贝那普利对氨氯地平药代动力学的影响

目的:比较受试者口服复方贝那普利(含盐酸贝那普利10 mg 和苯磺酸氨氯地平5 mg) 和氨氯地平(5 mg) 后体内氨氯地平的药代动力学特征, 研究氨氯地平和贝那普利之间的相互作用。方法:采用两制剂、两周期随机交叉试验设计, 12名男性健康受试者自身对照, 口服复方贝那普利或氨氯地平。应用LC/MS/MS 方法测定氨氯地平的血药浓度, 并采用WinNonLin 软件计算药代动力学参数。结果:复方和单方制剂中氨氯地平的平均药代动力学参数如下:C_max 分别为(2.6 ±0.6) 、(2.8 ±0.7) μg/L, t _max 分别为(5.8 ±1.3) 、(5.3 ±1.0) h, AUC_{0 -144} 分别为(99 ±39) 、(109 ±26) μg^。L^-1。h, t _1/2分别为(37 ±6) 、(44 ±12) h 。各参数在两制剂间均无统计学意义。结论:贝那普利对氨氯地平在人体内的药动学过程没有显著影响。

Effects of benazepril on pharmacokinetics of amlodipine in healthy volunteers

AIM:To study the pharmacokinetics of amlodipine after coadministration of benazepril (10mg) plus amlodipine (5mg), or amlodipine (5mg) alone in healthy volunteers, and to evaluate the effects of pharmacokinetic interaction between amlodipine and benazepril.METHODS:Twelve male healthy volunteers were enrolled in a randomized two-way crossover study. An LC-MS-MS method was established for the determination of amlodipine in human plasma, and the data were analysed by WinNonLin software.RESULTS:The mean pharmacokinetic parameters of amlodipine after coadministration with benazepril plus amlodipine, or amlodipine alone were as follows:C_max were (2.6 ±0.6) and (2.8 ±0.7) μg/L,AUC_{0 -144} were (99 ±39) and (109 ±26) μg^。L ^-1。h, t max were (5.8 ±1.3) and (5.3 ±1.0) h, t_1/2 were (37 ±6) and (44 ±12) h, respectively.There were no significant differences in these parameters between coadministration of benazepril plus amlodipine and amlodipine administered alone (P >0.05 ).CONCLUSION:Coadministration with benazepril did not significantly affect the pharmacokinetics of amlodipine.