Pediatric loperamide hydrochloride granules and preparation process thereof

Abstract

The invention belongs to the technical field of medicines, and particularly relates to pediatric loperamide hydrochloride granules and a preparation process thereof. By novel formulation and process, the dissolubility and the content uniformity of the granules can be effectively improved; the quality of the granules is obviously superior to that of a foreign original product; the pediatric loperamide hydrochloride granules are suitable for industrialized production.

Description

technical field [0001] The invention belongs to the field of medical technology preparation, and in particular relates to children's loperamide hydrochloride granules and a preparation method thereof. Background technique [0002] Loperamide hydrochloride is as shown in the following structural formula (I): [0003] [0004] Structural formula (I) which is chemically known as N,N-dimethyl-α,α-diphenyl-4-(p-chlorophenyl)-4-hydroxy-1-loperamide hydrochloride, Its chemical structure is similar to that of haloperidol and pethidine, but the therapeutic dose has no effect on the central nervous system, and its effect on intestinal smooth muscle is similar to that of opioids, which can inhibit the contraction of intestinal smooth muscle and reduce intestinal peristalsis; it can reduce intestinal wall Nerve endings release acetylcholine, which directly inhibits peristaltic reflex through the local interaction between cholinergic and non-cholinergic neurons; it can prolong the re...

AI Technical Summary

Problems solved by technology

Compared with my country, Japan has made great progress in the treatment of acute diarrhea in children. In October 1988, Japan approved Loperamide Hydrochloride Granules for the treatment of acute diarrhea in children. The instructions for children's loperamide hydrochloride granules disclosed by the Comprehensive Device Management Agency mention that its prescription consists of refined white sugar, magnesium aluminosilicate, hydroxypropyl cellulose, croscarmellose sodium, silicon dioxide, hard Magnesium fatty acid, spices, etc., but its dissolution rate is low. With water as the dissolution medium, the dissolution rate is only about 60% in 15 minutes, which affects the efficacy of the drug to a large extent, and the content uniformity of its products is not ideal.

[0007] Due to the above problems, when used clinically for the treatment of acute diarrhea in children, the therapeutic effect will be affected to a certain extent, and it may bring certain safety hazards to children patients

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