The aim of this investigation was to improve the dissolution properties of the water-insoluble drug ezetimibe (EZE) and potentially improve bioavailability.A combination of melt and adsorption techniques was employed for the preparation of solid dispersions.PEG 4000, PEG 6000, and Gelucire 44/14 were used as hydrophilic carriers, and lactose monohydrate was used as an adsorbent.Phase solubility curves are of A L type, indicating a linear relationship between drug solubility and carrier concentration.Dissolution studies reveal an improvement of in vitro drug release.Mathematical modeling indicates that drug release data are best described by the Korsmeyer-Peppas model, with Fickian diffusion as the possible drug-release mechanism.Physicochemical characterization of solid dispersions by Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and powder X-ray diffraction (PXRD) suggests a reduction in drug crystallinity following dissolution enhancement.Hence, the present investigation reveals that the dissolution characteristics of EZE could be ameliorated in a solid dispersion.
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Parmar et al. (2011) studied this question.
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