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Preparation method and application of pyridazinone myocardial perfusion PET radiopharmaceutical

A technology of radiopharmaceuticals and myocardial perfusion, which is applied in the direction of radioactive preparations, radioactive carriers, and pharmaceutical formulations in vivo, and can solve the problems of unclear process flow, unclear applicability of large-scale activity production, and low demand for Fmpp2 activity.

Active Publication Date: 2021-05-18
BEIJING SINOTAU INT PHARMA TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0010] 1. There are a lot of uncertain parameters in the route and the process flow is not clear enough
[0011] 2. Animal experiments[ 18 F] The activity requirement of Fmpp2 is low, and the applicability of this method for large-scale activity production is unclear
[0012] 3. This method cannot be produced automatically
The existing process cannot meet the activity requirement

Method used

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  • Preparation method and application of pyridazinone myocardial perfusion PET radiopharmaceutical
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  • Preparation method and application of pyridazinone myocardial perfusion PET radiopharmaceutical

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Embodiment 1

[0040] The automatic equipment selects the equipment of model AllinOne of Trasis Company. The power unit of the equipment is high-purity nitrogen and injector electric rotor, which can provide a vacuum system and is equipped with an HPLC purification system. Because this process uses automation equipment, the automation equipment is placed in a radiation shielding box, which can protect the operator from radiation damage and increase the operating dose. At the same time, due to the control of the computer, the control of the process steps can be more precise and repeatable. Reduce human bias.

[0041] 1) The existing technology generally adopts 10-50mCi 18 F initial dose, the present embodiment adopts large dose initial 18 F, the preferred initial activity is 800-1000mCi.

[0042] 2) Enrichment 18 F ion anion exchange column choose Waters brand QMA column, QMA column preferably 1mol / L NaHCO 3 activation.

[0043] 3) Using cryptane K 222 with K 2 CO 3 solution rinse, e...

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Abstract

The invention discloses a preparation method and application of a pyridazinone myocardial perfusion PET radiopharmaceutical. According to the invention, a large-dose initial 18F activity label is adopted, the precursor usage amount of a reaction, the reaction temperature and the purification HPLC condition are optimized, the reaction yield is improved, the preparation amount of [18F]Fmpp2 can reach 200 mCi, the chemical impurity amount is reduced, the radiochemical purity is high, and the key quality index is kept stable within 6 hours. A method for preparing a [18F]Fmpp2 solution for injection is improved, and the radiochemical purity and stability of the [18F]Fmpp2 are improved. The [18F]Fmpp2 prepared by the invention is subjected to miniature pig myocardial model PET imaging display; after the [18F]Fmpp2 is intravenously injected, the myocardial radioactive uptake is high, and the influence of peripheral organs on myocardial development is small; and normal myocardium, ischemic myocardium caused by chronic coronary artery stenosis and infarcted myocardium caused by acute coronary artery stenosis can be distinguished.

Description

technical field [0001] The invention belongs to the technical field of chemical pharmacy, and in particular relates to a preparation method and application of pyridazinone myocardial perfusion PET radiopharmaceuticals. Background technique [0002] Radionuclide myocardial perfusion imaging has become the mainstay of stress imaging in the evaluation of patients with suspected or known coronary artery disease (CAD). PET myocardial perfusion imaging can absolutely quantitatively measure myocardial blood flow and blood flow reserve function, and can diagnose coronary heart disease early. It has absolute advantages for patients with microvascular diseases, patients with balanced three-vessel disease, and obese patients. [0003] [ 18 F] Fmpp2, chemical name 2-tert-butyl-4-chloro-5-((3-((4-((2-(2-fluoro[ 18 F] Ethoxy)ethoxy)methyl)-1H-1,2,3-triazol-1-yl)methyl)benzyl)oxy)pyridazin-3(2H)-one. Chemical Structure: [0004] [0005] Molecular formula: C 23 h 29 Cl 18 FN 5 o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K47/10A61K51/04A61P9/10C07D403/12A61K101/02
CPCA61K51/0459A61K47/10A61K9/08A61K9/0019A61P9/10C07D403/12C07B2200/05
Inventor 王跃徐新盛
Owner BEIJING SINOTAU INT PHARMA TECH CO LTD
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