Magnetic resonance tumour target contrast media and preparing method thereof

A tumor targeting and contrast agent technology, applied in the direction of MRI/MRI contrast agent, etc., can solve the problems of increased pressure, poor enhancement effect, characteristics of blood supply of lesions, etc., achieve obvious biological effects, reduce toxic and side effects, The effect of improving the therapeutic effect

Inactive Publication Date: 2007-05-23
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Abstract
  • Description
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  • Application Information

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Problems solved by technology

[0002] In clinical magnetic resonance imaging (Magnetic Resonance Imag-ing, MRI), the application of common contrast agents for dynamic enhancement can improve the accuracy of lung cancer diagnosis, but it is based on the blood vessel density in nodules or masses, reflecting the blood of the lesion. The characteristics are not specific; the application of monoclonal antibody targeting contrast agent to human body will produce human anti-mouse antibody reaction, and the pressure in the tumor interstitium is increased, and the reason of poor permeability of coupled macromolecules makes the monoclonal antibody type Contrast agents do not target as well as one would expect
Unger et al. used an anti-CEA antibody coupled with gadolinium diethylenediaminepentaacetate (Gd-DTPA) to form an anti-CEA antibody-Gd-DTPA conjugate compound for MR imaging studies of colon adenocarcinoma, and found that there was a large amount of antibody, The shortcomings such as poor enhancement effect, and the occurrence of immune reactions in the human body, the production of anti-antibodies limits repeated use (references: E.C.Unger, W.G.Totty, D.M.Neufeld et al., Magneticresonance imaging using gadolinium labeled monoclonal antibody.Invest.Radiol. 20 (1985), 693-700)

Method used

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  • Magnetic resonance tumour target contrast media and preparing method thereof
  • Magnetic resonance tumour target contrast media and preparing method thereof
  • Magnetic resonance tumour target contrast media and preparing method thereof

Examples

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Embodiment 1

[0037] Example 1: A magnetic resonance tumor targeting contrast agent, which is a combination of folic acid, polylysine, and gadopentetate meglumine GD-DTPA, namely folic acid-PL-Gd-DTPA, with a molecular weight of 30,000 to 70,000 Leon.

Embodiment 2

[0038] Embodiment 2: a kind of method for preparing the magnetic resonance tumor targeting contrast agent described in embodiment 1, it comprises the following steps:

[0039] ①Synthesis of DTPA bis-anhydride (CaDTPA)

[0040] Suspend 10g of diethylenetriaminepentaacetic acid (DTPA) in a mixture of 30ml of acetic anhydride and 15ml of pyridine, stir and react at 60°C for 6h, add an appropriate amount of ethanol to filter after cooling, wash with ether, and dry to obtain a white solid DTPA bisanhydride (CaDTPA )Crude;

[0041] ② Preparation of DTPA-Poly-L-Lysine

[0042]Take Poly-L-Lysine 10mg, dissolve in 3ml 0.2mol / LNaH 2 CO 3 / Na 2 HCO 3 In the buffer solution (pH=9.6), add DTPA bis-acid anhydride (CaDTPA) solution under ice-bath stirring state, stir and react at room temperature for 16 hours, take out the reaction mixture, remove free CaDTPA with equilibrium dialysis, and switch to 0.2M NaAc / HAc (sodium acetate / acetic acid) buffer (pH=5). Take out the solution in the...

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Abstract

The present invention relates to a contrast medium capable of specifically making tumor be developed in magnetic resonance image formation and its preparation method. Said invention uses DTPA-Poly-L-Lysine as carrier of magnetic resonance paramagnetic gadolinium contrast medium, it is coupled with folic acid to form macromolecular polymer, and its molecular weight is 30000-70000. Said macromolecular polymer has the characteristics of high carrier Gd3+ concentration, stable chemical property, high purity and high affinity with folic acid receptor, etc.

Description

technical field [0001] The invention relates to the technical field of medical detection reagents, in particular to a contrast agent capable of specifically imaging tumors in magnetic resonance imaging and a preparation method thereof. Background technique [0002] In clinical magnetic resonance imaging (Magnetic Resonance Imag-ing, MRI), the application of common contrast agents for dynamic enhancement can improve the accuracy of lung cancer diagnosis, but it is based on the blood vessel density in nodules or masses, reflecting the blood of the lesion. The characteristics are not specific; the application of monoclonal antibody targeting contrast agent to human body will produce human anti-mouse antibody reaction, and the pressure in the tumor interstitium is increased, and the reason of poor permeability of coupled macromolecules makes the monoclonal antibody type The targeting effect of contrast agents is not as expected. Unger et al. used an anti-CEA antibody coupled wi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K49/08
Inventor 刘士远袁正钟高仁姜庆军
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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