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Gadolinium-containing magnetic resonance contrast agent and preparation method thereof

A magnetic resonance contrast agent and chelate technology, which can be used in pharmaceutical formulations, preparations for in vivo tests, and emulsion delivery, etc., can solve problems such as the limitation of nanoparticle drug loading, and achieve improved MRI contrast and cytotoxic side effects. Small, good sustained-release effect

Inactive Publication Date: 2011-02-23
EAST CHINA UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although this preparation method can improve the overall biocompatibility and has liver and spleen specificity, the improvement of the drug loading capacity of nanoparticles is limited.

Method used

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  • Gadolinium-containing magnetic resonance contrast agent and preparation method thereof
  • Gadolinium-containing magnetic resonance contrast agent and preparation method thereof
  • Gadolinium-containing magnetic resonance contrast agent and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Weighed 140 mg of mesoporous hollow spherical structure hydroxyapatite (HAP), added to 10 ml of 30 mg / ml Gd-DTPA aqueous solution with pH 7.0, and ultrasonicated for 10 min. Soak for 24 hours under stirring conditions, and freeze-dry. Prepare a sodium alginate solution with a concentration of 4 mg / ml, then add Gd-DTPA / HAP freeze-dried powder to 20 ml of sodium alginate solution for ultrasonic dispersion, and react with electromagnetic stirring for 20 minutes to obtain a suspension system. The suspension was ultracentrifuged and the resulting pellet was freeze-dried. The amount of Gd-DTPA loaded on the sample is 17%, and the average particle size is 850nm.

Embodiment 2

[0027] Weigh 45 mg of hydroxyapatite (HAP) with mesoporous hollow spherical structure, add it to 10 ml of 45 mg / ml Gd-DTPA aqueous solution with pH 7.0, and process it ultrasonically for 10 min. Soak for 24 hours under stirring conditions, and freeze-dry. Prepare a sodium alginate solution with a concentration of 3 mg / ml, then add Gd-DTPA / HAP lyophilized powder to 15 ml of sodium alginate solution for ultrasonic dispersion, and react with electromagnetic stirring for 20 minutes to obtain a suspension system. The suspension was ultracentrifuged and the resulting pellet was freeze-dried. The amount of Gd-DTPA loaded on the sample is 19%, and the average particle size is 760nm.

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Abstract

The invention relates to the field of magnetic resonance imaging, in particular to a gadolinium-containing magnetic resonance contrast agent and a preparation method thereof. The gadolinium-containing magnetic resonance contrast agent of the invention mainly comprises a gadolinium chelate, hydroxyapatite and sodium alginate, wherein the contrast agent is prepared by wrapping the gadolinium chelate-supported hydroxyapatite with the sodium alginate. The magnetic resonance contrast agent of the invention has small toxic or side effect on human body; the particle diameter of the particles is controllable (0.1 to 2.0mu m); the specificity of the liver part and the spleen part can be realized through passive targeting; and the contrast agent carries 12.5 to 20 mass percent of gadolinium chelate, has high sustained-release performance and can improve the development effect.

Description

technical field [0001] The invention relates to a magnetic resonance contrast agent for early tumor diagnosis, in particular to a gadolinium-containing magnetic resonance contrast agent and a preparation method thereof. Background technique [0002] Magnetic resonance imaging (MRI) has been widely used clinically. In order to improve the effect of magnetic resonance imaging, it is usually necessary to use nuclear magnetic resonance contrast agents. Contrast agents are used to enhance the intensity of images, by changing the local magnetic field strength or relaxation time of the tissue, or by enhancing the differences in imaging factors through the physiological and biochemical properties of contrast agents to achieve the purpose of contrast. Free gadolinium is highly toxic, distributing in the body to bone and liver, and can rapidly lead to liver necrosis. Therefore, all gadolinium-containing contrast agents are chelates, which can change their distribution in the body aft...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K49/12A61K49/18
Inventor 徐云龙张敏钱秀珍赵崇军
Owner EAST CHINA UNIV OF SCI & TECH
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