Quantitative assessment of the hepatic pharmacokinetics of the antimicrobial sitafloxacin in humans using in vivoF magnetic resonance spectroscopy

Br J Clin Pharmacol. 2005 Feb;59(2):244-8. doi: 10.1111/j.1365-2125.2004.02246.x.

Abstract

Aims: To measure hepatic concentrations of the fluorine-containing antimicrobial, sitafloxacin, using in vivo(19)F magnetic resonance spectroscopy (MRS).

Methods: Data were acquired from eight healthy subjects at 2, 5, 8 and 24 h following doses of 500 mg day(-1) for 5 days using a (1)H/(19)F surface coil in a 1.5T clinical MR system. Tissue water was used as a reference.

Results: Estimated liver concentrations at 2 h were 15.0 +/- 4.0 microg ml(-1) (mean +/- 95% CI), compared with 3.54 +/- 0.58 microg ml(-1) in plasma (n = 6), and fell below threshold concentrations (2 microg ml(-1)) by 24 h.

Conclusions: (19)F MRS is able to detect and quantify sitafloxacin in the liver. There was no evidence for the hepatic retention of the drug.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adolescent
  • Adult
  • Anti-Infective Agents / pharmacokinetics*
  • Chromatography, High Pressure Liquid
  • Fluorine Radioisotopes
  • Fluoroquinolones / pharmacokinetics*
  • Half-Life
  • Humans
  • Liver / metabolism*
  • Magnetic Resonance Spectroscopy / methods
  • Male

Substances

  • Anti-Infective Agents
  • Fluorine Radioisotopes
  • Fluoroquinolones
  • sitafloxacin