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作为吸入用喷雾干燥粉末赋形剂的亮氨酸。

Leucine as an excipient in spray dried powder for inhalation.

机构信息

Pharmaceutical and Molecular Biotechnology Research Centre (PMBRC), Waterford Institute of Technology, Waterford, Ireland.

Pharmaceutical and Molecular Biotechnology Research Centre (PMBRC), Waterford Institute of Technology, Waterford, Ireland; SSPC - The Science Foundation Ireland Research Centre for Pharmaceuticals, Ireland.

出版信息

Drug Discov Today. 2021 Oct;26(10):2384-2396. doi: 10.1016/j.drudis.2021.04.009. Epub 2021 Apr 17.

DOI:10.1016/j.drudis.2021.04.009
PMID:33872799
Abstract

Leucine is a promising excipient with several applications in the development of inhalable spray-dried powder of high- and low-dose drugs. The addition of leucine has exhibited significant enhancing effects on the aerosolization and physical stability of the produced particles. Here, we focus not only on the applications of leucine in inhalable spray-drying powders, but also on the underlying mechanisms by which the formulation and processing parameters dictate the behavior of leucine during the drying process and, therefore, its functionalities within the dried powder. Additionally, we highlight the current regulatory status of leucine. Such insights are important for more efficient utilization of leucine in the future, both for dry powder inhaler formulations and other pharmaceutical applications.

摘要

亮氨酸是一种很有前途的赋形剂,在开发高、低剂量药物的可吸入喷雾干燥粉末方面有多种应用。亮氨酸的添加对所产生颗粒的气溶胶化和物理稳定性有显著的增强作用。在这里,我们不仅关注亮氨酸在可吸入喷雾干燥粉末中的应用,还关注制剂和加工参数通过何种内在机制来控制亮氨酸在干燥过程中的行为,从而影响其在干粉中的功能。此外,我们还强调了亮氨酸的当前监管状况。这些见解对于未来亮氨酸在干粉吸入剂制剂和其他药物应用中的更有效利用非常重要。

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