Affiliations 

  • 1 Asian Institute of Medical Science and Technology (AIMST) University
  • 2 Birla Institute of Technology
  • 3 Kovai Medical Center and Hospital (KMCH) College of Pharmacy
MyJurnal

Abstract

exhibits extensive first pass metabolism with poor oral bioavailability (27%–50%) limiting its therapeutic efficiency. The present study involved an attempt to enhance its aqueous solubility by formulating as solid dispersions (SDs) using sodium starch glycollate (SSG) as a carrier. The dispersions were formulated by dispersion method and evaluated by phase solubility, drug content, in vitro release and mathematical modelling. Solid state characterisation of samples was carried out by X-ray diffraction (XRD), differential scanning calorimetric (DSC), Fourier transform infrared spectrophotometry (FTIR), near infrared (NIR), Raman analysis and wettability studies. The phase solubility and thermodynamic parameters indicated the spontaneity and solubilisation effect of carrier. The release rate from the dispersions was higher than pure drug and found to increase with an increase in carrier content. The optimised dispersions were selected based on release studies, profiles and dissolution parameters. XRD, DSC, FTIR, NIR and Raman analysis proved the crystallinity reduction, changes in crystal quality and compatibility between drug and carriers. Wettability studies proved the increased wettability in selected dispersions. Based on the findings, possible mechanisms that would have contributed to dissolution enhancement of CLZ were suggested. Such findings could be extrapolated to enhance the aqueous solubility of other poorly water-soluble drugs.