艾塞那肽长效缓释微球的制备及体内药效学研究.doc

文档介绍：艾塞那肽长效缓释微球的制备及体内药效学研究
刘斌1,2,董庆光1,王梦舒1,李纯1,孔维1,2,陈妍1*
(,长春 130012; ,长春 130012.)
摘要:目的制备艾塞那肽长效缓释微球,并考察其理化性质、体外释放特性及体内药效学。方法采用复乳-溶剂挥发法(W/O/W)制备包裹艾塞那肽的聚乳酸-羟基乙酸嵌段共聚物(PLGA)微球;考察微球的粒径分布、表面形态、载药量和包封率; 用micro-BCA试剂盒测定微球的体外释放速率;考察了微球在糖尿病模型小鼠体内的降血糖作用。结果微球外观光滑圆整,分散性好,艾塞那肽载药量为3%,包封率为75%;微球40d之内体外累积释放达到88%,其体外释放曲线近似零级释放模式;体内药效学实验结果显示,40d内微球组小鼠与模型对照组小鼠血糖相比具有显著性差异(P<)。结论采用复乳-溶剂挥发法成功制备了可以缓释40d的艾塞那肽长效微球,且40d之内在糖尿病小鼠体内具有明显的降血糖作用。
关键词:艾塞那肽;聚乳酸-羟基乙酸嵌段共聚物;微球;血糖
中图文类号: 文献标识码: 文章编号:
Preparation of Long-acting Release Microspheres of Exenatide and Studies on Their in vivo Pharmacodynamics
LIU Bin1,2,DONG Qing-Guang1,WANG Meng-Shu1,LI Chun1,KONG Wei1,2,CHEN Yan1*
(1. College of Life Science, Jilin University, Changchun 130012, China; 2. State Key Laboratory of Supramolecular Structure & Materials, Jilin University, Changchun 130012.,China.)
ABSTRACT: OBJECTIVE To prapere Exenatide loaded long-acting release microspheres, and to evaluate their physical and chemical characteristics、in vitro release behavior as well as in vivo pharmacodynamics. METHOD Exenatide loaded PLGA microspheres were prepared by double emulsion(W/O/W)method. The mean diameter、morphology、drug loading and encapsulation efficiency were evaluated. The micro-BCA protein assay was used for the in vitro release behavior. The effect of reducing plasma glucose were evaluated on the diabetes mice.