Monophase Solution for Enhancing Solubility and Dissolution of Ezetimibe by Spray Dried Microparticle

Abstract

The aim of the present study was to improve the solubility and dissolution rate of Ezetimibe by preparing crystals by spray drying technique using Isopropyl alcohol (IPA) and water as solvent system. Ezetimibe crystals were produced by spray drying using IPA as solvent to enhance solubility and dissolution rate. The prepared crystals were evaluated for solubility and in vitro dissolution. The prepared formulations were characterized by differential scanning calorimetry (DSC), Fourier transform infrared (FT-IR) spectroscopy, X-ray diffraction (XRD) and scanning electron microscopy (SEM). Dissolution profile of the prepared spray dried crystals was compared with its recrystallized and pure sample. Spray dried crystals exhibited decreased crystallinity. The solubility of spray dried crystals exhibited two-fold increase as compared to the commercial Ezetimibe and dissolution showed 59% release in 60 min. Consequently, from the above result it can be concluded that spray dried technique is a useful technique to improve the solubility and dissolution of poor water soluble drug like Fenofibrate.

Keywords: spray drying, crystals, Ezetimibe, crystallinity, solubility