title: Identification of mebeverine acid as the main circulating metabolite of mebeverine in man.
abstract: The intestinal spasmolytic drug mebeverine is known to undergo fast in vivo enzymatic hydrolysis into mebeverine alcohol and veratric acid. A reversed-phase HPLC method with coulometric detection was developed in order to assay the hitherto unidentified secondary metabolite mebeverine acid. After intake of a single oral dose of 405 mg mebeverine hydrochloride in four healthy human volunteers, peak plasma concentrations of mebeverine acid were found to be 1000-fold higher than those of mebeverine alcohol, i.e. approximately 3 microg/ml versus 3 ng/ml. The appearance of mebeverine acid in plasma (median T(max)=1.25 h) as well as its disappearance (median apparent t(1/2)=1.1 h) were rapid. The urinary excretion of mebeverine acid within the first 4 h after dosing amounted to 67% of the mebeverine dose (median range: 23-107%). Mebeverine acid appears to be a valuable marker of oral exposure to mebeverine.
authors.affiliation: SGS Biopharma S.A., 1301 Bierges, Belgium. arnel.stockis@ucb-group.com
authors.forename: Arnel
authors.initials: A
authors.lastname: Stockis
authors.forename: P J M
authors.initials: PJ
authors.lastname: Guelen
authors.forename: D
authors.initials: D
authors.lastname: de Vos
mesh_terms: D000284:Administration, Oral; D000328:Adult; D000927:Anticonvulsants / Q000008:administration & dosage / Q000378:metabolism* / Q000493:pharmacokinetics; D019540:Area Under Curve; D002851:Chromatography, High Pressure Liquid; D006207:Half-Life; D006801:Humans; D008297:Male; D010627:Phenethylamines / Q000008:administration & dosage / Q000097:blood* / Q000378:metabolism* / Q000493:pharmacokinetics / Q000652:urine
chemical_list: D000927:Anticonvulsants; D010627:Phenethylamines; C076513:mebeverine alcohol; C005096:mebeverine