聚羟基丁酸酯缓释微球的制备与性能

Preparation and Characterization of Diazepam-Polyhydroxybutyrate Microspheres

用溶剂蒸发法制备了以新型生物可降解材料聚羟基丁酸酯为载体、以安定为模药的缓释微球 ,讨论了药物与载体之比对药物含量与包封率的影响 ,以及制备微球条件对药物释放性能的影响 ;微球平均粒径为3 0～ 40 μm ,粒径分布在 1～ 1 .5之间 ,最大载药量为 1 9.5 1 % ;最高包封率为 67.1 1 % ;体外累积释放曲线呈“两相”释放特征并拌随初始的“突释效应”。扫描电镜观察微球表面呈皱缩表观形态结构 ,微球内部横断面具有孔道与孔洞 ,在 4℃与室温 (2 0～ 2 5℃ )条件下密封 ,避光环境下性质稳定。

In this paper, Diazepam(DZP) loaded microspheres were prepared using an emulsion solvent evaporation process from the biodegradable materials poly(3 hydroxybutyrate) (PHB). The effect of different variables on the preparation of DZP-PHB microspheres was studied. The mean diameter of microspheres is in the range of 30～40 μm. The paddle method was used to study the drug release properties of DZP PHB microspheres. The drug release tests for 30 day showed a characteristic biphasic release pattern with an initial burst effect. The Scanning Election Microscope (SEM) reveals that the microspheres have a shriveled appearance with discrete micropores from the surface to the inside. The numerous factors potentially responsible for the release characteristic are discussed in the light of this observation. The DZP PHB microspheres was stable after stored at 4 ℃ and room temperature under desiccated and free light condition.