title: Concentrations of gemifloxacin at the target site in healthy volunteers after a single oral dose.
abstract: 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.
authors.affiliation: Department of Clinical Pharmacology, Division of Clinical Pharmacokinetics, Medical University of Vienna, Allgemeines Krankenhaus, Waehringer Guertel 18-20, 1090 Vienna, Austria.
authors.forename: Florian
authors.initials: F
authors.lastname: Islinger
authors.forename: Rene
authors.initials: R
authors.lastname: Bouw
authors.forename: Mathias
authors.initials: M
authors.lastname: Stahl
authors.forename: Edith
authors.initials: E
authors.lastname: Lackner
authors.forename: Petra
authors.initials: P
authors.lastname: Zeleny
authors.forename: Martin
authors.initials: M
authors.lastname: Brunner
authors.forename: Markus
authors.initials: M
authors.lastname: Müller
authors.forename: Hans Georg
authors.initials: HG
authors.lastname: Eichler
authors.forename: Christian
authors.initials: C
authors.lastname: Joukhadar
mesh_terms: 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
chemical_list: D000900:Anti-Bacterial Agents; D024841:Fluoroquinolones; D009287:Naphthyridines; D000077735:Gemifloxacin