HYNIC-TOC LABELLED WITH ~(99m)Tc VIA AN INSTANT KIT FORMULATION: PRECLINICAL RESULTS

摘要

The aim of this work was the development of an instant kit formulation based on a ~(99m)Tc labelling of HYNIC-TOC using a coligand exchange from tricine to EDDA. The preparation of the labelled conjugate was achieved at elevated temperature and under optimized conditions of pH, EDDA and stannous ion concentrations. Quality control tests were carried out to evaluate different parameters such as radiochemical purity, dissolution time, pH, stability of the kits during storage at 4°C, sterility, apyrogenecity and internalization in AR42J cells. ~(99m)Tc-EDDA/HYNIC-TOC was obtained with high radiochemical purity (>95%) and retained biological activity after it was prepared by addition of 0.2M Na_2HPO_4 to a kit, followed by 1.1GBq ~(99m)Tc pertechnetate and stored for a period of up to six months.