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A specific targeting radionuclide marker and its preparation method and application

A technology of radionuclides and markers, which is applied in the field of specific targeting radionuclide markers and their preparation, can solve the problems of restricting the dose and effect of radiotherapy, non-specific systemic distribution, and destroying normal cells, etc., and achieve good clinical results. Application prospects, reduced side effects, good biocompatibility

Active Publication Date: 2021-06-29
王艳丽
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  • Abstract
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Problems solved by technology

However, radiotherapy has many disadvantages, such as rapid excretion of radionuclides after intravenous administration, nonspecific systemic distribution, and relatively low tumor uptake
In addition, low doses of radionuclides have certain lethality to tumors, but may make cancer cells resistant to radiation therapy, while high doses of radionuclides can damage normal cells and cause serious side effects, such as dysfunction and Imbalance, lack of energy, loss of appetite, weakness and fatigue, nausea and vomiting, fullness after eating, etc., and can cause skin and mucous membrane lesions
These severe side effects limit the dose and effect of radiotherapy

Method used

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  • A specific targeting radionuclide marker and its preparation method and application
  • A specific targeting radionuclide marker and its preparation method and application
  • A specific targeting radionuclide marker and its preparation method and application

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preparation example Construction

[0049] The present invention provides a method for preparing a specific targeting radionuclide marker described in the above technical scheme, comprising the following steps:

[0050] When the radionuclide is the first radionuclide, the PBS buffer solution of the linking reagent is mixed with the solution of the first radionuclide, and the first reaction is carried out under the action of an oxidizing agent to obtain the first reaction solution; The I reaction solution is mixed with the graphene-based tumor cell nucleus targeting fluorescent nanoprobe solution, and the second reaction is carried out to obtain specific targeting radionuclide markers;

[0051] When the radionuclide is the second radionuclide, the solution of the linking reagent is mixed with the PBS buffer solution of the graphene-based tumor cell nucleus targeting fluorescent nanoprobe, and the third reaction is carried out to obtain the third reaction solution; The third reaction solution is mixed with the sec...

Embodiment 1

[0075] Specific targeting radionuclide marker GTTN-BH- 131 The preparation of I, reaction route is shown in formula A and formula B:

[0076]

[0077]

[0078] Take 10 μL of BH reagent aqueous solution with a concentration of 10 mg / mL, dilute it to 100 μL with PBS buffer (pH 7.4), add it to the lodogen tube, add Na 131 I aqueous solution ( 131 I radioactivity is 1mCi), shake reaction 15min under room temperature (25 ℃) condition; The reaction system in the described lodogen tube is transferred in the centrifuge tube, add 1mL concentration and be the GTTN aqueous solution of 2mg / mL, pH value 8.3, Oscillating reaction at room temperature for 1 h; using a concentration of 0.9 wt% NaCl solution to rinse the G25 Sephadex chromatographic column for 3 times, and then adding the system (yellow) obtained after the above reaction to the G25 Sephadex chromatographic column ( Chromatographic column for short), use a 10mL centrifuge tube to collect the effluent from the lower end o...

Embodiment 2

[0085] Specific Targeting Radionuclide Labels 68 The preparation of Ga-DOTA-GTTN, the reaction route is shown in formula C and formula D:

[0086]

[0087] Mix 1 mL of GTTN PBS buffer (pH 8.7) with a concentration of 2 mg / mL and 1 mL of DOTA aqueous solution with a concentration of 1 mg / mL, stir and react for 2 h at room temperature, and add 68 GaCl 3 aqueous solution, so that the system 68 The Ga activity was 1mCi, the pH value was 5.0, and the reaction was stirred at room temperature for 10 minutes; the G25 Sephadex chromatographic column was rinsed with 0.9wt% NaCl solution for 3 times, and then the system obtained after the above reaction (in the form of Yellow) into G25 Sephadex chromatographic column (chromatographic column for short), use a 10mL centrifuge tube to collect the effluent from the lower end of the chromatographic column, and when the yellow system reaches the lower end of the chromatographic column, use a 1.5mL centrifuge tube to collect the effluent ...

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Abstract

The invention provides a specific targeting radionuclide marker and its preparation method and application, belonging to the technical field of nanomedicine and molecular imaging. In the present invention, the graphene-based tumor cell nucleus-targeting fluorescent nanoprobe (GTTN) is used as the nucleus-targeting molecular label radionuclide, and the obtained label can be directly used in single photon emission computed tomography (SPECT) and positron Emitting computed tomography (PET), and radionuclide therapy can be performed; in addition, the marker can be highly targeted to the tumor area by using GTTN's cell membrane permeability targeting mechanism, and can also be used by GTTN's fluorescence imaging and radioactive The SPECT or PET imaging of radionuclides can realize dual-mode imaging, achieve the effect of accurate diagnosis and treatment, and at the same time minimize the side effects of radionuclides on normal tissues, which has a good clinical application prospect.

Description

technical field [0001] The invention relates to the technical fields of nanomedicine and molecular imaging, in particular to a specific targeting radionuclide marker and its preparation method and application. Background technique [0002] The role and status of radiotherapy in tumor treatment are becoming more and more prominent, and it has become one of the main means of treating malignant tumors. Radionuclides used in radiotherapy can be used not only as radiopharmaceuticals in tumor therapy, but also as radioactive probes for tumor imaging. However, radiotherapy has many disadvantages, such as rapid excretion of radionuclides after intravenous administration, nonspecific systemic distribution, and relatively low tumor uptake. In addition, low doses of radionuclides have certain lethality to tumors, but may make cancer cells resistant to radiation therapy, while high doses of radionuclides can damage normal cells and cause serious side effects, such as dysfunction and I...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K51/02A61K49/00A61P35/00A61K101/02A61K103/34
CPCA61K49/0019A61K51/02A61P35/00
Inventor 王艳丽张建章俊峰李晨晨尹晓凤尹雪莲薛强华
Owner 王艳丽
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