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A hyperbranched polymer, and a preparing method and applications thereof

A technology of hyperbranched polymers and gadolinium compounds, which can be used in pharmaceutical formulations, preparations for in vivo tests, MRI/MRI contrast agents, etc., can solve the problems of limited application, incomplete excretion, etc. Low toxicity, simple preparation method, and the effect of improving relaxation efficiency

Inactive Publication Date: 2017-11-17
SUZHOU INST OF NANO TECH & NANO BIONICS CHINESE ACEDEMY OF SCI
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Problems solved by technology

However, most synthetic polymers are excreted slowly or incompletely in the body, which limits their clinical application

Method used

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  • A hyperbranched polymer, and a preparing method and applications thereof
  • A hyperbranched polymer, and a preparing method and applications thereof
  • A hyperbranched polymer, and a preparing method and applications thereof

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Embodiment Construction

[0032] Below, the embodiments of the present invention will be described in detail with reference to the accompanying drawings.

[0033] The present invention provides a kind of preparation method of the MRI contrast agent of hyperbranched polylysine as carrier, comprises the following steps:

[0034] Step 1: After fully grinding lysine hydrochloride and potassium hydroxide into a slurry in a mortar, use liquid paraffin oil as a heat transfer medium, and react at 150°C for 48 hours under a nitrogen protective atmosphere to obtain the main product overrun Polylysine backbone, as well as by-products and other impurities.

[0035] Wherein, the charging amount of described potassium hydroxide is 90% of the molar number of lysine hydrochloride.

[0036] Slowly cool to room temperature after the reaction in step 1 is completed. The liquid paraffin was poured off, washed repeatedly with petroleum ether, and then the petroleum ether was distilled off under reduced pressure to obtain...

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Abstract

The invention relates to the technical field of preparing a contrast agent by utilizing a hyperbranched polymer. A preparing method of the hyperbranched polymer includes reacting a lysine salt and caustic alkali in a mole ratio of 100:80-90 at 140-160 DEG C for 40-50 h in a protective atmosphere; mixing a hyperbranched polylysine skeleton and diethylenetriaminepentaacetic acid according to a mass ratio of at least 1:5 in water; reacting the mixture at room temperature for 6-8 h; mixing the first hyperbranched polylysine molecule and a gadolinium compound in water; reacting the mixture at 37-42 DEG C for 6-12 h, with the mass ratio of the first hyperbranched polylysine molecule to the gadolinium compound being 1:1-1:2; and mixing and reacting the second hyperbranched polylysine molecule and folic acid in a carbonate the pH value of which is 8-10 for 5-12 h. The hyperbranched polylysine contrast agent has good biocompatibility, low toxicity and a high relaxation rate and can be metabolized in vivo.

Description

technical field [0001] The invention relates to the technical field of preparation of medicines, in particular to a contrast agent for magnetic resonance imaging, its preparation method and application. Background technique [0002] With the development of science and technology, magnetic resonance imaging has become an effective means of clinical detection of diseases. Compared with other clinical imaging techniques, magnetic resonance imaging has many advantages in revealing anatomical structures, especially in detecting inflammatory tissues and solid tumors. In addition, magnetic resonance imaging also has no ionizing radiation damage, and multi-parameter imaging provides doctors with a large amount of diagnostic information and three-dimensional positioning capabilities. However, in order to further improve the sensitivity and accuracy of imaging, contrast agents are usually required to enhance the imaging contrast. [0003] At present, the clinical contrast agent is g...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K49/12C08G69/10A61K49/14A61K49/08
CPCA61K49/085A61K49/124A61K49/146C08G69/10
Inventor 裴仁军刘敏祖广月
Owner SUZHOU INST OF NANO TECH & NANO BIONICS CHINESE ACEDEMY OF SCI
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