溶剂蒸发法和热熔挤出法制备苯扎贝特固体分散体  

Preparation of Bezafibrate Solid Dispersions by Solvent Evaporation and Hot-melt Extrusion Method

作　　者：乔艳丽[1] 黄雷鸣[2] 赵琪[3] 赵锦花[3] 

机构地区：[1]天津大学药物科学与技术学院,天津300072 [2]中国药科大学药物制剂教研室,江苏南京210009 [3]天津天士力集团化学药物研究所,天津300402

出　　处：《中国医药工业杂志》2011年第9期660-664,共5页Chinese Journal of Pharmaceuticals

摘　　要：以水难溶性药物苯扎贝特为模型药物,以聚维酮(PVP K30)或新型辅料Soluplus^(?)为载体,分别采用溶剂法和热熔挤出法制备了苯扎贝特固体分散体。采用差示扫描量热法、傅里叶变换红外光谱法和X射线粉末衍射法对固体分散体进行了表征并考察了溶出度。结果显示,药物以无定形或分了状态存在于固体分散体中,两种工艺以及两种载体制备的固体分散体(药物-载体=1:3)均能提高苯扎贝特在水中的溶解度。热熔挤出法还能制备药物-载体重量比为1:1的固体分散体,提示热熔挤出法较溶剂蒸发法能更有效地促进药物与载体之间的相互作用。The bezafibrate solid dispersions with PVP K30 or Soluplus as carrier were prepared by solvent evaporation or hot-melt extrusio method. The solid dispersions were characterized by differential scanning calorimetry （DSC）, Fourier transform infrared spectroscopy （FT-IR） and powder X-ray diffraction （PXRD）. The in vitro dissolutions of the prepared dispersions were also investigated. The results showed that bezafibrate existed as amorphous or molecule state in solid dispersions. The water solubility of bezafibrate could be significantly improved by the solid dispersions with PVP K30 or Soluplus （drug-carrier = 1 ： 3） prepared by two methods. The solid dispersions with weight ratio of drugcarrier of 1 ： 1 could be prepared by hot-melt extrusion method, which indicated that this method was more efficient to promote the physical interaction of drug and carrier compared to solvent evaporation method.

关 键 词：固体分散体 苯扎贝特 溶剂法 热熔挤出法 

分 类 号：R944.9[医药卫生—药剂学]