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Starch based segmented intestine targeting specific adhesion material, preparation and application thereof

A technology of colon targeting and adhering materials, which is applied to natural polymer materials in the field of medicine to achieve the effects of good biocompatibility, improved colon targeting and improved bioavailability

Active Publication Date: 2009-02-18
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The research work on starch-based colon targeting-specific adhesion carrier materials has not been reported at home and abroad

Method used

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  • Starch based segmented intestine targeting specific adhesion material, preparation and application thereof
  • Starch based segmented intestine targeting specific adhesion material, preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] (1) Preparation of anti-digestible starch: mix starch and water in a mixing tank through mechanical stirring, so that the water mass percentage is controlled between 10% and 95% (w / w, calculated on dry basis of starch), and then the temperature range The temperature is 30-140°C, the pressure range is 0.5-3MPa, and the modification is performed for 0.1-4h; the treated material is transported to the enzyme reactor, fully enzymolyzed with heat-resistant α-amylase and glucoamylase, and then centrifuged, Resistant starch obtained after washing, filtering, drying and crushing.

[0023](2) Preparation of starch-based colon targeting-specific adhesive material: disperse the anti-digestible starch prepared above in 50% (w / w, based on the dry basis of anti-digestible starch) distilled water, at a temperature of 20 ° C, pH Under the condition of 2, add glutaraldehyde with a mass volume concentration of 1% (g / L, based on the dry basis of digestible starch) to activate the alcoholic...

Embodiment 2

[0025] Weigh the anti-digestive starch prepared in Example 1, disperse it in 80% (w / w, based on the dry basis of anti-digestive starch) distilled water, and add a mass volume concentration of 10% (g / L, based on the dry basis of the digestible starch) glutaraldehyde activates the alcoholic hydroxyl group of the digestible starch. After reacting for 6 hours, after fully washing with phosphate buffer, add 5% concanavalin A ( w / w (based on the dry basis of resistant starch) for coupling, the temperature of the coupling reaction is 30°C, the coupling time is 30h, and the starch material is obtained after the reaction is complete; the starch material is centrifuged and washed with phosphate buffer, and ethanolamine is added The unreacted activating group in the inactivated starch material is centrifuged and washed and then vacuum-dried to obtain a white powdery starch-based colon targeting-specific adhesion material.

Embodiment 3

[0027] Weigh the anti-digestive starch prepared in Example 1, disperse it in 60% (w / w, based on the dry basis of anti-digestive starch) distilled water, and add a mass volume concentration of 6% (g / L, based on the dry basis of digestible starch) glutaraldehyde activates the alcoholic hydroxyl group of digestible starch. After reacting for 4 hours, after fully washing with phosphate buffer, add 3% concanavalin A ( w / w (based on the dry basis of resistant starch) for coupling, the temperature of the coupling reaction is 20°C, the coupling time is 20h, and the starch material is obtained after the reaction is complete; the starch material is centrifuged and washed with phosphate buffer, and ethanolamine is added The unreacted activating group in the inactivated starch material is centrifuged and washed and then vacuum-dried to obtain a white powdery starch-based colon targeting-specific adhesion material.

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Abstract

The invention discloses a starch based colon idiosyncratic adhesion material for coupling concanavalin A and a method for preparing the same. The anti-digestion starch undergoes the activating treatment by glutaraldehyde, couples with the concanavalin A and is subjected to centrifuge washing by phosphate buffer and inactivation by ethanolamine to obtain the starch based colon idiosyncratic adhesion material. The invention also discloses application of the starch based colon targeting idiosyncratic adhesion material in preparing biomacromolecule medicines of polypeptide protein or medicines of treating colon diseases. For the first time, the invention utilizes the characteristics of the idiosyncratic adsorption between the concanavalin A and the colon epithelial cell, successfully prepares the carrier material of the starch based colon idiosyncratic adhesion material by coupling the concanavalin A with the anti-digestion starch molecule by the glutaraldehyde and uses the starch based colon idiosyncratic adhesion material as an oral taking colon targeting control-release carrier material, so that starch based colon idiosyncratic adhesion material and the method have the characteristics of cell adsorption, enzymolysis triggering targeting, good biocompatibility, safety and non-toxin, good targeting slow-release effect, and the like.

Description

technical field [0001] The present invention relates to the field of research and development of natural polymer materials in the field of medicine, in particular to a starch-based colon targeting specific adhesive material and its Preparation methods and applications. Background technique [0002] Bioadhesive materials can interact with the surface of body tissues to produce adhesive ability. Therefore, the use of bioadhesive materials can prolong the residence time of the drug delivery system in a specific part of the biofilm, and rely on the adhesive force between the material and the mucous membrane , so that the drug diffuses through the epithelial cell membrane on the mucosal surface into the circulatory system at a certain speed, prolongs the action time of the drug, and thus improves the bioavailability of the drug. [0003] The most abundant natural biodegradable renewable polymer starch in nature has long been used in the field of medicine as excipients and disint...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/42A61K9/20A61P1/00A61K38/16
Inventor 李晓玺陈玲王雪毓刘早李琳
Owner SOUTH CHINA UNIV OF TECH
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