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 r
2>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 r
2>0.98. The corresponding pharmacodynamic parameters were estimated. EC
50 , 64.6±16.9 μg·5L
-1 ,
Emax, 54±11 ms and s, 1.68±0.66.