In-vitro and in-vivo correlation of enhancement of dissolution rate of water insoluble drugs.
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.
al-Meshal
M A
MA
Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.
D000818:Animals; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid; D010653:Phenylbutazone / Q000097:blood / Q000493:pharmacokinetics*; D010938:Plant Oils; D011092:Polyethylene Glycols; D011817:Rabbits; D012995:Solubility; D013607:Tablets; D014867:Water; D014961:X-Ray Diffraction
D010938:Plant Oils; D013607:Tablets; D014867:Water; D011092:Polyethylene Glycols; C033084:polyethylene glycol oleyl ether; D010653:Phenylbutazone