A rapid and simple high-performance liquid chromatographic method with amperometric detection has been developed for the quantitation of cilazapril and its active metabolite and degradation product cilazaprilat in urine and tablets. The chromatographic system consisted of a microBondapak C18 column, using a mixture of methanol-5 mM phosphoric acid (50:50, v/v) as mobile phase, which was pumped at a flow-rate of 1.0 ml/min. The column was kept at a constant temperature of (40+/-0.2) degrees C. Detection was performed using a glassy carbon electrode at a potential of 1350 mV. Sample preparation for urine consisted of a solid-phase extraction using C8 cartridges. This procedure allowed recoveries greater than 85% for both compounds. The method proved to be accurate, precise and sensitive enough to be applied to pharmacokinetic studies and it has been applied to urine samples obtained from four hypertensive patients (detection limit of 50 ng/ml for cilazapril and 40 ng/ml for cilazaprilat in urine). Results were in good agreement with pharmacokinetic data.