A critical study on borosilicate glassware and silica-based QMA's in nucleophilic substitution with [18F]fluoride: influence of aluminum, boron and silicon on the reactivity of [18F]fluoride.
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.
University of Tromsø, Institute of Pharmacy, Department of Pharmaceutics and Biopharmaceutics, N-9037 Tromsø, Norway. anders.svadberg@uit.no
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Svadberg
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Clarke
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Dyrstad
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Martinsen
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Hjelstuen
D000077410:Aluminum Chloride; D017607:Aluminum Compounds / Q000737:chemistry; D001895:Boron / Q000737:chemistry*; D002712:Chlorides / Q000737:chemistry; D005459:Fluorides / Q000737:chemistry*; D005462:Fluorine Radioisotopes; D007553:Isotope Labeling / Q000379:methods*; D012825:Silicon / Q000737:chemistry*
D017607:Aluminum Compounds; D002712:Chlorides; D005462:Fluorine Radioisotopes; D000077410:Aluminum Chloride; D001895:Boron; D005459:Fluorides; D012825:Silicon