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Method for synthesizing polyvinyl alcohol embolization microspheres capable of loading chemotherapeutic drug pirarubicin

A technology of polyvinyl alcohol embolization microspheres and pirarubicin, which is applied in the field of medical materials, can solve the problems of incomplete arterial blockage, large liver tissue damage, and easy absorption by tumor tissue, etc. Smooth, Inexpensive Effects

Inactive Publication Date: 2018-07-03
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

At present, lipiodol is still the most commonly used TACE treatment for liver cancer in China, which has disadvantages such as insufficient thorough arterial occlusion, great damage to normal liver tissue, and easy absorption by tumor tissue in a short period of time.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Add 150 g of polyvinyl alcohol into a flask filled with pure water, stir and disperse evenly. Heat up to 96°C, after the polyvinyl alcohol is completely dissolved, cool down to below 25°C, add 3.0g of intermediate acrylamidoalkyldialkoxy acetal, N-acrylamidodimethoxy Ethyl acetal 3.0g, after stirring for 10 minutes, add 100ml of concentrated hydrochloric acid dropwise to the solution, continue to stir for 6 hours after the dropwise addition, then collect the crude product, wash and dry to obtain the desired functionalized macromolecular hydrogel (referred to as Calli-B).

Embodiment 2

[0020] Add 12 g of sodium 2-acrylamide-2-methylpropanesulfonate and 10 g of potassium persulfate into water in sequence, dissolve and mix evenly, then add 100 g of the functionalized macromolecular gel intermediate (Calli-B) prepared in Example 1 and stir evenly to obtain a polymer monomer solution. Add 10 g of butyl acetate and 5 g of cellulose acetate into the reaction vessel, and feed N at the same time. 2 Gas, stirring, heating, and then sequentially add the above-mentioned polymer monomer solution and tetramethylethylenediamine to form an oil-water mixed reaction system, heating and stirring for 3 hours. In this reaction, the stirring paddle is an axial-flow stirring paddle, the stirring speed is controlled at 450-500 rpm, and the temperature of the reaction system is controlled at 48-60° C. when the polymer monomer solution is added. After the reaction is finished, the reaction mixture is filtered to collect the microspheres, washed with butyl acetate, ethyl acetate and...

Embodiment 3

[0022] Dissolve 10mg pirarubicin in 2.0ml pure water, take the microsphere embolism synthesized in Example 2, accurately weigh 0.25g, put it into a 20ml vial, add 2ml of the above-mentioned pirarubicin solution, and make The microspheres were soaked in the pirarubicin solution, and the mixture was shaken occasionally. Use a micro-syringe to regularly sample 20 μL at the 5th, 10th, 20th, 40th, and 60th minute, add 5.0ml of pure water to dilute, measure the absorbance at 485nm, and substitute the absorbance into the standard curve equation to calculate the concentration of the drug contained in the sample. The drug-loaded amount of pirarubicin on the ball: drug-loaded amount=(drug-loaded solution-drug-loaded solution-drug-loaded solution) / microsphere weight. The measured microsphere loading pirarubicin drug loading is 67mg / gram microsphere.

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PUM

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Abstract

The invention relates to a method for synthesizing polyvinyl alcohol embolization microspheres capable of loading a chemotherapeutic drug pirarubicin. According to the present invention, based on theproblem of the loading of the chemotherapeutic drug pirarubicin by the existing polyvinyl alcohol embolization microspheres, a purpose of the present invention is to solve the disadvantage of the lowpirarubicin loading of the polyvinyl alcohol embolization microspheres; the technical scheme comprises that a ratio of a functionalized macromolecular hydrogel (Calli-B) to a drug-loading group 2-acrylamide-2-methyl propyl sodium sulfonate is 1.00:0.12, an axial flow type stirring paddle is selected, the stirring speed is controlled at 450-500 rpm, and the temperature of the reaction system is controlled at 48-60 DEG C when a polymer monomer solution is added; and by researching the use amount ratio of the drug-loading group 2-acrylamide-2-methyl propyl sodium sulfonate and the process, the problem of the loading of the pirarubicin in the polyvinyl alcohol embolization microspheres is solved, the microspheres can achieve a certain drug loading amount according to the requirements, and thedrug-loading microspheres can continuously release pirarubicin to the targeting tumor area at the tumor site, and are used for the drug-eluting bead transarterial chemoembolization on liver cancer.

Description

technical field [0001] The invention relates to a synthesis method of polyvinyl alcohol embolization microspheres capable of loading chemotherapeutic drug pirarubicin, and belongs to the technical field of medical materials. Background technique [0002] Minimally invasive interventional therapy is becoming more and more widely used in the field of medical technology, especially in the treatment of cancer tumors rich in blood vessels such as liver cancer, kidney cancer, and uterine fibroids, and has become an important tool for the treatment of tumors that cannot be surgically removed. preferred alternative to . The principle is to use high-definition medical imaging equipment to guide the catheter through the artery to the tumor site in the human body, and then infuse the embolism agent of anti-tumor drugs through the catheter to block the blood supply of the tumor tissue, so that the tumor shrinks in a short time. Therapeutic purposes of necrosis. [0003] In recent year...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61L24/06A61K9/16A61K47/32A61K31/7048A61P35/00
CPCA61L24/06A61K9/1635A61K31/7048A61L24/001A61L24/0015A61L2300/416A61L2300/60C08L51/003
Inventor 郁娅卿
Owner SUZHOU HENGRUI CALLISYN BIOLOGICAL MEDICINE TECH CO LTD
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