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

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

Example Embodiment

[0029] Example 1

[0030] 2g of chitosan with a degree of deacetylation of 95% was prepared into a 2wt% acetic acid solution of 2wt% in an acetic acid solution with a concentration of 2wt%, added to 100g of methanol, 0.64g of acetic anhydride was added dropwise under stirring, and left to stand. After aging for 24 hours, add it to 500g of 10wt% KOH anhydrous ethanol solution under the condition of stirring at 600 rpm, filter, wash with absolute ethanol to neutrality, dry and grind through 200 mesh sieve, and remove the sieve. It is a raw material for water-soluble chitosan.

[0031] Dissolve 2g of water-soluble chitosan in 48g of water to obtain 50g of water-soluble chitosan solution, take 25g of water-soluble chitosan solution, and uniformly disperse 0.4g of model drug rifampicin in it, as the water phase; 100g of liquid paraffin , 1.7g Span80 and 0.3g Tween80 are stirred together and uniformly used as the oil phase; the water phase is added to the oil phase and stirred at 1800 r...

Example Embodiment

[0033] Example 2

[0034] 2g of chitosan with a degree of deacetylation of 90% was prepared into 200g of 1wt% chitosan acetic acid solution in a 2wt% acetic acid solution, added to 150g of methanol, 0.61g of acetic anhydride was added dropwise under stirring, and left to stand. After aging for 24 hours, add it to 700g of 10wt% KOH absolute ethanol solution under stirring at 500 rpm, filter, wash with absolute ethanol to neutrality, dry and grind through a 200 mesh sieve, and remove the sieve It is a raw material for water-soluble chitosan.

[0035] Dissolve 2g of water-soluble chitosan in 48g of water to obtain 50g of water-soluble chitosan solution, take 25g of water-soluble chitosan solution, and disperse the model drug 0.2g cisplatin evenly in it as the water phase; mix 120g of olive oil, 1.8g Span60 and 0.2g Tween80 were stirred together and uniformly used as the oil phase; the water phase was added to the oil phase and stirred at 1500 rpm for 30 minutes to obtain an emulsion....

Example Embodiment

[0037] Example 3

[0038] 2g of chitosan with a degree of deacetylation of 85% was prepared into a 2wt% acetic acid solution of 2wt% in an acetic acid solution with a concentration of 2wt%, added to 100g of methanol, 0.58g of acetic anhydride was added dropwise under stirring, and left to stand. After aging for 24 hours, add it to 1000g of 5wt% KOH anhydrous ethanol solution under stirring at 500 rpm, filter, wash with absolute ethanol to neutrality, dry and grind through a 200 mesh sieve, and remove the sieve. It is a raw material for water-soluble chitosan.

[0039] Dissolve 2g of water-soluble chitosan in 48g of water to obtain 50g of water-soluble chitosan solution, take 27.8g of water-soluble chitosan solution, and disperse 0.2g of model drug secretin evenly in it, as the water phase; 150g of sunflower seeds The oil, 1.1g Span65 and 0.4g Tween40 were stirred together to form the oil phase; the water phase was added to the oil phase and stirred at 1600 rpm for 25 minutes to ob...

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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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