Method of producing aspirin nanocapsules in carrageenan

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.

1 dwg, 4 ex

 

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

Previously known methods for producing microcapsules.

In us Pat. RF 2173140, IPC A61K 009/50, A61K 009/127 published 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. RF 2359662, IPC A61K 009/56, A61J 003/07, B01J 013/02, A23L 001/00 published 27.06.2009, a method of producing microcapsules of sodium chloride with the use of 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/min Microcapsules according to the invention possess improved�'s internal 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/min).

The closest method is the method proposed in us Pat. RF 2134967, IPC A01N 53/00, A01N 25/28, published 27.08.1999. 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 producing nanocapsules, reduction of losses in obtaining nanocapsules (increase of the yield by weight).

The solution of a technical problem is achieved by a method of obtaining nanocapsules, characterized in that as the shell of the nanocapsules carrageenan is used, and as the kernel - aspirin when receiving the encapsulated particles by deposition of nerastvorim with the use of carbon tetrachloride as a precipitant, the process of obtaining nanocapsules can be made without special equipment�hardware.

A distinctive feature of the proposed method is to obtain nanocapsules by deposition of nerastvorim using carbon tetrachloride as the precipitant, and the use of carrageenan as the shell particles and aspirin - as the kernel.

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

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

A suspension of 5 g of aspirin dissolved in 5 ml of benzene and the resulting mixture was dispersed in a suspension of carrageenan in butanol containing 1 g of the specified polymer, in the presence of 0.01 g of the drug E472c (an ester of glycerol with one or two molecules of dietary fatty acids and one or two molecules of citric acid, and citric acid, tribasic, can be etherification other glycerides and as oxanilate - other fatty acids. Free acid groups can be neutralized with sodium) under stirring about 1000/sec. Next, pour 5 ml of carbon tetrachloride. The resulting suspension was filtered and dried at room temperature.

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

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

A suspension of 1 g of aspirin dissolved in 5 ml of benzene and disperging� the resulting mixture in a suspension of carrageenan in butanol, containing 3 g of the specified polymer, in the presence of 0.01 g of the drug E472c under stirring about 1000/sec. Next, pour 3 ml of carbon tetrachloride. The resulting suspension was filtered and dried at room temperature.

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

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

A suspension of 1 g of aspirin dissolved in 2 ml of benzene and the resulting mixture was dispersed in a suspension of carrageenan in butanol containing 1 g of the specified polymer, in the presence of 0.01 g of the drug Is under stirring about 1000/sec. Next, pour 2 ml of carbon tetrachloride. The resulting suspension was filtered and dried at room temperature.

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

EXAMPLE 4. Determining the size of the nanocapsules NTA method

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

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

The table shows the statistical characteristics of the distributions.

In Fig. 1 shows the distribution of particle size in the sample nanocapsules of aspirin in the carrageenan.

A method of producing nanocapsules of aspirin in the shell of carrageenan, characterized by the fact that receive a suspension of aspirin in benzene, the resulting mixture is dispersed in a suspension of carrageenan in butanol in the presence of the drug Is under stirring about 1000/sec, then pour the carbon tetrachloride, the resulting suspension of nanocapsules was filtered off and dried at room temperature.



 

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