多西他赛自乳化固体分散体的制备及体外特性研究  

Preparation and characteristics in vitro of docetaxel in self-emulsifying solid dispersion

作　　者：陈鹰[1] 张红[1] 史琼枝[1] 刘宏[1] 

机构地区：[1]广州军区武汉总医院药剂科,湖北武汉430070

出　　处：《广东药学院学报》2010年第3期221-225,共5页Academic Journal of Guangdong College of Pharmacy

基　　金：湖北省科技攻关课题(2007AA301B15)

摘　　要：目的制备多西他赛自乳化固体分散体(DTX-SESD),并考察其体外特性。方法以自乳化辅料和PEG6000为载体制备多西他赛固体分散体,进行溶解度、体外溶出度和稳定性实验,考察不同自乳化辅料、不同制备方法、不同介质对溶出度的影响。并采用差示扫描量热分析、X-射线粉末衍射分析以鉴别药物在载体中的存在状态。结果 DTX-SESD的溶解度和溶出度分别是原料药的约33.8倍和12.5(2 h)倍;自乳化辅料对药物溶出有显著影响;溶剂法和溶剂熔融法制备的自乳化固体分散体溶出度好于熔融法;溶出介质对溶出无显著影响;自乳化固体分散体中药物主要以分子状态存在。结论自乳化固体分散体能显著提高多西他赛的溶解度和溶出度。Objective To study on the preparation of docetaxel self-emulsifying solid dispersion（DTX-SESD） and its characteristics in vitro. Methods Self-emulsifying solid dispersion of docetaxel was prepared with PEG6000 and other self-emulsifying excipients.The solubility,stability and dissolution experiments were carried out with different self-emulsifying excipients,preparation methods and medias.Differential thermal analysis and powder X-ray diffraction were employed to identify the drug status in carriers.Results The solubility and dissolution of DTX-SESD were respectively 33.8 and 12.5（2 h）folds as those of the drug crude powder.Significant influence of different self-emulsifying excipients was observed on the dissolution of DTX-SESD,and the dissolution of DTX-SESD prepared by the solvent method and solvent-melting method were better than that with the melting method.There were no apparent differences among the dissolution medias.Drugs in DTX-SESD were mainly molecules.Conclusion It can greatly improve the solubility and dissolution of docetaxel with self-emulsifying solid dispersion.

关 键 词：多西他赛 固体分散体 自乳化释药系统 溶出度 

分 类 号：R94[医药卫生—药剂学]