Captopril kinetics

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Abstract
Captopril, an angiotensin-converting enzyme inhibitor with antihypertensive properties, was given orally and i.v. in 10-mg doses to 5 healthy subjects. After i.v. dosing, semilogarithmic plots of captopril blood levels:time showed a triexponential decay. Data were analyzed using an open 3-compartment model. The average volume of distribution (Vd) was 0.2 l/kg for the central compartment and 2 l/kg for the elimination (.beta.) phase. The Vd at steady-state was 0.7 l/kg. The total body clearance of captopril averaged 0.8 l/kg per h and the mean blood half-life during the .beta. phase was 1.9 h. In the 0- to 96-h urine, after i.v. and oral drug, excretion of radioactivity accounted for 87 and 61% of dose. In the 0- to 24-h urine, averages of 38% (i.v.) and 24% (oral) of the doses were excreted as unchanged captopril. Absolute absorption of the radioactive oral dose was 71% and the absolute oral bioavailability of captopril was 62%.

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