Pharmaceutical composition having an anabolic effect

 

The invention relates to the field of medicine and relates to pharmaceutical compositions for the treatment of complex and coronary heart disease, myocardial infarction, myocardiodystrophy, rhythm disturbances associated with the use of cardiac glycosides. The invention lies in the fact that the tool is made in the form of a solid dosage form that includes a core and a shell. The core contains Riboxin as active substance and additives target - gelatin, sugar, starch, calcium stearate or magnesium, with a specific content components. The shell consists of methylcellulose and/or oksipropilmetiltselljulozy, tween-80, titanium dioxide, vaseline oil, dye. The invention provides rapid release of the active substance in the gastrointestinal tract, the drug has a shelf life of 3 years. 3 C.p. f-crystals, 1 table.

The invention relates to the field of medicine and is suitable for the treatment of ischemic heart disease, myocardial infarction, myocardiodystrophy, rhythm disturbances associated with the use of cardiac glycosides, liver disease and for the treatment of urokoproporfirii.

Among the means regulating anabolic pri M. D. Medicines, so 2. Kharkov: Torsing, 1998, S. 173). The connection is derived (nuke) purine precursor of ATP and increases the activity of some enzymes of the Krebs cycle, stimulates the synthesis of nucleotides, has a positive effect on metabolic processes in the myocardium, improves coronary circulation, increases the energy balance of the myocardium.

Riboxin, like most substances, medicinal substances, has no ability to direct pelletizing. Therefore, to create stable for quite a long time, meet pharmacopoeial requirements of the dosage form should be used excipients in amounts determined pharmaceutical and therapeutic usefulness.

There are various dosage forms containing Riboxin tablets, solutions for intravenous administration.

Known drug "Rekabet" (RF, 20006224, 1994, a 61 K 31/00) containing Riboxin and biologically active substances: Riboflavin, pyridoxine, nicotinamide, ascorbic and glutamic acid, potassium chloride is in the following ratio, wt.%: Riboxin - 33,33-37,47 Riboflavin - 0.70 To 0.83 Pyridoxine - 0,70-0,83 Ascorbic acid-assured not disclosed.

The tool has a membrane stabilizing and antioxidant therapeutic effect, low toxicity, which allows its use in cardiovascular disease in geriatrically practice, persons of elderly and senile age.

In the industrial regulations 64-0206-13-90 for the production of tablets Riboxin 0.2 g, coated, developed by JSC "Biosynthesis", described composition for the preparation of medicines, anabolic action, in the form of tablets, most similar in composition to offer, including a core containing Riboxin as active ingredient, and other ingredients: stearic acid, methylcellulose as a binder agent, sugar powder, starch, and a shell consisting of beeswax, methyl cellulose, tartrazine, tween-80, titanium dioxide.

The ingredients contained in the kernel in the following ratio, in g per 1 tablet: Riboxin - 0,2
Stearic acid - 0,0027
Methylcellulose - 0,00323
Sugar - 0,0108
Starch - Rest
in the shell, in g per 1 tablet:
Beeswax - 0,001418
Methylcellulose - 0,00618
Tartrazine - 0,0000316
Tween-80 - 0,00083
Titanium dioxide - 0,000578
To get specified the tax solution of methylcellulose, mix to a smooth, dry, granularit, optivault the remaining starch and stearic acid, tabletirujut, applied film coating. 71,43% by weight is contained in the dosage form of starch is introduced into the composition outrivaled agent, the rest - in the composition of the filler.

Use in a well-known tool based on Riboxin specified kernel and above shell does not allow to obtain the required dosage form performance raspadaemosti and dissolution, it has a shelf life of 2 years.

The objective of the proposed invention is a solid dosage form of a drug, anabolic action, which has a longer shelf life, meets pharmacopoeial requirements and rapidly releases the active substance in the gastrointestinal tract.

This object is achieved in that the proposed anabolic means includes a core, containing the active substance Riboxin and as the target additives gelatin, sugar, calcium stearate or magnesium, starch, and a shell consisting of methylcellulose and/or oksipropilmetiltselljulozy, tween-80, titanium dioxide, oil vaselin,2
Gelatin - 0,003264
Sugar - 0,01632
Magnesium stearate or calcium - 0,00272
Starch - Rest
The claimed ratio of ingredients found experimentally and provides the necessary kernel of the composition. The use in the composition of gelatin instead of methylcellulose provides rapid release of the active substance from the core of the proposed dosage form. Raspadaemost kernel is 10 min, when it is dissolved in 45 minutes on Wednesday dissolution becomes more than 90% of Riboxin just made the remedy and more than 75% after 3 years and 3 months storage.

Use moisturizing composition of sugar solution has a positive effect on the stabilization indicator dissolve during the entire storage period. The increase in sugar content in the core of the inventive dosage form increases its stability during storage, which allows to increase the acceptable shelf life of up to 3 years.

Stearic acid is replaced by magnesium stearate or calcium. Its effectiveness as a moving substance they are the same and ensure proper operation of the tabletting process, but stearate or calcium more available.

A new pharmaceutical composition of uluchshit appearance of the medicinal product, increase stability during storage, improves raspadaemost and dissolution of tablets.

The optimal ratio of ingredients in the shell is, g per 1 tablet:
The methylcellulose and/or oksipropilmetiltselljuloza - 0,003396
Tween-80 - 0,00085
Titanium dioxide - 0,00068
Vaseline oil - 0,001063
Dye - 0,000011-0,000135
As the shell most acceptable was OPMC or its mixture with MC, as a polishing agent substances used vaseline oil, allowing you to get better coverage due to the uniformity of its application, having the necessary strength for the subsequent packaging of the medicinal product.

As the dye can be applied tropeolin Oh, KF 6001 or E-104.

The way to obtain a new composition involves several steps. Pre-prepared aqueous solution of gelatin and sugar and moisturize them mix the sifted powders of Riboxin and starch. The wet paste is dried, granularit. Granules optivault mixture of starch and calcium stearate or magnesium, and 76,4% of the mass contained in the dosage form of starch is injected in a mixture with other ingredients, and 23.6 per cent composition apadravya mixture. Change the percentage content of robodyne active substances in the inventive pharmaceutical compositions.

The method is illustrated by the following examples.

Example 1.

The mixture 748 g Riboxin with 129,4 g starch mix, moisturize 410 ml of an aqueous solution containing 12,09 gelatin and 60,44 sugar. The wet mass is dried at a temperature (40-50)oC to a residual moisture content (21)% and granularit.The granulate optivault 40 g starch, 10,07 g of calcium stearate, tabletirujut receive 970 cores with an average weight of 0.27, the Strength of the cores 91 N, raspadaemost 10 min. kernel is applied 3.94 g of paraffin oil, then film-forming composition containing 12,58 g oksipropilmetiltselljulozy, 0,0407 g tropeolin Oh, 2,52 g of titanium dioxide and 3.15 g of tween-80 in a mixture of 0.6 l of ethyl alcohol and 0.6 l of methylene chloride. Get 970 g of tablets with an average weight 0,272 g, which satisfy the requirements of the pharmaceutical agent.

Example 2.

The mixture 748 g Riboxin with 129,4 g starch mix, moisturize 410 ml of an aqueous solution containing 12,09 gelatin and 60,44 sugar. The wet mass is dried at a temperature (40-50)oC to a residual moisture content (21)% and granularit. The granulate optivault 40 g starch, 10,07 g of magnesium stearate, tabletirujut receive 970 cores with an average weight of 0.27, the Strength of the cores 91 N, raspadaemost 10 minutes For the poison is, ,0407 g tropeolin Oh, 2,52 g of titanium dioxide and 3.15 g of tween-80 in a mixture of 0.6 l of ethyl alcohol and 0.6 l of methylene chloride. Get 970 Ableton with an average weight of 0.2 g that satisfy the requirements of the pharmaceutical agent.

Example 3.

Get 970 cores with an average weight of 0.27 g, as in examples 1, 2. The strength of the cores 91 N, raspadaemost 10 min. kernel is applied 3.94 g of paraffin oil, then film-forming composition containing of 6.29 g of methylcellulose, 6,29 g oksipropilmetiltselljulozy, 0,0407 g tropeolin Oh, 2,52 g of titanium dioxide and 3.15 g of tween-80 in 2 l of water. Get 970 g of tablets with an average weight 0,272 g, which satisfy the requirements of the pharmaceutical agent.

Example 4.

Get 970 cores with an average weight of 0.27 g, as in examples 1, 2. The strength of the cores 91 N, raspadaemost 10 min. kernel is applied 3.94 g of paraffin oil, then film-forming composition containing 12,58 g oksipropilmetiltselljulozy, 0.5 g of dye KF 6001, 2,52 g of titanium dioxide and 3.15 g of tween-80 in a mixture of 0.6 l of ethyl alcohol and 0.6 l of methylene chloride. Get 970 g of tablets with an average weight 0,272 g, which satisfy the requirements of the pharmaceutical agent.

Example 5.

Get 970 cores with an average weight of 0.27 g, as in examples 1, 2. The strength of the cores 91 N, readabilities, 0.2 g of 2 dye E-104, 2,52 g of titanium dioxide and 3.15 g of tween-80 in a mixture of 0.6 l of ethyl alcohol and 0.6 l of methylene chloride. Get 970 g of tablets with an average weight 0,275 g, which satisfy the requirements of the pharmaceutical agent.

Analytical data on the quality and stability of Riboxin of coated tablets, 0.2 g" in the table.

Literature
1. Radar-the encyclopedia of medicine 2000. M.: Publishing house RLS, 2000.


Claims

1. Pharmaceutical composition having an anabolic effect, made in the form of a solid dosage form that includes a core containing Riboxin as active substance and as auxiliary substances (sugar, starch, binders and sliding agents, characterized in that the core as a bonding agent contains gelatin, and moving - stearate potassium or magnesium in the following ratio of ingredients, grams per 1 tablet:
Riboxin - 0,2
Gelatin - 0,003264
Sugar - 0,01632
The potassium stearate or magnesium - 0,00272
Starch - Rest
and the shell is composed of methyl cellulose and/or oksipropilmetiltselljulozy, tween-80, titanium dioxide, vaseline oil, dye.

2. The pharmaceutical composition ellulose and/or oksipropilmetiltselljuloza - 0,003396
Tween-80 - 0,00085
Titanium dioxide - 0,000068
Vaseline oil - 0,001063
Dye - 0,000011-0,000135
3. The pharmaceutical composition according to p. 1, wherein the amount of starch added to the powder, is 23.8% of the content in the composition.

4. The pharmaceutical composition according to p. 3, characterized in that the dye contains tropeolin Oh, CP 6001, E-104.

 

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