SINGLE-DOSE PHARMACOKINETICS OF FENSPIRIDE HYDROCHLORIDE - PHASE-I CLINICAL-TRIAL

The absolute bioavailability of fenspiride has been studied in twelve healthy volunteers. It was administered IV and orally in single doses of 80 mg fenspiride hydrochloride according to a randomised crossover pattern. Following IV administration, the plasma clearance of fenspiri de was about 184 ml . min-1, and its apparent volume of distribution w as moderately large (215 l). When given orally as a tablet, fenspiride exhibited fairly slow absorption; the maximum plasma concentration (2 06 ng . ml-1) was achieved 6 h after administration. The absolute bioa vailability was almost complete (90 %). The tablet had slow release ch aracteristics. The elimination half-life obtained from the plasma data was 14 to 16 h independent of the route of administration.