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Preparation method of narrow-particle-size polyvinyl acetate embolization microspheres with controllable drug loading performance

A technology of polyvinyl acetate embolization microspheres and vinyl acetate, which is applied in medical science, surgery, surgical adhesives, etc., can solve the problems of low drug loading, complex structure, and high preparation cost of Callisphere, and achieve a wide range of applicable drugs , The preparation process is simple, the drug loading effect is large

Active Publication Date: 2021-09-28
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, DC bead has the disadvantages of complex structure and high preparation cost; HepaSphere and Callisphere have the disadvantages of a wide range of microsphere particle size distribution; Callisphere also has the disadvantage of low drug loading

Method used

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  • Preparation method of narrow-particle-size polyvinyl acetate embolization microspheres with controllable drug loading performance
  • Preparation method of narrow-particle-size polyvinyl acetate embolization microspheres with controllable drug loading performance
  • Preparation method of narrow-particle-size polyvinyl acetate embolization microspheres with controllable drug loading performance

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Synthesis of embodiment 1 polyvinyl acetate embolic microspheres

[0039] (1) Put 100 mL of deionized water into a 250 mL three-necked flask connected with a condensing reflux device. Under nitrogen protection, 0.5 g of polyvinylpyrrolidone (molecular weight = 29000) was dissolved in 100 mL of deionized water in a three-necked flask under magnetic stirring (stirring speed: 300-350 rpm).

[0040](2) 0.134g of azobisisobutyronitrile (AIBN) was stirred and dissolved in 50mL of vinyl acetate (VAc), and the temperature of the solution in the three-necked flask was heated to 65°C. Then slowly pour the VAc monomer dissolved with AIBN into a three-necked flask, and raise the temperature of the solution to 70°C for two hours, and then raise the temperature of the solution to 75°C for two hours; during the reaction, keep Nitrogen was bubbled continuously (the nitrogen outlet was extended from the conduit to the bottom of the reaction solution).

[0041] (3) After the reaction w...

Embodiment 2

[0042] Synthesis of embodiment 2 polyvinyl acetate embolic microspheres

[0043] (1) Put 100 mL of deionized water into a 250 mL three-necked flask connected with a condensing reflux device. Under nitrogen protection, 1.5 g of polyvinyl alcohol 1788 was dissolved in 100 mL of deionized water in a three-necked flask under magnetic stirring (stirring speed: 300-350 rpm).

[0044] (2) 0.2 g of dibenzoyl peroxide (BPO) was stirred and dissolved in 50 mL of vinyl acetate (VAc), and the temperature of the solution in the three-necked flask was heated to 65° C. Then the VAc monomer dissolved with BPO was slowly poured into a three-necked flask, and the temperature of the solution was raised to 70° C. for two hours. Afterwards, the temperature of the solution was raised to 75° C. for two hours.

[0045] (3) After the reaction was finished, the three-necked flask was placed in room temperature and cooled slowly. After the cooling was finished, the reactant in the bottle was transfer...

Embodiment 3

[0046] Synthesis of embodiment 3 polyvinyl acetate embolic microspheres

[0047] (1) Put 100 mL of deionized water into a 250 mL three-necked flask connected with a condensing reflux device. Under nitrogen protection, 2.0 g of polyvinyl alcohol 1788 was dissolved in 100 mL of deionized water in a three-necked flask under magnetic stirring (stirring speed: 300-350 rpm).

[0048] (2) 0.134g of azobisisobutyronitrile (AIBN) was stirred and dissolved in 50mL of vinyl acetate (VAc), and the temperature of the solution in the three-necked flask was heated to 65°C. Then the VAc monomer dissolved with AIBN was slowly poured into a three-necked flask, and the temperature of the solution was raised to 70° C. for two hours. Afterwards, the temperature of the solution was raised to 75° C. for two hours.

[0049] (3) After the reaction was finished, the three-necked flask was placed in room temperature and cooled slowly. After the cooling was finished, the reactant in the bottle was tra...

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Abstract

The invention belongs to the technical field of embolism microsphere preparation, and particularly relates to a preparation method of narrow-particle-size polyvinyl acetate embolism microspheres with controllable drug loading performance. Vinyl acetate monomers are used as raw materials, and a free radical polymerization method and a suspension emulsion polymerization method are effectively combined to prepare the polyvinyl acetate embolization microsphere with the characteristics of good drug loading performance and narrow particle size distribution, and the defects that the current DEB-TACE microsphere product is low in drug loading capacity and wide in particle size distribution range are overcome. The preparation process is simple, the raw material cost is low, and the yield is high; the phase proportion and crystallinity of partially hydrolyzed polyvinyl acetate are controllable; the drug loading process is simple, the applicable drug range is wide, and the drug loading capacity is large; and the drug release process is easy to control, and the burst release phenomenon can be effectively inhibited.

Description

technical field [0001] The invention belongs to the technical field of preparation of embolic microspheres, and in particular relates to a preparation method of narrow-diameter polyvinyl acetate embolic microspheres with controllable drug loading performance. Background technique [0002] Transarterial chemoembolization (TACE) is currently the standard treatment for patients with intermediate-stage hepatocellular carcinoma (Hepatocellular carcinoma, HCC). According to the type of embolic material used, it can be mainly divided into conventional embolization (Conventional TACE, cTACE) and drug-eluting beads TACE (DEB-TACE). cTACE mixes different embolic agents (such as lipiodol, degradable starch microspheres, gelatin, etc.) and antitumor drugs (such as mitomycin, cisplatin, doxorubicin, etc.) In order to achieve the effect of inhibiting tumor growth. DEB-TACE loads anti-tumor drugs into embolic microspheres through the electrostatic interaction between drug molecules and e...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08F118/08C08F2/30A61L24/00A61L24/06
CPCC08F118/08C08F2/30A61L24/06A61L24/0015A61L24/001A61L2300/602A61L2300/416C08L31/04
Inventor 张超刘杨
Owner SUN YAT SEN UNIV
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