Abstract:
OBJECTIVE To improve in vitro dissolution of the poorly water soluble drug quercetin with preparation of its solid dispersion.
METHODS Using Eudragit EPO, PVP-K30 or PVP-VA(6∶4) as hydrophilic carrier, the technology of hot melt extrusion (HME) was employed to prepare solid dispersion of quercetin. Fourier transform infrared spectroscopy(FTIR), X-Ray diffraction(XRD) and differential scanning calorimetry(DSC) were employed to characterize the extrusions.
RESULTS In vitro dissolution of quercetin from all solid dispersions with EPO or PVPK30 as carrier was significantly improved than that of pure drug. In simulated gastric fluid, the accumulative dissolution of formulation quercetin-EPO (1∶9) reached 67% in 3 min, for formulation of quercetin-xylitol-PVPK30 (1∶3∶6), it reached 65% in 3min, while for pure drug, dissolution was less than 10% in 60min. The results of DSC and XRD showed quercetin was amorphously dispersed in carriers.
CONCLUSION Hot melt extrusion can be used to prepare quercetin solid dispersion, from which drug dissolution was significantly improved.