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Method for loading 5-fluorouracil by using metal-organic framework material

A technology of fluorouracil and organic framework, which is applied in the fields of biomedicine and material chemistry, can solve the problems of high preparation conditions, low drug loading of microspheres, unfavorable organisms, etc., and achieve the effect of simple operation

Inactive Publication Date: 2015-06-10
HARBIN UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

At present, there are many studies on fluorouracil microspheres coated with degradable polymer materials, all of which adopt O / O type and O / W type emulsification volatilization method and spray drying method to prepare fluorouracil polylactic acid microspheres, or use chitosan as the The disadvantage of carrier microspheres is that the microspheres prepared by the O / O type and O / W type emulsification and volatilization method have low drug loading, while the spray drying method requires higher preparation conditions, and the preparation process uses If organic solvents, surfactants and molding agents are removed, some of them will remain in the pharmaceutical preparations, which is harmful to the body.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Preparation of nanoscale metal-organic frameworks (MOFs): Azobenzene-4,4-dicarboxylic acid (0.25mmol) and zinc acetate (0.25mmol), 0.4g sodium dodecyl sulfate were added to polyvinyl fluoride Then add 20ml of N,N'-dimethylformamide, ethanol, and deionized water in a volume ratio of 5:1:0.1, and put it in an oven at 120°C for 12 hours. After cooling, the metal-organic framework crystallite with zinc as the node and azobenzene-4,4-dicarboxylic acid as the organic linker is precipitated. Through particle size measurement, the particle size of the metal-organic framework crystallite is 100-200 nanometers, that is Nanoscale metal-organic framework materials.

[0021] Dissolve 100 mg of 5-fluorouracil in 5 ml of hot water at 90°C, add 200 mg of MOF into the 5-fluorouracil aqueous solution, and cool down to 10°C under stirring with a gradient of 5°C / hour. Membrane filtration, the pore size of the filter membrane is 200 nanometers. The filtrate was centrifuged at a high spee...

Embodiment 2

[0023] Preparation of nanoscale metal-organic frameworks (MOFs): Azobenzene-4,4-dicarboxylic acid (0.25mmol) and zinc acetate (0.25mmol), 0.4g sodium dodecyl sulfate were added to polyvinyl fluoride Then add 20ml of N,N'-dimethylformamide, ethanol, and deionized water in a volume ratio of 5:1:0.1, and put it in an oven at 120°C for 12 hours. After cooling, the metal-organic framework crystallite with zinc as the node and azobenzene-4,4-dicarboxylic acid as the organic linker is precipitated. Through particle size measurement, the particle size of the metal-organic framework crystallite is 100-200 nanometers, that is Nanoscale metal-organic framework materials.

[0024] Dissolve 100 mg of 5-fluorouracil in 3 ml of hot water at 90°C, add 300 mg of MOF into the 5-fluorouracil aqueous solution, and cool down to 10°C under stirring with a gradient of 5°C / hour. Membrane filtration, the pore size of the filter membrane is 200 nanometers. The filtrate was centrifuged at a high spee...

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Abstract

The invention relates to a method for loading 5-fluorouracil by using a metal-organic framework material. The method comprises the following steps: adding the nanoscale metal-organic framework material (MOF) synthesized by a hydrothermal method into a 5-fluorouracil aqueous solution; and carrying out operations such as stirring, gradient cooling, filtering, centrifugalizing, freezing and drying and the like to prepare the MOF / 5-fluorouracil compound. The drug loading method has the advantages of controlled drug release, simple operation, no organic solvents and the like.

Description

technical field [0001] The invention relates to a method for loading 5-fluorouracil by using a metal-organic framework material, and belongs to the fields of biomedicine and material chemistry. Background technique [0002] 5-Fluorouracil is a broad-spectrum antitumor drug, especially for digestive system tumors, such as the basic drug for chemotherapy of liver cancer. At present, there are many disadvantages in the clinical use of 5-fluorouracil, such as difficult absorption after oral administration, fast metabolism in the body, short half-life (only 5-10 minutes), toxic and side effects, etc., and it needs large doses of long-term intravenous infusion to reach the effective concentration in the body and duration of action. In order to reduce the toxic and side effects of 5-fluorouracil and improve the utilization rate of the drug, it can be mixed with biodegradable polymer materials to make drug-loaded microspheres with sustained release, and the drug can be enriched aro...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K9/19A61K31/513A61P35/00
Inventor 张凤鸣丁为民刘欣李雪薇刘霞
Owner HARBIN UNIV OF SCI & TECH
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