8名男性的血浆中地尔硫䓬浓度与心电图PR间期的关系
Diltiazem concentrations in plasma vs PR intervals on electrocardiogram in 8 men.
作者信息
Liu X D, Xie L, Zhong B, Xu Q, Luan L B, Liu G Q
机构信息
Centre of Metabolism & Pharmacokinetics, China Pharmaceutical University, Nanjing, China.
出版信息
Zhongguo Yao Li Xue Bao. 1996 Sep;17(5):411-4.
AIM
To develop an acute tolerant model in describing relationship between diltiazem (Dil) concentrations in plasma and PR intervals on ECG in men.
METHOD
Both plasma concentrations of Dil and changes of ECG were simultaneously determined after po Dil 90 mg in 8 men.
RESULTS
A two-compartmental pharmacokinetic model with first-order input gave a good fitting for the plasma concentration of Dil. Corresponding pharmacokinetic parameters were estimated: t1/2 beta, 5.9 +/- 1.0 h; MRT, 15.9 +/- 1.0 h; t0, 0.38 +/- 0.07 h; tmax, 2.7 +/- 0.4 h, and Cmax, 161 +/- 60 micrograms.L-1. The good fittings for plasma concentration-effect data were obtained with tolerant model E = S x C/(1 + T/T50). The pharmacodynamic parameters were given as follows: S, 829 +/- 293 s.g-1.L; Kt0, 0.037 +/- 0.024 h-1 and T50, 10 +/- 4 micrograms.L-1.
CONCLUSION
Relationship between Dil concentrations in plasma and PR interval changes in men after po 90 mg was described using an acute tolerant model.
目的
建立一个急性耐受模型，以描述男性血浆中地尔硫䓬（Dil）浓度与心电图PR间期之间的关系。
方法
8名男性口服90mg地尔硫䓬后，同时测定血浆中地尔硫䓬浓度和心电图变化。
结果
具有一级输入的二室药代动力学模型对地尔硫䓬的血浆浓度拟合良好。估算了相应的药代动力学参数：t1/2β，5.9±1.0小时；平均滞留时间（MRT），15.9±1.0小时；t0，0.38±0.07小时；达峰时间（tmax），2.7±0.4小时，以及峰浓度（Cmax），161±60μg·L-1。采用耐受模型E = S×C/（1 + T/T50）获得了良好的血浆浓度-效应数据拟合。药效学参数如下：S，829±293 s·g-1·L；Kt0，0.037±0.024 h-1和T50，10±4μg·L-1。
结论
采用急性耐受模型描述了男性口服90mg后血浆中地尔硫䓬浓度与PR间期变化之间的关系。
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