Method of fenbendazole encapsulation

FIELD: chemistry.

SUBSTANCE: invention represents method of encapsulating medication by method of sedimentation with non-solvent, characterised by the fact that as medication used is fenbendazole, as coating - sodium carboxymethylcellulose, which is precipitated from solution in acetone by addition of water as non-solvent at 25C.

EFFECT: simplification and acceleration of the process of obtaining microcapsules, reduced loss in obtaining microcapsules.

3 ex

 

The invention relates to the field of encapsulation, in particular the production of microcapsules of fenbendazol.

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, Russian Federation, proposed a method for microencapsulation of drugs, based on the 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. 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. 2101010 IPC A61K 9/52, A61K 9/50, A62K 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 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. Polymer on which the freight 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. 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, 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 10C, the temperature at the outlet 28C, the speed of rotation of the spray drum 10000 rpm. who/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 10C, the temperature at the outlet 28C, the speed of rotation of the spray drum 10000 rpm).

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

The disadvantage of this method is the dispersion in the aquatic environment, which makes the proposed method applicable to the production of microcapsules of water-soluble drugs in water-soluble polymers.

The technical objective is the simplification and acceleration of the process of production of microcapsules, the reduction of losses upon receipt of the microcapsules (increase in mass).

The solution of the technical problem is achieved by the method of encapsulation of fenbendazol, characterized in that as the shell of the microcapsules used sodium carboxymethylcellulose when receiving physical-hee is a practical method of deposition nerastvorim using acetone as a precipitator, the retrieval process is carried out without special equipment.

A distinctive feature of the proposed method is the use of sodium carboxymethylcellulose as the shell of the microcapsules of fenbendazol as their cores, and the use of acetone as a precipitator.

The result of the proposed method are obtaining microcapsules of fenbendazol in the sodium carboxymethyl cellulose at 25C for 20 minutes. The output of the microcapsules is over 90%.

EXAMPLE 1 Obtaining microcapsules of fenbendazol with the dissolution of the drug in dioxane, the ratio of the core/polymer 1:3

100 mg of fenbendazol dissolved in 1 ml of dioxane and the resulting mixture was dispersed in a solution of sodium carboxymethyl cellulose in acetone, containing the specified 300 mg of the polymer in the presence of 0.01 drug E472c under stirring about 1000/sec. Then poured 1 ml of distilled water. The resulting suspension is filtered and dried at room temperature.

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

EXAMPLE 2 Obtaining microcapsules of fenbendazol with the dissolution of the drug in dimethyl sulfoxide (DMSO), the ratio of the core/polymer 1:3

100 mg of fenbendazol dissolved in 1 ml DMSO and the mixture was dispersed in a solution of sodium carboxymethyl cellulose in acetone, containing the specified 300 mg polymer clay is in the presence of 0.01 drug E472c under stirring about 1000/sec. Then poured 1 ml of distilled water. The resulting suspension is filtered and dried at room temperature.

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

EXAMPLE 3 Obtaining microcapsules of fenbendazol with the dissolution of the drug in dimethylformamide (DMF), the ratio of the core/polymer 1:3

100 mg of fenbendazol dissolved in 1 ml DMF and the resulting mixture was dispersed in a solution of sodium carboxymethyl cellulose in acetone, containing the specified 300 mg of the polymer in the presence of 0.01 drug E472c under stirring about 1000/sec. Then poured 1 ml of distilled water. The resulting suspension is filtered and dried at room temperature.

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

The obtained microcapsules of fenbendazol physico-chemical method for the deposition nerastvorim using acetone as a precipitator, which increases output and accelerates the process of microencapsulation. The process is simple to perform and lasts for 20 minutes, requires no special equipment.

The proposed method is suitable for the veterinary industry due to the minimal loss of speed, ease of acquisition and allocation of microcapsules.

The method of encapsulation of a medicinal product by precipitation with nerastvorim different is eat, as drug use fenbendazol, as the shell - sodium carboxymethylcellulose, which is precipitated from a solution in acetone by adding as nerastvorim water at 25C.



 

Same patents:

FIELD: chemistry.

SUBSTANCE: invention represents method of encapsulating medication by method of sedimentation with non-solvent, characterised by the fact that as medication used is fenbendazole, as coating - sodium carboxymethylcellulose, which is precipitated from solution in acetone by addition of isopropanol as non-solvent and water at 25C.

EFFECT: simplification and acceleration of the process of obtaining microcapsules, reduced loss in obtaining microcapsules.

3 ex

FIELD: chemistry.

SUBSTANCE: as medical preparation applied is fenbendazole, as envelope- sodium carboxymethylcellulose, which is precipitated from solution in dichloromethane by addition as non-solvent butanol and water at 25C.

EFFECT: simplification and acceleration of the process obtaining microcapsules, reduction of loss in the process of obtaining microcapsules.

3 ex

FIELD: chemistry.

SUBSTANCE: invention relates to the field of encapsulation and represents a method of obtaining microcapsules, possessing supramolecular properties, by a method of precipitation with a non-solvent, in accordance to which a flavouring agent "paprika", used as a nucleus of the microcapsules, is dissolved in butanol, with further dispersion of the obtained mixture in a solution of a fat-soluble polymer, used as a microcapsule envelope, in isopropanol in the presence of E472c.

EFFECT: invention provides simplification and acceleration of the process of obtaining the microcapsules, reduction of loss in the process of obtaining the microcapsules (increase of the output by weight).

2 ex, 1 dwg

FIELD: food industry.

SUBSTANCE: invention relates to the field of flavouring agents microencapsulation and represents a method for production of microcapsules having supramolecular properties by way of sedimentation with a nonsolvent; the method is as follows: "coffee" flavouring agent used as microcapsules core is dissolved in ethanol; then the produced mixture is dispersed in a suspension of sodium-carboxymethyl cellulose, used as microcapsule shell, in acetone in the presence of E472c.

EFFECT: invention ensures simplification and acceleration of the process of microcapsules production and weight yield increase.

2 ex, 2 dwg

FIELD: chemistry.

SUBSTANCE: as medical preparation applied is fenbendazole, as envelope - sodium carboxymethylcellulose, which is precipitated from chloroform solution by addition as non-solvent of methylcarbinol and water at 25C.

EFFECT: simplification and acceleration of process of obtaining microcapsules, reduction of loss in the process of obtaining microcapsules.

3 ex

FIELD: chemistry.

SUBSTANCE: as medication used is fenbendazole, as envelope used is sodium carboxymethylcellulose, precipitated from solution in diethyl ether by addition as non-solvent butanol and water at 25C.

EFFECT: simplification and acceleration of process of obtaining microcapsules, reduction of loss in the process of obtaining microcapsules.

3 ex

FIELD: chemistry.

SUBSTANCE: fenbendazole is used as medication, and sodium carboxymethylcellulose, precipitated from solution in heptanes by addition as non-solvent of butanol and water at 25C, is used as envelope.

EFFECT: simplification and acceleration of process of microcapsule obtaining, reduction of loss in the process of obtaining microcapsules.

3 ex

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 25C.

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

3 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 25C 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 25C.

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

3 ex

FIELD: chemistry.

SUBSTANCE: invention represents method of encapsulating medication by method of sedimentation with non-solvent, characterised by the fact that as medication used is fenbendazole, as coating - sodium carboxymethylcellulose, which is precipitated from solution in acetone by addition of isopropanol as non-solvent and water at 25C.

EFFECT: simplification and acceleration of the process of obtaining microcapsules, reduced loss in obtaining microcapsules.

3 ex

FIELD: chemistry.

SUBSTANCE: fenbendazole solution is dispersed in a solution of sodium carboxymethyl cellulose in ethyl acetate containing an E472c preparation, with ratio of fenbendazole to sodium carboxymethyl cellulose of 1:3, followed by addition of butanol and distilled water, filtering the obtained suspension of microcapsules and drying at room temperature.

EFFECT: simple and faster process of producing fenbendazole microcapsules and high mass output.

3 ex

FIELD: chemistry.

SUBSTANCE: as medical preparation applied is fenbendazole, as envelope- sodium carboxymethylcellulose, which is precipitated from solution in dichloromethane by addition as non-solvent butanol and water at 25C.

EFFECT: simplification and acceleration of the process obtaining microcapsules, reduction of loss in the process of obtaining microcapsules.

3 ex

FIELD: chemistry.

SUBSTANCE: invention relates to the field of encapsulation and represents a method of obtaining microcapsules, possessing supramolecular properties, by a method of precipitation with a non-solvent, in accordance to which a flavouring agent "paprika", used as a nucleus of the microcapsules, is dissolved in butanol, with further dispersion of the obtained mixture in a solution of a fat-soluble polymer, used as a microcapsule envelope, in isopropanol in the presence of E472c.

EFFECT: invention provides simplification and acceleration of the process of obtaining the microcapsules, reduction of loss in the process of obtaining the microcapsules (increase of the output by weight).

2 ex, 1 dwg

FIELD: food industry.

SUBSTANCE: invention relates to the field of flavouring agents microencapsulation and represents a method for production of microcapsules having supramolecular properties by way of sedimentation with a nonsolvent; the method is as follows: "coffee" flavouring agent used as microcapsules core is dissolved in ethanol; then the produced mixture is dispersed in a suspension of sodium-carboxymethyl cellulose, used as microcapsule shell, in acetone in the presence of E472c.

EFFECT: invention ensures simplification and acceleration of the process of microcapsules production and weight yield increase.

2 ex, 2 dwg

FIELD: chemistry.

SUBSTANCE: as medical preparation applied is fenbendazole, as envelope - sodium carboxymethylcellulose, which is precipitated from chloroform solution by addition as non-solvent of methylcarbinol and water at 25C.

EFFECT: simplification and acceleration of process of obtaining microcapsules, reduction of loss in the process of obtaining microcapsules.

3 ex

FIELD: chemistry.

SUBSTANCE: as medication used is fenbendazole, as envelope used is sodium carboxymethylcellulose, precipitated from solution in diethyl ether by addition as non-solvent butanol and water at 25C.

EFFECT: simplification and acceleration of process of obtaining microcapsules, reduction of loss in the process of obtaining microcapsules.

3 ex

FIELD: chemistry.

SUBSTANCE: fenbendazole is used as medication, and sodium carboxymethylcellulose, precipitated from solution in heptanes by addition as non-solvent of butanol and water at 25C, is used as envelope.

EFFECT: simplification and acceleration of process of microcapsule obtaining, reduction of loss in the process of obtaining microcapsules.

3 ex

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 25C.

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

3 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 25C 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 represents method of encapsulating medication by method of sedimentation with non-solvent, characterised by the fact that as medication used is fenbendazole, as coating - sodium carboxymethylcellulose, which is precipitated from solution in acetone by addition of isopropanol as non-solvent and water at 25C.

EFFECT: simplification and acceleration of the process of obtaining microcapsules, reduced loss in obtaining microcapsules.

3 ex

Up!