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Quantitative assessment of the hepatic pharmacokinetics of the antimicrobial sitafloxacin in humans using in vivo 19 F magnetic resonance spectroscopy
Author(s) -
Payne Geoffrey S.,
Collins David J.,
Loynds Peter,
Mould Graham,
Murphy Philip S.,
DzikJurasz Andrzej S. K.,
Kessar Preminda,
Haque Nazneen,
Yamaguchi Masayuki,
Atarashi Shogo,
Leach Martin O.
Publication year - 2005
Publication title -
british journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.216
H-Index - 146
eISSN - 1365-2125
pISSN - 0306-5251
DOI - 10.1111/j.1365-2125.2004.02246.x
Subject(s) - in vivo , pharmacokinetics , antimicrobial , nuclear magnetic resonance spectroscopy , chemistry , magnetic resonance imaging , nuclear medicine , pharmacology , medicine , biology , stereochemistry , microbiology and biotechnology , organic chemistry , radiology
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 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 19 F MRS is able to detect and quantify sitafloxacin in the liver. There was no evidence for the hepatic retention of the drug.