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Preparation method of surface-functionalized elution micro-spheres capable of carrying drugs

A technology of surface functionalization and microspheres, which is used in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc., to achieve the effects of product purity, complete reaction, and improved drug loading rate.

Active Publication Date: 2016-11-16
CHANGSHA JINGYI PHARM TECH CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] In view of the defects in the preparation and performance of the current elution microspheres, this patent synthesized a surface-functionalized drug-loaded elution microspheres

Method used

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  • Preparation method of surface-functionalized elution micro-spheres capable of carrying drugs
  • Preparation method of surface-functionalized elution micro-spheres capable of carrying drugs
  • Preparation method of surface-functionalized elution micro-spheres capable of carrying drugs

Examples

Experimental program
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Effect test

Embodiment 1

[0030] 1) Preparation of carboxymethyl chitosan microspheres:

[0031] Weigh 1.0 g of polyethylene glycol diglycidyl ether, add it to 10 ml of 4% carboxymethyl chitosan solution, and stir magnetically for 20 min at room temperature to mix the two evenly. Measure 40ml of n-heptane and put it into a 250ml three-necked flask, then add 0.27g (accounting for 1% of the mass of the oil phase) emulsifier APG0810, and stir mechanically at a speed of 300rad / min. After the emulsifier is uniformly dispersed, the above mixture is gradually dropped into n-heptane, emulsified and cross-linked at 30°C, and cross-linked for 24 hours. After the reaction, use a large amount of ethanol to break the emulsion, clean the microspheres, and wash repeatedly Finally, the microspheres were dried in a vacuum oven at 35°C for 24 hours, and the particle size of the obtained microspheres was concentrated at 350um.

[0032] 2) Preparation of surface functionalized drug-loaded eluted microspheres:

[0033] W...

Embodiment 2

[0035] Change 4% carboxymethyl chitosan solution into 1% carboxymethyl chitosan solution in embodiment 1, other consumption and its synthetic process are identical with embodiment 1.

Embodiment 3

[0037] Change 4% carboxymethyl chitosan solution into 2% carboxymethyl chitosan solution in embodiment 1, other consumption and its synthetic process are identical with embodiment 1.

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Abstract

The invention discloses a preparation method of surface-functionalized elution micro-spheres capable of carrying drugs, relating to the field of bio-medical materials. The preparation method comprises the following steps: (1) by taking carboxymethyl chitosan as a raw material and polyethylene glycol diglycidyl ether as a cross-linking agent, preparing cross-linking carboxymethyl chitosan micro-spheres of which the particle sizes are mainly distributed in 300-400mu m by a reverse micro-suspension cross-linking method; and (2) putting the prepared dry cross-linking carboxymethyl chitosan micro-spheres into an aqueous solution of 2-acrylamide-2-methylpropanesulfonic acid for soaking, and carrying out graft polymerization on the 2-acrylamide-2-methylpropanesulfonic acid on the surfaces of the micro-spheres by taking ammonium ceric nitrate as an initiator, so as to modify the micro-spheres. As the surfaces of the micro-spheres, modified by graft polymerization, have a large number of sulfonic acid groups, drugs with positive charges, such as doxorubicin hydrochloride, can be effectively carried, so that the elution micro-spheres can be hopefully prepared.

Description

technical field [0001] The invention relates to a preparation method of a biodegradable drug carrier, relates to the field of biomedicine, in particular to a preparation method of surface-functionalized drug-loaded elution microspheres. Background technique [0002] Primary liver cancer is a common malignant tumor with high morbidity and mortality. The global incidence of liver cancer is increasing year by year. my country is the country with the highest incidence and the highest number of deaths from liver cancer in the world. The incidence of liver cancer has become the third largest malignant tumor in terms of mortality after gastric cancer and lung cancer. The disease seriously threatens people's health. The common treatment for tumors is surgical resection, but for patients with advanced tumors, interventional therapy (ranscatheterarterial chemoembolization, TACE) is an ideal treatment. Interventional therapy refers to transcatheter arterial chemoembolization, that is,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/704A61K47/18A61K47/26A61P35/00
CPCA61K31/704A61K47/183A61K47/26A61K9/50A61K47/50A61K47/61A61P35/00A61K9/1617A61K9/1652A61K9/1682
Inventor 倪才华曹元龙石刚张丽萍
Owner CHANGSHA JINGYI PHARM TECH CO LTD
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