甲-乳糖单酸的结构,形态和表面特性与其粉末特性相关
Thai T H Nguyen1, Cai Y Ma1, Ioanna D Styliari2
1Centre for the Digital Design of Drug Products, School of Chemical and Process Engineering, Institute of Process, Research & Development, University of Leeds, Leeds LS2 9JT, UK.
Journal of pharmaceutical sciences
|October 31, 2024
概括
了解α-乳糖单水合物 (αLMH) 的晶体特性是制药配方的关键. 这项研究揭示了晶体形态和表面能量如何影响药物产品的性能,特别是气溶分散.
科学领域:
- 材料科学 材料科学 材料科学
- 制药科学 制药科学
- 晶体学 晶体学是指结晶学.
背景情况:
- 常见的制药辅助剂α-乳糖单酸盐 (αLMH) 的颗粒物特性对于药物产品的设计和性能至关重要.
- 了解晶体形态,表面化学和表面能量对于优化αLMH作为载体至关重要.
研究的目的:
- 对αLMH的分子和分子间性质进行多层次分析,包括晶体形态,表面化学和表面能量.
- 为了验证预测的晶体形态,使用X射线衍射 (XCT) 对比断层扫描.
- 为了将表面能量与晶体形态和气溶散射性能相关联.
主要方法:
- 集成的多尺度工作流程用于分子和分子间分析.
- 用X射线衍射 (XCT) 对比断层扫描进行形态验证.
- 逆气色谱用于测量表面能量.
主要成果:
- 来自水溶液的αLMH晶体的最快生长沿着b轴发生,受溶解效应的影响.
- 由于不对称的结合,β-乳糖的存在导致了托马霍克形态,从而产生极性.
- 水晶格子的能量主要是由范德瓦尔斯相互作用驱动的,静电相互作用也有所贡献.
- 预测的总表面能量与实验测量结果一致,尽管分散贡献不同.
- 表面能量在不同的晶体习惯表面上是一致的,支持同质的药物结合.
- 长长的晶体形态表现出比三角形或托马霍克形状更低的表面能量,与更好的气溶分散相关.
结论:
- 该研究提供了对αLMH物理化学的全面了解,将晶体结构与性能联系起来.
- 形态和表面能量是αLMH作为药物载体的适用性的关键决定因素,特别是在气溶药物中.
- 这些发现为合理设计和配制使用αLMH的药物产品提供了宝贵的见解.
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