Formulation and evaluation of a two-components lyophilized kit for Tc-sestamibi: Transchelation preparation of Tc-99m-sestamibi

Abstract The preparation of a single-component kit for 99m Tc-MIBI requires stringent control of lyophilization conditions. Hence, a two-components kit formulation, lyophilized under normal conditions, was standardized. The ligand was kept separate from the reductant stannous tin (preserved as stannous glucoheptonate) and advantage was taken of transchelation method, of Tc-GHA and Cu(I)-MIBI, for formation of Tc-MIBI. The product obtained was comparable in radiochemical purity (95 ± 2%), in heart uptake (2% injected dose) in rats and in blood clearance in rabbots, to that of the single-component kit/commercial product. Good-quality heart images in dog and monkey were also obtained.