美托洛尔与卡托普利在老年人体内的药动学特性和相互作用

PHARMACOKINETICS INTERACTION BETWEEN METOPROLOL AND CAPTOPRIL IN ELDERLY HEALTHY VOLUNTEERS

①目的 探讨老年人美托洛尔 (Met)、卡托普利 (Cap)合用后其药代动力学特性和相互作用。②方法对 12名健康老年志愿受试者进行随机交叉实验 ,分为 3组 ,每组 4名 ,每组先后分别给予Met 5 0mg ,Cap 5 0mg ,Met+Cap各 5 0mg .采用HPLC法测定血药浓度。用 3P87药代动力学程序对受试者药 时数据进行处理 ,拟合房室模型 ,计算药动学参数。③结果 Met的Ke值较单用时明显减小 (t=6 .73 ,P <0 .0 1) ;而T12 K,Cmax和AUC则明显增大(t=2 .99～ 4.39,P <0 .0 1)。Cap在单用及合用药时药动学参数无明显变化。④结论 两药合用后Met的肝脏代谢受到抑制。临床联合用药时应监测病人体内Met血药浓度 。

Objective\ To investigate the pharmacokinetic characteristics and interaction in old man when two drugs are given simultaneously.\ Methods\ Twelve elderly healthy volunteers were equally divided into three groups with each volunteer taking a single dose of metoprolol 50mg,captopril 50mg and both of them ,respectively,in an open randomized crossover study. HPLC method was used to determine plasma concentration of two drugs. Fit the different time plasma concentration values to 3P87 programe on computer to get pharmacokinetic parameters.\ Results\ Pharmacokinetic parameters Ke of metoprolol was decreased( t=6.73,P <0.01) while T 12K ,C max ,AUC were increased significantly( t=2.99-4.39,P <0.01) and parameters of captopril had no changes when two drugs being taken simultaneously. \ Conclusion\ Blood concentration of metoprolol should be monitored for averting harmful reactions because captopril inhibited Metoprolol metabolism in liver.