Abstract

BackgroundFast implementation of positron emission tomography (PET) into clinical and preclinical studies highly demands automated synthesis for the preparation of PET radiopharmaceuticals in a safe and reproducible manner. The aim of this study was to develop automated synthesis methods for these six 18F-labeled radiopharmaceuticals produced on a routine basis at the University of Pennsylvania using the AllinOne synthesis module.ResultsThe development of automated syntheses with varying complexity was accomplished including HPLC purification, SPE procedures and final formulation with sterile filtration. The six radiopharmaceuticals were obtained in high yield and high specific activity with full automation on the AllinOne synthesis module under current good manufacturing practice (cGMP) guidelines.ConclusionThe study demonstrates the versatility of this synthesis module for the preparation of a wide variety of 18F-labeled radiopharmaceuticals for PET imaging studies.

Highlights

  • Fast implementation of positron emission tomography (PET) into clinical and preclinical studies highly demands automated synthesis for the preparation of PET radiopharmaceuticals in a safe and reproducible manner

  • The 110 min half-life of fluorine-18 has firmly established itself as the radionuclide of choice for imaging applications since it allows for longer data acquisition for dynamic imaging studies and high count rates for metabolite analyses which are often required for quantitative PET imaging studies

  • We describe the fully automated syntheses on the AllinOne module of the six radiotracers described above (Fig. 1)

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Summary

Introduction

Fast implementation of positron emission tomography (PET) into clinical and preclinical studies highly demands automated synthesis for the preparation of PET radiopharmaceuticals in a safe and reproducible manner. The main limitation of PET is the short half-lives of the radionuclides used in the development of PET radiotracers. Among the most popular positron-emitting radionuclides, short half-life radionuclides like oxygen-15 and nitrogen-13 are used for brain perfusion studies ([15O]H2O) and heart perfusion studies ([13N]NH3) respectively (Bergmann et al, 1989; Grüner et al, 2011; Muzik et al, 1993). The 20.4 min half-life of carbon-11 and the rapid production of reactive intermediates such as [11C]methyl iodide and [11C]methyltriflate have facilitated the generation of 11C-labeled radiotracers for a variety of imaging applications. The 110 min half-life of fluorine-18 has firmly established itself as the radionuclide of choice for imaging applications since it allows for longer data acquisition for dynamic imaging studies and high count rates for metabolite analyses which are often required for quantitative PET imaging studies.

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