Stereoselective analysis of the disposition of tosufloxacin enantiomers in man.

The pharmacokinetics of tosufloxacin enantiomers after oral administration of racemic tosufloxacin were examined in healthy volunteers. Only small differences were observed in time to peak concentration (2.6 +/- 0.3 [mean +/- SEM] h for (+)-tosulfoxacin vs 2.4 +/- 0.2 h for (-)-tosufloxacin), elimination half-life (3.61 +/- 0.24 h vs 3.49 +/- 0.23 h), and area under the curve (2.78 +/- 0.19 h.micrograms/ml vs 2.87 +/- 0.19 h.micrograms/ml); however, peak concentration (0.40 +/- 0.03 microgram/ml vs 0.44 +/- 0.03 microgram/ml), renal clearance (226 +/- 10 ml/min vs 202 +/- 10 ml/min), and urinary recovery (35.4 +/- 2.2% vs 32.4 +/- 1.9%) differed significantly between enantiomers.