Method for cephalosporin bioencapsulation

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to chemical-pharmaceutical industry and represents a method for drug microencapsulation by non-solvent addition; the method is characterised by the fact that the above drugs are presented by cephalosporin preparations, while a coating is human serum albumin precipitated from an aqueous solution by adding methylcarbinol as a non-solvent and acetone at 25C.

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

3 ex

 

The invention relates to the field of bioencapsulation, particularly to the field of production of microcapsules drug group cephalosporins.

Previously known methods for producing microcapsules of drugs. Thus, in U.S. Pat. 2092155, IPC AC 047/02, AK 009/16 published 10.10.1997, 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 the use of ultraviolet radiation, which can influence the formation of microcapsules.

In Pat. 2095055, IPC AC 9/52, AK 9/16, AC 9/10, Russian Federation, published 10.11.1997, method for obtaining solid 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 -50C, and the separation of the obtained microspheres into fractions by size. The suspension is intended for administration by parenteral injection, contains an effective amount of these microspheres, dispersed in a pharmaceutically acceptable liquid vector, and pharmaceutically the active substance insoluble microspheres in a specified liquid medium.

Disadvantages of the proposed method: obtaining microcapsules by using spray cooling, complexity and duration of the process, the use of special equipment.

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

The disadvantage of this method is the use of a ball mill and the duration of the process.

In Pat. 2101010, IPC AC 9/52, AK 9/50, AK 9/22, AK 9/20, AK 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. 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. 2159037, IPC A01N 25/28, A01N 25/30, Russian Federation, published 20.11.2000, method for obtaining Mick is kapsul the polymerization reaction at the phase boundary, containing solid agrochemical material 0.1 to 55 wt.%, suspended in peremestivsheesya water organic liquid, from 0.01 to 10 wt.% non-ionic dispersant, active on the phase boundary and is not acting as an emulsifier.

Disadvantages of the proposed method: the complexity, duration, using wysokosciowe mixer.

In Pat. 2173140, IPC AC 009/50, AK 009/127, Russian Federation, published 10.09.2001, method for obtaining kremnijorganicheskih microcapsules using a rotary cavitation plants with high shear effort and powerful acoustic phenomena of sound and ultrasound range for dispersion.

The disadvantage of this method is the use of special equipment - rotary-quotational installation, which has ultrasonic action that affects the formation of microcapsules and can cause adverse reactions due to the fact that ultrasound destructive effect on the polymers of protein nature, therefore the proposed method is applicable when working with polymers of synthetic origin.

In Pat. 2359662, IPC AC 009/56, A61J 003/07, B01J 013/02, A23L 001/00 published 27.06.2009, Russian Federation, proposed a method of producing microcapsules using spray cooling in the spray tower Niro in the following the conditions: the temperature of the air inlet 10C, the air temperature at the outlet 28C, 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.

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 10C, the temperature at the outlet 28C, the speed of rotation of the spray drum 10000 rpm).

In Pat. 20110223314, IPC B05D 7/00 20060101 B05D 007/00, VS 3/02 20060101 VS 003/02; VS 11/00 20060101 VS 011/00; B05D 1/18 20060101 B05D 001/18; B05D 3/02 20060101 B05D 003/02; B05D 3/06 20060101 B05D 003/06 from 10.03. 2011 US described a method of producing microcapsules by the method of suspension polymerization, belonging to the group of chemical methods with the use of the new device and ultraviolet radiation.

The disadvantage of this method is the complexity and duration of the process, the use of special equipment, obtaining microcapsules by the method of suspension polymerization using ultraviolet radiation.

The closest method is the method proposed in U.S. Pat. 2134967 IPC A01N 53/00, A01N 25/28 published 27.08.1999,, Russian Federation (1999). Water is dispersed solution of a mixture of natural lipids and a PYRETHROID insecticide in the weight ratio of 2-4:1 in the op is adicheskim 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 in human serum albumin, reducing losses upon receipt of the microcapsules (increase in mass).

The solution of the technical problem is achieved by the method of encapsulating drugs group of cephalosporins, characterized in that as the shell of the microcapsules is used albumin human serum when receiving physical-chemical method for the deposition nerastvorim using two precipitators - methylcarbazole and acetone, the retrieval process is carried out without special equipment.

A distinctive feature of the proposed method is the use of albumin human serum as the shell of the microcapsules drug group cephalosporins.

The result of the proposed method are obtaining microcapsules drugs group of cephalosporins in human serum albumin at 25C within 20 m of the nut. The output of the microcapsules is over 90%.

EXAMPLE 1. Obtaining microcapsules Cefotaxime in albumin using methylcarbazole and acetone as the precipitating, the ratio of 1:1

To 13 g of 1% aqueous solution of albumin add 0,130 g powder Cefotaxime and 0.02 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 5 ml of methylcarbazole as the first precipitator, and then 8 ml of acetone 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 0,257 g white to yellowish powder. The yield was 99%.

EXAMPLE 2. Obtaining microcapsules Ceftriaxone in albumin using methylcarbazole and acetone as the precipitating, the ratio of 3:1

To 6 g of 2.5% aqueous solution of albumin add 0,450 g of Ceftriaxone powder and 0.02 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 5 ml meth is carbinol as the first precipitator, and then 15 ml of acetone 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 0,594 g white to yellowish powder. The yield was 99%.

EXAMPLE 3. Obtaining microcapsules is anticipated in the albumin using methylcarbazole and acetone as the precipitating, the ratio of 3:1

To 6 g of 2.5% aqueous solution of albumin add 0,450 g of Cefazolin powder and 0.02 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 5 ml of methylcarbazole as the first precipitator, and then 15 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 0,594 g white to yellowish powder. The yield was 99%.

The obtained microcapsules drugs group of cephalosporins in human serum albumin physico-chemical method for the deposition nerastvorim using two precipitators - methylcarbazole and acetone, which increases the of ihoda and accelerates the process of microencapsulation. The process is simple to perform and lasts for 20 minutes, requires no special equipment.

The proposed method is suitable for the pharmaceutical industry due to the minimal loss of speed, ease of acquisition and allocation of microcapsules cephalosporins in human serum albumin.

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 - albumin human serum, which is precipitated from aqueous solution by adding as herstories methylcarbazole and acetone at 25C.



 

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