石杉碱甲片在六名志愿者体内的药物动力学

摘要

目的:了解石杉碱甲片在人体内的药物动力学过程,为设计临床用药方案提供依据.方法:用反相高效液相色谱法测定六名健康志愿者口服片剂0.99 mg后的血药浓度,按3P87程序计算动力学参数.结果:石杉碱甲片在体内的药时过程符合一级吸收的一室开放模型.主要动力学参数:T1/2ka 12.6 min,T1/2ke 288.5min,Tmax79.6 min,Cmax8.4 μg L-1,AUC4.1 mg L-1min.结论:石杉碱甲吸收迅速,属于中等速率消除类药物.%AIM: To study pharmacokinetics of tablet huperzine A (Hup-A) in Chinese volunteers to help establishing its drug administration schedule. METHODS: For 6 volunteers after a single oral dose of 0.99 mg, drug concentrations in plasma were assayed by reverse phase high pressure liquid chromatography (HPLC)at 0.5, 0.75, 1.0, 1.25, 1.5, 2, 4, 6, 8,and 10 h. The pharmacokinetic parameters were calculated with a 3P87 program by computer. RESULTS: The time course of plasma concentrations conformed to a one-compartment open model with a first order absorption. The pharmacokinetic parameters were as follows: T1/2ka = 12.6 min, T1/2ke = 288. 5min, Tmax = 79.6 min, Cmax = 8.4 μg L-1,AUC = 4.1 mg L-1 min. CONCLUSION:Hup-A was absorbed rapidly, distributedwidely in the body, and eliminated at a moder-ate rate.