通过超临界流体染色学和高性能液体染色学对基于多糖的状静止阶段进行阿福索拉纳的状分离的比较研究
Can Xia1, Rong Zhu1, Yu-Xin Fan1
1School of Chemistry, Key Laboratory of Process Control and Quality Evaluation of Chiral Drugs, Guangdong Provincial Drug Administration, Guangzhou Key Laboratory of Biomedical Analytical Chemistry, South China Normal University, Guangzhou, China.
超临界流体染色学 (SFC) 提供了一种绿色和高效的方法,用于像afoxolaner这样的药品的奇拉分离. 这项研究优化了SFC条件,实现了快速和精确的分辨率,超过了传统的高性能液态色谱 (HPLC).
科学领域:
- 分析化学 分析化学
- 分离科学 分离科学
- 绿色化学 绿色化学
背景情况:
- 化拉分离对于药物开发至关重要.
- 超临界流体染色学 (SFC) 是一个有希望的绿色替代高性能液体染色学 (HPLC).
- 阿福索拉纳是一种新的合性药物,需要高效的分离方法.
研究的目的:
- 用SFC和HPLC比较研究阿福索拉纳的奇拉分离.
- 为了优化SFC条件,以分离afoxolaner反体.
- 阐明控制分离机制的分子相互作用.
主要方法:
- 对阿福索拉纳反体进行SFC和HPLC比较分析.
- 选五个基于多糖的性静止阶段 (CSPs).
- 优化SFC参数:修饰器类型/比率,流量,温度,反压.
- 分子对接研究,以了解相互作用机制.
- 定量分析以确定线性和量化的极限.
主要成果:
- 用纤维素三4-甲基酸涂层的CSP提供了最好的SFC分离 (分辨率=2.37).
- 优化的SFC在不到6分钟的时间内实现了阿福索拉纳反体化,比HPLC快得多.
- 分子对接揭示了键,键,疏水效应和π-π堆叠作为关键相互作用.
- SFC 显示出优异的线性 (R2 > 0.999) 和低量化极限 (0.025 mg/mL) 的阿福索拉纳反体.
结论:
- SFC是一种高效,快速和绿色的方法,用于奇拉制药分离.
- 优化的SFC条件为afoxolaner分辨率提供了比HPLC更好的替代方案.
- 了解分子相互作用可以提高CSP的选择和开发方法,以进行奇拉分离.
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