Pharmacokinetics of phenylbutazone given intravenously or orally in mature Holstein bulls

Abstract

SUMMARY Six mature Holstein bulls were each given 10 mg of phenylbutazone (pbz)/kg of body weight, po. Of the 6 bulls, 3 were given 10 mg of pbz/kg by rapid iv administration 4 weeks later. Plasma concentration-vs-time data were analyzed, using nonlinear regression modeling (sum of exponential functions). The harmonic mean of the biologic half-life of pbz was 62.6 ± 12.9 hours after oral administration and 61.6 ± 7.2 hours after iv administration. The mean residence time was 94.61 ± 8.44 hours and 90.49 ± 8.93 hours for oral and iv administration, respectively. The mean total body clearance was 0.0015 ± 0.0003 L/h/kg, with the mean apparent volume of distribution 0.134 ± 0.021 L/kg. Mean bioavailability was 73 ± 2% after oral administration. Phenylbutazone was adequately absorbed from the gastrointestinal tract in bulls. The apparent volume of distribution was small, indicating that pbz distributed mainly into plasma and extracellular fluid. The total body clearance was also small, which accounted for the long half-life of pbz in bulls.