title: HPLC analysis for amobarbital N-glycosides in urine.
abstract: A study was undertaken to determine if humans excrete both amobarbital N-glucuronides and N-glucosides in urine after an oral dose of amobarbital. Amobarbital N-glucuronides were synthesized and characterized. A reverse phase LC method using post-column pH adjustment and UV detection at 240 nm was developed and used for the quantification of the amobarbital N-glucosides and N-glucuronides in human urine. Amobarbital was administered orally to seven male subjects and the total urine was collected for a period of 48-53 h after dosing. After filtration, the urine was injected directly onto the HPLC column to analyze for the presence of metabolites. The previously identified (5S)-amobarbital N-glucoside was detected in all seven subjects. The (5R)-amobarbital N-glucoside was detected at lower concentrations in only four of the subjects. At the levels at which amobarbital N-glucosides were detected, there was no evidence for the formation and excretion of the amobarbital N-glucuronides. Amobarbital N-glucuronidation is not a quantitatively significant pathway for the biodisposition of amobarbital in humans.
authors.affiliation: Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond 23298-0540, USA.
authors.forename: V
authors.initials: V
authors.lastname: Nandi
authors.forename: W H
authors.initials: WH
authors.lastname: Soine
mesh_terms: D000328:Adult; D000654:Amobarbital / Q000031:analogs & derivatives* / Q000493:pharmacokinetics* / Q000652:urine; D002851:Chromatography, High Pressure Liquid; D005965:Glucuronates / Q000652:urine*; D006801:Humans; D008297:Male; D008875:Middle Aged; D013056:Spectrophotometry, Ultraviolet
chemical_list: C107330:5-ethyl-1-(glucopyranosyluronate)-5-(3'-methylbutyl)-2,4,6-(1H,3H,5H)-pyrimidinetrione; C107325:5-ethyl-5-(3'-methylbutyl)-1-(methylglucopyranosyluronate)-2,4,6-(1H,3H,5H)-pyrimidinetrione; D005965:Glucuronates; D000654:Amobarbital