Tablet containing ramelteon and copovidone

Abstract

The invention relates the technical field of medicinal preparations and discloses a tablet containing ramelteon and copovidone. Through use of copovidone, the tablet solves the problem of low bioavailability of the ramelteon preparation prepared by the prior art. Through common preparation methods, ramelteon, copovidone and other required components are mixed according to a preset ratio and the mixture is pressed to form the tablet. A preparation method of the tablet comprises the following steps of mixing ramelteon, copovidone and a needed excipient in a granulator to obtain a uniform mixture, adding a needed binder into the granulator, carrying out granulation, taking out the granules, carrying out drying, carrying out screening to obtain powder having required granule sizes, adding magnesium stearate and a required disintegrating agent into the powder of which the granule sizes are adjusted and carrying out mixing to obtain particles to be tabletted. The tablet provided by the invention has greatly improved in-vitro bioavailability.

Description

technical field [0001] The invention relates to a novel solid pharmaceutical composition, which contains ramelteon, an insoluble active ingredient, and copovidone, which improves the bioavailability of the active ingredient. Background technique [0002] Ramelteon (Rozerem) is an oral hypnotic drug developed by Takeda Corporation of Japan and approved by the US FDA in July 2005. It is the first melatonin receptor agonist used in the clinical treatment of insomnia. It is mainly used to treat insomnia with difficulty falling asleep, and it also has definite curative effect on chronic insomnia and short-term insomnia. Its chemical name is (S)-N-[2-(1,6,7,8 tetrahydro-2H-indeno-[5,4-b]furyl-8-)ethyl]propionamide, which is ( S) type corresponding structure, molecular formula C 16 h 21 NO 2 , relative molecular mass 259.34. This product is easily soluble in organic solvents, slightly soluble in water and pH3~11 buffer system. [0003] The dissolution behavior of the tablet i...

AI Technical Summary

Problems solved by technology

[0003] The dissolution behavior of the tablet is directly related to the bioavailability in the body. It is precisely because of the dissolution characteristics of ramelteon that the active ingredient disintegrates regardless of whether it is micronized, or various other binders are added, or the disintegration is increased. All the drugs dissolve slowly and fail to meet the standard requirements of the Chinese Pharmacopoeia 2010 edition, which directly affects the bioavailability in the body

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