Method for preparing drug microcapsules of cephalosporin in konjak gum in carbon tetrachloride

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

 

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. 2092155, IPC A61K 047/02, A61K 009/16 published. 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. 2095055, IPC A61K 9/52, A61K 9/16, A61K 9/10 published. 10.11.1997, method for obtaining solid non-porous microspheres includes 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 of these microspheres, raspredelennyh 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 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 A61K 9/52, A61K 9/50, A61K 9/22, A61K 9/20, A61K 31/19, 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 based on methacrylic acid.

The drawbacks of the invention: use of a copolymer based on methacrylic acid, to the data to the polymer coating can cause cancer; the complexity of the execution; the duration of the process.

In Pat. 2139046, IPC A61K 9/50, A61K 49/00, A61K 51/00 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 a surfactant, it is possible to 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.

Nedostatkami predlozennogo 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 solid agrochemical material 0.1 to 55 wt.%, suspended in peremestivsheesya water organic liquid, from 0.01 to 10 wt.% non-ionic dispersant, is active on the interface and not the de is concerned as the 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 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 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). The resulting poly-pccillin 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 an active center was microcapsular in his introduction to the composition of the aqueous phase. Tapered shape liofilizovannyh particles svidetelstvovat about 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 crucial in obtaining durable mi is roopal with high output.

The disadvantage of the proposed method of producing microcapsules is the complexity of the process, and hence the unpredictability of the output of the target capsules.

In Pat. 2173140, IPC A61K 009/50, A61K 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 A61K 009/56, A61J 003/07, B01J 013/02, A23L 001/00 published. 27.06.2009, the 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 at the outlet 28°C, the speed of rotation of the spray drum 10000 rpm/min Microcapsules according to the invention have improved a hundred what Iliescu 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 10000 rpm).

In Pat. WO/2010/076360, ES, IPC B01J 13/00; A61K 9/14; A61K 9/10; A61K 9/12, published. 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. 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 any the hydrated polysaccharide with a pH of 4.6 and below for a period of not less than 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, 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, the suspension is subject to the filtering process 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)), occurred microcapsules by denaturation of the protein, the complexity of the allocation obtained by way microca the Sul - filtering, using a number of filters that makes the process longer.

In Pat. WO/2011/003805 EP, IPC B01J 13/18; B65D 83/14; C08G 18/00 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 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, published. 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 A61K 8/11; B01J 2/00; B01J 13/06; C11D 3/37; C11D 3/39; C11D 17/00, published. 13.10.2011 proposed NESCO what are ways to obtain microcapsules: interfacial polymerization, thermointelligence 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; SV 67/00; C09D 11/02 published. 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 per 100 parts of solid product, by weight; and b) crosslinking the polyurethane dispersant in the presence of solid and liquid medium, so as to encapsulate the 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; A61K 8/11; B01J 13/02; C11D 3/50, published. 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 proposed polymer membranes are sufficiently impervious core material and materials in the environment in which the encapsulated benefit 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, 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 Pat. WO/2011/160733 EP, IPC B01J 13/16 published. 29.12.2011 described a method of producing microcapsules, which contain shell and core water-insoluble materials. An aqueous solution of protective stake is Aida and solution mixture of at least two structurally different bifunctional diisocyanate (a) and (b) insoluble in water together before formation of the emulsion, 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 A61K 8/11; B01J 13/14; B01J 13/16; C11D 3/50, published. 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 are used protective colloids. During the reaction of isocyanates and amines, should be protective colloid. This is preferably polyvinylpyrrolidone (PVP). Protective colloid - polymer system, which 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 and powdered detergents; personal care and hair care products, including shampoos, conditioners, styling cream, soap, body creams, etc.; de the odorants and deodorants.

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. 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 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, and obtaining microcapsules physico-chemical deposition method of nerist what realem using two precipitators - carbinol and carbon tetrachloride, 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 carbon tetrachloride.

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 cercon and konjac gum 3600.

EXAMPLE 1 Obtaining microcapsules Ceftriaxone in the konjak cerocon using carbinol and carbon tetrachloride as the precipitating with the dissolution of the drug in ethanol, the ratio of 1:3

To 6 g of 5% solution of konjac cerocon in carbon tetrachloride 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 Ceftriaxone powder dissolved in 0, ml ethanol and transferred into a solution of konjac cerocon in carbon tetrachloride. 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.

Obtained 0.35 g of a white powder. The yield was 88%.

EXAMPLE 2 Obtaining microcapsules Ceftriaxone in the konjak cerocon using carbinol and carbon tetrachloride as the precipitating, the ratio of 1:3

To 6 g of 5% solution of konjac cerocon in carbon tetrachloride 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 water and transferred into a solution of konjac cerocon in carbon tetrachloride. 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 0.39 g of white powder. The yield was 98%.

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

To 6 g of 5% solution of konjac gum 3600 in carbon tetrachloride 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 Ceftriaxone powder dissolved in 0.5 ml of water and transferred into a solution of konjac gum 3600 in carbon tetrachloride. 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 0,384 g of white powder. The yield was 96%.

EXAMPLE 4 Obtaining microcapsules Cefotaxime in konjak cerocon using carbinol and carbon tetrachloride as the precipitating, the ratio of 1:3

To 6 g of 5% solution of konjac cerocon in carbon tetrachloride 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 the powder Cefotaxime dissolved in 0.5 ml of water and transferred into a solution of konjac cerocon in carbon tetrachloride. 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.

Obtained 0.34 g of a white powder is. The yield was 89%.

EXAMPLE 5 Obtaining microcapsules is anticipated in the konjak cerocon using carbinol and carbon tetrachloride as the precipitating, the ratio of 1:3

To 6 g of 5% solution of konjac cerocon in carbon tetrachloride 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 carbon tetrachloride. 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%.

EXAMPLE 6 Obtaining microcapsules of cefepime in the konjak cerocon using carbinol and carbon tetrachloride as the precipitating, the ratio of 1:3

To 6 g of 5% solution of konjac cerocon in carbon tetrachloride 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 cefepime powder dissolved in 0.5 ml of water and transferred into a solution of konjac cerocon in carbon tetrachloride. After the formation of the cefepime with the 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%.

EXAMPLE 7 to Obtain microcapsules of cefepime in konjac gum 3600 using carbinol and carbon tetrachloride as the precipitating, the ratio of 1:3

To 6 g of 5% solution of konjac gum 3600 in carbon tetrachloride 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 cefepime powder dissolved in 0.5 ml of water and transferred into a solution of konjac gum 3600 in carbon tetrachloride. 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.

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

The obtained microcapsules drug group cephalosporins related to β-lactam antibiotics, in Konakovo gum physico-chemical method for the deposition nerastvorim using carbinol and carbon tetrachloride as nerastvorimaya. The process is simple in execution, dots is within 15 minutes no special equipment is required.

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)Tehnologicheskie 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.

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 in Konakovo gum in carbon tetrachloride, characterized in that as the shell of the microcapsules used Konakovo gum, with 6 g of a 5%solution of konjac gum 3600 in carbon tetrachloride added 0.01 g of the drug A with as a surfactant, and 0.1 g of powder antibiotic of cephalosporin group dissolved in 0.5 ml water or ethanol, and transfer it into a solution of konjac gum 3600 in carbon tetrachloride, after the formation of the antibiotic samostojatel the Noah solid phase very slowly added dropwise 5 ml of carbinol and 1 ml distilled water; the resulting suspension of microcapsules is filtered off, washed with acetone and dried, the process of production of microcapsules is carried out at a temperature of 25°C no special equipment.



 

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22 cl, 14 ex, 1 tbl

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: invention refers to chemical-pharmaceutical industry, and represents a method for preparing medicine microcapsules by non-solvent addition differing by the fact that the medical preparations are presented by the cephalosporin preparations, while a coating is polyvinyl alcohol that is precipitated by the addition of non-solvents that are carbinol and acetone at -25°C.

EFFECT: invention provides simplifying and accelerating the process for preparing the water-soluble cephalosporin microcapsules in polyvinyl alcohol, providing loss reduction in preparing the microcapsules (higher yield-mass).

16 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry, namely to a microcapsules for preventing or treating hepatic disorders. The microcapsules for preventing or treating hepatic disorders containing a capsule coating, an encapsulating suspension of a therapeutically effective hepatocyte count in a physical contact with a hepatocyte-stimulating amount of erythropoietin. A method for preparing microcapsules involving preparing the suspension of the therapeutically effective hepatocyte count and the hepatocyte-stimulating amount of erythropoietin to bring them in physical contact with each other, and encapsulating the suspension of hepatocytes and erythropoietin in a biologically compatible capsule shell so that to form a microcapsule. A method for preventing or treating a hepatic disorder in an individual in need thereof involving administering the microcapsules in the individual in need thereof. The method for introducing the hepatocytes in the individual involving administering the microcapsules in the individual. A method for hepatocyte culture in a culture medium involving hepatocyte culture in the microcapsules in the appropriate culture medium.

EFFECT: microcapsules are effective for preventing or treating the hepatic disorders.

20 cl, 1 dwg, 1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions refers to capsule suspensions prepared by coacervation, and to methods for reducing leakage of the capsule content in such suspensions during storage. Substance of the method for reducing leakage of the capsule content consists in storage of the capsules prepared by coacervation, in the capsule suspension containing min. 20 wt %, a moisturiser, which is at least a moisturiser specified in sorbitol, glycerol, polyethylene glycol, propylene glycol, xylitol, erythritol or betaine. What is also presented is the above capsule suspension containing at least one capsule prepared by coacervation and at least 20 wt % of the above moisturiser.

EFFECT: using the above moisturiser in the amount of min 20 wt % provides reducing the leakage rate of the capsule content.

21 cl, 4 tbl, 2 ex, 2 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to iron-enriched food product, which contains iron source in form of solid particles, where particles include core, containing iron alginate, and external layer, which contains calcium alginate, where particles are obtained by method which includes the following stages: (i) formation of core, which contains iron alginate, by contact of bioavailable water-soluble salt of iron and one water-soluble alginate salt, (ii) contact of core with water solution of calcium salt, in concentration, which constitutes from 0.025 M to concentration of lower than solution saturation point, and (iii) separation of obtained solid product. Iron-enriched food product is applied for prevention and treatment of iron deficiency conditions of people.

EFFECT: solid particles are applicable for enrichment of food products with iron and is characterised by improved load ability, as well as possesses good stability under standard storage and application conditions.

11 cl, 9 dwg, 13 tbl, 16 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine and pharmaceutical industry, particularly to creating a pharmaceutical composition of a submicron emulsion for parenteral administration, having anticonvulsant activity. The composition contains 5-carbamoyl-5H-dibenz-(b,f)-azepine, and additionally it contains soya been oil and sodium deoxycholate in the following proportions, wt %: 5-carbamoyl-5H-dibenz-(b,f)-azepine - 18.5-23.2, soya been oil - 2.1-2.3, sodium deoxycholate - 74.5-79.4. The composition has an average size of the deagglomerated microparticles of 108-132 nm.

EFFECT: composition enables the intravenous intraperitoneal administration of a low therapeutic dose with a high efficacy of the preparation, and reduction of dose-dependent adverse reactions, and extends the range of such preparations.

4 ex, 3 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to chemical-pharmaceutical industry and represents microspheres for treating schizophrenia, having a nucleus/coating structure and a spherical shape wherein the nucleus contains ariliprazol in the solid state, and the coating covers the entire surface or most of the nucleus and contains a biodegradable polymer.

EFFECT: invention provides producing the microspheres of ariliprazol characterised by the high content and sustained release of the active substance, and preparing an injectable aqueous suspension of the above microspheres.

17 cl, 18 ex, 14 dwg

FIELD: nanotechnology.

SUBSTANCE: invention relates to the use of nanoparticles for prevention and/or treatment of cancerous diseases, when the nanoparticles are injected with anti-cancer therapeutic agent, and the nanoparticles and anti-cancer agent are simultaneously present in the patient's body. The nanoparticles are free from binding with the anti-cancer medicinal product and have a coating which contains polycondensated aminosilanes.

EFFECT: simultaneous presence of nanoparticles and the anti-cancer therapeutic agent in the body of patients enables to increase the activity of the said anti-cancer agent with simultaneous reduction of the side effects.

12 cl, 1 tbl, 13 dwg, 196 ex

FIELD: medicine.

SUBSTANCE: group of inventions refers to medicine. A biocidal capsule for treating and diagnosing in vagina to be used in the biocidal preparation wherein at least one active ingredient is encapsulated with a wall insoluble or minimally soluble in an aqueous environment within the pH range lower than a threshold pH value, but soluble within the pH range higher than a threshold pH value wherein the threshold pH value is found between 4.6 to 6.0 and at least one of the walls and the content contains a tracer substance suitable for colour-coded indication. A tampon contains the biocidal preparation which in case of a vaginal tampon comprises a hygroscopic cylinder (1) preferentially swelling in a cross section under action of fluid, having a longer back flange (2) on an inner end inserted to a posterior vaginal vault, and a peritoneal flange (3) shorter than the back flange; and in between, there is a saddle (4) receiving a vaginal portion of neck of uterus.

EFFECT: invention provides using the preparation for medical and hygienic purposes, preferentially for elimination of pathogens of body surface, body openings, open and closed body cavities.

13 cl, 1 dwg, 1 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

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