Study on preparation of quercetin solid dispersions and its bioavailability in rats / 中草药

ABSTRACT

Objective Quercetin solid dispersions (QSD) with hydrophilic carriers were prepared in order to enhance its dissolution rate and oral bioavailability in rats. Methods QSD with different ratios of polyvinylpyrrolidone (PVPK30), PEG6000, and xylitol were prepared by solvent method or melting-solvent method. Dissolution characteristics of QSD were evaluated and compared with that of the pure drug. Differential scanning calorimetry (DSC) and X-ray powder diffraction (XRPD) were used to examine the crystallinity of solid dispersion, physical mixture, carriers and quercetin. Drug plasma concentrations were determined by high performance liquid chromatography mass spectrum (HPLC-MS) after oral administration in rats. Results The dissolution rate of quercetin from its solid dispersions was greatly enhanced. Dissolution percentages from the solid dispersion of quercentin-PVPK30-xylitol in 151 weight ratio were 40.63% and 68.58% at 5 min and 60 min respectively, while in the same time only 0.26% and 1.66% from pure quercetin. The results of DSC and XRPD demonstrated that quercetin was amorphously dispersed in solid dispersion. Oral bioavailability in rats of QSD was about 61-fold higher than that of pure drug. Conclusion QSD significantly improved quercetin dissolution rate and bioavailability in rat.