Hioavailability of Captopril Sustained-rdease Tablets / 第二军医大学学报

ABSTRACT

Bioavailable studies were performed based on plasma concentrations of captopril in 5 Beagle dogs and 5 male healthy volunteers after a single oral administration of captopril sustained-release tablet and sugar-coated tablet. A one-compartment model was adopted. Relative bioavailability of sustained-release tablet to sugar-coated one was 131.6% for dogs and 111.0% for humans. Their mean residence times (MRTs) were 4.52 h and 1.96 h in dogs, 4.28 h and 2.77 h in humans, respectively. The maximum concentrations were 995.9 ng/ml and 2470.8 ng/ml in dogs, 126.2 ng/ml and 251.2 ng/ml in humans for two kinds of tablets, respectively. The duration time, in which plasma concentration staved above 50% inhibitory concentration of angiotensin converting enzyme activity, was more than 10 h for sustained-release tablets and 6h for sugar-coated tablets at the same dose (37.5 mg). consequently, it could be expected that the sustained-release tablet dosed twice a day should have a greater efficiency than marketed sugar-coated tablet taken 3 times daily.