Concentrations of gemifloxacin at the target site in healthy volunteers after a single oral dose.
Free gemifloxacin concentrations in the interstitial space fluid of skeletal muscle and subcutaneous adipose tissue were measured by means of in vivo microdialysis to characterize the ability of gemifloxacin to penetrate human soft tissues. Twelve healthy volunteers received a single oral dose of 320 mg of gemifloxacin. The mean areas under the concentration-time curves from 0 to 10 h (AUC(0-10)) were significantly higher for soft tissue than for unbound gemifloxacin in plasma (P < 0.05). The ratios of the mean AUC(0-10) for tissue to the AUC(0-10) for free gemifloxacin in plasma were 1.7 +/- 0.7 (mean +/- standard deviation) for skeletal muscle and 2.4 +/- 1.0 for adipose tissue. The AUC(0-24) ratios for free gemifloxacin in tissues to the MIC at which 90% of frequently isolated bacteria are inhibited were close to or higher than 100 h. Therefore, based on pharmacokinetic and pharmacodynamic calculations, we conclude that gemifloxacin might be a useful therapeutic option for the treatment of soft tissue infections.
Islinger
Florian
F
Department of Clinical Pharmacology, Division of Clinical Pharmacokinetics, Medical University of Vienna, Allgemeines Krankenhaus, Waehringer Guertel 18-20, 1090 Vienna, Austria.
Bouw
Rene
R
Stahl
Mathias
M
Lackner
Edith
E
Zeleny
Petra
P
Brunner
Martin
M
Müller
Markus
M
Eichler
Hans Georg
HG
Joukhadar
Christian
C
D000273:Adipose Tissue / Q000378:metabolism; D000328:Adult; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D019540:Area Under Curve; D001682:Biological Availability; D024841:Fluoroquinolones / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D000077735:Gemifloxacin; D006207:Half-Life; D006801:Humans; D008297:Male; D017551:Microdialysis; D018482:Muscle, Skeletal / Q000378:metabolism; D009287:Naphthyridines / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D015231:Sexually Transmitted Diseases, Bacterial / Q000188:drug therapy / Q000382:microbiology
D000900:Anti-Bacterial Agents; D024841:Fluoroquinolones; D009287:Naphthyridines; D000077735:Gemifloxacin