Technetium-99m-labelled colchicine complex, preparation method thereof and purpose thereof

A technology of -99m, colchicine, applied in the field of radiopharmaceutical preparation and application, can solve the problem of no drug activity, etc., and achieve the effects of good water solubility, good tumor/muscle ratio, good tumor uptake and retention

Active Publication Date: 2016-06-01
INST OF HIGH ENERGY PHYSICS CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the ligands in the above-mentioned technetium complexes have no corresponding drug activity, and the targeting needs to be improved.

Method used

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  • Technetium-99m-labelled colchicine complex, preparation method thereof and purpose thereof
  • Technetium-99m-labelled colchicine complex, preparation method thereof and purpose thereof
  • Technetium-99m-labelled colchicine complex, preparation method thereof and purpose thereof

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Embodiment Construction

[0029] (1) Synthesis of DTPA-CHC ligand

[0030] Dissolve DTPA anhydride (35.7mg, 0.1mmol) and trimethylcolchicinic acid (34.3mg, 0.1mmol) in 1mL DMF, then add 20μL DIPEA, stir at room temperature for 1h; add 1mL water, shake well, filter, and the filtrate is purified by HPLC . HPLC purification method: Kromasil100-5C18 purification column (100 * 250mm), mobile phase is to contain 0.1% TFA (trifluoroacetic acid) water (A phase) and contain 0.1% TFA methanol (B phase), flow velocity 3mL / min; t= 0, A / B=6.5 / 3.5; t=15min, A / B=1 / 9; t=20min, A / B=1 / 9; t=25min, A / B=6.5 / 3.5. The fraction with a retention time of 11.35 min was collected and freeze-dried to obtain DTPA-CHC (48.1 mg, 67.0%) as a white powdery solid. ESI-MS: 719.26 (MH + ), 741.25 (M+Na + ).

[0031] Preparation of technetium-99m-labeled colchicine complex: Dissolve 1 mg DTPA-CHC ligand in 0.5 mL water, add 50 μL SnCl 2 Solution (1mg / mL, pH=1) and 0.1mL freshly rinsed sodium pertechnetate solution (3mCi), then add 0....

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Abstract

The invention discloses a technetium-99m-labelled colchicine complex, a preparation method thereof and a purpose thereof. The preparation method is characterized in that trimethyl colchicum acid and DTPA acid anhydride are subjected to coupling and hydrolysis to obtain a novel ligand DTPA-CHC, the ligand is subjected to <99m>Tc direct labeling under reducing action of stannous to obtain the technetium-99m-labelled colchicine complex, complex radiochemical purity is greater than 90%, the complex exists at room temperature for more than 6 h in a stable mode, and lipid-water partition coefficients determination shows that <99m>Tc-DTPA-CHC is a water-soluble compound. The technetium-99m-labelled colchicine complex has good tumor ingestion and detention effects, tumor / muscle ratio is high, tumor imaging is clear, and the technetium-99m-labelled colchicine complex can be used for SPECT imaging diagnosis for tumor.

Description

technical field [0001] The present invention relates to a compound labeled with radionuclide, and a preparation method and application of the compound, in particular to a technetium-99m-labeled colchicine complex, which belongs to the field of radiopharmaceutical preparation and application. Background technique [0002] Malignant tumor is one of the main diseases that lead to abnormal death of human beings. It has become the second cause of human death, second only to cardiovascular and cerebrovascular diseases, and has risen to the first place in some places, posing a huge threat to human beings. One of the most difficult diseases to deal with. [0003] Early diagnosis and treatment of cancer are crucial to improving the cure rate and quality of life of patients. The most important application value of radiopharmaceuticals is the study of physiological and chemical changes in the life process; PET or SPECT imaging using radionuclide-labeled biological functional molecules...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C233/32C07C231/02A61K51/04A61K103/10
Inventor 汪建军刘宇杨文江张延华薛井泉
Owner INST OF HIGH ENERGY PHYSICS CHINESE ACAD OF SCI
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