Solubility and Dissolution Enhancement Bosentan by Third Generation Solid Dispersion

Abstract

The objectives of present investigation was to enhance the solubility and dissolution rate of poorly water soluble drug bosentanby third generation solid dispersion using Gelucire 50/13 as a carrier. Solid dispersion of bosentan with hydrophilic carrier were prepared in various drug to carrier ratios(1:1, 1:2, 1:3, 1:4 and 1:5) by kneading technique. Prepared dispersions was evaluated forsaturation solubility, percentage yield, drug content and in vitro dissolution.Infrared (FTIR) spectroscopy studyshowed no interaction between drug and carrier. Differential scanning calorimetry (DSC)and X-ray diffraction (XRD)study confirmed the conversion of crystalline drug in to amorphous form. All solid dispersions prepared with hydrophilic carrier showed increase in drug solubility and dissolution rate as compare to pure drug. It was confirmed that the Gelucire 50/13based third generation solid dispersion is aneffective approach to enhance the solubility and dissolution rate of bosentan.