Egginger G, Lindner W, Vandenbosch C, Massart D L
Institute of Pharmaceutical Chemistry, Karl-Franzens-University, Graz, Austria.
Biomed Chromatogr. 1993 Nov-Dec;7(6):277-95. doi: 10.1002/bmc.1130070602.
The recent developments in enantioselective HPLC-separation techniques are impressive and are driven by industrial and academic interests; thus there is for instance a high demand for developing stereoselective assays for chiral drugs in biological fluids. The beta-blocking agents, which possess an amino-propanol- or -ethanol side chain with at least one chiral centre, represent one of the most intensively investigated groups of more than 40 drugs introduced world wide. Seven of the most popular beta-blockers were chosen as representatives: atenolol; betaxolol; carvedilol; metoprolol; pindolol; propranolol; and sotalol, these span the whole range of lipophilicity to hydrophilicity (polarity). Enantioselective HPLC bioassays for these beta-blockers published so far, including techniques based on chiral derivatizing agents (CDAs), chiral stationary phases (CSPs) and chiral mobile phase additives (CMPAs) have been reviewed and documented in the light of general aspects together with pharmacokinetic and pharmacodynamic considerations.
对映体选择性高效液相色谱分离技术的最新进展令人瞩目，且受到工业界和学术界的关注推动；因此，例如对开发生物流体中手性药物的立体选择性分析方法有很高的需求。β受体阻滞剂具有带有至少一个手性中心的氨基丙醇或氨基乙醇侧链，是全球推出的40多种药物中研究最为深入的类别之一。选择了七种最常用的β受体阻滞剂作为代表：阿替洛尔；倍他洛尔；卡维地洛；美托洛尔；吲哚洛尔；普萘洛尔；和索他洛尔，这些药物涵盖了从亲脂性到亲水性（极性）的整个范围。迄今为止已发表的针对这些β受体阻滞剂的对映体选择性高效液相色谱生物分析方法，包括基于手性衍生化试剂（CDA）、手性固定相（CSP）和手性流动相添加剂（CMPA）的技术，已结合一般方面以及药代动力学和药效学考虑因素进行了综述和记录。
