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Water-solubility 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: 2008-07-09
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-solubility chitosan microsphere for carrying medicament and preparation thereof
  • Water-solubility 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 Oil, 1.1g Span65 and 0.4g Tween40 were stirred together to form an oil phase; the water phase was added to the oil phase, and stirred at 1600 rpm for 25 minutes to obt...

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Abstract

The present invention provides water soluble chitosan microspheres which can be used for loading drug and a preparation method thereof. The structure of the microsphere is that the outside of crosslinking state water soluble chitosan core which can load the drug is orderly enwrapped with a crosslinking state water soluble chitosan coating layer and a crosslinking solidified outer surface layer, which can be used for loading and controlling releasing the drug. The preparation method is that the drug which is mixed with the water soluble chitosan and corresponding water dispersion and oil component are used to form W / O type mixture which is reacted with twain-aldehyde crosslinking agent to obtain microsphere core; water soluble chitosan solution is used to form crosslinking state coating layar at the outer side of the microsphere core; finally, the crosslinking solidified outer surface layer is formed through the second crosslinking reaction. The chitosan microsphere for loading the drug has controllable particle size distribution and slow-release effect, obviously improved intensity and good biological compatibility and biological adhesion, which enlarges the application range for loading drug and has good effect of drug loading, controlling and releasing; the chitosan microsphere for loading the drug can be applied to a plurality of medication forms, such as hypodermic, intravenous and intraperitoneal injection medications, orally taking, etc., the preparation method is simple and feasible with mild condition and low production cost.

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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IPC IPC(8): A61K9/16A61K47/36
Inventor 李玉宝李峻峰张利左奕孙爱民
Owner SICHUAN UNIV
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