Method of obtaining microcapsules of medications of cephalosporin group in poludanum

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

 

The invention relates to the field of microencapsulation of drugs of cephalosporin group related to the (3-lactam antibiotics, Poludan physico-chemical method for the deposition aristotelem.

Previously known methods for producing microcapsules. Thus, in U.S. Pat. RF 2092155, IPC AC 047/02, AK 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. RF 2095055, IPC AC 9/52, AK 9/16, AC 9/10, published 10.11.1997, method for obtaining 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 a temperature of from -15 to -50°C and separation of the resulting microspheres into fractions by size. The suspension is intended for administration by parenteral injection, contains an effective amount of these microspheres distributed in pharmaceutics and 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 and the use of special equipment.

In Pat. RF 2091071, IPC AC 35/10, published 27.09.1997, method for obtaining the drug by dispersion in a ball mill to obtain microcapsules.

The disadvantage of this method is the use of a ball mill and the duration of the process.

In Pat. RF 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. RF 2101010, IPC AC 9/52, AK 9/50, AK 9/22, AK 9/20, AK 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 polymer coating, VK is causehe 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, as these polymer coatings can cause cancer; complexity; the duration of the process.

In Pat. RF 2139046, IPC AC 9/50, AK 49/00, AK 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.

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. RF 2159037, IPC A01N 25/28, A01N 25/30, published 20.11.2000,before ogen 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, 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 "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 soon the be 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-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 terephthaloylchloride. 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 indicates obtaining microcapsules or particles tank types. When otoplenie thus microcapsules are not damaged after 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, hence the low yield of the final products.

In Pat. RF 2173140, IPC AC 009/50, AK 009/127 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-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 Pat. RF 2359662, IPC AC 009/56, A61J 003/07, B01J 013/02, A23L 001/00 published 27.06.2009, 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 Rev/mi is. 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 10000 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, in which 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/2009/070011 NL, IPC AC 1/00; AC 1/16; A23L 1/30; A23L 1/48; B01J 13/04 was investigated, published 4.06.2009 described a method of producing microcapsules containing a hydrophobic core and is based coat proteins. Proposed particles are particularly well suited for food, feed, cosmetic and pharmaceutical industries. Method of producing microcapsules includes the following stages: a) preparation of a dispersion of hydrophobic material in a continuous aqueous phase containing the activated Assembly protein; b) providing an aqueous solution or suspension of the protein, which are capable of forming disulfide cross-links, C) representation of an aqueous solution or suspension for the treatment of protein, obtaining aqueous suspension of activated protein aggregates, specified suspension with the reactivity of at least 5.0 μmol thiol groups per gram protein; g) heated to temperatures above 40°C and pressures in excess of 50 MPa.

The disadvantage of the proposed method is a multistage process, which complicates the microencapsulation of hydrophobic cores in membrane protein-based.

In Pat. WO/2010/076360 ES, IPC B01J 13/00; AC 9/14; AC 9/10; AC 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 morphology is.

The disadvantage of the proposed method is the complexity of the process and, therefore, unstable yield of the target products.

In Pat. WO/2010/014011 NL, IPC AC 9/50; B01J 13/02; A61K 9/50; 01J 3/02, published 4.02.2010 described a method of producing microcapsules with a diameter of from 0.1 μm to 25 μm, comprising the core of the particle 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 copolymers based acrylic ester and/or methacrylic acid, ester, 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 Pat. WO/2010/119041 EP, IPC A23L 1/00, published 21.10.2010, method for obtaining the beads, aderrasi active component, 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 the 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 to 80°C., suitably within 30 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). As a rule, suspension of the filtration process is carried out through multiple filters with a gradual decrease in pore size. Ideally, the fine filter has a submicron pore sizes, for example from 0.1 to 0.9 μm. The preferred method according to the teachings of 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 this method of microcapsules filtering using multiple filters, which makes the process longer.

In .WO/2011/003 805 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. US 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 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 used in isawanya ultraviolet irradiation, which can lead to the destruction of the microcapsules.

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 and low yield of the target capsules.

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 Losert, Belgium)).

In Pat. WO/2011/104526 GB, IPC B01J 13/00; B01J 13/14; SV 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 per 100 parts of the solid product by weight; and b) crosslinking the polyurethane dispersant PR is the presence of solid and liquid media, so as to encapsulate solids 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; C11D 3/50, published 1105.2011 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, polyester, 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 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 dioxide, PU glue, which I and others

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 01J 13/16, published on 29.12.2011 described a method of producing microcapsules, which contain shell and kernel of 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), not soluble 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 Pat. WO/2011/161229 EP, IPC AC 8/11; B01J 13/14; B01J 13/16; C11D3/50, 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 are used protective colloids. During the reaction of isocyanates and amines should be protective colloid. This is preferably polyvinylpyrrolidone (PVP). Protection is hydrated 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 and powder detergents, personal care products and hair care, including shampoos, conditioners, styling cream, soap, body lotions, 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 AC 8/11; A61Q 13/00; B01J 13/16; 01J 13/18, published on 19.01.2012, describes how to obtain particles with an average diameter of less than 50 μm, 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 radical polymerization), 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 polim the polarization at the temperature, when a 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. RF 2134967, IPC A01N 53/00, A01N 25/28 published 27.08.1999. 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 Poludan, 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, the tives such as those that as the shell of the microcapsules is used Poludan, and obtaining microcapsules physico-chemical deposition method by nerastvorim using two precipitators - carbinol and isopropyl 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 p-lactam antibiotics, Poludan, and obtaining microcapsules physico-chemical deposition method by nerastvorim using two precipitators - carbinol and isopropyl alcohol.

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%.

EXAMPLE 1. Obtaining microcapsules Cefotaxime in Poludan using carbinol and isopropyl alcohol as a precipitating, the ratio of 3:1.

To 2 g of 1% aqueous poludana add to 0.060 g of powder Cefotaxime and 0.05 g of the drug A with as surfactants. The resulting mixture was put on a magnetic stirrer and include mixing. After the dissolution of the components of the reaction mixture formed to the I clear solution is slowly poured dropwise 1 ml of carbinol as the first precipitator, and then 5 ml of isopropyl alcohol as the second. 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 0,090 g of white powder. The yield was 90%.

EXAMPLE 2. Obtaining microcapsules Ceftriaxone in Poludan using carbinol and isopropyl alcohol as a precipitating, the ratio of 3:1.

To 2 g of 1% aqueous poludana add to 0.060 g of Ceftriaxone powder and 0.05 g of the drug A with as surfactants. The resulting mixture was put on a magnetic stirrer and include stirring.

After the dissolution of the components of the reaction mixture until a clear solution is formed very slowly poured dropwise 1 ml of carbinol as the first precipitator, and then 5 ml of isopropyl alcohol as the second. 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 0,095 g of white powder. The yield was 95%.

EXAMPLE 3. Obtaining microcapsules is anticipated in Poludan using carbinol and isopropyl alcohol as a precipitating, the ratio of 3:1.

To 2 g of 1% aqueous poludana add to 0.060 g of Cefazolin powder and 0.05 g of the drug A with as surfactants. According to the scientists put the mixture on a magnetic stirrer and include mixing. After the dissolution of the components of the reaction mixture until a clear solution is formed very slowly poured dropwise 1 ml of carbinol as the first precipitator, and then 5 ml of isopropyl alcohol as the second. 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 0,091 g of white powder. The yield was 91%.

EXAMPLE 4. Obtaining microcapsules of cefepime in Poludan using carbinol and isopropyl alcohol as a precipitating, the ratio of 3:1.

To 2 g of 1% aqueous poludana add to 0.060 g of cefepime powder and 0.05 g of the drug A with as surfactants. The resulting mixture was put on a magnetic stirrer and include mixing. After the dissolution of the components of the reaction mixture until a clear solution is formed very slowly poured dropwise 1 ml of carbinol as the first precipitator, and then 5 ml of isopropyl alcohol as the second. 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 0,096 g of white powder. The yield was 96%.

The obtained microcapsules drug group cephalosporins related to β-lactam antibiotics, in Poludan the physico-chemical method for the deposition nerastvorim using carbinol and isopropyl alcohol as nerastvorimaya. The process is simple to perform and lasts for 15 minutes, requires no special equipment.

Poludan - biosynthetic polyribonucleotides complex polyadenylate and prioritylevel acid (equimolar proportions). The inducer of the synthesis of endogenous interferon. Stimulates the formation of mainly alpha-interferon, to a lesser extent, β - and γ-interferons. Has a pronounced antiviral and immunomodulatory activity.

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 P-lactam antibiotics, Poludan.

The method of producing microcapsules drugs group of cephalosporins in Poludan, characterized by the fact that 2 g of 1% aqueous solution poludana added 0.06 g of a powder of a cephalosporin and 0.05 g of the drug E472c as a surfactant, the resulting mixture is stirred until complete dissolution of the components of the reaction mixture after formation of a clear solution is slowly poured dropwise 1 ml of carbinol as the first precipitator, and then 5 ml of isopropyl alcohol as the second precipitator obtained a suspension of microcapsules is filtered off, washed with acetone and dried in a desiccator, the entire process of gaining the microcapsules is carried out at a temperature of 25°C without special equipment.



 

Same patents:

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 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 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: 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 microcapsulation of cephalosporins related to β-lactam antibiotics. A method for preparing cephalosporin microcapsules is implemented by physicochemical non-solvent addition. That involves using two non-solvents that are carbinol and isopropyl alcohol taken in ratio 1:4. The microcapsule yield makes more than 90%.

EFFECT: method for cephalosporin microcapsules provides accelerating the process for preparing and simplifying the method.

3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to microcapsulation of drug preparations, vitamins, herbicides, flavouring agents and polysaccharides. The microcapsules are prepared by physical-chemical nonsolvent addition with using benzol as a precipitator.

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

48 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to microcapsulation of drug preparations of cephalosporins referred to β-lactam antibiotics in konjac gum by physical-chemical precipitation in a non-solvent. Konjac gum is used as a microcapsule membrane. The microcapsules are prepared by physical-chemical precipitation in the non-solvent with using two precipitation agents - carbinol and chloroform. The process of microcapsules is carried out at 25°C with no special equipment required.

EFFECT: method according to the invention provides simplifying and accelerating the process of microcapsules of drug preparations of cephalosporins, and reducing losses (higher weight yield).

4 ex

FIELD: chemistry.

SUBSTANCE: invention relates to microencapsulation, particularly microencapsulation of pesticides. The method consists in physical-chemical precipitation using two precipitants - butanol and ethanol. The microcapsule cladding is sodium carboxymethyl cellulose.

EFFECT: invention increases mass output of microcapsules while simplifying the process of producing microcapsules.

7 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to microencapsulation of drugs through the example of rivanol which can be used as an antimicrobial, antifungal topical preparation. A method for preparing microcaplues of rivanol in a water-soluble polymer representing polyvinyl alcohol or polyvinyl pyrrolidone is implemented by physical-chemical precipitation with a solvent wherein a precipitant is acetone. The process is carried out at 25°C with no special equipment required.

EFFECT: method for preparing the microcapsules of rivanol provides simplifying the process of microencapsulation.

13 dwg, 5 ex

FIELD: nanotechnology.

SUBSTANCE: device (50) for preparation of nanoparticles on a continuous basis comprises the first feeding device (1a) with the first feeding load (9) connected to the source (7) of the starting material, the first reactor (2) comprising the first heated reaction zone (13), the second reactor (3) comprising the second heated reaction zone (15), where all the said devices are connected to the channel of the material flow successively in the said order, at least one pressure control unit (18) mounted in the said channel of the material flow, a mixer (5) mounted in the said channel of the material flow between the first reactor (2) and the second reactor (3), the second feeding device (lb) with the second feeding pump (10) connected to the source (8) of the starting material, and the second feeding pump (10) is in liquid junction with the mixer (5), the control device (22) made with the ability to control the pressure value setting with the said pressure control unit (18) and/or the temperature value of the said heated reaction zones (13 and 15). The device is characterised in that after each heated reaction zone (13) in the channel of the material flow the appropriate cooling device (14, 16) is mounted for reducing the size of the nanoparticles in the process of their preparation, and the cooling devices (14, 16) are additionally made with the ability to cease this process of nanoparticles preparation. Also the invention relates to use of the device for preparation of nanoparticles/nanoemulsions/colloidal solutions.

EFFECT: invention enables to obtain nanoparticles which properties can be modified in the course of this process.

8 cl, 10 dwg

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: 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: invention refers to an implantable drug depot applicable for the release, prevention or treatment of a postoperative pain in a patient in need thereof; the implantable drug depot contains a therapeutically effective amount of clonidine or its pharmaceutically acceptable salt and polymer; the drug depot is implantable into percutaneously for the release, prevention or treatment of postoperative paints; the drug depot can release: 1) approximately 5% approximately to 45% of clonidine or its pharmaceutically acceptable salt to total clonidine or its pharmaceutically acceptable salt as a part of the depot for a first period making up to 48 hours; 2) approximately 55% approximately to 95% of clonidine or its pharmaceutically acceptable salt to total clonidine or its pharmaceutically acceptable salt as a part of the depot for the following period making at least 3 days.

EFFECT: implantable form enables the easy accurate implantation of the drug depot with minimum physical and psychological traumas of the patient.

15 cl, 2 tbl, 20 dwg, 6 ex

Up!