Development and Evaluation of User-Friendly Single Vial DOTA-Peptide Kit Formulations, Specifically Designed for Radiolabelling with 68Ga from a Tin Dioxide 68Ge/68Ga Generator. 2017

Deidré Prince, and Daniel Rossouw, and Claudia Davids, and Sietske Rubow
Radionuclide Production Department, iThemba LABS, PO Box 722, Somerset West, 7129, South Africa. deidre@tlabs.ac.za.

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 68Ge/68Ga generator. Kits were formulated with 35 μg DOTA-Tyr3-Thre8-octreotide, DOTA-[Tyr3]-octreotide and DOTA-[NaI3]-octreotide (DOTATATE, DOTATOC and DOTANOC) and sodium acetate powder, vacuum-dried and stored at -20 °C for up to 12 months. Labelling of the kits was carried out with 2 ml 68Ga eluate. Comparative labelling was carried out using aqueous DOTA-peptide stock solutions kept frozen at -20 °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 68Ga-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.

UI MeSH Term Description Entries
D009942 Organometallic Compounds A class of compounds of the type R-M, where a C atom is joined directly to any other element except H, C, N, O, F, Cl, Br, I, or At. (Grant & Hackh's Chemical Dictionary, 5th ed) Metallo-Organic Compound,Metallo-Organic Compounds,Metalloorganic Compound,Organometallic Compound,Metalloorganic Compounds,Compound, Metallo-Organic,Compound, Metalloorganic,Compound, Organometallic,Compounds, Metallo-Organic,Compounds, Metalloorganic,Compounds, Organometallic,Metallo Organic Compound,Metallo Organic Compounds
D011933 Reagent Kits, Diagnostic Commercially prepared reagent sets, with accessory devices, containing all of the major components and literature necessary to perform one or more designated diagnostic tests or procedures. They may be for laboratory or personal use. Diagnostic Reagent Kits,Diagnostic Reagents and Test Kits,Diagnostic Test Kits,In Vitro Diagnostic Device,In Vitro Diagnostic Devices,In Vitro Diagnostic Medical Device,In Vitro Diagnostic Medical Devices,Kits, Diagnostic Reagent,Diagnostic Reagent Kit,Diagnostic Test Kit,Kit, Diagnostic Reagent,Kit, Diagnostic Test,Kits, Diagnostic Test,Reagent Kit, Diagnostic,Test Kit, Diagnostic,Test Kits, Diagnostic
D002851 Chromatography, High Pressure Liquid Liquid chromatographic techniques which feature high inlet pressures, high sensitivity, and high speed. Chromatography, High Performance Liquid,Chromatography, High Speed Liquid,Chromatography, Liquid, High Pressure,HPLC,High Performance Liquid Chromatography,High-Performance Liquid Chromatography,UPLC,Ultra Performance Liquid Chromatography,Chromatography, High-Performance Liquid,High-Performance Liquid Chromatographies,Liquid Chromatography, High-Performance
D005857 Germanium A rare metal element with a blue-gray appearance and atomic symbol Ge, atomic number 32, and atomic weight 72.63.
D006863 Hydrogen-Ion Concentration The normality of a solution with respect to HYDROGEN ions; H+. It is related to acidity measurements in most cases by pH pH,Concentration, Hydrogen-Ion,Concentrations, Hydrogen-Ion,Hydrogen Ion Concentration,Hydrogen-Ion Concentrations
D015282 Octreotide A potent, long-acting synthetic SOMATOSTATIN octapeptide analog that inhibits secretion of GROWTH HORMONE and is used to treat hormone-secreting tumors; DIABETES MELLITUS; HYPOTENSION, ORTHOSTATIC; HYPERINSULINISM; hypergastrinemia; and small bowel fistula. Octreotide Acetate,Compound 201-995,Octreotide Acetate Salt,SAN 201-995,SM 201-995,SMS 201-995,Sandostatin,Sandostatine,Sandoz 201-995,Compound 201 995,Compound 201995,SAN 201 995,SAN 201995,SM 201 995,SM 201995,SMS 201 995,SMS 201995,Sandoz 201 995,Sandoz 201995
D017971 Tin Compounds Inorganic compounds that contain tin as an integral part of the molecule. Compounds, Tin
D019275 Radiopharmaceuticals Compounds that are used in medicine as sources of radiation for radiotherapy and for diagnostic purposes. They have numerous uses in research and industry. (Martindale, The Extra Pharmacopoeia, 30th ed, p1161) Radiopharmaceutical

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