Pharmacokinetics of verapamil and norverapamil from controlled release floating pellets in humans.

摘要

Pharmacokinetics of verapamil (V) in a dose of 40 mg and its metabolite norverapamil (N) from the new oral drug formulation in a form of capsule filled with floating pellets was determined. Conventional 40-mg tablets used in a medical practice served as a reference. Bioavailability studies were carried out in 12 healthy volunteers including six men and six women. In an in vitro test the pellets floated on the surface of the extraction fluid for 6 h. Mean value of maximum plasma concentration (C(max)) of V for floating pellets was 28.27 ng ml(-1) and t(max) 3.75 h. The value of the area under the concentrations versus time, AUC(0-infinity) was calculated as 364.65 ng ml(-1) h, biological half-lives of the absorption and elimination (t(0.5el)) phase were 0.5 h and 10.68 h, respectively. For the reference conventional tablets those values were 33.07 ng ml(-1), 1.21 h, 224.22 ng ml(-1) h, 0.36 h and 6.17 h, respectively. The average concentration of N in plasma was similar to that of V.