PHARMACOKINETICS AND TOLERANCE OF A NEW FLUOROQUINOLONE ANTIMICROBIALDRUG AFTER SINGLE ORAL DOSES IN HEALTHY-VOLUNTEERS

1. The pharmacokinetics and tolerance of DV-7751a were investigated in healthy male Caucasian volunteers after single oral doses (100, 200, 400 and 800mg). 2. DV-7751a was rapidly absorbed in the fasted state. The mean maximum concentration in plasma (C-max) ranged from 0.27 to 1 .98 mu g/ml for the 100-800-mg dose and the mean time to reach C-max ( t(max)) ranged from 1.1 to 1.9 h. The terminal half-life ranged from 8 .75 to 10.0h. A good linear correlation (r = 0.974) was found between doses from 100 to 800mg and the resulting area under the concentration -time curve (AUG). The plasma protein binding of the drug was in the r ange of 57-65%. 3. Within 48h, the cumulative urinary excretion of unc hanged drug amounted to 22.0-26.8% of the dose administered. Faecal re covery of the drug up to 72 h after the 400-mg dose was about 12% of t he dose given. 4. Adverse events thought to be possibly related to the drug included headache, rash, leg cramp, diarrhoea, abdominal pain, C NS depression and dizziness. DV-7751a, however, was well tolerated wit h no serious adverse events at any doses and all subjects completed th e study. No drug crystals were observed in the urine