Kumar Sumit, Gokhale Rajeev, Burgess Diane J
University of Connecticut, School of Pharmacy, 69 North Eagleville Road, Storrs, CT 06269, USA.
AbbVie Pte Ltd, Research and Development, 11 Biopolis Way, Helios, #05-06, Singapore 138667, Singapore.
Int J Pharm. 2014 Aug 25;471(1-2):303-11. doi: 10.1016/j.ijpharm.2014.05.060. Epub 2014 Jun 2.
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.
在本研究中，评估了低分子量和高分子量糖类对通过喷雾或冷冻干燥制备的吲哚美辛纳米晶悬浮粉末的影响。Dowfax 2A1（带负电荷的表面活性剂）用作吲哚美辛纳米悬浮液的稳定剂。对含或不含糖类的干燥结晶粉末进行了结晶度、粒度和粉末产率的表征。利用红外光谱和接触角测量研究了纳米悬浮液稳定剂（即Dowfax 2A1）与糖类之间的相互作用。与含多糖的纳米悬浮液配方相比，含小分子量糖类的纳米悬浮液配方不会聚集。此外，在喷雾干燥过程中，含玻璃化转变温度较高的糖类的配方具有更高的粉末产率。含玻璃化转变温度较低的糖类的配方会粘在喷雾干燥器的玻璃壁上，从而导致产率较低。红外光谱和接触角数据表明，小分子量糖类与Dowfax 2A1表现出良好的相互作用，这可能导致在喷雾或冷冻干燥过程中纳米晶体的聚集最小。糖类（即小分子量糖类和多糖）的组合可用于实现更高的喷雾干燥产率和无聚集的纳米晶粉末。
