右布洛芬缓释干混悬剂处方前研究.docVIP

右布洛芬缓释干混悬剂处方前研究 　　[摘要]目的 为研究右布洛芬缓释干混悬剂，测定药物在不同介质中的溶解度，进行原料药的稳定性及原辅料相容性研究。方法 测定药物在不同pH缓冲液（pH 1.2、pH 4.5、pH 5.0、pH 6.8和pH 7.4）、水以及乙醇中的溶解度，在高温（60℃）高湿（RH 92.5%）、光照（4500 Lx）条件下，分别于第5、10天对原料药进行有关物质测定。在高温（60℃）、高湿（RH 92.5%）、光照（4500 Lx）条件下，分别于第5、10天对原辅料混合物进行有关物质测定。结果 在pH 1.2～7.4范围内，药物溶解度随pH值升高而升高，易溶于乙醇。原料药对光照稳定，在高温条件下有关物质增加明显，在高湿条件下轻微吸潮，但3种条件下有关物质均0.3%。在高温、高湿、光照条件下，原辅料混合物的有关物质均0.3%。结论 右布洛芬的溶解度受pH值影响，原料药对热较敏感，但与所选择辅料无配伍禁忌。 　　[关键词]右布洛芬；缓释干混悬剂；溶解度；稳定性；原辅料相容性 　　[中图分类号] R927.1 [文献标识码] A [文章编号] 1674-4721（2018）1（a）-0016-03 　　[Abstract]Objective To determine the solubility of drug in different media，to evaluate the stability of raw material and drug/excipient interactions for the development of Dexibuprofen Sustained-Release Dry Suspensions.Methods The solubility of the drug was determined indifferent pH buffer solutions （pH 1.2，pH 4.5，pH 5.0，pH 6.8 and pH 7.4），water and ethanol.The related substances of raw material were analyzed at the 5th and 10th days after storage under high temperature （60℃），high humidity（RH 92.5%） and strong light （4500 Lx）.The drug-excipient interactions were also studied at the 5th and 10th days under high temperature （60℃），high humidity （RH 92.5%） and strong light （4500 Lx）.Results The solubility of drug increased as the pH of solution increased in the range from pH 1.2 to pH 7.4.The drug was highly soluble in ethanol.The related substances of raw material slightly increased under high temperature and showed hygroscopicity under high humidity.But the related substancesafter storage under three different conditions were all less than 0.3%.The related substances from drug-excipient interactions under three conditions were below 0.3%.Conclusion The drug solubility showed a pH dependent manner.The raw material was quite sensitive to high temperature.No drug-excipientinteractions were observed between the drug and excipients. 　　[Key words]Dexibuprofen；Sustained-release dry suspension；Solubility；Stability；Drug-excipient interactions 　　布洛芬是抗炎解?嵴蛲蠢?OTC产品，是临