| Abstract
| - This report describes the 99mTc labeling of a hydrazinonicotinamide (HYNIC)-conjugated LTB4 receptorantagonist (SG380). The ternary ligand technetium complex [99mTc(SG38)(tricine)(TPPTS)] (RP517)was prepared using a non-SnCl2-containing formulation ((2001) J. Pharm. Sci.90, 114−123). Unlikeother HYNIC-conjugated small biomolecules, SG380 is lipophilic and has low solubility in the kitmatrix. Using a combination of a solubilizing agent (Lysolecithin) and a cosolvent (ethanol), we havedeveloped a new formulation for routine preparation of RP517. Using this formulation, RP517 can beprepared in high radiochemical purity (RCP > 90%) and remains stable in the kit matrix for at least6 h. We also prepared the corresponding 99Tc analogue, [99Tc]RP517. An HPLC concordance experimentusing RP517 and [99Tc]RP517 showed that the same technetium complex was prepared at both thetracer and macroscopic levels. The LC-MS data are completely consistent with the 1:1:1:1 compositionfor Tc:SG380:tricine:TPPTS.
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