Method for preparing drug microcapsules of cephalosporins in konjak gum in butyl alcohol

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to microcapsulation of cephalosporins related to β-lactam antibiotics. The method is characterised by the fact that konjac gum is used as a microcapsule membrane; a konjak solution cerocon in butyl alcohol is added with the preparation E472 as a surfactant; a powdered antibiotic of cephalosporin is dissolved in water and transferred into the konjak solution cerocon in butyl alcohol; after the antibiotic forms an independent solid phase, carbinol and distilled water are added slowly drop-by-drop; the prepared microcapsule suspension is filtered in acetone and dried; the microcapsule process is performed at 25°C with no special equipment required; the relation of carbinol and butyl alcohol makes 1:3.

EFFECT: invention provides simplified and accelerated preparation of the water-soluble drug microcapsules of cephalosporins in konjac gum, loss reduction in preparing the microcapsules (higher yield-mass).

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The invention relates to the field of microencapsulation of drugs of cephalosporin group related to β-lactam antibiotics, in Konakovo gum physico-chemical method for the deposition aristotelem.

Previously known methods for producing microcapsules of drugs. Thus, in U.S. Pat. Of the Russian Federation No. 2092155 IPC AC 047/02, AK 009/16 publ. 10.10.1997 the method of microencapsulation of drugs, based on the use of special equipment use of irradiation with ultraviolet rays.

The disadvantages of this method are the duration of the process and the use of ultraviolet radiation, which can influence the formation of microcapsules.

In Pat. Of the Russian Federation No. 2095055 IPC AC 9/52, AK 9/16, AC 9/10, publ. 10.11.1997 method for obtaining a solid non-porous microspheres, which comprises melting pharmaceutically inactive substance carrier, the dispersion of a pharmaceutically active substance in the melt in an inert atmosphere, spraying the resulting dispersion in the form of a mist in the freezing chamber under pressure, in an inert atmosphere, at temperatures from - 15 to - 50°C, and the separation of the obtained microspheres into fractions by size. The suspension is intended for administration by parenteral injection, contains an effective amount of these microspheres, the distribution is Alannah in a pharmaceutically acceptable liquid vector, and the pharmaceutically active substance is insoluble microspheres in a specified liquid medium.

Disadvantages of the proposed method: the complexity and duration of the process, the use of special equipment.

In Pat. Of the Russian Federation No. 2076765 IPC B01D 9/02 publ. 10.04.1997 method for obtaining dispersed particles of soluble compounds in the microcapsules by crystallization from a solution, wherein the solution is dispersed in an inert matrix, cooled and, by changing the temperature, get dispersed particles.

The disadvantage of this method is the difficulty of execution: obtaining microcapsules by dispersion with subsequent change of temperatures, which slows down the process.

In Pat. Of the Russian Federation No. 2101010 IPC AC 9/52, AK 9/50, AK 9/22, AK 9/20, AK 31/19 publ. 10.01.1998 proposed chewable form of the drug with taste masking, having the properties of a controlled release drug product that contains microcapsules with a size of 100-800 microns in diameter and consists of pharmaceutical kernel crystalline ibuprofen and polymeric coating comprising a plasticizer, elastic enough to resist chewing. The polymer coating is a copolymer based on methacrylic acid.

The drawbacks of the invention: use of a copolymer based on methacrylic acid, chandanie polymer coating can cause cancer; obtaining microcapsules by the method of suspension polymerization; complexity; the duration of the process.

In Pat. Of the Russian Federation No. 2139046 IPC AC 9/50, AK 49/00, AK 51/00 publ. 10.10.1999 method for obtaining microcapsules as follows. Emulsion oil-in-water prepared from organic solution containing dissolved mono-, di-, triglyceride, preferably of tripalmitin or tristearin, and possibly therapeutically active substance, and an aqueous solution containing surface-active agent may evaporate part of the solvent, add redispersible agent and the mixture is subjected to drying by freezing. Subjected to drying by freezing the mixture is then dispersed in an aqueous medium to separate the particles from organic substances and a hemispherical or spherical microcapsules dried.

Disadvantages of the proposed method are the complexity and duration of the process, the use of drying by freezing, which takes time and slows down the process of production of microcapsules.

In Pat. Of the Russian Federation No. 2159037 IPC A01N 25/28, A01N 25/30 publ. 20.11.2000 method for obtaining microcapsules polymerization reaction at the phase boundary, containing solid agrochemical material 0.1 to 55 wt.%, suspended in peremestivsheesya water organic liquid, from 0.01 to 10 wt.% non-ionic dispersant, Akti is tion on the phase boundary and is not acting as an emulsifier.

Disadvantages of the proposed method: the complexity, duration, using wysokosciowe mixer.

In the article "Razrabotka microencapsulated and gel products and materials for various industries", Russian chemical journal, 2001, .XLV, No. 5-6, s-135 is described a method of producing microcapsules of drugs by the method of gas-phase polymerization, since the authors considered unsuitable method of chemical koatservatsii from aqueous media for microencapsulation of drugs due to the fact that most of them are water-soluble. The process of microencapsulation by the method of gas-phase polymerization usingn-xylylene includes the following basic stages: evaporation dimern-xylylene (170°C), thermal decomposition of it into the pyrolysis furnace (650°C at a residual pressure of 0.5 mm Hg), the transfer of the reaction products in the "cold" chamber of polymerization (20°C, the residual pressure of 0.1 mm Hg), deposition and polymerization on the surface of the protected object. Luggage polymerization is performed in the form of a rotating drum, the optimal speed for powder coating 30 rpm, the Thickness of the shell is governed by the time of coating. This method is suitable for the encapsulation of any solids (except prone to intense sublimation). Developed the first poly-n-xylylene - vysokokritichnyh polymer with high orientation and dense packing, provides a conformal coating.

Disadvantages of the proposed method are the complexity and duration of the process, using the method of gas-phase polymerization, which makes the method inapplicable to obtain microcapsules of drugs in polymers protein nature due to the denaturation of proteins at high temperatures.

In the article "Development of micro - and nano drug delivery", Russian chemical journal, 2008, t.LII, No. 1, p.48-57 presents a method of obtaining microcapsules included with proteins, which does not significantly reduce their biological activity carried out by the process of interfacial crosslinking of soluble starch or hydroxyethylamine and bovine serum albumin (BSA) using terephthaloyl chloride. The proteinase inhibitor is Aprotinin, either native or protected with the active site, was microcapsular in his introduction to the composition of the aqueous phase. Tapered shape liofilizovannyh particles indicates obtaining microcapsules or particles tank types. Thus prepared microcapsules were not damaged after lyophilization and easily restored its spherical shape after rehydration in a buffered environment. The pH value of the aqueous phase was to define the criterion upon receipt of solid microcapsules with high output.

The disadvantage of the proposed method of producing microcapsules is the complexity of the process, and hence low yield of microcapsules.

In Pat. Of the Russian Federation No. 2173140 IPC AC 009/50, AK 009/127 publ. 10.09.2001 method for obtaining kremnijorganicheskih microcapsules using a rotary cavitation plants with high shear effort and powerful acoustic phenomena of sound and ultrasound range for dispersion.

The disadvantage of this method is the use of special equipment - rotary-cavity setup, which has the ultrasonic action that affects the formation of microcapsules and can cause adverse reactions due to the fact that ultrasound destructive effect on the polymers of protein nature, therefore the proposed method is applicable when working with polymers of synthetic origin.

In path No. 2359662 IPC AC 009/56, A61J 003/07, B01J 013/02, A23L 001/00 publ. 27.06.2009 method for obtaining microcapsules using spray cooling in the spray tower Niro under the following conditions: air temperature at the inlet 10°C, the temperature at the outlet 28°C, the speed of rotation of the spray drum 10000 rpm Microcapsules according to the invention have improved stability and provide adjustable and/or prolonged in the release of the active ingredient.

Disadvantages of the proposed method are the duration of the process and the use of special equipment, a set of conditions (temperature of inlet air 10°C, the temperature at the outlet 28°C, the speed of rotation of the spray drum 10,000 rpm).

In Pat. WO/2010/076360 ES IPC B01J 13/00; AC 9/14; AC 9/10; AC 9/12 publ. 08.07.2010 proposed a new method for obtaining solid micro - and nanoparticles with a homogeneous structure with a particle size less than 10 μm, where the treated solid connections have a natural crystalline, amorphous, polymorphous, and other conditions associated with the reference compound. The method allows to obtain a solid micro - and nanoparticles with a substantially spheroidal morphological.

The disadvantage of the proposed method is the complexity of the process and low yield of the final product.

In Pat. WO/2010/014011 NL IPC AC 9/50; B01J 13/02; A61K 9/50; B01J 13/02 publ. 4.02.2010 described a method of producing microcapsules with a diameter of from 0.1 μm to 25 μm, comprising: a core particle with a diameter of 90 nm to 23 μm, containing at least 3% active ingredient by weight of the particles; a coating that completely covers the basic particles containing at least 20% by weight of a hydrophobic polymer selected from cellulose esters, cellulose ethers, shellac, gluten, polyacryl, hydrophobic starch derivatives, polyvinyl acetate, polymers or FOSS is Kerov based on esters of acrylic acid and/or methacrylic acid, and combinations thereof. The active ingredient is not released when introduced into aqueous food products, beverages, food or pharmaceutical composition. Once inside, however, the active ingredient is excreted quickly.

The disadvantages of this method are the complexity, the length of the process, as well as the use of ultrasound and special equipment, the use of the shells of the microcapsules copolymers of acrylic or methacrylic acid, which can cause cancer.

In .WO/2010/119041 EP IPC A23L 1/00 publ. 21.10.2010 method for obtaining the beads that contains the active ingredient encapsulated in the gel matrix whey protein, comprising denatured protein, serum and active components. The invention relates to a method for production of beads that contain components such as probiotic bacteria. The method of receiving beads includes a stage production of beads in accordance with the method of the invention, and the subsequent curing of the beads in the solution of anionic polysaccharide with a pH of 4.6 and below for at least 10, 30, 60, 90, 120, 180 minutes. Examples of suitable anionic polysaccharides: pectins, alginates, carrageenan. Ideally, whey protein is teplogeneriruyuschim, although other methods of denaturation is also applicable, for example, denaturation inducir the private pressure. In a preferred embodiment, whey protein denaturised at a temperature of from 75°C to 80°C properly within from 30 minutes to 50 minutes. Typically, whey protein mixed with thermal denaturation. Accordingly, the concentration of the whey protein is from 5 to 15%, preferably from 7 to 12%, and ideally from 9 to 11% (weight / volume). Typically, filtering is carried out through multiple filters with a gradual decrease in pore size. Ideally, the fine filter has a submicron pore size, for example from 0.1 to 0.9 microns. The preferred method of obtaining the beads is a method using vibration encapsulation (Inotech, Switzerland) and machinery manufacturing Nisco Engineering AG. Typically, the nozzles have openings 100 and 600 μm, and ideally about 150 microns.

The disadvantage of this method is the use of special equipment (vibration encapsulation (Inotech, Switzerland)), obtaining microcapsules by denaturation of the protein, the complexity of the allocation obtained by way of microcapsules filtering using multiple filters, which makes the process longer.

In Pat. WO/2011/003805 EP IPC B01J 13/18; B65D 83/14; C08G 18/00 publ. 13.01.2011 described a method of producing microcapsules, which are suitable for use in compositions forming sealants, foams, coatings or adhesives.

A disadvantage before the its method is the use of centrifugation to separate from the fluid the length of the process, and the use of this method not in the pharmaceutical industry.

In Pat. 20110223314 IPC B05D 7/00 20060101 B05D 007/00, VS 3/02 20060101 VS 003/02; VS 11/00 20060101 VS 011/00; B05D 1/18 20060101 B05D 001/18; B05D 3/02 20060101 B05D 003/02; B05D 3/06 20060101 B05D 003/06 from 10.03. 2011 US described a method of producing microcapsules by the method of suspension polymerization, belonging to the group of chemical methods with the use of the new device and ultraviolet radiation.

The disadvantage of this method is the complexity and duration of the process, the use of special equipment, the use of ultraviolet radiation.

In Pat. WO/2011/150138 US IPC C11D 3/37; B01J 13/08; C11D 17/00 publ. 01.12.2011 described a method of producing microcapsules solid water-soluble agents polymerization method.

The disadvantages of this method are the complexity and duration of the process.

In Pat. WO/2011/127030 US IPC AC 8/11; B01J 2/00; B01J 13/06;

C11D 3/37; C11D 3/39; C11D 17/00 publ. 13.10.2011 proposed several methods for producing microcapsules: interfacial polymerization, thermoanaerobium separation of the phases, spray drying, evaporation of the solvent and other

The disadvantages of the proposed methods is the complexity, duration processes, as well as the use of special equipment (filter (Albet, Dassel, Germany), spray dryer for collecting particles (Spray-M Dryer from Losert, Belgium).

In Pat. WO/2011/104526 GB IPC B01J 13/00; B01J 13/14; SV 67/00; C09D 11/02 publ. 01.09.2011 method for obtaining a dispersion of encapsulated solid particles in a liquid medium, comprising: a) grinding compositions, including solid, liquid medium and a polyurethane dispersant with an acid number of from 0.55 to 3.5 mmol per gram of dispersant, the composition comprises from 5 to 40 parts of the polyurethane dispersant per 100 parts of solid product, by weight; and b) crosslinking the polyurethane dispersant in the presence of solid and liquid environment.

Disadvantages of the proposed method are the complexity and duration of the process of production of microcapsules, and that the encapsulated particles obtained by the proposed method, are used as colorants in inks, especially ink jet printing for the pharmaceutical industry this technique is not applicable.

In .WO/2011/056935 US IPC C11D 17/00; A61K 8/11; B01J 13/02; C11D 3/50 publ. 12.05.2011 described a method of producing microcapsules with a size of 15 microns. As the shell material proposed polymers of the group consisting of polyethylene, polyamides, polystyrene, polyisoprenes, polycarbonates, polyesters, polyacrylates, polyureas, polyurethanes, polyolefins, polysaccharides, epoxy resins, vinyl polymers and mixtures thereof. The core of the encapsulated agents may include perfume, silicone Mac is a, waxes, hydrocarbons, higher fatty acids, essential oils, lipids, cooling the skin fluids, vitamins, sunscreens, antioxidants, glycerin, catalysts, bleach particles, particles of silicon dioxide and other

Disadvantages of the proposed method are the complexity, the length of the process, using as the shells of the microcapsules polymers of synthetic origin, and mixtures thereof.

In .WO/2011/160733 EP IPC B01J 13/16 publ. 29.12.2011 described a method of producing microcapsules, which contain shell and core water-insoluble materials. An aqueous solution of protective colloid and a solution of a mixture of at least two structurally different bifunctional diisocyanate (a) and (C), insoluble in water, gather together before the formation of the emulsion, is then added to the mixture of bifunctional amines and heated to a temperature of at least 60°C until the formation of microcapsules.

Disadvantages of the proposed method are the complexity, the length of the process, using as the shells of the microcapsules polymers of synthetic origin, and mixtures thereof.

In .WO/2011/161229 EP IPC AC 8/11; B01J 13/14; B01J 13/16; C11D 3/50 publ. 29.12.2011 described a method of producing microcapsules containing a shell of polyurea and spirits in oil, where the shell is obtained by the reaction of two structurally different diisocyanates in the form of em is lsii. In the process of production of microcapsules are used protective colloids. During the reaction of isocyanates and amines should be protective colloid. This is preferably polyvinylpyrrolidone (PVP). Protective colloid - polymer system, in which the suspension or dispersion prevents sticking (agglomeration, coagulation, flocculation). With this method can be used for perfume and all sorts of consumer goods. An exhaustive list of consumer goods may not be listed. Illustrative examples of consumer products include all kinds of uses, including liquid and powder detergents; all personal care products and hair care, including shampoos, conditioners, creams, and Soaps, body creams, etc.; deodorants and antiperspirants.

The disadvantages of this method of producing microcapsules are long and complex process, use as the shell of the microcapsules diisocyanates, which are the result of the reaction of the two isocyanates.

The closest method is the method proposed in U.S. Pat. Of the Russian Federation No. 2134967 IPC A01N 53/00, A01N 25/28 publ. 27.08.1999). Water is dispersed solution of a mixture of natural lipids and a PYRETHROID insecticide in a weight ratio of 2(4:1) in an organic solvent, which leads to simplification of the method of microencapsulation.

Insufficient the MD method is that the dispersion in the aqueous medium, what makes the proposed method applicable to the production of microcapsules of water-soluble drugs in water-soluble polymers.

The technical objective is the simplification and acceleration of the process of obtaining the microcapsules vodorastvorimyh drugs group of cephalosporins in Konakovo gums, reducing losses upon receipt of the microcapsules (increase in mass).

The solution of the technical problem is achieved by a method of producing microcapsules drug group cephalosporins related to β-lactam antibiotics, characterized in that as the shell of the microcapsules is Konakova gum, as well as obtaining microcapsules physico-chemical deposition method by nerastvorim using two precipitators - carbinol butilovogo alcohol, the retrieval process is carried out without special equipment.

A distinctive feature of the proposed method is the use as the shell of the microcapsules drug group cephalosporins related to β-lactam antibiotics, Konakovo gums, and obtaining microcapsules physico-chemical deposition method by nerastvorim using two precipitators - carbinol butyl alcohol.

The result of the proposed method are obtaining microcapsules drug preparatory cephalosporins, related to β-lactam antibiotics, in Konakovo gum at 25°C for 15 minutes. The output of the microcapsules is over 90%.

Required for microencapsulation of Konakova gum was industrial production under the trade name konjac cercon and konjac gum 3600.

EXAMPLE 1. Obtaining microcapsules Cefotaxime in konjac gum 3600 using carbinol and butyl alcohol as a precipitating the ratio 1:3

To 6 g of 5% solution of konjac gum 3600 in butyl alcohol added 0.01 g of the drug A as surfactants. The resulting mixture was put on a magnetic stirrer and include mixing. 0.1 g of the powder Cefotaxime dissolved in 0.5 ml of water and transferred into a solution of konjac gum 3600 in butyl alcohol. After the formation of the Cefotaxime independent solid phase very slowly added dropwise 5 ml of carbinol and 1 ml of distilled water. The resulting suspension of microcapsules is filtered by the filter SCHOTT 16 class then washed with acetone, dried in a desiccator over calcium chloride.

Received and 0.37 g of white powder. The yield was 92%.

EXAMPLE 2. Obtaining microcapsules Ceftriaxone in konjac gum 3600 using carbinol and butyl alcohol as a precipitating the ratio 1:3

To 6 g of 5% solution of konjac gum 3600 in butyl alcohol added 0.01 g of the drug A as the surface is surface-active substances. The resulting mixture was put on a magnetic stirrer and include mixing. 0.1 g of Ceftriaxone powder dissolved in 0.5 ml of water and transferred into a solution of konjac gum 3600 in butyl alcohol. After the formation of the Ceftriaxone independent solid phase very slowly added dropwise 5 ml of carbinol and 1 ml of distilled water. The resulting suspension of microcapsules is filtered by the filter SCHOTT 16 class then washed with acetone, dried in a desiccator over calcium chloride.

Received 0,376 g of white powder. The yield was 93%.

EXAMPLE 3. Obtaining microcapsules is anticipated in the konjac gum 3600 using carbinol and butyl alcohol as a precipitating the ratio 1:3

To 6 g of 5% solution of konjac gum 3600 in butyl alcohol added 0.01 g of the drug A as surfactants. The resulting mixture was put on a magnetic stirrer and include mixing. 0.1 g of Cefazolin powder dissolved in 0.5 ml of water and transferred into a solution of konjac gum 3600 in butyl alcohol. After the formation of the anticipated independent solid phase very slowly added dropwise 5 ml of carbinol and 1 ml of distilled water. The resulting suspension of microcapsules is filtered by the filter SCHOTT 16 class then washed with acetone, dried in a desiccator over calcium chloride.

Obtained 0.36 g of a white powder. The yield was 90%.

PR IS MEASURES 4. Obtaining microcapsules Cefotaxime in konjak cerocon using carbinol and butyl alcohol as a precipitating the ratio 1:3

To 6 g of 5% solution of konjac cerocon in butyl alcohol added 0.01 g of the drug A as surfactants. The resulting mixture was put on a magnetic stirrer and include mixing. 0.1 g of the powder Cefotaxime dissolved in 0.5 ml of water and transferred into a solution of konjac cerocon in butyl alcohol. After the formation of the Cefotaxime independent solid phase very slowly added dropwise 5 ml of carbinol and 1 ml of distilled water. The resulting suspension of microcapsules is filtered by the filter SCHOTT 16 class then washed with acetone, dried in a desiccator over calcium chloride.

Received 0,372 g of white powder. The yield was 93%.

EXAMPLE 5. Obtaining microcapsules Ceftriaxone in the konjak cerocon using carbinol and butyl alcohol as a precipitating the ratio 1:3

To 6 g of 5% solution of konjac cerocon in butyl alcohol added 0.01 g of the drug A as surfactants. The resulting mixture was put on a magnetic stirrer and include mixing. 0.1 g of Ceftriaxone powder dissolved in 0.5 ml of water and transferred into a solution of konjac cerocon in butyl alcohol. After the formation of the Ceftriaxone independent solid phase very slowly dropwise on billaut 5 ml carbinol and 1 ml of distilled water. The resulting suspension of microcapsules is filtered by the filter SCHOTT 16 class then washed with acetone, dried in a desiccator over calcium chloride.

Received 0,372 g of white powder. The yield was 95%.

EXAMPLE 6. Obtaining microcapsules is anticipated in the konjak cerocon using carbinol and butyl alcohol as a precipitating the ratio 1:3

To 6 g of 5% solution of konjac cerocon in butyl alcohol added 0.01 g of the drug A with as surfactants. The resulting mixture was put on a magnetic stirrer and include mixing. 0.1 g of Cefazolin powder dissolved in 0.5 ml of water and transferred into a solution of konjac cerocon in butyl alcohol. After the formation of the anticipated independent solid phase very slowly added dropwise 5 ml of carbinol and 1 ml of distilled water. The resulting suspension of microcapsules is filtered by the filter SCHOTT 16 class then washed with acetone, dried in a desiccator over calcium chloride.

Received 0,356 g of white powder. The yield was 89%.

The obtained microcapsules drug group cephalosporins related to β-lactam antibiotics, in Konakovo gum physico-chemical method for the deposition nerastvorim using carbinol and butyl alcohol as nerastvorimaya. The process is simple to perform and lasts for 15 minutes, do not require the t special equipment.

Konakova gum is widely used in the pharmaceutical industry drugs for weight loss and regulation chair, as a binder in tablets. In the Russian Federation is permitted in food in an amount up to 10 g/kg of product (p SanPiN 2.3.2.1293-03). Technological function: thickener, gelling, stabilizer, means for tableting. Composition: neutral polysaccharide glucomannan consists of D-glucose and D-mannose in a ratio of from 1:4 to 2:3. Receiving: three tubers of Amorphophallus plants, weighing more than a kilogram, cut, dried, milled and sieved flour is subjected to swelling in water, treated with lime milk and filtered. Glucomannan is precipitated from the filtrate with alcohol and dried.

The proposed method is suitable for the pharmaceutical industry due to the minimal loss of speed, ease of acquisition and allocation of microcapsules cephalosporins related to β-lactam antibiotics, in Konakovo gums.

The method of producing microcapsules drugs group of cephalosporins, characterized in that as the shell of the microcapsules is Konakova gum, the solution of konjac cerocon in butyl alcohol add drug E472 as surfactants, and the powder antibiotic of cephalosporin group is dissolved in water and the PE UNOSAT in a solution of konjac cerocon in butyl alcohol, after the formation of the antibiotic independent solid phase very slowly added dropwise carbinol and distilled water, the resulting suspension of microcapsules is filtered off with acetone and dried, the process of production of microcapsules is carried out at 25°C without special equipment, the ratio of the carbinol and butyl alcohol is 1:3.



 

Same patents:

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to method of obtaining microcapsules of medication of cephalosporin group in konjac gum. In accordance with claimed method cephalosporin powder, preliminarily dissolved in dimethylformamide, and surface-active substance are added to konjac gum solution in isopropyl alcohol, with addition of carbinol after formation of independent solid phase by cephalosporin. Obtained suspension of microcapsules is filtered, washed with acetone and dried in dessicator.

EFFECT: invention makes it possible to simplify and accelerate process of obtaining microcapsules of water-soluble medications of cephalosporin groups in konjac gum, as well as to increase their output by weight.

4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to method of obtaining microcapsules of medication of cephalosporin group in poludanum. In accordance with claimed method cephalosporin powder and surface-active substance are added to aqueous solution of poludanum, mixture is mixed until components dissolve completely, after formation of transparent solution carbinol and after it isopropyl alcohol are additionally poured in. Obtained suspension of microcapsules is filtered, washed with acetone and dried in dessicator.

EFFECT: invention makes it possible to simplify and accelerate process of obtaining microcapsules of water-soluble medications of cephalosporin groups in poludanum, as well as to increase their output by weight.

4 ex

FIELD: veterinary medicine.

SUBSTANCE: method comprises the use of encapsulated fenbendazol. Sodium carboxymethyl cellulose is used as coating of the microcapsules. The microcapsules are obtained by the physico-chemical method of nonsolvent addition using two precipitators - carbinol and cyclohexanol. The ratio of core/polymer is 1:3. The preparation is given to animals at a dose of 22.5 mg/kg (15 mg/kg as active agent) as a single dose.

EFFECT: method is simple to use and is highly effective in the treatment of cattle with strongylatosis.

1 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to drug microencapsulation, particularly for preparing fenbendazole microcapsules. The method is characterised by the fact that a microcapsule coating is carboxymethyl cellulose; fenbendazole dissolved in dioxane or dimethyl sulphoxide (DMSO), or dimethyl formamide (DMFM) is dispersed into the solution of sodium carboxymethyl cellulose in dioxane in the presence of the preparation E472c; further, isopropanol and distilled water are added; the prepared microcapsule suspension is filtered and dried; a process of microcapsules is conducted at 25°C for 20 minutes with no special equipment; with nucleus/polymer ratio making 1:3.

EFFECT: invention provides simplifying and accelerating the process of preparing the fenbendazole microcapsules in carboxymethyl cellulose, reducing losses in preparing the microcapsules (higher weight yield).

3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a method for preparing drug microcapsules of cephalosporins in konjak gum in dioxane. According to the declared method, a konjak gum solution in dioxane is added with a surfactant that is a cephalosporin powder pre-dissolved in ethanol, and with carbinol after cephalosporin forms an independent solid phase. The prepared microcapsule suspension is filtered, washed in acetone and dried in a drying oven.

EFFECT: invention enables simplifying and accelerating the process of water-soluble drug microcapsules of cephalosporins in konjak gum, as well as increasing a mass yield.

4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to chemical-pharmaceutical industry, and represents a method for preparing drug microcapsules by non-solvent addition differing by the fact that the drug preparations are presented by the cephalosporin preparations, while a coating is konjak gum that is precipitated in tetrahydrofurane by the addition of non-solvents that are carbinol and water at 25°C.

EFFECT: invention provides simplified and accelerated preparation of the water-soluble drug microcapsules of cephalosporins in konjac gum, loss reduction in preparing the microcapsules (higher yield-mass).

4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine. What is described is an implanted drug delivery device on the basis of polyurethane for the delivery of biologically active compounds at a constant speed for a long period of time, and a method for preparing it. The device is high biocompatible and bioresistant, and applicable as an implant for patients (human and animals) for the delivery of biologically active compounds to tissues and organs.

EFFECT: implanted device provides the delivery at a constant speed for a long period of time.

26 cl, 5 tbl, 14 dwg, 8 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry, particularly to a method for preparing drug microcapsules of cephalosporin. The method for preparing drug microcapsules of cephalosporin consists in adding a konjak solution in carbon tetrachloride with a surfactant; a powder of cephalosporin is dissolved in water or ethanol and transferred into the konjak solution in carbon tetrachloride; once the antibiotic has formed an independent solid phase, carbinol and distilled water are added drop-by-drop; the prepared suspension of microcapsules is filtered, washed in acetone and dried; the process of microcapsules is carried out in the certain environment.

EFFECT: method provides simplifying and accelerating the process of microcapsules of water-soluble drug preparations.

7 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: composition for treating oxidative stress comprises ball-shaped lipoic acid or one of salts thereof, and at least one lipophilic medium. The lipoic acid balls represent particles consisting of an inert core (a nucleus) coated with lipoic acid which is coated with a first layer of an isolating polymer, and with a second polymer layer resistant (stable) at gastric pH. What is also described is a preparation for treating oxidative stress with an unified dose containing the above composition. The preparation is presented in the form of a soft gelatin capsule.

EFFECT: compositions according to the invention are stable in the lipophilic medium.

22 cl, 15 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a method for preparing interferon-coated cephalosporin microcapsules. The declared method is characterized by mixing 1% aqueous solution of human leukocyte α- or β-interferon, cephalosporin powder and preparation E472c as a surfactant. The prepared mixture is stirred until the reaction components are fully dissolved, and after a transparent solution is generated, methanol 1 ml as a first non-solvent and then isopropyl alcohol 5 ml as a second non-solvent are slowly added drop-by-drop, then filtered, washed in acetone and dried.

EFFECT: invention provides preparing the high-yield cephalosporin microcapsules and ensuring the loss reduction.

8 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention relates to application of a pharmaceutical drug form for peroral introduction to reduce inter-individual variability in paracetamol-containing compositions in a diabetic patient with gastric dismotility. The said drug form contains in a form of a granulate: paracetamol in amount 60-80 wt %, calcium carbonate in amount 5-20 wt %, at least, one first binding substance and, at least, one disintegrating substance, as well as, at least, one hydrophilic colloid as an extragranular component.

EFFECT: invention ensures improvement of an active substance absorption in the patient with gastric dismotility.

13 cl, 1 tbl, 3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to method of obtaining microcapsules of medication of cephalosporin group in konjac gum. In accordance with claimed method cephalosporin powder, preliminarily dissolved in dimethylformamide, and surface-active substance are added to konjac gum solution in isopropyl alcohol, with addition of carbinol after formation of independent solid phase by cephalosporin. Obtained suspension of microcapsules is filtered, washed with acetone and dried in dessicator.

EFFECT: invention makes it possible to simplify and accelerate process of obtaining microcapsules of water-soluble medications of cephalosporin groups in konjac gum, as well as to increase their output by weight.

4 ex

FIELD: medicine.

SUBSTANCE: drug preparation represents a composition containing: lappaconitine hydrobromide 0.02 - 0.06 g, pregelatinised starch 0.0335 - 0.0536 g, lactose monohydrate 0.058 - 0.122 g, hypromellose 0.078 - 0.161 g, calcium stearate 0.002 - 0.004 g and colloidal silicone dioxide 0.002 - 0.004 g.

EFFECT: prolonged antiarrhythmic action of the active ingredient lappaconitine hydrobromide with accessory alkaloids.

5 cl, 1 tbl

FIELD: medicine.

SUBSTANCE: invention refers to a method for preparing a pectin gel of an elevated part of willow herb. The declared method enables dissolving pre-recovered pectin from the elevated part of willow herb in water, cooling and applying onto a frozen chitosan solution and further gel formation.

EFFECT: invention enables preparing a degradable biomaterial possessing the antimicrobial activity on Escherichia coli and Staphylococcus aureus cells.

1 tbl, 1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a method for preparing drug microcapsules of cephalosporins in konjak gum in dioxane. According to the declared method, a konjak gum solution in dioxane is added with a surfactant that is a cephalosporin powder pre-dissolved in ethanol, and with carbinol after cephalosporin forms an independent solid phase. The prepared microcapsule suspension is filtered, washed in acetone and dried in a drying oven.

EFFECT: invention enables simplifying and accelerating the process of water-soluble drug microcapsules of cephalosporins in konjak gum, as well as increasing a mass yield.

4 ex

FIELD: chemistry.

SUBSTANCE: disclosed is a polysaccharide containing carboxyl functional groups, one of which is substituted with a hydrophobic alcohol derivative. Also disclosed is a pharmaceutical composition containing one of the disclosed polysaccharides and one active ingredient.

EFFECT: invention enables to obtain novel amphiphilic polysaccharide derivatives, having good biocompatibility.

26 cl, 1 tbl, 12 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical composition in the form of a skin protection paste. The composition contains a film-forming agent representing poly(butyl methacrylate-co-methyl methacrylate), hydrocolloid, a filling agent, a softening agent and an alcoholic diluent in the certain proportions.

EFFECT: pharmaceutical composition has a prolonged shelf life and is able to ensure a uniform skin coverage which is characterised by the balanced characteristics of durability and flexibility.

3 cl, 2 tbl, 5 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry, particularly to a method for preparing drug microcapsules of cephalosporin. The method for preparing drug microcapsules of cephalosporin consists in adding a konjak solution in carbon tetrachloride with a surfactant; a powder of cephalosporin is dissolved in water or ethanol and transferred into the konjak solution in carbon tetrachloride; once the antibiotic has formed an independent solid phase, carbinol and distilled water are added drop-by-drop; the prepared suspension of microcapsules is filtered, washed in acetone and dried; the process of microcapsules is carried out in the certain environment.

EFFECT: method provides simplifying and accelerating the process of microcapsules of water-soluble drug preparations.

7 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to medicine and described a complex prepared of a polysaccharide, particularly dextran, and a heparin-binding protein with the above polysaccharide being formed by (1,6) and/or (1,4) and/or (1,3) and/or (1,2) glycoside bonds and functionalised by at least one salt-forming or salt-transformed tryptophan derivative. The present invention also concerns a pharmaceutical composition containing the complex according to the invention.

EFFECT: using the complex ensures providing the better solubility and stability of the heparin-binding proteins.

10 cl, 12 ex, 2 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine and concerns a combined pharmaceutical composition having antibacterial activity. As an active substance, the composition contains a clindamycin salt or ester, a base which is a combination of a hydrophobic ingredient, a hydrophilic ingredient and an emulsifier, and a gelling polymer. A method of preparing the declared composition involves the fact that a solution of the clindamycin salt or ester in a part of the hydrophilic ingredient is added with the gelling polymer, then the emulsion prepared of a residual part of the hydrophilic ingredient, the hydrophobic ingredient and the emulsifier, and the prepared mixture is agitated until smooth.

EFFECT: new pharmaceutical formulation is characterised by a high level of antibacterial activity, stability both at storage temperature (25°C), and at temperature of use (37°C), good packaging extrusion.

15 cl, 1 dwg, 2 tbl, 4 ex

FIELD: medicine.

SUBSTANCE: composition contains phospholipids in the form of liposomes with the average particle size 0.05-0.22 mcm that are presented by phosphatidylcholine and/or cardiolipin, sulphated glycosaminoglycans in the form of keratan sulphate sodium salt and chondroitin sulphate sodium salt, a hypotensive preparation. Sulphated glycosaminoglycans and the hypotensive preparation are integrated into the liposomes, and placed outside the liposomes in a physiological solution. The composition additionally contains Oleamide, lisocyme and albumin. The ingredients are used in the declared amounts.

EFFECT: using the invention enables forming a protective layer of the lubricant on the ocular surface, reducing lachrymal film evaporation, normalising metabolic processes in the corneal epithelial cells that intensifies regenerative processes in the ocular surface structures.

7 ex

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