Disposition of human drug preparations in the horse. IV. Orally administered fenoprofen.
Plasma and urinary concentrations of the non-steroidal anti-inflammatory drug fenoprofen were determined by a high-performance liquid chromatographic procedure following oral administration of a dose of 3 g to fed and fasted horses. In plasma, fenoprofen was present in detectable concentrations for 6-12 h. Free access to hay significantly reduced the peak plasma concentration and bioavailability of fenoprofen, and large interindividual differences in absorption and elimination pattern occurred. In fasted horses, fenoprofen was rapidly absorbed with a mean half-life of 0.10 h. Maximum concentrations were found 0.63 +/- 0.21 h after dosing. The elimination half-life was 0.9 h. As early as 1 h after dosage, fenoprofen could be detected in hydrolysed and unhydrolysed urine, and remained detectable up to 48 h. The maximum excretion rate and peak concentration occurred 2 h after administration, irrespective of the feeding schedule. In fed horses, a second maximum occurred after 9 h. The percentage of the dose excreted as unchanged fenoprofen in 12 h was 13.0 +/- 6.8%. A recovery of 21.9 +/- 7.4% and 42.2 +/- 7.0% of the dose was obtained after enzymatic and alkaline hydrolysis, respectively. At least three hydroxylated metabolites were detected in hydrolysed urine.
Delbeke
F T
FT
Farmacie & Toxicologie, Falculteit Diergeneeskunde, Universiteit Gent, Merelbeke, Belgium.
Landuyt
J
J
Debackere
M
M
D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D001711:Biotransformation; D001798:Blood Proteins / Q000378:metabolism; D002851:Chromatography, High Pressure Liquid; D004300:Doping in Sports; D005215:Fasting / Q000378:metabolism; D005260:Female; D005279:Fenoprofen / Q000493:pharmacokinetics*; D018565:Food-Drug Interactions; D008401:Gas Chromatography-Mass Spectrometry; D006736:Horses / Q000378:metabolism*; D006863:Hydrogen-Ion Concentration; D006868:Hydrolysis; D007202:Indicators and Reagents; D011485:Protein Binding; D013696:Temperature; D013997:Time Factors
D001798:Blood Proteins; D007202:Indicators and Reagents; D005279:Fenoprofen