Medicinal product on the basis of carbamazepine

 

(57) Abstract:

The invention relates to medicine, in particular to drugs on the basis of carbamazepine, which have significant anticonvulsant (antiepileptic) and a moderate degree of antidepressant (timolepticheskoe) and narkoticheskoe action. The essence of the invention is that the tool is in the form of tablets include the active ingredient carbamazepine, starch, magnesium stearate and targeted supplements, which are used microcrystalline cellulose, polyvinylpyrrolidone, and the tool further comprises poperechnyy a homopolymer of N-vinyl-2-pyrrolidone containing nitrogen, 11-12,8% in the amount indicated in the claims. The technical result is the creation of a simple and accessible form of the drug in tablet form, containing as the active ingredient carbamazepine, as well as increasing the strength of the tablets at the same time quick raspadaemosti in the water. table 1.

The present invention relates to medicine, in particular to drugs on the basis of carbamazepine, which have significant anticonvulsant (antiepileptic) and a moderate degree of antidepressant (thymoleptic the essential medicines, acting on the Central nervous system /Mashkovsky M. D. Medicines, T. 1, M, 2000/.

There are various forms of medicines on the basis of carbamazepine, for example, in the form of a polymer gel (U.S. Pat. USA 5980942), water (U.S. Pat. USA 6051253).

Known oral dosage form based on carbamazepine, comprising a core and a shell, in which there is a hole connecting the core with the environment (U.S. Pat. Germany 3725824). The core consists of, in wt.%: carbamazepine - 40,8, microcrystalline cellulose 4,1, oksipropilmetiltselljulozy - 2,6, copolymer of vinylpyrrolidone and vinyl acetate, taken in the ratio of 60:40 - 16,3, polyethylene glycol - 16,3, sodium chloride - 16,3, sodium lauryl sulphate - 1,2, stearate and 2.4. The shell consists of, in wt.%: cellulose acetate - 90,0, polyethylene glycol - 10,0. The disadvantages of this structure should be attributed rather complex technology of its production and the necessity of using micronized carbamazepine.

Known drug (wt%) on the basis of carbamazepine - 34,5, lactose - 34,5, starch - 24,3, gelatin and 0.5, talc - 4,1, stearate - 0,7, silicon dioxide - 1,4 (U.S. Pat. Switzerland 649080). Carbamazepine is mixed with lactose and a part of the starch, the mixture oblast, the Alka, magnesium stearate and silicon dioxide and the resulting pellet mass is pressed into tablets. However, the composition has a relatively low content of carbamazepine (35%). In addition, the presence of talc in excess of the permitted GF X1 (3%), and also increases irritant effect of carbamazepine on the mucous membrane of the gastrointestinal tract.

Known dosage form of carbamazepine delayed release of the active substance-containing film former in combination with the softening agent in the aqueous solution and/or dispersion deposited on carbamazepine in the granulator with psevdoozhizhennom layer (U.S. Pat. RF 2141825). As the foaming agent is a mixture of polymethacrylates, and as softener glyceryltrinitrate or triethylcitrate. Optionally, the dispersion of the foaming agent injected release agents, for example talc, and/or sprayed them later in the fluidized bed in the form of separate suspensions. Covered carbamazepine with other vspomogatelnymi agents (microcrystalline cellulose, polyvidone, silicon dioxide, magnesium stearate) pressed into scored tablets or Packed in capsules. The disadvantages of the known formylamino object is known medicine, containing carbamazepine, starch, magnesium stearate and other additives target, used as Aerosil, glycerin, gelatin, (U.S. Pat. RF 2157212).

Well-known member of the tablets of the prototype has a low strength. The presence of Aerosil significantly impairs the process of manufacture of the dosage form, creates high dustiness level.

The purpose of this invention is to provide a simple and accessible form of the drug in tablet form, containing as the active ingredient carbamazepine, increase the strength of the tablets at the same time quick it raspadaemosti in water.

This goal is achieved through the use of a medicinal product on the basis of carbamazepine, containing starch, magnesium stearate and targeted supplements, which are used microcrystalline cellulose, polyvinylpyrrolidone, and the tool further comprises poperechnyy a homopolymer of N-vinyl-2-pyrrolidone containing nitrogen, 11-12,8%, in the following ratio of ingredients, wt.%

Carbamazepine - 60,0-70,0

Microcrystalline cellulose - 15,0-21,0

Polyvinylpyrrolidone - 2,0-3,0

Poperechnyy a homopolymer of N-vinyl-2-pyrrolidone - 0,5-1,5

Starch - 10.0 cancellation with subsequent drying of the granules. The granules then optivault and pressed into tablets.

The starch is pre-dried at a temperature of 70-80oC. All the ingredients are sieved through a sieve. Prepare a solution of polyvinylpyrrolidone by adding the calculated amount of water. Carbamazepine, microcrystalline cellulose, starch mix. Then add a solution of polyvinylpyrrolidone is mixed, granularit, dried, re-granularit. Then dry granules optivault the stearate and Poperechnaya homopolymer N-vinyl-2-pyrrolidone containing nitrogen, 11-12,8%. Powdered mass tabletirujut.

Use Poperechnaya of homopolymer N-vinyl-2-pyrrolidone containing nitrogen, 11-12,8% lets get when pelletizing the solid form, and at the same time, when dissolved in water pill very quickly disintegrates and after 45 min carbamazepine goes completely into solution. Without using this additive was not able to get the desired result.

The results of the experiment are summarized in table.

Medicinal product on the basis of carbamazepine, including starch, magnesium stearate and additives target, wherein the target additives use of microcrystalline celluon with nitrogen 11-12,8% in the following ingredients, wt. %:

Carbamazepine - 60,0 - 70,0

Microcrystalline cellulose - 15,0 - 21,0

Polyvinylpyrrolidone - 2,0 - 3,0

Poperechnyy a homopolymer of N-vinyl-2-pyrrolidone - 0,5 - 1,5

Starch - 10,0 - 20,0

Magnesium stearate - 0,5 - 1,0

 

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