Pharmaceutical combination containing Mosapride citrate and method of preparing the same

Abstract

The invention relates to a pharmaceutical composition containing mosapride citrate which is applicable to the usage of direct powder compression for preparation and a preparation method thereof. The pharmaceutical composition further contains a disintegrant, a thinner, a lubricant, a glidant and an adhesive in addition to the active component of the mosapride citrate. The pharmaceutical composition is applicable to the preparation of dispersible tablets which can be fully disintegrated in 2 minutes in water under the temperature of 19 DEG C to 21 DEG C and pass through a No. 2 screen, the hardness is 8 to 11Kg, and the dissolution rate is in line with the relevant provisions, thus solving the problems of higher relevant substances, instable quality and difficult packaging of the mosapride citrate dispersible tablets prepared by wet granulation.

Description

field of invention [0001] The invention relates to the field of pharmaceutical preparations, in particular to a pharmaceutical composition containing mosapride citrate and a preparation method thereof. Background technique [0002] Mosapride citrate, namely (±)-4-amino-5-chloro-2-ethoxy-N-{[4-(4-fluorobenzyl)-2-morpholine]methyl}benzene Formamide citrate dihydrate is a third-generation gastric motility drug developed by Dainippon Pharmaceutical Co., Ltd., see, for example, Japanese patent JP3090274, European patent EP0243959, and US patent US4870074. Mosapride citrate is a new type of gastric motility drug, a potent and selective 5-HT4 receptor agonist, which increases the release of acetylcholine from nerve endings, thereby promoting gastric emptying [Katayama K, Morio Y, Haga K, et al . cisapride. a gastroprokinetic agent, binds to 5-HT4 receptors [J]. Nippon Yakurigaku Zasshi, 1995, 105(6): 461---468.]. It is clinically used for the relief of a series of gastrointestina...

AI Technical Summary

Problems solved by technology

[0004] 1. Inconvenient to use

[0005] 2. Not easy to preserve, easy to deteriorate and pollute

[0006] On the other hand, the ordinary tablet of mosapride citrate also has disadvantages: the ordinary tablet has the disadvantages of slow dissolution rate and low solubility, which has a certain influence on the absorption of the drug

A large amount of disintegrants have been used in this patent formula, and the preparation method of wet granulation, drying, and tabletting has been adopted. Mosapride is unstable and will produce more related substances. The related substances increase relatively quickly during long-term storage at room temperature, and the product is not stable enough. In order to ensure product quality, the validity period will be shorter; The mosapride citrate dispersible tablet process is complicated, the production cycle is long, and the production cost is high; third, the mosapride citrate dispersible tablet prepared by this patent has low hardness, and the packaging equipment needs special improvement to adapt to the packaging requirements. Require

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