Method for preparing drug microcapsules of cephalosporins in konjak gum in acetone

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to the 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 cephalosporin preparations, while a coating is a konjak gum that is precipitated in acetone by 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 the konjac gum, loss reduction in preparing the microcapsules (higher yield-mass).

6 ex

 

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. Thus, in U.S. Pat. 2092155, IPC AC 047/02, AK 009/16 published 10.10.1997, Russian Federation, proposed a method for 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. 2095055, IPC AC 9/52, AK 9/16, AC 9/10, Russian Federation, published 10.11.1997, method for obtaining solid non-porous microspheres comprising 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 a temperature of 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 specified is trosper, distributed 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. 2076765, IPC B01D 9/02, Russian Federation, published 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. 2101010, IPC AC 9/52, AK 9/50, AK 9/22, AK 9/20, AK 31/19, Russian Federation, published 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 on the basis of meth is krylovii acid.

The drawbacks of the invention: use of a copolymer based on methacrylic acid, as these polymer coatings can cause cancer; complexity; the duration of the process.

In Pat. 2139046, IPC AC 9/50, AK 49/00, AK 51/00, Russian Federation, published 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. 2159037, IPC A01N 25/28, A01N 25/30, Russian Federation, published 20.11.2000, proposed a method of producing microcapsules by polymerization reaction at the phase boundary, containing TBE is every agrochemical material 0.1 to 55 wt.%, suspended in peremestivsheesya water organic liquid, from 0.01 to 10 wt.% non-ionic dispersant, active 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 "Development of microencapsulated and gel products and materials for various industries", Russian chemical journal, 2001, .XLV, No. 5-6, s-135, describes 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 using n-xylylene includes the following basic stages: evaporation dimer n-xylylene (170°C), thermal decomposition of it into the pyrolysis furnace (650°C at a residual pressure of 0.5 mm RT. century), the transfer of the reaction products in the "cold" chamber of polymerization (20°C, the residual pressure of 0.1 mm RT. Art.), 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 reg is niruetsya time of coating. This method is suitable for the encapsulation of any solids (except prone to intense sublimation). The resulting 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, .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 by the Le lyophilization and easily restored its spherical shape after rehydration in a buffered environment. The pH value of the aqueous phase was decisive in obtaining a solid microcapsules with high output.

The disadvantage of the proposed method of producing microcapsules is the complexity of the process, which, in turn, leads to reduction of the yield of the final capsules.

In Pat. 2173140, IPC AC 009/50, AK 009/127, Russian Federation, published 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-quotational installation, which has 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 Pat. 2359662, IPC AC 009/56, A61J 003/07, B01J 013/02, A23L 001/00 published 27.06.2009, Russian Federation, proposed a method of producing microcapsules using spray cooling in the spray tower Niro under the following conditions: air temperature at the inlet 10°C, the temperature on the ode 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 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/2009/148058 JP, IPC B01J 13/04 was investigated, A23L 1/00, AK 35/20, AK 45/00, AK 47/08, AK 47/26, AK 47/32, AK 47/34, AK 47/36, AK 9/50, B01J 2/04, B01J 2/06 published 10.12.2009, described the process of production of microcapsules, applicable for industrial production, which has a high content of hydrophilic biologically active substances enclosed in the shell. The proposed microcapsules can be used in food, pharmaceutical and other industries. In the production process applied dispersant composition consisting of a hydrophilic biologically active substances and surfactants in solid fat. Temperature not lower than the melting point of the solid fat.

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

In Pat. WO/2010/076360 ES, IPC B01J 13/00; AC 9/14; AC 9/10; AC 9/12 published 08.07.2010, a new method is proposed floor is solid micro - and nanoparticles with a homogeneous structure with a particle size less than 10 microns, 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 hence the low yield of the final product.

In Pat. WO/2010/014011 NL, IPC AC 9/50; B01J 13/02; AC 9/50; B01J 13/02, published 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, polylactide, hydrophobic starch derivatives, polyvinyl acetate, polymers or copolymers based acrylic ester acid and/or methacrylic acid, ether, 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 use as shells of microcapsules copolymers of acrylic or methacrylic acid, which can cause cancer.

In Pat. WO/2010/119041 EP, IPC A23L 1/00, published 21.10.2010, method for obtaining the beads containing 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 induced by pressure. In a preferred embodiment, whey protein denaturised at a temperature of from 75°C to 80°C, is 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 ostatnim reduction of pore size. Ideally, the fine filter has a submicron pore sizes, 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, published on 13.01.2011, described a method of producing microcapsules, which are suitable for use in compositions forming sealants, foams, coatings or adhesives.

The disadvantage of the proposed 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 the 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, published on 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, published on 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 ProCepT, Belgium)).

In Pat. WO/2011/104526 GB, IPC B01J 13/00; B01J 13/14; C09B 67/00; C09D 11/02, published on 01.09.2011, a 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 to 100 parts TV is rdih products, by weight; and b) crosslinking the polyurethane dispersant in the presence of solid and liquid media, for encapsulating solid particles which polyurethane dispersant contains less than 10% by weight of the recurring elements of polymeric alcohols.

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

In Pat. WO/2011/056935 US, IPC C11D 17/00; AC 8/11; B01J 13/02; 11D 3/50, published on 12.05.2011, describes how to obtain 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 proposed polymer membranes are sufficiently impervious core material and materials in the environment, in which are encapsulated. The agent will be used to provide benefits that will be received. The core of the encapsulated agents may include perfume, silicone oils, waxes, hydrocarbons, higher fatty acids, E. the IRNA oil, 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 Pat. WO/2011/160733 EP, IPC B01J 13/16, published on 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 (b) insoluble in water together before 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 Pat. WO/2011/161229 EP, IPC AC 8/11; B01J 13/14; B01J 13/16; C11D 3/50, published on 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 an emulsion. In the process of production of microcapsules and the use of 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 applications, including liquid detergents, powder detergents; all personal care products and hair care, including shampoos, conditioners, creams, styling cream, soap, 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.

In Pat. WO/2012/007438 EP, IPC A61K 8/11; A61Q 13/00; B01J 13/16; B01J 13/18, published on 19.01.2012, describes how to obtain particles with an average diameter of less than 50 microns, consisting of at least one shell, the method of stepwise polymerization involving isocyanate monomer. At least one shell formed chain reaction polymerization growth (preferably free-radiculoneuropathy), which is not associated with isocyanate. The invention also relates to a method for producing such particles, in which the casing is formed to chain growth polymerization at a temperature at which the chain reaction of growth is suppressed. The invention also provides a fully formulated products, preferably liquids and gels that contain these particles.

Disadvantages of the proposed method are the complexity and duration of the process, obtaining microcapsules by chemical method step polymerization. Obtained in this way particles have a sufficiently large size is 50 ám.

The closest method is the method proposed in U.S. Pat. 2134967, IPC A01N 53/00, A01N 25/28 published 27.08.1999, Russian Federation (1999). Water is dispersed solution of a mixture of natural lipids and a PYRETHROID insecticide in the weight ratio of 2-4:1 in an organic solvent, which leads to simplification of the method of microencapsulation.

The disadvantage of this method is the dispersion in the aquatic environment, which 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 production of microcapsules of water-soluble drugs group of cephalosporins in Konakovo gum, cutting losses when receiving the AI 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, and obtaining microcapsules physico-chemical deposition method by nerastvorim using two precipitators - carbinol and acetone, 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 and acetone.

The result of the proposed method are obtaining microcapsules drug group 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 cerocon and konjac gum 3600.

EXAMPLE 1. Obtaining microcapsules of cefepime in the konjak Shoop using carbinol and acetone is as precipitators, the ratio of 1:3

To 6 g of 5% solution of konjac cerocon in acetone added 0.01 g of the drug Is as surfactants. The resulting mixture was put on a magnetic stirrer and include mixing. 0.1 g of cefepime powder dissolved in 0.5 ml of water and transferred into a solution of konjac cerocon in acetone. After the formation of the cefepime 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 of 0.332 g of white powder. The yield was 83%.

EXAMPLE 2. Obtaining microcapsules of cefepime in konjac gum 3600 using carbinol and acetone as the precipitating, the ratio of 1:3

To 6 g of 5% solution of konjac gum 3600 in acetone added 0.01 g of the drug Is as surfactants. The resulting mixture was put on a magnetic stirrer and include mixing. 0.1 g of cefepime powder dissolved in 0.5 ml of ethanol and transferred into a solution of konjac gum 3600 in acetone. After the formation of the cefepime 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 madherishem calcium.

Received 0,352 g of white powder. The yield was 88%.

EXAMPLE 3. Obtaining microcapsules Ceftriaxone in the konjak cerocon using carbinol and acetone as the precipitating, the ratio of 1:3

To 6 g of 5% solution of konjac cerocon in acetone added 0.01 g of the drug Is 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 ethanol and transferred into a solution of konjac cerocon in acetone. 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 0,356 g of white powder. The yield was 89%.

EXAMPLE 4. Obtaining microcapsules Ceftriaxone in konjac gum 3600 using carbinol and acetone as the precipitating, the ratio of 1:3

To 6 g of 5% solution of konjac gum 3600 in acetone added 0.01 g of the drug Is 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 ethanol and transferred into a solution of konjac gum 3600 in acetone. After the formation of the Ceftriaxone independent solid phase PTS is ery 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%.

PRIMER 5. Obtaining microcapsules is anticipated in the konjak cerocon using carbinol and acetone as the precipitating, the ratio of 1:3

To 6 g of 5% solution of konjac cerocon in acetone added 0.01 g of the drug Is 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 ethanol and transferred into a solution of konjac cerocon in acetone. 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 0,344 g of white powder. The yield was 86%.

EXAMPLE 6. Obtaining microcapsules is anticipated in the konjac gum 3600 using carbinol and acetone as the precipitating, the ratio of 1:3

To 6 g of 5% solution of konjac gum 3600 in acetone added 0.01 g of the drug Is as surfactants. The resulting mixture was put on a magnetic stirrer and include mixing. 0.1 g of the powder is anticipated Rast is oraut in 0.5 ml of ethanol and transferred into a solution of konjac gum 3600 in acetone. 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 0,336 g of white powder. The yield was 84%.

The obtained microcapsules drug group cephalosporins related to β-lactam antibiotics, in Konakovo gum physico-chemical method for the deposition nerastvorim using carbinol and acetone as nerastvorimaya. The process is simple to perform and lasts for 15 minutes, requires no 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 products according to TI 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 of cut, dried, milled and sieved flour is subjected to swelling in water, the mod is functioning well with the milk of lime 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 of drugs by precipitation with aristotelem, characterized in that the quality of drugs used drugs group of cephalosporins, as the shell - Konakova gum, which is precipitated from a solution in acetone by adding as herstories carbinol and water at 25°C.



 

Same patents:

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to the field of pharmaceutics, in particular to microcapsulation of medications of a cephalosporin group, belonging to β-lactam antibiotics, in human serum albumin.

EFFECT: realisation of invention results in simplification and acceleration of the process of obtaining microcapsules of water-soluble medications of the cephalosporin group in human serum albumin, reduction of loss in the process of obtaining microcapsules (increase of the output by weight).

2 ex

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3 ex

FIELD: medicine, pharmaceutics.

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4 ex

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16 ex

FIELD: medicine.

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FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to the field of pharmaceutics, in particular to microcapsulation of medications of a cephalosporin group, belonging to β-lactam antibiotics, in human serum albumin.

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2 ex

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3 ex

FIELD: chemistry.

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3 cl, 4 dwg, 1 ex

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).

6 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, 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.

SUBSTANCE: invention refers to biochemistry. What is involved is a qualitative assessment of the efficacy of oleic acid as an RNA carrier through biological membranes. The biological membrane is presented by soft sac cells of ripe pulp of honey pomelo of the genus Citrus. The RNA carrier is presented by oleic acid from the preparation Vitalang-2 in an amount of 10.8% and forming a complex with RNA. The preparation Vitalang-1 containing pure RNA is used as a reference. The pomelo cells are poured separately with aqueous solutions of the preparations Vitalang-1, Vitalang-2 and distilled water in an amount of 4.8 ml in each flask. They are incubated for 22 hours at room temperature. A spectrophotometer is used to measure optical density of the solutions versus distilled water with determining the RNA content in the pomelo cells and surrounding solution. Comparing the derived optical densities of the solutions provides stating the fact that Vitalang-2 penetrates through the biological membranes by 4.7-4.9 times more effectively than the preparation Vitalang-1. It is stated that absorption spectra of RNA recovered from the soft sacs are identical to those for the initial compounds.

EFFECT: invention enables assessing the efficacy of oleic acid used as the RNA carrier through the biological membranes.

1 ex

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