Improved compositions and improvements associated therewith

FIELD: medicine, pharmaceutical.

SUBSTANCE: invention relates to solid composition for treatment of reflux esophagitis, gastritis, or ulcers, method for production thereof and uses in therapy. Claimed composition contains alginate, bicarbonate and/or carbonate, and poly(C1-C5-alkylene glycol) hawing molecular mass of at least 6000 in amount of 1-50 %.

EFFECT: composition of decreased foam-forming properties and improved organoleptic characteristics.

12 cl, 18 ex

 

The present invention relates to pharmaceutical compositions and, in particular, to compositions for the treatment of reflux oesophagitis, gastritis, dyspepsia or peptic ulcers or for use as compositions with a slow release or targeted delivery.

Reflux esophagitis occurs when small amounts of gastric juice, food, and/or bile acids fall in the lower part of the esophagus and cause its inflammation accompanied by pain, which manifests itself in the form of heartburn.

One approach to solving the problems associated with reflux esophagitis, is the introduction of the drug, which upon contact with gastric acid to form a saturated carbon dioxide gel foam or mass that floats on the surface of gastric contents. When the reverse current, the mass falls into the esophagus before the contents of the stomach and protects the mucosa from further irritation. Known compositions of this type include a liquid composition containing sodium alginate, sodium bicarbonate or potassium, and calcium carbonate. Such compositions are sold under the trademarks GAVISCON and GAVISCON ADVANCE, they are described in GB-A-1524740 and WO 95/11668.

Other such compositions are solid compositions, for example compositions in the form of powders or tablets, which are also sold under the trade the OI brand GAVISCON. Such compositions contain alginic acid, sodium bicarbonate and calcium carbonate. Alginic acid and bicarbonate and carbonate react in the aqueous environment of the oral cavity with the formation of alginate foam, which is then eaten. In the acidic environment of the stomach alginate again becomes insoluble alginic acid, which then forms a mass on the surface of gastric contents.

It is established that solid compositions, which form a foam in the mouth, it is difficult and sometimes unpleasant to swallow. To provide non-lathering solid compositions of the authors of this invention have tried to replace the alginic acid in the alginate. However, they found that such compositions cause a very unpleasant feeling in the mouth. Alginate is sticky and causes the adhesion of the composition to the sky and especially to the teeth.

The authors of this invention have unexpectedly discovered that the feeling in the mouth and stickiness caused by such compositions can be improved by including in the composition an additional component.

Accordingly, the present invention provides a solid composition for oral administration containing:

A. alginate;

b. bicarbonate and/or carbonate and

S.2-C5the polyol or poly(C2-C5allenglish), molecular weight which is at least 6000.

Com is azizia the present invention has a lower foaming, than pills that are sold currently under the trademark GAVISCON, because it contains more of alginate than alginic acid. It causes a good feeling in the mouth and does not stick to the teeth as a composition that does not contain a polyol or polyalkyleneglycol.

The composition of the present invention contains alginate. You can use any alginate, but it is particularly desirable to use a salt of an alkali metal such as sodium alginate or potassium. Preferably use a brand of alginate with low viscosity. Typically, this brand of alginate aqueous solution with a concentration of 10% (weight/volume) has a viscosity, determined on a Brookfield viscometer RVT with rotating axis No. 3 at 20 rpm at 20°With, in the interval from 200 to 1500 MPa·C. for Example, a suitable commercial brand of sodium alginate with low viscosity is Protanal LFR 5/60, supplied by FMC BioPolymer. You can also use the brand of alginate with high viscosity. Typically, this brand of alginate aqueous solution with a concentration of 1% (weight/volume) has a viscosity, determined on a Brookfield viscometer RVT with rotating axis No. 3 at 20 rpm at 20°above 500 MPa·C. for Example, a suitable commercial brand of sodium alginate with high viscosity is Protanal SF200, also supplied by FMC BioPolymer.

The content of the alginate in the compositions of the infusion is his invention typically ranges from 2 to 90 wt.%, preferably from 5 to 50 wt.%, in relation to the total weight of the composition.

Compositions of the present invention also contain bicarbonate and/or carbonate. Examples of bicarbonate are the bicarbonates of alkali metals such as sodium bicarbonate and potassium and bicarbonates of alkaline earth metals. You can use one, two or more different bicarbonate. Examples of carbonates are carbonates of alkali metals, such as carbonates of sodium and potassium, carbonates of alkaline earth metals, such as carbonates of calcium and magnesium. You can also use aluminum carbonate and mixed carbonates of alkali metals, such as nitroglicerina. You can also use one, or two, or several different carbonates. In addition, you can use one or more of bicarbonates with one or more carbonates. Particularly preferred combinations are combinations of sodium bicarbonate and/or potassium, and calcium carbonate.

The carbonate and/or bicarbonate are present in the stomach in such quantities that provide the volume of gas (carbon dioxide), is sufficient for the gel formed in the stomach upon contact of alginate with gastric acid, was kept on the surface. The stiffness and thickness of the layer of carbonate masses depend, for example, from the relative amounts of carbonate and/libtelnet, and from a brand name alginate.

If you only use bicarbonate, his number in the compositions of the present invention typically ranges from 1.5 to 35 wt.%, preferably from 2 to 15 wt.%, most preferably from 3 to 10 wt.%. If only the carbonate, the quantity in the compositions of the present invention typically ranges from 0.2 to 55 wt.%, preferably from 0.5 to 10 wt.%, most preferably from 1 to 4 wt.%.

Preferably, the bicarbonate and carbonate may also be present in the composition together, preferably from 1 to 20 wt.%, for example, in a total amount of from 1 to 40 wt.%, preferably from 1 to 12 wt.%. Bicarbonate and carbonate may be present in the composition in approximately equal numbers. Alternatively, the composition may contain more bicarbonate than carbonate. The mass ratio of bicarbonate to carbonate may range from 1:1 to 2:1.

Compositions of the present invention may contain a2-C5the polyol or poly(C2-C5allenglish). Suitable polyols containing 2, 3, 4 or 5 carbon atoms and 2 or more hydroxyl groups, such as 2, 3, 4, or 5 hydroxyl groups. Examples of suitable compounds are ethylene glycol, propylene glycol, glycerin and eritra.

Poly(C2-C5allenglish) preferably represents polie jingleball or polypropylenglycol. Polyalkyleneglycol can contain any number alkalophilic elements, for example, having a molecular weight of at least 6000. The polyalkylene glycols can be liquid or solid at room temperature (20°). For ease of processing and inclusion in the mixture is preferably used in solid form, especially in the form of a free flowing powder.

The amount of polyol or poly(C2-C5alkalophiles) in the compositions of the present invention typically ranges from 1 to 50 wt.%, preferably from 1 to 15 wt.%, preferably from 1.5 to 10 wt.%, most preferably from 2 to 6 wt.%.

The polyol or poly(C2-C5allenglish) and alginate may, for example, be present in the compositions of the present invention in a weight ratio of from 2:1 to 1:25, preferably from 1:4 to 1:12,5.

Compositions of the present invention may also optionally contain additional components.

For example, compositions of the present invention preferably contain a source of divalent or trivalent metal ions. Such ions strengthen formed in the stomach a lot. Suitable metal ions are calcium ions and aluminium. These ions can be represented as part of the bicarbonate and/or carbonate, but, if desired, they can also contain other anions. For example, suitable what sources of calcium ions are carbonate, lactate, chloride, gluconate, phosphate, hydrogen phosphate, sulfate, tartrate or citrate of calcium and suitable sources of aluminum ions are carbonate, lactate, glycinate or aluminum phosphate, carbonate, hydroxide or malardrottningen, aluminiumtrihydrate or aluminometasilicate. In the case of calcium ions is preferably present in an amount of from 8 to 800 parts, and the aluminum ions are preferably present in an amount of from 2 to 500 parts for 500 mass parts of alginate.

Compositions of the present invention may also contain a preservative to prevent contamination and subsequent deterioration caused by microorganisms. Examples of suitable preservatives are methyl-, ethyl-, propyl - and butylperoxybenzoate and their salts, which are preferably used in combination, for example, methyl and propyl or ethyl and butyl. Compositions of the present invention does not necessarily contain this preservative, but if the preservative is present, it can be used in amounts of, for example, up to 0.5 wt.% in relation to the total weight of the composition.

Compositions of the present invention can also contain one or more coloring agents, sweeteners, flavors, ingredients, providing the desired pH value, and fillers. If the composition of the present invention p is right for use in the form of compositions with delayed release, they also contain at least one active ingredient, suitable for specific delivery in the stomach, such as medicines. Examples of suitable drugs include analgesics (for example, suitsetamine, ibuprofen, naproxen, diclofenac, Ketoprofen, holinsalitsilat, benzydamine, buprenorphine, hydrocortisone, betamethasone); decongestants tools (e.g., pseudoephedrine, phenylephrine, Oxymetazoline, Xylometazoline); a means of suppressing the cough (e.g., dextromethorphan, codeine, valocodin); expectorants (for example, guaifenesin, n-acetylcysteine, Bromhexine); antiseptics (e.g., triclosan, chloroxylenol, amylmetacresol, hexylresorcinol, dichlorobenzoyl alcohol, benzyl alcohol); cardiovascular drugs (e.g., glyceryl trinitrate); local anesthetics (eg, benzocaine, lignocaine); antacids (eg, calcium carbonate, sodium bicarbonate, trisilicate, magnesium hydroxide, magaldrate aluminum); antiulcer means (for example, carbenoxolone, sukralfat, cimetidine, ranitidine, nizatidine, famotidine, omeprazole, pantoprazole); antihistamines (for example, loratadine, terfenadine, diphenhydramine, chlorpheniramine, triprolidine, acrivastine); anti-emetics (e.g., prochlorperazine, sumatriptan); means regulating operation is the ability of the intestine (for example, Diphenoxylate, loperamide, sennoside); antifungal medicines (e.g. clotrimazole); antimicrobial agents and antibiotics (for example, fusafungine, tyrothricin).

Compositions of the present invention can also contain alginic acid, although this is not preferred, as alginic acid can cause in the mouth undesirable foaming.

Compositions of the present invention can be presented in any solid form. For example, they can be represented in the form of tablets, such as a chewable tablet. They may also be in the form of chewing gum, candies such as Fudge or caramel, or in the form of particles or granules, which, for example, are in a free flowing condition or enclosed in a capsule, such as soft or hard gel capsule.

The composition of the present invention can be used in a method of treatment of a human or animal, especially for the treatment of reflux oesophagitis, gastritis, dyspepsia or peptic ulcers or for use as a composition with a slow release or targeted delivery.

The composition of the present invention can be used in the production of drugs for the treatment of reflux oesophagitis, gastritis, dyspepsia or peptic ulcers or for use as a composition with samedl the authorized release or targeted delivery.

The composition of the present invention can be used in a method for the treatment of reflux oesophagitis, gastritis, dyspepsia or peptic ulcers, or for slow release or targeted delivery composition, which comprises oral administration to a subject, who has the need or tendency to such needs, an effective amount of the composition.

The composition is typically administered in an amount corresponding to from 100 to 2000 mg of alginate per dose.

Compositions of the present invention can be obtained by simple mixing of the ingredients. Especially, it is preferable to mix the ingredients in dispersed form and then be pelletized or glomerulopathy particles, using a suitable granulating agent, such as water, With2-C4alcohol, for example ethanol or isopropanol, or a mixture. This method is particularly suitable if you are using solid PEG. You also can pelletize the rest of the ingredients, using PEG as granulating means, if it is in liquid form. You can also use other granulating binders such as povidone, a derivative of cellulose, such as HPMC, starch or paste. Preferably when using starch paste as a granulating solvent use water and povidone about is commonly used with ethanol or isopropanol as solvent. Unexpectedly, the authors of this invention have found that when performing wet granulation is possible to reduce the amount of polyol or polyalkyleneglycol, while maintaining a satisfactory feeling in the mouth. For conventional granulation may require a mass ratio of polyol or polyalkyleneglycol to the alginate approximately 1:1. However, when using the wet granulation method, the mass ratio of polyol or polyalkyleneglycol to the alginate can be reduced to less than 0.25:1, especially less than about 0.15:1, while maintaining a satisfactory feeling in the mouth.

After granulating, you can add one or more components. In particular, the polyol or polyalkyleneglycol can be added after granulation, although this is not preferred, so as to achieve a suitable feeling in the mouth may require an increased amount of this component. It is preferable to avoid the application of excessive polyol or polyalkyleneglycol, since the quantity of this component, which can be taken orally, may be limited to regulating (drug) bodies.

In the preferred method of obtaining the composition of the present invention alginate, sodium carbonate and/or bicarbonate and a polyol or polyalkyleneglycol roleroot together dried and sieved before mixing with any other components. You can also, for example, to pelletize only alginate and polyol or polyalkyleneglycol and then adding the remaining components.

Further, the present invention is described using the following examples.

Example 1

The following disperse components (each of which has a maximum particle size of 1 mm) are mixed in a mixer with large shear forces in a 1 minute:

Sodium alginate LFR 5/60250 g
Sodium bicarbonate133,5 g
Calcium carbonate80 g
PEG 2000030 g

The mixture is then granularit in the granulator, using as a granulating means 75 ml of distilled deionized water.

The granules are dried in a fluidized bed dryer at 40°C for 20 minutes and then grind on the Quadro Comill, using the first sieve 610 μm, and then the sieve 457 microns. After grinding the granulate is mixed with the following ingredients in the mixer with turning low shear effort within 5 minutes:

Mannitol522,75 g
Crosspovidone (dispersing medium) 55 g
Flavor 15.5 g
Flavor 21.1 g
Acesulfame K5.5 g
Aspartame1,65 g

Finally, in a mixer add 15 g of magnesium stearate and stirring is continued for a further 2 minutes.

Then the granules are pressed, receiving tablets, each of which contains 250 or 500 mg of sodium alginate. Tablets possess a homogeneous, slightly viscous when chewing texture, they do not stick to teeth or have no adhesive residue.

Example 2

Tablets of 250 and 500 mg get by the method of example 1, but using the following components:

Sodium alginate LFR5/60250 g
Sodium bicarbonate133,5 g
Calcium carbonate80 g
PEG 2000030 g
Mannitol516,5 g
Crosspovidone55 g
Flavor10 g
Aspartame10 g
Magnesium stearate15 g

Comparative example 1 and examples 3-7

A comparative analysis is performed to illustrate the beneficial effects of polyalkyleneglycol on the sensation in the mouth caused by the comp is the position.

Enjoy the following composition:

Examples
Ingredient(mg)Srvnet34567
Protana LFR 5/60520500500500500500
NaHCO3177170170170170170
Mannitol11789506009501125300
Mg-stearate313030303030
Kollidon 90F104-----
PEG 20000--7003501751000
PEG 3000-350----
Total weight (mg)201020002000200020002000
PEG:alginate-1:1,43 1:0,711:1,431:2,861:0,5
The feeling in the mouthVery sticky + scores teethA satisfactory degree of stickinessNon-sticky or will not clog the teeth. Slightly oily/creamyFirst, drying, slightly grainy. Then creamy. Non-sticky.Creamy, non-sticky.Quickly dissolves. Very pleasant in the mouth, i.e. non-sticky or will not clog the teeth.

Comparative example 2 and example 8

Tablets get below way and then analyze created their feeling in the mouth.

IngredientExample
Comparative 28
mg tabletmg tablet
Sodium alginate LFR 5/60250,00250,00
Sodium bicarbonate133,50133,50
Calcium carbonate80,0080,00
Mannitol607,75432,75
The polyethylene glycol 200000,00175,00
Flavor 15,505,50
Flavor 21,101,10
Sweetener 15,505,50
Sweetener 21,651,65
Magnesium stearate15,0015,00
Weight pills1100 mg1100 mg

Manufacturing technology

Mass produced boot (series) (Batch size produced) 550,

1. Ingredients, except magnesium stearate, are mixed together for 5 minutes using a mixer with turning the turbula T2C..

2. Add magnesium stearate and mix for a further 2 minutes.

3. Pressed into tablets using a tablet press Riva Piccola, stamped FBE 16 mm

Tableting composition of comparative example 2, which does not contain PEG, runs poorly with the separation and destruction.

The organoleptic properties of the resulting tablets analyze in the laboratory:

ExampleThe degree of clogging of the teethThe feeling in the mouthTasteVK is financial feeling after Total
Example 8Very lowDrier, more crumbly. Tablet rapidly disintegratesPleasant, mintNoAcceptable
Cf. example 2Worst of all seriesPleasant, mintNoMalonebailey

For analysis of the ability to form mass and outside of mass four crushed tablets (a total of 1 g of sodium alginate) is mixed with 20 ml of water and pour into a glass with a volume of 250 ml containing 150 ml 0,1M HCl at 37°C. the Ability to form a uniform foaming gel "mass", floating on the surface of the acid, see after 30 minutes.

In both cases, floating on the surface of the mass produced quickly. It extends entirely across the surface of the glass and resistant to rupture. The differences between the two compositions are not observed.

Therefore, the addition to the composition of the PEG has a significant impact on the generated product sensation in the mouth, without affecting the ability to form a mass, bulk reverse current.

Example 9

Get tablets containing the following components:

Sodium alginate LFR5/60 250,00 mg
Sodium bicarbonate133,50 mg
Calcium carbonate80,00 mg
Mannitol516,50 mg
The polyethylene glycol 2000030,00 mg
Crosspovidone55,00 mg
Mint flavor10,00 mg
Sweetener10,00 mg
Magnesium stearate15,00 mg
Weight pills1100 mg

Way

1. Granulating components

1.1. In a food processor Bowl (mixer Magimix 3000, equipped with a large tank) add the sodium alginate LFR5/60, sodium bicarbonate, calcium carbonate and polyethylene glycol 20000.

1.2. Include the combine and mix the powder for 2 minutes.

1.3. Granularit, spraying water until you begin to form a wet mass (approximately 70-110 g of water).

1.4. Dried granules in a fluidized bed dryer (Aeromatic Strea 1) when the temperature of the incoming air 40°C.

1.5. Sift the dried granules through the mill Quadro Comil equipped with a sieve 457 microns.

1.6 Sieved granules through a sieve of 850 μm.

2. Mix for the production of tablets

2.1. The obtained granules and the corresponding amount of the other ingredients, except magnesium stearate, mix with perevoracivala the m for 5 minutes.

2.2. Add magnesium stearate and mix with turning for a further 2 minutes.

3. Manufacturing tablets

3.1 Tabletirujut obtained pellet mixture, using table rotary tablet press Riva Piccola with stamps FBE size 16 mm

It was found that the wet granulation components containing PEG, allows you to use a lower amount of PEG than under a dry granulation of example 8, as this remains an acceptable sensation in the mouth.

Example 10

Tablets are obtained from the following compositions using the method described in example 9.

Sodium alginate LFR5/60500,00 mg
Bicarbonate of potassium, medium100,00 mg
Calcium carbonate100,00 mg
The polyethylene glycol 2000060,00 mg
Mannitol1260,00 mg
Crosspovidone110,00 mg
Mint flavor20,00 mg
Sweetener20,00 mg
Magnesium stearate30,00 mg
Only2200 mg

Get tablets weighing 500 mg, using a tool with a flat beveled edge 22 mm

These tablets give udovletvoritelno sensation in the mouth and masloobraznaya, and their consistency at least is as good as the tablets obtained in example 9.

Example 11

Repeat example 10, using the following composition:

Sodium alginate LFR 5/60250 g
Sodium bicarbonate133,5 g
Calcium carbonate80 g
PEG 2000030 g
Mannitol571,5 g
Mint flavor10 g
Sweetener10 g
Magnesium stearate15 g

Despite the fact that the obtained tablets do not contain crosspovidone, they give a better feeling in the mouth than the tablets of example 10.

Examples 12-17

Tablets are obtained from the following songs:

Ingredient
121314151617
mg tabletmg tabletmg tabletmg tabletmg tabletmg tablet
Sodium alginate LFR5/60250,00250,0025000 250,00250,00250,00
Sodium bicarbonate50,00250,0050,00133,00133,0050,00
Calcium carbonate25,0010,00100,0020,0080,00100,00
The polyethylene glycol 20000175,00175,00175,00175,00--
The polyethylene glycol 3000----175,00175,00
Crosspovidone1,101,101,101,101,101,10
Flavor5,505,505,505,505,505,50
Sweetener1,651,651,651,651,651,65
Magnesium stearate15,0015,0015,0015,0015,0015,00
Mannitolqsqsqsqsqsqs
Weight pills1100 m, the 1100 mg1100 mg1100 mg1100 mg1100 mg

Example 18

Tablets are obtained from the following songs:

Ingredientmg tablet
Sodium alginate500,00
The potassium bicarbonate100,00
Calcium carbonate100,00
The polyethylene glycol 2000060,00
Mannitol1370,00
Flavor20,00
Sweetener20,00
Magnesium stearate30,00
Only2200,00

1. Solid composition suitable for the treatment of reflux oesophagitis, gastritis, dyspepsia or peptic ulcers for oral administration, containing

A. alginate;

Ü. bicarbonate and/or carbonate; and

C. poly(C2-C5allenglish), molecular weight which is

at least 6000, and which is present in the composition in an amount of

1 to 50 wt.%.

2. The composition according to claim 1, where the poly With2-C5allenglish is a polyethylene glycol (PEG).

3. The composition according to claim 1, where the alginate is sodium alginate.

4. Comp the position according to claim 1, where bicarbonate is a bicarbonate.

5. The composition according to claim 1, where the carbonate is a carbonate of calcium.

6. The composition according to claim 1, which is represented in the form of tablets.

7. Composition according to any one of claims 1 to 6 for use in the method of treatment of a human or animal.

8. The use of a composition according to any one of claims 1 to 6 for the treatment of reflux oesophagitis, gastritis, dyspepsia or peptic ulcers.

9 a Method for the treatment of reflux oesophagitis, gastritis, dyspepsia or peptic ulcers, which comprises oral administration to a subject, who has the need or tendency to such needs, an effective amount of a composition according to any one of claims 1 to 6.

10. A method of obtaining a composition according to any one of claims 1 to 6, which involves mixing of alginate, bicarbonate and/or carbonate and poly2-C5alkalophiles.

11. The method according to claim 10, where the components granularit together by the wet granulation.

12. The method according to claim 11, where the mass ratio of polyol or polyalkyleneglycol to the alginate is less than 0.25:1.



 

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2 ex

FIELD: medicine, gastroenterology.

SUBSTANCE: it is necessary to apply omeprasol 20 mg twice daily, furasolidone at 100 mg thrice daily and hydrogen sulfide solution at concentration of 10 mg/l per 150 ml thrice daily. Therapeutic course corresponds to 10 d. Due to additional anti-Helicobacter impact of hydrogen sulfide solution at hydrogen sulfide concentration being 10 mg/l the present innovation provides efficient eradication of Helicobacter pylori without using antibiotics.

EFFECT: higher efficiency of therapy.

3 ex

FIELD: pharmacology, cosmetology, active iodine-containing agents.

SUBSTANCE: claimed composition contains 1,3-diethylbenzimidazolium triiodide as active ingredient, solvent, low molecular medical polyvinyl pyrrolidone as solubilizer and stabilizer for active ingredient, polyethylene glycol, and dimexid and/or glycerol as solvent in specificcomponent ratio.

EFFECT: composition for preventing of skin tissue pathologies caused by various traumatic factors.

4 ex

FIELD: pharmacy.

SUBSTANCE: invention proposes an oral composition for immediate release that comprises solid homogenous and thermodynamically stable solution of difficultly water-soluble solution of biologically active substance, a nonionogenic hydrophilic surface-active agent in liquid state at temperature 15-30°C in the amount 20-70% of the total composition mass, a pharmaceutically acceptable organic polymer or mixture of polymers in liquid state at temperature above 60°C and in solid state at temperature below 30°C in the amount 5-70% of the total composition mass and optionally a loosening agent in the amount 1-10% of the total composition mass. Indicated difficultly water-soluble active substance represents preferably 3-[[[1-[2-(ethoxycarbonyl)-4-phenylbutyl]cyclopentyl]carbonyl]amine]-2,3,4,5-tetrahydro-2-oxo-1H-1-benzazepine-1-acetic acid calcium salt. Invention provides improved bioavailability of active substance as compared with conventional medicinal formulation. The composition can be prepared by usual technology and equipment without large investments.

EFFECT: improved and valuable properties of composition, improved preparing method.

12 cl, 3 tbl, 6 dwg, 4 ex

FIELD: medicine.

SUBSTANCE: means has photosensitizer, amphiphilic transporting additive and amphiphilic water-solution polymer. The amphiphilic transporting additive is block-copolymer of propyleneoxide and ethyleneoxide. The amphiphilic water-solution polymer is selected from sodium carboxymethyl cellulose, polyvinyl alcohol, chitosan sulfate. The means contains Dimegin or Photogem or Photoditazin or Photosense as photosensitizer.

EFFECT: enhanced effectiveness of treatment; reduced preparation immunogenicity and toxicity.

4 cl

FIELD: medicine, pharmaceutical technology, pharmacy.

SUBSTANCE: invention relates to injection moxifloxacin solution containing polysaccharide and accessory substance, and to a method for its preparing. The solution contains lactic or glycolic acid copolymer as accessory substance, and mannitol as polysaccharide in the following ratio of components, weight %: moxifloxacin, 2-3; lactic acid homopolymer or copolymer of lactic and glycolic acids, 23-26; mannitol, 4.0-5.5; polyvinyl alcohol, 0.8-1.3, and water, the balance, to 100%. The claimed method involves dissolving the therapeutically permitted amounts of moxifloxacin in water followed by addition of accessory substances solution. Lactic acid homopolymer solution or copolymer of lactic and glycolic acids in methylene chloride is used as accessory substances solution wherein moxifloxacin aqueous phase is added, and polyvinyl alcohol is added to the prepared emulsion to the concentration 0.8-1.3% and mannitol is added to the concentration 4.0-5.5%. The claimed composition and a method for its preparing provides preparing agent convenient in using and providing high therapeutic effectiveness and allow avoiding crystallization of active substance for prolonged time.

EFFECT: improved preparing method.

3 cl, 2 tbl, 1 ex

FIELD: pharmacy.

SUBSTANCE: invention proposes a pharmaceutical agent comprising a hardly pressed substance, and a filing agent composition consisting of 5-30 wt.-% of copolymer of polyvinylpyrrolidone with vinyl acetate and siliconized microcrystalline cellulose. The used copolymer consists of 60-80 wt.-% of polyvinylpyrrolidone and 20-40 wt.-% of vinyl acetate. Invention provides preparing a pharmaceutical tablet showing the strength index at least 3 kPa at pressing effort 2000-500 pounds being without increasing a tablet size. Prepared hardness is sufficient in order to prevent damage of tablet in its further processing including applying a cover and package.

EFFECT: improved properties of filling agent.

2 cl, 7 dwg

FIELD: organic chemistry, medicine.

SUBSTANCE: invention relates to a complex of polyvinylpyrrolidone and 2,3-bis-(hydroxymethyl)quinoxaline 1,4-di-N-oxide (dioxydinium) of the formula (I) that possesses antibacterial activity with prolonged effect against anaerobic and aerobic infections. Complexes are prepared by interaction of polyvinylpyrrolidone with dioxydinium in the range of weight ratio of reagents = (10:1)-(6:1) (1:0.05-1:0.09 mole) in an aqueous solution at temperature 20-25°C. The structural formula of prepared complexes is confirmed by IK-spectroscopy data. Complexes of polyvinylpyrrolidone with dioxydinium possess antibacterial effect on aerobes and anaerobes and can be used against mixed infections..

EFFECT: valuable medicinal properties of complexes.

3 cl, 1 tbl, 3 ex

FIELD: medicine, pharmacy.

SUBSTANCE: invention relates to a pharmaceutical composition for controlled release that comprises a medicinal agent, polyethylene oxide with molecular mass 2000000 Da or above and a special size-regulating agent for indicated polyethylene oxide and wherein indicated medicinal agent and size-regulating agent are dispersed uniformly in polyethylene oxide. Also, invention relates to a method for preparing indicated pharmaceutical composition for controlled release and a pharmaceutical preparation for controlled release comprising indicated pharmaceutical composition for controlled release. The pharmaceutical composition with controlled release possesses good uniformity of the content and can be prepared using polyethylene oxide powder particles showing properties suitable for making tablets that is prepared by uniform dispersing a size-regulating agent for polyethylene oxide.

EFFECT: improved and valuable pharmaceutical properties of composition.

32 cl, 1 tbl, 16 ex

FIELD: medicine, obstetrics, gynecology.

SUBSTANCE: due to instrumental technique one should pre-detect the volume of uterine cavity and its longest length against the cervix. Moreover, it is necessary to fix a woman's body in position at which the upper edge of uterine cavity bottom is below against the lower edge of uterine cervical opening till the moment of complete filling in uterine cavity with blood. With the help of a catheter one should introduce medicinal preparation heated up to +42- +45° C into uterine cavity through an opening in uterine cervix into area of cavitary bottom at the volume exceeding the half of cavitary volume. Moreover, as the above-mentioned medicinal preparation it is necessary to apply dehydrated silicone gel impregnated with equal volume of 3%-hydrogen peroxide solution. The innovation enables to interrupt postpartum hypotonic uterine hemorrhage efficiently and safely.

EFFECT: higher efficiency.

2 ex

FIELD: medicine.

SUBSTANCE: composition has hydrophilic gel produced from chitosan and hydrophilic poly(N-vinyl lactame) having kinematic viscosity index less than 60. When deposited on cracks, the gel absorbs exudate undergoing no structural transformations.

EFFECT: improved skin compatibility properties.

34 cl

FIELD: medicine, dermatology, pharmacy.

SUBSTANCE: invention relates to a pharmaceutical gel composition for applying on skin. The composition comprises at least one vitamin D or analog of vitamin D, at least one corticosteroid, at least one solvent and an excipient enhancing viscosity. Viscosity value of the composition is in the range from 5 mPa x s to 500 mPa x s. The composition is designated for treatment of psoriasis and associated states in humans. The composition is suitable for applying on skin, shows the improved absorption and stable at 40°C in storage for 3 months.

EFFECT: improved and valuable properties of composition.

22 cl, 2 tbl, 1 ex

FIELD: veterinary science.

SUBSTANCE: agent for treatment of wounds in animals comprises bird muscle stomach cuticle, bentonite, phosphogypsum, lactic acid, methylcellulose and distilled water in the following ratio of components, wt.-%: bird muscle stomach cuticle, 19.0; bentonite, 25.0; phosphogypsum, 10.0; lactic acid, 1.0; methylcellulose, 0.8, and distilled water, 44.2. Agent possesses the high effectiveness in treatment, it doesn't cause complications and has no contraindications.

EFFECT: enhanced effectiveness and valuable veterinary properties of agent.

1 tbl

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