目的研究猕猴iv天花粉蛋白突变体(MTCS)的药动学。方法猕猴ivMTCS220μg/kg后, 采用酶联免疫分析(ELISA)测定动物血清中的药物质量浓度, 血药浓度-时间数据用3P97药动程序拟合分析并计算药动学参数。结果MTCS在猕猴体内消除符合二房室模型。6只猕猴的平均消除半衰期(t_1/2β)为(3.82±1.42)h, 平均消除速率(CL)为(276.51±118.61)mL/(kg·h), 药时曲线下面积(AUC_0-24h)为(1124.1±189.5)ng·h/mL。结论用ELISA方法能准确测定动物血清中MTCS质量浓度和研究其药动学。

Objective To study the pharmacokinetics on mutant of trichosanthes(MTCS)after iv administration in macaque.Methods Serum drug concentration was measured by an enzyme-linked 1mmunosorhent assay(ELlSA)after iv injection at a dose of 220μg/kg to macaque,the pharmaeokinetic model and parameters were fited and calculated from the concentration-time data by a 3P97 program.Results The serum drug concentration time curve was fited to a two-compartment model.The pharma-cokinetic parameters were as follows：the mean elimination half life(t_1/2β)was(3.82±l.42)h；the mean serum clearance(CL)was(276.51±118.61)mL/(kg·h)and the mean area under the serum concentration-time curve(AUC_0-24h)was(1 124.1士189.5)ng·h/mL.Conelusion The enzyme-linked immunosorbent assay is shown to be accurate for determination of serum concentration of MTCS and suitable for pharmacokinetic study of MTCS.

国家“863”计划资助项目(2003AA2Z347D);国家“973”计划资助项目(2004CB518902)