Analytical Chemistry and Pharmaceutical Technology, Center for Pharmaceutical Research, Vrije Universiteit Brussel, Brussels, Belgium.
Electrophoresis. 2011 Oct;32(19):2718-26. doi: 10.1002/elps.201100264. Epub 2011 Sep 5.
A generic strategy for the chiral separation of non-acidic pharmaceuticals was updated to complete an approach defined earlier. The selected chiral stationary phases are all polysaccharide selectors, chlorinated, and non-chlorinated, namely Lux(®) Amylose 2, Chiralcel(®) OD-RH, Lux(®) Cellulose 4, and Chiralpak(®) AD-RH. In this study, the screening step of a strategy defined earlier was updated and the optimization steps were re-evaluated for the applied chiral stationary phases. These screening and optimization conditions were studied by analyzing 20 pharmaceuticals at different organic modifier contents, temperatures, or applied voltages. The proposed chiral separation strategy was then evaluated with a test set of 19 non-acidic drugs. Seventeen compounds (89.5%) of the latter set could be resolved of which eight (42%) were baseline separated. The strategy thus proved to be applicable on compounds different from those used for its development.
一种手性拆分非酸性药物的通用策略被更新,以完成之前定义的方法。所选的手性固定相均为多糖类手性选择剂,包括氯代和非氯代的 Lux(®) 直链淀粉 2、Chiralcel(®) OD-RH、Lux(®) 纤维素 4 和 Chiralpak(®) AD-RH。在这项研究中,更新了之前定义的策略的筛选步骤,并重新评估了所应用的手性固定相的优化步骤。通过在不同有机溶剂含量、温度或施加电压下分析 20 种药物来研究这些筛选和优化条件。然后,用一组 19 种非酸性药物对所提出的手性拆分策略进行评估。在后一组中,有 17 种化合物(89.5%)可以拆分,其中 8 种(42%)可以基线分离。因此,该策略被证明适用于与其开发中使用的化合物不同的化合物。