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氨氯地平在健康人体内的药动学和药效学
引用本文:张梅,杨永革,徐琳,邸晓辉,徐娟,姜楠,许雪廷. 氨氯地平在健康人体内的药动学和药效学[J]. 中国医院药学杂志, 2011, 0(18)
作者姓名:张梅  杨永革  徐琳  邸晓辉  徐娟  姜楠  许雪廷
作者单位:北京军区总医院药理科;
摘    要:
目的:研究苯磺酸氨氯地平片在健康人体的药动学,及血药浓度与降血压效应的关系。方法:24名健康受试者单次口服10 mg苯磺酸氨氯地平片,服药后不同时间采集血样,采用LC-MS-MS法测定血浆中氨氯地平浓度,采用坐位动脉收缩压(SBP)和舒张压(DBP)的变化值为降压药效指标。结果:氨氯地平体内代谢呈二室模型,消除半衰期约36 h,表观分布容积较大,提示为全身分布,峰浓度约为(6.1±1.5)ng.mL-1。动脉收缩压和舒张压在用药后呈波动性下降,用药10 h后药效逐渐消失,可见一个药效滞后环。AUC0-120 h(ng.h.mL-1)和AUEC0-48(mmHg.h-1)分别为(237.1±77.2)和(126.1±49.8)(SBP)、(192.6±47.7)(DBP);Cmax(ng.mL-1)和Emax(mmHg)分别为(6.1±1.5)和(6.3±3.2)(SBP)、(10.1±2.9)(DBP);tmax(h)和TEmax(h)分别为(3.9±0.7)和(8.1±2.3)(SBP)、(9.2±1.2)(DBP)。结论:苯磺酸氨氯地平对动脉收缩压和舒张压均有降低作用,药效达峰时间在给药后6~10 h,均...

关 键 词:氨氯地平  药动学  药效学  动脉收缩压  舒张压  

Study on the pharmacokinetics and pharmacodynamics of amlodipine in healthy chinese subjects
ZHANG Mei,YANG Yong-ge,XU Lin,DI Xiao-hui,XU Juan,JIANG Nan,XU Xue-ting. Study on the pharmacokinetics and pharmacodynamics of amlodipine in healthy chinese subjects[J]. Chinese Journal of Hospital Pharmacy, 2011, 0(18)
Authors:ZHANG Mei  YANG Yong-ge  XU Lin  DI Xiao-hui  XU Juan  JIANG Nan  XU Xue-ting
Affiliation:ZHANG Mei,YANG Yong-ge,XU Lin,DI Xiao-hui,XU Juan,JIANG Nan,XU Xue-ting (Department of Pharmacy,the General Hospital of Beijing Military area commond,Beijing 100700,China)
Abstract:
OBJECTIVE To study the pharmacokinetics and pharmacodynamics of amlodipine in healthy subjects and explore the relationship between the blood concentration of amlodipine and the antihypertensive effect. METHODS 24 male volunteers were administered 10 mg amlodipine by single dose.The blood samples of different time points in these subjects were sampled and the drug concentrations of amlodipine were analyzed by LC-MS-MS,and the primary variables measured in this study were systolic and diastolic blood pressur...
Keywords:amlodipinel  pharmacokinetics  pharmacodynamics  SBP  DBP  
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