利培酮生物可降解注射型植入剂的制备及体外释放特性的研究.pdf

利培酮生物可降解注射型植入剂的制备及体外释放特性的研究 ＊ # 朱 薇 ，黄 华 ，单雪峰，赖 超（重庆医科大学药学院药剂学教研室，重庆市 400016） + 中图分类号 R971.4 文献标识码 A 文章编号 1001- 0408（2010）09- 0837- 03 摘 要 目的：制备利培酮生物可降解注射型植入剂并考察其体外释放特性。方法：选用聚乳酸乙醇酸共聚物（PLGA ）为载体和 N- 甲基吡咯烷酮（NMP ）为溶剂，制备利培酮生物可降解注射型植入剂。考察制剂在30d 内累积释药率、PLGA 在降解过程中分 子量的变化情况以及固体聚合物在降解过程表面孔径的变化情况。结果：所制制剂30d 内释药曲线平稳，累积释药率为89.01％， 前24h 突释量较小，为13.8％。聚合物降解30d 后分子量从43000减少到10000左右，表面孔径逐渐变大。结论：利培酮生物可 降解注射型植入剂可在体外30d 持续稳定释药。 关键词 利培酮；生物可降解注射型植入剂；聚合物；体外释放 Preparation and in Vitro Release of Risperidone Injectable Biodegradable Implants ZHU Wei ，HUANG Hua ，SHAN Xue-feng ，LAI Chao （Dept. of Pharmacy ，College of Pharmacy of Chongqing Medical University ，Chongqing 400016，China ） ABSTRACT OBJECTIVE ：To prepare risperidone injectable biodegradable implants and study its in vitro release. METHODS ： Polylactide- co- glycolide copolymer （PLGA ）was chosen for carrier and N- Methyl pyrolidone （NMP ）as solvent to prepare risperi- done injectable biodegradable implants. The percentage of accumulative drug release within 30 days ，the change in molecular weight of copolymer and superficial opening diameters of copolymer in function time were observed. RESULTS ：Drug release curve of risperidone injectable biodegradable implants for 30 days was stable with small burst. The percentage of accumulative drug release was 89.01％and the percentage of burst accounted for 13.8％at the first 24hours. The average molecular weight of copoly- mer decreased to about 10000 from 43 000 after 30 days and the size of the superficial openings became larger and larger. CON- CLUSION ：Risperidone injectable biodegradable implants can release continuously and stably in vitro for 30days. KEY WORDS Risperidone ；Injectable biodegradable implants ；Copolymer ；In vitro drug release 120 复合