Physicochemical method for preparing cephalosporin microcapsules

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to microcapsulation of cephalosporins related to β-lactam antibiotics. A method for preparing cephalosporin microcapsules is implemented by physicochemical non-solvent addition. That involves using two non-solvents that are carbinol and isopropyl alcohol taken in ratio 1:4. The microcapsule yield makes more than 90%.

EFFECT: method for cephalosporin microcapsules provides accelerating the process for preparing and simplifying the method.

3 ex

 

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

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. 2095055, IPC A61K 9/52, A61K 9/16, A61K 9/10 of the Russian Federation published 10.11.1997 method for obtaining a 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 temperatures 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 distributed in Pharma is efticiency acceptable liquid vector, and the pharmaceutically active substance is insoluble microspheres in a specified liquid medium.

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

In Pat. 2091071, IPC A61K 35/10 Russian Federation 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, which can lead to the destruction of the microcapsules and the duration of the process.

In Pat. 2076765, IPC B01D 9/02 Russian Federation 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. 2101010, IPC A61K 9/52, A61K 9/50, A61K 9/22, A61K 9/20, A61K 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 which comprises pharmaceutical kernel crystalline ibuprofen and polymer coating, including 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. 2139046, IPC A61K 9/50, A61K 49/00, A61K 51/00 Russian Federation 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.

Nedostatkami predlozennogo 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. 2159037, the PC A01N 25/28, A01N 25/30 Russian Federation published 20.11.2000 method for obtaining microcapsules 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 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. 2359662, IPC A61K 009/56, A61J 003/07, B01J 013/02, A23L 001/00 published 27.06.2009 Russian Federalprison 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 air 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).

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 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, the use of ultraviolet radiation.

In Pat. WO/2011/127030 US, IPC A61K 8/11; B01J B01J 2/00 13/06; C11D 3/37; C11D 3/39; C11D 17/00 published on 13.10.2011 proposed several methods for producing microcapsules: interfacial polymerization, thermoanaerobium separation of the phases, spray drying, evaporation of the solvent and other

The disadvantages of the proposed methods is the complexity, duration processes, as well as the use of special equipment (filter (Albet, Dassel, Germany), spray dryer for collecting particles (Spray-M Dryer from ProCepT, Belgium)).

In Pat. WO/2011/104526 GB, IPC B01J 13/00; B01J 13/14; SV 67/00; C09D 11/02 published on 01.09.2011 method for obtaining a dispersion of encapsulated solid particles in a liquid medium, comprising: a) grinding compositions, including solid, liquid medium and a polyurethane dispersant with an acid number of from 0.55 to 3.5 mmol per gram of dispersant, the composition comprises from 5 to 40 parts of the polyurethane dispersant per 100 parts of solid product, by weight; and b) crosslinking the polyurethane dispersant in the presence of solid and liquid medium, so as to encapsulate the solid particles, which polyurethane dispersant contains less than 10% by weight of the recurring elements of polymeric alcohols.

Disadvantages of the proposed method are the complexity and duration of the process of production of microcapsules, and that the encapsulated particles of the proposed method is useful as & rsquo; s the th in the ink, especially ink jet printing for the pharmaceutical industry this technique is not applicable.

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, characterized in that upon receipt of the microcapsules physico-chemical deposition method by nerastvorim uses two precipitator - carbinol and isopropyl alcohol. As the primary wasp-makers in the proposed method is used isopropyl alcohol and a carbinol - as updat the Executive, the retrieval process is carried out without special equipment.

A distinctive feature of the proposed method is the use of isopropyl alcohol as the primary precipitator and carbinol as an additional when obtaining microcapsules physico-chemical method for the deposition aristotelem.

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

EXAMPLE 1 Obtaining microcapsules Cefotaxime in polyvinyl alcohol (PVA) using carbinol and isopropyl alcohol as a precipitating, the ratio of 1:1

To 6 g of 5% aqueous solution of PVA added 0.3 g of powder Cefotaxime and 0.02 g of the drug E (ester of glycerol with one or two molecules of dietary fatty acids and one or two molecules of citric acid, and citric acid, as Tihonova may be etherification other glycerides and as oxanilate - other fatty acids. Free acid groups can be neutralized with sodium) as a surfactant. The resulting mixture was put on a magnetic stirrer and include mixing. After the dissolution of the components of the reaction mixture to about who produced a clear solution is slowly poured dropwise 5 ml of carbinol as the first precipitator, and then 20 ml of isopropyl alcohol 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 of white powder. The yield was 94%.

EXAMPLE 2 Obtaining microcapsules Ceftriaxone in polyvinyl alcohol (PVA) using carbinol and isopropyl alcohol as a precipitating, the ratio of 1:1

To 6 g of 5% aqueous solution of PVA added 0.3 g of Ceftriaxone powder and 0.02 g of the drug A with 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 carbinol as the first precipitator, and then 20 ml of isopropyl alcohol 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 0,576 g of white powder. The yield was 96%.

EXAMPLE 3 Method for producing microcapsules is anticipated in polyvinyl alcohol (PVA) using carbinol and isopropyl alcohol as a precipitating, the ratio of 1:1

To 6 g of 5% aqueous solution of PVA added 0.3 g of Cefazolin powder and 0.02 g of the drug A with in to the amount of surface-active substances. The resulting mixture was put on a magnetic stirrer and include stirring.

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 isopropyl alcohol 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 0,552 g of white powder. The yield was 92%.

The obtained microcapsules drug group cephalosporins related to β antibiotics in polyvinyl alcohol physico-chemical method for the deposition nerastvorim using isopropyl alcohol as the primary precipitator and carbinol - as optional, which increases output and accelerates the process of microencapsulation. The process is simple to perform and lasts for 20 minutes, requires no special equipment.

It should be noted that obtaining microcapsules of water-soluble drugs in water-soluble polymers is a particularly difficult task. To achieve this goal, the selection of the method of production of microcapsules. For microencapsulation was selected physico-chemical method due to expressnet and easy implementation. As the precipitating use is demonstrated isopropyl alcohol and carbinol, since polyvinyl alcohol is isopropanol and the carbinol.

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, in polyvinyl alcohol.

The method of producing microcapsules drugs of cephalosporin group of physico-chemical method, characterized in that upon receipt of the microcapsules physico-chemical deposition method by nerastvorim uses two precipitator - carbinol and isopropyl alcohol, taken by volume in the ratio of 1:4.



 

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