Two different formulations of phenylbutazone, one made to contain 0.5% w/v Brij 96 and the other without surfactant, were prepared by conventional crystallization and compressed to tablets by direct compression using a single punch tabletting machine fitted with 3 mm punches. The relative bioavailability of phenylbutazone was determined in Newzealand rabbits. The results were compared with the in-vitro intrinsic dissolution rate values. Phenylbutazone serum levels were determined by a high pressure liquid chromatographic method developed in our laboratory. Samples containing 0.5% w/v Brij 96 showed a 2-fold increase in dissolution rate, as well as an enhancement in the bioavailability of phenylbutazone. The maximum blood concentration (Cmax) exhibited a 2-fold increase with a significant reduction in the time required for the maximum blood concentration (Tmax), and a 3-fold increase in the area under the curve (AUC) for samples containing the surfactant was observed.
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