Method for bioencapsulation

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to chemical-pharmaceutical industry and represents a method for preparing drug microcapsules by nonsolvent addition differing by the fact that the drugs represent the preparations of cephalosporin group, and a coating is poludan deposited from an aqueous solution by adding diethyl ester and isopropanol at 25 °C as a nonsolvent.

EFFECT: invention provides simplifying and accelerating the process of microcapsules, reducing the microcapsule loss (higher weight yield).

3 ex

 

The invention relates to the field of bioencapsulation, in particular microencapsulation of drugs of cephalosporin group related to β-lactam antibiotics, Poludan physico-chemical method for the deposition aristotelem.

Previously known methods for producing microcapsules. Thus, in U.S. Pat. EN 2092155, IPC A61K 047/02, A61K 009/16 published 10.10.1997, the method of microencapsulation of drugs, based on the use of special equipment use of irradiation with ultraviolet rays.

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

In Pat. EN 2095055, IPC A61K 9/52, A61K 9/16, A61K 9/10, published 10.11.1997 proposed a method of obtaining a hard, non-porous microspheres includes melting pharmaceutically inactive substance carrier, the dispersion of a pharmaceutically active substance in the melt in an inert atmosphere, spraying the resulting dispersion in the form of a mist in the freezing chamber under pressure, in an inert atmosphere at a temperature of from 15 to 50°C and separation of the resulting microspheres into fractions by size. The suspension is intended for administration by parenteral injection, contains an effective amount of these microspheres distributed the pharmaceutically acceptable liquid vector, and the pharmaceutically active substance is insoluble microspheres in a specified liquid medium.

Disadvantages of the proposed method: the complexity and duration of the process and the use of special equipment.

In Pat. EN 2091071 A61K 35/10, published 27.09.1997 method for obtaining the drug by dispersion in a ball mill to obtain microcapsules.

The disadvantages of the method are the use of a ball mill and the duration of the process.

In Pat. EN 2076765, IPC B01D 9/02, published 10.04.1997 method for obtaining dispersed particles of soluble compounds in the microcapsules by crystallization from a solution, wherein the solution is dispersed in an inert matrix, cooled and, by changing the temperature, get dispersed particles.

The disadvantage of this method is the difficulty of execution: obtaining microcapsules by dispersion with subsequent change of temperatures, which slows down the process.

In Pat. EN 2101010, IPC A61K 9/52, A61K 9/50, A61K 9/22, A61K 9/20, A61K 31/19, 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 polymer coating, including the Plaza is idicator, elastic enough to resist chewing. The polymer coating is a copolymer based on methacrylic acid.

The drawbacks of the invention: use of a copolymer based on methacrylic acid, as these polymer coatings can cause cancer; complexity; the duration of the process.

In Pat. EN 2139046, IPC A61K 9/50, A61K 49/00, A61K 51/00, published 10.10.1999 method for obtaining microcapsules as follows. Emulsion oil-in-water prepared from organic solution containing dissolved mono-, di-, triglyceride, preferably of tripalmitin or tristearin, and possibly therapeutically active substance, and an aqueous solution containing a surfactant, it is possible to evaporate part of the solvent, add redispersible agent and the mixture is subjected to drying by freezing. Subjected to drying by freezing the mixture is then dispersed in an aqueous medium to separate the particles from organic substances and a hemispherical or spherical microcapsules dried.

Disadvantages of the proposed method are the complexity and duration of the process, the use of drying by freezing, which takes time and slows down the process of production of microcapsules.

In Pat. EN 2359662, IPC A61K 009/56, A61J 003/07, B01J 013/02, A23L 001/00 published 27.6.2009, method for obtaining 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 Microcapsules according to the invention have improved stability and provide adjustable and/or prolonged release of the active ingredient.

Disadvantages of the proposed method are the duration of the process and the use of special equipment, a set of conditions (temperature of inlet air 10°C, the temperature at the outlet 28°C, the speed of rotation of the spray drum 10,000 rpm).

In Pat. EP WO/2011/003805, IPC B01J 13/18; B65D 83/14; C08G 18/00, published on 13.01.2011 described a method of producing microcapsules, which are suitable for use in compositions forming sealants, foams, coatings or adhesives.

The disadvantage of the proposed method is the use of centrifugation to separate from the fluid, the length of the process, and the use of this method not in the pharmaceutical industry.

The closest method is the method proposed in U.S. Pat. EN 2134967, IPC A01N 53/00, A01N 25/28 published 27.08.1999, (1999). Water is dispersed solution of a mixture of natural lipids and a PYRETHROID insecticide in the weight respect to the research Institute 2-4:1 in an organic solvent, which leads to simplification of the method of microencapsulation.

The disadvantage of this method is the dispersion in the aquatic environment, which makes the proposed method applicable to the production of microcapsules of water-soluble drugs in water-soluble polymers.

The technical objective is the simplification and acceleration of the process of obtaining the microcapsules vodorastvorimyh drugs group of cephalosporins, the reduction of losses upon receipt of the microcapsules (increase in mass).

The solution of the technical problem is achieved by the method of bioencapsulation, characterized in that as the shell of the microcapsules is used Poludan, and obtaining microcapsules physico-chemical deposition method by nerastvorim using two precipitators - diethyl ether and isopropanol, the retrieval process is carried out without special equipment.

A distinctive feature of the proposed method is the use as the shell of the microcapsules drug group cephalosporins related to β-lactam antibiotics, poludana, and obtaining microcapsules physico-chemical deposition method by nerastvorim using two precipitators - diethyl ether and isopropanol.

The result of the proposed method are obtaining microcapsules drug group is ephalosporins, related to β-lactam antibiotics in Poludan at 25°C for 15 minutes. The output of the microcapsules is over 90%.

EXAMPLE 1. Obtaining microcapsules Cefotaxime in Poludan using diethyl ether and isopropanol as the precipitating, the ratio of 3:1

To 2 g of 1% aqueous poludana add to 0.060 g of powder Cefotaxime and 0.05 g of the drug Is as surfactants. The resulting mixture was put on a magnetic stirrer and include mixing. After the dissolution of the components of the reaction mixture until a clear solution is formed very slowly poured dropwise 1 ml of diethyl ether as the first precipitator, and then 5 ml of isopropanol as the second. The resulting suspension of microcapsules is filtered by the filter SCHOTT 16 class then washed with acetone, dried in a desiccator over calcium chloride.

Received 0,077 g of white powder. The yield was 77%.

EXAMPLE 2. Obtaining microcapsules Ceftriaxone in Poludan using diethyl ether and isopropanol as the precipitating, the ratio of 3:1

To 2 g of 1% aqueous poludana add to 0.060 g of Ceftriaxone powder and 0.05 g of the drug Is as surfactants. The resulting mixture was put on a magnetic stirrer and include mixing. After the dissolution of the components of the reaction mixture prior to the formation prozrachnoj the solution slowly poured dropwise 1 ml of diethyl ether as the first precipitator, and then 5 ml of isopropanol as the second. The resulting suspension of microcapsules is filtered by the filter SCHOTT 16 class then washed with acetone, dried in a desiccator over calcium chloride.

Received 0,098 g of white powder. The yield was 98%.

EXAMPLE 3. Obtaining microcapsules is anticipated in Poludan using diethyl ether and isopropanol as the precipitating, the ratio of 3:1

To 2 g of 1% aqueous poludana add to 0.060 g of Cefazolin powder and 0.05 g of the drug Is as surfactants. The resulting mixture was put on a magnetic stirrer and include mixing. After the dissolution of the components of the reaction mixture until a clear solution is formed very slowly poured dropwise 1 ml of diethyl ether as the first precipitator, and then 5 ml of isopropanol as the second. The resulting suspension of microcapsules is filtered by the filter SCHOTT 16 class then washed with acetone, dried in a desiccator over calcium chloride.

Received 0,096 g of white powder. The yield was 96%.

The obtained microcapsules drug group cephalosporins related to β-lactam antibiotics, Poludan physico-chemical method for the deposition nerastvorim using diethyl ether and isopropanol as nerastvorimaya. The process is simple to perform and lasts for those who begins 15 minutes no special equipment is required.

Poludan - biosynthetic polyribonucleotides complex polyadenylate and prioritylevel acid (equimolar proportions). The inducer of the synthesis of endogenous interferon. Stimulates the formation of mainly alpha-interferon, to a lesser extent β - and γ-interferons. Has a pronounced antiviral and immunomodulatory activity.

The proposed method is suitable for the pharmaceutical industry due to the minimal loss of speed, ease of acquisition and allocation of microcapsules cephalosporins related to β-lactam antibiotics, Poludan.

The method of producing microcapsules of drugs by precipitation with aristotelem, characterized in that the quality of drugs used drugs group of cephalosporins, as the shell - Poludan, which is precipitated from aqueous solution by adding as herstories diethyl ether and isopropanol at 25 °C.



 

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