Bioencapsulation method

FIELD: medicine.

SUBSTANCE: cephalosporine preparations are used as therapeutic preparations; a coating is poludan deposited from an aqueous solution by adding butanol and isopropanol as a non-solvent at 25°C.

EFFECT: simplifying and accelerating the process of water-soluble cephalosporin preparation microcapsules, reducing losses of preparing the microcapsules.

3 ex

 

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

Previously known methods for producing microcapsules. Thus, in U.S. Pat. 2092155, IPC A61K 047/02, A61K 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 A61K 9/52, A61K 9/16, A61K 9/10, Russian Federation, 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 temperatures from - 15 to - 50°C, and the separation of the obtained microspheres into fractions by size. The suspension is intended for administration by parenteral injection, contains an effective amount is in the above microspheres, 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 and the use of special equipment.

In Pat. 2091071, IPC A61K 35/10, Russian Federation, 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. 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 A61K 9/52, A61K 9/50, A61K 9/22, A61K 9/20, A61K 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 razmera-800 microns in diameter and consists of pharmaceutical kernel crystalline ibuprofen and polymer coating, including 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. 2139046, IPC A61K 9/50, A61K 49/00, A61K 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 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. 2359662,IPC A61K 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 at the outlet 28°C, the speed of rotation of the spray drum 10000 rpm/min 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/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.

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) is dispersed In water solution 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, the reduction of losses upon receipt of the microcapsules (increase in mass).

The solution of the technical problem is achieved by the method of bioencapsulation, characterized in that as the shell of the microcapsules is used Poludan, and obtaining microcapsules physico-chemical deposition method by nerastvorim using two precipitators - butanol and isopropanol, 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, poludana, and obtaining microcapsules physico-chemical deposition method by nerastvorim using two precipitators - butanol and isopropanol.

The result of the proposed method are obtaining microcapsules drugs group of cephalosporins, from asasasa to β-lactam antibiotics in Poludan at 25°C for 15 minutes. The output of the microcapsules is over 90%.

EXAMPLE 1. Obtaining microcapsules Cefotaxime in Poludan using butanol and isopropanol as the 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 Is 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 butanol as the first precipitator, and then 5 ml of isopropanol 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 0,087 g of white powder. The yield was 87%.

EXAMPLE 2. Obtaining microcapsules Ceftriaxone in Poludan using butanol and isopropanol as the 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 E472c 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 butanol as the first precipitator, and then 5 ml from ropanol - 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 0,088 g of white powder. The yield was 88%.

EXAMPLE 3. Obtaining microcapsules is anticipated in Poludan using butanol and isopropanol as the 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 Is 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 butanol as the first precipitator, and then 5 ml of isopropanol 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 0,086 g of white powder. The yield was 86%.

The obtained microcapsules drug group cephalos-Parinov related to β-lactam antibiotics, Poludan physico-chemical method for the deposition nerastvorim using butanol and isopropanol 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 β-lactam antibiotics, Poludan.

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 - Poludan, which is precipitated from aqueous solution by adding as herstories butanol and isopropanol at 25°C.



 

Same patents:

FIELD: chemistry.

SUBSTANCE: invention provides a method of producing pesticide microcapsules via a nonsolvent deposition method, characterised by that the active substances used are heterocyclic compounds of the triazine series and the envelope is polyvinyl alcohol, which is deposited from an aqueous solution by adding butanol and isopropanol at 25°C as the nonsolvent.

EFFECT: simple process of producing microcapsules of a preparation in water-soluble polymers, high mass output.

3 ex

FIELD: chemistry.

SUBSTANCE: invention provides a method of encapsulating a medicinal preparation via nonsolvent deposition, characterised by that the medicinal preparation used is fenbendazole, the envelope used is sodium carboxymethyl cellulose which is deposited from a solution in dichloromethane by adding, as the nonsolvent, isopropanol and water at 25°C.

EFFECT: simple and faster process of producing microcapsules, reduced losses when producing microcapsules.

3 ex

FIELD: chemistry.

SUBSTANCE: invention provides a method of encapsulating a medicinal preparation via nonsolvent deposition, characterised by that the medicinal preparation used is fenbendazole, the envelope used is sodium carboxymethyl cellulose which is deposited from a solution in tetrachloromethane by adding, as the nonsolvent, isopropanol and water at 25°C.

EFFECT: simple and faster process of producing microcapsules, reduced losses when producing microcapsules, high mass output.

3 ex

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

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

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to the field of pharmaceutics, in particular, to obtaining fenbendazole capsules. In realisation of a method simplification and acceleration of the process of obtaining microcapsules, reduction of loss in the process of obtaining microcapsules (increase of the output by weight) are ensured.

EFFECT: claimed method is characterised by application of sodium carboxymethylcellulose as an envelope of microcapsules, fenbendazole as their core, as well as application of two precipitants - butanol and dioxane.

3 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 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.

SUBSTANCE: invention relates to food, pharmaceutical and cosmetic industry, in particular deals with oil-in-water emulsion, containing disperse oil drops which have nano-size self-arranging structured internal contents, including: (i) oil, (ii) lipophilic additive (LPA), (iii) hydrophilic domains in form of drops or small canals, containing water or non-water polar liquid, and continuous water phase, which contains emulsion stabilisers or emulsifiers, in which oil drops with diametre from 5 nm to 900 mcm possess nano-size self-arranging structuring with formation of hydrophilic domains with diametre from 0.5 to 200 nm due to presence of lipophilic additive.

EFFECT: invention provides structures able to solubilise not only lipophilic but at the same time hydrophilic and/or amphiphilic, or hydrotropic, or crystalline components.

8 cl, 16 ex, 18 dwg

FIELD: industrial biotechnology; methods of production of the microcapsules.

SUBSTANCE: the invention is pertaining to the industrial biotechnology and is intended for production of the micro-capsulated biopreparations of the natural compounds. The purpose of the invention is development of the effective method of production of the microcapsules of the liquid-phase natural substances. The method is exercised by the emulsification of the encapsulated substance in the polymer solution and sedimentation of the polymer on the surface of the emulsion drips. The sedimentation(is conducted three times at the temperature of 75-80°C during 5-10 minutes at the continuous stirring with the subsequent treatment with the acetone In the capacity of the polymer solution use 1-2.5 % solution of methyl cellulose with the content of the metoxyl groups from 27.5 up to 32 %. In the capacity of the emulsifier use the rape oil in amount of 7.5-40 mass % from the amount of the polymer solution.

EFFECT: the invention ensures development of the effective method of production of the microcapsules of the liquid-phase natural substances.

4 cl, 4 ex

FIELD: chemistry.

SUBSTANCE: invention provides a method of producing pesticide microcapsules via a nonsolvent deposition method, characterised by that the active substances used are heterocyclic compounds of the triazine series and the envelope is polyvinyl alcohol, which is deposited from an aqueous solution by adding butanol and isopropanol at 25°C as the nonsolvent.

EFFECT: simple process of producing microcapsules of a preparation in water-soluble polymers, high mass output.

3 ex

FIELD: chemistry.

SUBSTANCE: invention provides a method of encapsulating a medicinal preparation via nonsolvent deposition, characterised by that the medicinal preparation used is fenbendazole, the envelope used is sodium carboxymethyl cellulose which is deposited from a solution in dichloromethane by adding, as the nonsolvent, isopropanol and water at 25°C.

EFFECT: simple and faster process of producing microcapsules, reduced losses when producing microcapsules.

3 ex

FIELD: chemistry.

SUBSTANCE: invention provides a method of encapsulating a medicinal preparation via nonsolvent deposition, characterised by that the medicinal preparation used is fenbendazole, the envelope used is sodium carboxymethyl cellulose which is deposited from a solution in tetrachloromethane by adding, as the nonsolvent, isopropanol and water at 25°C.

EFFECT: simple and faster process of producing microcapsules, reduced losses when producing microcapsules, high mass output.

3 ex

FIELD: medicine.

SUBSTANCE: what is described is hydrogel composition containing sodium acrylate, a linking agent, biologically active substances, polyvinyl pyrrolidone, glycerol, propanediol, water, a catalyst agent and a radical polymerisation indicator in the following proportions, wt %: sodium acrylate 2.0-10.0, catalyst agent 0.045-0.48, linking agent 0.195-0.21, radical polymerisation indicator 0.045-0.06, glycerol 4.5-7.5, propanediol 3.0-10.5, biologically active substances 0-1.5, polyvinyl pyrrolidone 0.3-1.5, water - the rest. What is described is a surgical dressing containing a carrier with the hydrogel composition applied thereon.

EFFECT: higher efficacy of the hydrogel composition and surgical dressing thereof, lower labour intensity of the method for preparing the above composition.

10 cl, 1 tbl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to pharmaceutical industry, in particular to method of obtaining microcapsules of medications of cephalosporin group. Method of obtaining microcapsules of medications of cephalosporin group consists in the following: surface-active substance is added to konjac solution in toluene, after that, powder of preparation of cephalosporin group is dissolved in dimethylformamide and transferred into solution of konjac in toluene, after formation by antibiotic of its own solid phase carbinol and distilled water are added in drops, obtained suspension of microcapsules is filtered, washed with acetone and dried, with process of obtaining microcapsules being carried out under specified conditions.

EFFECT: method ensures simplification and acceleration of the process of obtaining microcapsules of water-soluble medications.

8 ex

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

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

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to the field of pharmaceutics, in particular, to obtaining fenbendazole capsules. In realisation of a method simplification and acceleration of the process of obtaining microcapsules, reduction of loss in the process of obtaining microcapsules (increase of the output by weight) are ensured.

EFFECT: claimed method is characterised by application of sodium carboxymethylcellulose as an envelope of microcapsules, fenbendazole as their core, as well as application of two precipitants - butanol and dioxane.

3 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a method of modifying envelopes of polyelectrolyte capsules with magnetite nanoparticles. The disclosed method involves producing a container matrix in form of porous calcium carbonate microparticles, forming envelopes of polyelectrolyte capsules by successive adsorption of polyallyl amine and polystyrene sulphonate and modifying with magnetite nanoparticles on the surface of the container matrix or after dissolving the matrix through synthesis of magnetite nanoparticles via chemical condensation.

EFFECT: invention enables to obtain modified polyelectrolyte capsules, designed to deliver medicinal substances which do not harm the human body.

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.

SUBSTANCE: treating and/or preventing overweight and/or obesity related disorders, including type II diabetes mellitus are/is ensured by using a pharmaceutical composition containing metformin and its salts and sibutramine and its salts as ingredients in the following daily dose: sibutramine and its salts of 10 or 15 mg, metformin and its salts of 850 or 1700 mg, microcrystalline cellulose of 158.5 or 153.5 mg. There are also presented: usage and a method of treating and/or preventing the overweight and/or obesity related disorders.

EFFECT: group of inventions possess a synergetic effect, which manifests in the higher effect when used as the ingredients of the combination of metformin and sibutramine.

6 cl, 3 tbl, 1 ex

Up!