Abstract

An amorphous solid dispersion technique, in which hydrophobic drug molecules are dispersed in an amorphous matrix comprised solely of a sugar, was applied to curcumin that has excellent physiological functions. The sole-amorphous-sugar-based solid dispersion (SAS-SD) of curcumin was prepared by vacuum foam drying from methanol, using various disaccharides as the drug carrier-forming component. Aqueous dissolution of curcumin from the SAS-SD showed “spring-and-parachute” shape profile and was markedly increased when a sugar (α-maltose or trehalose) was added in a composition range ≥100 g-sugar/g-curcumin. Further dissolution was achieved by heating the SAS-SD at close to and above the melting points of curcumin.

摘要

将疏水性药物分子分散在仅由糖组成的无定形基质中的无定形固体分散技术应用于具有优异生理功能的姜黄素。以各种双糖为载药组分，通过真空泡沫干燥法制备姜黄素的单一无定形糖基固体分散体（SAS-SD）。来自 SAS-SD 的姜黄素的水溶出显示出“弹簧和降落伞”形状特征，并且当添加糖（α-麦芽糖或海藻糖）的成分范围≥100 g-糖/g-姜黄素时，其溶解度显着增加。通过在接近和高于姜黄素熔点的温度下加热 SAS-SD，实现进一步溶解。