Fenbendazole encapsulation method

FIELD: chemistry.

SUBSTANCE: invention relates to encapsulation, particularly a method of producing fenbendazole microcapsules in a sodium carboxymethyl cellulose capsule. The method includes dissolving fenbendazole in dioxane or dimethyl sulphoxide or dimethyl formamide, adding the obtained fenbendazole solution to a solution of sodium carboxymethyl cellulose in tetrachloromethane in the presence of E472c while stirring at a rate of 1000 rps. Fenbendazole and sodium carboxymethyl cellulose are taken in weight ratio of 1:3. Methanol and distilled water, taken in ratio of 2:1 vol/vol, are then added. The obtained suspension of microcapsules is filtered and dried. The process is carried out at 25°C for 20 minutes.

EFFECT: invention simplifies and speeds up the process of producing microcapsules, reduces losses during production thereof (high mass output).

3 ex

 

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

Previously known methods for producing microcapsules of drugs. So, in us Pat. 2092155, IPC A61K 047/02, A61K 009/16, publ. 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 application of ultraviolet radiation, which can influence the formation of microcapsules.

In us Pat. 2091071, IPC A61K 35/10 Russian Federation, publ. 27.09.1997, a method of producing the drug by dispersing in a ball mill to obtain microcapsules.

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

In us Pat. 2101010, IPC A61K 9/52, A61K 9/50, A61K 9/22, A61K 9/20, A61K 31/19, Russian Federation, publ. 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 coating made�ing a copolymer based on methacrylic acid.

Disadvantages of the invention: use of a copolymer based on methacrylic acid, as these polymer coatings can cause cancer; the difficulty of execution; the duration of the process.

In us Pat. 2173140, IPC A61K 009/50, A61K 009/127, Russian Federation, publ. 10.09.2001, a method of producing kremnijorganicheskih microcapsules using a rotary cavitation equipment with high shear forces and powerful hydroacoustic phenomena sonic and ultrasonic range for dispersion.

The disadvantage of this method is the use of special equipment - rotary-cavitational installation, which has the ultrasonic effect, which influences the formation of the microcapsules and thus may cause adverse reactions due to the fact that ultrasound has a destructive effect on polymers of protein nature, therefore, the proposed method is applicable when working with polymers of synthetic origin.

In us Pat. 2359662, IPC A61K 009/56, A61J 003/07, B01J 013/02, A23L 001/00, publ. 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 Microcaps�crystals according to the invention have improved stability and provide adjustable and/or prolonged release of the active ingredient.

The disadvantages of the proposed method are the duration of the process and the use of special equipment, certain set of conditions (the air temperature at the inlet 10°C, the temperature at the outlet 28°C, the speed of rotation of the spray drum 10000 rpm).

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

The disadvantage is the dispersion in an aqueous medium, which makes the proposed method applicable for obtaining microcapsules of water-soluble drugs in water-soluble polymers.

The technical objective is the simplification and acceleration of the process of production of microcapsules, reducing loss upon receipt of the microcapsules (increase of the yield by weight).

The solution of a technical problem is achieved by a method of encapsulation of fenbendazol, characterized in that as the shell of the microcapsules used sodium carboxymethylcellulose when receiving physical-chemical method for the deposition nerastvorim using two precipitators - carbinol and carbon tetrachloride, the 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 fenbendazole as their nucleus, and the use of two precipitators - carbinol and carbon tetrachloride.

The result of the proposed method is to obtain microcapsules of fenbendazol in the sodium carboxymethyl cellulose at 25°C for 20 minutes. The output of the microcapsules is more than 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 is dispersed in a solution of sodium carboxymethyl cellulose in carbon tetrachloride containing the specified 300 mg of the polymer in the presence of 0.01 g of the drug E472c under stirring about 1000/sec. Next, pour 2 ml of carbinol and 1 ml of distilled water. The resulting suspension was filtered and dried at room temperature.

Received 0,396 g of a white to yellowish powder. The yield was 99%.

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 resulting mixture is dispersed in a solution of sodium carboxymethyl cellulose in carbon tetrachloride containing specified�wow 300 mg of the polymer in the presence of 0.01 g of the drug E472c under stirring about 1000/sec. Next, pour 2 ml of carbinol and 1 ml of distilled water. The resulting suspension was filtered and dried at room temperature.

Received 0,396 g of a white to yellowish powder. The yield was 99%.

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 is dispersed in a solution of sodium carboxymethyl cellulose in carbon tetrachloride containing the specified 300 mg of the polymer in the presence of 0.01 g of the drug E472c under stirring about 1000/sec. Next, pour 2 ml of carbinol and 1 ml of distilled water. The resulting suspension was filtered and dried at room temperature.

Received 0,396 g of a white to yellowish powder. The yield was 99%.

The obtained microcapsules of fenbendazol physico-chemical deposition method by nerastvorim using two precipitators - carbinol and carbon tetrachloride, 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.

Method of encapsula�AI of fenbendazole in a shell of sodium carboxymethylcellulose, characterized by the fact that fenbendazol dissolved in dioxane, or dimethylsulfoxide, or dimethylformamide, is added, the resulting solution of fenbendazole to a mixture of sodium carboxymethyl cellulose in carbon tetrachloride in the presence Es under stirring about 1000/sec, wherein the fenbendazole and sodium carboxymethylcellulose take in a weight ratio of 1:3, then add methanol and distilled water in the ratio 2:1 vol./about. accordingly, the resulting suspension of microcapsules is filtered off and dried, wherein the process of obtaining microcapsules is carried out at 25°C for 20 min.



 

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