Oral biological macromolecular medicine administrating system based on biological adhesive microballoon

A technology of bioadhesion and microspheres, which is applied in the direction of pharmaceutical formulations, medical preparations of non-active ingredients, powder delivery, etc., to achieve the effects of improving bioavailability, having more active groups, and being easy to modify

Inactive Publication Date: 2003-05-14
BEIJING LIANXINSHENG SCI TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The use of natural polymer polysaccharides to prepare bioadhesive microsphere drug delivery systems to achieve oral administration of biomacromolecules has not been reported in the literature

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Get 150ml of liquid paraffin, stir (n=300rpm) while heating, when the temperature rises to 80°C, add 10ml of 15% (w / v) pectin solution and mix with 10ml of 1% (w / v) xanthan gum solution After the solution, the temperature is maintained between 80-90 ° C, after stirring for 10 minutes, adding a concentration of 2% chitosan (or chitosan derivatives) solution 5ml; adding 20% ​​polycarbophil solution 10ml. Cool naturally at room temperature, and continue stirring until the temperature drops to room temperature and stop. The resultant is fully washed with petroleum ether and deionized water, and dried at 30°C to obtain porous natural polymer polysaccharide bioadhesive microspheres. The particle size of the microspheres is 0.95-1.30 mm (>80%).

Embodiment 2

[0039] Get 400ml of sunflower oil, stir (n=400rpm) while heating, when the temperature rises to 40°C, add 10ml of 30% (w / v) pectin solution and 20ml of 2% (w / v) xanthan gum solution The temperature of the mixed solution was kept at about 40° C., and after stirring for 20 minutes, 10 ml of a 3% chitosan (or chitosan derivative) solution was added; 10 ml of a 10% polycarbophil solution was added. Stirring was continued for 20 minutes and 1 ml of 0.025M glutaraldehyde was added. Heating was stopped, and the crosslinking reaction stopped after 1.5 hours. The resultant is fully washed with ether and deionized water, and dried at 20°C to obtain natural polymer polysaccharide bioadhesive microspheres. The particle size of the microspheres is 0.86-1.00 mm (>80%).

Embodiment 3

[0041] Get peanut oil 300ml, stir (n=300rpm) and heat simultaneously, when temperature rises to 50 ℃, after adding 10ml 30% (w / v) pectin solution and 5ml 1.5% (w / v) xanthan gum solution and mix The temperature of the solution was kept at about 50°C, and after stirring for 40 minutes, 8 ml of a 4% chitosan (or chitosan derivative) solution was added; 12 ml of a 15% polycarbophil solution was added. Stirring was continued for 20 minutes before heating was discontinued. Fully wash the product with volatile organic solvents (such as petroleum ether, ether, ethanol and isopropanol, etc.), deionized water, and then exchange the microspheres in a 0.01M alkaline solution of epichlorohydrin (pH=10). Linked for 2 hours, then washed with volatile organic solvents and deionized water, and dried at 15°C to obtain cross-linked natural polymer polysaccharide bioadhesive microspheres. The particle size of the microspheres is 0.98-1.42 mm (>85%).

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Abstract

The present invention provides one kind of biologically degradable adhesive natural polymer polysaccharide microballoon, its preparation, treating composition and medicine administrating system carrier. The microballoon is prepared by an oil-water two-phase process including dispersing pectin and xanthan gum in oil phase, adding chitosan and polycarbophil to graft, separation, cleaning and drying. It is biologically degradable and has good biocompatibility and strong biological adhesion. It is used in orally taken biological macromolecular medicine administrating system to raise the biological utilization of medicine.

Description

technical field [0001] The invention relates to a biodegradable natural polymer polysaccharide bioadhesive microsphere, a preparation method of the microsphere, a therapeutic composition composed of the microsphere and a biomacromolecular therapeutic agent, and the bioadhesive microsphere The microsphere is used as a drug delivery system carrier to prepare an oral biomacromolecule drug delivery system. Background technique [0002] The drug delivery and release system is a key link in the development and research of new drugs. How to ensure that the drug can maximize the curative effect shown in the in vitro experiment in the body, and at the same time minimize the toxic and side effects on other tissues, nerves, and organs of the body is an essential and important content in the development of new drugs. [0003] With the rapid development of recombinant DNA technology, more and more polypeptide and protein drugs have emerged. For example, the global sales of erythropoieti...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K47/36C08L5/06
Inventor 董春宏
Owner BEIJING LIANXINSHENG SCI TECH
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