Evaluation of an automated double-synthesis module: efficiency and reliability of subsequent radiosyntheses of FHBG and FLT

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• 作者：Sabrina Niedermoser^a ; Manuela Pape^a ; Franz Josef Gildehaus^a ; Carmen Wä ; ngler^a ; Markus Hartenbach^b ; Ralf Schirrmacher^c ; Peter Bartenstein^a ; Bjö ; rn Wä ; ngler^a ; ^d ; ^{bjoern.waengler@med.uni-muenchen.de}
• 关键词：[18F]FLT ; [18F]FHBG ; Double synthesis ; Explora GN
• 刊名：Nuclear Medicine and Biology
• 出版年：2012
• 期刊代码：43_09698051
• 类别：ph
• 出版时间：May, 2012
• 卷：39
• 期：4
• 页码：586-592
• 文件大小：408 K

摘要

We optimized the synthesis methods for 3鈥?deoxy-3鈥?[¹⁸F]fluorothymidine ([¹⁸F]FLT) and 9-(4-[¹⁸F]fluoro-3-[hydroxymethyl]butyl)guanine) ([¹⁸F]FHBG) and automated them on an Explora General Nucleophilic double-synthesis module. Furthermore, the synthesis efficiency and reliability and the formation of cross-contaminations of the products when preparing two consecutive batches were evaluated. Whereas the preinstalled FLT synthesis conditions required substantial modification in reaction and neutralization conditions to achieve radiochemical yields of up to 60%within 70卤10 min including high-performance liquid chromatography purification, the synthesis of FHBG had to be implemented to the module to obtain competitive radiochemical yields of up to 40%in an overall synthesis time of 60卤10 min. The radiochemical purities obtained were 鈮?9%and 鈮?6%for the synthesis of [¹⁸F]FLT and [¹⁸F]FHBG, respectively. No significant changes in yield or purity could be observed between both batch productions. We found that the yields and purities also did not change when performing FLT after FHBG syntheses and vice versa. Hence, we developed a synthesis setup that offers the opportunity to perform two subsequent syntheses of either [¹⁸F]FLT, [¹⁸F]FHBG or [¹⁸F]FLT after [¹⁸F]FHBG without decrease in radiochemical yields and purities. Also, no cross-contaminations were observed, which can be attributed to the use of separate product delivery tubes, purification columns and聽an automated intermediate cleaning program. These results open up the possibility of producing consecutively either two equal ¹⁸F-fluorinated tracers or two different ones in high yields on the same synthesis module.