Oral preparation of Tegaserod or its acid salt and its preparing process

Abstract

The invention relates to an oral preparation containing tegaserod or its pharmaceutically acceptable salt and its preparation, wherein the oral preparation is a drop pill prepared by mixing add medicinal effective dose of tegaserod with salt and right amount of base material. The preparation method includes adding tegaserod or its acid into salt, melting it with its base material, instiling into cooling liquid, thus preparing drop pills.

Description

(1) Technical field [0001] The invention relates to an oral preparation containing tegaserod or a pharmaceutically acceptable salt thereof and a preparation method thereof, belonging to the technical field of western medicine preparations. (2) Background technology [0002] Tegaserod or 3-(5-methoxy-1H-indole-3-methylene)-N-pentyl-iminoguanidine is a 5-HT 4 Receptor partial agonists, disclosed in EP505322, it can activate 5-HT throughout the gastrointestinal tract 4 Receptors to speed up colonic transit, so it can be used to treat irritable bowel syndrome mainly manifested as constipation. Its acid addition salt is mainly used clinically, preferably maleate. [0003] It has been reported that tegaserod has a solubility in water at 25°C of about 0.02% and is acid sensitive. The prior art related to increasing the dissolution rate of oral preparations of tegaserod or pharmaceutically acceptable salts thereof is mainly achieved by adding disintegrants to the preparations, su...

AI Technical Summary

Problems solved by technology

[0006] Although the above mentioned disintegrant is added, the dissolution rate is improved, but its cost is relatively high, and there is more dust during production, which is not conducive to labor protection.

Images