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Magnetic resonance imaging contrast medium based on metal fullerene and its prepn process

A metallofullerene, magnetic resonance imaging technology, applied in nuclear magnetic resonance/magnetic resonance imaging contrast agents, nanotechnology for sensing, nanotechnology, etc., can solve problems such as vascular obstruction, reduce economic costs, save Materials, excellent imaging efficiency

Inactive Publication Date: 2006-08-02
INST OF CHEM CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But in acidic and neutral solutions Gd@C 82 (OH) x It is easy to agglomerate into large particles, and if it is applied in animals or humans, it will encounter the problem of vascular obstruction

Method used

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  • Magnetic resonance imaging contrast medium based on metal fullerene and its prepn process
  • Magnetic resonance imaging contrast medium based on metal fullerene and its prepn process
  • Magnetic resonance imaging contrast medium based on metal fullerene and its prepn process

Examples

Experimental program
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Effect test

Embodiment 1

[0024] Example 1: Weigh 11mg NaOH, 24.3mg β-alanine, add 0.5mL water to dissolve, add 2mL absolute ethanol, add this mixture dropwise to about 5mL purified Gd@C 82 (about 1.3 mg) in toluene solution, stirred at room temperature for 5 days, then separated by liquid separation, and the lower layer was washed twice with toluene to remove unreacted Gd@C 82 , after concentrating under reduced pressure, use Sephadex G-25 as the stationary phase, use high-purity water as the eluent, and collect the brown component with pH=6-7, which is the Gd@C of the present invention 92 Carboxylated water-soluble derivatives (AAD-EMF).

[0025]

[0026] According to the stoichiometric ratio shown in Equation 1 above, reactant A can be reacted as completely as possible if (B) is in large excess. OH in base - will also work with Gd@C 82 Nucleophilic addition reaction occurs, yellow-green Gd@C 82 The toluene solution will gradually turn colorless, while the underlying alcoholic aqueous layer tu...

Embodiment 2

[0027] Embodiment 2: use purified Gd@C 82 (about 1.3mg) is mixed with toluene solution, and the alkali solution concentration of taurine is 0.2mol / L, also can take place nucleophilic addition reaction, stirs 5 days under normal temperature, all the other conditions are with embodiment 1.

Embodiment 3

[0028] Example 3: Using another purified nitrogen-containing metal fullerene Gd with contrast effect 3 N@C 80 (about 1.3 mg) is prepared into a toluene solution and an alkaline solution of β-alanine or taurine, and a nucleophilic addition reaction can also occur. In this embodiment, β-alanine or taurine and metal-rich Stir at room temperature for 3 days at a molar ratio of 100:1, and the rest of the conditions are the same as in Example 1.

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Abstract

The magnetic resonance imaging contrast medium based on metal fullerene has the molecular expression of Gd@C82OHx(NH2CH2CH2COOH)y.Gd@C82OHx(HNCH2CH2SO3H)y, where x=16-22 and yú¢6-8. The preparation process is the neucleophilic addition reaction between metal fullerene material Gd@C82 and the alkali solution of beta-alanine or amino ethyl sulfuric acid to form the water- soluble metal fullerene derivative with decorating carboxyl radical or sulfo radical. The preparation process is simple and mild, and may be used in industrial production. The water- soluble derivative of the present invention has magnetic resonance imaging efficiency obviously higher than available Gd-divinyl triamino penta acetic acid chelate.

Description

technical field [0001] The invention relates to a magnetic resonance imaging contrast agent. [0002] The present invention also relates to a preparation method of the above magnetic resonance imaging contrast agent. Background technique [0003] Magnetic resonance imaging (MRI) technology has now developed into a common method in clinical medical diagnosis, and it is one of the most effective methods for diagnosing tumors. In order to enhance the contrast and clarity between diseased tissue and normal tissue images, it is necessary to select an appropriate contrast enhancer to reveal anatomical features. Most of these contrast enhancement agents utilize the paramagnetic properties of metal ions. Gd 3+ Because of its strong paramagnetism, its complexes are currently the most widely used and most effective class of contrast enhancement agents. Recent research results show that Gd@C 82 (OH) 40 The efficiency of MRI imaging is 20 times that of the clinically used Gd-DTPA ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K49/06
CPCB82Y15/00
Inventor 王春儒舒春英白春礼甘利华
Owner INST OF CHEM CHINESE ACAD OF SCI
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