Preparation, Characterization and Evaluation <i>In Vitro</i> of Naringenin-PVP K-30 Solid Dispersions

Abstract

Solid dispersions (SD) were prepared with naringenin and polyvinyl pyrrolidone k-30 (PVP k-30) by the solvent evaporation method with three drying methods (microwave-vacuum drying, MVD; and spray drying, SPD; vacuum drying, VD). The physical state was characterized by DSC, PXRD, SEM, and FT-IR. The results showed that the vitro dissolution rate and extent of naringenin was improved significantly by SD as compared with the pure drug and physical mixtures (PM). The results of FT-IR showed that naringenin is possibly interacted with PVP k-30 via intermolecular hydrogen bond, the results of DSC and PXRD showed that all of the SD prepared with three drying methods was completely amorphous. Compared with other drying methods, the MVD method can save time and energy. The physical state of SD prepared with the three drying methods that stored in the 40 °C/75% RH chamber was stable in three month. These results suggest that MVD is feasible to replace the traditional time-consuming and low efficiency drying procedure for preparation of SD.

Mid-infrared spectroscopy as a polymer selection tool for formulating amorphous solid dispersions

“…[9] Naringenin has a reported aqueous solubility of 45 mg/ml (37°C, pH 3) [10] and quercetin has an aqueous solubility of 0.4 mg/ml (room temperature, pH 3). [11] For the purpose of improving the solubility of these flavonoids, a variety of techniques has been used, including particle size reduction, [12][13][14] solid dispersions [14][15][16][17][18][19] and the formation of inclusion complexes. [10,14,[20][21][22] Among these methods, formulating as an amorphous solid dispersion is very attractive for the flavonoid compounds.…”