title: The disposition of ketoprofen enantiomers in man.
abstract: 1. The disposition of ketoprofen enantiomers was studied in 21 patients taking racemic ketoprofen (Orudis SR). 2. In each patient the plasma concentrations of the R- and S-enantiomers were similar at all times over a 24 h dosing interval. The mean (+/- s.e. mean) time-averaged plasma ketoprofen concentrations over the dosage interval were 0.76 (+/- 0.06) mg l-1 for R-ketoprofen and 0.78 (+/- 0.06) mg l-1 for S-ketoprofen. 3. Creatinine clearances for the 21 patients ranged from 6-162 ml min-1. There was no correlation between creatinine clearance and time-averaged plasma concentration for either R- or S-ketoprofen. 4. Approximately 30% of the dose was recovered in urine (unconjugated + glucuronide conjugate) and this was made up of 43% R-ketoprofen and 57% S-ketoprofen. Because of incomplete urine recoveries of ketoprofen it was not possible to determine whether inversion from the R- to the S-enantiomer takes place in man. 5. The data suggest that in terms of total (bound + unbound) ketoprofen, half the concentration value derived by a non-enantiospecific analysis would give a reasonable approximation of the pharmacologically active S-enantiomer concentration in plasma.
authors.affiliation: Department of Clinical Pharmacology, Flinders University of South Australia, Adelaide.
authors.forename: B C
authors.initials: BC
authors.lastname: Sallustio
authors.forename: Y J
authors.initials: YJ
authors.lastname: Purdie
authors.forename: A G
authors.initials: AG
authors.lastname: Whitehead
authors.forename: M J
authors.initials: MJ
authors.lastname: Ahern
authors.forename: P J
authors.initials: PJ
authors.lastname: Meffin
mesh_terms: D000368:Aged; D002851:Chromatography, High Pressure Liquid; D003404:Creatinine / Q000097:blood; D005260:Female; D006801:Humans; D007660:Ketoprofen / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine; D008297:Male; D010666:Phenylpropionates / Q000493:pharmacokinetics*; D013237:Stereoisomerism
chemical_list: D010666:Phenylpropionates; D007660:Ketoprofen; D003404:Creatinine