초록 |
Ginsenoside Rg3 is an active pharmaceutical ingredient that exists only in plants of the genus Ginseng. In general, the amorphization has been recently considered as one of the feasible strategy for the solubility/dissolution enhancement, since the amorphous form of drug substances are well known to have higher solubility characteristics than crystalline forms of the same materials. However, since the unstable amorphous active ingredient undergoes transition to a stable crystalline form, a manufacturing method capable of stabilizing the amorphous form is desired. In this study, the grinding and ball milling methods were employed to manufacture the co-amorphous solid forms between Rg3 and various additives. Among them, effective as co-amorphization agent were the saccharin and caffeine. Resulting amorphous materials were pretreated suitably and characterized via the PXRD and thermal analysis including DSC. It was found that the mass ratio between the drug substance and co-amophization agent plays an important role in determining the pathway of co-amorphous solid formation. As compared to the pure Rg3 powder, the co-amorphous solid powders showed substantially improved solubility. |