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Pharmacokinetics, Pharmacodynamics, and Tolerability of Single and Multiple Doses of Trandolapril, an Effective Angiotensin-Converting Enzyme Inhibitor, in Healthy Chinese Subjects 期刊论文

编号：

85e9104a-fafe-45c4-a16f-774c02465902
作者：

Li, Xiaojiao(李晓娇)#^[1]Liu, Chang(刘畅)#^[2]Wu, Min(武敏)^[1]Zhang, Hong(张洪)^[1]Sun, Yanfu^[1];Cheng, Longmei^[3];Chen, Hong(陈红)^[1]Liu, Chengjiao^[1];Yang, Lizhi^[1];Zhang, Qi^[1];Cao, Yuchen^[4];Gu, Jingkai(顾景凯)^[3]Ding, Yanhua(丁艳华)*^[1]
语种：

英文
期刊：

EUROPEAN JOURNAL OF DRUG METABOLISM AND PHARMACOKINETICS ISSN：0378-7966 2016 年 41 卷 4 期 (373 - 384) ; AUG
收录：
摘要：

Trandolapril is the pro-drug of trandolaprilat, a non-sulfhydryl angiotensin-converting enzyme inhibitor. This study was designed to assess the pharmacokinetics (PK), pharmacodynamics (PD), and tolerability of single and multiple doses of trandolapril in healthy Chinese subjects. Healthy subjects (six men and six women) were randomized into a single-dose, 3 x 3 crossover study (1-2-4 mg, 2-4-1 mg, and 4-1-2 mg), and a multiple-dose study (2 mg/day, 6 days). Serial blood and urine samples were collected after drug administration and analyzed using a validated LC-MS/MS method, and the trandolapril and trandolaprilat PK parameters were obtained. PD was evaluated by the changes in blood pressure and heart rates after dosing. Tolerability was assessed by monitoring adverse events, vital signs, ECGs, and changes in laboratory tests. In the single-dose study, trandolapril was absorbed rapidly, and peak plasma levels (C (max), 1.57, 3.77, and 7.99 ng/mL) and AUCs (1.89, 3.46, and 6.47 ng/mL) were dose-dependent. The AUC(0-a) of trandolaprilat was dose-dependent, but in a non-linear fashion. The cumulative urine excretion of trandolapril and trandolaprilat was 5.51, 6.20, and 7.41 % for three doses, respectively. In the multiple-dose study, steady-state pharmacokinetics was observed; there was no trandolapril accumulation, but there was mild trandolaprilat accumulation (R = 1.67). Trandolapril was well tolerated. The most pronounced reductions in blood pressure were observed at 8 h after administration, which was later than T (max). No orthostatic hypotension occurred. The pharmacokinetics and pharmacodynamics following single and multiple oral doses trandolapril in healthy Chinese subjects are similar to those observed in non-Chinese healthy subjects.
推荐引用方式
GB/T 7714：

Li Xiaojiao,Liu Chang,Wu Min, et al. Pharmacokinetics, Pharmacodynamics, and Tolerability of Single and Multiple Doses of Trandolapril, an Effective Angiotensin-Converting Enzyme Inhibitor, in Healthy Chinese Subjects [J].EUROPEAN JOURNAL OF DRUG METABOLISM AND PHARMACOKINETICS,2016,41(4):373-384.
APA：

Li Xiaojiao,Liu Chang,Wu Min,Zhang Hong,&Ding Yanhua.(2016).Pharmacokinetics, Pharmacodynamics, and Tolerability of Single and Multiple Doses of Trandolapril, an Effective Angiotensin-Converting Enzyme Inhibitor, in Healthy Chinese Subjects .EUROPEAN JOURNAL OF DRUG METABOLISM AND PHARMACOKINETICS,41(4):373-384.
MLA：

Li Xiaojiao, et al. "Pharmacokinetics, Pharmacodynamics, and Tolerability of Single and Multiple Doses of Trandolapril, an Effective Angiotensin-Converting Enzyme Inhibitor, in Healthy Chinese Subjects" .EUROPEAN JOURNAL OF DRUG METABOLISM AND PHARMACOKINETICS 41,4(2016):373-384.
入库时间：

12/16/2019 3:18:07 PM
更新时间：

12/16/2019 3:18:07 PM
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