Formulation of combined pharmaceutical chondroprotective drug

FIELD: medicine, pharmaceutics.

SUBSTANCE: declared formulation of the combined pharmaceutical chondroprotective drug presented in a solid dosage form contains as active substances sodium chondroitin sulphate and glucosamine sulphate sodium chloride, a binding agent, antifriction substances, an aerating agent, an excipient; the composition is film-coated. The ingredients are taken in proportions, wt %: sodium chondroitin sulphate - 10-35, glucosamine sulphate sodium chloride - 15-45, the binding agent (low-molecular povidone and potato starch) - 3.1-11, the antifriction substances (aerosil, calcium stearate and talc) - 2.7-5, the aerating agent (kollidon) - 1.7-10, the excipient (ludipress) - 10-44.2. The coating ingredients are taken in proportions, wt %: film-forming material (hypromellose) - 1-2, a plasticiser (macrogol and propylene glycol) - 1-1.8, a pigment (titanium dioxide) - 0.5-1.

EFFECT: auxiliary ingredients enables high release rate of a tabletted mass, complete drug absorption and shelf-life stability of all measures.

3 dwg, 3 ex

 

The invention relates to medicine, in particular for medical preparations in the form of tablets, film coated liner for therapeutic purposes with the existing substances in the form of sulfated polysaccharides.

Known solid dosage form of chondroitin sulfate, containing as active ingredient chondroitin sulfate, as well as auxiliary substances - friction, binder and filler (patent RF №2254862, IPC AC 31/737, from 24.05.2004,, publ. 27.06.2005,).

The disadvantage of this drug is the lack of efficiency of the regeneration of cartilage tissue in the joints and spine with his admission of patients, due to insufficient quantity of active ingredient.

The specified medication selected by the applicant as the closest analogue (prototype).

The task of the invention is solved by the authors, is to provide a composition in the form of tablets for oral administration with an optimal ratio of active substances - chondroitin sodium sulfate and glucosamine sulfate sodium chloride solution, providing stimulation of regeneration of cartilage tissue in the joints and spine, but at the expense included in the composition of auxiliary substances, to ensure the high strength of the composition, the rapid release of active ingredients and high pokazatel the dissolution.

This object is achieved in that in the composition of the combined pharmaceutical hondroprotektor made in the form of a solid dosage form comprising as active ingredients chondroitin sodium sulfate and glucosamine sulfate sodium chloride, binder, anti-friction agents, baking powder, filler, when this composition is covered with a film cover. According to the invention the ratio of ingredients of the composition is, wt.%: chondroitin sulfate sodium - 10-35, glucosamine sulfate sodium chloride - 15-45, binder, which is a low molecular weight povidone and starch - 3,1-11, anti-friction substances Aerosil, calcium stearate or talc - 2,7-5, the baking powder, which Calligonum CL - 1,7-10, filler, which ludipress - 10-44,2, and the ratio of ingredients of the shell is, wt.%: the film, which hypromellose, - 1-2, plasticizer, which macrogol or propylene glycol - 1-1,8, the pigment being titanium dioxide, and 0.5-1.

Execution ingredients active ingredients in the compositions of the claimed ratio, i.e. chondroitin sulfate sodium 10-35%, glucosamine sulfate sodium chloride 15-45% is optimal for effective stimulation of regeneration of cartilage tissue in the joints and spine with the use of the drug with the estva sick, since the active substances involved in the synthesis of connective tissue, helping to prevent the destruction of cartilage.

Glucosamine sulfate sodium chloride enhances the production of cartilage matrix and provide non-specific protection against chemical damage to the cartilage and metabolic destruction caused by nonsteroidal anti-inflammatory drugs, as well as its own moderate anti-inflammatory effect.

Chondroitin sulfate sodium is an additional substrate for the formation of healthy cartilage matrix, stimulates the formation hyaluronan, the synthesis of proteoglycans and collagen type II, and protects hyaluronan from enzymatic degradation and from the damaging effects of free radicals, supports the viscosity of synovial fluid, stimulates cartilage repair mechanisms and inhibits the activity of those enzymes that break down cartilage. When osteoarthritis treatment relieves symptoms and reduces the need for non-steroidal anti-inflammatory drugs.

The presence of a binder in the form of low molecular weight povidone (Fund 42-0345-4368-03 Eur. Ph) and potato starch(GOST 7699-78, variety "extra" Eur. Ph), having a viscosity ratio of 3.1-11%, provides for the manufacture of tablet mass education granules ingredients tablet m is ssy, providing good compressibility and strength of the tablets.

The presence of anti-friction substances in the form of Aerosil (Eur. Ph, USP) calcium stearate (Eur. Ph, USP) and talc (TU 2432-003-48602470, Eur. Ph, USP)with sliding and lubricating properties, with a ratio of 2.7-5%, provides uniform after tableting mass from the hopper into the matrix, which ensures the accuracy and consistency of dosage. Also these substances prevent the formation of scratches and chips on the surface of the tablet cores.

The presence of baking powder in the form of kollidon DL (ND 42-8871-05, Eur. Ph), with the declared value, i.e. a 1.7-10%, provides a fast mechanical destruction tablets in gastric juice, the release and subsequent absorption of active substances.

The presence of filler in the form of ludipress (ND 42-8803-05, Eur. Ph) in the claimed ratio, i.e. 10-44,2% provides constant weight pills, promotes good flowability tablet mass and forming tablets-cores.

The presence of the ingredients of the shell in the claimed ratio, i.e. a film-forming agent in the form of hypromellose ((Eur. Ph, USP) 1-2%, allows to obtain a durable film that protects the core from exposure to the environment and at the same time, quickly dissolving under the influence of acids and enzymes of the gastric juice, the plasticizer in the form of a macrogol (TU 2483-008-71150986-2006, USP) and propylene glycol (a(Eur. Ph, USP) 1-1,8%, called the em to ensure the elasticity of the formed film, that enables you to evenly apply it on the entire surface of the core pigment in the form of titanium dioxide (FS 42-0104-03, (Eur. Ph, USP)) 0,5-1% helps provide uniform white color film coating.

Thus, included in the composition excipients give tableting mass necessary technological properties, good desirement and the compressibility and provide tablets of the required quality. Chosen ratio of auxiliary components ensures a high rate of release and the completeness of absorption of drugs, and also provides stability for all quality indicators during the entire shelf life.

As a result of patent trials have revealed similar technical solutions, characterized by the claimed combination of features that allows us to conclude that the claimed technical solution has a "novelty" and "inventive step", can find application in the pharmaceutical industry, i.e. is "industrially applicable".

The invention is illustrated by drawings, where figure 1 is a plot of time of dissolution of the claimed compositions of the claimed ratio of active ingredients and auxiliary substances according to the specific example 1; figure 2 - graph of time dissolve the texts of the claimed compositions of the claimed ratio of active ingredients and auxiliary substances according to the specific example 2; figure 3 - graph of time of dissolution of the claimed compositions of the claimed ratio of active ingredients and auxiliary substances according to the specific example 3.

The claimed composition is combined pharmaceutical hondroprotektor made in the form of a solid dosage form that contains as active ingredients chondroitin sodium sulfate and glucosamine sulfate sodium chloride, binder, anti-friction agents, baking powder, filler, when this composition is covered with a film cover, and the ratio of ingredients of the composition is, wt.%: chondroitin sulfate sodium - 10-35, glucosamine sulfate sodium chloride - 15-45, binder, which is a low molecular weight povidone and starch - 3,1-11, anti-friction substances Aerosil, calcium stearate or talc - 2,7-5, the baking powder, which Calligonum CL, - 1.7 to 10, filler, which ludipress, - 10-44,2, and the ratio of ingredients of the shell is, wt.%: the film, which hypromellose, - 1-2, plasticizer, which macrogol or propylene glycol, - 1-1,8, the pigment being titanium dioxide, and 0.5-1.

The invention is illustrated by examples of specific performance of the composition.

Example 1

The composition is prepared in the following ratio of ingredients, wt.%: glucose is in the sodium sulfate - 15, chondroitin sulfate sodium - 10, Aerosil - 1, calcium stearate - 1, talc, 3 - kollidon CL - 10, low molecular weight povidone - 10, potato starch - 1, ludipress - 44,2, hypromellose - 2, macrogol - 1,5, propylene glycol and 0.3, titanium dioxide 1.

First prepare the granulate glucosamine sulfate sodium chloride, which in the mixer load ground substance glucosamine sulfate sodium chloride, kollidon CL and Aerosil, the mixture was mixed thoroughly and added in several portions combined binder consisting of starch paste and low molecular weight povidone. Wet weight granularit, dried at a temperature not exceeding 40°C to a residual moisture of 4-6% and the dry granulate is passed through a granulator with a cell diameter of 3 mm.

Then prepare the granulate chondroitin sulfate sodium, which in the mixer load substance chondroitin sodium sulfate and kollidon CL. The mixture was thoroughly stirred and portions add an alcoholic solution of povidone obtained by dissolving the sample of povidone in the estimated amount of ethyl alcohol. Wet weight granularit and dried at a temperature not exceeding 40°C to a residual moisture content of 12-16%. The dry granulate is passed through a granulator with a cell diameter of 3 mm.

Dry pellets of glucosamine sulfate sodium chloride and chondroitin sulfate sodium unite and optivault mixture of stearate cal the Oia, talc, kollidon CL and ludipress. The mixture is stirred and tabletirujut.

Next, prepare the film-forming solution using hypromellose, macrogol, propylene glycol and titanium dioxide. As solvents are methylene chloride and ethyl alcohol in a 2:1 ratio. The obtained tablet cover film-forming solution.

In the above example, the ratio of active substances allows to obtain a composition with which it is possible to achieve the desired result is to stimulate the regeneration of cartilage tissue in the joints and spine.

And the ratio of auxiliary substances, i.e. the maximum number of the stated ratios, provide: binder - good compressibility and strength tablets; anti-friction substance - even after tableting mass; baking powder - fast mechanical destruction of the tablets in the stomach with the release and subsequent absorption of the active substances; filler - constant weight of the tablets.

The membrane obtained with the specified in the example, the ratio of ingredients, has no elasticity, making it difficult to cover it tableting mass.

Example 2

The composition is prepared in the following ratio of ingredients, wt.%: glucosamine sulfate sodium - 35,4, chondroitin sulfate sodium - 28,2 Aerosil - 0,5, ka is ice stearate - 0,96, talc - 2,9, kollidon CL - 9,6, low molecular weight povidone - 4,9, potato starch - 0.3, ludipress - 13,33, hypromellose - 1,54, macrogol - 1,3, propylene glycol - 0,14, titanium dioxide - 0,93.

First prepare the granulate glucosamine sulfate sodium chloride, which in the mixer load ground substance glucosamine sulfate sodium chloride, kollidon CL and Aerosil, the mixture was mixed thoroughly and added in several portions combined binder consisting of starch paste and low molecular weight povidone. Wet weight granularit, dried at a temperature not exceeding 40°C to a residual moisture of 4-6%, and the dry granulate is passed through a granulator with a cell diameter of 3 mm.

Then prepare the substance of chondroitin sulfate sodium, which in the mixer load substance chondroitin sodium sulfate and kollidon CL. The mixture was thoroughly stirred and portions add an alcoholic solution of PVP, obtained by dissolving the sample of povidone in the estimated amount of ethyl alcohol. Wet weight granularit and dried at a temperature not exceeding 40°C to a residual moisture content of 12-16%. The dry granulate is passed through a granulator with a cell diameter of 3 mm.

Dry the granules glucosamine sodium sulphate and chondroitin sulphate sodium unite and optivault a mixture of calcium stearate, talc, kollidon CL and Ludi press. The mixture is stirred and tabla is irout.

Next, prepare the film-forming solution using hypromellose, macrogol, propylene glycol and titanium dioxide. As solvents are methylene chloride and ethyl alcohol in a 2:1 ratio. The obtained tablet cover film-forming solution.

In the above example, the aforementioned ratio of active substances allows to obtain a composition with which it is possible to achieve the desired result is to stimulate the regeneration of cartilage tissue in the joints and spine, i.e. their ratio is optimal.

The specified ratio of auxiliary substances is also optimal for achieving good pressuemosti and strength tablets, uniform expiration tableting mass rapid dissolution of the tablet in the stomach with the release and subsequent absorption of the active substances, to obtain tablets constant weight.

The membrane obtained with the specified in the example, the ratio of ingredients, has an elasticity that provides uniform coverage it tableting mass.

Thus, the ratio of active ingredients and auxiliary components allows to form tablet cores with tensile fracture 120-160 N and abrasion resistance of not less than 97%. Composition of tablets provide release of the active substances n is less than 75% within 60 minutes.

Example 3

The composition is prepared in the following ratio of ingredients, wt.%: glucosamine sulfate sodium - 45, chondroitin sulfate sodium - 35, Aerosil - 0,2, calcium stearate and 0.5, talc - 2.0, kollidon CL - 1,7, low molecular weight povidone - 3.0, potato starch - 0.1, ludipress - 10,0, hypromellose - 1,0, macrogol - 0.9, propylene glycol, and 0.1, titanium dioxide and 0.5.

First prepare the granulate glucosamine sulfate sodium chloride, which in the mixer load ground substance glucosamine sulfate sodium chloride, kollidon CL and Aerosil, the mixture was mixed thoroughly and added in several portions combined binder consisting of starch paste and low molecular weight povidone. Wet weight granularit, dried at a temperature not exceeding 40°C to a residual moisture of 4-6% and the dry granulate is passed through a granulator with a cell diameter of 3 mm.

Then prepare the substance of chondroitin sulfate sodium, which in the mixer load substance chondroitin sodium sulfate and kollidon CL. The mixture was thoroughly stirred and portions add an alcoholic solution of PVP. Wet weight granularit and dried at a temperature not exceeding 40°C to a residual moisture content of 12-16%. The dry granulate is passed through a granulator with a cell diameter of 3 mm.

Dry the granules glucosamine sodium sulphate and chondroitin sulphate sodium unite and optivault mixture is calcium stearate, talc, kollidon CL and ludipress. The mixture is stirred and tabletirujut.

Next, prepare the film-forming solution using hypromellose, macrogol, propylene glycol and titanium dioxide. As solvents are methylene chloride and ethyl alcohol in a 2:1 ratio. The obtained tablet cover film-forming solution.

In the above example, the ratio of active substances maximum that may increase the toxicity of tablets, slow release of active substances and their dissolution.

And the ratio of auxiliary substances, i.e. the minimum number of the stated ratios, provides: binder - good compressibility and strength tablets; anti-friction substance - even after tableting mass; baking powder - fast mechanical destruction of the tablets in the stomach with the release and subsequent absorption of the active substances; filler - constant weight of the tablets.

The membrane obtained with the specified in the example, the ratio of ingredients, not too fluid, making it difficult to cover it tableting mass.

Thus, the claimed composition is combined pharmaceutical hondroprotektor stimulates the regeneration of cartilage tissue in the joints and spine, and part compositioncontainer substances give tableting mass necessary technological properties, good desirement and the compressibility and provide tablets of the required quality. Chosen ratio of auxiliary components ensures a high rate of release and the completeness of absorption of drugs, and also provides stability for all quality indicators during the entire shelf life.

The composition of the combined pharmaceutical hondroprotektor made in the form of a solid dosage form comprising as active ingredients chondroitin sodium sulfate and glucosamine sulfate sodium chloride, binder, anti-friction agents, baking powder, filler, when this composition is covered with a film cover, characterized in that the ratio of ingredients of the composition is, wt.%: chondroitin sulfate sodium - 10-35, glucosamine sulfate sodium chloride - 15-45, binder, which is a low molecular weight povidone and starch potato, - 3,1-11, anti-friction substances Aerosil, calcium stearate and talc - 2,7-5, the baking powder, which Calligonum CL, - 1.7 to 10, filler, which ludipress, - 10-44,2, and the ratio of ingredients of the shell is, wt.%: the film, which hypromellose, - 1-2, plasticizer, which macrogol and propylene glycol, - 1-1,8, the pigment being titanium dioxide, and 0.5-1.



 

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,

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42 cl, 2 dwg, 4 tbl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention claims per oral drug form of neramexam with modified release, which is applied for long therapy of patients with such diseases and states as dimentia in Alzheimer's disease and neuropathic pain. Neramexane is dispersed inside hard matrix, which contains release-regulating filler. Filler is selected from copolymer of polyvinylpyrrolidone and vinyl acetate, hydroxypropylmethylcellulose. Hydroxypropylmethylcellulose is present in mixture with microsrystalline cellulose. Content of said filler is selected in such a way as to obtain profile of neramexan release in vitro, characterised by dissolution time of, at least, 1 hour for amount of neramexane, constituting 50 wt %.

EFFECT: profile of release ensures concentrations of neramexane in plasma with fluctuation index 0,4 or lower with introduction of matrix tablet of neramexane one time per day at steady state.

23 cl, 4 tbl, 7 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to chemical-pharmaceutical industry, namely to creation of pharmaceutical composition in form of hard peroral drug form for treatment of gastrointestinal tract diseases. Pharmaceutical composition contains the following ingredients: trimebutin maleate, lactose, colloidal silicon dioxide, talc, corn starch, magnesium stearate.

EFFECT: obtained pharmaceutical composition ensures high clinical effect.

5 cl, 2 ex, 1 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, and consists in development of a new dosage of the preparation 6-methyl-2-ethyl-3-hydroxypyridine succinate providing modified release of an active substance. A unit dosage form contains 6-methyl-2-ethyl-3-hydroxypyridine succinate in amount 30.0-70.0 wt %, as a release modifier - cellulose derivatives and/or polyacrylic resins in amount 1.0-20.0 wt %, as an excipient - microcrystalline cellulose in amount 20.0-50.0 wt % and lubricants. The unit dosage form represents a tablet or a capsule consisting of a variety of small dense spheroids containing 6-methyl-2-ethyl-3-hydroxypyridine succinate as a major component. A combination of matrix and instant, coated and uncoated spheroids enables preparation of a drug in the various dosage forms with controlled release rate.

EFFECT: invention allows to produce the unit dosage forms of the preparation 6-methyl-2-ethyl-3-hydroxypyridine succinate for certain treatment regimens of various diseases.

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to pharmaceutical industry and solid dosage form of calcium atorvastatin. Solid dosage form consists of core containing the following components, wt %: calcium atorvastatin - 1.5-25; microcrystalline cellulose - 2-30; calcium carbonate - 5-30; croscarmellose sodium - 0.5-5; stearic acid and/or its salt - 0.5-1.04; lactose "Lactopress Spraydry" - balance; and shell containing the following components, wt %: polyethylene glycol - 6-28; titanium dioxide - 10-35; talc - 5-25; silicon emulsion - 0.05-4; dye - 0-3; polyvinyl alcohol - balance.

EFFECT: invention provides for production of calcium atorvastatin pills satisfying requirements of National pharmacopeia XI.

4 cl, 5 tbl

FIELD: medicine.

SUBSTANCE: invention concerns a solid oral dosage form composition containing therapeutically effective amount of aliskiren or its pharmaceutically acceptable salt in amount exceeding 46 wt %. The oral dosage form represents a tablet or a film-coated tablet. Aliskiren tablet is made by wet granulation with using mixed organic solvents or organic binding solutions.

EFFECT: elimination of aqueous granulation provides high stability of the dosage form of aliskiren and prolonged shelf-life.

18 cl, 2 ex

FIELD: food industry.

SUBSTANCE: present invention relates to gastral retentive composition containing active agent granulated together with the mixture of the first and the second gelatinating agents and mentioned composition production method the first gelatinating agent is a mixture of microcrystalline cellulose and sodium-carboxymethyl cellulose the second gelatinating agent is a compound with viscosity of 1% water solution which makes at least 600 centipoise at 25°C active agent is chosen from antibacterial compounds such as fluoroquinolones, antidiabetic compounds and antihypertensive medicinal agents.

EFFECT: invention provides gastral retentive composition with sustained release effect, which stays in stomach; medical agent has maximal absorption with improved therapeutic action there.

24 cl, 2 ex

FIELD: medicine.

SUBSTANCE: group of inventions refers to veterinary science. A method for improving xenobiotic deactivation in an animal involves animal feeding with a food composition containing lipoic acid where lipoic acid is found in an amount at least 150 portions/million. A kit applicable for introduction of lipoic acid to the animal comprises in separate containers in a single package or in separate containers in a virtual package as it may be required, at least one lipoic acid in the food composition where lipoic acid is found in the amount at least 150 portions/million and at least one of: (1) one or more ingredients applicable for consumption by animals, (2) instructions to combine lipoic acid and one or more ingredients applicable for consumption by animals for improving xenobiotic deactivation by liver, and (3) instructions to use lipoic acid and one or more ingredients applicable for consumption by animals. The food composition applicable for improving xenobiotic deactivation by liver in animals, contains a life-sustaining amount of nutrients and lipoic acid more than 150 portions/million.

EFFECT: group of inventions provides improved liver function in animals.

14 cl, 1 ex, 1 dwg

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