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Simple preparation and purification of ethanol-free solutions of 3'-deoxy-3'-[18F]fluorothymidine by means of disposable solid-phase extraction cartridges.

Abstract：

INTRODUCTION:3'-Deoxy-3'-[(18)F]fluorothymidine ([(18)F]FLT) shows great potential as a tracer for proliferative studies with PET. However, its regular application is often limited by low radiochemical yields and the use of a troublesome HPLC separation. Moreover, a high content of ethanol, at least one-fold higher than the European Pharmacopoeia and US Pharmacopoeia's established limit, is always present in the final product. The present study reports an optimization of the reaction conditions and a simple and straightforward purification step which affords a solution of [(18)F]FLT suitable for human use. METHODS:Several conditions and materials were tested for both the nucleophilic substitution and purification step. The latter was achieved by means of a series of commercial solid-phase extraction cartridges. Very conveniently, the whole one-pot synthesis was carried out on commercial automated modules using basically the same setup employed for the synthesis of [(18)F]FDG. RESULTS:Under routine conditions, radiochemical yields of 37% [decay-corrected to start of synthesis (SOS)] were achieved in ca. 39 min from SOS, with radiochemical purities >98% (usually >99%). The negligible radiolysis observed could be easily suppressed by adding 0.5% of EtOH. Typical unlabelled chemical impurities detected were thymidine (0.15 ppm), thymine (0.28 ppm) and stavudine (0.05 ppm). CONCLUSIONS:A reliable, simple and efficient preparation of [(18)F]FLT has been developed, able to afford an ethanol-free solution of the tracer with no need for any HPLC purification. Because of its similarity to the [(18)F]FDG synthesis, the method can be readily implemented on basically all the commercial modules developed for this common radiotracer.

journal_name

Nucl Med Biol

journal_title

Nuclear medicine and biology

authors

Pascali C,Bogni A,Fugazza L,Cucchi C,Crispu O,Laera L,Iwata R,Maiocchi G,Crippa F,Bombardieri E

doi

10.1016/j.nucmedbio.2011.10.005

subject

Has Abstract

pub_date

2012-05-01 00:00:00

pages

540-50

issue

eissn

0969-8051

issn

1872-9614

pii

S0969-8051(11)00238-1

journal_volume

pub_type

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Simple preparation and purification of ethanol-free solutions of 3'-deoxy-3'-[18F]fluorothymidine by means of disposable solid-phase extraction cartridges.