STEREOSELECTIVE ANALYSIS OF THE DISPOSITION OF TOSUFLOXACIN ENANTIOMERS IN MAN

The pharmacokinetics of tosufloxacin enantiomers after oral administra tion 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 (+)-tosufloxacin vs 2.4 +/- 0.2 h for (-)-t osufloxacin), elimination half-life (3.61 +/- 0.24 h vs 3.49 +/- 0.23 h), and area under the curve (2.78 +/- 0.19 h . mug/ml vs 2.87 +/- 0.1 9 h . mug/ml); however, peak concentration (0.40 +/- 0.03 mug/ml vs 0. 44 +/- 0.03 mug/ml), renal clearance (226 +/- 10 ml/min vs 202 +/- 10 ml/min), and urinary recovery (35.4 +/- 2.2 % vs 32.4 +/- 1.9 %) diffe red significantly between enantiomers.