固体分散体技术改善多西他赛的体外溶出特性  

Improvement in the dissolution properties of docetaxel using solid dispersion technology

作　　者：陈戈[1] 陈鹰[1] 史琼枝[1] 刘宏[1] 汤韧[1] 

机构地区：[1]广州军区武汉总医院,湖北武汉430070

出　　处：《中国医院药学杂志》2010年第14期1186-1190,共5页Chinese Journal of Hospital Pharmacy

摘　　要：目的:研制多西他赛(DTX)固体分散体以提高其体外溶出度。方法:以聚乙二醇6000(PEG6000)、泊洛沙姆188(F68)为载体制备多西他赛固体分散体,差热分析、X-射线粉末衍射分析以鉴别药物在载体中的存在状态,并进行了稳定性、体外溶出度及影响因素考查。结果:DTX-PEG6000固体分散体中药物主要以分子状态存在。DTX-PEG6000的稳定性远好于DTX-F68。溶剂法的溶出度好于熔融法和溶剂熔融法;载体的用量和投药量的不同对药物溶出有一定影响;介质对溶出影响不大。结论:用溶剂法制备多西他赛固体分散体DTX-PEG6000(1∶6)能显著提高药物的溶出速度和程度。OBJECTIVE To prepare docetaxel solid dispersion （DTX-SD） and improve its dissolution. METHODS DTX-SD was prepared with PEG6000,F68 as carriers. Differential thermal analysis and powder X-ray diffraction were used to determine the status of drug in carriers. The stability test,dissolution in vitro and its effective factors were also studied. RESULTS Drug in DTX PEG6000 solid dispersion almost existed as molecule. The drug in DTX-PEG6000 was more stable than in DTX F68. The dissolution of DTX-PEG6000 prepared by solvent method was better than others. And the dissolution of DTX-PEG6000 was influenced by carrier ratios and the drug content given. There were no apparent differences among different dissolution medias. CONCLUSION DTX PEG6000（1：6） solid dispersion prepared by solvent method can greatly improve the dissolution of docetaxel.

关 键 词：多西他赛 固体分散体 体外溶出度 

分 类 号：R943[医药卫生—药剂学]