In vitro dissolution and physicochemical characterizations of novel PVP-based solid dispersions containing valsartan prepared by a freeze-drying method

Abstract

Valsartan (VAL) shows poor oral bioavailability mainly as a result of its low water solubility at low pH. This study is designed to investigate the dissolution properties and physicochemical characteristics of novel PVP-based solid dispersions (SDs) containing VAL. The SDs were prepared with polyvinylpyrrolidone (PVP-K30) as a hydrophilic polymer, sodium hydroxide (NaOH) as an alkalizer, and poloxamer 188 (F68) as a surfactant, without using any organic solvents by a freeze-drying method. The dissolution study was carried out and the physicochemical properties of SDs were also characterized by using differential scanning calorimetry (DSC), fourier transform-infrared (FT-IR) spectroscopy, X-ray diffractometry (XRD) and scanning electron microscopy (SEM). The dissolution rates of SDs were significantly improved at pH1.2 and pH6.8 compared to that of pure drug. The results of physicochemical properties suggested that some interactions between VAL and carriers had occurred in the molecular level and the drug presented in the SDs was amorphous. It was concluded that the novel PVP-based SDs has been successfully prepared by a freeze-drying method, resulting in significant dissolution improvement of VAL.