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Water-soluble chitosan microsphere for carrying medicament and preparation thereof

A water-soluble chitosan, drug-loading technology, applied in pharmaceutical formulations, medical preparations with inactive ingredients, bulk delivery, etc., can solve the problem of poor strength, easy drug elution, and low drug encapsulation rate. And other issues

Inactive Publication Date: 2009-12-23
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, because it is also prepared into water-soluble chitosan microspheres by the common emulsification and cross-linking method, the obtained microspheres also have poor strength. If they are directly used for drug loading, the drug will be Easy to be eluted, the drug encapsulation rate is low and the sudden release phenomenon is serious, which seriously affects the drug loading effect

Method used

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  • Water-soluble chitosan microsphere for carrying medicament and preparation thereof
  • Water-soluble chitosan microsphere for carrying medicament and preparation thereof
  • Water-soluble chitosan microsphere for carrying medicament and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] The deacetylation degree is 95% chitosan 2g, is configured in the acetic acid solution of 2wt% 2wt% chitosan acetic acid solution 100g in concentration, joins in 100g methanol, drips 0.64g acetic anhydride under stirring, stand Aging for 24 hours, under the condition of stirring at 600 rpm, adding to 500 g of 10wt% KOH absolute ethanol solution, filtering, washing with absolute ethanol until neutral, drying and grinding through a 200-mesh sieve, and taking the undersize It is the raw material of water-soluble chitosan.

[0031] Dissolve 2 g of water-soluble chitosan in 48 g of water to obtain 50 g of water-soluble chitosan solution, get 25 g of water-soluble chitosan solution, and uniformly disperse 0.4 g of the model drug rifampin in it as the water phase; 100 g of liquid paraffin , 1.7g Span80 and 0.3g Tween80 were stirred together uniformly as the oil phase; the water phase was added to the oil phase, and stirred at 1800 rpm for 30 minutes to obtain an emulsion.

[...

Embodiment 2

[0034] 2 g of chitosan with a degree of deacetylation of 90% is configured into 200 g of 1 wt % chitosan acetic acid solution in 2 wt % acetic acid solution, added to 150 g of methanol, and 0.61 g of acetic anhydride is added dropwise under stirring, and left to stand Aging for 24 hours, adding to 700 g of 10wt% KOH absolute ethanol solution with stirring at 500 rpm, filtering, washing with absolute ethanol until neutral, drying and grinding through a 200-mesh sieve, and taking the undersize It is the raw material of water-soluble chitosan.

[0035] 2g of water-soluble chitosan was dissolved in 48g of water to obtain 50g of water-soluble chitosan solution, 25g of water-soluble chitosan solution was taken, and 0.2g of cisplatin as the model drug was uniformly dispersed therein as the water phase; 120g of olive oil, Stir 1.8g of Span60 and 0.2g of Tween80 together to form an oil phase; add the water phase to the oil phase, and stir at 1500 rpm for 30 minutes to obtain an emulsio...

Embodiment 3

[0038] 2g of chitosan with a deacetylation degree of 85% is configured into 100g of 2wt% chitosan acetic acid solution in a 2wt% acetic acid solution, added to 100g of methanol, and 0.58g of acetic anhydride is added dropwise under stirring, and left to stand Aging for 24 hours, under the condition of stirring at 500 rev / min, add it to 1000 g of 5wt% KOH absolute ethanol solution, filter, wash with absolute ethanol until neutral, dry and finely pass through a 200-mesh sieve, and take the undersize It is the raw material of water-soluble chitosan.

[0039] Dissolve 2 g of water-soluble chitosan in 48 g of water to obtain 50 g of water-soluble chitosan solution, take 27.8 g of water-soluble chitosan solution, and uniformly disperse 0.2 g of the model drug secretin in it as the water phase; 150 g of sunflower seeds Stir oil, 1.1g Span65 and 0.4g Tween40 together to form an oil phase; add the water phase to the oil phase, and stir at 1600 rpm for 25 minutes to obtain an emulsion. ...

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Abstract

Water-soluble chitosan microspheres that can be used to load drugs and a preparation method thereof. The structure of the microsphere is that the cross-linked water-soluble chitosan core that can be loaded with drugs is sequentially wrapped with a cross-linked water-soluble chitosan coating layer and a cross-linked cured outer layer, which can be used for drug loading and control. freed. The preparation method is to first form a W / O mixture of water-soluble chitosan and corresponding water-dispersed drugs and oily ingredients, react with dialdehyde cross-linking agents to obtain drug-loaded microsphere cores, and then water-soluble shells The polysaccharide solution forms a cross-linked covering layer on its outside, and finally forms a cross-linked solidified surface layer through a second cross-linking reaction. The particle size distribution and sustained release effect of the chitosan drug-loaded microspheres are controllable, the strength is significantly improved, the biocompatibility and bioadhesion are good, the application range of drug loading is expanded, and the drug entrapment and controlled release effects are good. It can be used in multiple administration methods such as subcutaneous, intravenous and intraperitoneal injection, oral administration, etc., and the preparation method is simple and easy, the conditions are mild, and the production cost is low.

Description

technical field [0001] The invention relates to a water-soluble chitosan microsphere which can be used for loading medicine and a preparation method. The microsphere can be used for encapsulating and controlling the release of drugs. Background technique [0002] Drug-loaded microspheres generally refer to spherical polymer microspheres prepared from polymer materials or their monomers, and their surfaces can carry chemically reactive, pH-sensitive, porous, radioactive or other functional groups. Group, which can have a variety of functions. Microspheres can effectively prolong the circulation half-life of drugs in the human body, thereby prolonging the effect of the drug, and through the slow and controlled release of the drug, reduce the frequency of medication, reduce the fluctuation of blood drug concentration, and keep the blood drug concentration constant at Within the therapeutic window, reduce the toxic and side effects of the drug, and maintain a long-lasting and ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/36C08J3/24A61K9/16
Inventor 李玉宝李峻峰张利左奕孙爱民
Owner SICHUAN UNIV
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