Quantitative assessment of the hepatic pharmacokinetics of the antimicrobial sitafloxacin in humans using in vivoF magnetic resonance spectroscopy.
OBJECTIVE
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.
Payne
Geoffrey S
GS
Cancer Research UK Clinical Magnetic Resonance Research Group, The Institute of Cancer Research and Royal Marsden NHS Trust, Sutton, Surrey, UK. gsp@icr.ac.uk
Collins
David J
DJ
Loynds
Peter
P
Mould
Graham
G
Murphy
Philip S
PS
Dzik-Jurasz
Andrzej S K
AS
Kessar
Preminda
P
Haque
Nazneen
N
Yamaguchi
Masayuki
M
Atarashi
Shogo
S
Leach
Martin O
MO
D000293:Adolescent; D000328:Adult; D000890:Anti-Infective Agents / Q000493:pharmacokinetics*; D002851:Chromatography, High Pressure Liquid; D005462:Fluorine Radioisotopes; D024841:Fluoroquinolones / Q000493:pharmacokinetics*; D006207:Half-Life; D006801:Humans; D008099:Liver / Q000378:metabolism*; D009682:Magnetic Resonance Spectroscopy / Q000379:methods; D008297:Male
D000890:Anti-Infective Agents; D005462:Fluorine Radioisotopes; D024841:Fluoroquinolones; C076246:sitafloxacin