10名中国志愿者口服维拉帕米缓释片的药代动力学和心电图研究
[Pharmacokinetic and electocardiographic study of oral verapamil sustained-release tablet in 10 Chinese volunteers].
作者信息
Liu X D, Xie L, Wang J, Zhou Y S, Wang Z, Liu G Q
机构信息
Cente of Pharmacokinetics and Metabolism, China Pharmaceutical University, Nanjing.
出版信息
Yao Xue Xue Bao. 1996;31(7):487-91.
Both verapamil pharmacokinetics and electrocardio graphic changes in 10 Chinese volunteers were studied after po 240 mg of verapamil sustained release tablet. A one-compartment model with zero-order absorption gave a better fitting to concentration--time data with values of r2 > 0.96. The main pharmacokinetic parameters obtained were: Tmax, 5.9 +/- 1.6 h; Cmax, 118.9 +/- 37.2 micrograms.L-1; T1, 5.4 +/- 1.5 h; k0, 30.5 +/- 17.5 micrograms.L-1.h-1; T1/2, 10.8 +/- 4.9 h; MRT, 15.4 +/- 3.2 h and AUC. 1.96 +/- 0.82 mg.h.L-1. There were significant prolongations of PR intervals after dose. Relationships between PR interval changes and plasma concentrations of verapamil were better fitted to sigmoidal model, with r2 > 0.98. The corresponding pharmacodynamic parameters were estimated. EC50, 64.6 +/- 16.9 micrograms.L-1, Emax, 54 +/- 11 ms and s, 1.68 +/- 0.66.
对10名中国志愿者口服240mg维拉帕米缓释片后的维拉帕米药代动力学和心电图变化进行了研究。零级吸收的单室模型对浓度-时间数据拟合效果更好，r2值>0.96。获得的主要药代动力学参数为：达峰时间（Tmax），5.9±1.6小时；峰浓度（Cmax），118.9±37.2微克·升-1；吸收相末端时间（T1），5.4±1.5小时；零级吸收速度常数（k0），30.5±17.5微克·升-1·小时-1；半衰期（T1/2），10.8±4.9小时；平均滞留时间（MRT），15.4±3.2小时；药时曲线下面积（AUC），1.96±0.82毫克·小时·升-1。给药后PR间期有显著延长。PR间期变化与维拉帕米血药浓度之间的关系更好地拟合了S形模型，r2>0.98。估计了相应的药效学参数。半数有效浓度（EC50），64.6±16.9微克·升-1；最大效应（Emax），54±11毫秒；s，1.68±0.66。
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