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Technetium-99m labelled Melphalan complex as well as preparation method and application thereof

A -99m, complex technology, applied in the field of radiopharmaceutical preparation and application, can solve the problem of no drug activity, etc., and achieve the effects of easy availability of raw materials, low cost, and good tumor/muscle ratio

Active Publication Date: 2016-08-24
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 Melphalan complex as well as preparation method and application thereof
  • Technetium-99m labelled Melphalan complex as well as preparation method and application thereof
  • Technetium-99m labelled Melphalan complex as well as preparation method and application thereof

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Experimental program
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Embodiment Construction

[0031] (1) Synthesis of DTPA-MFL ligand

[0032] DTPA anhydride (35.7 mg, 0.1 mmol) and melphalan (30.4 mg, 0.1 mmol) were dissolved in 1 mL of DMF, then 20 μL of DIPEA was added, and stirred at room temperature for 1 h; 1 mL of water was added, shaken, filtered, and the filtrate was purified by HPLC. HPLC purification method: Kromasil 100-5C18 purification column (100 × 250mm), the mobile phase is water (phase A) containing 0.1% TFA (trifluoroacetic acid) and methanol (phase B) containing 0.1% TFA, and the flow rate is 3mL / min; =0, A / B=5 / 5; t=15min, A / B=1 / 9; t=20min, A / B=1 / 9; t=25min, A / B=5 / 5. The fraction with a retention time of 10.3 min was collected and freeze-dried to obtain DTPA-MFL (36.2 mg, 53.2%) as a white powdery solid. ESI-MS: 680.21 (MH + ).

[0033] Preparation of technetium-99m-labeled melphalan complex:

[0034] Dissolve 1 mg of DTPA-MFL ligand in 0.5 mL of water, add 50 μL of SnCl in sequence 2 Solution (1mg / mL, pH=1) and 0.1mL freshly rinsed sodium pert...

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Abstract

The invention discloses a technetium-99m labelled Melphalan complex as well as a preparation method and application thereof. The preparation method is characterized by coupling and hydrolyzing Melphalan and DTPA (diethylenetriaminepentaacetic acid) anhydride to obtain a novel ligand DTPA-MFL, and then carrying out <99m>Tc direct labelling on the ligand under the stannous reducing action, thus obtaining the technetium-99m labelled Melphalan complex. The Melphalan complex has the beneficial effects that the radiochemical purity of the complex is more than 90%; the complex can stably exist at room temperature for more than 6 hours; and water partition coefficient determination indicates that the complex is a water-soluble compound. The technetium-99m labelled Melphalan complex has good tumor uptake and retention and tumor / muscle ratio, is clearer in tumor imaging and can be used for SPECT (single-photon emission computed tomography) imaging diagnosis of tumors.

Description

technical field [0001] The invention relates to a compound labeled with radionuclides, a preparation method and application of the compound, specifically relates to a technetium-99m labeled melphalan complex, and belongs to the field of preparation and application of radiopharmaceuticals. 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 ca...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C237/12C07C231/02C07F13/00A61K51/04A61K103/10
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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