RU2570380C2 - Method for obtaining losartan potassium nanocapsules in xanthan gum - Google Patents

Abstract

FIELD: chemistry.

SUBSTANCE: invention relates to method for obtaining losartan potassium nanocapsules in xanthan gum. Claimed method consists in the following: losartan potassium is dissolved in chloroform and obtained mixture is dispersed into xanthan gum suspension in benzene in presence of preparation E472c with mixing, after that acetone and water are poured in, obtained suspension is filtered and dried, with envelope/core ratio in nanocapsules constituting 3:1 or 1:5.

EFFECT: invention provides simplification and acceleration of the process of obtaining losartan potassium nanocapsules, as well as increase of their output by weight.

1 dwg, 1 tbl, 3 ex

Description

The method of obtaining nanocapsules of losartan potassium in xanthan gum

The invention relates to the field of encapsulation.

Previously known methods for producing microcapsules.

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 phenomena 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 sodium chloride 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, publ., 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 to the technical problem is achieved by the method of producing nanocapsules of potassium losartan, characterized in that xanthan gum is used as the shell of the nanocapsules, and potassium losartan is used as the core for the preparation of encapsulated particles by non-solvent deposition using acetone 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 acetone as a precipitant, as well as the use of xanthan gum as a particle shell and potassium losartan as a core.

The result of the proposed method are the preparation of potassium losartan nanocapsules.

EXAMPLE 1 Obtaining nanocapsules of potassium losartan in xanthan gum, the ratio of the shell: core 3: 1 (Fig. 1)

1 g of losartan potassium is dissolved in 2 ml of chloroform and the resulting mixture is dispersed in a suspension of xanthan gum in benzene containing 3 g of the indicated polymer in the presence of 0.01 g of the preparation E472 s (glycerol ester with one or two food-grade fatty acids and one two molecules of citric acid, moreover, citric acid as a tribasic acid can be esterified with other glycerides and an oxo acid with other fatty acids. Free acid groups can be neutralized with sodium) with stirring at 1000 rpm. Next, 5 ml of acetone and 1 ml of water are poured. The resulting suspension is filtered and dried at room temperature.

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

EXAMPLE 2 Obtaining nanocapsules of losartan potassium in xanthan gum, the ratio of the shell: core 1: 5

5 g of losartan potassium is dissolved in 5 ml of chloroform and the resulting mixture is dispersed in a suspension of xanthan gum in benzene containing 1 g of the indicated polymer in the presence of 0.01 g of the preparation E472 s with stirring 1000 rps. Then pour 3 ml of acetone and 1 ml of water. The resulting suspension is filtered and dried at room temperature.

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

EXAMPLE 3 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 the measurement, the device parameters were selected: Camera Level = 16, Detection Threshold = 10 (multi), Min Track Length: Auto, Min Expected Size: Auto. The duration of a single measurement is 215s, the use of a syringe pump.

As can be seen from table 1, the average size of the nanocapsules of losartan potassium in xanthan gum is 163 nm.

Claims (1)

A method of producing nanosapsules of potassium losartan in xanthan gum, characterized in that the potassium losartan is dissolved in chloroform and the resulting mixture is dispersed into a suspension of xanthan gum in benzene in the presence of E472c with stirring, 1000 rps are added, the acetone and water are poured, the suspension is filtered off and dried at room temperature, while the ratio of the shell / core in nanocapsules is 3: 1 or 1: 5.

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