乙醇对口服调释制剂中药物突释的影响及监管情况简介  

Effect of alcohol on dose dumping of oral modified-release preparations and regulatory considerations

作　　者：陈洁 刘倩[1] 南楠[1] 许鸣镝[1] 陈德俊 CHEN Jie1, LIU Qian1, NAN nan1, XU Mingdi1, CHEN Dejun2(1. National Institute for Food and Drug Control, Beijing 100050, China ;2. Shandong Institute for Food and Drug Control, Jinan 250101, China)

机构地区：[1]中国食品药品检定研究院,北京100050 [2]山东省食品药品检验研究院,山东济南250101

出　　处：《药物评价研究》2018年第8期1408-1414,共7页Drug Evaluation Research

基　　金：国家"重大新药创制"科技重大专项资助项目(2017ZX09101001)

摘　　要：在某些特殊情况下,口服调释制剂中控制释放的高分子辅料或膜控材料被酒精提前溶解,或部分溶解及变性,导致活性成分的释放方式、速率或程度发生变化,使其血液浓度短时间内升高,产生突释效应。综述了乙醇对调释制剂药物生物利用度和生物等效性的影响,对美国食品药品监督管理局、欧洲药物管理局等药品监管机构对剂量突释试验的要求以及减少酒精引起的调释制剂药物突释风险的方法进行介绍,以指导调释制剂的研发及一致性评价,为我国仿制药质量和疗效的一致性评价提供借鉴。In some special cases, high polymer materials or membrane materials of oral controlled release formulation dissolved or partly dissolved and degenerated in advance by alcohol lead to changes of the release mode, rate, and degree of active ingredients, which may result in an uncontrolled and immediate drug release. The effect of alcohol on dose dumping of modified-release preparations and regulatory considerations of US Food and Drug Administration and European Medicines Agency were studied and analyzed. Moreover, the design of modified-release formulations resistant to alcohol-induced dose dumping was discussed. To guide the development and consistency evaluation of release preparations and to provide reference for the agreement evaluation of the quality and efficacy of generic drug products in China.

关 键 词：突释效应 乙醇 溶出试验 调释制剂 仿制药质量和疗效一致性评价 

分 类 号：R954[医药卫生—药学]