口服控释制剂的发展.pdfVIP

Evolution of Oral Controlled/Modified Release Dosage Forms 口服控释/改良释放剂型的发展 刘晓华博士 Global Technical Manager MR Technologies, Colorcon eliu@ Oral CR/MR Dosage Forms 口服CR/MR 剂型 “Extended-Release” “延长释放” “Delayed-Release” “延迟释放” Controlled Release ↔Modified Release 控制释放↔改良释放 Potential Benefits of Controlled Release Dosage Forms 控释剂型的潜在优点 • Enhanced activity duration for short half-life drugs • 提高短半衰期药物的有效作用时间 • Reduction of side effects • 降低副反应 • Less frequent dosing - improved patient compliance • 减少给药频率-提高患者顺应性 • Protecting labile drugs - improved product stability • 保护不稳定药物-提高产品的稳定性 • Potential for localization of drug to site of action • 将药物固定于起效部位的可能性 • Potential for extended patent protection • 延长专利保护的可能性 Oral CR/MR Dosage Forms 口服CR/MR剂型 How did we get here and where are we going? 我们是如何达到现在的水平并 将向哪方面发展？ Early Slow-Release Oral Dosage Forms in Chinese Medicine 中药中的早期缓释口服剂型 ● 2nd Century B.C. – Animal-fats as binder for pills [“Recipes for Fifty-Two Ailment”, Mawangdui Medical Manuscript, dated 168 B.C.] 公元前2世纪－动物脂肪作为丸剂的粘合剂 〔“52种疾病的处方”， 马王堆医学手稿，日期公元前168〕 ●4th Century A.D. – Wax and fat pills [“Handbook of Prescriptions for Urgent Cases”, Ko Hung (281-341)] 公元4世纪－蜂蜡和脂肪丸剂 〔”肘后救卒方“葛洪(281-341 〕 th ●13 Century – Wax pills for slow-release [“Rules and Correspondences in the Use of Drugs”, Li Kao (1180-1251) “Medications Administered as Decoctions”, Wang Hao-ku (mid-13th century)] 13世纪－缓慢释放的蜡丸 〔” 药物使用中的规则和依据“Li Kao (1180-1251) ”按汤剂服用“ 〕