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  

Preparation and in Vitro Release of Risperidone Injectable Biodegradable Implants

作　　者：朱薇[1] 黄华[1] 单雪峰[1] 赖超[1] 

机构地区：[1]重庆医科大学药学院药剂学教研室,重庆市400016

出　　处：《中国药房》2010年第9期837-839,共3页China Pharmacy

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。OBJECTIVE： To prepare risperidone injectable biodegradable implants and study its in vitro release. METHODS： Polylactide-co-glycolide copolymer （PLGA） was chosen for cartier and N-Methyl pyrolidone （NMP） as solvent to prepare risperidone 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 24 hours. The average molecular weight of copolymer decreased to about 10 000 from 43 000 after 30 days and the size of the superficial openings became larger and larger. CONCLUSION： Risperidone injectable biodegradable implants can release continuously and stably in vitro for 30 days.

关 键 词：利培酮 生物可降解注射型植入剂 聚合物 体外释放 

分 类 号：R971.4[医药卫生—药品]