热熔挤出技术制备普罗布考固体分散体及其大鼠体内药动学研究  

Preparation and Pharmacokinetics in Rats of Probucol Solid Dispersions by Hot-melt Extrusion Process

作　　者：黄健[1,2] 顾王文[2] 蒋世军[2] 张志文[2] 陈伶俐[2] 

机构地区：[1]江苏大学药学院,江苏镇江212013 [2]中国科学院上海药物研究所,上海201203

出　　处：《中国医药工业杂志》2011年第12期902-906,共5页Chinese Journal of Pharmaceuticals

基　　金：国家重点基础研究发展计划(2009CB930304)

摘　　要：以Soluplus为载体,采用热熔挤出技术制备普罗布考固体分散体,并评价其平衡溶解度、溶出度及大鼠体内药动学行为。结果表明,普罗布考-Soluplus比例为1:3(w/w)的固体分散体,在30 min时的体外累积溶出率为97%。差示扫描量热和粉末X-射线衍射分析表明药物主要以分子状态分散于固体分散体中。大鼠体内药动学研究表明,普罗布考固体分散体的c_(max)和口服生物利用度是原药的3.26倍和3.02倍。The probucol solid dispersions were prepared with Soluplus as the carrier by hot-melt extrusion process. The equilibrium solubility, dissolution rate and pharmacokinetic behavior in rats of the products were evaluated. The results showed that the cumulative release amount at 30 min from the solid dispersions with the probucol/Soluplus weight ratio of 1 ; 3 was 97%. The results of differential scanning calorimetry and powder X-ray diffraction suggested that probucol dispersed mainly in the molecular state. The results of pharmacokinetics in rats showed that the Cmax and A UC of probucol solid dispersions were 2.26 times and 2.02 times higher than those of bulk drug, respectively.

关 键 词：热熔挤出 固体分散体 普罗布考 溶出度 生物利用度 

分 类 号：R944.9[医药卫生—药剂学]