Sugars as bulking agents to prevent nano-crystal aggregation during spray or freeze-drying
Sugars as bulking agents to prevent nano-crystal aggregation during spray or freeze-drying
复制标题
DOI：
10.1016/j.ijpharm.2014.05.060
复制
发表时间：
2014-08-25
影响因子：
5.8
通讯作者：
Burgess, Diane J.
中科院分区：
文献类型：
--
作者：
Kumar, Sumit;Gokhale, Rajeev;Burgess, Diane J.
本研究评估了低分子量和高分子量糖对喷雾或冷冻干燥制备的吲哚美辛纳米晶体悬浮粉末的影响。 Dowfax 2A1（带负电荷的表面活性剂）用作吲哚美辛纳米混悬剂稳定剂。对含有或不含糖的干燥结晶粉末的结晶度、粒度和粉末产率进行表征。利用红外光谱和接触角测量研究了纳米悬浮稳定剂（即 Dowfax 2A1）和糖之间的相互作用。与含有多糖的纳米混悬剂制剂相比，含有小分子量糖的纳米混悬剂制剂不聚集。此外，在喷雾干燥过程中，含有玻璃化转变温度较高的糖的制剂观察到较高的粉末产率。含有低玻璃化转变温度糖的制剂粘附在喷雾干燥器玻璃壁上，因此导致产率较低。红外和接触角数据表明，小分子量糖与 Dowfax 2A1 表现出良好的相互作用，可能导致喷雾或冷冻干燥过程中纳米晶体聚集最小化。可以利用糖的组合（即小分子量和多糖）来实现更高的喷雾干燥产率和非聚集的纳米晶体粉末。由 Elsevier B.V. 出版
In this study, the effect of low and high molecular weight sugars on indomethacin nano-crystalline suspension powders prepared by spray or freeze-drying was evaluated. Dowfax 2A1 (negatively charged surfactant) was utilized as indomethacin nanosuspensions stabilizer. Dried crystalline powders with or without sugars were characterized for crystallinity, particle size and powder yield. Interactions between the nanosuspension stabilizer (i.e. Dowfax 2A1) and sugars were investigated by utilizing IR spectroscopy and contact angle measurements. The nanosuspension formulations containing small molecular weight sugars were non-aggregating compared to those containing polysaccharides. Additionally, higher powder yields were observed with formulations containing sugars with higher glass transition temperature during spray drying. The formulations containing low glass transition temperature sugars were sticking to the spray drier glass walls and thus resulted in lower yields. The small molecular weight sugars showed favorable interactions with Dowfax 2A1, as evident by the IR and contact angle data, possibly resulting in minimal nano-crystal aggregation during spray or freeze-drying. A combination of sugars (i.e. small molecular weight and polysaccharides) may be utilized to achieve higher spray-drying yields and non-aggregating nano-crystalline powders. Published by Elsevier B.V.