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Method for preparing paramagnetic polyphosphazene nanotube magnetic resonance imaging contrast agent

A technology of magnetic resonance imaging and polyphosphazene, which is applied in the directions of nuclear magnetic resonance/magnetic resonance imaging contrast agents, preparations for in vivo experiments, pharmaceutical formulations, etc. Fibrosis and other problems, to achieve the effects of good biocompatibility and degradability, low cost and simple processing technology

Inactive Publication Date: 2010-11-24
JIANGSU UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

At present, the commonly used MRI contrast agent in clinical practice, such as Magnevist Gd-DTPA, is a small-molecule ionic MRI contrast agent with high osmotic pressure in the body, short retention time in the body, and is easily excreted after renal metabolism. Selectively, the free Gd(III) leaked in the body will cause the Fenton reaction of intracellular iron deposition, resulting in cell fibrosis, etc.

Method used

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  • Method for preparing paramagnetic polyphosphazene nanotube magnetic resonance imaging contrast agent
  • Method for preparing paramagnetic polyphosphazene nanotube magnetic resonance imaging contrast agent
  • Method for preparing paramagnetic polyphosphazene nanotube magnetic resonance imaging contrast agent

Examples

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example 1

[0019] Add 5 grams (14.4 millimoles) of hexachlorocyclotriphosphazene and 10.8 grams (43.2 millimoles) of 4,4'-dihydroxydiphenylsulfone in a 1000 milliliter flask, then add 400 milliliters of anhydrous tetrahydrofuran, stir to dissolve, and then Add 8.7 g (86.4 mmol) of triethylamine in 150 ml of anhydrous tetrahydrofuran solution into the above reactor, and at 25 ° C, use an ultrasonic cleaner to vigorously stir and react for half an hour. After the reaction is completed, filter the crude The product was washed three times with tetrahydrofuran, then three times with deionized water, and finally dried in a vacuum oven for 24 hours to obtain 12.5 g of cross-linked polyphosphazene nanotubes, with a yield of 93% based on hexachlorocyclotriphosphazene.

[0020] Add 8.8 grams of synthesized cross-linked polyphosphazene nanotubes to a 500 ml flask, add 350 ml of deionized water, stir vigorously with an ultrasonic cleaner for half an hour, add GdCl 3 ·6H 2 3.75 g of O solid was reac...

example 2

[0026]Add 5 grams (14.4 millimoles) of hexachlorocyclotriphosphazene and 10.8 grams (43.2 millimoles) of 4,4'-dihydroxydiphenylsulfone in a 1000 milliliter flask, then add 400 milliliters of anhydrous tetrahydrofuran, stir to dissolve, and then Add 8.7 g (86.4 mmol) of triethylamine in 150 ml of anhydrous tetrahydrofuran solution into the above reactor, and at 25 ° C, use an ultrasonic cleaner to vigorously stir and react for half an hour. After the reaction is completed, filter the crude The product was washed three times with tetrahydrofuran, then washed three times with deionized water, and finally dried in a vacuum oven for 24 hours to obtain cross-linked polyphosphazene nanotubes.

[0027] Add 8.8 grams of synthesized cross-linked polyphosphazene nanotubes to a 500 ml flask, add 350 ml of deionized water, stir vigorously with an ultrasonic cleaner for half an hour, add MnCl 2 2.45 g of solids were reacted for 6 hours at 25° C. with an ultrasonic power of 240 watts. After...

example 3

[0029] Add 5 grams (14.4 millimoles) of hexachlorocyclotriphosphazene and 10.8 grams (43.2 millimoles) of 4,4'-dihydroxydiphenylsulfone in a 1000 milliliter flask, then add 400 milliliters of anhydrous tetrahydrofuran, stir to dissolve, and then Add 8.7 g (86.4 mmol) of triethylamine in 150 ml of anhydrous tetrahydrofuran solution into the above reactor, and at 25 ° C, use an ultrasonic cleaner to vigorously stir and react for half an hour. After the reaction is completed, filter the crude The product was washed three times with tetrahydrofuran, then washed three times with deionized water, and finally dried in a vacuum oven for 24 hours to obtain cross-linked polyphosphazene nanotubes.

[0030] Add 8.8 grams of synthesized cross-linked polyphosphazene nanotubes to a 500 ml flask, add 350 ml of deionized water, stir vigorously with an ultrasonic cleaner for half an hour, add FeCl 2 2.55 g of solids were reacted for 6 hours at 25° C. with an ultrasonic power of 240 watts. Afte...

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Abstract

The invention discloses a method for preparing a paramagnetic polyphosphazene nanotube magnetic resonance imaging contrast agent. The method is characterized by firstly taking hexachlorocyclotriphosphazenes and 4,4'-dihydroxydiphenylsulfone as comonomers and triethylamine as an acid binding agent to carry out polymerization under room temperature to prepare the polyphosphazene nanotube and obtaining a polyphosphazene nanotube ligand after purifying the polyphosphazene nanotube; and then reacting the ligand with paramagnetic metal inorganic salt, finally centrifuging the reactant, washing the product three times respectively with water and absolute ethyl alcohol, thus obtaining the solid powder of the magnetic resonance imaging contrast agent after drying. The method is strong in operability, wide in application range, simple in equipment requirement, low in cost and high in yield and can be used for mass production in industry application. The magnetic resonance imaging contrast agent of the invention is a novel polymer nanotube magnetic resonance imaging contrast agent. The relaxation rate of the magnetic resonance imaging contrast agent is as high as 42.88-237.83mmol / L*s and is 12-65 times that of the commercial magnetic resonance imaging contrast agents Gd-DTPA (with relaxation rate of 3.64mmol / L*s).

Description

technical field [0001] The invention relates to the technical field of magnetic resonance imaging, in particular to a preparation method of a novel magnetic resonance imaging contrast agent. Background technique [0002] Magnetic Resonance Imaging (MRI) is a diagnostic technique that uses the nuclear magnetic resonance phenomenon of a certain nucleus in human tissue, and processes the radio frequency signal obtained by a computer to reconstruct an image of a certain level of the human body. In clinical magnetic resonance imaging, more than 30% to 40% of diagnoses require the use of MRI contrast agents. MRI contrast agents are some paramagnetic and superparamagnetic substances, which can shorten the local proton relaxation time, indirectly change the signal intensity generated by these protons, and improve the imaging contrast between normal and diseased parts, thereby showing the functional status of internal organs. At present, the commonly used MRI contrast agent in clini...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G79/04A61K49/06A61K49/12
Inventor 张小燕张岐龚玉珍吴静波韩同伟
Owner JIANGSU UNIV
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