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pubmed-article:1576065pubmed:abstractText1. The concentrations of the R- and S-enantiomers of flurbiprofen and its metabolites were measured in plasma and urine following the oral administration of 50 mg racemic flurbiprofen to six normal volunteers. 2. The AUC and half-life of the R-enantiomer were significantly lower than the corresponding S-enantiomer values reflecting the greater clearance of R-flurbiprofen (20.42 +/- 4.71 vs 16.12 +/- 3.60 ml min-1). 3. Ex vivo protein binding studies indicated that the percent unbound of R-flurbiprofen was (not significantly) greater than that of the S-enantiomer (0.055 +/- 0.008 vs 0.049 +/- 0.009) and the corresponding unbound clearances did not show enantioselectivity. 4. Both enantiomers were cleared primarily by metabolism to an acylglucuronide and 4'-hydroxyflurbiprofen. There was significant enantioselectivity (R greater than S) in the formation clearances of these metabolites which remained when unbound metabolite formation clearances were considered. 5. In conclusion, the disposition of the enantiomers of flurbiprofen exhibits enantioselectivity at the level of protein binding and metabolite formation.lld:pubmed
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pubmed-article:1576065pubmed:articleTitleStereoselective disposition of flurbiprofen in normal volunteers.lld:pubmed
pubmed-article:1576065pubmed:affiliationDepartment of Medicine, Indiana University School of Medicine, Indianapolis 46202.lld:pubmed
pubmed-article:1576065pubmed:publicationTypeJournal Articlelld:pubmed
pubmed-article:1576065pubmed:publicationTypeResearch Support, U.S. Gov't, P.H.S.lld:pubmed
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