mixture is transferred into the car to drop. The melted mixture to drip at a temperature of 65°C in the cooling fluid (dimethylsilicone oil)having a temperature of 22°C, with a speed of 35 drops per minute. After giving drops form dimethylsilicone oil from the surface of the tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determining the time and decay according to the Chinese Pharmacopoeia (2000) show that tablet in the form of drops completely and easily pass through a wire sieve on average for 3,55 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 60

The extract of Radix Salviae Miltiorrhizae and Radix Notoginseng (Chinese patent number CN 1348815 A) 22 g, borneol 1.5 g, ether of sucrose 40 g of polyoxyethylene the monostearate 15,

The sucrose esters and borneol added to the extract, fully stirred and heated to the melting temperature using a water bath at 85°C. of Polyoxyethylene the monostearate melted separately and mixed with the above mixture. Then the mixture is transferred into the car to drop. The melted mixture to drip at a temperature of 64°C in the cooling fluid (dimethylsilicone oil)having a temperature of 18°C, with a rate of 40 drops per minute. After giving drops form dimethylsilicone oil from the surface of the tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve in an average of 4.25 is in, that meets the requirements of Chinese Pharmacopoeia.

Example 61

Extracts of Flos Lonicerae, Radix Scutellariae, Fructus Forsythiae with weight ratio of 1:1:2.

These extracts 20 g sucrose esters 35 g of polyoxyethylene the monostearate 15,

Ether of sucrose added to the extract, fully stirred and heated to the melting temperature using a water bath at 95°C. of Polyoxyethylene the monostearate melted separately and mixed with the above mixture. Then the mixture is transferred into the car to drop. The melted mixture to drip at a temperature of 64°C in the cooling fluid (dimethylsilicone oil)having a temperature of 10°C, with a speed of 35 drops per minute. After giving drops form dimethylsilicone oil from the surface of the tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve on average for 3,68 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 62

Starlily ether 22 g, ether is aharony 30 g, of polyoxyethylene the monostearate 20 g, sodium carboxymethylcellulose cross 2 g of silicon dioxide (food grade) 2,

Ether of sucrose added to stimulirovano ether, fully stirred and heated to the melting temperature using a water bath at 85°C. of Polyoxyethylene the monostearate melted separately and mixed with the above mixture. Then the mixture is transferred into the car to drop where add sodium carboxymethylcellulose cross and silicon dioxide (food category).

The melted mixture to drip at a temperature of 75°C in the cooling fluid (dimethylsilicone oil)having a temperature of 30°C, with a speed of 35 drops per minute. After giving drops form dimethylsilicone oil from the surface of the tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve in an average of 3.10 min, which meets the requirements of the Chinese Pharmacopoeia.

Note the R 63

Essential oil of Rhizoma Chuanxiong received by way supercritical extraction, the residue was extracted with ethanol concentration was low and concentrated to obtain an extract.

Called extract, 22 g, ether of sucrose 30 g of polyoxyethylene the monostearate 22g, sodium carboxymethylcellulose cross 4 g of silicon dioxide (food grade) 4,

Ether of sucrose added to the extract, fully stirred and heated to the melting temperature using a water bath at 85°C. of Polyoxyethylene the monostearate melted separately and mixed with the above mixture. Then the mixture is transferred into the car to drop where add sodium carboxymethylcellulose cross and silicon dioxide (food category). The melted mixture to drip at a temperature of 65°C in the cooling fluid (dimethylsilicone oil)having a temperature of 20°C, with a speed of 35 drops per minute. After giving drops form dimethylsilicone oil from the surface of the tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determining the time of the collapse of ways according to the Chinese Pharmacopoeia (2000) show that tablet in the form of drops completely and easily pass through a wire sieve on average for 3,22 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 64

Extract of Erigeron brevsicapus (Vant) Hand-Mazz, Folium Ginkgo, Radix Salviae Miltiorrhizae and natural borneol was prepared according to the method of preparation of tablets in the form of drops wendsankma (yinzhanxinmai) (National Assembly Specifications Preparation of Proprietary Traditional Chinese Medicine, part of the Internal medicine and Heart).

Called extract, 22 g, ether of sucrose 30 g of polyoxyethylene the monostearate 14 g, sodium carboxymethylcellulose cross 0.2 g of silicon dioxide (food category) 0,2,

Ether of sucrose added to the extract, fully stirred and heated to the melting temperature using a water bath at 90°C. of Polyoxyethylene the monostearate melted separately and mixed with the above mixture. Then the mixture is transferred into the car to drop where add sodium carboxymethylcellulose cross and silicon dioxide (food category). The melted mixture to drip at a temperature of 75°C in the cooling fluid (dimethylsilicone oil)having a temperature of 21°C, with a speed of 35 drops per minute. After giving drops form dimethylsilicone oil from the surface of the tablets in the form of drops absorb through absorb the dominant paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve in an average of 4.16 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 65

Extract of Rhizoma Chuanxiong ethyl ester 33 g; extract of Radix Angelicae Sinensis ethyl ester 31 g; ether of sucrose 30 g of polyoxyethylene the monostearate 27 g, sodium carboxymethylcellulose cross 24,

Ether of sucrose added to the extract, fully stirred and heated to the melting temperature using a water bath at 85°C. of Polyoxyethylene the monostearate melted separately and mixed with the above mixture. Then the mixture is transferred into the car to drop where add sodium carboxymethylcellulose cross. The melted mixture to drip at a temperature of 70°C in the cooling fluid (dimethylsilicone oil)having a temperature of 10°C, with a speed of 35 drops per minute. After giving drops form dimethylsilicone oil from the surface of the tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops by drying at nor the coy temperature. The results show that the obtained tablets in the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve on average for at 3.35 min, which meets the requirements of the Chinese Pharmacopoeia.

Example 66

Sonqi tofal in saponins std. 12 g of the ether of sucrose 30 g of polyoxyethylene the monostearate 5 g, sodium carboxymethylcellulose cross 21,

Ether of sucrose added to the extract, fully stirred and heated to the melting temperature using a water bath at 90°C. of Polyoxyethylene the monostearate melted separately and mixed with the above mixture. Then the mixture is transferred into the car to drop where add sodium carboxymethylcellulose cross. The melted mixture to drip at a temperature of 85°C in the cooling fluid (dimethylsilicone oil)having a temperature of 10°C, with a speed of 35 drops per minute. After giving drops form dimethylsilicone oil from the surface of the tablets in the form of drops absorb with absorbent paper and then get a tablet in the form of drops drying at low temperature. The results show that the obtained tablet is the form of droplets have a spherical shape with the same size, uniform color and no gluing. The results of determination of the disintegration time according to the Chinese Pharmacopoeia (2000) show that the tablets in the form of drops completely and easily pass through a wire sieve on average for the 4.65 min, which meets the requirements of the Chinese Pharmacopoeia.

With the aim of better understanding the present invention are further explained the advantages of the present invention on the example of some experiments, such as determining time raspadaemosti, deviations of weight, hardness, viscosity tablets in the form of drops, prepared on the basis of binding of auxiliary substances from the Sample 10.

Experimental example 1

Comparative experimental example of defining a time raspadaemosti and variance weight

Comparing tablets in the form of drops, prepared on the basis of binding of auxiliary substances of the present invention, with tablets in the form of drops, prepared on the basis of polyethylene glycol, respectively, during raspadaemosti was measured to determine whether the first show satisfactory release of the active substance, and also measured the deviation of the weight and other indicators to determine the maturity of the production process and the possibility to adapt it to production scale.

1. Samples:

tablets in the Orme drops, made from extract of Chinese medicines, disclosed in Chinese patent no : CN 1348815 A as an active ingredient and a new auxiliary binder substance of the present invention as a binder excipient (hereinafter designated as "new");

tablets in the form of drops, made from extract of Chinese medicines, disclosed in Chinese patent no : CN 1348815 A as the active ingredient and polyethylene glycol as a binder excipient (hereinafter designated as "known").

2. Method and results

Limit raspadaemosti was measured by the method corresponding to the Chinese Pharmacopoeia; variation in weight was measured by a method corresponding to the Chinese Pharmacopoeia. The results are shown in table 1.

Table 1
Comparison of limit raspadaemosti and variance weight 3 series of tablets in the form of drops, prepared on the basis of a new binder excipient (labeled "new") and polyethylene glycol as the main excipient (marked as "known")
Criterion0 month 1st month2nd month3rd month6-ILSAC12 months18th month
Results
1-I seriesDeviation weight (±15%)up to ±10%up to ±10%up to ±10%up to ±10%up to ±10%up to ±10%up to ±10%
Time (new) decay (known)2'05"2'09"2'16"2'15"2'16"2'20"2'23"
5'11"5 b"5'15"5'19"5'26"5'16"5'35"
2nd seriesDeviation weight(±15%)up to ±10%up to ±10%up to ±10%up to ±10% up to ±10%up to ±10%up to ±10%
Time (new) decay (known)1'57"1'59"1'56"2'04"2'09"2'10"2'08"
5'14"5'18"5'21"5'19"5'26"5'34"5'32"
3 seriesDeviation weight (±15%)up to ±10%up to ±10%up to ±10%up to ±10%up to ±10%up to ±10%up to ±10%
Time (new) decay (known)2'12"2'09"2'15"2'13"2'17"2'20"2'25"
5'10"5'17" 5'21"5'23"5'26"5'30"5'37"

Experimental data showed that the limit raspadaemosti for tablets in the form of drops, prepared on the basis of a new binder excipient is less than that for tablets in the form of drops, prepared on the basis of polyethylene glycol as the main excipient, and the deviation of the weight for new and well-known tablets in the form of drops are within the scope defined in the Chinese Pharmacopoeia. Experimental data also showed that the speed of disintegration of tablets in the form of drops, prepared on the basis of a new binder excipient, higher and better contributes to the onset of effect of the active ingredient as quickly as possible. Variation in weight of new and known tablets in the form of drops is within the scope defined in the Chinese Pharmacopoeia, the differences between them are not statistically significant. So called binder excipient can replace existing chemically synthesized excipients in scale industrial applications.

Experimental example 2

Comparative experimental example of the determination of hardness and viscosity of tablets in the form of drops, preparation, is the R-based binder auxiliary substances according to the present invention and polyethyleneglycol as the main excipient.

1. Examples:

tablets in the form of drops (new) was obtained with the extracts of Chinese medicines, disclosed in Chinese patent no : CN 1348815 And, as the active ingredient and on the basis of the new link excipients according to the present invention as a binder of auxiliary substances (hereinafter referred to as "new");

tablets in the form of drops (known) was obtained with the extracts of Chinese medicines, disclosed in Chinese patent no : CN 1348815 A, as the active ingredient and on the basis of polyethylene glycol as a binder excipient (hereinafter referred to as "known").

2. Method and results:

Was taken for analysis 3 series of tablets in the form of drops, respectively, were placed in a porcelain bottle and tightly corked tubes; capped bottles were placed in a desiccator with a saturated solution of sodium chloride (humidity 75%) at the bottom and then the desiccator was placed in a dry room at a constant temperature of 40°C. Samples were taken at regular intervals of time to determine the hardness and viscosity of tablets in the form of drops. The results are shown in table 2.

Table 2
Comparison of the characteristics of 3 series of tablets in the form of a cap is l, prepared on the basis of new link excipients (new) and polyethyleneglycol as a binder excipient (known)
Criterion0 month1st month2nd month3rd month6th month12 months18th month
Results
1-I seriesViscosity*(therm.)*(therm.)*(therm.)*(therm.)**(therm.)**(therm.)*(therm.)
*(new)*(new)*(new)*(new)*(new)**(new)*(new)
HardnessAnd(therm.)And(therm.) And(therm.)And(therm.)In(therm.)With(known.)With(known.)
A(new)A(new)A(new)A(new)A(new)A(new)With(new)
2nd seriesViscosity*(therm.)*(therm.)*(therm.)*(therm.)*(therm.)**(therm.)**(therm.)
*(new)*(new)*(new)*(new)*(new)*(new)**(new)
HardnessAnd(therm.)And(therm.)And(therm.)And(therm.)In(therm.) With(known.)With(known.)
A(new)A(new)A(new)A(new)A(new)A(new)With(new)
3 seriesViscosity*(therm.)*(therm.)*(therm.)*(therm.)**(therm.)**(therm.)***(therm.)
*(new)*(new)*(new)*(new)*(new)*(new)**(new)
HardnessAnd(therm.)And(therm.)And(therm.)And(therm.)And(therm.)With(known.)With(known.)
A(new) A(new)A(new)A(new)A(new)A(new)With(new)
Note:* = not sticky; ** = slightly sticky; *** = sticky;
A = solid; = hardness below normal;
C = hardness is much lower than normal.

Experimental data showed that in comparison with tablets in the form of drops, prepared on the basis of polyethylene glycol, variations in the hardness of the tablets in the form of drops, prepared on the basis of a new binder auxiliary substances are similar or slightly larger. Experimental data also showed that the differences in hardness and viscosity of new and known tablets in the form of drops are similar. So called binder excipient can replace existing chemically synthesized excipients in the scale of industrial production.

Industrial applicability

In addition to the traditional advantages of tablets in the form of drops, such as ease of manufacture of the population, stable quality, the introduction of liquid active ingredient in a solid dosage form, the traditional route of administration, as well as high efficacy and rapid onset of effect, the biggest advantage of tablets in the form of drops obtained according to the present invention, consists in the following: a binder excipient used in the present invention, derived from plants. Connecting auxiliary substances derived from natural plants, not only are pharmaceutically acceptable, and widely used in the food industry as additives, as mentioned binder excipient is not only absolutely safe without any toxic and side effects, but are also very cheap and affordable, it has a great value for the application and promotion that creates a solid Foundation for the internationalization of these tablets in the form of drops.

Meanwhile, the hardness and the viscosity of the tablets in the form of drops, made on the basis of a new binder excipient of the present invention, similar to the indicators of tablets in the form of drops, prepared on the basis of polyethylene glycol as a binder excipient; this shows that the natural binder excipient can replace existing chemical C is testirovanie excipients in the scale of industrial production.

1. The tablet is in the form of droplets, characterized in that it contains a pharmaceutically active ingredient and at least one pharmaceutically acceptable binding of auxiliary substances selected from the group consisting of a monosaccharide, oligosaccharide, polysaccharide, ether, sugar, sugar alcohol structure, alpha-hydroxy acid, a derivative of the higher fatty acids, higher aliphatic alcohol, polyol, urea, and derived poly(ethylene oxide).

2. The tablet is in the form of a droplet according to claim 1, characterized in that the pharmaceutically active ingredient is an extract of the crude drug.

3. The tablet is in the form of a droplet according to claim 1, characterized in that the pharmaceutically active ingredient is a chemically synthesized drug, antibiotic drug or biochemical means.

4. The tablet is in the form of a droplet according to claims 1 to 3, characterized in that the named as a binder excipient monosaccharide is a D-ribose, fructose, glucose, xylose; named as a binder excipient oligosaccharide represents trehalose, raffinose, maltose; named as a binder excipient polysaccharide is geloso; named as a binder auxiliary materials is inogo substances the sugar ester is a sucrose esters, γ-lactone D-ribnovo acid; named as a binder excipients sugar alcohol structure is erythritol, sorbitol, xylitol, arabitol, isomaltitol, lactitol; named as a binder excipient alpha hydroxycitrate represents malic acid, citric acid; named as a binder excipient derivative of the higher fatty acid is a sodium stearate, glycerol stearate, glycerol palmitate, shellac; named as a binder excipient aliphatic alcohol is cetyl alcohol, stearyl alcohol; named as a binder excipient derived poly(ethylene oxide) is a of polyoxyethylene the monostearate, polyoxyethyleneglycol ether; and the above-mentioned compounds containing crystal water.

5. The tablet is in the form of a droplet according to claim 4, characterized in that the binder excipient is at least one of the auxiliary natural substances of vegetable origin selected from the group consisting of the following: sorbitol, xylitol, lactitol, maltose, sucrose esters, as well as the above-mentioned compounds containing crystal water.

6. The tablet is in the form of drops at p., characterized in that the above-mentioned, the tablet is in the form of droplets further comprises at least one plasticizer selected from the group consisting of the following: starch and its derivatives, cellulose and its derivatives, Arabian gum, dextran, chitin, sesbania (sesbania) gum, karragenana (carrageen) gum, Indian gum, Danish agar, tragakant, carrageenan, tamarind gum, pectin, xanthan gum, alginic acid and its salt, dextrin, cyclodextrin, agar, lactose, polyvinylpyrrolidone, polyvinylpyrrolidone cross, carbomer, polyvinyl alcohol resin acrylic acid, poloxamer, silicon dioxide, gluten, glycerol monostearate, polyoxyethylene the monostearate.

7. The tablet is in the form of a droplet according to claim 6, characterized in that the plasticizing component is one or more substances selected from the group which consists of the following: pregelatinized starch, carboximetilkrahmal, methylcellulose, sodium carboxymethyl cellulose, hypromellose, Arabian gum, alginic acid, dextrin, cyclodextrin, agar, lactose, glycerol monostearate, polyoxyethylene the monostearate, sodium carboxymethyl cellulose cross, silicon dioxide.

8. The tablet is in the form of a droplet according to claim 6, characterized in that the named St. is based excipient contains lactitol and starch.

9. The tablet is in the form of a droplet according to claim 7, characterized in that the binder excipient contains xylitol and Arabian gum.

10. The tablet is in the form of a droplet according to claim 7, characterized in that the binder excipient contains sucrose esters and glycerol monostearate or polyoxyethylene the monostearate.

11. The tablet is in the form of a droplet according to claim 7, characterized in that the binder excipient contains sucrose esters, polyoxyethylene the monostearate and sodium carboxymethylcellulose cross.

12. The tablet is in the form of a droplet according to claim 7, characterized in that the binder excipient contains sucrose esters, polyoxyethylene the monostearate, sodium carboxymethylcellulose cross and silicon dioxide.

13. The tablet is in the form of a droplet according to claim 1, characterized in that the weight ratio of the binder excipients and pharmaceutically active ingredient is in the range of 1:0.1 to~1:1.

14. The tablet is in the form of a droplet according to claim 1, characterized in that the weight ratio of the binder excipients and pharmaceutically active ingredient is in the range 1:0,1~1:0,6.

15. Binder and excipients for tablets in the form of droplets, characterized in that it contains xylitol and starch in a weight ratio of 1:0,2~1:0,3.

16. Swazoo is its excipients for tablets in the form of drops, characterized in that it contains lactitol and starch in a weight Botosani 1:0,2~1:0,3.

17. Binder and excipients for tablets in the form of droplets, characterized in that it contains xylitol and Arabian gum in a weight ratio of 1:0,2~1:0,4.

18. Binder and excipients for tablets in the form of droplets, characterized in that it contains the sucrose esters and glycerol monostearate or polyoxyethylene the monostearate in a weight ratio of 1:0.1 to~1:1.

19. Binder and excipients for tablets in the form of droplets, characterized in that it contains the sucrose esters, polyoxyethylene the monostearate and sodium carboxymethyl cellulose with cross connections in a weight ratio of 1:(0,1~1):(0,1~1).

20. Binder and excipients for tablets in the form of droplets, characterized in that it contains ether of sucrose, a plasticizing component, including polyoxyethylene the monostearate, sodium carboxymethyl cellulose cross and silicon dioxide in a weight ratio of 15:(7~15):(0,1~2):(0,1~2).



 

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9 cl, 7 tbl, 26 ex

FIELD: medicine; pharmacology.

SUBSTANCE: invention includes as active substances one or several fibrates and one or several statins or their pharmaceutically comprehensible salt, in carrier chosen from group, consisting of i) admixtures of polyethyleneglycol and poloxamer in the ratio from 2:1 to 3:1 and with the subsequent dispersion on lactose, ii) glyceryl monostearate with the subsequent spraying on lactose or on an admixture of lactose and hydroxypropymethylcellulose; and iii) polyethyleneglycol, with subsequent spraying on Aeroperl. Besides, the invention concerns firm dosed out forms including specified material and way of their obtaining.

EFFECT: possibility to establish suitable biological availability of both active ingredients at peroral insertion.

56 cl, 15 tbl, 15 ex

FIELD: medicine.

SUBSTANCE: agent for superficial mycoses treatment contains antimycotic Ketoconazole; emulsion carrier including emulsifiers, castor oil, water; end additives stabiliser and preserving agent. Agent is aerosol liniment additionally containing antioxidant Dibunolum or butylhydroxytoluene. As emulsifier agent contains emulsifiers of the first and second type that are distilled monoglycerides, emulsion wax, Tvin 80; as stabiliser it contains oxymethylpropylcellulose (OMPC), and preserving agent is mixture of Nipaginum and Nipazole.

EFFECT: provided lasting contact medicinal substance with affected region and its environmental protection; lowered risk of mycosis transfer from infected person to other people and higher sedimentation stability of agent.

3 tbl, 4 ex

FIELD: medicine; pharmacology.

SUBSTANCE: pharmaceutical composition of controlled release, specifically composition of pulse release, includes nucleus containing physiologically active substance, unstable in acidic medium, leavening agent and alkaline additive. Nucleus has release control coating containing water-insoluble polymer, entero-soluble polymer and hydrophobic wax. Amount of hydrophobic wax in coating is 20-35 wt % of release control coating weight. Physiologically active substance, unstable in acidic medium represents compound based on benzimidazole or its pharmaceutically acceptable salt.

EFFECT: invention provides slight delay difference in composition dissolution and dissolution percent with the course of time providing high reliability of dissolution properties.

28 cl, 16 dwg, 23 tbl, 16 ex

FIELD: medicine; rheumatology.

SUBSTANCE: preparation includes 0.1-3.0 mass % of methotrexate within phospholipid nanoparticles. Nanoparticles consist of phospholipids, glycyrrhizic acid or its salt and adjuvants. The total content of phospholipids and glycyrrhizic acid and its salts is 2-80 mass %. Mass ratio of phospholipids and glycyrrhizic acid or its salts is no more 4:1. Invention also concerns method of rheumatic diseases treatment by means of specified preparation.

EFFECT: decrease in preparation by-effects and maintenance of its therapeutic potential for rheumatic diseases treatment.

4 cl, 3 dwg, 1 tbl, 1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to chemical-pharmaceutical industry and concerns composition, production method and application of agent based on perfluorcarbon-fat emulsions, used for blood substitute parenteral nutrition. Perfluorcarbon-fat emulsion composition can include one perfluorcarbon only, and mixed two, three or four perfluorcarbons: "ПФД" or "ПФТБА", either "ПФОБ", or "ПФМЦП", in ratio 1:1 to 10:10 and one oil selected of group: either soy, or cottonseed, or corn, olive oil, or cod-liver oil, and besides, can include sodium chloride, proxanole and/or phospholipids (soy or egg) as emulsifier; and in addition can contain either glycerol or sorbitol, or xylitol.

EFFECT: can be used for blood substitute parental nutrition.

96 cl, 13 ex, 1 dwg

FIELD: medicine.

SUBSTANCE: invention refers to methods and compositions for treatment and/or prevention maintenance of infectious condition in liquid-containing organ or organ with natural external aperture. Composition includes antibacterial agent, and also, probably, other active agents, amphipathic oil which is soluble in water and insoluble in ethanol, microcrystalline wax and pharmaceutically acceptable nonaqueous carrier. The method of treatment is realised by introduction of a pharmaceutical composition in body through natural external aperture.

EFFECT: regarding composition, invention provides stability of the active agent against oxidising decomposition, low interfacial tension of composition, easy solubility in liquids, and short time of excretion; invention provides effective treatment and reduction of by-effects and toxicity.

61 cl, 12 ex

FIELD: medicine; pharmacology.

SUBSTANCE: proposed suppository along with consistent base (lipophilic, hydrophilic or diphilic) and stabiliser selected from chlorhexidine bigluconate, nypagine and sodium carboxymethyl cellulose as natural endogenous interferon inductor, is supplied with sodium salt complex of alpha-helical and double-helical RNA from killer yeast Saccharomyces cerevisiae. Quantitative amount of specified ingredients per suppository of mass 1.0 g is: sodium salt complex of alpha-helical and double-helical RNA from killer yeast Saccharomyces cerevisiae - 50-150 mcg; stabiliser - 10-30 mcg; additives - others.

EFFECT: extended range of therapeutic antiviral agents and reduced toxicity with maintained efficiency.

6 cl, 4 ex, 3 tbl

FIELD: veterinary.

SUBSTANCE: invention is used for inflammatory organs containing liquid and natural external opening, for example diary animal udder or hearing apparatus. Method includes introduction of pharmaceutical composition containing effective amount of antiphlogistic agent. In addition, the above composition contains (a) amphiphile oil, which is water-soluble and ethanol insoluble, (b) microcristalline paraffine and (c) nonaqueous component which is pharmaceutically suitable.

EFFECT: easily dissolved in liquid contained in organ.

15 cl, 7 ex

FIELD: medicine.

SUBSTANCE: pharmaceutical composition is intended for cancer treatment. As active ingredient composition contains suberoylanilide-hydroxamic acid (SAHA) or its pharmaceutically acceptable salt or hydrate. Invention also relates to method of obtaining crystalline active ingredient SAHA.

EFFECT: definite profile of SAHA particles distribution according to their size, which in its turn results in improved profile of solubility in vitro and optimal SAHA bioavailability.

27 cl, 16 dwg, 22 tbl, 17 ex

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