Soluplus-Mediated Diosgenin Amorphous Solid Dispersion with High Solubility and High Stability: Development, Characterization and Oral Bioavailability.

摘要: Background and purpose The traditional Chinese medicine, diosgenin (Dio), has attracted increasing attention because it possesses various therapeutic effects, including anti-tumor, anti-infective anti-allergic properties. However, the commercial application of Dio is limited by its extremely low aqueous solubility inferior bioavailability in vivo. Soluplus, a novel excipient, great solubilization capacity crystallization inhibition. this study was to prepare Soluplus-mediated amorphous solid dispersions (ASDs) improve solubility, stability. Methods inhibition studies were firstly carried out select excipients using solvent shift method. According dissolution results, preparation methods ratios drug excipient further optimized. interaction between Soluplus characterized differential scanning calorimetry (DSC), fourier transform infrared (FT-IR) spectroscopy, electron microscopy (SEM), powder X-ray diffraction (PXRD) molecular docking. pharmacokinetic conducted explore potential ASDs for oral administration. Furthermore, long-term stability also investigated. Results preliminarily selected from optimized significantly improved due amorphization interactions as evidenced test vitro, DSC, FT-IR SEM, PXRD docking technique. rats revealed that about 5 times. In addition, stable when stored at 40°C 75% humidity 6 months. Conclusion These results indicated ASDs, with high stability, would open promising way pharmaceutical applications.