Compound for capsules
SUBSTANCE: invention concerns pharmaceutical technology and medicine and concerns a compound for capsules. An antimicrobial and interferon inducing agent includes a γ-modification of aminobenzenesulphamide as active substance. It also contains talc, calcium stearate and sucrose at a certain parity of components.
EFFECT: invention provides maximum therapeutic concentration of the preparation in blood.
The invention relates to pharmaceutical technology and medicine, and more specifically to a composition for capsules.
When using capsules drug is protected from the external environment, the actions of the gastrointestinal tract excluded the possibility of penetration into the respiratory tract. Capsules are convenient in use, easily ingested. In addition, by adjusting the composition of the capsule's shell, it can extend the action of medicinal substances. In some cases, oral administration of certain drugs using capsules is the most preferred. Such substances include fine "dusty" substance, some of which are exposed to the medium already in the mouth, losing its therapeutic effect. Such substances include, in particular, the γ-modification of paraaminobenzoic.
It is known that the γ-modification of paraaminobenzoic has antimicrobial and interferon-inducing effect (patent RF №2033153).
However, this substance is a highly dispersed substance and belongs to the category of dusty, so use it orally is extremely difficult. In addition, it has a bitter taste, irritating effect on the mucous membrane of the gastrointestinal tract and with the passage of the gastrointestinal tract, starting with ro the new cavity, it is partially metabolized, turning in acetylated form, which does not has an antibacterial effect. Therefore, the number of active (deacetylating) form is reduced, resulting in not ensured maximum therapeutic concentration of drug in the blood.
One of the most convenient dosage forms γ-modification of paraaminobenzoic oral its application can serve capsules.
However, the γ-modification of paraaminobenzoic has a low flowability and bulk mass and, in addition, the powder is strongly electrified. All this requires the use of auxiliary substances for the introduction of this drug in capsules. Such auxiliary substances, as a rule, are substances that are functional are diluents, disintegrating agents, and slip agents, approved for medical use: lactose, saccharose, flour, talc, corn starch or potato, calcium phosphate one-deputizing etc.
The basis of the invention is to create such a composition for capsules, which would be convenient for encapsulation and would have a high bioavailability of the active substance γ-modification of paraaminobenzoic, and would preserve the physico-chemical and technological properties of the each of the selected excipients, providing flowability of the mass composition.
This problem is solved by the fact that features such a composition for capsules containing talc, calcium stearate, sucrose, which according to the invention also includes γ-modification of paraaminobenzoic, in the following ratio, wt.%:
|γ-Modification of paraaminobenzoic||of 9.30-19,95|
Depending on the desired dose of the medicinal substance can be obtained capsule mixture of different sizes of capsules. For this it is necessary to vary the number of components while preserving their chosen correlations between them.
In this song, sucrose, talc and calcium stearate eliminate the effect of the electrification of the γ-modification of paraaminobenzoic. Calcium stearate and talc reduce internal friction between the particles of the composition and external friction between the particles of the composition and surface equipment.
The main characteristic of the bioavailability of oral dosage forms is the rate of dissolution.<> The rate of dissolution of γ-modification of paraaminobenzoic enclosed in capsules of the composition, determine the device "Rotary basket" by well-known methods (the State Pharmacopoeia of the USSR, eleventh edition (release 2), Westergeest, 1991, str). Environment dilution water is purified, the rotation speed of the basket is 80 rpm, volume environment dissolving 250 ml, temperature 37°C. the Content of γ-modification of paraaminobenzoic in solution determined by a spectrophotometric method for the optical density of the solution at a wavelength of 258 nm in a cell with a layer thickness of 10 mm
In the result, it was found that after 30 minutes, there is an almost complete transition of medicinal substances in the water (97,89%). After a 30-minute study is the decrease in optical density of the solution, indicating no accumulation amount of drug. Thus, the proposed structure provides high bioavailability of γ-modification of paraaminobenzoic.
Also determine the bioavailability of γ-modification of paraaminobenzoic and the proposed composition of the "in vivo".
The study of the biological availability of the medicinal substance in the capsule composition of the mixture was carried out in comparison with the substance of this matter on 4 rabbits sa is Zach breed chinchilla weight of 3,350-3,600 kg For 14 hours before the start of the experiment, animals were deprived of food. At the 1st stage of the study, the rabbits injected only γ-modification of paraaminobenzoic. At the 2nd stage after a 3-week break rabbits injected with the proposed structure. Pure substance and the composition is taken at the rate of 100 mg of the active substance (γ-modification of paraaminobenzoic) per 1 kg of body weight of the animal and before the introduction of the substance and the composition is pre-mixed with 10 ml of water to obtain a homogeneous suspension. The introduction is carried out in the esophagus using a syringe and probe. Then after 0.5, 1, 2, 4 and 6 hours after administration in each group determine the concentration of γ-modification of paraaminobenzoic in the blood. Blood samples (1 ml taken from the marginal ear vein of rabbits in a test tube with 15 ml of purified water, mix, and then add 4 ml of 15%trichloroacetic acid, and again thoroughly mixed and filtered through a paper filter.
The concentration of γ-modification of paraaminobenzoic in the blood is performed by the method of Prestige-Gavrilova.
In the result, it was found that the introduction of capsule mixture of γ-modification of paraaminobenzoic in the blood is higher than the introduction of one substance γ-modification of paraaminobenzoic, namely: after 0.5 hour after administration 1.69 times, 1 hour later - is 1.21 times.
The maximum concentration of γ-modification of paraaminobenzoic after the introduction of a pure substance is 15,16±1,64, and after the introduction of capsule mix - 18,31±1,04 g/ml, respectively.
As a result of the research it was revealed that the maximum concentration in the blood and the degree of bioavailability of γ-modification of paraaminobenzoic in the capsule composition of the mixture is considerably superior than when using a single substance.
The selected auxiliary ingredients and their quantities provide the necessary technological characteristics composition: flowability, bulk weight, bulk density while providing maximum bioavailability of the active substance. We offer capsule composition has the following technological features:
|The flowability of the composition||1.5-2.5 g/s|
|Bulk density||0,8569 g/cm3|
|Bulk density||0,5592 g/cm3.|
Thus, the proposed capsule composition containing γ-modification of paraaminobenzoic, provides high technological characteristics of the drug substance, as well as what its biological availability. The latter even exceeds the value of the biological availability of pure γ-modification of paraaminobenzoic.
Capsule composition has a low flowability, not electrified, which makes it easy to measure with great precision.
The mass of the proposed composition completely fills the capsule volume, in particular of 0.50 cm3, thus eliminating the phenomenon of "flotation", resulting from the free air space capsules. This is quite an important factor, since otherwise there is a reduction in contact area of the medicinal substance in the gastrointestinal tract, which in turn slows down the dissolution rate of a drug and, consequently, reducing the bioavailability of the dosage form.
If you want to use composition with greater or lesser content of γ-modification of paraaminobenzoic accordingly, it is necessary to use capsules of larger or smaller size. For this purpose it is only necessary to change the number of selected components, saving them the specified value.
The method of obtaining the proposed composition for capsules containing γ-modification of paraaminobenzoic, simple in technological performance and is as follows.
Prepare gelatin mass. Its preparation, the tion carried out in the traditional way, namely, after the preliminary swelling of gelatin at room temperature it is heated to complete dissolution. Then, the resulting gelatinous mass is formed into a gelatinous membrane by immersion, vacuum and thermostatic.
Composition for capsules prepared by mixing γ-modification of paraaminobenzoic and sucrose in selected quantities in round bottom flask for 10-15 min, followed by "dusting" sliding agents (talc, calcium stearate), for example, in the mixer type "turbula".
After this hard gelatin capsules filled the received contents using the capsule machine and close the lid.
For a better understanding of the present invention are the following specific examples.
Example 1. Prepare capsule mixture of the following composition, g:
|γ-Modification of paraaminobenzoic||0,04|
For this mix 0.04 g of γ-modification of paraaminobenzoic and 0,3728 g of sucrose in a round bottom flask for 10 minutes the mixture is podryvayut mixture 0,0129 g of talc and 0,0043 g of calcium stearate in "turbula".
The resulting composition has a flowability 2.5 g/s, bulk mass 0,8569 g/cm3, bulk density 0,5592 g/ cm3.
Example 2. Prepare capsule mixture of the following composition, g:
|γ-Modification of paraaminobenzoic||0,005|
The mixture is prepared as described in example 1.
The resulting composition has a flowability 2.0 g/s, bulk mass 0,8569 g/cm3, bulk density 0,5592 g/ cm3.
Example 3. Prepare capsule mixture of the following composition, g:
|γ-Modification of paraaminobenzoic||0,06|
The mixture is prepared as in example 1.
The resulting composition has a flowability of 1.5 g/s, bulk mass 0,8569 g/cm3, bulk density 0,5592 g/cm3.
Antimicrobial and online is hereinafterbe means on the basis of the γ-modification of paraaminobenzoic,
characterized in that it is made in the form of capsules and additionally contains talc, calcium stearate and sucrose in the following ratio, wt.%:
|sucrose||82,05 to 86.7|
SUBSTANCE: medicinal preparation for diabetes treatment contains active pharmaceutical ingredients, obtained from root of rehmania (Radix Rehmanniae), root of astragalus (Radix Astragali), rhizomes of yam (Rhizoma Dioscoreae), root of kudzu hemp (Radix Puerariae Lobatae), root of snake gourd (Radix Trichosanthis), baculums with stigmas of corn (Stylus Zeae Maydis), fruits of schizandra (Fructus Schisandrae Sphenantherae) and Glibenclamidum (Glibenclamide), taken in a certain parity. Way of preparation of a medicinal preparation in the form of drop-pills. A way of preparation of a medicinal preparation in the form of pills. A way of preparation of a medicinal preparation in the form of capsules. A way of preparation of a medicinal preparation in the form of tablets. A way of preparation of a medicinal preparation in the form of granules. A way of preparation of a medicinal preparation in the form of soft capsules. A way of preparation of a medicinal preparation in the form of a powder.
EFFECT: efficiency for diabetes treatment.
14 cl, 3 tbl, 18 ex
SUBSTANCE: invention concerns a dispersion of crystals or granules of active substance in lipophilic filler where crystals or granules are covered for taste masking. The invention also concerns chewing or quickly dissolved soft gelatinous capsules filled with the specified dispersion, and also a way of manufacture of such forms. Use of considerable quantities of active substance which should be accepted at unitary introduction, and maintenance of satisfactory release of active substance in vivo is possible.
EFFECT: new dosed out forms are stable throughout all period of storage.
15 cl, 17 tbl, 5 ex
SUBSTANCE: present invention concerns area of medical products, in particular, to the capsule of a medicinal preparation made in the form of an elastic, soluble in a human body, monolithic body with a cavity for placing of a liquid medicinal preparation, having an inflow with a notch on an outer side, with the through aperture executed in it; the capsule is fixed on clothes. Such performance of the capsule excludes leak of a liquid medicinal preparation at an abruption from it, it is convenient for the patient as allows receiving a medicinal preparation in time.
EFFECT: exclusion of leak of a liquid medicinal preparation at an abruption from it, it is convenient for the patient as allows receiving a medicinal preparation in time.
1 dwg, 1 tbl, 5 ex
SUBSTANCE: invention refers to chemical-pharmaceutical industry and medicine, namely to oral gindarine medicine characterised as a tranquilizer. Said medicine contains gindarine hydrochloride as an active material and auxiliary components and represents a solid gelatinous capsule. Gindarine is included as a compound of the mass filling capsules as mixed powders of gindarine and auxiliary components or as a granulated material. As the auxiliary components, the medicine contains bulking agent either alone, or combined with a disintegrant or antifriction material or with their mixture. There is also provided method of production of specified oral medicine.
EFFECT: invention provides simplified technological process for making the gindarine medicine, reduction of defective goods, reduced production cost, higher bioavailability of gindarine in comparison with a tableted medical product.
4 cl, 3 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention concerns medical products and concerns capsules for delivery of biologically active agent, containing: a water-soluble, washed away, blasted and-or bulking up cover; and b) the water filling composition including one or more active agents, the water which is in quantity from at least approximately 10% of masses/masses, to less than approximately 70% of masses/weights; and water-soluble derivative cyclodextrin, present at quantity of at least 30% of mass/mass, in recalculation on a total weight of water and derivative cyclodextrin in a filling composition where the quantity derivative cyclodextrin is enough for suppression of dissolution, washing out, destruction and-or a swelling of the cover, caused by water in a filling composition and where the capsule has a period of storage at least one week. Also the way of stabilisation of a capsule is opened.
EFFECT: creation of capsules with steady against dissolution, washing out, destruction and swelling covers.
51 cl, 11 dwg, 11 tbl, 10 ex
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
SUBSTANCE: invention refers to chemical-pharmaceutical industry, and concerns an oral drug delivery system including biliquid foam containing continuous hydrophilic phase 1 to 20 wt %, pharmaceutically acceptable oil 70 to 98 wt % producing discontinuous phase. A slightly water-soluble drug 0.1 to 20 wt % is dissolved or dispersed in said pharmaceutically acceptable oil. The drug delivery system also contains biliquid foam with included surface-active substance 0.5 to 10 wt % to produce stable biliquid foam with all the amounts specified in percentage of total composition.
EFFECT: drug delivery system ensures high bioavailability of slightly water-soluble oral drugs.
22 cl, 16 ex, 1 tbl
FIELD: medicine; biotechnologies.
SUBSTANCE: method of DNA storage in a redistilled water containing preservative in the form of manganic sulphate in concentration 0.08125 8.125 mM, at temperature -20°C is offered.
EFFECT: prevention of DNA damage by free radicals when storing and can be used in the field of molecular-genetic researches.
1 dwg, 8 ex
SUBSTANCE: present invention pertains to crystalline substance for peroral solid medicinal preparation, which is an indoline compound (KMD-3213), which exhibits blocking action to α1-adrinaline receptors, is suitable for use as a therapeutic medium in case of dysuria and is represented by formula (I) . The x-ray diffraction picture of the powder of this compound is characterised by main peaks 5.5°±0.2°, 6.1°±0.2°, 9.8°±0.2°, 11.1°±0.2°, 12.2°±0.2°, 16.4°±0.2°, 19.7°±0.2° and 20.0°±0.2°, as 2θ.
EFFECT: obtaining solid medicinal preparations for treating dysuria, containing this crystalline substance as an active ingredient.
14 cl, 3 dwg, 2 tbl, 9 ex
FIELD: medicine; pharmacology.
SUBSTANCE: pharmaceutical composition includes soft gelatin capsule with filler containing retinoid as active substance, 50 to 80 wt % of natural vegetable oil, 15 to 35 wt % of partially hydrogenised natural vegetable oil, and 3 to 20 wt % of middle-chain triglycerides. Additionally the filler contains 1 to 10 wt % of natural wax. Most preferable implementation version involves soft gelatin capsule includes combination of the described composition and capsule coating containing pig gelatin.
EFFECT: improved composition solubility.
18 cl, 5 ex
FIELD: biotechnology, veterinary medicine.
SUBSTANCE: invention relates to the development of biological preparation for prophylaxis and treatment of colibacillosis (escherichiosis) and for control of carriage of escherichious infections pathogens in animals and poultries also. Also, invention can be used in producing curative fodders and ecologically pure human foodstuffs. Biopreparation for prophylaxis and treatment of escherichiosis in animals and poultries comprises strains of bacteriophages Phagum Escherichia coli Ec022-DEP and/or Phagum Escherichia coli Ec021-DEP, and/or Phagum Escherichia coli Ex0782-DEP, and/or Phagum Escherichia coli Ec0781-DEP, and/or Phagum Escherichia coli EPZ-1-DEP, and/or Phagum Escherichia coli EPZ-2-DEP, and/or Phagum Escherichia coli EG-5-DEP, and/or Phagum Escherichia coli BC-1-DEP, and/or Phagum Escherichia coli M78-DEP, and/or Phagum Escherichia coli Sheksna 2k-DEP taken in the effective amount. The biopreparation comprises also antiseptic, for example, quinosol and a stabilizing agent. Protein (for example, soybean protein), vegetable meal, organic polymer, milk, serum, albumin can be used as a stabilizing agent. Among organic polymers can be used: dextran, polyglucin, starch, polyvinylpyrrolidone. The biopreparation can be dried by lyophilization, granulated and placed in polymeric matrix. The biopreparation has no toxic properties on animals, it shows good hygroscopicity and can be good dispersed in water. The biopreparation can be used in liquid and dry prescription formulations and in different methods of its administrations: both by subcutaneous, intraperitoneal, intramuscular injections and as an aerosol, by administration of phage particles into lung compartments including applying as curative fodder and supplement to fodder, and by applying on surface of cutaneous integuments. Invention provides enhancing the effectiveness of treatment of animals and poultries with gastroenteric infections due to reducing treatment period, expanding spectrum of lytic effect of the biopreparation, resistance to effect of digestive tract enzymes and convenience in using.
EFFECT: valuable veterinary properties of biopreparation.
9 cl, 5 tbl, 7 ex
FIELD: medicine, pharmacy.
SUBSTANCE: invention discloses compositions with sustained-release of active component and masking taste that comprise one of more active components included in tricomponent matrix structure as a globule. This structure is formed successively by amphiphilic, lipophilic or inert matrices and included as globule or dispersed in hydrophilic matrix. Applying large amount of systems for regulation of dissolving active component provides modulating the dissolving rate of active component in aqueous and/or biological fluids by regulating thus kinetics in releasing active component in digestive tract.
EFFECT: valuable pharmaceutical properties of compositions.
14 cl, 14 ex
FIELD: medicine, pharmacy.
SUBSTANCE: invention relates to a pharmaceutical composition as a capsule for oral administration that comprises testosterone undecanoate as an active component dissolved in pharmaceutically acceptable liquid carrier wherein liquid carrier involves at least 50 wt.-% of castor oil. Using castor oil as a liquid carrier in combination with testosterone undecanoate as androgen provides preparing a solution that can contain about 200-250 mg of testosterone undecanoate/ml that represents the new achievement for testosterone solution for oral administration. Solution can contain lipophilic surface-active substance, such as lauryl glycol also. The composition shows good absorption in human body and elicits higher activity as compared with the known composition of undecanoate.
EFFECT: improved and valuable properties of composition.
7 cl, 1 ex
FIELD: medicine, gastroenterology, phytotherapy, pharmacy.
SUBSTANCE: invention relates to solid medicinal formulations, namely capsules "Gastrobiol-TSD". Gelatin capsule contain the natural pharmacologically active component - sea-buckthorn oil concentrate, cyclodextrin, vitamin U and magnesium oxide taken in the definite ratio of components given in the invention description. Invention provides preparing a medicinal formulation eliciting an anti-ulcer, analgetic and protective effect on mucosa effect being with minimal risk for development of adverse effect.
EFFECT: valuable medicinal properties of preparation.
1 tbl, 1 ex
FIELD: medicine, pharmacy.
SUBSTANCE: invention relates to a medicinal agent made as a gelatin capsule. A medicinal agent as gelatin capsule consists of cycloserine and accessory additives wherein calcium phosphate dihydrate, aerosil and calcium stearate taken in the definite components are used as accessory additives. Also, gelatin capsule comprises additionally glutamic acid, gelatin and water, Invention provides rapid and complete release of agent in intake and the development of a medicinal formulation reducing toxicity of an active substance and eliciting stability in storage.
EFFECT: improved and valuable pharmaceutical and medicinal properties of agent.
1 tbl, 1 ex
FIELD: medicine, pharmacy.
SUBSTANCE: invention relates to a pharmaceutical composition for oral administration in treatment or prophylaxis of obesity or hyperlipidemia. The composition comprises orlistat and at least one ester of fatty acids and polyols. Melting point of fatty acid ester exceeds the body temperature and polyol is taken among group including glycerol, sugars, derivatives of sugars and their mixtures. Also, invention relates to a method for preparing above described composition and to a method for treatment or prophylaxis of obesity. Invention enhances effectiveness and activity of orlistat by reducing variability of effectiveness and/or activity of orlistat between patients and frequency and severity of adverse effects.
EFFECT: improved and valuable pharmaceutical properties of compositions.
24 cl, 1 tbl, 10 ex
SUBSTANCE: means is manufactured as capsule containing dibunol and 15% oil extraction of propolis.
EFFECT: enhanced effectiveness of treatment; prolonged regenerating and antibacterial action.
SUBSTANCE: the present innovation deals with cyclosporin-containing and practically oil-free compositions being of immunosuppressive action. The composition contains a hydrophilic surface-active substance, a lipophilic component, a lipophilic surface-active substance and ethanol. As a hydrophilic surface-active substance this composition contains ether of fatty acid and polyoxyethylene sorbitane and product of either natural or hydrogenised castor oil and ethylenoxide; as a lipophilic component and lipophilic surface-active substance it contains ether of fatty acid and sorbitane. The suggested composition has been designed as a gelatinous capsule with solid covering. The present innovation solves the problem dealing with stability of galena compositions with cyclosporin: at treating with water the composition develops practically stable microemulsion.
EFFECT: higher efficiency of application.
11 cl, 2 ex
SUBSTANCE: the present innovation deals with peroral liquid compositions which could be designed into gelatinous capsules. The suggested pharmaceutical composition includes a pharmaceutically active agent, a solubilizing agent and, not obligatory, a surface-active substance and a plastifying agent. The pharmaceutically active agent has got, at least, one acidic fragment, preferrably, that of carbonic acid being chosen out of the group of non steroid antiphlogistic preparations being acid-soluble at acid : dissolved substance ratio being from 3:1 to 10000:1. New compositions provide increased rates and degrees of absorption of pharmaceutically active agent and minimize side effects caused by such active substances.
EFFECT: higher efficiency of application.
42 cl, 39 ex
FIELD: chemical-pharmaceutical industry, pharmacy.
SUBSTANCE: invention relates to a new pharmaceutical composition comprising benzamide derivative and one or some additives taken among the following substances: 1) mixture of polyethylene glycol and surface-active substance; 2) amino acid or inorganic acid salt, and 3) propylene carbonate. The composition comprises benzamide derivative taken in the amount from 0.001 to 1000 mg per a single dosing formulation. The composition shows the enhanced solubility and absorption capacity in oral route of administration.
EFFECT: improved medicinal and pharmaceutical properties of composition.
9 cl, 4 tbl, 1 dwg, 5 ex