The pharmacokinetics and tissue penetration of gemifloxacin were determined
during a 24 h period following oral administration of a single 320 mg dose
to each of 10 healthy male volunteers. Concentrations of the drug in plasm
a, inflammatory blister fluid and urine were determined using a microbial a
ssay. A peak plasma concentration (mean +/- S.D.) of 2.33 +/- 0.5 mg/L was
reached at 1.20 +/- 0.4 h. Mean penetration into inflammatory fluid was 61.
19 +/- 10.4%. A peak concentration of 0.74 +/- 0.3 mg/L was reached in the
inflammatory fluid at a mean time of 3.40 +/- 1.7 h. The mean elimination h
alf-life from serum and inflammatory fluid was 5.94 +/- 0.4 and 6.27 +/- 2.
4 h, respectively. Urinary excretion of the drug at 24 h post-dose was 36.1
1% of the total given. These results demonstrate that gemifloxacin penetrat
es into the site of inflammation and reaches sufficient concentrations to i
nhibit many pathogens.