Improvement in the elution behavior of rutin via binary amorphous solid with flavonoid using a mechanochemical process

Abstract The solubility of rutin (Rut), which is low in water, was improved by binary amorphous solid with other excipients using a mechanochemical technique. Four potential excipients; l -methionine, naringin hydrate, quercetin dihydrate, and hesperidin (Hes) were used for attempting to preparation of the co-amorphization with Rut. After grinding, the samples were characterized using powder X-ray diffraction, differential scanning calorimetry, electron spin resonance, and ultraviolet-visible spectroscopy. It was found that Hes could suppress the recrystallization of Rut after the mechanochemical process, in contrast to the other excipients. The recrystallization temperature of Hes increased after grinding with Rut, which indicated the possibility of a co-amorphization between Rut and Hes. The produced particles from this process expressed radicals with changes in crystal structure, resulting in a link between structural changes and radical expression. The radical formation may improve the dissolution rate of Rut due to the co-amorphization of Rut and Hes. The radical species identified from the co-amorphization of Rut and Hes would be attributed to the sugar moiety of Hes having coordinated with Rut.