Method for preparing cephalosporin microcapsules

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to chemical-pharmaceutical industry, and represents a method for preparing medicine microcapsules by non-solvent addition differing by the fact that the medical preparations are presented by the cephalosporin preparations, while a coating is polyvinyl alcohol that is precipitated by the addition of non-solvents that are carbinol and acetone at -25°C.

EFFECT: invention provides simplifying and accelerating the process for preparing the water-soluble cephalosporin microcapsules in polyvinyl alcohol, providing loss reduction in preparing the microcapsules (higher yield-mass).

16 ex

 

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

Previously known methods for producing microcapsules of drugs. Thus, in U.S. Pat. 2092155 IPC A61K 047/02, A61K 009/16 published 10.10.1997 Russian Federation proposed a method for 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. 2359662 IPC A61K 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 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 (the temperature is and the air inlet 10°C, the air temperature at the outlet 28°C, the speed of rotation of the spray drum 10000 rpm).

In Pat. 2173140 IPC A61K 009/50, A61K 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 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, using ultra is violet 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 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 of cephalosporin group in the polyvinyl alcohol, the reduction of 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, polyvinyl alcohol characterized in that in order to accelerate coagulation in obtaining microcapsules physico-chemical method for the deposition nerastvorim uses two precipitator - carbinol and acetone, the retrieval process is carried out without special equipment.

A distinctive feature of the proposed method is the use of two precipitators - carbinol and acetone PR is obtaining microcapsules drugs of cephalosporin group in the polyvinyl alcohol, related to β-lactam antibiotics, method of deposition nerastvorim that simplifies the process of microencapsulation as a result of accelerating the coagulation of the particles due to the addition of carbinol.

The result of the proposed method are obtaining microcapsules drugs of cephalosporin group in the polyvinyl alcohol-related β-lactam antibiotics in polyvinyl alcohol at 25°C for 20 minutes. The output of the microcapsules is 90%.

EXAMPLE 1. Obtaining microcapsules Cefotaxime in polyvinyl alcohol (PVA), a ratio of 1:5

To 10 g of 5% aqueous solution of PVA added 0.1 g of a powder of Cefotaxime and 0.02 g of the product OS-20 as surfactant. 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 carbinol as the first precipitator, and then 25 ml of acetone as the second. The resulting suspension of microcapsules leave on for 1 minute, then sucked on the filter SCHOTT 16 class then washed with acetone, dried in a desiccator over calcium chloride.

Received 0,546 g of white powder. The yield was 91%.

EXAMPLE 2. Obtaining microcapsules Cefotaxime in polyvinyl alcohol (PVA), a ratio of 1:3

To 18 g of 5% aqueous races the thief PVA add 0.3 g of powder Cefotaxime and 0.02 g product OS-20 as surfactant. 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 10 ml of carbinol as the first precipitator, and then 50 ml of acetone as the second. The resulting suspension of microcapsules leave on for 1 minute, then sucked on the filter SCHOTT 16 class then washed with acetone, dried in a desiccator over calcium chloride.

Received of 1.03 g of white powder. The yield was 86%.

EXAMPLE 3. Obtaining microcapsules Cefotaxime in polyvinyl alcohol (PVA), a ratio of 1:1

To 12 g of 5% aqueous solution of PVA added 0.6 g of powder Cefotaxime and 0.02 g product OS-20 as surfactant. 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 10 ml of carbinol as the first precipitator, and then 30 ml of acetone as the second. The resulting suspension of microcapsules leave on for 1 minute, then sucked on the filter SCHOTT 16 class then washed with acetone, dried in a desiccator over calcium chloride.

Obtained 1.07 g of white powder. The yield was 89%.

EXAMPLE 4. Obtaining microcapsules Cefotaxime in polyvinyl alcohol (PVA) ratio of 3:1

To 6 g of 5% aqueous solution of PVA added 0.9 g of powder Cefotaxime and 0.02 g product OS-20 as surfactant. 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 carbinol as the first precipitator, and then 20 ml of acetone as the second. The resulting suspension of microcapsules leave on for 1 minute, then sucked on the filter SCHOTT 16 class then washed with acetone, dried in a desiccator over calcium chloride.

Received 1,104 g of white powder. The yield was 92%.

EXAMPLE 5. Obtaining microcapsules Cefotaxime in polyvinyl alcohol (PVA), a ratio of 5:1

To 6 g of 5% aqueous solution of PVA added 1.5 g of powder Cefotaxime and 0.02 g product OS-20 as surfactant. 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 carbinol as the first precipitator, and then 20 ml of acetone as the second. The resulting suspension of microcapsules leave on for 1 minute, then sucked on the filter SCHOTT 16 class then washed with acetone, dried in a desiccator over calcium chloride

Received 1,670 g of white powder. The yield was 93%.

EXAMPLE 6. Obtaining microcapsules Ceftriaxone in polyvinyl alcohol (PVA), a ratio of 1:5

To 10 g of 5% aqueous solution of PVA added 0.1 g of Ceftriaxone powder and 0.02 g of the product OS-20 as surfactant. 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 carbinol as the first precipitator, and then 25 ml of acetone as the second. The resulting suspension of microcapsules leave on for 1 minute, then sucked on the filter SCHOTT 16 class then washed with acetone, dried in a desiccator over calcium chloride.

Received 0,540 g of white powder. The yield was 90%.

EXAMPLE 7. Obtaining microcapsules Ceftriaxone in polyvinyl alcohol (PVA), a ratio of 1:3

To 18 g of 5% aqueous solution of PVA added 0.3 g of Ceftriaxone powder and 0.02 g of the product OS-20 as surfactant. 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 10 ml of carbinol as the first precipitator, and then 50 ml of acetone as the second. Received suspense the microcapsules leave on for 1 minute, then sucked on the filter SCHOTT 16 class then washed with acetone, dried in a desiccator over calcium chloride.

Received 1,128 g of white powder. The yield was 94%.

EXAMPLE 8. Obtaining microcapsules Ceftriaxone in polyvinyl alcohol (PVA), a ratio of 1:1

To 12 g of 5% aqueous solution of PVA added 0.6 g of Ceftriaxone powder and 0.02 g of the product OS-20 as surfactant. 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 10 ml of carbinol as the first precipitator, and then 30 ml of acetone as the second. The resulting suspension of microcapsules leave on for 1 minute, then sucked on the filter SCHOTT 16 class then washed with acetone, dried in a desiccator over calcium chloride.

Received 1,092 g of white powder. The yield was 91%.

EXAMPLE 9. Obtaining microcapsules Ceftriaxone in polyvinyl alcohol (PVA), a ratio of 3:1

To 6 g of 5% aqueous solution of PVA added 0.9 g of Ceftriaxone powder and 0.02 g of the product OS-20 as surfactant. 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 drop is poured 5 ml of carbinol as the first precipitator, and then 20 ml of acetone as the second. The resulting suspension of microcapsules leave on for 1 minute, then sucked on the filter SCHOTT 16 class then washed with acetone, dried in a desiccator over calcium chloride.

Obtained 1.08 g of white powder. The yield was 90%.

EXAMPLE 10. Obtaining microcapsules Ceftriaxone in polyvinyl alcohol (PVA), a ratio of 5:1

To 6 g of 5% aqueous solution of PVA added 1.5 g of Ceftriaxone powder and 0.02 g of the product OS-20 as surfactant. 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 carbinol as the first precipitator, and then 20 ml of acetone as the second. The resulting suspension of microcapsules leave on for 1 minute, then sucked on the filter SCHOTT 16 class then washed with acetone, dried in a desiccator over calcium chloride.

Received 1.73 g of white powder. The yield was 96%.

PRIMER 11. Obtaining microcapsules is anticipated in polyvinyl alcohol (PVA), a ratio of 1:5

To 10 g of 5% aqueous solution of PVA added 0.1 g of Cefazolin powder and 0.02 g of the product OS-20 as surfactant. The resulting mixture was put on a magnetic stirrer and include mixing. After dilution to the of mponents the reaction mixture until a clear solution is formed very slowly poured dropwise 5 ml of carbinol as the first precipitator, and then 25 ml of acetone as the second. The resulting suspension of microcapsules leave on for 1 minute, then sucked on the filter SCHOTT 16 class then washed with acetone, dried in a desiccator over calcium chloride.

Obtained 0.52 g of white powder. The yield was 86%.

EXAMPLE 12. Obtaining microcapsules is anticipated in polyvinyl alcohol (PVA), a ratio of 1:3

To 18 g of 5% aqueous solution of PVA added 0.3 g of Cefazolin powder and 0.02 g of the product OS-20 as surfactant. 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 10 ml of carbinol as the first precipitator, and then 50 ml of acetone as the second. The resulting suspension of microcapsules leave on for 1 minute, then sucked on the filter SCHOTT 16 class then washed with acetone, dried in a desiccator over calcium chloride.

Obtained 1.04 g of white powder. The yield was 87%.

EXAMPLE 13. Obtaining microcapsules is anticipated in polyvinyl alcohol (PVA), a ratio of 1:1

To 12 g of 5% aqueous solution of PVA added 0.6 g of Cefazolin powder and 0.02 g of the product OS-20 as surfactant. The resulting mixture was put on a magnetic stirrer and include mixing. After the dissolution of whom is onenew the reaction mixture until a clear solution is formed very slowly poured dropwise 10 ml of carbinol as the first precipitator, and then 30 ml of acetone as the second. The resulting suspension of microcapsules leave on for 1 minute, then sucked on the filter SCHOTT 16 class then washed with acetone, dried in a desiccator over calcium chloride.

Received of 1.02 g of white powder. The yield was 85%.

PRIMER 14. Obtaining microcapsules is anticipated in polyvinyl alcohol (PVA), a ratio of 3:1

To 6 g of 5% aqueous solution of PVA added 0.9 g of Cefazolin powder and 0.02 g of the product OS-20 as surfactant. 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 carbinol as the first precipitator, and then 20 ml of acetone as the second. The resulting suspension of microcapsules leave on for 1 minute, then sucked on the filter SCHOTT 16 class then washed with acetone, dried in a desiccator over calcium chloride.

Obtained 1.06 g of white powder. The yield was 88%.

EXAMPLE 15. Obtaining microcapsules is anticipated in polyvinyl alcohol (PVA), a ratio of 3:2

To 12 g of 5% aqueous solution of PVA added 0.9 g of Cefazolin powder and 0.02 g of the product OS-20 as surfactant. The resulting mixture was put on a magnetic stirrer and include mixing. After dissolving the components of the clients of the reaction mixture until a clear solution is formed very slowly poured dropwise 5 ml of carbinol as the first precipitator, and then 20 ml of acetone as the second. The resulting suspension of microcapsules leave on for 1 minute, then sucked on the filter SCHOTT 16 class then washed with acetone, dried in a desiccator over calcium chloride.

Obtained 1.3 g of white powder. The yield was 86%.

EXAMPLE 16. Obtaining microcapsules is anticipated in polyvinyl alcohol (PVA), a ratio of 5:1

To 6 g of 5% aqueous solution of PVA added 1.5 g of Cefazolin powder and 0.02 g of the product OS-20 as surfactant. 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 carbinol as the first precipitator, and then 20 ml of acetone as the second. The resulting suspension of microcapsules leave on for 1 minute, then sucked on the filter SCHOTT 16 class then washed with acetone, dried in a desiccator over calcium chloride.

Received 1,53 g of white powder. The yield was 85%.

Thus, the obtained microcapsules 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 equipped with the I.

The data presented above shows that all samples have a spherical shape, the outputs range from 85 to 96%. It should also be noted that the process of production of microcapsules is accelerated by the introduction of the second precipitator - carbinol because of the rapid coagulation, which facilitates filtering as a way of separating the obtained microcapsules.

The proposed method is suitable for the pharmaceutical industry because of its speed and ease of acquisition and allocation of microcapsules cephalosporins related to β-lactam antibiotics, in polyvinyl alcohol.

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 - polyvinyl alcohol, which is then precipitated by adding as herstories carbinol and acetone at 25°C.



 

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