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Developable composite microsphere embolization agent and preparation method thereof

A technology of composite microspheres and embolizing agent, applied in the field of medicine, can solve problems such as inability to develop, and achieve the effect of facilitating clinical operation

Active Publication Date: 2014-08-13
SOUTHEAST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the current carrageenan-gelatin microspheres can only realize their drug loading and embolization functions, and have the disadvantage of being unable to develop
[0006] Embolization microspheres are the first choice in the treatment of some unresectable tumors, but there is no report on CT-visible carrageenan-gelatin microspheres and their preparation process

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1: Preparation of CT-developable composite microsphere embolism by emulsification cross-linking method (using lipophilic contrast agent)

[0028] Weigh 60mg PLA and 60μL iodized oil and dissolve in 2mL dichloromethane solution, sonicate in an ice bath for 1min to make the inner oil phase. Weigh 0.6g of gelatin and 0.6g of carrageenan powder, slowly sprinkle the powder in 10mL of pure water, swell at 55°C for 20min, add 0.1g of Tween60 dropwise to make a water phase. Measure 50mL of liquid paraffin, add 0.5g of Span60 dropwise, and preheat at 55°C to make the outer oil phase. Slowly inject the inner oil phase into the water phase, stir at 55°C and 800rpm for 30min, and form O / W colostrum after dichloromethane volatilizes. Add colostrum dropwise to the external oil phase preheated to 55°C, adjust the rotation speed to 500rpm, and continue stirring at 55°C for 15 minutes to form O / W / O type double emulsion. Stir and cool for 30 min, add 1.5 ml of 25% glutaraldehyd...

Embodiment 2

[0029] Example 2: Preparation of CT-developable composite microsphere embolic agent by emulsification cross-linking method (using lipophilic contrast agent)

[0030] Weigh 45mg PLA and 30μL iodized oil and dissolve in 2mL dichloromethane solution, sonicate in ice bath for 1min to make the inner oil phase. Weigh 0.9g of gelatin and 0.3g of carrageenan powder, slowly sprinkle the powder in 10mL of pure water, swell at 55°C for 20min, add 0.08g of Tween80 dropwise to make a water phase. Measure 50mL of liquid paraffin, add 0.4g of Span80 dropwise, and preheat at 55°C to make the outer oil phase. Slowly inject the inner oil phase into the water phase, stir at 55°C and 800rpm for 30min, and form O / W colostrum after dichloromethane volatilizes. Add colostrum dropwise to the external oil phase preheated to 55°C, adjust the rotation speed to 500rpm, and continue stirring at 55°C for 15 minutes to form O / W / O type double emulsion. Stir and cool for 30 min, add 1.5 ml of 25% glutaralde...

Embodiment 3

[0031] Example 3: Preparation of CT-developable composite microsphere embolic agent by emulsification cross-linking method (using water-soluble contrast agent)

[0032]Weigh 1.0g of gelatin and 0.2g of carrageenan powder, slowly sprinkle the powder in 10mL of pure water, add 100ul of N,N'-bis(2,3-dihydroxypropyl)-5-[N- (2,3-Dihydroxypropyl)acetamido]-2,4,6-triiodoisophthalamide solution was swelled at 55°C for 20 minutes, and 0.1g of Tween60 was added dropwise to prepare an aqueous phase. Measure 50mL of liquid paraffin, add 0.5g of Span60 dropwise, and preheat at 55°C to make an oil phase. Add the water phase dropwise to the oil phase preheated to 55°C, adjust the rotation speed to 500rpm, and continue stirring at 55°C for 15min. Stir and cool for 30 min, add 1.5 ml of 25% glutaraldehyde solution dropwise, and continue stirring for 1 h. Finally, add 30ml of isopropanol and stir for dehydration for 15 minutes, then wash with isopropanol, water and absolute ethanol in stages,...

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Abstract

The invention discloses a developable composite microsphere embolization agent and a preparation method thereof. The developable composite microsphere embolization agent contains mixed gel composed of carrageenan and gelatin, a biodegradable polymer, an emulsifier, a crosslinking agent and a contrast agent. The developable composite microsphere embolization agent is a novel microsphere integrating embolization, CT development and administration functions and can be used for treating such diseases as tumor and the like. The preparation method of the composite microsphere embolization agent is used for loading the contrast agent in a microsphere in a water in oil or an oil in water manner, achieving synchronous development and embolization and accurately capturing the embolization position to facilitate the clinical operation of doctors. The prepared microsphere has the advantages of wide particle size distribution range, convenient CT development, large drug-loading rate and long embolization time, and the functions of the existing microsphere are perfected; moreover, the preparation process is simple, the operation is convenient and benefit is brought to patients.

Description

technical field [0001] The invention relates to a composite microsphere embolic agent and a preparation method thereof, in particular to a developable composite microsphere embolic agent and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Transcatheter arterial chemoembolization (TACE) was proposed by Japanese scholar Dr. Yamada in 1977. It was first applied to the treatment of liver cancer. It refers to perfusion of chemotherapy drugs through a catheter inserted into the target artery under X-ray fluoroscopy. Embolization with embolic agents not only blocks the blood supply of the tumor, making the tumor lack the necessary nutrient supply, but also enhances the lethality of the drug to the tumor and reduces the systemic toxicity of the drug, which has obvious advantages over traditional chemotherapy. The basic principle is that most of the blood supply to liver tumors (95-99%) comes from the hepatic artery, while the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/42A61K47/36A61K9/16A61K49/04A61P35/00
Inventor 熊非刘坤良顾宁
Owner SOUTHEAST UNIV
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