Preparation and Characterization of Taxifolin Form II by Antisolvent Recrystallization.

To improve the aqueous solubility and dissolution rate of taxifolin, taxifolin form II was successfully prepared through antisolvent recrystallization, in which 1‐butyl‐3‐methylimidazolium tetrafluoroborate and dichloromethane were used as solvent and antisolvent, respectively. The properties of taxifolin form II were characterized by scanning electron microscopy, Fourier transform infrared spectroscopy, X‐ray diffraction, differential scanning calorimetry, solid‐state NMR spectroscopy, the dissolving capability test, and the bioavailability test. The chemical structure of taxifolin form II was not changed, but its morphology and crystalline structure changed during the recrystallization process. Moreover, taxifolin form II showed higher solubility, faster dissolution rate, and better bioavailability than taxifolin form I. Different crystal forms of drugs can have different physicochemical properties. Taxifolin form II, prepared through the antisolvent recrystallization method by using 1‐butyl‐3‐methylimidazolium tetrafluoroborate as a solvent and dichloromethane as an antisolvent, has enhanced solubility and dissolution rate for potential application in high bioavailability oral taxifolin formulations. [ABSTRACT FROM AUTHOR]