RU2607589C2 - Method of producing nanocapsules of amino acids in konjac gum - Google Patents

Abstract

FIELD: chemistry.

SUBSTANCE: invention relates to encapsulation. Described is a method of producing nanocapsules of L-arginine or norvaline. Shell of nanocapsules used is konjak gum. According to disclosed method, L-arginine or norvaline is added to suspension konjak gum in butyl alcohol in presence of an E472c preparation, at a weight ratio of core: shell 5:1 or 1:3, or 1:1 respectively. Ethyl acetate is then added. Obtained suspension of nanocapsules is filtered and dried.

EFFECT: invention provides a simpler and faster process of producing nanocapsules, reduces losses during production thereof (high mass output).

1 cl, 1 dwg, 7 ex

Description

The invention relates to the field of nanotechnology, pharmaceuticals and pharmaceuticals.

Previously known methods for producing microcapsules.

In US Pat. 2173140, IPC A61K 009/50, A61K 009/127, Russian Federation, 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 dispersion ranges 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. 2359662, IPC A61K 009/56, A61J 003/07, B01J 013/02, A23L 001/00, published June 27, 2009, Russian Federation, a method for producing sodium chloride microcapsules using spray cooling in a Niro spray cooling tower under the following conditions: temperature inlet air 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. 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 nanocapsules in konjac gum of amino acids, characterized in that konjac gum is used as the shell of the nanocapsules, and the amino acids are used as the core for the preparation of nanocapsules by non-solvent deposition using ethyl acetate as a precipitant, the process of obtaining nanocapsules is carried out without special equipment .

A distinctive feature of the proposed method is the preparation of nanocapsules by non-solvent precipitation using ethyl acetate as a precipitant, as well as the use of konjac gum as a shell of particles and amino acids as a core.

The result of the proposed method are obtaining nanocapsules of amino acids.

EXAMPLE 1 Obtaining nanocapsules of L-arginine in konjak gum, the ratio of the core: shell 5: 1

5 g of L-arginine is slowly added in portions to a suspension of 1 g of konjac gum in 6 ml of butyl alcohol, in the presence of 0.01 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 tribasic can be esterified with other glycerides and as an oxo acid with other fatty acids. Free acid groups can be neutralized with sodium) with stirring 1300 r / sec. Next, 5 ml of ethyl acetate 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 L-arginine in konjac gum, the ratio of the core: shell 1: 3

1 g of L-arginine is slowly added in portions to a suspension of 3 g of konjac gum in 6 ml of butyl alcohol, in the presence of 0.01 preparation E472c with stirring at 1300 r / sec. Next, 5 ml of ethyl acetate are poured. 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 L-arginine in konjak gum, the ratio of the core: shell 1: 1

1 g of L-arginine is slowly added in portions to a suspension of 1 g of konjac gum in 6 ml of butyl alcohol, in the presence of 0.01 preparation E472c with stirring 1300 r / sec. Next, 5 ml of ethyl acetate are poured. The resulting suspension is filtered and dried at room temperature.

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

EXAMPLE 4 Preparation of norvaline nanocapsules in konjac gum, core: shell ratio 5: 1

5 g of norvaline is slowly added in portions to a suspension of 1 g of xanthan gum in 6 ml of butyl alcohol, in the presence of 0.01 of the preparation E472c with stirring at 1300 r / sec. Next, 5 ml of ethyl acetate are poured. The resulting suspension is filtered and dried at room temperature.

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

EXAMPLE 5 Obtaining nanocapsules of norvaline in konjac gum, the ratio of core: shell 1: 3

1 g of norvaline is slowly added in portions to a suspension of 3 g of xanthan gum in 6 ml of butyl alcohol, in the presence of 0.01 of the preparation E472c with stirring at 1300 r / sec. Next, 5 ml of ethyl acetate are poured. The resulting suspension is filtered and dried at room temperature.

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

EXAMPLE 6 Preparation of norvaline nanocapsules in konjac gum, core: shell ratio 1: 1

1 g of norvaline is slowly added in portions to a suspension of 1 g of xanthan gum in 6 ml of butyl alcohol, in the presence of 0.01 of the preparation E472c with stirring at 1300 r / sec. Next, 5 ml of ethyl acetate are poured. The resulting suspension is filtered and dried at room temperature.

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

EXAMPLE 7 Determination of the size of nanocapsules by the NTA method.

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 Nanoparticle Tracking Analysis (NTA) method described in ASTM E2834.

The optimal dilution for dilution was 1: 100. For 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 215s, use of a syringe pump.

Thus, amino acid nanocapsules with a high yield were obtained without special equipment for 10 min.

Claims (1)

A method of producing nanocapsules of L-arginine or norvaline, which consists in the fact that konjac gum is used as the shell of the nanocapsules, and L-arginine or norvaline is used as the core, with a mass ratio of the core: shell of 5: 1, or 1: 3, or 1 : 1, respectively, while L-arginine or norvinine is added to a suspension of konjac gum in butyl alcohol in the presence of the preparation E472c with stirring at 1300 r / s, then ethyl acetate is added, the resulting suspension of nanocapsules is filtered off and dried at room temperature.

Images