VALIDATION AND APPLICATION OF A SOLID-PHASE CHEMISTRY METHOD FOR PREPARATION OF HIGH EFFECTIVE SPECIFIC ACTIVITY TC-99M RADIOPHARMACEUTICALS

Solid phase chemistry with UltraLink(TM) Iodoacetyl gel was investigat ed as a method for removing excess ligand present in preparations of d iaminedithiol (DADT) Tc-99m radiopharmaceuticals. The process was opti mized and tested under Tc-99m labeling conditions with 2,2,4,9,9-penta methyl-4,7-diaza-1,10-decanedithiol (N-methyl-DADT), 1, and 4-(1-(2'-m ethoxyphenyl) )-2,2,9,9-tetramethyl-4,7-diaza-1,10-decanedithiol (DADT -4C-MPP), 2, a serotonin receptor binding ligand. The results illustra ted that this gel removed greater than or equal to 99.9% excess ligand used in labeling reactions, and was comparable to the level of purifi cation usually obtained by the more labor intensive method of HPLC. (C ) 1997 Elsevier Science Inc.