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氨氯地平对贝那普利及其代谢物药动学的影响 被引量:6

Effect of amlodipine on pharmacokinetics of benazepril and its metabolite in healthy volunteers
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摘要 目的:比较受试者口服复方贝那普利(含盐酸贝那普利10mg和苯磺酸氨氯地平5mg)和贝那普利(10mg)后体内的药动学特征,研究贝那普利和氨氯地平之间的相互作用。方法:采用两制剂、两周期交叉实验设计,12例健康受试者自身对照,口服复方贝那普利或贝那普利。应用LC/MS/MS方法测定贝那普利的血药浓度,并采用WinNonLin软件计算药动学参数。结果:①复方和单方制剂中贝那普利原型的平均药动学参数如下:C_(max) (150.3±68.4)和(154.1±79.9)μg·L^(-1),T_(max)(0.53±0.18)和(0.46±0.16)h,AUC_(0-10b)(138.9±61.9)和(132.5±59.4)μg·h·L^(-1),t_(1/2)(1.2±0.7)和(1.5±1.1)h。②复方和单方制剂中代谢物贝那普利拉的平均药动学参数如下:C_(max)(146.7±79.8)和(119.3±50.9)μg·L^(-1),T_(max)(2.0±0.9)和(1.6±0.5)h,AUC_(0~10h)(546.7±218.5)和(515.1±230.9)μg·h·L^(-1),各参数在两制剂间均不存在显著性差异。结论:氨氯地平对贝那普利在人体内的药动学过程没有显著影响。 Objective: To study the pharmacokinetics of benazepril after co-administration of benazepril ( 10 mg) plus amlodipine(5 mg) ,or benazepril( 10 mg) alone in healthy volunteers, and to evaluate the pharmacokinetic interaction between benazepril and amlodipine. Methods: Twelve male healthy volunteers were enrolled in a randomized two-way crossover study. A LC-MS-MS method was established for the determination of benzaepril and its metabolite benazeprila in human plasma, and the data were analyzed by WinNonLin software. Results: The mean pharmacokinetic parameters of benazepril after co-administration of benazepril plus amlodipine, or benazepril alone were as follows : Cmax ( 150.3 ± 68.4) and (154.1±79.9) μg·L^-1,Tmax(0.53±0. 18)and (0.46±0. 16)h,AUC0-10h(138.9±61. 9) and ( 132.5 ± 59.4) μg·h·L^-1, t1/2 ( 1.2 ± 0.7) and ( 1.5 ± 1.1 ) h, respectively. The mean pharmacokinetic parameters of benazeprila were as follows : Cmax ( 146.7±79.8 ) and ( 119.3 ± 50.9) μg·L^-1, Tmax(2.0±0.9) and (1.6±0.5) h, AUC0-10h (546.7±218.5) and (515.1±230.9)μg·h·L^-1 ,respectively. There were no significant differences in these parameters between co-administration of benazepril plus amlodipine and benazepril alone (P 〉 0.05 ). Conclusion : Amlodipine did not significantly affect the pharmacokinetics of benazepril after co-administration drug.
出处 《中国新药杂志》 CAS CSCD 北大核心 2007年第20期1705-1708,共4页 Chinese Journal of New Drugs
基金 863国家攻关项目<临床试验关键技术及平台研究>(2004AA223760)
关键词 贝那普利 氨氯地平 液相色谱-质谱法 药动学 相互作用 benazepril amlodipine HPLC-MS-MS pharmacokinetics interaction
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参考文献8

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二级参考文献5

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