Svadberg A, Clarke A, Dyrstad K, Martinsen I, Hjelstuen O K
University of Tromsø, Institute of Pharmacy, Department of Pharmaceutics and Biopharmaceutics, N-9037 Tromsø, Norway.
Appl Radiat Isot. 2011 Feb;69(2):289-94. doi: 10.1016/j.apradiso.2010.09.013. Epub 2010 Oct 30.
Leachables of borosilicate glassware and silica-based anion exchange columns (QMAs) may influence nucleophilic substitution with [(18)F]fluoride ([(18)F]F(-)). Aluminum, boron and silicon, all constituents of borosilicate glass, were found as water soluble leachables in a typical PET synthesis setup. Relevant ranges of the leachable quantities were studied based on an experimental design, in which species of the three elements were added to the labeling of the precursor for anti-1-amino-3-[(18)F]fluorocyclobutyl-1-carboxylic acid ([(18)F]FACBC). Levels of 0.4-2 ppm aluminum as AlCl(3) had a strong negative influence on labeling yield while 4-20 ppm of boron as KBO(2) and 50-250 ppm of silicon as Na(2)SiO(3) did not have a significant impact. Interesting interaction effects between the elements were observed, where particularly KBO(2) reduced the negative effect of AlCl(3) on labeling yield. It can be concluded that leachables of borosilicate glassware easily can influence nucleophilic substitution with n.c.a. [(18)F]F(-) and give variable yields.
硼硅酸盐玻璃器皿和硅基阴离子交换柱（QMA）的可浸出物可能会影响用[（18）F]氟化物（[（18）F]F-）进行的亲核取代反应。硼硅酸盐玻璃的所有成分铝、硼和硅，在典型的正电子发射断层扫描（PET）合成装置中被发现是水溶性可浸出物。基于实验设计研究了可浸出量的相关范围，在该实验设计中，将这三种元素的种类添加到抗1-氨基-3-[(18)F]氟环丁基-1-羧酸（[(18)F]FACBC）前体的标记中。以AlCl3形式存在的0.4 - 2 ppm铝对标记产率有强烈的负面影响，而以KBO2形式存在的4 - 20 ppm硼和以Na2SiO3形式存在的50 - 250 ppm硅没有显著影响。观察到元素之间有趣的相互作用效应，特别是KBO2降低了AlCl3对标记产率的负面影响。可以得出结论，硼硅酸盐玻璃器皿的可浸出物很容易影响用无载体[（18）F]F-进行的亲核取代反应，并产生可变的产率。
