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

To measure hepatic concentrations of the fluorine-containing antimicrobial, sitafloxacin, using in vivo(19)F magnetic resonance spectroscopy (MRS). 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 1.5...

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Veröffentlicht in:British journal of clinical pharmacology 2005-02, Vol.59 (2), p.244-248
Hauptverfasser: Payne, Geoffrey S, Collins, David J, Loynds, Peter, Mould, Graham, Murphy, Philip S, Dzik-Jurasz, Andrzej S K, Kessar, Preminda, Haque, Nazneen, Yamaguchi, Masayuki, Atarashi, Shogo, Leach, Martin O
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container_title British journal of clinical pharmacology
container_volume 59
creator Payne, Geoffrey S
Collins, David J
Loynds, Peter
Mould, Graham
Murphy, Philip S
Dzik-Jurasz, Andrzej S K
Kessar, Preminda
Haque, Nazneen
Yamaguchi, Masayuki
Atarashi, Shogo
Leach, Martin O
description To measure hepatic concentrations of the fluorine-containing antimicrobial, sitafloxacin, using in vivo(19)F magnetic resonance spectroscopy (MRS). 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. 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. (19)F MRS is able to detect and quantify sitafloxacin in the liver. There was no evidence for the hepatic retention of the drug.
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subjects Adolescent
Adult
Anti-Infective Agents - pharmacokinetics
Chromatography, High Pressure Liquid
Fluorine Radioisotopes
Fluoroquinolones - pharmacokinetics
Half-Life
Humans
Liver - metabolism
Magnetic Resonance Spectroscopy - methods
Male
title Quantitative assessment of the hepatic pharmacokinetics of the antimicrobial sitafloxacin in humans using in vivoF magnetic resonance spectroscopy
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