PPERFORMANCE EVALUATION OF TWO MIPS FOR THE SPE-LC-UV DETERMINATION OF p-[18F]MPPF IN PLASMA

FP6 STRP 516984 MI-lab-on-chi

DEVELOPMENT AND VALIDATION OF A METHOD FOR THE LC DETERMINATION p-[18F]MPPF IN PLASMA USING A MISPE

Peer reviewe

Methof for the elution of 18F fluoride trapped on an anion-exchange phase in a form suitable for efficient radiolabelling without any evaporation step

publication date: 2008-08-28; filing date: 2008-02-19The invention relates to a method to ext. out of an aq. soln., conc. and​/or reformulate [18F] fluorides without any evapn. step, characterized in that the eluting soln. is a low water content, preferably <3​% water, org. soln. contg. at least: a first compd. (A) which is a tertiary alc.-​function bearing mol., a second compd. (B) which is a phase transfer agent suitable for radiolabeling and which is necessary to the anion exchange process. Said org. solvent is selected from acetonitrile (ACN)​, DMSO)​, dimethylacetamide, DMF, THF, di-​Et ether, dioxane, Et acetate, acetone, isobutyronitrile, benzonitrile, pyridine, di-​Et carbonate, sulfolane, hexamethylphosphotriamide (HMPA​/HMPT)​, and any mix of these solvents. Said nonpolar org. solvent is selected from pentane, hexane, heptane, octane, nonane, decane, and cyclohexane

Fully Automated Preparation and Conjugation of N-Succinimidyl 4-[(18)F]Fluorobenzoate ([ (18)F]SFB) with RGD Peptide Using a GE FASTlab Synthesizer.

PURPOSE: The aim of this work was to automate the radiosynthesis of [(18)F]SFB, a widely used reagent for the labeling of biomolecules with (18)F on a new generation commercial synthesis module (FASTLab, GE Healthcare). PROCEDURES: Two synthesis approaches were implemented on this module: the classical "two-pot radiosynthesis" and the more recently described "one-pot" method. RESULTS: The "two-pot" approach affords [(18)F]SFB with a 42% decay-corrected yield in 57 min (n = 24) with a chemical purity sufficient to avoid an intermediate HPLC purification. The recently established "one-pot" method, afforded a product with a lower chemical purity, in the conditions used in this report. The lower d.c. yield obtained (32% (n = 15)) was related to the low (18)F labeling yields obtained in MeCN compared with DMSO. The subsequent conjugation step with a RGD (PRGD2) peptide was also successfully automated. CONCLUSIONS: The formulated [(18)F]FPRGD2 was obtained without any operator manipulation with a d.c. yield of 13% +/- 3% (n = 13) in 130 min, a radiochemical purity >98% and a specific activity of 140 +/- 40 TBq/mmol