Journal of Drug Metabolism & Toxicology
Open Access
ISSN: 2157-7609
+44-20-4587-4809
ISSN: 2157-7609
+44-20-4587-4809
Rainsford KD
Biomedical Research Centre,
Howard Street, Sheffield, S1 1WB
United Kingdom
Research Article
The Biotransformation and Pharmacokinetics of 14C-Nimesulide in Humans Following a Single Dose Oral Administration
Author(s): David Macpherson, Stuart A Best, Layla Gedik, Alan T Hewson, Rainsford KD and Simona ParisiDavid Macpherson, Stuart A Best, Layla Gedik, Alan T Hewson, Rainsford KD and Simona Parisi
Nimesulide is a preferential cyclo-oxygenase-2 inhibitory non-steroidal anti-inflammatory drug has, infrequently, been associated with hepatic reactions. To establish the extent of formation of various metabolites (some of which might be hepato-reactive) the whole body metabolism, plasma kinetics and routes of excretion of the radio-labelled drug was undertaken in 4 fasted male volunteers following an oral dose of 100 mg [14C]-nimesulide. Urine, faecal and plasma samples were collected up to 168 h post dose, the total radioactivity and plasma concentrations of nimesulide and its principle metabolite, 4-hydroxynimesulide, were determined. Radio labelled metabolites in these samples was identified by combined liquid chromatography-mass spectrometry. The mean elimination half-life of total radioactivity in the plasma and whole blood was circa 4.8 h; the ratio whole blood and plasma being ci.. View More»
DOI:
10.4172/2157-7609.1000140