Аннотация:Zolidronic acid (ZA) was chosen as the object for investigation due to it therapeutic effect and accumulation in the bone metastases. Aim To investigate the reaction conditions (pH, concentration of SnCl2 and ligand, temperature, reaction time, adding of different antioxidants and carrier) for the preparation of 188Re-ZA using carrier-free 188Re from the 188W/188Re generator. Biodistribution of 188Re-ZA was also studied.Materials and methods Rhenium-188 was eluted from commercially produced 188W/188Re generator (IPPI, Russia). The labeling was carried out as follows: To ZA aqueous solution, aqueous solution of antioxidant (ascorbic, citric or gentisic acids), SnCl2 (in 1 M HCl), and 188Re eluate were added. The reaction mixture was allowed to react at different temperatures. Radiochemical yields of 188Re-ZA, 188ReO4- and reduced hydrolyzed rhenium were determined by TLC on silica gel in acetone and paper chromatography in saline.Biodistribution of 188Re-ZA was studied in rats with bone pathology.ResultsIt was found that the labelling yield of 188Re-ZA was 85 - 90 % in the pH range 1.0-2.0 at room temperature. The maximum labelling yields of 188Re-ZA in optimum conditions were 94.4 %, 95.3 % and more than 90 % using ascorbic, citric and gentisic acids, correspondently. ConclusionOptimum conditions for labeling ZA with carrier-free 188Re were: reaction volume 1.5-2.0 ml, pH 0.5-1.5, SnCl2 0.9-1.0 mg/ml, molar ratio [ZA]/[Sn] 2-3, concentration of gentisic acid 2.2- 2.6 mg/ml, reaction time 30 min at room temperature. The yield of labeling ZA with carrer-free 188Re was 88-91 % and about 94 % if carrier was added (0.02 mg Re/ml). Before intravenous injection pH of 188Re-ZA was adjusted with NaHCO3 solution 188Re-ZA showed moderate accumulation in the skeleton. CDU was 1,5-2,4.