在药品中揭开多态性和多态性相互转换:基化的特殊案例
Inês C B Martins1, Anders S Larsen1, Anders Ø Madsen1
1Department of Pharmacy, University of Copenhagen Universitetsparken 2 2100 Copenhagen Denmark ines.martins@sund.ku.dk thomas.rades@sund.ku.dk.
Chemical science
|October 27, 2023
概括
这项研究探讨了基亚胺 (HCT) 的多态性,揭示了具有不同稳定性的三个不同的形式. 火冷却方法产生了最稳定的HCT多态,为固态现象提供了洞察力.
科学领域:
- 固态化学 固态化学
- 材料科学是一种材料科学.
- 制药科学 制药科学 制药科学
背景情况:
- 多态性,即固体以多种无形形式存在的能力,在分子层面上不太清楚.
- 虽然报告了无机系统和一些有机化合物,但其在药品中的发生和特征仍然不清楚.
研究的目的:
- 调查多态形态形式在酸化 (HCT) 中的发生和相互转化.
- 描述不同HCT多态的物理和热稳定性.
- 为了阐明HCT多态体之间的分子水平差异.
主要方法:
- 使用喷雾干燥 (SD),冷却冷却 (QC) 和球磨 (BM) 系统地制备HCT多态化合物.
- 物理和热稳定性和放松性能的实验性表征.
- 分子动力学模拟来分析分子组织和二面角分布.
主要成果:
- 成功制备了三种不同的HCT多态,每一种都有独特的稳定性和放松性.
- 由QC生产的HCT多态II,与多态I (SD) 和III (BM) 相比,具有更高的物理稳定性.
- 多态 I 和 III 可以通过 QC 转换为多态 II,但多态 II 不能通过 SD 或 BM 转换为其他形式. 分子动力学揭示了多态形体I和II之间二面角分布的显著差异.
结论:
- 甲 (HCT) 呈现多态性,不同的形式具有不同的稳定性和分子排列.
- 火冷却是一种有效的方法,可以生产出更稳定的物理HCT多态.
- 分子构造的差异,特别是二面角,可能是HCT多态体中观察到的物理化学性质变异的基础.
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