Pharmacokmetics and tolerance of a new fluoroquinolone antimicrobial drug after single oral doses in healthy volunteers

Abstract

1. The pharmacokinetics and tolerance of DV-7751a were investigated in healthy male Caucasian volunteers after single oral doses (100, 200, 400 and 800 mg).

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 μg/ml for the 100–800-mg dose and the mean time to reach C_max (t_max) ranged from 1·1 to 1·9h. 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 (AUC). The plasma protein binding of the drug was in the range of 57–65%.

3. Within 48h, the cumulative urinary excretion of unchanged drug amounted to 22·0–26·8% of the dose administered. Faecal recovery of the drug up to 72 h after the 400-mg dose was about 12% of the dose given.

4. Adverse events thought to be possibly related to the drug included headache, rash, leg cramp, diarrhoea, abdominal pain, CNS depression and dizziness. DV-7751a, however, was well tolerated with no serious adverse events at any doses and all subjects completed the study. No drug crystals were observed in the urine