制药盐酸盐的相图来自机械化学
Fragkoulis Theodosiou1, Toby J Blundell1, John S O Evans1
1Department of Chemistry, Durham University, Durham, UK.
Nature communications
|January 7, 2026
概括
控制溶剂活性液体辅助研磨 (CSA-LAG) 快速确定制药溶剂的稳定性. 这种机械化学方法有效地绘制相位边界,使药物开发速度更快,并合理选择固体形式.
科学领域:
- 固态化学 固态化学
- 机械化学 机械化学
- 制药发展 制药发展
背景情况:
- 结晶酸盐,包括水合物,在制药中具有显著的潜力.
- 目前用于评估溶剂物理稳定性的方法是繁且耗时的.
- 由于稳定性表征的困难,硫酸盐的利用是有限的.
研究的目的:
- 引入一种新的机械化学协议,即控制溶剂活性液体辅助研磨 (CSA-LAG).
- 为了快速阐明溶解物相界限.
- 为了促进药品固体形式的合理选择和工艺设计.
主要方法:
- CSA-LAG协议涉及二元/三元混合物中的不同溶剂活性.
- 对平衡的固体形式进行分析,以确定相位边界.
- 使用少量的活性药物成分 (API) 和已知的热力学活动.
主要成果:
- CSA-LAG在几分钟内达到平衡,比传统的泥快得多.
- 该方法准确量化了对整洁,水合和溶解域的关键溶剂活动.
- 在四种制药化合物中成功复制了各种溶解行为的泥边界和量化活性值.
结论:
- CSA-LAG将经验选转化为快速,热力学引导的工作流.
- 能够在药物形式选择和工艺设计中做出明智的决策.
- 提供了一种可重现和高效的方法,用于溶解物相界限的阐明.
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