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Polymer-modified mesoporous carbon nanoparticle and preparation and application thereof

A mesoporous carbon and polymer technology, applied in the field of medicine, can solve the problems of poor water solubility, low bioavailability, and the treatment of diseases that affect the clinical efficacy of drugs

Active Publication Date: 2019-05-28
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, a considerable number of drugs, due to their poor water solubility, are difficult to absorb in the gastrointestinal tract, resulting in low bioavailability, which seriously affects the clinical efficacy of drugs and the treatment of diseases.

Method used

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  • Polymer-modified mesoporous carbon nanoparticle and preparation and application thereof
  • Polymer-modified mesoporous carbon nanoparticle and preparation and application thereof
  • Polymer-modified mesoporous carbon nanoparticle and preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Add 20mL of distilled water, 0.1mL of ammonia water, 4mL of absolute ethanol and 1g of 25% CTAC solution into the Erlenmeyer flask, stir at room temperature for 20min, then add 0.2g of resorcinol and continue stirring for 30min. Measure 0.36mL tetraethyl orthosilicate (TEOS) and 0.28mL formaldehyde solution and add dropwise to the above reaction solution, place in a water bath and heat to 30°C, and keep stirring for 24h. After the reaction, the obtained product was centrifuged, washed twice with distilled water and absolute ethanol, and the precipitate was collected and dried in an oven. The resulting solid was ground, sieved, and 2 Carbon-silicon mixture was obtained by carbonizing at a high temperature of 700° C. for 3 hours under the same conditions, and soaking the carbon-silicon mixture in 10% hydrofluoric acid solution for 24 hours to remove the silica template to obtain spherical mesoporous carbon.

Embodiment 2

[0054] Add 20 mL of distilled water, 0.1 mL of ammonia water, 6 mL of absolute ethanol and 1 g of 25% CTAC solution into the Erlenmeyer flask, stir at room temperature for 20 min, then add 0.2 g of resorcinol and continue stirring for 30 min. Measure 0.36mL tetraethyl orthosilicate (TEOS) and 0.28mL formaldehyde solution and add dropwise to the above reaction solution, place in a water bath and heat to 30°C, and keep stirring for 24h. After the reaction, the obtained product was centrifuged, washed twice with distilled water and absolute ethanol, and the precipitate was collected and dried in an oven. The resulting solid was ground, sieved, and 2 Carbon-silicon mixture was obtained by carbonizing at a high temperature of 700° C. for 3 hours under the same conditions, and soaking the carbon-silicon mixture in 10% hydrofluoric acid solution for 24 hours to remove the silica template to obtain spherical mesoporous carbon.

Embodiment 3

[0056] Add 20mL of distilled water, 0.1mL of ammonia water, 8mL of absolute ethanol and 1g of 25% CTAC solution into the Erlenmeyer flask, stir at room temperature for 20min, then add 0.2g of resorcinol and continue stirring for 30min. Measure 0.36mL tetraethyl orthosilicate (TEOS) and 0.28mL formaldehyde solution and add dropwise to the above reaction solution, place in a water bath and heat to 30°C, and keep stirring for 24h. After the reaction, the obtained product was centrifuged, washed twice with distilled water and absolute ethanol, and the precipitate was collected and dried in an oven. The resulting solid was ground, sieved, and 2 Carbon-silicon mixture was obtained by carbonizing at a high temperature of 700° C. for 3 hours under the same conditions, and soaking the carbon-silicon mixture in 10% hydrofluoric acid solution for 24 hours to remove the silica template to obtain spherical mesoporous carbon.

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Abstract

The invention belongs to the technical field of medicine, and relates to preparation of mesoporous carbon with an adjustable particle size, and preparation of a Polymer-modified mesoporous carbon nanoparticle and application thereof as a poorly soluble drug carrier to promoting oral absorption. First, the mesoporous carbon with a particle size ranging from 50 to 1000 nm is prepared by adjusting the formulation process using a 'one-step method'. After the prepared mesoporous carbon is carboxylated, polyethyleneimine-polyacrylic acid is modified on the surface of the carboxylated carbon sphere by a classical EDC-NHS amide reaction to obtain the polymer-modified mesoporous carbon nanoparticle. The polymer-modified mesoporous carbon prepared by the invention has no stimulating effect on the gastrointestinal tract and is non-cytotoxic, and is suitable for use as an oral drug carrier. The poorly soluble drug (fenofibrate) is loaded into the polymer-modified mesoporous carbon by a solvent evaporation method to achieve high drug dispersion. The drug carrying system can significantly increase the dissolution rate and oral bioavailability of the drug.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to the preparation of mesoporous carbon with adjustable particle size, the preparation of polymer-modified mesoporous carbon and its application as an insoluble drug carrier to promote oral absorption. Background technique [0002] As we all know, oral administration has become the most widely used administration method because of its convenience and easy acceptance by patients, and it is also the preferred administration route for most drugs. However, a considerable number of drugs, due to their poor water solubility, are difficult to absorb in the gastrointestinal tract, resulting in low bioavailability, which seriously affects the clinical efficacy of drugs and the treatment of diseases. Therefore, how to improve the oral bioavailability of poorly soluble drugs has become one of the key problems to be solved urgently in the field of pharmacy. Emerging nanotechnology brings great ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/04A61K31/216
Inventor 王思玲赵勤富崔羽
Owner SHENYANG PHARMA UNIVERSITY
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