Department of Analytical Chemistry, China Pharmaceutical University, Nanjing, PR China.
Electrophoresis. 2010 Jan;31(2):371-7. doi: 10.1002/elps.200900343.
A wide variety of chiral selectors have been employed in CZE, and among them macrocyclic antibiotics including glycopeptides, ansamycins, aminoglycosides and polypeptides exhibited prominent enantioselective properties toward abundant racemic compounds. Compared with CZE, the use of macrocyclic antibiotics as chiral selectors in NACE has not been reported previously. In this study, an approach to the enantioseparation of basic drugs by means of NACE with erythromycin lactobionate (EL) belonging to the group of macrolide antibiotics has been investigated. Especially different from the above four classes of antibiotics, there are no reports concerned with the use of macrolides which belong to macrocyclic antibiotics as chiral selectors in CE. In this work EL is first used as a chiral selector in NACE for the enantiomeric separations of two racemic basic drugs that possess high separability consisting of propranolol and duloxetine. Furthermore, EL possesses advantages such as high solubility and low viscosity in the solvent and very weak UV absorption. The chiral separations were achieved using Tris-boric acid as the BGE and methanol as the organic medium. In the course of this work we observed that both migration time and enantioseparation were influenced by several parameters such as the pH and composition of the BGE, EL concentration, capillary temperature and applied voltage. Consequently, these parameters were systematically optimized in order to obtain the optimum enantioseparations.
已在 CZE 中使用了多种手性选择剂，其中包括糖肽、安莎霉素、氨基糖苷和多肽等大环抗生素，它们对大量外消旋化合物表现出突出的对映选择性。与 CZE 相比，以前没有报道过在 NACE 中使用大环抗生素作为手性选择剂。在这项研究中，我们研究了通过 NACE 用属于大环抗生素的红霉素乳糖酸盐 (EL) 对碱性药物进行对映体分离的方法。与上述四类抗生素不同，没有关于将属于大环抗生素的大环内酯类抗生素用作 CE 中手性选择剂的报道。在这项工作中，EL 首次被用作 NACE 中的手性选择剂，用于对具有高分离度的两种外消旋碱性药物（普萘洛尔和度洛西汀）进行对映体分离。此外，EL 在溶剂中具有高溶解度、低粘度和非常弱的紫外吸收等优点。手性分离是在 Tris-硼酸作为 BGE 和甲醇作为有机介质的条件下实现的。在这项工作中，我们观察到迁移时间和对映体分离都受到几个参数的影响，如 BGE 的 pH 和组成、EL 浓度、毛细管温度和施加电压。因此，为了获得最佳的对映体分离，我们系统地优化了这些参数。
