Mosapride citrate co-grinded product, preparation method thereof and medicine composition containing mosapride citrate co-grinded product

Abstract

The invention discloses a mosapride citrate co-grinded product, a preparation method thereof and a medicine composition containing the mosapride citrate co-grinded product. The mosapride citrate co-grinded product is prepared by co-grinding mosapride citrate with a hydrophilic macromolecular auxiliary material in a mass ratio of 10-55%: 90-45%, wherein the hydrophilic macromolecular auxiliary material is selected from one or more of beta-cyclodextrin, low-substituted hydroxypropyl cellulose, hydroxypropyl methylcellulose, povidone and polyethylene glycol 6000. The medicine composition prepared by virtue of the mosapride citrate co-grinded product is capable of remarkably improving the dissolution rate of mosapride citrate, simple in preparation process, and suitable for industrialized production.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a co-ground mosapride citrate, a preparation method thereof and a pharmaceutical composition containing the mosapride citrate. Background technique [0002] Functional Gastrointestinal Disorder (FGID) is one of the most common frequently-occurring diseases among gastrointestinal digestive diseases, with a total incidence rate as high as 42-61%. FGID seriously affects the physical and mental health, work efficiency and quality of life of patients. Due to the rapid economic development and the increasingly tense pace of life, the incidence of FGID is still increasing year by year, so the drug market for this type of disease will also grow steadily. [0003] Drugs that promote gastrointestinal motility can be divided into 4 generations. The representative drug of the first generation of gastrointestinal motility drugs is metoclopramide hydrochloride, which is a dopamine ...

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Problems solved by technology

[0006] Because mosapride citrate is a poorly soluble drug, it is almost insoluble in water, so the problem of low dissolution rate is often encountered in the actual production of mosapride citrate oral solid preparations, and because mosapride citrate The content of Lizai in the preparation is low, it is difficult to fully mix during preparation, and there are often problems with large differences in dissolution rate during dissolution testing

Moreover, the low bioavailability of mosapride due to its low dissolution rate has always been a key factor limiting its clinical application.

Described pharmaceutical formula is suitable for preparing dispersible tablet, yet the dissolution effect of mosapride citrate dispersible tablet prepared by the prescription disclosed in this document and preparation process is lower than 60% under the condition of pH 6.8 phosphate buffer, not Conforms to the dissolution standards of the Japanese Pharmacopoeia

[0010] Chinese patent application CN101816639A discloses a tablet containing mosapride citrate and a preparation method thereof, but the patent does not disclose the dissolution medium used for the dissolution of mosapride citrate tablets

Experiments have proved that the dissolution rate of mosapride citrate is the smallest in pH 6.8 phosphate buffer solution. This study found that the dissolution rate of mosapride citrate tablets prepared in Chinese patent application CN101816639A is low in pH 6.8 phosphate buffer solution More than 60%, does not meet the dissolution standards of the Japanese Pharmacopoeia

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