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Developing agent for detecting glioma as well as preparation method and application thereof

An imaging agent and glioma technology, applied in the field of imaging medicine, can solve problems such as low resolution of SPECT imaging images, inability to diagnose and grade gliomas, difficulty in displaying early small tumors, etc., and achieve high-resolution imaging. image, high sensitivity, and high-resolution imaging

Pending Publication Date: 2021-07-23
THE FIRST AFFILIATED HOSPITAL OF SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The problem with cranial magnetic resonance examination is that it cannot diagnose and grade glioma well
Specifically: For the convenience of image analysis of glioma, a weighted image appears. A weighted image is an image that determines the grayscale of a brain MRI image through a specific imaging parameter. Cranial MRI The examination shows the glioma in the brain through the weighted image, but the weighted image can only reflect the degree of damage to the blood-brain barrier of the brain glioma, but cannot accurately show the boundary of the brain glioma
[0004] There are two problems with SPECT imaging. One is that SPECT imaging uses planar imaging, and there is a phenomenon of radioactive superimposition. The second is that the image resolution of SPECT imaging is low, and it is difficult to display early small tumors (<2.5cm)

Method used

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  • Developing agent for detecting glioma as well as preparation method and application thereof
  • Developing agent for detecting glioma as well as preparation method and application thereof
  • Developing agent for detecting glioma as well as preparation method and application thereof

Examples

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Effect test

preparation example Construction

[0039] Main experimental instruments and experimental materials in the preparation method of the imaging agent of the embodiment of the present invention include:

[0040] The SEP-PAK light QMA column is a solid phase extraction column produced by Waters Corporation of the United States;

[0041] Amino polyether, the English name is Kryptofix222 (abbreviated as K 222 ), produced by ABX Company of Germany;

[0042] HLB is a hydrophilic-lipophilic balanced adsorbent, which is a modified styrene divinylbenzene copolymer;

[0043] 0.01M PBS (PH=7.4), produced by Guangzhou Zhanchen Biotechnology Co., Ltd.;

[0044] Anhydrous acetonitrile (MeCN), produced by U.S. Sigma-Aldrich company;

[0045] Chlorotoxin (Chlorotoxin), produced by Japan Peptide Institute, Inc.;

[0046] Sep-Pak C18 column, produced by American Waters Company;

[0047] Fluorine multi-functional chemical synthesis module (PET-MF-2V-IT-I), produced by Beijing Petrochemical Co., Ltd.;

[0048] Inveon Micro PET-C...

Embodiment 1

[0060] The imaging agent used to detect glioma in this embodiment is 68Ga -Fluorobenzoic acid-chlorotoxin, English as 68Ga -FP-Chlorotoxin, its structural formula is:

[0061]

[0062] Wherein, L is the amino acid sequence shown in SEQ ID NO:1.

[0063] The preparation method of the imaging agent used to detect glioma in this embodiment comprises the following steps:

[0064] (1) Synthesis of 68Ga-N-succinimide 4-[68Ga]fluorobenzoic acid;

[0065] (2) 68Ga -N-succinimide 4-[ 68Ga ] coupling reaction of fluorobenzoic acid and chlorotoxin;

[0066] Wherein, step (1) comprises the following steps in order:

[0067] (A) Preparation 68Ga- : passed by the cyclotron 18 O(p,n) 68Ga nuclear reaction 68Ga -F - , under He gas transmission, through the SEP-PAK light QMA column placed in the radioactive detector, 68Ga- Trapped on the SEP-PAK light QMA column;

[0068] (B) Preparation [K / K 222 ] 68Ga- : Under the action of vacuum pump, use 1mL of K 222 (Amino polyether) s...

Embodiment 2

[0076] The imaging agent used in this embodiment to detect glioma is the same as that in Embodiment 1.

[0077] The preparation method of the imaging agent used to detect glioma in this embodiment comprises the following steps:

[0078] (1) Synthesis of 68Ga-N-succinimide 4-[68Ga]fluorobenzoic acid;

[0079] (2) 68Ga -N-succinimide 4-[ 68Ga ] coupling reaction of fluorobenzoic acid and chlorotoxin;

[0080] Wherein, step (1) comprises the following steps in order:

[0081] (A) Preparation 68Ga- : passed by the cyclotron 18 O(p,n) 68Ga nuclear reaction 68Ga -F - , under He gas transmission, through the SEP-PAK light QMA column placed in the radioactive detector, 68Ga- Trapped on the SEP-PAK light QMA column;

[0082] (B) Preparation [K / K 222 ] 68Ga- : Under the action of vacuum pump, use 1mL of K 222 (Amino polyether) solution will 68Ga- Rinse to form a mixed solution in the first reaction bottle, pass nitrogen gas (100ml / min) into the first reaction bottle, heat ...

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Abstract

The invention relates to the technical field of imaging medicine, in particular to a developing agent for detecting glioma as well as a preparation method and application thereof. The developing agent is 68Ga-fluorobenzoic acid-chlorotoxin. The developing agent disclosed by the invention has the following advantages: (1) the boundary of glioma can be accurately defined; (2) the sensitivity is high: the chlorotoxin marked by 68Ga can be detected through PET imaging, the focus of 6 mm can be detected by PET, and the resolution is far higher than that of SPECT; (3) a brand-new direction is provided for diagnosis of glioma, and important clinical value is achieved in the aspects of early diagnosis of glioma, definition of the boundary of the glioma, curative effect evaluation, delivery of targeted drugs and the like; and (4) the developing agent can be applied to PET, the boundary of glioma can be accurately defined, high-resolution imaging can be realized, a focus of 6mm can be detected, and the resolution of the developing agent is far higher than that of SPECT in the prior art.

Description

technical field [0001] The invention relates to the technical field of imaging medicine, in particular to an imaging agent for detecting glioma and its preparation method and application. Background technique [0002] Glioma is a tumor derived from the neuroectoderm, accounting for 40-50% of brain tumors, and is the most common intracranial malignant tumor. The most commonly used methods for non-invasive diagnosis of glioma in clinical practice are cranial magnetic resonance examination and SPECT imaging. [0003] The problem with cranial MRI is that it cannot diagnose and grade glioma well. Specifically: For the convenience of image analysis of glioma, a weighted image appears. A weighted image is an image that determines the grayscale of a brain MRI image through a specific imaging parameter. Cranial MRI The examination shows the glioma in the brain through the weighted image, but the weighted image can only reflect the degree of damage to the blood-brain barrier of the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K51/08C07K14/00C07K1/16C07K1/13
CPCA61K51/08C07K14/00
Inventor 初建平
Owner THE FIRST AFFILIATED HOSPITAL OF SUN YAT SEN UNIV
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