摘要
目的制备注射用醋酸艾塞那肽缓释微球,以达到缓释作用,从而减少用药次数。方法以聚乳酸-羟基乙酸为载体,羧甲基纤维素钠水溶液为分散介质,乙酸乙酯为有机溶剂,甘露醇为保护剂,通过复乳-液中干燥法和冷冻干燥法制备注射用醋酸艾塞那肽缓释微球。以微球收率、粒径、包封率为指标,采用正交试验法来优化微球的处方和制备工艺。采用透析法考察含药微球的体外释药特性,计算微球累积释药百分率,绘制体外释药曲线。结果通过正交设计筛选出制备注射用醋酸艾塞那肽缓释微球的处方和制备工艺,载药量为21.3%,包封率为94.6%,Zeta电位为(-29.3±1.51)mV,含药缓释微球的体外释药过程符合Higuchi方程。结论制备的注射用醋酸艾塞那肽缓释微球具有30 d的缓释效果。
Objective To prepare Exenatide Acetate Sustained-release Microspheres to realize the sustained-release effect and reduce the frequency of drug use. Methods Exenatide Acetate Sustained-release Microspheres were prepared by the method of double-elusion drying in liquid with PLGA as the carrier, ethyl acetate as the organic solvent, CMC-Na water solution as the dispersion medium and mannitol as the diluents and the method of freezing drying.The prescription and preparation process were optimized by orthogonal test with particle size,yield and encapsulation as the investigating index.The property of releasing drug in vitro was investigated by the method of dialysis.The cumulative drug-releasing percentage of Sustained-release Microspheres was calculated and the drug-releasing curve was drawn. Results The prescription and preparation process were screened according to the orthogonal test with a drug loading capacity of 21.3%,an encapsulation efficiency of 94.6% and a Zeta potential of （-29.3＋1.51） mV.The releasing profile in vitro was in accordance with Higuchi equation. Conclusion The Exenatide Acetate Sustained-release Microspheres for injection have releasing effect of 30 days.
出处
《中国当代医药》
2015年第27期10-13,共4页
China Modern Medicine
关键词
醋酸艾塞那肽
缓释微球
体外释放
Exenatide Acetate
Sustained-release Microspheres
Release in vitro
