...
【24h】

Are fluorine-rich pharmaceuticals lost by partition into fluorous phases?

机译:富氟药物是否会因分配到氟相而损失掉?

获取原文
获取原文并翻译 | 示例
           

摘要

The recently developed technology of droplet microfluidics has demonstrated great potential for many applications such as biochemical assay, high throughput screening, cell culture, directed evolution, and chemical synthesis. Intrigued by its capabilities for miniaturization, flexible manipulation, rapid reagent mixing and high throughput experimentation and analysis, the pharmaceutical industry has begun to investigate droplet microfluidic implementation in medicinal and process chemistry. Segmented by an immiscible secondary phase, usually perfluorinated oil, aqueous or organic droplets serve as individual micro-reactors without suffering cross-contamination. As many drug molecules contain fluorines, it is necessary to investigate whether such compounds will be preferentially extracted into the fluorous phase via fluorophilic solvation, which could lead to erroneous analytical results. In this work, we chose drugs with up to 10 fluorines to probe their partition into perfluorodecalin (PFD) from a variety of organic solvents. A fast and straightforward MISER (Multiple Injections in a Single Experimental Run) LC-MS method was applied to measure the loss of drug after mixing with PFD. We found that no significant partition occurred, with the concentration of drugs in the 'experimental' group measured as +/- 10% of the 'control' group. The RSD% of multiple injections is <5%. The finding was further validated by the conventional LC-MS approach. (C) 2016 Elsevier B.V. All rights reserved.
机译:液滴微流控技术的最新发展已显示出在许多应用中的巨大潜力,例如生化测定,高通量筛选,细胞培养,定向进化和化学合成。凭借其小型化,灵活的操作,快速的试剂混合以及高通量实验和分析的能力,制药行业开始研究液滴微流控技术在医药和过程化学中的应用。由不可混溶的第二相(通常是全氟化的油),水性或有机液滴进行分段,可充当单个微反应器,而不会遭受交叉污染。由于许多药物分子都含有氟,因此有必要研究这些化合物是否会通过亲氟溶剂化而优先提取到氟相中,这可能导致错误的分析结果。在这项工作中,我们选择了最多含10个氟的药物,以探究它们从各种有机溶剂中分配到全氟萘烷(PFD)中的情况。快速,简单的MISER(单次实验多次注射)LC-MS方法用于与PFD混合后测量药物的损失。我们发现没有发生明显的分配,“实验”组中的药物浓度为“对照组”的+/- 10%。多次进样的RSD%<5%。常规LC-MS方法进一步证实了这一发现。 (C)2016 Elsevier B.V.保留所有权利。

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号