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目的 探讨健康人单用美多洛尔 (Met)、卡托普利 (Cap)及合用两药时体内的药代动力学过程并进行比较 ,考察两药同时服用后其药代动力学特性和相互作用。方法 对 12名健康志愿受试者进行随机交叉实验 ,分 3组 ,每组 4人 ,每组先后分别给予Met 5 0mg ,Cap 5 0mg,Met+Cap各 5 0mg。采用HPLC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 ,求算药代动力学参数。结果 美多洛尔的Ke值较单用时明显减少 (P <0 .0 1) ;而t1/2K,cmax和AUC则明显增大。卡托普利在单用及合用时药代动力学参数无明显变化。结论 两药合用后美多洛尔的肝脏代谢受到抑制。提示临床联合用药时应监测患者体内美多洛尔血药浓度 ,避免不良反应发生。
Objective To investigate the pharmacokinetics and pharmacokinetics of metoprolol (Met) alone, captopril (Cap) and the combination of two drugs in healthy volunteers and to compare their pharmacokinetics with interaction. Methods Twelve healthy volunteers were randomly divided into three groups with 4 in each. Met 50 mg, Cap 50 mg, and Met + Cap 50 mg were given to each group. The plasma concentration was determined by HPLC. The 3P87 pharmacokinetics program was used to process the drug-time data of the subjects, fitting the atrioventricular model and calculating the pharmacokinetic parameters. Results The values of Keratolol decreased significantly (P <0.01), while the values of t1 / 2K, cmax and AUC increased significantly. Captopril alone and in combination with no significant changes in pharmacokinetic parameters. Conclusion The hepatic metabolism of metoprolol is inhibited after the two drugs are combined. Prompt clinical combination therapy should be monitored in patients with metoprolol blood concentration, to avoid adverse reactions.