Stable sitafloxacin medicinal composition and preparation method thereof

Abstract

The invention relates to a stable medicinal composition of sitafloxacin or salt thereof or a hydrate thereof and a preparation method. The composition contains the sitafloxacin or the salt thereof or the hydrate thereof and a medicinal pharmaceutical adjunct, wherein the medicinal pharmaceutical adjunct contains a diluting agent, a disintegrating agent, a lubricant and a powder coating material containing an opacifier. The preparation method of the composition is characterized by comprising the following steps: firstly, adopting a powder coating technology to carry out powder coating on the raw materials and part of the auxiliary materials and then carrying out the next preparation process. The opportunities that the raw materials contact with light are reduced after coating processing, thereby reducing the generation of a photodegradation product and enhancing the stability of the preparation greatly.

Description

technical field The invention relates to a pharmaceutical composition and a preparation method thereof, in particular to a stable sitafloxacin composition and a preparation method thereof. Background technique Sitafloxacin (DU-6859A, C 19 h 18 CIF 2 N 3 o 3 ) is a new generation of quinolone antibacterial drugs developed by Daiichi Sankyo Co., Ltd. in Japan. Its chemical name is: 7-[(7S)-7-amino-5-azaspiro[2.4]hept-5-yl]-8-chloro-6-fluoro-1-[(1R,2S)-cis- 2-fluorocyclopropyl]-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid sesquihydrate. 7-[(7S)-7-Amino-5-azaspiro[2.4]heptan-5-yl]-8-chloro-6-fluoro-1-[(1R,2S)-2-fluorocyclopropyl]-1,4- dihydro-4-oxoquinoline-3-carboxylic acid sesquihydrate Chemical Structure: Molecular formula: C 19 h 18 CIF 2 N 3 o 3 1.5 H 2 o Molecular weight: 436.84 Sitafloxacin has a wide antibacterial spectrum against aerobic and anaerobic Gram-positive bacteria, Gram-negative bacteria, and non-stereotyped bacteria. Moraxella catarr...

AI Technical Summary

Problems solved by technology

Studies have shown that sitafloxacin raw materials will change color under light conditions and produce two types of degradation products under light (the toxicity of the degradation products has not been studied in depth)