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Preparation and applications of oral absorption enhancer built based on natural P-glycoprotein inhibitor

A technology of glycoprotein inhibitor and absorption enhancer, which is applied in the field of biomedical materials to achieve the effects of promoting absorption, improving solubility and easy operation

Inactive Publication Date: 2014-12-24
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, oral administration is easily affected by drug solubility, permeability, gastrointestinal environment, intestinal P-glycoprotein (P-gp) efflux, and liver metabolic system.

Method used

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  • Preparation and applications of oral absorption enhancer built based on natural P-glycoprotein inhibitor
  • Preparation and applications of oral absorption enhancer built based on natural P-glycoprotein inhibitor
  • Preparation and applications of oral absorption enhancer built based on natural P-glycoprotein inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] The synthesis of embodiment 1 carboxymethyl chitosan-quercetin conjugate

[0049] Weigh an appropriate amount of carboxymethyl chitosan and place it in a reaction bottle, add 10 mL of distilled water to swell overnight. Add quercetin in DMF under cold water bath and stirring, then add DMAP (5% of the mass of the reactant), EDC and NHS (EDC:NHS=1:1.4), react at room temperature for 30 minutes, and stir for 24 hours in the dark. After the reaction, the reaction product was precipitated with acetone, and the precipitate was obtained by suction filtration. The precipitate was washed with acetone until it was colorless, and then the reaction product was washed with absolute ethanol until it was colorless. After the solvent was drained, the reaction product was dissolved in water, and the probe was sonicated for 20 minutes in an ice bath, centrifuged at 3000 rpm for 10 minutes, the supernatant was passed through a 0.8 μm filter membrane, and the filtrate was transferred to a ...

Embodiment 2

[0050] The synthesis of embodiment 2 carboxymethyl chitosan-emodin conjugate

[0051] Weigh an appropriate amount of carboxymethyl chitosan and place it in a reaction bottle, add 10 mL of distilled water to swell overnight. Add emodin ethanol solution under cold water bath and stirring, then add DMAP (5% of the reactant mass), EDC and NHS (EDC:NHS=1:2), react at room temperature after 30min, and stir for 24h in the dark. After the reaction, the reaction product was precipitated with acetone, and the precipitate was obtained by suction filtration. The precipitate was washed with acetone until it was colorless, and then the reaction product was washed with absolute ethanol until it was colorless. After the solvent was drained, the reaction product was dissolved in water, and the probe was sonicated for 20 minutes in an ice bath, centrifuged at 3000 rpm for 10 minutes, the supernatant was passed through a 0.8 μm filter membrane, and the filtrate was transferred to a dialysis bag ...

Embodiment 3

[0052] The synthesis of embodiment 3 carboxymethyl chitosan-baicalein conjugates

[0053] Weigh an appropriate amount of carboxymethyl chitosan and place it in a reaction bottle, add 10 mL of distilled water to swell overnight. Add the DMF solution of baicalein in a cold water bath with stirring, then add DMAP (5% of the mass of the reactant), EDC and NHS (EDC:NHS=1:3), react at room temperature for 30 minutes, and stir for 12 hours in the dark. After the reaction, the reaction product was precipitated with acetone, and the precipitate was obtained by suction filtration. The precipitate was washed with acetone until it was colorless, and then the reaction product was washed with absolute ethanol until it was colorless. After the solvent was drained, the reaction product was dissolved in water, and the probe was sonicated for 20 minutes in an ice bath, centrifuged at 3000 rpm for 10 minutes, the supernatant was passed through a 0.8 μm filter membrane, and the filtrate was trans...

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Abstract

The invention relates to a preparation method and applications of an oral absorption enhancer built based on a natural P-glycoprotein (P-gp) inhibitor. The preparation method is implemented through grafting natural small molecules with a P-gp efflux inhibition function to a chitosan derivative through chemical coupling, so that the oral absorption enhancer with a P-gp efflux inhibition function is synthesized. The oral absorption enhancer has the following characteristics: (1) after the small molecules with the P-gp efflux inhibition function are coupled with the chitosan derivative, a synthesized conjugate has the P-gp efflux inhibition function, and can promote the absorption of drugs in gastrointestinal tracts by inhibiting the efflux of P-gp; (2) the synthesized conjugate can be independently used as a new polymer drug; and (3) the synthesized conjugate has amphipathy, and can be self-assembled in water so as to form a micelle for encapsulating a hydrophobic antitumor drug, so that the water solubility of drugs is increased, the drug intake of gastrointestinal tracts is increased, and the bioavailability of drugs is improved. The preparation method disclosed by the invention is simple, low in cost, and suitable for large-scale continuous production.

Description

[0001] Technical field: The present invention belongs to the field of biomedical materials, and specifically relates to a preparation method of an oral absorption enhancer based on a natural P-glycoprotein inhibitor and its application in promoting the oral absorption of antineoplastic drugs. Background technique: [0002] With the urbanization and industrialization of society, the increase of environmental pollution and various food additives, and the impact of people's unhealthy lifestyle and behavior habits, malignant tumors have become a serious threat to human life and health and bring heavy burdens to families and society. one of the diseases. The incidence and mortality of malignant tumors are increasing year by year. At present, the main way of administration of chemotherapy is intravenous injection, and due to the limitation of low bioavailability of drugs, the development of oral administration is relatively slow. [0003] Oral administration is convenient to use, h...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K47/36A61P35/00
Inventor 姚静周建平王晓颖
Owner CHINA PHARM UNIV
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