RU2558084C1 - Method of producing aspirin nanocapsules in carrageenan - Google Patents

Abstract

FIELD: chemistry.

SUBSTANCE: invention relates to nanotechnology, particularly a method of producing aspirin nanocapsules in a carrageenan envelope. The disclosed method includes preparing an aspirin suspension in benzene; dispersing the obtained mixture into a carrageenan suspension in butanol in the presence of an E472c preparation while mixing at 1000 rps; adding tetrachloromethane; filtering the obtained nanocapsule suspension and drying at room temperature.

EFFECT: method provides a simpler and faster process of producing nanocapsules and increases mass output.

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Description

The invention relates to the field of nanotechnology, in particular to a method for producing aspirin nanocapsules in carrageenan.

Previously known methods for producing microcapsules.

In US Pat. RF 2173140, IPC A61K 009/50, A61K 009/127, published September 10, 2001, a method for producing silicon organolipid microcapsules using a rotary-cavitation unit with high shear forces and powerful sonar acoustic 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 US Pat. RF 2359662, IPC A61K 009/56, A61J 003/07, B01J 013/02, A23L 001/00, published 06/27/2009, a method for producing sodium chloride microcapsules using spray cooling in a Niro spray cooling tower under the following conditions: air temperature inlet 10 ° C; outlet air temperature 28 ° C; spray drum rotation speed 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 US Pat. RF 2134967, IPC A01N 53/00, A01N 25/28, published on 08.27.1999. 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 nanocapsules, characterized in that carrageenan is used as the shell of the nanocapsules, and aspirin is used as the nucleus for the production of encapsulated particles by non-solvent deposition using carbon tetrachloride as a precipitant; the process of producing nanocapsules is carried out without special equipment.

A distinctive feature of the proposed method is the preparation of nanocapsules by non-solvent precipitation using carbon tetrachloride as a precipitant, as well as the use of carrageenan as a particle shell and aspirin as a nucleus.

The result of the proposed method is to obtain aspirin nanocapsules.

EXAMPLE 1. Obtaining nanocapsules of aspirin in carrageenan, the ratio of the shell: core 1: 5

A suspension of 5 g of aspirin is dissolved in 5 ml of benzene and the resulting mixture is dispersed in a suspension of carrageenan in butanol containing 1 g of the indicated polymer in the presence of 0.01 g of the preparation E472c (glycerol ester with one to two molecules of food fatty acids and one to two molecules citric acid, and citric acid, as tribasic, can be esterified with other glycerides and as an acid with other fatty acids. Free acid groups can be neutralized with sodium) with stirring at 1000 rpm. Next, 5 ml of carbon tetrachloride are poured. The resulting suspension is filtered and dried at room temperature.

Received 6 g of nanocapsule powder. The yield was 100%.

EXAMPLE 2. Obtaining nanocapsules of aspirin in carrageenan, the ratio of the shell: core 3: 1

A suspension of 1 g of aspirin is dissolved in 5 ml of benzene and the resulting mixture is dispersed in a suspension of carrageenan in butanol containing 3 g of the indicated polymer in the presence of 0.01 g of the preparation E472c with stirring 1000 rps. Next, 3 ml of carbon tetrachloride are added. The resulting suspension is filtered and dried at room temperature.

Received 4 g of nanocapsule powder. The yield was 100%.

EXAMPLE 3. Obtaining nanocapsules of aspirin in carrageenan, the ratio of the shell: core 1: 1

A suspension of 1 g of aspirin is dissolved in 2 ml of benzene and the resulting mixture is dispersed in a suspension of carrageenan in butanol containing 1 g of the indicated polymer in the presence of 0.01 g of the preparation E472c with stirring 1000 rps. Next, 2 ml of carbon tetrachloride are added. The resulting suspension is filtered and dried at room temperature.

Received 2 g of nanocapsule powder. The yield was 100%.

EXAMPLE 4. Determination of the size of nanocapsules by NTA

The measurements were carried out on a Nanosight LM0 multiparameter nanoparticle analyzer manufactured by Nanosight Ltd (Great Britain) in the HS-BF configuration (Andor Luca high-sensitivity video camera, 405 nm semiconductor laser with a power of 45 mW). The device is based on the method of analysis of trajectories of nanoparticles (Nanoparticle Tracking Analysis, NTA) described by bASTM E2834.

The optimal ratio for dilution was chosen 1: 100. For the measurement, the device parameters were selected: Camera Level = 16, Detection Threshold = 10 (multi), Min Track Length: Auto, Min Expected Size: Auto. Duration of a single measurement of 215s, the use of a syringe pump.

The table shows the statistical characteristics of the distributions.

In fig. Figure 1 shows the particle size distribution in a sample of aspirin nanocapsules in carrageenan.

Claims (1)

A method of producing aspirin nanocapsules in a carrageenan shell, characterized in that a suspension of aspirin in benzene is obtained, the mixture is dispersed into a suspension of carrageenan in butanol in the presence of E472c with stirring at 1000 rpm, then carbon tetrachloride is added, the resulting suspension of nanocapsules is filtered off and dried room temperature.

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