In-vitro and in-vivo correlation of enhancement of dissolution rate of water insoluble drugs
Al-Meshal, M.A.
Research Communications in Chemical Pathology and Pharmacology 67(3): 415-418
1990
ISSN/ISBN: 0034-5164 PMID: 2343187 Document Number: 364381
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.