STABLE CONCENTRATED SOLUTIONS OF RADIONUCLIDE COMPLEXES Russian patent published in 2023 - IPC A61K51/08 A61K9/08 A61K103/30 

FIELD: pharmaceutics.

SUBSTANCE: present invention relates to an aqueous solution of a radiopharmaceutical product. The proposed solution contains: (a) complex formed with (ai) ¹⁷⁷Lu radionuclide (lutetium-177) and (aii) peptide binding to a somatostatin receptor, connected to DOTA chelate-forming agent, and (b) at least two different stabilizers preventing radiolitic decomposition, where the stabilizer preventing radiolitic decomposition is selected from gentisinic acid and ascorbic acid. At the same time, (bi) gentisinic acid is present at a concentration from 0.5 to 2 mg/ml, preferably from 0.5 to 1 mg/ml, and (bii) ascorbic acid is present at a concentration from 2.0 to 5.0 mg/ml. The specified radionuclide is present at such a concentration, which provides volumetric radioactivity from 250 to 500 MMC/ml. The aqueous solution of the pharmaceutical product contains less than 1% of ethanol. A method for the manufacture of an aqueous solution of a radiopharmaceutical product is also proposed.

EFFECT: invention allows for obtainment of a highly concentrated solution of a radionucleotide complex, which is very chemically and radio-chemically stable, even if it is stored at ambient temperatures or, for a short time, at elevated temperatures, so that it can be produced at an industrial scale and supplied in the form of a ready-to-use radiopharmaceutical product.

28 cl, 2 tbl, 3 ex