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Enantioselective pharmacokinetics of ketoprofen in calves after intramuscular administration of a racemic mixture

Elke Plessers (UGent) , Anneleen Watteyn (UGent) , Heidi Wyns (UGent) , Bart Pardon (UGent) , Siegrid De Baere (UGent) , Patrick De Backer (UGent) and Siska Croubels (UGent)
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Abstract
The pharmacokinetic properties of ketoprofen were determined in 4-week-old calves after intramuscular (IM) 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 (AUC0→∞) (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 (Vd/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 IM administration.
Keywords
Ketoprofen, Pharmacokinetics, Enantiomers, Calves, Intramuscular, NONSTEROIDAL ANTIINFLAMMATORY DRUGS, DIFFERING PHYSIOLOGICAL STATUS, CHIRAL PHARMACOKINETICS, DAIRY-CATTLE, PHARMACODYNAMICS, ENANTIOMERS, INVERSION, (R)-KETOPROFEN, DISPOSITION, ABSORPTION

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Chicago
Plessers, Elke, Anneleen Watteyn, Heidi Wyns, Bart Pardon, Siegrid De Baere, Patrick De Backer, and Siska Croubels. 2015. “Enantioselective Pharmacokinetics of Ketoprofen in Calves After Intramuscular Administration of a Racemic Mixture.” Journal of Veterinary Pharmacology and Therapeutics 38 (4): 410–413.
APA
Plessers, E., Watteyn, A., Wyns, H., Pardon, B., De Baere, S., De Backer, P., & Croubels, S. (2015). Enantioselective pharmacokinetics of ketoprofen in calves after intramuscular administration of a racemic mixture. JOURNAL OF VETERINARY PHARMACOLOGY AND THERAPEUTICS, 38(4), 410–413.
Vancouver
1.
Plessers E, Watteyn A, Wyns H, Pardon B, De Baere S, De Backer P, et al. Enantioselective pharmacokinetics of ketoprofen in calves after intramuscular administration of a racemic mixture. JOURNAL OF VETERINARY PHARMACOLOGY AND THERAPEUTICS. 2015;38(4):410–3.
MLA
Plessers, Elke, Anneleen Watteyn, Heidi Wyns, et al. “Enantioselective Pharmacokinetics of Ketoprofen in Calves After Intramuscular Administration of a Racemic Mixture.” JOURNAL OF VETERINARY PHARMACOLOGY AND THERAPEUTICS 38.4 (2015): 410–413. Print.
@article{5762970,
  abstract     = {The pharmacokinetic properties of ketoprofen were determined in 4-week-old calves after intramuscular (IM) 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(\unmatched{2012}) 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(\unmatched{2012}) and S(+) ketoprofen. More in specific, a greater value for the mean area under the plasma concentration-time curve (AUC0{\textrightarrow}\ensuremath{\infty}) (46.92 {\textpm} 7.75 and 11.13 {\textpm} 2.18 {\textmu}g.h/mL for the S(+) and R(\unmatched{2012}) enantiomer, respectively), a lower apparent clearance (Cl/F) (32.8 {\textpm} 5.7 and 139.0 {\textpm} 25.1 mL/h.kg for the S(+) and R(\unmatched{2012}) enantiomer, respectively) and a lower apparent volume of distribution (Vd/F) (139 {\textpm} 14.7 and 496 {\textpm} 139.4 mL/kg for the S(+) and R(\unmatched{2012}) enantiomer, respectively) were calculated for the S(+) enantiomer, indicating enantioselective pharmacokinetics for ketoprofen in calves following IM administration.},
  author       = {Plessers, Elke and Watteyn, Anneleen and Wyns, Heidi and Pardon, Bart and De Baere, Siegrid and De Backer, Patrick and Croubels, Siska},
  issn         = {0140-7783},
  journal      = {JOURNAL OF VETERINARY PHARMACOLOGY AND THERAPEUTICS},
  keyword      = {Ketoprofen,Pharmacokinetics,Enantiomers,Calves,Intramuscular,NONSTEROIDAL ANTIINFLAMMATORY DRUGS,DIFFERING PHYSIOLOGICAL STATUS,CHIRAL PHARMACOKINETICS,DAIRY-CATTLE,PHARMACODYNAMICS,ENANTIOMERS,INVERSION,(R)-KETOPROFEN,DISPOSITION,ABSORPTION},
  language     = {eng},
  number       = {4},
  pages        = {410--413},
  title        = {Enantioselective pharmacokinetics of ketoprofen in calves after intramuscular administration of a racemic mixture},
  url          = {http://dx.doi.org/10.1111/jvp.12186},
  volume       = {38},
  year         = {2015},
}

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