METHOD OF OBTAINING THE TECHNETIUM-99m COMPLEX WITH OCTREOTIDE FOR DIAGNOSING OF NEUROENDOCRINE TUMORS Russian patent published in 2018 - IPC C07K7/06 C07F13/00 A61K51/08 A61K103/10 

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to pharmaceutical chemistry, namely to a process for the preparation of a technetium-99m complex with octreotide, which is used to diagnose neuroendocrine tumors. Method involves use of octreotide modified with a chelating agent, addition of tin(II) dichloride dihydrate, coupling of the obtained reagent with technetium-99m. Octreotide is modified with chelating agent succinimid-1-yl-6-(bis(pyridin-2-ylmethyl)amino)hexanoate in dimethylformamide in the presence of triethylamine at room temperature for at least 24 hours with stirring. Resulting solution is purified semi-preparatively using liquid chromatography, distillation of volatile solvents and drying are carried out by lyophilization. To octreotide modified with a chelating agent, sodium citrate and tin(II) citrate dichloride dihydrate are added, mixed, a liquid reagent is obtained which is sterilized by filtration and lyophilized with pre-freezing to -50 °C, and then pertechnetate with a concentration of technetium-99m 1 GBq/ml is added to the sodium lyophilizate obtained and incubated for at least 30 minutes at room temperature.

EFFECT: invention allows to increase the radiochemical purity and yield of the technetium-99m complex with octreotide.

1 cl, 2 ex