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Functionalized modified polyvinyl alcohol embolic microsphere and preparation method thereof

A technology of polyvinyl alcohol embolization and polyvinyl alcohol, which is applied in the field of functionalized modified polyvinyl alcohol embolization microspheres and its preparation, can solve the problems of cumbersome operation process, achieve good suspension and deformation elasticity, and moderate drug loading capacity. The effect of improved controlled release ability and good drug loading performance

Active Publication Date: 2017-05-31
SUZHOU HENGRUI CALLISYN BIOLOGICAL MEDICINE TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the actual operation process is cumbersome, such as demulsification with absolute ethanol, repeated soaking and washing in deionized water to remove unreacted residues during the reaction process.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Add 250 mL of 2.5 mol / L sodium hydroxide solution into the four-neck flask, cool down to 3.3°C in an ice-salt bath, add 26.6 g of aspartic acid, start stirring, and adjust the stirring speed to 320 rpm. After stirring evenly, add acryloyl chloride dropwise. During the dropping process, control the temperature of the system at about 3.3°C. The pH meter monitors the pH value of the system in real time. When the pH value reaches 7.0, stop adding acryloyl chloride dropwise. After the dropwise addition, continue stirring at 3.3°C. 30 minutes, then slowly rise to room temperature and continue to react for 2.5 hours. After the reaction, adjust the pH value of the system to 1.0 with hydrochloric acid, then add 800mL ethyl acetate to extract 4 times, collect the extract and then concentrate it by rotary evaporation. The concentrated solution is recrystallized to obtain a white The powdery solid product, namely the acylated aspartic acid product, weighed 43.7 g.

Embodiment 2

[0032] Add 300 mL of 2.0 mol / L sodium hydroxide solution into the four-neck flask, cool down to 7.8°C in an ice-salt bath, add 26.8 g of 2-hydroxysuccinic acid, start stirring, and adjust the stirring speed to 400 rpm. After stirring evenly, add crotonoyl chloride dropwise. During the dropping process, control the temperature of the system at about 7.8°C. The pH meter monitors the pH value of the system in real time. When the pH value reaches 7.5, stop adding crotonyl chloride dropwise. The dropwise addition is completed at 7.8°C. Continue to stir for 20 minutes, then slowly rise to room temperature and continue the reaction for 1 hour. After the reaction, adjust the pH value of the system to 2.0 with hydrochloric acid, then add 600mL ethyl acetate to extract twice, collect the extract and concentrate it by rotary evaporation. After the concentrate is recrystallized A white powdery solid product was obtained, namely the acylated 2-hydroxysuccinic acid product, weighing 46.6 g. ...

Embodiment 3

[0034] Add 400 mL of 1.0 mol / L sodium hydroxide solution into the four-neck flask, cool down to 10°C in an ice-salt bath, add 64.0 g of 2-amino-5-hydroxynaphthalene-1,7 disulfonic acid, and start stirring. Adjust the stirring speed to 300 rpm. After stirring evenly, add acryloyl chloride dropwise. During the dropping process, control the temperature of the system at about 10°C. The pH meter monitors the pH value of the system in real time. When the pH value reaches 7.8, stop adding acryloyl chloride dropwise. After the dropwise addition, continue stirring at 10°C. 30 minutes, then slowly rise to room temperature and continue to react for 2 hours. After the reaction, adjust the pH value of the system to 0.5 with hydrochloric acid, then add 1200mL ethyl acetate to extract 4 times, collect the extract and concentrate it by rotary evaporation. The concentrated solution is recrystallized to obtain a white The powdery solid product, namely the acylated 2-amino-5-hydroxynaphthalene-1...

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Abstract

The invention relates to a functionalized modified polyvinyl alcohol embolic microsphere and a preparation method thereof, and belongs to the field of medical intervention treatment. The functionalized modified polyvinyl alcohol embolic microsphere is prepared by taking polyvinyl alcohol as a base material, taking amino / hydroxyl carboxylic acid derivatives / sulfonic acid derivatives capable of crosslinking after acylation as a modifying agent and performing modification. The modified microsphere prepared by the method has perfect sphere shape, uniform size, high suspending property and shape change elasticity of the polyvinyl alcohol microsphere before modification. Meanwhile, a polycarboxylic / mucopolysacchariden functional group with negative charges is introduced and can be combined with micromolecular anti-tumor medicines with positive charges, so that the microsphere has high medicine loading property. Compared with the polyvinyl chloride microsphere which is not functionalized and cannot carry medicines or the microsphere which only introduces single group with negative charges and has low medicine carrying quantity in the prior art, the microsphere increases the medicine carrying quantity and improves the controlled release capability greatly.

Description

technical field [0001] The invention relates to functionalized modified polyvinyl alcohol embolic microspheres and a preparation method thereof, belonging to the field of medical interventional therapy. Background technique [0002] With the development of clinical medical technology, transcatheter vascular embolization has been more and more widely used in the field of interventional radiotherapy due to its advantages of minimal invasiveness, whole-process image guidance, selective target vessel insertion technology, and accurate positioning. The principle of transcatheter vascular embolization is to use high-definition medical imaging equipment to inject synthetic embolic materials loaded with anti-tumor drugs into blood vessels through catheters to block blood vessels, thereby blocking blood supply from blood vessels to tumor sites and releasing anti-tumor agents. Drugs that cause tumors to shrink and die. The key to transcatheter vascular embolization is to choose the a...

Claims

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Application Information

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IPC IPC(8): A61L24/06A61K9/16A61K47/32A61P35/00
CPCA61K9/0002A61K9/1635A61L24/0015A61L24/06A61L2300/416A61L2300/602C08L29/04
Inventor 汪青松徐伟春柳小平施海萍
Owner SUZHOU HENGRUI CALLISYN BIOLOGICAL MEDICINE TECH CO LTD
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