Solubility and Dissolution Enhancement of Sulfasalazine by Solid Dispersion Technique

Abstract

The solubility behavior of drug remains one of the most challenging aspects in formulation development. Most NCE are poorly water soluble, drug not well absorbed after oral administration. Solid dispersion is an increasingly important approach to enhance dissolution rate and solubility of poorly water soluble drug. Sulfasalazine is derivative of mesalazine. Sulfasalazine and its metabolite 5-aminosalicylic acid (5-ASA) are poorly absorbed from gut so its main mode of action is believed to be inside the intestine. It exhibits slow GI absorption rate and inter individual variation of its bioavailability. Thus solubility enhancement and dissolution enhancement of sulfasalazine from its dosage form is an important issue for its in vivo bioavailability and therapeutic efficacy. It was planned to improve the solubility of sulfasalazine by using polymer like Gelucire50/13. Different ratio were employed as 1: 1, 1: 3, 1: 5 and Solid dispersion were prepared by Solvent evaporation method, Physical mixture and Kneading method. Preformulation study was done before going to formulation in that melting point, solubility and compatibility study was done. The prepared solid dispersion also evaluated for percentage yield, percent drug content. Solubility study was done in water. Solid dispersion also characterized by FTIR, DSC, PXRD. In-vitro dissolution study was done in pH6.8 phosphate buffer using USP dissolution test apparatus type II.