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Functionally degradable medicine elution microsphere and preparation method thereof

A functionalized, microsphere technology, applied in the fields of polymer materials and biomedical engineering, can solve the problems of short sustained release period and low drug content in microspheres, and achieve the goal of increasing the surface area, improving the ability of adsorbing drugs, and improving drug content. Effect

Active Publication Date: 2021-01-05
SHANDONG RIENTECH MEDICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

By increasing the amount of charge and optimizing the structure of microspheres, the problems of low drug content in microspheres and short sustained release period are solved, and the therapeutic effect is significantly improved.

Method used

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  • Functionally degradable medicine elution microsphere and preparation method thereof
  • Functionally degradable medicine elution microsphere and preparation method thereof
  • Functionally degradable medicine elution microsphere and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Example 1 Preparation of a lactide-glycolide copolymer with a molecular weight of 2000 activated by the carboxyl group

[0051] Dissolve the lactide-glycolide copolymer with a molecular weight of 2000 and DCC in dichloromethane at a molar ratio of 1:1, react at 4°C for 0.2h, then add 1 equivalent (DCC) of NHS, and continue the reaction for 10h , The obtained product was precipitated in ethanol, and the white solid obtained after vacuum drying was a lactide-glycolide copolymer with a molecular weight of 2000 and an amino group at the end.

Embodiment 2

[0052] Example 2 Preparation of a polylactide-polyethylene glycol block copolymer with a molecular weight of 40,000 activated by the carboxyl group

[0053] Dissolve the lactide-glycolide copolymer with a molecular weight of 40000 and DCC in ethyl acetate at a molar ratio of 1:50, react at 4°C for 0.1h, then add 1.5 equivalents (DCC) of NHS, and continue the reaction for 5h , the obtained product was precipitated in ethanol, and the white solid obtained after vacuum drying was a polylactide-polyethylene glycol block copolymer with an amino terminal group and a molecular weight of 40,000.

Embodiment 3

[0054] Example 3 Preparation of glycolide-caprolactone copolymer with a molecular weight of 400,000 activated by the carboxyl group

[0055] The lactide-glycolide copolymer with a molecular weight of 400,000 and DCC were dissolved in acetone at a molar ratio of 1:25, reacted at 4°C for 0.3h, then added 2 equivalents (DCC) of NHS, and continued to react for 12h. The obtained product is precipitated in ethanol, and the white solid obtained after vacuum drying is a glycolide-caprolactone copolymer with an amino group at the end and a molecular weight of 400,000.

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Abstract

The invention relates to a functionally degradable medicine elution microsphere and a preparation method thereof, and belongs to the field of medical high molecular materials. Firstly, the high molecular material is subjected to surface modification so as to increase the sulfonic acid group content of the high molecular material and improve an amount of the negative charges of the high molecular material, the capacity of the material to adsorb medicines can be improved, and medicine releasing time is prolonged. The porous microsphere prepared by an improved solvent volatilization method enlarges a medicine contact surface area and improves an amount of microsphere medicines. The surface of the porous microsphere prepared by the preparation method disclosed by the invention is provided witha great quantity of sulfonic acid groups, so that the medicine containing the positive charges can be effectively loaded, and the porous microsphere has a good application prospect in interventionalmedical science.

Description

technical field [0001] The invention belongs to the fields of polymer materials and biomedical engineering, and in particular relates to a functional degradable drug-eluting microsphere and a preparation method thereof. Background technique [0002] The morbidity and mortality of primary liver cancer are gradually increasing, and currently ranks 4th to 5th in the incidence of tumors in the world, especially in Asia and Africa. my country is a country with a high incidence of hepatitis B, and about half of the new cases of liver cancer occur in my country every year. The research results show that the incidence of liver cancer in my country may still increase, and the total number of new cases of liver cancer will increase. Transarterial chemoembolization (TACE) has been used in the treatment of hepatocellular carcinoma (HCC) for more than 30 years. The treatment of choice for advanced hepatocellular carcinoma. TACE includes traditional TACE (iodol + chemotherapeutic drugs...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K47/34A61K45/00A61P35/00C08G81/00
CPCA61K9/1641A61K9/1647A61K45/00A61P35/00C08G81/00C08G2230/00
Inventor 张海军周超张军伟冯相蓺其他发明人请求不公开姓名
Owner SHANDONG RIENTECH MEDICAL TECH
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