Method for producing sel-plex nanocapsules possessing supramolecular properties

FIELD: medicine.

SUBSTANCE: invention describes a method for producing Sel-Plex nanocapsules possessing the supramolecular properties by non-solvent addition, characterised by the fact that Sel-Plex is dissolved in dimethyl sulphoxide; the prepared mixture is dispersed in xanthum gum solution used as a nanocapsule shell, in butanol, in the presence of E472c preparation while stirring at 1000 cycles per second; the mixture is added with the precipitator benzol, filtered and dried at room temperature.

EFFECT: simplifying and accelerating the process of nanoencapsulation and ensuring higher weight yield.

4 ex, 12 dwg

 

The invention relates to the field of nanotechnology and veterinary medicine, in particular nanocapsules SEL-Plex with supramolecular properties. SEL-Plex selenium found primarily in the composition of the amino acids Selenomethionine and selenocystine. Increases antioxidant status of the organism and survival of young, supports and increases the motility and fertilizing capacity of sperm, improves productivity in the presence of mycotoxins in feed, improves the condition of the plumage. Used in the manufacture of mixed fodders and premixes as a source of Se instead of sodium Selenite and other inorganic compounds of this element for all animal species.

Previously known methods for producing microcapsules of drugs. So, in us Pat. 2092155, IPC A61K 047/02, A61K 009/16 published 10.10.1997, the Russian Federation proposed a method for microencapsulation of drugs, based on the use of irradiation with ultraviolet rays.

The disadvantages of this method are the duration of the process and application of ultraviolet radiation, which can influence the formation of microcapsules.

In us Pat. 2091071, IPC A61K 35/10, Russian Federation, published 27.09.1997 a method of producing the drug by dispersing in a ball mill to obtain microcapsules.

p> The disadvantage of this method is the application of the ball mill and the duration of the process.

In us Pat. 2101010, IPC A61K 9/52, A61K 9/50, A61K 9/22, A61K 9/20, A61K 31/19, Russian Federation, published 10.01.1998 proposed chewable form of the drug with taste masking, having the properties of a controlled release drug product that contains microcapsules with a size of 100-800 microns in diameter and consists of pharmaceutical kernel crystalline ibuprofen and polymeric coating comprising a plasticizer, elastic enough to resist chewing. Polymer coating is a copolymer based on methacrylic acid.

Disadvantages of the invention: use of a copolymer based on methacrylic acid, as these polymer coatings can cause cancer; the difficulty of execution; the duration of the process.

In us Pat. 2173140, IPC A61K 009/50, A61K 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 possesses�AET ultrasonic action, what 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 A61K 009/56, A61J 003/07, B01J 013/02, A23L 001/00 published 27.06.2009, the Russian Federation proposed a method of producing microcapsules using 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 have improved 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).

The closest method is the method proposed in us Pat. 2134967, IPC A01N 53/00, A01N 25/28, published 27.08.1999 G., Russian Federation (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, copepodid to simplify 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, reducing loss upon receipt of the microcapsules (increase of the yield by weight).

The solution of a technical problem is achieved by a method of encapsulating SEL-Plex, characterized in that as the shell of the nanocapsules xanthan gum is used when receiving physical-chemical method for the deposition nerastvorim using precipitator - benzene, the process is carried out without special equipment.

A distinctive feature of the proposed method is the use of xanthan gum as the shell of the nanocapsules SEL-Plex as their nucleus, and the use of precipitator - benzene.

The result of the proposed method is to obtain nanocapsules SEL-Plex in xanthan gum for 20 minutes. The output of the nanocapsules is over 90%.

Fig.1 shows confocal images of fractal compositions from solution nanocapsules SEL-Plex in the shell xanthan gum (ratio of sheath:core 3:1) at a concentration of 0.25% that: a) the increase in 505 times, b) the increase in 620 times) increase in 930 times, g) took�argument in 1200 times d) an increase in 1770 times, (e) increase in 2830 times.

Fig.2 shows confocal images of fractal compositions from solution nanocapsules SEL-Plex in the shell xanthan gum (ratio of sheath:core 3:1) at a concentration of 0.125%: a) an increase in 505 times, b) the increase in 620 times) increase in 930 times, g) magnification of 1200 times, d) the increase in 1770 times, (e) increase in 2830 times.

EXAMPLE 1. Obtaining nanocapsules SEL-Plex with the dissolution of the drug in dimethyl sulfoxide (DMSO), the ratio of the core/polymer 1:3

100 mg SEL-Plex suspension in 1 ml DMSO and the resulting mixture is dispersed in a solution of xanthan gum in butanol containing the specified 300 mg of the 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/s. Next, pour 4 ml of benzene and 1 ml of distilled water. The resulting suspension was filtered and dried at room temperature.

Received 0,396 g of a white powder. The yield was 99%.

EXAMPLE 2. Obtaining nanocapsules SEL-Plex with the dissolution of the drug in dimethyl sulfoxide (DMSO), aspect]�the determination of the core/polymer 1:2

100 mg SEL-Plex dissolved in 1 ml DMSO and the resulting mixture is dispersed in a solution of xanthan gum in butanol containing specified 200 mg of the polymer in the presence of 0.01 g of the drug Is under stirring about 1000/s. Next, pour 3 ml of benzene and 1 ml of distilled water. The resulting suspension was filtered and dried at room temperature.

Received 0,297 g of a white to yellowish powder. The yield was 99%.

EXAMPLE 3. Obtaining nanocapsules SEL-Plex with the dissolution of the drug (DMSO), the ratio of the core/polymer 1:1

100 mg SEL-Plex dissolved in 1 ml DMSO and the resulting mixture is dispersed in a solution of xanthan gum in butanol containing specified 100 mg of the polymer in the presence of 0.01 g of the drug Is under stirring about 1000/s. Next, pour 2 ml of benzene and 1 ml of distilled water. The resulting suspension was filtered and dried at room temperature.

Received 0,190 g of a white to yellowish powder. The yield was 95%.

EXAMPLE 4. Investigation of self-nanocapsules from solutions

From the powder of nanocapsules obtained according to the method described in the examples, there were prepared aqueous solutions of concentrations 1%, 0,5%, 0,25%, 0,125% etc. by dilution of the solution twice. A drop of each of the prepared solutions were placed on a glass slide prior to complete drying and dried over�spine was performed confocal scanning microscopy.

The formation of nanocapsules occurs spontaneously through non-covalent interactions and this suggests that they are characterized by self-Assembly. Shown in Fig.1, 2 patterns are ordered, so they are self-organizing. Consequently, encapsulated SEL-Plex has a supramolecular properties.

The obtained nanocapsules Villages of the Complex physico-chemical deposition method by nerastvorim using precipitator - benzene, which increases output and accelerates the process of nanocapsule. The process is simple to perform and lasts for 20 minutes, requires no special equipment.

The proposed method is suitable for the veterinary industry due to the minimal loss of speed, ease of obtaining and allocation of nanocapsules.

A method of producing nanocapsules SEL-Plex with supramolecular properties, by deposition of aristotelem, characterized by the fact that SEL-Plex was dissolved in dimethylsulfoxide and the resulting mixture is dispersed in a solution of xanthan gum that is used as the shell of the nanocapsules, in butanol, in the presence of the drug As with stirring at 1000 Rev/s, then pour the precipitator - benzene, filtered off and dried at room temperature.



 

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