正电子药品氨基聚醚（2.2.2）含量测定方法研究进展

正电子类放射性药品（简称“正电子药品”）是采用正电子核素标记制备的诊断用放射性药品。现有正电子药品的主要类型是［¹⁸F］氟标记药品。在制备时其［¹⁸F］氟标记反应大多使用有毒的氨基聚醚（2.2.2）（即K 2.2.2）作催化剂，故正电子药品中K 2.2.2的残留量应予以控制。正电子药品辐射水平较高，剂量小，衰变快，测定其K 2.2.2含量需要便捷、专属、灵敏、稳定的方法。通过总结已报道方法，梳理其发展历程、方法特点和方法学参数可知，目前K 2.2.2的分析方法体系包含分光光度滴定法（ST法）、薄层色谱法（TLC法）、紫外分光光度法（UV法）、比色法（colorimetry法）、气相色谱法（GC法）、高效液相色谱法（HPLC法）、流动注射法（FIA法）及毛细管电泳法（CE法）。这些方法的机制不同，方法学指标各异，分别适用于不同的样品、设备条件和目标需求，其中TLC法和HPLC法凭借其特定优势占据了主导地位。如何更好地平衡各方法学指标，实现微型化、自动化以及同时测定包括K 2.2.2在内的多个质控指标成分，将是今后方法学研究的重点方向。K 2.2.2含量测定方法已形成体系，其开发和改进将对提高正电子药品的质控水平发挥积极作用。

Positron emission radio-pharmaceuticals (PERs) are the tracers labeled with positron emission isotopes for clinical imaging.[¹⁸F]Fluoro-labeled tracers are the majority of PERs. In most[¹⁸F]Fluoro-labeling reactions,toxic aminopolyether (2.2.2) (i.e. K 2.2.2) is employed as a catalyst. So the residue of K 2.2.2 should be controlled. High radiation,small dose and fast decay are the typical properties of positron emission radio-pharmaceuticals,which require convenient,fast,specific,sensitive and robust methods for the determination of K 2.2.2. In this review,we summarized the history,features and methodological parameters of the published methods. In general,the system of the methods consists of spectrophotometric titration (ST),thin-layer chromatography (TLC),ultra-violet spectrophotometry (UV),colorimetry,gas chromatography (GC),high performance liquid chromatography (HPLC),flow injection analysis (FIA) and capillary electrophoresis (CE). These methods have different mechanisms and methodological parameters,suitable for various samples,equipment conditions and purposes. TLC and HPLC are the dominant ones in the method system due to their specific advantages. A better balance between various methodological parameters,minimization,automation and the simultaneous determination of multiple quality-control indexes including K 2.2.2 are the key directions of future research. Conclusively,the system of K 2.2.2 analytical methods has established.The development and optimization of it will help to improve the quality control of PERs.

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