Quantitative assessment of the hepatic pharmacokinetics of the antimicrobial sitafloxacin in humans using in vivo 19F magnetic resonance spectroscopy

Abstract

Aims: To measure hepatic concentrations of the fluorine-containing antimicrobial, sitafloxacin, using in vivo 19F 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 1H/19F 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 μg ml-1 (mean ± 95% CI), compared with 3.54 ± 0.58 μg ml-1 in plasma (n = 6), and fell below threshold concentrations (2 μg ml-1) by 24 h. Conclusions: 19F MRS is able to detect and quantify sitafloxacin in the liver. There was no evidence for the hepatic retention of the drug.