RU2559571C1 - Method to produce albendazole nanocapsules - Google Patents

Abstract

FIELD: nanotechnologies.

SUBSTANCE: invention describes the method of production of albendazole nanocapsules by method of deposition with a non-dissolvent, where albendazole is added in small portions into a suspension of carrageenan, used as a shell of nanocapsules, in butanol in presence of 0.01 g of preparation E472c and during mixing at 1000 rotations/seconds, then the precipitator is added - butyl chloride, filtered and dried at room temperature.

EFFECT: simplified and accelerated process of nanocapsule production and increased yield by mass.

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Description

The invention relates to the field of nanotechnology and veterinary medicine, in particular the production of albendazole nanocapsules.

Previously known methods for producing microcapsules of drugs. So, in the patent of the Russian Federation 2092155, IPC A61K 047/02, A61K 009/16, publ. 10.10.1997, a method of microencapsulation of drugs based on the use of ultraviolet radiation is proposed.

The disadvantages of this method are the duration of the process and the use of ultraviolet radiation, which can affect the process of formation of microcapsules.

In the patent of the Russian Federation 2091071, IPC A61K 35/10, publ. 09/27/1997, a method for producing the drug by dispersion in a ball mill with the receipt of microcapsules is proposed.

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

In the patent of the Russian Federation 2101010, IPC A61K 9/52, A61K 9/50, A61K 9/22, A61K 9/20, A61K 31/19, publ. 01/10/1998 a chewing mask of a taste-masked drug with the properties of controlled release of the drug is proposed that contains microcapsules 100-800 μm in diameter and consists of a pharmaceutical core with crystalline ibuprofen and a polymer coating that includes a plasticizer that is flexible enough to withstand chewing. The polymer coating is a methacrylic acid based copolymer.

The disadvantages of the invention: the use of a copolymer based on methacrylic acid, as these polymer coatings can cause cancerous tumors; complexity of execution; the duration of the process.

In the patent of the Russian Federation 2173140, IPC A61K 009/50, A61K 009/127, publ. 09/10/2001 a method for producing silicon organolipid microcapsules using a rotary-cavitation unit with high shear forces and powerful sonar effects of sound and ultrasonic range for dispersion is proposed.

The disadvantage of this method is the use of special equipment - a rotary cavitation unit, which has an ultrasonic effect, which affects the formation of microcapsules and can cause adverse reactions due to the fact that ultrasound destructively affects polymers of a protein nature, therefore, the proposed method is applicable when work with polymers of synthetic origin.

In the patent of the Russian Federation 2359662, IPC A61K 009/56, A61J 003/07, B01J 013/02, A23L 001/00, publ. 06/27/2009, a method for producing microcapsules using spray cooling in a Niro spray tower is proposed under the following conditions: inlet air temperature 10 ° C, outlet air temperature 28 ° C, spray drum rotation speed of 10,000 rpm. The microcapsules of the invention have improved stability and provide controlled 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, a set of certain conditions (air temperature at the inlet 10 ° C, air temperature at the outlet 28 ° C, rotation speed of the spray drum 10,000 rpm).

The closest method is the method proposed in the patent of the Russian Federation 2134967, IPC A01N 53/00, A01N 25/28 published on 08.27.1999, Russian Federation (1999). A solution of a mixture of natural lipids and a pyrethroid insecticide in a weight ratio of 2-4: 1 in an organic solvent is dispersed in water, which simplifies the microencapsulation method.

The disadvantage of this method is dispersion in an aqueous medium, which makes the proposed method inapplicable for producing microcapsules of water-soluble preparations in water-soluble polymers.

The technical task is to simplify and accelerate the process of obtaining nanocapsules, reduce losses in obtaining nanocapsules (increase in yield by mass).

The solution of the technical problem is achieved by the method of producing albendazole nanocapsules, characterized in that carrageenan is used as the nanocapsule shell when they are obtained by the physicochemical method of precipitation with a non-solvent using a precipitant - butyl chloride, the production process is carried out without special equipment.

A distinctive feature of the proposed method is the use of carrageenan as a shell of nanocapsules, albendazole as their core, as well as the use of a precipitant, butyl chloride.

The result of the proposed method is the preparation of albendazole nanocapsules in carrageenan at 25 ° C for 20 minutes. The yield of nanocapsules is more than 90%.

EXAMPLE 1

Obtaining nanocapsules of albendazole, the ratio of core / polymer 1: 3

1 g of albendazole is added in small portions to a suspension of carrageenan in butanol containing 3 g of carrageenan in the presence of 0.01 g of the preparation E472c (glycerol ester with one or two molecules of food fatty acids and one or two molecules of citric acid, with citric acid as a tribasic be esterified with other glycerides and like oxoacid with other fatty acids, free acid groups can be neutralized with sodium), with stirring 1000 rpm. Next, 6 ml of butyl chloride are added. The resulting suspension is filtered and dried at room temperature.

Received 4 g of a white powder. The yield was 100%.

EXAMPLE 2

Obtaining nanocapsules of albendazole, the ratio of core / polymer 3: 1

3 g of albendazole is added in small portions to a suspension of carrageenan in butanol containing 1 g of carrageenan in the presence of 0.01 g of the preparation E472c, with stirring 1000 r / sec. Then 10 ml of butyl chloride are added. The resulting suspension is filtered and dried at room temperature.

Received 4 g of a white powder. The yield was 100%.

EXAMPLE 3

Obtaining nanocapsules of albendazole, the ratio of core / polymer 20: 1

10 g of albendazole are added in small portions to a suspension of carrageenan in butanol containing 0.5 g of carrageenan in the presence of 0.01 g of the preparation E472c, with stirring 1000 r / sec. Then pour 25 ml of butyl chloride. The resulting suspension is filtered and dried at room temperature.

Received 10.5 g of a white powder. The yield was 100%.

Albendazole nanocapsules were obtained by the physicochemical method of non-solvent precipitation using a precipitant, butyl chloride, which helps to increase the yield and accelerates the process of nanocapsulation. The process is simple to execute and lasts for 20 minutes, does not require special equipment.

The proposed technique is suitable for the veterinary industry due to minimal losses, speed, ease of preparation and isolation of nanocapsules.

Claims (1)

A method for producing albendazole nanocapsules by non-solvent precipitation, characterized in that albendazole is added in small portions to a suspension of carrageenan, which is used as a shell of nanocapsules, in butanol in the presence of 0.01 g of the preparation E472c and with stirring 1000 rps, then the butyl chloride precipitator is added, filtered and dried at room temperature.