Pharmaceutics Research Laboratory, School of Life Sciences, University of Sussex, Brighton, BN1 9QJ, UK.
Drug Applied Research Center and Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran.
Drug Deliv Transl Res. 2020 Oct;10(5):1418-1427. doi: 10.1007/s13346-020-00707-6.
Although in dry powder inhaler (DPI) formulations a single carrier is used, a single carrier is not able to provide an excellent aerosolization performance when it is used in DPI formulations. Thereby, the aim of this study was to engineer a suitable ternary mixture of mannitol-lactose-leucine to be used in a DPI formulation with enhanced aerosolization performance. To this end, binary mixtures of mannitol:lactose containing a constant amount of leucine (5% w/w of carriers) were spray-dried as a single solution. Spray-dried samples were blended with salbutamol sulfate to determine the efficiency of their aerosolization performance. Interestingly, note that lactose was in its amorphous state stabilized by the presence of mannitol in the samples. Spray-dried mannitol without lactose showed a combination of the α- and β-polymorphic forms which was the case in all other ratios of mannitol:lactose. It was shown that the highest fine particle fraction (FPF) was 62.42 ± 4.21% which was obtained for the distinct binary mixtures (1:3 mannitol:lactose) compared to a single carrier. This study opens a new window to investigate further the implementation of binary mixtures of sugar carriers containing leucine in DPI formulations to overcome poor aerosolization performance the mentioned DPI formulations.
虽然在干粉吸入器（DPI）制剂中使用单一载体，但当它在 DPI 制剂中使用时，单一载体无法提供出色的气溶胶化性能。因此，本研究的目的是设计一种合适的甘露醇-乳糖-亮氨酸三元混合物，用于具有增强的气溶胶化性能的 DPI 制剂。为此，将含有恒定量亮氨酸（载体的 5%w/w）的甘露醇：乳糖的二元混合物作为单一溶液进行喷雾干燥。喷雾干燥的样品与硫酸沙丁胺醇混合，以确定其气溶胶化性能的效率。有趣的是，请注意，乳糖在样品中甘露醇的存在下处于无定形状态。不含乳糖的喷雾干燥甘露醇显示出α-和β-多晶型的组合，所有其他甘露醇：乳糖比例的情况都是如此。结果表明，最高的细颗粒分数（FPF）为 62.42±4.21%，这是在明显的二元混合物（1:3 甘露醇：乳糖）中获得的，而不是在单一载体中获得的。这项研究为进一步研究在 DPI 制剂中实施含有亮氨酸的糖载体二元混合物以克服上述 DPI 制剂中较差的气溶胶化性能开辟了新的窗口。
