Absorption and Excretion of Cinepazide (Vasodilator) after Single and Multiple Oral Doses in Man

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The concentrations of cinepazide in human plasma and urine were studied byusing high-performance liquid chromatography. Each of 7 healthy, male volunteersreceived 200 and 400 mg of cinepazide on separate occasions for single doseexperiments. In the case of the 200 mg single dose, a rapid peak of plasma concentrationat2.8-4.9μg/ml was observedat 1-3hr, and 57.6% of the cinepazidewas excreted in urine within 24 hr. The peak plasma level increased proportionallywith the dose of cinepazide, whereas the extent of cinepazide excretionincreased slightly with the dose.<BR>In multiple dose experiments, each of these volunteers received, on two separateoccasions, 200 mg of cinepazide t. i. d. at 9: 00 am, 1: 00 pm and 5: 00 pm eachday for 1 day and 5 days, respectively. The results on the peak and valley plasmalevels of multiple dose cinepazide indicated reproducible absorption in comparisonwith values predicted using a computer program describing a one compartment, open pharmacokinetic model. The extent of cumulative urinary excretion ofcinepazide was nearly constant during multiple dose experiments . No side effectswere noted.
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