Method of obtaining microcapsules of medications of cephalosporin group in human serum albumin

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to the field of pharmaceutics, in particular to microcapsulation of medications of a cephalosporin group, belonging to β-lactam antibiotics, in human serum albumin.

EFFECT: realisation of invention results in simplification and acceleration of the process of obtaining microcapsules of water-soluble medications of the cephalosporin group in human serum albumin, reduction of loss in the process of obtaining microcapsules (increase of the output by weight).

2 ex

 

The invention relates to the field of microencapsulation of drugs of cephalosporin group related to β-lactam antibiotics, albumin human serum.

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 A61K 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 -50°C, 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 the liquid vector, and the pharmaceutically active substance is 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 PA the. 2159037, IPC A01N 25/28, A01N 25/30, Russian Federation, published 20.11.2000, proposed a method of producing microcapsules by 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, 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, 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/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 10°C, the temperature at the outlet 28°C, 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, USA 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 the 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 by the 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 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 in human serum albumin, reducing losses upon receipt of the microcapsules (increase in mass).

The solution of the technical problem is achieved by a method of producing microcapsules drug group cephalosporins related to β-lactam antibiotics, as the shell of the microcapsules is used albumin human serum when receiving physical-chemical method for the deposition nerastvorim using two precipitators - carbinol 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 Leka the preparations of the group of cephalosporins, related to β-lactam antibiotics.

The result of the proposed method are obtaining microcapsules drug group cephalosporins related to β-lactam antibiotics in human serum albumin at 25°C for 20 minutes. The output of the microcapsules is over 90%.

EXAMPLE 1. Obtaining microcapsules Cefotaxime in albumin using carbinol 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 A with as surfactants. The resulting mixture was put on a magnetic stirrer and include mixing. After dissolution of the components of the reaction mixture until a clear solution is formed very slowly poured dropwise 5 ml of carbinol 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 0,240 g white to yellowish powder. The yield was 92%.

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

To 6 g of 2.5% aqueous solution of albumin add 0,450 g powder Cefotaxime and 0.02 g of the drug A with as surfactants. The resulting mixture was put on a magnetic stirrer and include mixing. After dissolution of the components of the reaction mixture until a clear solution is formed very slowly poured dropwise 5 ml of 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 0,564 g white to yellowish powder. The yield was 94%.

The obtained microcapsules drug group cephalosporins related to β-lactam antibiotics in human serum albumin physico-chemical method for the deposition nerastvorim using two precipitators - carbinol and acetone, which increases output 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 related to β-lactam antibiotics, albumin human serum.

The method of producing microcapsules of drugs by precipitation with aristotelem, characterized in that the quality of a medicinal product used drugs group of cephalosporins, as the shell - albumin human serum, which is precipitated from aqueous solution by adding as herstories carbinol and acetone at 25°C for 20 minutes.



 

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