索法酮固体分散体的制备及体外溶出度的研究  

Preparation and dissolution of Sofalcone solid dispersion

作　　者：代孔恩[1] 任晓文[2] 李洪起[2] 连潇嫣[2] 何应[1] 

机构地区：[1]天津大学药物科学与技术学院,天津300072 [2]天津药物研究院,天津300193

出　　处：《天津药学》2008年第3期27-30,共4页Tianjin Pharmacy

摘　　要：目的:提高制剂中索法酮体外溶出度。方法:选择水溶性载体聚乙二醇4000(PEG4000)和聚乙烯吡咯烷酮K30(PVPK30)用熔融法制备索法酮固体分散体,建立紫外-可见分光光度法测定固体分散体的溶出度的方法。结果:紫外-可见分光光度法测定索法酮的溶出度,方法准确可靠、稳定且无载体的干扰。制备的固体分散体能显著地提高索法酮的体外溶出度;以聚乙二醇(PEG4000)为载体制备的固体分散体溶出度高于聚乙烯吡咯烷酮K30(PVPK30)。差示扫描热量法(DSC)研究表明,在质量比为1∶8索法酮-聚乙二醇4000(PEG4000)固体分散体中,索法酮以无定形的状态分散在固体分散体中,其熔点吸热峰消失。结论:索法酮固体分散体的体外溶出度增大,与载体的结构及其在良好载体固体分散体中的无定形状态有关。OBJECTIVE To improve the dissolution of sofalcone in vitro. METHODS Sofalcone solid dispersion was prepared. The dissolutions of the solid dispersion were detected with a UV - visible spectrophotometer. RESULTS The dissolution of sofalcone solid dispersion by UV - visible spectrophotometry was accurate, reliable, stable and non - carrier interference. Preparation of solid dispersion significantly improved its dissolution in vitro. The solid dispersion carrier by PEG4000 dissolves was more rapidly than the one by polyethylenepyrrolidone K30 （ PVPk30/. DSC studies showed that sofalcone was dispersed in solid dispersion （ so- falcone -PEG = 1： 8） by amorphous state and its melting point endothermic peak disappeared. CONCLUSION Sofaleone solid dispersion is able to enhance its dissolution in vitro ,which is concerned with the cartier structure and the amorphous state of good carrier solid dispersing medium.

关 键 词：索法酮 固体分散体 差示扫描量热法(DSC) 溶出度 

分 类 号：TQ460.6[化学工程—制药化工] R96[医药卫生—药理学]