PHARMACOKINETICS OF ELTOPRAZINE IN HEALTHY MALE-SUBJECTS AFTER SINGLE DOSE ORAL AND INTRAVENOUS ADMINISTRATION

The kinetics, safety and tolerability of eltoprazine hydrochloride were studied in an open, cross‐over, partially randomised design after single oral (8 mg) and intravenous (3 and 8 mg) doses to 12 healthy male subjects. After intravenous administration, the mean t1/2 ranged from 7 to 9 h, the MRT was 11 h, CL was 487 +/‐ 148 (3 mg dose) and 471 +/‐ 56 (8 mg dose) ml kg‐1 h‐1, while CLR was 226 +/‐ 124 (3 mg dose) and 189 +/‐ 38 (8 mg dose) ml kg‐1 h‐1. The Vss was 3.3 +/‐ 0.7 (3 mg dose) and 3.8 +/‐ 0.5 (8 mg dose) 1 kg‐1. Cumulative renal excretion was 40%. The AUC and the cumulative urinary excretion were directly proportional to dose within the range of 3‐8 mg. Values of tmax varied from 1 to 4 h after oral administration. The mean Cmax value was 24 ng ml‐1 after an oral dose of 8 mg. The plasma elimination half‐life after oral administration was 9.8 +/‐ 3.9 h. Absolute oral bioavailability was 110 +/‐ 32%. Dose‐dependent somnolence was observed. 1990 The British Pharmacological Society