高端固体口服制剂的仿制_ 新型给药系统峰会课件.ppt

* * * * * * * * * * * * * * * * * * * * * * * * * * * * * * * 开发申报规范市场仿制药的过程 Milestone for the Development 项目开发 (Product Development) 处方设计（System Design） 处方开发 (Formulation Development) Prototype Formulation Pilot BE Study 中试放大 （Scale up） 报批产品的准备 （Exhibit Batch or Pivotal Batch) 稳定性考察 （Stability study) 生物等效实验 （BE Study） 准备报批材料 （CTD document) 报批 （Submit） 上海星泰医药科技有限公司 某特殊缓释胶囊 Special ER Formulation 上海星泰医药科技有限公司 Special ER Formulation -Rythmol SR 上海星泰医药科技有限公司 上海星泰医药科技有限公司 Special ER Formulation -Rythmol SR 上海星泰医药科技有限公司 上海星泰医药科技有限公司 Special ER Formulation-Rythmol SR Brand Product Micro-Tablets in Capsules 95% of API existed in Finished Product System and Process Patented Orange Book Patent 上海星泰医药科技有限公司 US-5,681,588 Claim 1. A cylindrical delayed release microtablet with a convex or flat upper side and lower side of .beta.-phenylpropiophenone derivatives of the formula I as active ingredient ##STR2## where R is n-propyl or 1,1-dimethylpropyl, and their pharmacologically acceptable salts, wherein a) the height and diameter are, independently of one another, 1-3 mm, b) the active ingredient content is in the range from 81 to 99.9% of the weight of the microtablet, c) the active ingredient density is greater than 1, d) the release of active ingredient in the USP paddle method at 50 rpm is 80% as a maximum after 3 hours and as a minimum after 24 hours, e) the release rate is virtually independent of the pressure when compressing the tablets, and f) the tablet contains no release-delaying ancillary substance but 0.1-5% by weight of a lubricant and 0-18.9% by weight of other conventional ancillary substances. 上海星泰医药科技有限公司 对策 设计一特殊的给药系统，其药物释放行为与原研药相似 用特殊的生产过程得到致密的大颗粒 大颗粒填充于胶囊 上海星泰医药科技有限公司 Special ER Formulation-Rythmol SR 产品外观的比较 上海星泰医药科技有限公司 Special ER Formulation-Rythmol SR 产品溶出的比较 上海星泰医药科技有限公司 Special ER Formulation-Rythmol SR PRODUCT P DATA (Log Transformed Data, Fast, n-12) Ratio of Geometric Means x 100 90% CI of Log Transformed Data CV (%) Test A vs Refe