Magnetic resonance imaging contrast agent having bone tissue targeting detection based on metal fullerene and the preparation thereof

A technology of metallofullerene and magnetic resonance imaging, which is applied in the direction of nuclear magnetic resonance/magnetic resonance imaging contrast agents, etc., can solve the problems of reducing detection sensitivity and not having targeted detection functions, and achieves convenient operation, leakage prevention, The effect of simplifying the compositing steps

Active Publication Date: 2007-10-31
赤峰福纳康生物技术有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, since the surface of the carbon cage is not modified with a functional group that has affinity with a specific tissue of the organism, the substance does not have a targeted detection function, which greatly reduces the detection sensitivity at the same dosage.

Method used

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  • Magnetic resonance imaging contrast agent having bone tissue targeting detection based on metal fullerene and the preparation thereof
  • Magnetic resonance imaging contrast agent having bone tissue targeting detection based on metal fullerene and the preparation thereof
  • Magnetic resonance imaging contrast agent having bone tissue targeting detection based on metal fullerene and the preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Add 1g NaH to Gd@C 82 (5mg) in anhydrous toluene solution (25mL), add dropwise anhydrous toluene solution (0.5mL) of tetraethylmethylene diphosphate (10μL) while stirring, after stirring at 25°C for 1h, pour into the mixture Deionized water (50 mL) was slowly added dropwise into the mixture, and stirring was continued at 25° C. for 24 h until the toluene layer completely faded. The brown water layer is washed three times with analytically pure toluene, then concentrated under reduced pressure, using Sephadex G-25 as the stationary phase, and deionized water as the eluent, and collecting the brown components with pH=6-7 is the present invention Prepared Gd@C containing osteotropic functional group phospholipid 82 water soluble derivatives of

[0040] Gd@C 82 o 2 (OH) 16 (C(PO 3 Et 2 ) 2 ) 10 (Gd-TEMDP).

[0041]

[0042] Figure 1 depicts the metallofullerene-based Gd@C 82 Preparation of Extracaged Phospholipid-Based Magnetic Resonance Imaging Contrast Agent...

Embodiment 2

[0056] Use purified TNT-type metallofullerenes containing Gd, such as Gd 2 ScN@C 80 (about 10 mg) was prepared into a toluene solution, and Bingel addition reaction could also occur with tetraethylmethylene diphosphate in the presence of NaH, stirred at 30°C for 2 hours, and the other conditions were the same as in Example 1.

Embodiment 3

[0058] Using another purified Gd-containing metal fullerene Gd with contrast effect 2 @C 80 (about 5 mg) was prepared into a toluene solution, and Bingel addition reaction with tetraethylmethylene diphosphate could also occur in the presence of NaH, stirred at 23°C for 2h, and the other conditions were the same as in Example 1.

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Abstract

The invention discloses a high effective magnetic resonance image-forming contrast agent with bone tissue target taxis teat base on metallic enriched ocimene and preparing method, which is characterized by the following: setting molecule formula at Gd@C82Ox(OH)y(C(PO3Et2)2)10 or GdaM3-aN@C80Ox(OH)y(C(PO3Et2)2)10 or Gd2@C80Ox(OH)y(C(PO3Et2)2)10; setting a at 1, 2 or 3; setting M as Sc or Er; setting x as 2-8; setting y as 12-16; setting Et as ethyl group; choosing metallic enriched ocimene with Gd as raw material; proceeding Bingel addition reaction with tetraethyl methano diphosphate under existence of NaH; proceeding nucleophilic additive reaction with OH-; synthesizing water-soluble metallic enriched ocimene derivant with outer cage modification phosphatide group with big scale. This invention possesses the advantages of convenient operation and big scale production.

Description

technical field [0001] The invention relates to a high-efficiency magnetic resonance imaging contrast agent with bone tissue targeting detection, and also relates to a preparation method of the magnetic resonance imaging contrast agent. Background technique [0002] 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 MRI imaging efficiency of Gd-DTPA [diethylenetriaminepe...

Claims

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Application Information

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IPC IPC(8): A61K49/06
Inventor 王春儒舒春英
Owner 赤峰福纳康生物技术有限公司
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