The aim of the present study was to label a therapeutic dose of zoledronic acid (ZOL) with Tc-99m, evaluate its in vitro stability and compare its biodistribution to (99m)Tc-methylene biphosphonate ((99m)Tc-MDP) in normal rabbits. Preparation of 0.50 mg of (99m)Tc-ZOL was carried out by the reduction of (99m)Tc-pertechnetate in the presence of stannous chloride. The radiolabeling efficiency was found to be greater than 99%. The labeled complex was stable at least up to 6 h at room temperature determined by paper chromatography. (99m)Tc-ZOL and (99m)Tc-MDP were administered intravenously to the rabbits for scintigraphic studies. Between (99m)Tc-ZOL and (99m)Tc-MDP, there were no significant differences in the ratios of femur/BG and lumbar vertebrae/BG, whereas epiphysis/BG and the kidney/BG ratios of (99m)Tc-MDP were higher than (99m)Tc-ZOL at the static studies. (C) 2009 Elsevier Ltd. All rights reserved.