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A kind of 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 complex structure, low drug loading of Callisphere, and high preparation cost, and achieve simple preparation process, Applicable to a wide range of drugs and the effect of large drug loading

Active Publication Date: 2022-07-26
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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  • A kind of preparation method of narrow particle size polyvinyl acetate embolization microspheres with controllable drug loading performance
  • A kind of preparation method of narrow particle size polyvinyl acetate embolization microspheres with controllable drug loading performance
  • A kind of 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] Embodiment 1 Synthesis of polyvinyl acetate embolization 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 of 300-350 rpm).

[0040](2) 0.134 g of azobisisobutyronitrile (AIBN) was dissolved in 50 mL of vinyl acetate (VAc) with stirring, and the temperature of the solution in the three-necked flask was heated to 65°C. Then the VAc monomer dissolved in AIBN was slowly poured into the three-necked flask, and the temperature of the solution was raised to 70°C for two hours, and then the temperature of the solution was raised to 75°C for two hours; during the reaction, it should be kept Nitrogen bubbling was continued (the nitrogen outlet extended from the conduit to the bottom of the reaction solution).

...

Embodiment 2

[0042] Embodiment 2 Synthesis of polyvinyl acetate embolization 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 of 300-350 rpm).

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

[0045] (3) After the reaction is completed, the three-necked flask is placed in a room temperature environment and slowly cooled. After cooling, the reactants in the bottle were tran...

Embodiment 3

[0046] Embodiment 3 Synthesis of polyvinyl acetate embolization 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 of 300-350 rpm).

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

[0049] (3) After the reaction is completed, the three-necked flask is placed in a room temperature environment and slowly cooled. After cooling, the reactants in the bottl...

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Abstract

The invention belongs to the technical field of the preparation of embolization microspheres, and in particular relates to a preparation method of narrow-diameter polyvinyl acetate embolization microspheres with controllable drug-loading properties. The polymerization method and the suspension emulsion polymerization method are effectively combined to prepare a polyvinyl acetate embolization microsphere with good drug loading performance and narrow particle size distribution, which solves the problem of low drug loading in the current DEB‑TACE microsphere products. , the disadvantage of a wide range of particle size distribution. The preparation process of the invention is simple, the cost of raw materials is low, and the output is large; the proportion and crystallinity of the 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; the drug release process is easy to control , which can effectively suppress the bursting phenomenon.

Description

technical field [0001] The invention belongs to the technical field of the preparation of embolization microspheres, and in particular relates to a preparation method of narrow particle size polyvinyl acetate embolization microspheres with controllable drug-carrying properties. Background technique [0002] Transarterial chemoembolization (TACE) is currently the standard treatment for patients with intermediate-stage hepatocellular carcinoma (HCC). According to the type of embolization material used, it can be mainly divided into traditional embolization (Conventional TACE, cTACE) and drug-eluting beads TACE (DEB-TACE). cTACE works by mixing different embolic agents (such as lipiodol, degradable starch microspheres, gelatin, etc.) with antitumor drugs (such as mitomycin, cisplatin, doxorubicin, etc.), and then injecting them into tumor blood vessels to inhibit tumor growth. DEB-TACE loads antitumor drugs into the embolic microspheres through the electrostatic interaction b...

Claims

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Application Information

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Patent Type & Authority Patents(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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