基于化学反应的药物与辅料相容性对制剂有关物质影响分析  

Analysis of the influence of compatibility of API and excipient on related substances of preparation based on chemical reaction

作　　者：李杰 江娟 丁锐 邹洁 仲兆民[3] LI Jie;JIANG Juan;DING Rui;ZOU Jie;ZHONG Zhaomin(Key Laboratory of Chongqing Industry and Informatization,Southwest Pharmaceutical Co.,Ltd.,Chongqing,400038 P.R.China;Laboratory of New Product Development,Chengdu Yukang Science and Technology Co.,Ltd.,Chengdu,Sichuan,610000 P.R.China;School of Biology&Basic Medical Sciences,Soochow University,Suzhou,Jiangsu,215123 P.R.China)

机构地区：[1]西南药业股份有限公司重庆市工业和信息化重点实验室,重庆400038 [2]成都与康科技有限公司新品开发实验室,四川成都610000 [3]苏州大学基础医学与生命科学学院,江苏苏州215000

出　　处：《华西药学杂志》2022年第6期704-710,共7页West China Journal of Pharmaceutical Sciences

基　　金：国家自然科学基金资助项目(批准号:81701347);江苏省青年基金项目(BK20170351)。

摘　　要：从化学反应机理的角度,分析药物与辅料的相容性及作用机制,以利于制剂工作者更好地进行处方设计。结合近年来国内外相关文献,分析辅料与药物的直接反应、辅料中杂质与药物的间接反应。药物与辅料的相互作用可改变药物的药剂学性质,影响药物的稳定性和有效性。药物与辅料间的化学反应类型繁多,且受多种因素的影响,开发者应合理选择辅料,规避潜在反应条件,以质量源于设计(QbD)的理念为指导进行研究。In this review,compatibility and interaction between active pharmaceutical ingredient(API)and excipient have been analyzed,in order to facilitate the pharmacist to better design prescription.Related literatures in recent years were reviewed,and the direct reactions between excipient and API and the indirect reactions between impurities in excipient and API were analyzed.The interaction between API and excipient can change the pharmaceutical properties and affect the stability and effectiveness of drug.There are many types of chemical reactions between API and excipient,and they are affected by many factors;researchers should choose the excipient reasonably to avoid the potential reaction conditions,and conduct research under the guidance of QbD.

关 键 词：化学反应 活性药物成分 辅料 相容性 制剂 有关物质 质量源于设计 药动学 

分 类 号：R914[医药卫生—药物化学]