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Respiratory-tract magnetic-resonance spray contrast agent and preparation method thereof

A contrast agent and magnetic resonance technology, which is applied in the direction of nuclear magnetic resonance/magnetic resonance imaging contrast agent, emulsion delivery, drug delivery, etc., can solve the problem of unsatisfactory display effect of gadolinium contrast agent, and is suitable for large-scale preparation and improvement. Sensitivity and specificity, easy-to-use results

Inactive Publication Date: 2010-02-03
RENJI HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The object of the present invention is to provide a respiratory magnetic resonance spray contrast agent, which solves the technical problem that the gadolinium contrast agent used in magnetic resonance in the prior art has an unsatisfactory display effect

Method used

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  • Respiratory-tract magnetic-resonance spray contrast agent and preparation method thereof
  • Respiratory-tract magnetic-resonance spray contrast agent and preparation method thereof
  • Respiratory-tract magnetic-resonance spray contrast agent and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0027] Gadolinium-lipid complexes were prepared from lecithin, cholesterol and cationic lipid DOTAP (1,2-dioleoyl-3-trimethylammoniopropane). 540 milligrams of lecithin, 180 milligrams of cholesterol and 180 milligrams of DOTAP are dissolved in 10 milliliters of chloroform, and rotary evaporation obtains lipid film, and adding concentration is 30 milliliters of the gadopentetate meglumine aqueous solution of 12 mg / ml (get the gadopentetate meglumine injection Add water to dilute to the required concentration), hydrate, sonicate, and extrude through a 400nm membrane to obtain a gadolinium-lipid complex with a concentration of 12 mg / ml. As determined by PCS, the average particle size of the complex is 400nm, and the zeta potential is 70mv. Ultrasonic nebulization of the obtained compound was carried out to measure the average diameter of the droplets D 50 5um, D 90 It is 8um (Spraytec, British Malvern Company).

[0028] In vitro airway imaging study of gadolinium-lipid comple...

Embodiment 2

[0031] Gadolinium-lipid complexes were prepared from soybean lecithin, cholesterol and polycationic lipid dioctadecylamidoglycyl spermine (DOGS). 540 milligrams of soybean lecithin, 180 milligrams of cholesterol and 90 milligrams of DOGS are dissolved in 10 milliliters of chloroform, and rotary evaporation obtains lipid film, and adding concentration is 30 milliliters of the aqueous solution of 5 mg / ml of gadobeglumine (get the gadobenate meglumine injection Add water to dilute to the desired concentration), hydrate, sonicate, and homogenize under high pressure to obtain a gadolinium-lipid complex with a concentration of 5 mg / ml. As determined by PCS, the average particle size of the complex is 600nm, and the Zeta potential is 90mv. Ultrasonic nebulization of the obtained compound was carried out to measure the average diameter of the droplets D 50 4um, D 90 It is 9um (Spraytec, British Malvern Company). The results of MRI imaging and gadolinium distribution measurement sho...

Embodiment 3

[0033] Gadolinium-lipid complexes were prepared from DSPC (distearoylphosphatidylcholine), cholesterol and stearylamine. 600 mg of soybean lecithin, 300 mg of cholesterol and 120 mg of stearylamine are dissolved in 20 milliliters of tert-butanol, and 5 ml of concentration of 90 mg / ml of gadopentetate meglumine aqueous solution (dilute gadopentetate meglumine injection with water to desired concentration), and mix well to obtain a clear solution. Freeze-dried for 72 hours, took out and added 30ml of water, hydrated, ultrasonicated, and homogenized under high pressure. A gadolinium-lipid complex was obtained at a concentration of 15 mg / ml. As determined by PCS, the average particle size of the complex is 800nm, and the Zeta potential is 50mv. Ultrasonic nebulization of the obtained compound was carried out to measure the average diameter of the droplets D 50 5.5um, D 90 It is 10um (Spraytec, British Malvern Company). The results of MRI imaging and gadolinium distribution me...

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Abstract

The invention provides a respiratory-tract magnetic-resonance spray contrast agent, which is a gadolinium-lipid compound formed from a gadolinium contrast agent and a lipid, wherein the average diameter of the compound is less than 1,000 nm, and the mean value of the Zeta potential of the compound is more than 40 mv. The lipid component is selected from at least one or combination of phospholipids, glycolipids, sterol, cationic lipids, surfactant, amphiphilic polymers, and at least contains a positive-charge lipid component. The invention also provides a method for preparing the respiratory-tract magnetic-resonance spray contrast agent. After the contrast agent is atomized and inhaled, gadolinium is effectively distributed on the surface of far-end respiratory-tract mucosa by utilizing theelectrostatic interaction between positive charges carried by the compound and negative charges on the surface of the respiratory-tract mucosa, and the distribution uniformity of spray drips on the surface of the mucosa by means of the action of the surface activity of the lipid, so that the problem that the gadolinium is only distributed on near-end respiratory tracts, is easy to gather and flows to the lower parts of the respiratory tracts after gadolinium aqueous solution is sprayed is solved, and the surface of the whole respiratory-tract mucosa is completely and clearly shown.

Description

technical field [0001] The present invention relates to articles for human life, in particular to medical preparations, in particular to contrast agents, in particular to a preparation method of a respiratory magnetic resonance (MRI) spray-type contrast agent. Background technique [0002] There are many types of respiratory tract lesions, such as benign lesions such as inflammatory lesions, external pressure lesions, congenital mutations, emphysema, and malignant lesions such as airway tumors. Although the incidence of benign lesions is not high, the changes in airway morphology are more complicated. Lung cancer has the highest incidence of airway malignancies, and the morbidity and mortality of primary lung cancer are on the rise in many countries and regions in the world. The results of a sample survey of lung cancer in my country in 2000 showed that the mortality rate of males was 40.1 / 100,000, and that of females was 13.48 / 100,000, a significant increase from the early...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K49/06A61K49/18
Inventor 许建荣徐宇虹吴华伟魏晓慧
Owner RENJI HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
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