Method of obtaining microcapsules of medications of cephalosporin group in konjac gum in toluene

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to pharmaceutical industry, in particular to method of obtaining microcapsules of medications of cephalosporin group. Method of obtaining microcapsules of medications of cephalosporin group consists in the following: surface-active substance is added to konjac solution in toluene, after that, powder of preparation of cephalosporin group is dissolved in dimethylformamide and transferred into solution of konjac in toluene, after formation by antibiotic of its own solid phase carbinol and distilled water are added in drops, obtained suspension of microcapsules is filtered, washed with acetone and dried, with process of obtaining microcapsules being carried out under specified conditions.

EFFECT: method ensures simplification and acceleration of the process of obtaining microcapsules of water-soluble medications.

8 ex

 

The invention relates to the field of microencapsulation of drugs of cephalosporin group related to β-lactam antibiotics, in Konakovo gum physico-chemical method.

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 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 AC 9/52, AK 9/16, AC 9/10, Russian Federation, published 10.11.1997, method for obtaining solid non-porous microspheres comprising 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 separation of the resulting microspheres into fractions by size. The suspension is intended for administration by parenteral injection, contains an effective amount specified m is crosher, distributed in a 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, 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 disadvantages of the method are the use of a ball mill 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 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 RA is the mayor of 100-800 microns in diameter and consists of 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; obtaining microcapsules by the method of suspension polymerization; complexity; the duration of the process.

In Pat. 2139046, IPC AC 9/50, AK 49/00, AK 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.

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

In Pat. 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. 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 the van 27.06.2009, The 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 (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. WO/2010/076360 ES, IPC B01J 13/00; AC 9/14; AC 9/10; AC 9/12 published 08.07.2010, proposed a new method for obtaining solid micro - and nanoparticles with a homogeneous structure with a particle size less than 10 μm, where the treated solid connections have a natural crystalline, amorphous, polymorphous, and other conditions associated with the reference compound. The method allows to obtain a solid micro - and nanoparticles with a substantially spheroidal morphology.

The disadvantage of the proposed method is the complexity of the process that leads to the production of capsules with a floating output.

In Pat. WO/2010/119041 EP, IPC A23L 1/00, SDA is published 21.10.2010, method for obtaining the beads that contains the active ingredient encapsulated in the gel matrix whey protein, comprising denatured protein, serum and active components. The invention relates to a method for production of beads that contain components such as probiotic bacteria. The method of receiving beads includes a stage production of beads in accordance with the method of the invention and the subsequent curing of the beads in the solution of the anionic polysaccharide with a pH of 4.6 and below for at least 10, 30, 60, 90, 120, 180 minutes. Examples of suitable anionic polysaccharides: pectins, alginates, carrageenan. Ideally whey protein is heat-denaturing, although other methods of denaturation is also applicable, for example, denaturation induced by pressure. In a preferred embodiment, whey protein denaturised at a temperature of from 75°C to 80°C, is properly within from 30 minutes to 50 minutes. Typically, whey protein mixed with thermal denaturation. Accordingly, the concentration of the whey protein is from 5 to 15%, preferably from 7 to 12%, and ideally from 9 to 11% (weight / volume). Typically, the process is carried out by filtering through a lot of filters with a gradual decrease in pore size. Ideally, the filter thin acadimie submicron pore size, for example from 0.1 to 0.9 microns. The preferred method of obtaining the beads is a method using vibration encapsulation (Inotech, Switzerland) and machinery manufacturing Nisco Engineering AG. Typically, the nozzles have openings 100 and 600 μm, and ideally about 150 microns.

The disadvantage of this method is the use of special equipment (vibration encapsulation (Inotech, Switzerland)), obtaining microcapsules by denaturation of the protein, the complexity of the allocation obtained by this method of microcapsules filtering using multiple filters, which makes the process longer.

In Pat. WO/2011/003805 EP, IPC B01J 13/18; B65D 83/14; C08G 18/00, 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.

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 exposed the deposits.

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/2011/150138 US, IPC C11D 3/37; B01J 13/08; C11D 17/00, published on 01.12.2011 described a method of producing microcapsules solid water-soluble agents polymerization method.

The disadvantages of this method are the complexity and duration of the process.

In Pat. WO/2011/127030 US IPC AC 8/11; B01J 2/00; B01J 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 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-4M8 Dryer from Losert, Belgium)).

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-4M8 Dryer from Losert, 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, a method for obtaining a dispersion of encapsulated solid particles in a liquid medium, comprising: a) ismalic the tion of the composition, 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 the 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 are useful as colorants in inks, especially ink jet printing for the pharmaceutical industry this technique is not applicable.

In Pat. WO/2011/056935 US, IPC C11D 17/00; AC 8/11; B01J 13/02; C11D 3/50, published on 12.05.2011, describes how to obtain microcapsules with a size of 15 microns. As the shell material proposed polymers of the group consisting of polyethylene, polyamides, polystyrene, polyisoprenes, polycarbonates, polyesters, polyacrylates, polyureas, polyurethanes, polyolefins, polysaccharides, epoxy resins, vinyl polymers and mixtures thereof. The proposed polymer membranes are sufficiently impervious core material and materials in the environment is the first environment, in which is encapsulated agent, the benefit will be used to provide benefits that will be received. The core of the encapsulated agents may include perfume, silicone oils, waxes, hydrocarbons, higher fatty acids, essential oils, lipids, cooling the skin fluids, vitamins, sunscreens, antioxidants, glycerin, catalysts, bleach particles, particles of silicon dioxide and other

Disadvantages of the proposed method are the complexity, the length of the process, using as the shells of the microcapsules polymers of synthetic origin, and mixtures thereof.

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 group of cephalosporins in Konakovo gums, reducing losses receive the Institute of microcapsules (increase in mass).

The solution of the technical problem is achieved by the fact that as the shell of the microcapsules used Konakovo gum, with 6 g of 5% solution of konjac in toluene added 0.01 g E with as a surfactant, and 0.1 g of powder antibiotic of cephalosporin group dissolved in 1 ml of dimethylformamide and transfer it into a solution of konjac in toluene, after the formation of the antibiotic independent solid phase very slowly added dropwise 3 ml of carbinol and 1 ml of distilled water, the resulting suspension of microcapsules is filtered off, washed with acetone and dried, the process of production of microcapsules is carried out at a temperature of 25°C no special equipment.

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

Required for microencapsulation of Konakova gum was industrial production under the trade name konjac cercon and konjac gum 3600.

EXAMPLE 1 Obtaining microcapsules Cefotaxime in konjak cerocon in toluene, the ratio of 1:3

To 6 g of 5% solution of konjac cerocon in toluene added 0.01 g E with as surfactants. The resulting mixture was put on a magnetic stirrer and include p is remesiana. 0.1 g of the powder Cefotaxime dissolved in 1 ml of dimethylformamide and transferred into a solution of konjac cerocon in toluene. After the formation of the Cefotaxime independent solid phase very slowly added dropwise 3 ml of carbinol, and then 1 ml of distilled water. 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 of 0.38 g of white powder. The yield was 94%.

EXAMPLE 2 Obtaining microcapsules Cefotaxime in konjac gum 3600 in toluene, the ratio of 1:3

To 6 g of 5% solution of konjac gum 3600 in toluene added 0.01 g E with as surfactants. The resulting mixture was put on a magnetic stirrer and include mixing. 0.1 g of the powder Cefotaxime dissolved in 1 ml of dimethylformamide and transferred into a solution of konjac gum 3600 in toluene. After the formation of the Cefotaxime independent solid phase very slowly added dropwise 3 ml of carbinol, and then 1 ml of distilled water. The resulting suspension of microcapsules is filtered by the filter SCHOTT 16 class then washed with acetone, dried in a desiccator over calcium chloride.

Obtained 0.36 g of a white to cream color powder. The yield was 91%.

EXAMPLE 3 Obtaining microcapsules Ceftriaxone in the konjak cerocon in toluene, the ratio of 1:3

To 6 g of 5% solution of konjac cerocon the toluene added 0.01 g E with as surfactants. The resulting mixture was put on a magnetic stirrer and include mixing. 0.1 g of Ceftriaxone powder dissolved in 1 ml of dimethylformamide and transferred into a solution of konjac cerocon in toluene. After the formation of the Ceftriaxone independent solid phase very slowly added dropwise 3 ml of carbinol, and then 1 ml of distilled water. 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 of 0.38 g of white powder. The yield was 95%.

EXAMPLE 4 Obtaining microcapsules Ceftriaxone in konjac gum 3600 in toluene, the ratio of 1:3

To 6 g of 5% solution of konjac gum 3600 in toluene added 0.01 g E with as surfactants. The resulting mixture was put on a magnetic stirrer and include mixing. 0.1 g of Ceftriaxone powder dissolved in 1 ml of dimethylformamide and transferred into a solution of konjac gum 3600 in toluene. After the formation of the Ceftriaxone independent solid phase very slowly added dropwise 3 ml of carbinol, and then 1 ml of distilled water. 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 of 0.38 g of white to cream color powder. The yield was 96%.

EXAMPLE 5 Obtaining the microcapsules refusal is on the konjak cerocon in toluene, the ratio of 1:3

To 6 g of 5% solution of konjac cerocon in toluene added 0.01 g E with as surfactants. The resulting mixture was put on a magnetic stirrer and include mixing. 0.1 g of Cefazolin powder dissolved in 1 ml of dimethylformamide and transferred into a solution of konjac cerocon in toluene. After the formation of Cefazolin independent solid phase very slowly added dropwise 3 ml of carbinol, and then 1 ml of distilled water. The resulting suspension of microcapsules is filtered by the filter SCHOTT 16 class then washed with acetone, dried in a desiccator over calcium chloride.

Obtained 0.35 g of a white powder. The yield was 88%.

EXAMPLE 6 Obtaining microcapsules is anticipated in the konjac gum 3600 in toluene, the ratio of 1:3

To 6 g of 5% solution of konjac gum 3600 in toluene added 0.01 g E with as surfactants. The resulting mixture was put on a magnetic stirrer and include mixing. 0.1 g of Cefazolin powder dissolved in 1 ml of dimethylformamide and transferred into a solution of konjac gum 3600 in toluene. After the formation of the anticipated independent solid phase very slowly added dropwise 3 ml of carbinol, and then 1 ml of distilled water. The resulting suspension of microcapsules is filtered by the filter SCHOTT 16 class then washed with acetone, dried in a desiccator over calcium chloride.

On the scientific 0.35 g of white to cream color powder. The yield was 87%.

EXAMPLE 7 to Obtain microcapsules of cefepime in the konjak cerocon in toluene, the ratio of 1:3

To 6 g of 5% solution of konjac cerocon in toluene added 0.01 g E with as surfactants. The resulting mixture was put on a magnetic stirrer and include mixing. 0.1 g of cefepime powder dissolved in 1 ml of dimethylformamide and transferred into a solution of konjac cerocon in toluene. After the formation of Cefazolin independent solid phase very slowly added dropwise 3 ml of carbinol, and then 1 ml of distilled water. 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 0.39 g of white powder. The yield was 98%.

EXAMPLE 8 to Obtain microcapsules of cefepime in konjac gum 3600 in toluene, the ratio of 1:3

To 6 g of 5% solution of konjac gum 3600 in toluene added 0.01 g E with as surfactants. The resulting mixture was put on a magnetic stirrer and include mixing. 0.1 g of cefepime powder dissolved in 1 ml of dimethylformamide and transferred into a solution of konjac gum 3600 in toluene. After the formation of the anticipated independent solid phase very slowly added dropwise 3 ml of carbinol, and then 1 ml of distilled water. The resulting suspension of microcapsules is filtered by the filter SCHOTT 16 is Lassa long washed with acetone, dried in a desiccator over calcium chloride.

Received 0.39 g of white to cream color powder. The yield was 97%.

The obtained microcapsules drug group cephalos-Parinov related to β-lactam antibiotics, in Konakovo gum physico-chemical method for the deposition nerastvorim using carbinol and toluene as nerastvorimaya. The process is simple to perform and lasts for 15 minutes, requires no special equipment.

Konakova gum is widely used in the pharmaceutical industry drugs for weight loss and regulation chair, as a binder in tablets.

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 Konakovo gums.

The method of producing microcapsules drugs group of cephalosporins in Konakovo gum in toluene, characterized in that as the shell of the microcapsules used Konakovo gum, with 6 g of 5% solution of konjac in toluene added 0.01 g E with as a surfactant, and 0.1 g of powder antibiotic of cephalosporin group dissolved in 1 ml of dimethylformamide and transfer it into a solution to the of NACA in toluene, after the formation of the antibiotic independent solid phase very slowly added dropwise 3 ml of carbinol and 1 ml of distilled water, the resulting suspension of microcapsules is filtered off, washed with acetone and dried, the process of production of microcapsules is carried out at a temperature of 25°C no special equipment.



 

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3 ex

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1 tbl

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4 ex

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7 ex

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8 ex

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3 ex

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6 ex

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2 ex

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3 ex

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3 cl, 4 dwg, 1 ex

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6 ex

FIELD: medicine, pharmaceutics.

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4 ex

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4 ex

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1 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to drug microencapsulation, particularly for preparing fenbendazole microcapsules. The method is characterised by the fact that a microcapsule coating is carboxymethyl cellulose; fenbendazole dissolved in dioxane or dimethyl sulphoxide (DMSO), or dimethyl formamide (DMFM) is dispersed into the solution of sodium carboxymethyl cellulose in dioxane in the presence of the preparation E472c; further, isopropanol and distilled water are added; the prepared microcapsule suspension is filtered and dried; a process of microcapsules is conducted at 25°C for 20 minutes with no special equipment; with nucleus/polymer ratio making 1:3.

EFFECT: invention provides simplifying and accelerating the process of preparing the fenbendazole microcapsules in carboxymethyl cellulose, reducing losses in preparing the microcapsules (higher weight yield).

3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a method for preparing drug microcapsules of cephalosporins in konjak gum in dioxane. According to the declared method, a konjak gum solution in dioxane is added with a surfactant that is a cephalosporin powder pre-dissolved in ethanol, and with carbinol after cephalosporin forms an independent solid phase. The prepared microcapsule suspension is filtered, washed in acetone and dried in a drying oven.

EFFECT: invention enables simplifying and accelerating the process of water-soluble drug microcapsules of cephalosporins in konjak gum, as well as increasing a mass yield.

4 ex

FIELD: chemistry.

SUBSTANCE: invention discloses a pharmaceutical composition in the form of a solution, having nootropic and neuromodulating activity, characterised by that it contains N-carbamoylmethyl-4-phenyl-2-pyrrolidone as an agent, hydroxyethyl starch as an auxiliary substance and water for injection. The invention also relates to a method of producing such a pharmaceutical composition, which includes adding hydroxyethyl starch to the water for injection which is preheated to 85-90°C and mixing until complete dissolution, adding N-carbamoylmethyl-4-phenyl-2-pyrrolidone powder and mixing at temperature of 75-85°C until complete dissolution, adding water for injection to obtain the end volume of the solution and mixing once more, holding the obtained solution for 35-40 minutes at temperature of 75-85°C, cooling to 20-30°C, sterilising by filtering through filters with pore diameter of 0.22 mcm and packing in ampoules, which are further sterilised for 8 minutes at temperature of 120°C.

EFFECT: composition is effective, safe and can be used for a long period of time.

2 cl, 3 ex

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