Method of obtaining particles of encapsulated by liposoluble polymeric envelope unabi, possessing supermolecular properties

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to chemical-pharmaceutical industry and represents method of obtaining microcapsules of medication, which possess supermolecular properties, by method of precipitation with non-solvent, characterized by the fact that as medication applied is powder of unabi berries, preliminarily dissolved in butanol, as envelope - carrageenan, which is precipitated from solution in acetone by addition as non-solvent of ethanol and water, with the following drying at room temperature.

EFFECT: invention ensures simplification and acceleration of process of obtaining microcapsules, reduction of loss in the process of obtaining microcapsules (increase of output by weight).

2 ex, 18 dwg

 

The invention relates to the field of encapsulation.

Previously known methods for producing microcapsules.

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 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 A61K 009/56, A61J 003/07, B01J 013/02, A23L 001/00 published 27.06.2009, 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 have improved stability and provide�have 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. 2134967 IPC A01N 53/00, A01N 25/28 published 27.08.1999 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, 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 production of microcapsules, 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 obtaining particles of encapsulated fat-soluble polymeric membrane antioxidant, with supramolecular properties, characterized in that as the shell of the microcapsules used fat-soluble polymer, and as the kernel - jujube when receiving the encapsulated particles by deposition not�rastvoritele with the use of butanol and ethanol as precipitants, the process of obtaining microcapsules is carried out without special equipment.

A distinctive feature of the proposed method is the production of microcapsules by the method of deposition by nerastvorim using butanol and ethanol as precipitating reagents, and the use of lipid-soluble polymer as the shell particles and ziziphus - as the kernel.

The result of the proposed method is to obtain microcapsules jujube in fat-soluble polymeric shell.

Ziziphus or "jujube" belongs to the buckthorn family. The pulp of the fruit of the jujube has medicinal properties. Contained in the fruit substances strengthen the heart muscle, lowers blood pressure and very useful for hypertension patients. Now the fruits of ziziphus is used as a diuretic for kidney stones and inflammation of the bladder. They are also used as a tonic. The fruits of ziziphus include in the diet in diseases of liver, hypertension (both downward pressure and a diuretic), diseases of the respiratory system (it is noted that they have a softening effect in bronchitis, tracheitis, throat disorders). A decoction of the leaves and bark of ziziphus is used in pulmonary diseases, and externally against skin.

Fig 1. Presents the results of self capsules jujube in carrageenan at a concentration of 0.5%: a - �Velicina in 505 times b - increase in number 620, - increase in 930 times, g - an increase of 1,200 times, d - increase in 1770 times, e - increase in 2830 times.

Fig 2. Presents the results of self capsules jujube in carrageenan at a concentration of 0.25% and an increase in 505 times, b - magnification 620), - increase in 930 times, g - an increase of 1,200 times, d - increase in 1770 times, e - increase in 2830 times.

Fig 3. Presents the results of self capsules jujube in carrageenan at a concentration of 0.125%: a - increase in 505 times, b-magnification 620), - increase in 930 times, g - an increase of 1,200 times, d - increase in 1770 times, e - increase in 2830 times.

EXAMPLE 1. Obtaining microcapsules jujube in carrageenan

100 mg powder of jujube berries dissolved in 1 ml of butanol and the resulting mixture is dispersed in a solution of carrageenan in acetone 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, tribasic, can be etherification other glycerides and as oxanilate - other fatty acids. Free acid groups can be neutralized with sodium) with stirring 1300 Rev/sec. Next, pour 2 ml of ethanol and 1 ml of water. The resulting suspension was filtered and dried at room temperature.

Received 0,396 g �orosco microcapsules. The yield was 99%.

EXAMPLE 2. Investigation of self-microcapsules from solutions

From the powder of the microcapsules obtained by the method described in example 1 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 the dried surface was carried out confocal scanning microscopy.

Thus, the obtained microcapsules jujube with high output without special equipment within 10 min. the Formation of microcapsules occurs spontaneously through non-covalent vzaimodeistvie and this suggests that they are characterized by self-Assembly. Shown in Fig.2-3 patterns are ordered, so they are self-organizing. Consequently, the encapsulated fat-soluble polymeric shell jujube has the supramolecular properties.

A method of producing microcapsules of the drug with supramolecular properties, by deposition of aristotelem, characterized in that the medicinal product is used powder of jujube berries, previously dissolved in butanol, as the shell - carrageenan, which is precipitated from solution in acetone by adding as herstorical� of ethanol and water, with subsequent drying at room temperature.



 

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