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1、高端固体口服制剂的仿制 ACCELARATED DEVELOPMENT FOR MODIFIED GENERIC FORMULATIONS,上海星泰医药科技有限公司 SunTech Pharmaceuticals Co., Ltd 何平,第二届新型给药系统中国峰会2012年10月22-24 上海,Contents,上海星泰医药科技有限公司,开发仿制药的重要性和机遇 研发仿制药的团队 高端口服固体制剂特点分析 怎样开发申报规范市场的仿制药,Opportunity of Generic Drugs Development Team Modified Release Oral Drug Delive
2、ry System Generic Drug for Regulated Market,上海星泰医药科技有限公司,创新药与仿制药-NDA verses ANDA 开发仿制药与我国药物研发的海外战略,开发仿制药的重要性和机遇 Opportunity of Generic Drugs,药物制剂目标主流市场-Pharmaceutical Market,2011,上海星泰医药科技有限公司,研发团队 国外仿制药公司研发团队的一般设置 我国制药公司研发团队的现状 管理团队,研发仿制药的团队 Build up a Team,Development Team General Set up of a Devel
3、opment Team Current situation in China Management Team,上海星泰医药科技有限公司,国外仿制药公司研发团队的一般设置 General Set up of a Development Team项目经理 （Project Manager) 制剂研发部 (Product Development) 制剂分析部 (Analytical Research & Development) 法规部 (Regulatory) 专利部 (Legal) 生物药剂学 (Biopharmaceutical) 信息部 (Information),上海星泰医药科技有限公司,
4、REGULATORY,仿制药研发团队 BUILD UP A TEAM,Project Manager,上海星泰医药科技有限公司,研发团队 我国制药公司研发团队的现状 管理团队,研发仿制药的团队 Build up a Team,Development Team Current situation in China Management Team,上海星泰医药科技有限公司,高端口服固体制剂特点分析Modified Release Oral Drug Delivery System,上海星泰医药科技有限公司,典型的缓控释制剂释放曲线 Dissolution Profile of a Typical
5、Oral Solid Formulation,上海星泰医药科技有限公司,原研药(品牌药)高难制剂的释放特点 Dissolution Profile for Novel Drug Delivery Systems,上海星泰医药科技有限公司,高端制剂特点分析-Advanced Drug Delivery systems,优点 变速释放 复制有难度 缺点 制剂工艺复杂 需使用体殊设备 成本相对较高,包芯片（片中片）系统 Tablet in Tablet,Advantage Unique dissolution Difficult to copy Disadvantage Complicate pro
6、cess Special equipment Costly,上海星泰医药科技有限公司,优点 吸收释放受外层材料控制 可漂浮 不易复制 缺点 制剂工艺复杂 需使用体殊设备 成本高,三层片系统-Multilayered Tablet,高端制剂特点分析-Advanced Drug Delivery systems,Advantage Unique dissolution Difficult to copy Disadvantage Complicate process Special equipment Costly,Geomatrix,上海星泰医药科技有限公司,优点 零级(线性)释放 释放速度不受
7、外界的影响 无食物效应 不易复制 缺点 制剂工艺复杂 需使用体殊设备 成本高,渗透泵系统-Osmotic Pump System,高端制剂特点分析-Advanced Drug Delivery systems,Advantage Zero-order dissolution Deliveries may be delayed or pulsed if desired Drug release is independent Difficult to copy Disadvantage Complicate process Special equipment Costly,上海星泰医药科技有限公司
8、,优点 特性释放 释放速度不受外界的影响 无食物效应 难复制 缺点 制剂工艺复杂 需使用体殊设备 成本高,多层片的渗透泵-Sandwiched Osmotic Tablets,高端制剂特点分析-Advanced Drug Delivery systems,Advantage Unique dissolution Drug release is independent Difficult to copy Disadvantage Complicate process Special equipment Costly,上海星泰医药科技有限公司,优点 多单元体系，均匀度高 复制有难度 缺点 需使用体
9、殊设备 生产周期较长 成本相对较高,包衣微丸1-缓释胶囊，微丸压片-Coated pellets,高端制剂特点分析-Advanced Drug Delivery systems,Advantage Multi-particular system Difficult to copy Disadvantage Complicate and long process Special equipment Costly,上海星泰医药科技有限公司,优点 变速（如多级释放） 多组分 复制有难度 缺点 需使用体殊设备 生产过程复杂 成本相对较高,包衣微丸2-多元系统 （如用多种微丸填充胶囊）,高端制剂特点分析
10、-Advanced Drug Delivery systems,Advantage Variable dissolution Multiple components Difficult to copy Disadvantage Complicate process Special equipment Costly,上海星泰医药科技有限公司,优点 提高难溶药物的生物利用度 缺点 需使用体殊设备 成本高,纳米技术-Nano-Technology,高端制剂特点分析-Advanced Drug Delivery systems,Advantage Improved bio-availability f
11、or poor water soluble drugs Disadvantage Special equipment Costly,上海星泰医药科技有限公司,研发高端仿制药的一些体会Case Study,上海星泰医药科技有限公司,Case Study-1 Tablet in Tablet,由于药物在内片和外片中含量有所不同,使药物的释放速度随时间发生变化.,上海星泰医药科技有限公司,利用我公司建立的技术平台设计了药物给药系统,并进行体外体内的评估以及相关的考查.,Case Study-1 Tablet in Tablet,上海星泰医药科技有限公司,Pilot Bio-study-Fast,Ca
12、se Study-1 Tablet in Tablet,Pilot Bio-study-Fed,上海星泰医药科技有限公司,用成本和制备方法相对低廉简单的固架系统去仿制复杂的渗透泵系统，极具挑战性,Case Study-2 Osmotic Pump,上海星泰医药科技有限公司,利用我公司建立的技术平台设计了药物给药系统,并进行体外体内的评估以及相关的考查.,Case Study-2 Osmotic Pump,上海星泰医药科技有限公司,Case Study-2 Osmotic Pump,Pilot Bio-study-Fast,Pilot Bio-study-Fed, 熟悉规范市场的法律法规和申报要
13、求 Familiar with regulation and application criteria 达到cGPM标准的制剂车间 Upgraded cGMP manufacturing facility 有完善的质量监管系统以及专业人才 Completed QA system and management team 研发贯穿“质量源于设计”的理念 Development guided by “Quality by Design” 核心：质量可控，生物等效 Goal: Predefined Quality, Bio-Equivalent,怎样开发申报规范市场的仿制药？ Generic Drug
14、 for Regulated Market,上海星泰医药科技有限公司,仿制药的研发过程 Generic Product Development Roadmap,准备工作 信息（Information）： 有关原研产品的信息 Orange Book PDR （Physicians Desk Reference） SBOA （ Summary Basis of Approval) 专利 (Patent Evaluation) 原研公司的专利 (Orange Book Patents) 非原研公司的专利,上海星泰医药科技有限公司,怎样开发申报规范市场的仿制药？ Generic Drug for Re
15、gulated Market,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 （
16、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
17、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
18、, 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 acti
19、ve 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.,
