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Amphiphilic xylan carrier and preparation method thereof

A xylan and amphiphilic technology, which is applied in the field of amphiphilic xylan carrier and its preparation, can solve the problem that xylan is not suitable as a drug carrier, and can improve the release capacity, bioavailability and drug release capacity. Enhanced, poorly soluble effects

Active Publication Date: 2021-07-09
ZHEJIANG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Aiming at the problem that existing xylan is not suitable as a drug carrier, etc., the object of the present invention is to provide a method for preparing an amphiphilic xylan carrier with xylan as a skeleton, and the prepared amphiphilic xylan carrier With high drug loading capacity, it can improve the dissolution rate of poorly soluble drugs, protect the drug from the physiological environment of the gastrointestinal tract, have the potential to deliver the drug to the colon, and improve the bioavailability of the drug. It can be used to carry drugs for the treatment of colitis, colon cancer, etc.

Method used

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  • Amphiphilic xylan carrier and preparation method thereof
  • Amphiphilic xylan carrier and preparation method thereof
  • Amphiphilic xylan carrier and preparation method thereof

Examples

Experimental program
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Embodiment example 1

[0045] (1) The sodium hydroxide solution of 0.66g xylan and 3.0ml20% concentration carries out alkalization reaction, and the NaOH mol ratio in xylan and solution is 1:3, and reaction temperature is 25 ℃, and the reaction time is 30 minutes; After the reaction temperature was increased to 70° C., 17.5 g of sodium chloroacetate was added for reaction. The mol ratio of xylan and sodium chloroacetate in the system is 1:3, and the reaction time is 75 minutes, obtains reaction system;

[0046] (2) Adjust the pH value of the reaction system obtained in step (1) to neutral with 4% dilute acetic acid, precipitate the product with 15ml of absolute ethanol, wash the precipitate four times with 95% ethanol, and dissolve the precipitate in 10ml of distilled water , dialyzed in a deionized water environment for 4 days, and the resulting solution was freeze-dried to obtain carboxymethylxylan (abbreviated as CX);

[0047] (3) 0.2g CX was dissolved in 50ml deionized water, and the pH value o...

Embodiment example 2

[0062] (1) 0.66g xylan is alkalized with 2.7ml 30% sodium hydroxide solution, the molar ratio of xylan to NaOH in the solution is 1:4, the reaction temperature is 40°C, and the reaction time is 40 minutes; After raising the reaction temperature to 85°C, add 2.33g of sodium chloroacetate for reaction, the molar ratio of xylan and sodium chloroacetate in the system is 1:4, and the reaction time is 90 minutes;

[0063] (2) Adjust the pH value of the above reaction system to neutral with 6% dilute acetic acid, precipitate the product with 15ml of absolute ethanol, wash the precipitate four times with 95% ethanol, dissolve the precipitate in 10ml of distilled water, and deionize Dialysis in water environment for 4 days. The resulting solution is freeze-dried to obtain carboxymethylxylan (CX);

[0064] (3) Dissolve 0.2g CX in 50ml deionized water, adjust the pH value of the solution to 7.8 with 2% NaOH solution, H 2 SO 4 Dilute to 7% and use as titrant. Stop titration when the p...

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Abstract

The invention discloses an amphiphilic xylan carrier and a preparation method thereof. The method comprises the following steps: (1) alkalifying xylan through NaOH, then reacting xylan with sodium chloroacetate, introducing a hydrophilic group carboxymethyl, calculating the substitution degree of carboxymethyl xylan through a titration method, and dialyzing and freeze-drying the product to obtain purified carboxymethyl xylan; and (2) activating fatty acid by using DIC and DMAP, reacting the activated fatty acid with carboxymethyl xylan so as to introduce a hydrophobic group fatty acid carbon chain into carboxymethyl xylan, and dialyzing and freeze-drying the product to obtain the purified amphiphilic xylan carrier. The obtained amphiphilic xylan carrier has high drug encapsulation efficiency, can keep the drug stable in the pH environment of the stomach and the small intestine and release the drug in the pH environment of the colon, and can significantly improve the cytotoxicity and bioavailability of the drug.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to an amphiphilic xylan carrier with certain colon targeting performance and a preparation method thereof. Background technique [0002] Xylan, the main component of hemicellulose, is one of the most abundant biopolymers present in biomass waste. The characteristic structure of xylan generally contains a D-xylose backbone connected by β-(1→4) glycosidic bonds. According to various data, the backbone can be substituted by various sugar units and side groups, such as arabinose, glucuronic acid, and acetyl groups. The structural formula of xylan is as follows: [0003] [0004] Because xylan has the advantages of anti-oxidation, biocompatibility, non-toxicity and biodegradability, the application of xylan in the field of medicine has attracted great attention. It has been reported that xylan cannot be degraded in the stomach and small intestine bec...

Claims

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Application Information

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IPC IPC(8): C08B37/00A61K47/36A61P1/00A61P29/00A61P35/00
CPCC08B37/0057A61K47/36A61P1/00A61P29/00A61P35/00
Inventor 张琦红苏晨苏为科俞静波
Owner ZHEJIANG UNIV OF TECH
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