Dissolution Enhancement of Ezetimibe by Solid Dispersion

The aim of this study was to increase the aqueous solubility of Ezetimibe (EZE) by solid dispersions with polyethylene glycol 6000 (PEG 6000) and polyvinylpyrrolidone K-30 (PVP K30). Amorphous solid dispersions were prepared by freeze drying technique. The interaction of EZE with the hydrophilic polymers was evaluated by differential scanning calorimetry (DSC), powder x-ray diffractometry (PXRD) Fourier transformation-infrared spectroscopy (FTIR), Scanning electron microscopy (SEM). PXRD and DSC analysis confirmed the amorphous state of freeze dried formulations with respect to the plain drug. The influence of type of polymer, the ratio of drug to polymer on the solubility and dissolution rate of the drug were also evaluated. The solubility and dissolution rates of EZE were significantly increased by solid dispersions as well as their physical mixtures. The improvement of solubility using polymers was in the following order: PVP K30 > PEG 6000.