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Radiopaque polyvinyl alcohol microsphere

A technology of microspheres and triiodobenzyl alcohol, applied in the field of medicine, can solve the problems of slow absorption rate of medicine, long reaction time and the like

Active Publication Date: 2019-10-25
赵修文
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The present invention aims to solve the problems of long reaction time and slow drug absorption rate of similar microspheres in the past, and specifically provides a radiopaque microsphere and its preparation method. The radiopaque microsphere has the excellent performance of rapidly absorbing drugs

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1 Synthesis of 2,3,5-triiodobenzaldehyde

[0033] (1) Synthesis of 2,3,5-triiodobenzyl alcohol

[0034] in N 2 Under protection, accurately measure BH 3 • THF solution (1.0 M, 10 mmol) was added to a solution of 2,3,5-triiodobenzoic acid (2.5 g, 5 mmol) in 20 mL of THF. After stirring at 25°C for 20 hours, the solution gradually turned milky white. After the reaction, the solution was first added dropwise with absolute ethanol to quench the remaining BH 3 · THF, then dropwise added deionized water for hydrolysis. After rotary evaporation, the product was filtered with a sand core funnel to remove inorganic salts to obtain pure 2,3,5-triiodobenzyl alcohol.

[0035] (2) Synthesis of 2,3,5-triiodobenzaldehyde

[0036] Then pyridinium chlorochromate (PCC) (2.45 g, 11.4 mmol) and dry diatomaceous earth (2.00 g) were weighed, 20 mL of anhydrous dichloromethane was added, and the suspension was stirred at room temperature for 15 minutes. Add 5 mL of anhydrous di...

Embodiment 2

[0037] Embodiment 2 Synthetic 2,3,5-triiodobenzaldehyde

[0038] Change the amount of pyridinium chlorochromate added in step (2) of Example 1 from 11.4mmol to 4.35mmol, that is, the molar ratio of pyridinium chlorochromate to 2,3,5-triiodobenzyl alcohol is 1:1 , the remaining steps and reaction conditions are the same as in Example 1, and the total reaction yield of 2,3,5-triiodobenzaldehyde is 74%.

Embodiment 3

[0039] Example 3 Synthesis of 2,3,5-triiodobenzaldehyde

[0040] The amount of pyridinium chlorochromate added in step (2) of Example 1 is changed from 11.4mmol to 17.4mmol, that is, the molar ratio of pyridinium chlorochromate to 2,3,5-triiodobenzyl alcohol is 4:1 , the remaining steps and reaction conditions are the same as in Example 1, and the total reaction yield of 2,3,5-triiodobenzaldehyde is 82%.

[0041] Known from above-mentioned embodiment 1-3, in the reaction step (2) pyridinium chlorochromate and 2,3,5-triiodobenzyl alcohol molar ratio have significant impact on the total yield of reaction end product, wherein pyridinium chloride When the molar ratio of chromate to 2,3,5-triiodobenzyl alcohol was 2.6:1, the total reaction yield was the highest.

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PUM

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Abstract

The invention relates to a radiopaque polyvinyl alcohol microsphere and a preparation method thereof, wherein the radiopaque polyvinyl alcohol microsphere comprises a polyvinyl alcohol hydrogel bead,2, 3, 5-triiodobenzaldehyde and organic acids. The radiopaque polyvinyl alcohol microspheres prepared by the invention have the advantages of short synthesis time, fast absorption rate of drugs and the like.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a radiopaque microsphere. Background technique [0002] Transcatheter arterial embolization (TAE) is a technique in which embolic agents are injected through a catheter into the blood vessel to be embolized under the guidance of imaging equipment to achieve the desired therapeutic purpose, also known as embolization therapy. Transcatheter arterial chemoembolization (TACE) is a treatment method that combines chemotherapy and embolization. Traditional TACE is an interventional treatment in which chemotherapeutic drugs are first infused locally and then embolized with a blank embolic agent. TACE is one of the main treatment methods for advanced liver cancer. It can effectively prolong the survival period of patients and improve the quality of life of patients. It is currently recognized as the first choice for non-surgical treatment of liver cancer. [0003] Microspheres loaded with chemoth...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C45/29C07C47/55C07C29/147C07C33/46A61L31/18A61L31/16A61L31/04
CPCA61L31/048A61L31/16A61L31/18A61L2300/216A61L2300/23A61L2300/416C07C29/147C07C45/292C08L29/04C07C33/46C07C47/55
Inventor 赵修文邹英华阴国印
Owner 赵修文
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