关键词: Chiral separation Enantiomers High performance liquid chromatography Positron emission tomography Radiotracer Super fluidical chromatography

Mesh : Chromatography, High Pressure Liquid / methods Ligands Positron-Emission Tomography Radiopharmaceuticals / chemistry isolation & purification Stereoisomerism Temperature

来  源:   DOI:10.1016/j.chroma.2020.461611   PDF(Sci-hub)

Abstract:
Chiral column chromatography (CCC) is a revolutionary analytical methodology for the enantioseparation of novel positron emission tomography (PET) tracers in the primary stages of drug development. Due to the different behaviors of tracer enantiomers (e.g. toxicity, metabolism and side effects) in administrated subjects, their separation and purification is a challenging endeavor. Over the last three decades, different commercial chiral columns have been applied for the enantioseparation of PET-radioligand (PET-RL) or radiotracers (PET-RT), using high-performance liquid chromatography (HPLC). The categorization and reviewing of them is a vital topic. This review presents a brief overview of advances, applications, and future prospectives of CCC in radiopharmaceutical approaches. In addition, the effective chromatographic parameters and degravitation trends to enhance enantioseparation resolution are addressed. Moreover, the application and potential of chiral super fluidical chromatography (CSFC) as an alternative for enantioseparation in the field of radiopharmaceutical is discussed. Finally, the crucial application challenges of CCC are explained and imminent tasks are suggested.
摘要:
手性柱层析(CCC)是一种革命性的分析方法,用于在药物开发的主要阶段对新型正电子发射断层扫描(PET)示踪剂进行对映分离。由于示踪剂对映体的不同行为(例如毒性,代谢和副作用)在给药的受试者中,它们的分离和纯化是一项具有挑战性的工作。在过去的三十年里,不同的商业手性柱已用于PET-放射性配体(PET-RL)或放射性示踪剂(PET-RT)的对映分离,采用高效液相色谱法(HPLC)。对它们进行分类和审查是一个至关重要的主题。这篇综述简要概述了进展,应用程序,以及CCC在放射性药物方法中的未来前景。此外,讨论了有效的色谱参数和重力趋势,以提高对映体分离分辨率。此外,讨论了手性超流体色谱(CSFC)作为放射性药物领域对映分离的替代方法的应用和潜力。最后,解释了CCC的关键应用挑战,并提出了迫在眉睫的任务。
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