PMID: 9531520May 16, 1998Paper

Stereoselective metabolism of benoxaprofen in rats. Biliary excretion of benoxaprofen taurine conjugate and glucuronide

Drug Metabolism and Disposition : the Biological Fate of Chemicals
Kiminori MohriLeslie Z Benet

Abstract

Benoxaprofen (BOP) was administered iv to bile duct-cannulated rats at a dose of 10 mg/kg. BOP and its metabolites in plasma, urine, and bile were quantified using HPLC. A previously unidentified BOP metabolite was found in HPLC chromatograms of rat bile, and the metabolite was isolated chromatographically. Positive-ion fast-atom bombardment (FAB) MS analysis of the compound showed [M+H]+ at m/z 409, i.e. 108 mass units greater than the molecular weight of BOP (301 mass units). In the 1H NMR spectrum of the compound, two signals assigned to two methylene groups appeared at 2.53 ppm and 3. 30 ppm, in addition to BOP signals. Analysis of FAB mass spectra and 1H-1H and 1H-13C correlated NMR spectra of the isolated metabolite suggested that the new metabolite was a BOP taurine conjugate (BOP-T). A BOP-T standard was chemically synthesized, and physicochemical data were compared with those for the isolated metabolite. Identical results, i.e. RF values from TLC, RT values from HPLC, and FAB MS and 1H-13C correlated NMR findings, were obtained, establishing that the new metabolite found in rat bile was BOP-T. In five rats, mean values for per cent excretion of the dose in bile over 12 hr for BOP glucuronide (BOP-G), BOP-T, and unchang...Continue Reading

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