口服控释改良释放剂型的发展.ppt

Evolution of Oral Controlled/Modified Release Dosage Forms口服控释/改良释放剂型的发展 Oral CR/MR Dosage Forms口服CR/MR 剂型 “Extended-Release” “延长释放” “Delayed-Release” “延迟释放” Potential Benefits of Controlled Release Dosage Forms控释剂型的潜在优点 Types of Long-Acting Preparations, 1959长效制剂的类型，1959 Coating the active drug with gastro-resistant and slowly enterosoluble substances (e.g. fats, waxes, fatty acids, ets.) 使用抗胃液和减慢肠溶解的物质包裹活性药物（比如，脂肪，蜂蜡，脂肪酸等等） The use of ion exchange resins to bind active drugs 使用离子交换树脂与活性药物结合 The formation of chemical addition compounds or complexes 化学添加物或合成物的形成 Impregnating or embedding the drug in a base which gradually releases the active principle 将药物浸渍或包埋在一个基质中，该基质可缓慢释放活性有效成分 Major Historical Milestones Affecting the Direction of Oral Controlled Release Dosage Forms影响口服控释剂型发展方向的主要历史里程碑 Availability of semi-synthetic and synthetic polymers for enteric coating (1940’s through 1990’s) 半合成和合成聚合物用于肠溶包衣（二十世纪四十年代到九十年代） Introduction of first oral sustained release products by Smith Kline French using the Spansule technology: Dexedrine (dextroamphetamine sulfate) (1952) and Contac, the cold remedy (1960). Smith Kline French介绍了首个口服持续释放产品，使用了缓释胶囊剂（Spansule）技术： Dexedrine（右旋硫酸右苯丙胺）（1952）和Contac（复方盐酸苯丙醇胺），感冒药（1960） Introduction of semi-synthetic and synthetic hydrophilic gel forming polymers for designing oral sustained release products (1950’s and 1960’s) 半合成和合成亲水凝胶形成的聚合物介入口服持续释放产品设计（二十世纪五十年代和六十年代） Invention and first commercialization of oral osmotic drug delivery systems by ALZA (1970’s through 1980’s) ALZA发明并首次商业使用的口腔渗透药物释放系统（二十世纪七十年代到八十年代） “The delayed action tablet which was an extension of the enteric coating principle, represented the initial approach in controlling the release of a drug in the gastro-intestinal tract”“延迟起效片剂是肠溶包衣原理的扩展，它代表在胃肠道中控制药物释放开始起步”  - Lazarus and Cooper (1959) Enteric Coatings肠溶包衣 1884 –Dr. Paul Unna introduced keratin-coated pills 1884 –Paul Unna 博士引入了角质素包衣丸剂 Late 1880’s to 1930’s – Numerous substances and their combination