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Abstract

Formulation and In Vitro Evaluation of solid dispersions of BCS Class II Drug Febuxostat by employing L-HPC

P.Tripura Sundari* and Krutika Lad

Febuxostat (FBX) is a non purine selective inhibitor of xanthine oxidase/xanthine reductase. Because of low solubility the bioavailability of the drug is hampered, food also interferes with the absorption of drug and decreases the Cmax by 38-49%. In the category of poorly soluble drugs the change in surface area of the drug will show considerable changes in the solubility and dissolution of the drug. In the present study, the attempts were made to improve the bioavailability of FBX by solid dispersions technique by employing L-HPC as carrier molecules. Different ratios on weight basis were prepared viz 1:1, 1:2, 1:3, 2:1. These preparations were characterized in liquid state by phase solubility studies and in solid state by Differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), Powdered X ray diffraction studies (PXRD) and Scanning electron microscopy (SEM). The aqueous solubility of FBX is favored by the presence of carrier polymer. Solid state characterization indicated that FBX was present as fine amorphous form in the carrier polymeric molecules. In contrast to the solution rate of pure FBX the dissolution of drug in carrier considerably improved the dissolution rate, this can be attributed to the increased wettability and dispersibility as well as decreased crystallinity and increased amorphous fraction of drug.


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