Method for preparing drug microcapsules of cephalosporin in konjac gum in chloroform

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to microcapsulation of drug preparations of cephalosporins referred to β-lactam antibiotics in konjac gum by physical-chemical precipitation in a non-solvent. Konjac gum is used as a microcapsule membrane. The microcapsules are prepared by physical-chemical precipitation in the non-solvent with using two precipitation agents - carbinol and chloroform. The process of microcapsules is carried out at 25°C with no special equipment required.

EFFECT: method according to the invention provides simplifying and accelerating the process of microcapsules of drug preparations of cephalosporins, and reducing losses (higher weight yield).

4 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 for the deposition aristotelem.

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 of the Russian Federation published 10.11.1997 method for obtaining a solid non-porous microspheres which comprises 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 perfor the number of these microspheres, 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. 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 of a drug, which 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 on the basis of macrolevel 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, which takes 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 method for obtaining microcapsules reacts is her polymerization 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 the article "Razrabotka microencapsulated and gel products and materials for various industries. Russian chemical journal, 2001, .XLV, No. 5-6, s-135 is described a method of producing microcapsules of drugs by the method of gas-phase polymerization, since the authors considered unsuitable method of chemical koatservatsii from aqueous media for microencapsulation of drugs due to the fact that most of them are water-soluble. The process of microencapsulation by the method of gas-phase polymerization using n-xylylene includes the following basic stages: evaporation dimer n-xylylene (170°C), thermal decomposition of it into the pyrolysis furnace (650°C at a residual pressure of 0.5 mm Hg), the transfer of the reaction products in the "cold" chamber of polymerization (20°C, the residual pressure of 0.1 mm Hg), deposition and polymerization on the surface of the protected object. Luggage polymerization is performed in the form of a rotating drum, the optimal soon the be for powder coating 30 rpm The thickness of the shell is governed by the time of coating. This method is suitable for the encapsulation of any solids (except prone to intense sublimation). The resulting poly-n-xylylene vysokokritichnyh polymer with high orientation and dense packing, provides a conformal coating.

Disadvantages of the proposed method are the complexity and duration of the process, using the method of gas-phase polymerization, which makes the method inapplicable to obtain microcapsules of drugs in polymers protein nature due to the denaturation of proteins at high temperatures.

In the article "Development of micro - and nano drug delivery", Russian chemical journal, 2008, .LII, No. 1, p.48-57 presents a method of obtaining microcapsules included with proteins, which does not significantly reduce their biological activity carried out by the process of interfacial crosslinking of soluble starch or hydroxyethylamine and bovine serum albumin (BSA) using terephthaloyl chloride. The proteinase inhibitor is Aprotinin, either native or protected with an active center was microcapsular in his introduction to the composition of the aqueous phase. Tapered shape liofilizovannyh particles indicates obtaining microcapsules or particles tank types. Sentence is blennie thus microcapsules are not damaged after lyophilization and easily restored its spherical shape after rehydration in a buffered environment. The pH value of the aqueous phase was crucial in obtaining a solid microcapsules with high output.

The disadvantage of the proposed method of producing microcapsules is the complexity of the process, and hence floating output target capsules.

In Pat. 2173140 IPC AC 9/50, AK 9/127 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-cavity setup, which has the 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 9/56, A61J 3/07, B01J 13/02, A23L 1/00 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 is found 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 and duration of the process.

In Pat. WO/2010/119041 EP IPC A23L 1/00 published 21.10.2010 method for obtaining the beads containing 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 probe the political 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 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 product is filtered through a set of filters with a gradual decrease in pore size. Ideally, the fine filter has a 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 way is as 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 published on 13.01.2011 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 2006.01.01. B05D 007/00, VS 3/02 US 003/02; VS 11/00 US 011/00; B05D 1/18 B05D 001/18; B05D 3/02 B05D 003/02; B05D 3/06 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/2011/150138 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 of execution and shall littelest 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

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 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% the 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 proposed the method useful as colorants in ink, 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 described a method of producing 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 in which the agent is encapsulated, 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.

In Pat. WO/2011/160733 EP IPC B01J 13/16 published on 29.12.2011 describes a method for Mick is kapsul, which contain shell and core water-insoluble materials. An aqueous solution of protective colloid and a solution of a mixture of at least two structurally different bifunctional diisocyanate (a) and (C), insoluble in water, gather together before the formation of the emulsion, is then added to the mixture of bifunctional amines and heated to a temperature of at least 60°C until the formation of microcapsules.

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. 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 production of microcapsules of water-soluble drugs group of cephalosporins in Konakovo gums, reducing losses upon receipt of the microcapsules (the expansion of the exit by weight).

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 as the shell of the microcapsules is Konakova gum, and obtaining microcapsules physico-chemical deposition method by nerastvorim using two precipitators - carbinol and chloroform, the retrieval process is carried out without special equipment.

A distinctive feature of the proposed method is the use as the shell of the microcapsules drug group cephalosporins related to β-lactam antibiotics in Konakovo gums, and obtaining microcapsules physico-chemical deposition method by nerastvorim using two precipitators - carbinol and chloroform.

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 Ceftriaxone in konjac gum 3600 using carbine is and chloroform as the precipitating, the ratio of 1:3

To 6 g of 5% solution of konjac gum 3600 in chloroform 0.01 g of the drug Is as surfactants. The resulting mixture was put on a magnetic stirrer and include stirring, 0.1 g of Ceftriaxone powder dissolved in 0.5 ml of water and transferred into a solution of konjac gum 3600 in chloroform. After the formation of the Ceftriaxone independent solid phase very slowly added dropwise 5 ml of carbinol and 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 0,396 g of white powder. The yield was 99%.

EXAMPLE 2 Obtaining microcapsules Ceftriaxone in the konjak cerocon using carbinol and chloroform as the precipitating, the ratio of 1:3

To 6 g of 5% solution of konjac cerocon in chloroform 0.01 g of the drug Is (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 surface-active substances. The resulting mixture was put on a magnetic stirrer and include stirring, 0.1 g of powder of Ceftriaxone restore the t in 0.5 ml of water and transferred into a solution of konjac cerocon in chloroform. After the formation of the Ceftriaxone independent solid phase very slowly added dropwise 5 ml of carbinol and 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 0,396 g of white powder. The yield was 99%.

EXAMPLE 3 Obtaining microcapsules of cefepime in konjac gum 3600 using carbinol and chloroform as the precipitating, the ratio of 1:3

To 6 g of 5% solution of konjac gum 3600 in chloroform 0.01 g of the drug Is as surfactants. The resulting mixture was put on a magnetic stirrer and include stirring, 0.1 g of cefepime powder dissolved in 0.5 ml of water and transferred into a solution of konjac gum 3600 in chloroform. After the formation of the cefepime independent solid phase very slowly added dropwise 5 ml of carbinol and 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 powder. The yield was 90%.

EXAMPLE 4 Obtaining microcapsules of cefepime in the konjak cerocon using carbinol and chloroform as the precipitating, the ratio of 1:3

To 6 g of 5% solution of konjac cerocon in chloroform 0.01 g of the drug As as over OSTO-active substances. The resulting mixture was put on a magnetic stirrer and include stirring, 0.1 g of cefepime powder dissolved in 0.5 ml of water and transferred into a solution of konjac cerocon in chloroform. After the formation of the cefepime independent solid phase very slowly added dropwise 5 ml of carbinol and 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 0,364 g of white powder. The yield was 91%.

The obtained microcapsules drug group cephalosporins related to β-lactam antibiotics, in Konakovo gum physico-chemical method for the deposition nerastvorim using carbinol and chloroform 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. In the Russian Federation is permitted in food products according to TI in an amount up to 10 g/kg of product (p. 3.6.23 SanPiN 2.3.2.1293-03). Technological function: thickener, gelling, stabilizer, means for tableting. Composition: neutral polysaccharide glucomannan consists of D-glucose and D-mannose in a ratio of 1:4 to 2:3.

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 chloroform, characterized in that as the shell of the microcapsules is Konakova gum, and obtaining microcapsules carry out physico-chemical deposition method by nerastvorim using two precipitators - carbinol and chloroform, the retrieval process is carried out at 25°C without special equipment.



 

Same patents:

FIELD: chemistry.

SUBSTANCE: invention relates to microencapsulation, particularly microencapsulation of pesticides. The method consists in physical-chemical precipitation using two precipitants - butanol and ethanol. The microcapsule cladding is sodium carboxymethyl cellulose.

EFFECT: invention increases mass output of microcapsules while simplifying the process of producing microcapsules.

7 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to microencapsulation of drugs through the example of rivanol which can be used as an antimicrobial, antifungal topical preparation. A method for preparing microcaplues of rivanol in a water-soluble polymer representing polyvinyl alcohol or polyvinyl pyrrolidone is implemented by physical-chemical precipitation with a solvent wherein a precipitant is acetone. The process is carried out at 25°C with no special equipment required.

EFFECT: method for preparing the microcapsules of rivanol provides simplifying the process of microencapsulation.

13 dwg, 5 ex

FIELD: nanotechnology.

SUBSTANCE: device (50) for preparation of nanoparticles on a continuous basis comprises the first feeding device (1a) with the first feeding load (9) connected to the source (7) of the starting material, the first reactor (2) comprising the first heated reaction zone (13), the second reactor (3) comprising the second heated reaction zone (15), where all the said devices are connected to the channel of the material flow successively in the said order, at least one pressure control unit (18) mounted in the said channel of the material flow, a mixer (5) mounted in the said channel of the material flow between the first reactor (2) and the second reactor (3), the second feeding device (lb) with the second feeding pump (10) connected to the source (8) of the starting material, and the second feeding pump (10) is in liquid junction with the mixer (5), the control device (22) made with the ability to control the pressure value setting with the said pressure control unit (18) and/or the temperature value of the said heated reaction zones (13 and 15). The device is characterised in that after each heated reaction zone (13) in the channel of the material flow the appropriate cooling device (14, 16) is mounted for reducing the size of the nanoparticles in the process of their preparation, and the cooling devices (14, 16) are additionally made with the ability to cease this process of nanoparticles preparation. Also the invention relates to use of the device for preparation of nanoparticles/nanoemulsions/colloidal solutions.

EFFECT: invention enables to obtain nanoparticles which properties can be modified in the course of this process.

8 cl, 10 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical microcapsulation of cephalosporins related to β-lactam antibiotics. As a microcapsule shell, the method of pharmaceutical microcapsulation of cephalosporins uses konjac gum; the microcapsules are prepared by physical-chemical technology implying the precipitation in a non-solvent using two precipitants - carbinol and diethyl ester in ratio 1:3; the method is conducted at 25°C with no special equipment.

EFFECT: invention provides simplified and accelerated preparation of the water-soluble pharmaceutical microcapsules of cephalosporins in konjac gum, loss reduction in preparing the microcapsules (higher yield-mass).

3 ex

FIELD: medicine.

SUBSTANCE: claimed invention relates to medicine and describes method of obtaining delivering particles of fragrance, containing core material and envelope, said envelope at least partially surrounds said core material and at least 75% of said delivering particles of fragrance are characterised by tensile strength from approximately 0.2 MPa to approximately 10 MPa, with particle size from approximately 1 micron to approximately 80 micron and thickness of particle walls from approximately 60 nm to approximately 250 nm; and said delivering particles of fragrance are characterised by release of fragrance from 0% to approximately 30%. In addition to creation of possibility to reduce number of agent which produces favourable impact, such particles make it possible to extend spectrum of applied agents which produce favourable impact.

EFFECT: in cases of application in compositions, for instance, detergents, or compositions for fabric care, such particles increase efficiency of delivery of agent which produces favourable impact, making it possible to use reduced amounts of agents which produce favourable impact.

11 cl, 9 tbl, 13 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a powder coating composition obtained from aqueous dispersion containing polymer-encapsulated particles, said particles including particles encapsulated in a brittle polymer which can easily break up under ambient conditions. The invention also discloses a method of preparing an aqueous dispersion of particles encapsulated in a brittle polymer, a base which is at least partially coated with a coating deposited from said composition, a multilayer composite coating, a method of preparing a powder coating composition, a method of preparing an aqueous dispersion of particles encapsulated in a brittle polymer and a powder coating composition formed from said dispersion prepared using said method, as well as a reflecting surface which is at least partially coated with a layer which gives the colour of an uncovered coating deposited from disclosed powder coating compositions.

EFFECT: obtaining aqueous dispersion of particles encapsulated in a brittle polymer in which repeated agglomeration of particles is minimised and which enables to obtain a powder coating composition which contains multiple polymer-encapsulated particles having maximum turbidity so that the coating has absorption or reflection in the visible spectrum which is close to that of the given coating.

22 cl, 14 ex, 1 tbl

FIELD: process engineering.

SUBSTANCE: invention relates to production of minor spherical particles of active agent in sole liquid phase solution. Sole liquid phase comprises active agent, agent facilitating phase separation and first thinner. Phase separation is induced at controller rate in solution to cause separation active agent into "fluid-solid" and to form liquid and solid phases. Note here that inducing comprises solution cooling. Solid phase contains minor spherical particles of active agent. Liquid phase comprises agent facilitating phase separation and thinner. Minor spherical particles feature particle size varying from 0.01 mcm to about 200 mcm.

EFFECT: minor spherical particles of active agent in sole liquid phase solution.

77 cl, 49 dwg, 4 tbl, 36 ex

FIELD: process engineering.

SUBSTANCE: invention maybe used for efficient fire extinguishing, fast cooling of overheated structures and production of lower-flammability compounds. Microcapsules have a micro-sphere-like core containing water or water solution in gel state, main shell around said core to provide for core stable shape and composition and rule out water evaporation therefrom the core, and, additionally, comprises outer shell with lyophilic properties. Versions of proposed methods comprises producing aforesaid core via interaction of appropriate initial water solutions to be placed in microsphere and containing appropriate components of the shell with components of solutions to be precipitated and used for producing and cross-linking of gel, and producing additional lyophilic shell via interaction of components of initial solutions with appropriate components in organic medium.

EFFECT: high efficiency in fire extinguishing or fast cooling of overheated structures.

21 cl, 1 tbl, 10 ex

FIELD: chemistry.

SUBSTANCE: invention relates to use of polymer material, and specificaly to use of particulate polymer material as an active agent carrier. The polymer material is a polymer obtained from copolymerisation of pyrrole with quadratic or croconic acid or its derivative.

EFFECT: use in accordance with the invention enables to use polymer material as a composition in form of particles as an absorbent or prolonged release agent.

16 cl, 8 dwg, 1 tbl, 10 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a solid re-dispersible emulsion which is a direct emulsion of fabric softener encapsulated in a polysaccharide shell which is stabilised by ions of polyvalent metals selected from Ca2+, Sr2+, Ba2+, Al3+, Cu2+, Zn2+, where the shell is initially insoluble in water but becomes soluble in water through ion donation. The polysaccharide is biodegradable and is selected from a group comprising alginates and carrageenans. Similar solid re-dispersible emulsions are primarily used in agents for washing or taking care of clothes. Powdered fabric softeners are easy to store, apportion and, if necessary, combine with powdered detergents during production.

EFFECT: invention enables production of fabric softeners previously produced as liquid compositions in solid powdered form.

14 cl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to microencapsulation of drugs through the example of rivanol which can be used as an antimicrobial, antifungal topical preparation. A method for preparing microcaplues of rivanol in a water-soluble polymer representing polyvinyl alcohol or polyvinyl pyrrolidone is implemented by physical-chemical precipitation with a solvent wherein a precipitant is acetone. The process is carried out at 25°C with no special equipment required.

EFFECT: method for preparing the microcapsules of rivanol provides simplifying the process of microencapsulation.

13 dwg, 5 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical microcapsulation of cephalosporins related to β-lactam antibiotics. As a microcapsule shell, the method of pharmaceutical microcapsulation of cephalosporins uses konjac gum; the microcapsules are prepared by physical-chemical technology implying the precipitation in a non-solvent using two precipitants - carbinol and diethyl ester in ratio 1:3; the method is conducted at 25°C with no special equipment.

EFFECT: invention provides simplified and accelerated preparation of the water-soluble pharmaceutical microcapsules of cephalosporins in konjac gum, loss reduction in preparing the microcapsules (higher yield-mass).

3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: declared group of inventions refers to a pharmacological composition for intranasal introduction for cerebral delivery, and a method for preparing said composition. The declared composition comprises a container base formed by porous particles of calcium carbonate and titanium dioxide of particle size 100-5000 nm and a pharmacologically active component - loperamide. The container surface is modified by surfactants specified in polysorbates, or by polymers specified in a group containing glycosaminoglycanes and polypeptides, or their combination. A method for preparing the pharmacological composition consists in preparing the container base by porous particle synthesis, sorption of loperamide in its pore spaces and modification of the container surface by polymers and surfactants by container incubation in their solutions.

EFFECT: invention provides preparing the pharmacological composition which is applicable for cerebral loperamide delivery after the intranasal introduction.

5 cl, 5 dwg, 1 ex

FIELD: medicine.

SUBSTANCE: invention relates to composition for peroral introduction, which possesses properties of modified release. According to invention composition includes pharmaceutically acceptable excipients and complex medication-ion-exchanging resin with coating with modified release, which contains pharmaceutically active medication, combined with pharmaceutically acceptable ion-exchanging resin. Complex has solidified barrier coating with high rupture strength, water-permeable, water-insoluble, which contains polyvinyl acetate polymer, stabiliser and efficient amount of plastifier. Said coating is in fact non-sticky, when applied onto complex in absence of anti-adhesive preparation, if composition presents tablet, complex medication-ion-exchanging resin with coating additionally contains release-retarding substance in matrix together with complex medication-ion-exchanging resin. Invention also relates to product with modified release, including package which contains composition described above.

EFFECT: invention ensures regulated prolonged active agent release without breaking coating integrity, without application of water-soluble impregnating substances and without agglomeration of complex particles during application of coating.

27 cl, 22 ex

FIELD: medicine.

SUBSTANCE: there are described oral dosage forms of risedronate containing safe and effective amount of a pharmaceutical composition containing risedronate, a chelating agent and an agent for effective delayed release of risedronate and the chelating agent in small intestine. The pharmaceutical composition is directly released in a small intestine of a mammal with ensuring pharmaceutically effective absorption of bisphosphonate together with or without food or drinks. Present invention essentially reduces interaction between risedronate and food or drinks which leads to that the active component of bisphosphonate becomes inaccessible to absorption. Thus, the final oral dosage form can be taken with and without food. Further, present invention covers delivery of risedronate and the chelating agent in a small intestine, essentially reducing irritation of upper gastrointestinal tract associated with bisphosphonate therapy. These advantages simplify previous, complicated regimens and can lead to more complete observance of the bisphosphonate therapy regimen.

EFFECT: present invention essentially reduces interaction between risedronate and food or drinks which leads to that the active component of bisphosphonate becomes inaccessible to absorption.

23 cl, 12 ex

FIELD: medicine.

SUBSTANCE: invention refers to a carrier for drugs, biologically active substances, biological objects used in medicine for diagnostics and treatment in pharmaceutical industry. The carrier represents a material sensitive to external magnetic or electric fields and consisting of magnetic or ferroelectric material filmed with biocompatible thermosensitive, biodegradable polymer and/or dispersed in thermosensitive medium properties of which change with varying temperature relative to that of human body within 15.9 to 42°C. The magnetic or ferroelectric materials are made of substance with great magnetocaloric or electrocaloric component effect 1 to 13 K, have temperature of magnetic or ferroelectric phase transition within temperature range 33 to 37°C, and are chosen from the group including rare-earth, transition and precious metals, their alloys and compounds.

EFFECT: invention also concerns methods of controlled drug delivery by means of such carrier with enabling release thereof (regulated desorption) in the preset point.

32 cl, 9 ex

FIELD: medicine; pharmacology.

SUBSTANCE: minitablets have a kernel and an external cover which makes 2-15% of gross weight of minitablets, the kernel of the specified minitablets, includes a venlafaxine hydrochloride, microcrystallic cellulose and a polyvinylpyrolidone, and the specified cover includes polymer, insoluble in water, and a polymer, soluble in water.

EFFECT: provision of levels of concentration in a blood plasma above the minimum therapeutic concentration during the long period of time.

10 cl, 1 dwg, 1 tbl, 5 ex

FIELD: medicine.

SUBSTANCE: invention discovers improved composition for profile control of active compound release through the digestive tract, including particles, especially granules, containing the active compounds. They are covered with coating material, solution of which depends on pH value, or polymethacrylate material, solution of which, for preference, depends on pH value, the definite thickness, desirable place and speed of the active compound release. In preferable compositions two or more particles, in which particles of each multitude are covered with the coating material, the solution which depends on pH value, or polymethacrylate material, of different thickness in comparison with the particles of each other multitude, are contained in capsules with enterosoluble coating and provide the active substance release in different desirable places of the digestive tract.

EFFECT: provision of active substance release in desirable places of digestive tract.

28 cl, 7 dwg, 9 ex

FIELD: medicine, pharmacy.

SUBSTANCE: invention relates to sustained-release medicinal formulation composition comprising venlafaxin hydrochloride as an active component. In this formulation venlafaxin hydrochloride in common with a binding agent is applied on inert core as lozenge form (nonpareil) followed applying with a cover-insulating polymeric layer for providing stability and additional cover with external polymeric layer providing the sustained-release of venlafaxin hydrochloride.

EFFECT: improved and valuable properties of composition.

18 cl, 1 tbl, 4 ex

FIELD: medicine.

SUBSTANCE: the [present innovation deals with manufacturing intestinally soluble capsular forms of medicinal preparations, particularly, to the technology for creating capsular membranes of improved protective properties. The innovation deals with the method for obtaining capsular membrane out of calcium alginate due to successive keeping capsular nuclei in solutions of sodium alginate and calcium chloride, in which sodium alginate solution at concentration of 1.5-2.0% (weight/volume) should be pre-treated with ultrasound for about 8-10 at the power of 400-450 W/sq. cm. Calcium chloride solution should be applied at concentration of 2.0-2.5%, moreover, the terms for keeping capsular nuclei in solutions of sodium alginate and calcium chloride corresponds to 5 min in every solution.

EFFECT: higher efficiency.

1 dwg, 3 ex, 1 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry and represents a method for preparing adsorbed male bee brood differing by the fact that 1 portion of a homogenate of make bee brood and 3-30 weight portions of an adsorbent are taken; the adsorbent is either lactose, or glucose, or fructose, or any combinations of these substances to be mixed and delivered to drying not later than 55 minutes once the male bee brood removed from honeycombs, and dried under no-heat vacuum to moisture no more than 1.5%.

EFFECT: invention provides maintaining and stabilising all the biological characteristics of the male bee brood for a long period of time.

8 cl

Up!