Peng Wei-Bing, Sun Wei-Zhi, Jiang Tao, Li Guo-Qiang, Dai Sheng-jun
Key Laboratory of Marine Drugs, Ministry of Education & Marine Drug and Food Institute, Ocean University of China, Qingdao, China.
J Asian Nat Prod Res. 2010 Oct;12(10):879-93. doi: 10.1080/10286020.2010.508283.
The in vitro metabolism of two novel phosphate prodrugs of glycyrrhetic acid (GA) was studied by the method of incubation in the rat liver microsome and the in vivo plasma pharmacokinetics after injecting intravenously (i.v.) into six rats was investigated, respectively. The prodrugs diminished gradually with time and most of the parent drugs were released in 30 min in vitro. In this paper, the in vivo plasma concentration data were analyzed by compartmental modeling. Both the prodrugs and the corresponding released parent drugs could be described by a two-compartment model, which existed for 48 h in rats. The t(1/2) increases remarkably after i.v. administration to rats when compared with injecting the parent drugs directly.
采用大鼠肝微粒体孵育法研究了两种新型甘草次酸（GA）磷酸酯前药的体外代谢情况，并分别对6只大鼠静脉注射后进行了体内血浆药代动力学研究。前药随时间逐渐减少，体外30分钟内大部分母体药物被释放出来。本文通过房室模型分析体内血浆浓度数据。前药及其相应释放的母体药物均可用二房室模型描述，该模型在大鼠体内存在48小时。与直接注射母体药物相比，大鼠静脉注射前药后t(1/2)显著增加。
