Identification of a benzhydrolic metabolite of ketoprofen in horses by gas chromatography—mass spectrometry and high-performance liquid chromatography

Enantioselective pharmacokinetics of ketoprofen in piglets: the significance of neonatal age

“…, 2004), while the relevance of other biotransformations such as hydroxylation of the aromatic ring of the benzoic group, reduction of the ketone group and chiral inversion varies between species (Populaire et al. , 1973; Benoit et al. , 1992; Alkatheeri et al.…”

“…In general, differences in clearance between enantiomers may be a consequence of enantioselectivity in metabolism, including chiral inversion of R-ketoprofen to S-ketoprofen, in excretion, protein or tissue binding or to a combination of these factors. In most species, conjugation to an acylglucuronide is a major metabolic transformation of ketoprofen (Populaire et al, 1973;Skordi et al, 2004), while the relevance of other biotransformations such as hydroxylation of the aromatic ring of the benzoic group, reduction of the ketone group and chiral inversion varies between species (Populaire et al, 1973;Benoit et al, 1992;Alkatheeri et al, 1999). The extent of chiral inversion in piglets could not be determined in this study because only racemic ketoprofen was administered, and R-ketoprofen was not commercially available.…”

Pharmacokinetic parameters and milk concentrations of ketoprofen after administration as a single intravenous bolus dose to lactating goats

“…The finding of a 2‐compartment model for ketoprofen was similar to reports in cattle (DeGraves et al ., 1996), horses (Benoit et al ., 1992; Owens et al ., 1995), and humans (Debruyne et al ., 1987). The initial distribution phase was very rapid, t ½α = 0.08 ± 0.05 h; the early rapid decline of the serum concentration‐time curve is primarily caused by distribution of the drug from the central, highly perfused compartment to tissues.…”

Pharmacokinetics of ketoprofen after multiple intravenous doses to mares

“…Recently. Benoit et al (1992) identified a 'benzhydrolic' metabolite of ketoprofen ( Fig. l), result-ing lnnn reduction of the keto group, in horse plasma and urine.…”