Pharmacokinetics and tissue penetration of gemifloxacin following a single oral dose.
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 plasma, inflammatory blister fluid and urine were determined using a microbial assay. 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 half-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 36.11% of the total given. These results demonstrate that gemifloxacin penetrates into the site of inflammation and reaches sufficient concentrations to inhibit many pathogens.
Department of Medical Microbiology, City Hospital NHS Trust, Birmingham B18 7QH, UK.
T
T
Gee
J M
JM
Andrews
J P
JP
Ashby
G
G
Marshall
R
R
Wise
D000284:Administration, Oral; D000328:Adult; D000890:Anti-Infective Agents / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine; D001768:Blister / Q000378:metabolism; D003627:Data Interpretation, Statistical; D024841:Fluoroquinolones; D000077735:Gemifloxacin; D006207:Half-Life; D006801:Humans; D007249:Inflammation / Q000097:blood / Q000378:metabolism / Q000652:urine; D008297:Male; D009287:Naphthyridines / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine; D012867:Skin / Q000378:metabolism / Q000473:pathology
D000890:Anti-Infective Agents; D024841:Fluoroquinolones; D009287:Naphthyridines; D000077735:Gemifloxacin