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A macromolecular imaging agent for lymph node inspection and preparation method thereof

An imaging agent and macromolecule technology, applied in the field of macromolecular imaging agent for lymph node examination and its preparation, can solve the problems of only one, affecting the stability and effect of the drug, and inhomogeneity, so as to improve the effectiveness, The effect of improving uniformity and increasing retention capacity

Inactive Publication Date: 2019-12-24
JIANGSU INST OF NUCLEAR MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Therefore, the technical problem to be solved by the present invention is to overcome the uncontrollability of the modifying groups in the lymph node imaging agent in the prior art, which leads to differences and inhomogeneities between molecules, and even there is only one kind on a certain molecule. group, thereby affecting the stability and effect of the drug, thereby providing a macromolecular imaging agent for lymph node inspection and its preparation method

Method used

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  • A macromolecular imaging agent for lymph node inspection and preparation method thereof
  • A macromolecular imaging agent for lymph node inspection and preparation method thereof
  • A macromolecular imaging agent for lymph node inspection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Embodiment 1 macromolecular compound imaging agent 1

[0053] (1) Gly-gly-gly connection:

[0054] In a 100ml round bottom flask add 5g dextran, 0.21g gly-gly-gly and 50ml DMSO. A drop of acetic acid was used as a catalyst and reacted at 80°C for two hours to obtain the first intermediate product. After cooling to room temperature, add 0.084g NaBH 4 and stir overnight. Then add 20ml deionized water and shake well. Finally, the mixed solution was first filtered with a 0.45 μm membrane, and then dialyzed with 10 times of deionized water. The molecular weight cut-off of the semipermeable membrane was 3000. Finally, the dialyzate was concentrated and freeze-dried to obtain the first product.

[0055] (2) Connection of Mannose: The connection of Mannose is divided into two steps.

[0056] The first step is the oxidation of the hydroxyl groups on the dextran backbone. Add 1 g of the gly-gly-gly connected product in the previous step, 7.06 g of Dess-Martin oxidant, and ...

Embodiment 2

[0067] Embodiment 2 macromolecular compound imaging agent 2

[0068] (1) Gly-gly-gly connection:

[0069] In a 100ml round bottom flask add 20g dextran, 1g gly-gly-gly and 50ml DMSO. 4 drops of acetic acid were used as a catalyst, and reacted at 80°C for two hours to obtain the first intermediate product. After cooling to room temperature, add 0.5 g NaBH 4 and stir overnight. Then add 80ml deionized water and shake well. Finally, the mixed solution was first filtered with a 0.45 μm membrane, and then dialyzed with 10 times of deionized water. The molecular weight cut-off of the semipermeable membrane was 3000. Finally, the dialyzate was concentrated and freeze-dried to obtain the first product.

[0070] (2) Connection of Mannose: The connection of Mannose is divided into two steps.

[0071] The first step is the oxidation of the hydroxyl groups on the dextran backbone. Add 1 g of the gly-gly-gly connected product in the previous step, 6.2 g of Dess-Martin oxidant, and 3...

Embodiment 3

[0081] Embodiment 3 macromolecular compound imaging agent 3

[0082] (1) Gly-gly-gly connection:

[0083] In a 100ml round bottom flask add 5g dextran, 0.21g gly-gly-gly and 50ml DMSO. A drop of acetic acid was used as a catalyst and reacted at 80°C for two hours to obtain the first intermediate product. After cooling to room temperature, add 0.084g NaBH 4 and stir overnight. Then add 20ml deionized water and shake well. Finally, the mixed solution was first filtered with a 0.45 μm membrane, and then dialyzed with 10 times of deionized water. The molecular weight cut-off of the semipermeable membrane was 3000. Finally, the dialyzate was concentrated and freeze-dried to obtain the first product.

[0084] (2) Connection of Mannose: The connection of Mannose is divided into two steps.

[0085]The first step is the oxidation of the hydroxyl groups on the dextran backbone. Add 1 g of the gly-gly-gly connected product in the previous step, 7.06 g of Dess-Martin oxidant, and 3...

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Abstract

The invention discloses a macromolecule developer for lymphonodus examination and a preparation method thereof, and belongs to the technical field of pharmaceutical synthesis. According to the developer disclosed by the invention, dextran is used as skeleton molecules, and the skeleton molecules are modified and connected with gly-gly-gly and mannose groups; a ratio of Gly-gly-gly to Mannose on the skeleton molecules is 1:2. According to the macromolecule developer for lymphonodus examination, which is disclosed by the invention, homogeneity of pharmaceutical molecules is improved, so that effectiveness of a medicine is improved.

Description

technical field [0001] The invention relates to the technical field of drug synthesis, in particular to a macromolecular imaging agent for lymph node inspection and a preparation method thereof. Background technique [0002] The changes of lymph nodes are closely related to the occurrence, development, diagnosis and treatment of many diseases, especially the observation of the diagnosis, metastasis and development of tumors. Lymph nodes are distributed throughout the body, and general examinations can only detect changes in superficial lymph nodes in various parts of the body. Therefore, lymph node imaging is of great significance for monitoring the discovery, development, and further diagnosis and treatment of diseases. [0003] In many studies, the selected radioactive imaging agents are almost all radioactive colloids ( 99m Tc-sulfur colloid or 99m Tc-human serum albumin, etc.), the particle size is not uniform, and the secondary lymphatic system is developed. In March...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K5/083C07K1/02A61K51/08A61K51/04A61K103/10
CPCA61K51/0491A61K51/088C07K5/0806
Inventor 王刚陈志明吴二明汪洋黄荷云徐越
Owner JIANGSU INST OF NUCLEAR MEDICINE
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