Magnetic resonance liver targeting contrast medium and preparation method thereof

A contrast agent and liver-targeting technology, applied in the direction of nuclear magnetic resonance/magnetic resonance imaging contrast agent, etc., can solve the problem of short half-life and achieve the effect of strong affinity and increased ability

Inactive Publication Date: 2009-09-23
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Second, it has a short half-life and is easily cleared from the blood compartment, resulting in the release of paramagnetic metal ions that can be toxic

Method used

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  • Magnetic resonance liver targeting contrast medium and preparation method thereof
  • Magnetic resonance liver targeting contrast medium and preparation method thereof
  • Magnetic resonance liver targeting contrast medium and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0057] Weigh 0.6 g of soy lecithin, dissolve it with 10 ml of ether, place it in a 250 ml three-necked bottle, and disperse the ether to form a film of soy lecithin on the bottle wall. Add FeCl 3 Put 50ml (1.0%) of the solution in a 250ml three-necked bottle and stir. Weigh 0.13g FeCl 2 , dissolved in 50ml of water, transferred to a three-necked bottle. Add 1.5mol·L dropwise -1 NaOH solution. Meanwhile give a quick stir. After the reaction is completed, centrifuge to obtain magnetic oxides. The morphology and particle size of nanoparticles were observed with JEM-2000EXII high resolution electron microscope (high resolution transmission electron microscope). The results are shown in Fig.1(a), Fig.1(b) shows the morphology of the sample, and the magnetic iron oxide generated in the ordered body (bilayer liposome) composed of soy lecithin and water is observed and measured by TEM The particle size is about 7nm. And spread out very well. The particle size is 7nm, and the ...

Embodiment 2

[0059] FeCl 3 and FeCl 2 Mix and add to 100ml of water at a molar ratio of 2:1, mix well and place in a 250ml three-neck bottle, and turn on the stirrer at the same time. Add 10 g of dextran solution to the three-necked flask. In a constant temperature water bath at 70-80°C, add 1.5mol·L -1 NaOH solution. The mixture was aged at 80 °C for 50 min, then cooled to room temperature. Adjust the pH to 5.0 with HCl. The pellet and supernatant were centrifuged. The precipitate was washed three times with water and dried at 70°C to constant weight. to obtain magnetic oxides. TEM observation results are shown in Fig.2(a), Fig.2(b)

[0060] The particle size is 5nm, and the saturation magnetization (M s ) is 36.4emu / g, the residual magnetization (M r ) is 5.7emu / g, and there is no coercive force (jHc), jHc is 0.0Oe.

Embodiment 3

[0062] Get 140ml of the mixed solution of 500ml iron salt and ferrous salt. It contains 32gFeCl 2 .4H 2 O and 75.5 g FeCl 3 .6H 2 O, add to 500ml 3mol·L -1 NaOH solution containing 1000 grams of dextran. The resulting suspension was heated at 100°C for 10 minutes while stirring, cooled and centrifuged for 10 minutes, and the supernatant was diluted with water to make the total volume 2L, after which it was added to 500ml of 1M sodium citrate solution, and the mixture was washed with Dialyze with a 10 mM ammonium citrate buffer solution, adjust the pH to 8.2 with ammonia water, add 1 g of mannitol, and sterilize under high pressure at 121° C. for 30 minutes to obtain a liver-targeting nano-contrast agent.

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Abstract

The invention relates to a magnetic resonance liver targeting contrast medium and a preparation method thereof, belonging to the technical field of medicine. The magnetic resonance liver targeting contrast medium is a superparamagnetism contrast medium which takes magnetic nanometer iron oxide granules as main components, the surface of a superparamagnetism iron oxide nanoparticle is modified by phospholipids or sugar anhydrides, wherein the phospholipids are taken as a nanometer reactor, the sugar anhydrides are taken as surface modifying materials, and the ratio of the magnetic nanometer iron oxides to the phospholipids is 1-40 to 1-50; besides, the magnetic resonance liver targeting contrast medium also comprises penetration regulators, such as the sugar anhydrides, a stabilizing agent, and the like, and a PH regulator and is prepared by a coprecipitation method under normal temperature and pressure. The invention takes biodegradable and metabolizable superparamagnetism metal oxides used inside bodies as the MR contrast medium, and the metabolizable superparamagnetism metal oxides exist in a dispersing medium which is physiologically accepted in a superparamagnetism granule dispersoid or a superparamagnetism fluid way and can be accumulated on a special targeting organ to be imaged.

Description

Technical field: [0001] The invention relates to an injection for radiological diagnosis, in particular to a magnetic resonance contrast agent and a manufacturing method thereof. In particular, it relates to a magnetic resonance liver targeting contrast agent and a manufacturing method thereof. Background technique: [0002] Today, human diseases have undergone major changes, and malignant tumors have become the primary disease that threatens human life and health, with high morbidity and mortality. According to reports, there are more than 350 million infectious hepatitis virus carriers in the world, and there are about 240 million hepatitis virus carriers in China. This is the main cause of liver cancer, and 10% of them develop into liver cancer. In view of the fact that most cancer patients are already in the middle and late stages when they are discovered, it is difficult or unsuitable for surgical treatment. How to locate and diagnose malignant tumors at an early stag...

Claims

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Application Information

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IPC IPC(8): A61K49/06
Inventor 李铁福邓英杰
Owner SHENYANG PHARMA UNIVERSITY
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