Development and Evaluation of User-Friendly Single Vial DOTA-Peptide Kit Formulations, Specifically Designed for Radiolabelling with Ga-68 from a Tin Dioxide Ge-68/Ga-68 Generator

作者：Prince Deidr^*; Rossouw Daniel; Davids Claudia; Rubow Sietske

来源：Molecular Imaging and Biology, 2017, 19(6): 817-824.

DOI：10.1007/s11307-017-1077-7

• DOTA-peptides
• Ga-68 eluate
• SnO2-based Ge-68/Ga-68 generator
• Radiolabelling efficiency
• Radiochemical yields
• Single vial kit

This study was aimed to develop single vial 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA)-peptide kits to be used with fractionated eluates from a SnO2-based Ge-68/Ga-68 generator.
Kits were formulated with 35 mu g DOTA-Tyr(3)-Thre(8)-octreotide, DOTA-[Tyr(3)]-octreotide and DOTA-[NaI3]-octreotide (DOTATATE, DOTATOC and DOTANOC) and sodium acetate powder, vacuum-dried and stored at -20 A degrees C for up to 12 months. Labelling of the kits was carried out with 2 ml Ga-68 eluate. Comparative labelling was carried out using aqueous DOTA-peptide stock solutions kept frozen at -20 A degrees C for up to 12 months.
The quality of the kits was found to be suitable over a 1-year storage period (pH, sterility, endotoxin content, radiolabelling efficiency and radiochemical yields of Ga-68-labelled DOTA-peptides). Radiochemical yields ranged from 73 to 83 %, while those obtained from stock solutions from 64 to 79 %. No significant decline in kit labelling yields was observed over a 12-month storage period.
The single vial kit formulations met the quality release specifications for human administration and appear to be highly advantageous over using peptide stock solutions in terms of stability and user-friendliness.

• 出版日期2017-12