Department of Industrial and Physical Pharmacy .
Pharm Dev Technol. 2014 Mar;19(2):247-56. doi: 10.3109/10837450.2013.775157. Epub 2013 Mar 12.
Amorphous and crystalline solids are commonly found together in a variety of pharmaceutical and food products. In this study, the influence of co-formulation of amorphous maltodextrins (MDs) and crystalline sucrose (S) on moisture sorption, deliquescence, and glass transition (Tg) properties of powder blends was investigated. Individual components and binary mixtures of four different molecular weight MDs with sucrose in 1:1 w/w ratios were exposed to various relative humidity (RH) environments and their equilibrium and dynamic moisture contents were monitored. The deliquescence point (RH0) and dissolution behavior of sucrose alone and in blends was also monitored by polarized light microscopy and second harmonic generation imaging. In S:MD blends, the deliquescence RH of sucrose was lower than the RH0 of sucrose alone, and synergistic moisture sorption also occurred at RHs lower than the RH0. Intimate contact of sucrose crystals with the amorphous MDs resulted in complete dissolution of sucrose at RH < RH0. When blends were stored at conditions exceeding the Tg of the individual MDs (25 °C and 60%, 49% and 34%RH for MD21, MD29 and MD40, respectively), the Tg of the blends was lower than that of individual MDs. Thus, co-formulation of amorphous MDs with crystalline sucrose sensitizes the blend to moisture, potentially leading to deleterious changes in the formulation if storage conditions are not adequately controlled.
无定形和结晶固体在各种药物和食品产品中通常同时存在。在这项研究中,研究了无定形麦芽糊精(MD)和结晶蔗糖(S)共配方对粉末混合物的水分吸附、潮解和玻璃化转变(Tg)性质的影响。将四个不同分子量的 MD 与蔗糖以 1:1 w/w 比例的单个成分和二元混合物暴露于各种相对湿度(RH)环境中,并监测其平衡和动态水分含量。通过偏光显微镜和二次谐波成像还监测了单独的蔗糖和混合物的潮解点(RH0)和溶解行为。在 S:MD 混合物中,蔗糖的潮解 RH 低于单独的蔗糖 RH0,并且在 RH0 以下的 RH 下也发生协同水分吸附。蔗糖晶体与无定形 MD 之间的紧密接触导致在 RH<RH0 时蔗糖完全溶解。当混合物在超过单个 MD 的 Tg 的条件下储存时(对于 MD21、MD29 和 MD40,分别为 25°C 和 60%、49%和 34%RH),混合物的 Tg 低于单个 MD。因此,无定形 MD 与结晶蔗糖的共配方使混合物对水分敏感,如果储存条件得不到充分控制,可能会导致配方发生有害变化。