银杏内酯固体分散体的制备和体外特性研究  

Preparation and characterization of solid dispersions of ginkgolides

作　　者：马琳怡[1,2] 韩丽妹[2] 张志荣[1] 王建新[2] 

机构地区：[1]四川大学华西药学院药剂学系,四川成都610041 [2]复旦大学药学院药剂学教研室,上海200032

出　　处：《中国中药杂志》2009年第11期1368-1372,共5页China Journal of Chinese Materia Medica

基　　金：上海市科委中药现代化重大专项(08DZ1970900)

摘　　要：目的:优选银杏内酯固体分散体的制备工艺,提高银杏内酯的体外溶出度。方法:以银杏内酯B的体外溶出度为指标,通过单因素试验,考察处方和工艺因素对银杏内酯固体分散体中药物溶出的影响;以X-射线衍射法和差示扫描量热法对固体分散体进行表征。结果:差示扫描量热法和X-射线衍射分析试验表明药物以无定形态存在于固体分散体中。银杏内酯B从PVP固体分散体中的溶出速率比原药粉末显著提高,且药物中银杏内酯A,B,C和白果内酯从固体分散体中的溶出相似性(f2值均大于50)优于原药粉末。结论:将银杏内酯制成固体分散体能显著提高药物的溶出速率,可用于进一步制备其固体剂型。Objective： To optimize the preparation process of solid dispersions of ginkgolides to improve the drug dissolution. Method： The influence of formulation and preparation technology on drug release from solid dispersions was investigated by single factor test. The X-ray diffraction analysis （XRD） and differential scanning calorimetry （DSC） were used to characterize the solid dispersions of ginkgolides. Result： The solubilization efficiency of solid dispersions using PVP k30 as cartier was better than that taking poloxamer 188 or HPMC as matrix. The results of XRD and DSC showed that ginkgolides existed in solid dispersion at amorphous form or solvates form. The dissolution rate of ginkgolide B in solid dispersion was increased dramatically compared with raw material. Conclusion： Solid dispersions could significantly improve solubility and dissolution rate of ginkgolides.

关 键 词：银杏内酯 固体分散体 溶出度 

分 类 号：TQ461[化学工程—制药化工]