摘要
目的 :探索以新型生物可降解材料聚羟基丁酸酯 羟基戊酸酯共聚物 (PHBV)为载体的地西泮药物中长期缓释微球制备工艺 ;方法 :以溶剂蒸发法制备微球 ,用扫描电镜SEM观察微球表面及内部横断面形态结构 ;结果 :微球的平均粒径为 3 0 .5μm ,平均载药量 (1 8.66± 0 .2 3 ) % ,包封率 (80 .85± 1 .0 1 ) %。体外释放第一天呈突释效应 ,而后药物释放基本符合零级动力学过程 .其释放曲线方程为 Q =2 0 .55+ 2 .3 99t,r=0 .9569;结论 :开发与研制PHBV为载体的中长期缓释微球具有较好应用前景。
OBJECTIVE:To explore the preparation technology of diazepam sustained microspheres using the new biodegradable materials poly(3 hydroxybutyrate hydroxyvalerate) as the drug carrier.METHOD:Microspheres were prepared using an emulsion solvent evaporation process. The ultrastructural morphology of microspheres on surface and inside section topography was observed by Scanning Electron Microscope(SEM);RESULTS: The mean diameter of the microspheres was 30.5μm. The mean drug loading was (18.66±0.23)% and the drug embedding ratio was (80.85±1.01)%. The pattern of drug release for 30 days in vitro fitted to zero order release plot, with an initial burst effect at the first day. The release rate was expressed by following equation: Q=20.55+2.399t(d), r=0.9569; CONCLUSION:The exploitation of PHBV microspheres as middle term-sustained drug release may lead to a prosperity in clinical use.
出处
《中国药学杂志》
CAS
CSCD
北大核心
2000年第4期244-246,共3页
Chinese Pharmaceutical Journal
基金
国家自然科学基金资助项目!第399770223号
关键词
缓释微球
地西泮
PHBV
可降解材料
poly(3 hydroxybutyrate hydroxyvalerate),diazepam,sustained release microspheres