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Title: Preparation of gallium-68 radiopharmaceuticals for positron tomography. Progress report, November 1, 1980-December 31, 1981

Technical Report ·
OSTI ID:6299356

Although the germanium-68 ..-->.. gallium-68 generator is probably the only source of positron-emitting radionuclides that could enable the widespread application of positron tomography, the commercially available /sup 68/Ga//sup 68/Ge generator system suffers from several major disadvantages. The most important of these is that the generator is eluted with EDTA, which forms a very strong chelate with gallium. In order to produce radiopharmaceuticals other than /sup 68/Ga-EDTA, it is first necessary to break the stable EDTA complex and remove all traces of EDTA. This procedure adds several steps and a significant amount of time to procedures for preparing /sup 68/Ga-radiopharmaceuticals. Several years ago, we developed a new generator using a solvent extraction system which produces /sup 68/Ga-oxine (8-hydroxyquinoline), a weak chelate. We have also carried out studies to compare generator systems which produce /sup 68/Ga in an ionic form. Using the gallium-68 eluted from these various generator systems, several /sup 68/Ga-labeled radiopharmaceuticals have been synthesized and tested in vitro and in vivo. In addition, attempts have been made to design and synthesize a lipophilic ligand for gallium-68. The stability of radiogallium complexed with a series of potentially lipophilic complexing agents has been studied using chromatographic techniques and in vivo distribution data. The potential of these complexing agents for altering the biodistribution of gallium radiopharmaceuticals has also been investigated.

Research Organization:
Washington Univ., St. Louis, MO (USA). Edward Mallinckrodt Inst. of Radiology
DOE Contract Number:
AS02-77EV04318
OSTI ID:
6299356
Report Number(s):
DOE/EV/04318-4; ON: DE81029092; TRN: 81-015389
Country of Publication:
United States
Language:
English