刘晓东, 谢林, 王进, 周云曙, 王珍, 刘国卿. 十名志愿者口服维拉帕米缓释片药代动力学和心电图研究J. 药学学报, 1996, 31(7): 487-491.
引用本文: 刘晓东, 谢林, 王进, 周云曙, 王珍, 刘国卿. 十名志愿者口服维拉帕米缓释片药代动力学和心电图研究J. 药学学报, 1996, 31(7): 487-491.
XD Liu, L Xie, J Wang, YS Zhou, Z Wang , GQ Liu, . PHARMACOKINETIC AND ELECTROCARDIOGRAPHIC STUDY OF ORAL VERAPAMIL SUSTAINED RELEASE TABLET IN 10 CHINESE VOLUNTEERSJ. Acta Pharmaceutica Sinica, 1996, 31(7): 487-491.
Citation: XD Liu, L Xie, J Wang, YS Zhou, Z Wang , GQ Liu, . PHARMACOKINETIC AND ELECTROCARDIOGRAPHIC STUDY OF ORAL VERAPAMIL SUSTAINED RELEASE TABLET IN 10 CHINESE VOLUNTEERSJ. Acta Pharmaceutica Sinica, 1996, 31(7): 487-491.

十名志愿者口服维拉帕米缓释片药代动力学和心电图研究

PHARMACOKINETIC AND ELECTROCARDIOGRAPHIC STUDY OF ORAL VERAPAMIL SUSTAINED RELEASE TABLET IN 10 CHINESE VOLUNTEERS

  • 摘要: 对10名男性受试者单剂量po240mgVer缓释片药代动力学及心电图变化进行研究。血药浓度—时间数据用零级吸收过程的一室模型拟合,其药代动力学参数:Tmax5.9±1.6h;Cmax118.9±37.2μg·L-1;T1 5.4±1.5h;k030.5±17.5μg·L-1·h-1;T1/210.8±4.9h。PR间期延长有显著意义,血药浓度与PR间期变化满足S型模型,其药效学参数:EC50 64.6±16.9μg·L-1; Emax54±11ms;s 1.68±0.66。

     

    Abstract: 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 μg·5L-1 ; T1, 5.4±1.5 h; k0, 30.5±17.5 μg·5L-1 5h -1 ; T1/2, 10.8 ±4.9 h; MRT, 15.4±3.2 h and AUC. 1.96±0.82 mg·5h·5L-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 μg·5L-1 , Emax, 54±11 ms and s, 1.68±0.66.

     

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