Method of producing resveratrol nanocapsules in pectin

FIELD: chemistry.

SUBSTANCE: invention relates to encapsulation, particularly a method of producing resveratrol nanocapsules in an envelope made of low- or highly esterified apple or citrus pectin. According to the disclosed method, resveratrol is dispersed in a suspension of low- or highly esterified apple or citrus pectin in benzene in the presence of an E472c preparation while stirring at 1000 rps. Tetrachloromethane is then added. The obtained suspension of nanocapsules is filtered and dried. The process of producing the nanocapsules is carried out at 25°C for 10 minutes.

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

9 ex, 1 dwg

 

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

Previously known methods for producing microcapsules.

In us Pat. 2173140, IPC AC 009/50, AK 009/127, Russian Federation, 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. 2359662, IPC AC 009/56, A61J 003/07, B01J 013/02, A23L 001/00 published 27.06.2009, the Russian Federation proposed a method of obtaining 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 �stabilnosti 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).

The closest method is the method proposed in us Pat. 2134967, IPC A01N 53/00, A01N 25/28, published 27.08.1999, Russian Federation. 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 of resveratrol, characterized in that as the shell of the nanocapsules used high - and nizkoteploprovodnye Apple and citrus pectins, and as the kernel - resveratrol when receiving the encapsulated particles by deposition of nerastvorim with the use of carbon tetrachloride in the quality�e precipitator, the process of obtaining nanocapsules can be made without special equipment.

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 pectin as the shell particles and resveratrol - as the kernel.

The result of the proposed method javlautsa obtaining nanocapsules of resveratrol.

EXAMPLE 1. Obtaining nanocapsules of resveratrol in vysokodetalizirovannom Apple pectin, the ratio of sheath:core 3:1

1 g of resveratrol is dispersed in the slurry vysokotarifitsirovannyh Apple pectin in benzene containing 3 g of the specified polymer, in the presence of 0.01 g of the drug Is (an ester of glycerol with one or two molecules of dietary fatty acids and one or two molecules of citric acid, and citric acid as 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 4 g of powder of nanocapsules. The yield was 100%.

EXAMPLE 2. Obtaining nanocapsules of resveratrol in you�ametripitline Apple pectin, the ratio of sheath:core 1:5

5 g of resveratrol is dispersed in the slurry vysokotarifitsirovannyh Apple pectin in benzene 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 3 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 3. Obtaining nanocapsules of resveratrol in low-esterified Apple pectin, the ratio of sheath:core 3:1

1 g of resveratrol was dispersed in a suspension of low-esterified Apple pectin in benzene containing 3 g of the specified polymer, in the presence of 0.01 g of the drug Is under stirring about 1000/sec. Next, pour 5 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 4. Obtaining nanocapsules of resveratrol in low-esterified Apple pectin, the ratio of sheath:core 1:5

5 g of resveratrol was dispersed in a suspension of low-esterified Apple pectin in benzene 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 3 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 5. Obtaining nanocapsules of resveratrol in vysokodetalizirovannom citrus pectin, the ratio of sheath:core 3:1

1 g of resveratrol is dispersed in the slurry vysokotarifitsirovannyh citrus pectin in benzene containing 3 g of the specified polymer, in the presence of 0.01 g of the drug Is under stirring about 1000/sec. Next, pour 5 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 6. Obtaining nanocapsules of resveratrol in vysokodetalizirovannom citrus pectin, the ratio of sheath:core 1:5

5 g of resveratrol is dispersed in the slurry vysokotarifitsirovannyh citrus pectin in benzene 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 3 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 7. Obtaining nanocapsules of resveratrol in low-esterified citrus pectin, the ratio of sheath:core 3:1

1 g of resveratrol was dispersed in a suspension of low-esterified citrus pectin in benzene containing 3 g specified�CSOs polymer, in the presence of 0.01 g of the drug Is under stirring about 1000/sec. Next, pour 5 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 8. Obtaining nanocapsules of resveratrol in low-esterified citrus pectin, the ratio of sheath:core 1:5

5 g of resveratrol was dispersed in a suspension of low-esterified citrus pectin in benzene 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 3 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 9. 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 in ASTM E2834.

The optimal dilution 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 Expected Size:Auto snapshot length�there is a single measurement 215s, the use of a syringe pump.

Thus, the obtained nanocapsules of resveratrol with high yield within 10 min.

A method of producing nanocapsules of resveratrol, characterized by the fact that the linkage of resveratrol is dispersed in a low - or vysokotarifitsirovannyh Apple or citrus pectin in a solution of benzene in the presence of the drug Is under stirring about 1000/sec, then pour the carbon tetrachloride as a precipitant, the resulting suspension was filtered off and dried, while the ratio of sheath:core is used as 3:1 and 1:5.



 

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1 tbl, 2 ex, 1 dwg

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16 ex

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2 ex

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