Method for preparing floating-biological adhesion synergistic microparticle

A bioadhesion and microparticle technology, which is applied in the direction of non-active ingredient medical preparations, pharmaceutical formulations, block delivery, etc., can solve the problems of decreased adhesion performance, premature drug release, and microsphere shedding, so as to reduce toxicity , short time, good biocompatibility

Inactive Publication Date: 2007-01-10
DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Commonly used coating materials include carbomer, hydroxypropyl cellulose, acrylic resin Eudragit S, etc. These materials form a gel layer on the surface of the microspheres, but during the transit of the gastrointestinal tract, sometimes they will excessively absorb water and swell when they encounter gastric juice. Easy to fall off from the microspheres, resulting in premature drug release and reduced adhesion
The introduction of cross-linking agents such as glutaraldehyde can control the excessive water-absorbing swelling of the gel layer to a certain extent, but the cross-linking agent has certain toxicity to the body, and sometimes reacts with the drug, reducing the efficacy of the drug.

Method used

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  • Method for preparing floating-biological adhesion synergistic microparticle
  • Method for preparing floating-biological adhesion synergistic microparticle
  • Method for preparing floating-biological adhesion synergistic microparticle

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Embodiment 1: take dichloromethane as solvent, the ethyl cellulose solution of concentration 4% (w / v) is as dispersed phase (O), with concentration 0.5% (w / v) polyvinyl alcohol (PVA) and concentration 0.01 % (w / v) sodium dodecylsulfonate aqueous solution is used as the continuous phase (W), the O / W ratio is 1:40, the temperature is controlled at 20°C, the stirring speed is 1200rpm, and the stirring time is 5h. ~100 μm ethylcellulose microspheres. Evenly disperse the prepared ethylcellulose microspheres and 0.05mol / L insoluble calcium salt into a 0.5% (w / v) sodium alginate solution, and then disperse the mixed solution to a solution containing 0.5% (w / v) sodium In the liquid paraffin of Span80 (Span80) and 0.5% (w / v) Tween 20 (Tween20), the water-oil phase volume ratio is between 1:4, add 0.2ml of 10% (v / v) glacial acetic acid, continue Stir for 20 minutes and control the temperature at 20°C to obtain sodium alginate-ethylcellulose microparticles. Disperse the prepared...

Embodiment 2

[0025] Embodiment 2: take chloroform as solvent, the ethyl cellulose solution of concentration 15% (w / v) is as dispersed phase (O), with concentration 10% (w / v) polyvinyl alcohol (PVA) and concentration 0.2% ( w / v) Sodium dodecylsulfonate aqueous solution is used as the continuous phase (W), the O / W ratio is 1:10, the temperature is controlled at 40°C, the stirring speed is 600rpm, the stirring time is 2h, and the prepared particle size is 100~200μm ethylcellulose microspheres. Evenly disperse the prepared ethylcellulose microspheres and 0.3mol / L insoluble calcium salt into a 3% (w / v) sodium alginate solution, and then disperse the mixed solution into a solution containing 2.5% (w / v) sodium alginate In the liquid paraffin of Pan 80 (Span80) and 2.5% (w / v) Tween 20 (Tween20), the water-oil phase volume ratio is between 1:10, add 10ml of 50% (v / v) glacial acetic acid, and continue to stir 5min, the temperature is controlled at 20°C, and sodium alginate-ethylcellulose microparti...

Embodiment 3

[0026] Embodiment 3: take normal hexane as solvent, the ethyl cellulose solution of concentration 1% (w / v) is as dispersed phase (O), with concentration 2% (w / v) polyvinyl alcohol (PVA) and concentration 0.1% (w / v) Sodium dodecylsulfonate aqueous solution is used as the continuous phase (W), the O / W ratio is 1:6, the temperature is controlled at 30°C, the stirring speed is 900rpm, and the stirring time is 4h. 150 μm ethylcellulose microspheres. Evenly disperse the prepared ethylcellulose microspheres and 0.2mol / L insoluble calcium salt into a 1.5% (w / v) sodium alginate solution, and then disperse the mixed solution into a solution containing 1% (w / v) sodium alginate In the liquid paraffin of Pan 80 (Span80) and 1% (w / v) Tween 20 (Tween20), the water-oil phase volume ratio is between 1:6, add 5ml of 30% (v / v) glacial acetic acid, continue to stir After 15 minutes, the temperature is controlled at 30°C to obtain sodium alginate-ethylcellulose microparticles. Disperse the prepa...

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Abstract

The present invention relates to a preparation method of floatation-bioadhesion synergistic type microgranules. Said preparation method includes the following steps: firstly, utilizing drying system in the water to prepare ethyl cellulose floatation microspheres, then using sodium alginate to make coating in the emulsification system, finally the sodium alginate and ethyl cellulose microparticles are dispersed in chitosan solution to produce ion gelatification and form chitosan film so as to obtain the invented floatation-bioadhesion synergistic type microgranules.

Description

technical field [0001] The invention relates to a method for preparing intragastric floating-bioadhesion synergistic microparticle preparations, which adopts the drying-emulsification / internal gelation coupling technology in water, and the raw materials for preparing microparticles are widely used in pharmaceutical research and application fields, and have the advantages of Good biocompatibility biomaterials ethyl cellulose, sodium alginate, chitosan. This floating-bioadhesive synergistic particle can be used to carry small water-soluble or water-insoluble small molecule drugs that function in the stomach, and can also be used to carry many acidic drugs absorbed in the stomach and absorbed in the digestive tract above the duodenum Drug. The preparation can significantly prolong the residence time of the drug in the stomach and improve the bioavailability of the drug. Background technique [0002] The traditional oral sustained (controlled) release drug delivery system rele...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K47/38
Inventor 马小军郑建华刘朝武包德才于炜婷
Owner DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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