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Enantioselective pharmacokinetics of ketoprofen in calves after intramuscular administration of a racemic mixture
Author(s) -
Plessers E.,
Watteyn A.,
Wyns H.,
Pardon B.,
De Baere S.,
De Backer P.,
Croubels S.
Publication year - 2015
Publication title -
journal of veterinary pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.527
H-Index - 60
eISSN - 1365-2885
pISSN - 0140-7783
DOI - 10.1111/jvp.12186
Subject(s) - enantiomer , pharmacokinetics , ketoprofen , chemistry , volume of distribution , enantioselective synthesis , racemic mixture , pharmacology , chromatography , high performance liquid chromatography , stereochemistry , medicine , biochemistry , catalysis
The pharmacokinetic properties of ketoprofen were determined in 4‐week‐old calves after intramuscular (i.m.) injection of a racemic mixture at a dose of 3 mg/kg body weight. Due to possible enantioselective disposition kinetics and chiral inversion, the plasma concentrations of the R(−) and S(+) enantiomer were quantified separately, using a stereospecific HPLC ‐ UV assay. A distinct predominance of the S(+) enantiomer was observed, as well as significantly different pharmacokinetic parameters between R(−) and S(+) ketoprofen. More in specific, a greater value for the mean area under the plasma concentration–time curve ( AUC 0→∞ ) (46.92 ± 7.75 and 11.13 ± 2.18 μg·h/mL for the S(+) and R(−) enantiomer, respectively), a lower apparent clearance (Cl/F) (32.8 ± 5.7 and 139.0 ± 25.1 mL/h·kg for the S(+) and R(−) enantiomer, respectively) and a lower apparent volume of distribution (V d /F) (139 ± 14.7 and 496 ± 139.4 mL/kg for the S(+) and R(−) enantiomer, respectively) were calculated for the S(+) enantiomer, indicating enantioselective pharmacokinetics for ketoprofen in calves following i.m. administration.