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Paramagnetic metal complex modified by aspartic acid-phenylalanine copolymer and its preparation method and application

A technology of phenylalanine copolymer and aspartic acid, which can be used in preparations and pharmaceutical formulations for in vivo experiments, can solve the problems of low biodegradability, liver targeting and low immunity, and achieve imaging time. Long, good water solubility, good imaging effect

Inactive Publication Date: 2017-01-04
CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The present invention aims to solve the technical problems of low biodegradability, low liver targeting and immunity in the prior art, and provides a modified aspartic acid-phenylalanine copolymer Paramagnetic metal complexes and their preparation methods and applications

Method used

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  • Paramagnetic metal complex modified by aspartic acid-phenylalanine copolymer and its preparation method and application
  • Paramagnetic metal complex modified by aspartic acid-phenylalanine copolymer and its preparation method and application
  • Paramagnetic metal complex modified by aspartic acid-phenylalanine copolymer and its preparation method and application

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Embodiment 1

[0045] Preparation of aspartic acid-phenylalanine copolymer via 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetate gadolinium complex modified by ethylenediamine

[0046] (1) Mix 20 grams of L-aspartic acid with 10 grams of L-phenylalanine, add 10 grams of the mass fraction of the mixed mixture into 85% phosphoric acid solution and stir evenly. (24mmHg) for 5 hours, the reaction temperature was controlled at 165°C, precipitated with deionized water, filtered, washed, and dried under reduced pressure to obtain an aspartic acid-phenylalanine copolymer;

[0047] (2) Dissolve the aspartic acid-phenylalanine copolymer synthesized in (1) in N,N-dimethylformamide solution at room temperature, and add ethylenediamine and ethylenediamine dropwise while stirring. The mass ratio of amine to aspartic acid-phenylalanine copolymer was 2.8:1, stirred at room temperature for 4 hours, precipitated with ether, filtered, dialyzed, and freeze-dried to obtain aminated aspartic acid-phenylalanine...

Embodiment 2

[0051] Preparation of aspartic acid-phenylalanine copolymer via 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetate gadolinium complex modified by ethylenediamine

[0052] (1) Mix 20 grams of L-aspartic acid with 20 grams of L-phenylalanine, add 15 grams of the mass fraction of the mixed mixture into 85% phosphoric acid solution and stir evenly. (30mmHg) for 5 hours, the reaction temperature was controlled at 165°C, precipitated with deionized water, filtered, washed, and dried under reduced pressure to obtain an aspartic acid-phenylalanine copolymer;

[0053] (2) Dissolve the aspartic acid-phenylalanine copolymer synthesized in (1) in N,N-dimethylformamide solution at room temperature, and add ethylenediamine and ethylenediamine dropwise while stirring. The mass ratio of amine to aspartic acid-phenylalanine copolymer was 2.8:1, stirred at room temperature for 4 hours, precipitated with ether, filtered, dialyzed, and freeze-dried to obtain aminated aspartic acid-phenylalanine...

Embodiment 3

[0057] Preparation of aspartic acid-phenylalanine copolymer via 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetate gadolinium complex modified by ethylenediamine

[0058] (1) Mix 20 grams of L-aspartic acid with 20 grams of L-phenylalanine, add 15 grams of the mass fraction of the mixed mixture into 85% phosphoric acid solution and stir evenly. (200mmHg) for 5 hours, the reaction temperature was controlled at 100°C, precipitated with deionized water, filtered, washed, and dried under reduced pressure to obtain an aspartic acid-phenylalanine copolymer;

[0059] (2) Dissolve the aspartic acid-phenylalanine copolymer synthesized in (1) in N,N-dimethylformamide solution at room temperature, and add ethylenediamine and ethylenediamine dropwise while stirring. The mass ratio of amine to aspartic acid-phenylalanine copolymer was 2.8:1, stirred at room temperature for 4 hours, precipitated with ether, filtered, dialyzed, and freeze-dried to obtain aminated aspartic acid-phenylalanin...

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Abstract

The invention relates to a paramagnetic metal complex modified by asparaginic acid-phenylalanine copolymer, a preparation method and application of the paramagnetic metal complex, aiming to solve the technical problems that an existing liver macromolecular contrast agent has the defects of low biodegradability, relatively low liver target performance, low immunity and the like. The paramagnetic metal complex modified by the asparaginic acid-phenylalanine copolymer is prepared by using the asparaginic acid-phenylalanine copolymer as a carrier and an annular 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacethyl ligand which is connected to the side chain of the carrier. Corresponding characteristics of a polyaminopolycarboxylate complex are maintained in a magnetic resonance imaging contrast agent prepared from the paramagnetic metal complex modified by the asparaginic acid-phenylalanine copolymer, and thus the magnetic resonance imaging contrast agent has excellent stability, water solubility and relaxation rate and has targeting performance on liver, so that target imaging is realized, and the imaging contrast ratio and resolution can be increased. The paramagnetic metal complex modified by the asparaginic acid-phenylalanine copolymer has an excellent effect for improving the early diagnosis level of liver diseases.

Description

technical field [0001] The invention relates to a magnetic resonance imaging contrast agent, in particular to a paramagnetic metal complex modified by aspartic acid-phenylalanine copolymer and its preparation method and application. Background technique [0002] In order to improve the signal contrast between lesion and normal tissue, about 45% of MRI diagnosis requires the use of contrast agent. At present, MRI contrast agents commonly used in clinical practice, such as Dotarem (Gd-DOTA), have a short retention time in the body, poor imaging effect, and no tissue or organ selectivity. At present, one of the important research directions of MRI contrast agents in the world is the polymerization of contrast agents and the targeting of organs and tissues. Among them, the organ-targeted contrast agent can enrich the contrast agent in a specific organ or tissue, prolong the contrast time, thereby realizing targeted imaging, improving imaging contrast and definition, and reducin...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K49/12
Inventor 李晓晶肖研薛蓉湛游洋齐晨丽裴奉奎
Owner CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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