Modified beta-cyclodextrin/chitosan compound, and preparation method and application thereof

A cyclodextrin and chitosan technology, which is applied in the field of modified β-cyclodextrin/chitosan complex and its preparation, can solve the problems of poor water solubility and insignificant long-term sustained release effect, and achieves easy access to raw materials. , good slow release effect, low synthesis cost effect

Active Publication Date: 2016-03-09
SOUTH CHINA AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Tacrolimus has poor water solubility, and the main application methods are oral and intravenous injection at present, and the long-term sustained-release effect is not obvious

Method used

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  • Modified beta-cyclodextrin/chitosan compound, and preparation method and application thereof
  • Modified beta-cyclodextrin/chitosan compound, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] (1) Preparation of intermediate product: reaction of β-cyclodextrin and acrylic acid. Heat to dissolve β-cyclodextrin in distilled water, add a small amount of polyethylene glycol (PEG-400) modification and a small amount of catalyst NaH 2 PO 4 , then add a cross-linking agent (acrylic acid), reflux at 50°C for 1 h, and precipitate and wash with acetone to obtain an intermediate product; the molar ratio of the β-cyclodextrin to the cross-linking agent is 2:1.

[0042] (2) Preparation of the complex: Dissolve chitosan in 2% acetic acid solution, add the intermediate product obtained in step (1), add a small amount of catalyst, reflux at 50°C for 3h, collect the product, and obtain the modified β-ring Dextrin / chitosan compound; the molar ratio of the chitosan monomer in the chitosan to the intermediate product is 2:1.

[0043] (3) Dissolve tacrolimus in ethanol, add to the modified β-cyclodextrin / chitosan complex obtained in step (2) and stir overnight, the final concen...

Embodiment 2

[0046] (1) Preparation of intermediate product: reaction of β-cyclodextrin and acrylic acid. Heat to dissolve β-cyclodextrin in distilled water, add a small amount of polyethylene glycol (PEG-400) modification and a small amount of catalyst NaH 2 PO 4 , then add a cross-linking agent (acrylic acid), reflux at 90°C for 5h, and precipitate and wash with acetone to obtain an intermediate product; the molar ratio of the β-cyclodextrin to the cross-linking agent is 4:1.

[0047] (2) Preparation of the complex: dissolving chitosan in 2% acetic acid solution, adding the intermediate product obtained in step (1), adding a small amount of catalyst, and reacting at reflux at 90°C for 6h, collecting the product to obtain the modified β-ring Dextrin / chitosan compound; the molar ratio of the chitosan monomer in the chitosan to the intermediate product is 4:1.

[0048] (3) Dissolve tacrolimus in ethanol, add to the modified β-cyclodextrin / chitosan complex obtained in step (2) and stir ove...

Embodiment 3

[0050] (1) Preparation of intermediate product: reaction of β-cyclodextrin and acrylic acid. Heat to dissolve β-cyclodextrin in distilled water, add a small amount of polyethylene glycol mixture (PEG-1000 and PEG-400 mixed at a molar ratio of 1:1) to modify and a small amount of catalyst NaH 2 PO 4, and then add a cross-linking agent (acrylic acid), reflux reaction at 70°C for 3h, and precipitate and wash with acetone to obtain an intermediate product; the molar ratio of the β-cyclodextrin to the cross-linking agent is 2.5:1.

[0051] (2) Preparation of the complex: Dissolve chitosan in 2% acetic acid solution, add the intermediate product obtained in step (1), add a small amount of catalyst, reflux at 70°C for 5 hours, collect the product, and obtain the modified β-ring Dextrin / chitosan compound; the molar ratio of the chitosan monomer in the chitosan to the intermediate product is 3:1.

[0052] (3) Dissolve tacrolimus in ethanol, add to the modified β-cyclodextrin / chitosan...

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Abstract

The invention discloses a modified beta-cyclodextrin/chitosan compound, and a preparation method and an application thereof. The preparation method has the advantages of simplicity, easy obtaining of raw materials, and low synthesis cost. Beta-CD is adopted to load a medicine, and the beta-CD has external cavity hydrophilicity and inner cavity hydrophobicity characteristics, so the beta-CD can load multiple hydrophobic medicines, and a medicine loaded composite film has large space in the fields of medicine loading and slow release. Films with different transparencies can be made by using the compound through adjusting the molar ratio of chitosan (monomer) to the beta-CD in order to meet requirements of different medicinal positions; and the composite films made by using the modified beta-cyclodextrin/chitosan compound are transparent and flexible, have good biocompatibility and slow release effects, and have no toxic or harmful effects on human bodies.

Description

technical field [0001] The invention belongs to the field of polymer modification and composites, in particular to a modified β-cyclodextrin / chitosan composite and its preparation method and application. Background technique [0002] Transplant rejection refers to that after recipients undergo allogeneic tissue or organ transplantation, foreign tissues or organs and other transplants are recognized by the recipient's immune system as a "foreign component", and the latter initiates attacks, destruction and clear. Since it is difficult to find a donor and recipient with the same human leukocyte antigen (HLA) in the population, rejection will occur in allogeneic tissue or organ transplants except for identical twin organ transplants. The success or failure of organ transplantation depends largely on the prevention and treatment of transplant rejection. At present, the prevention and treatment of transplantation mainly focus on strict selection of donors, suppression of immune ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08L5/08C08L51/02C08L5/16C08L71/02C08J3/24C08J5/18A61K9/70A61K47/48A61K31/436A61P37/06A61K47/69
CPCA61K9/7007A61K31/436C08J3/24C08J5/18C08J2305/08C08J2305/16C08J2405/16C08J2451/02C08L5/08C08L2203/16C08L2205/025C08L2205/03C08L2205/035C08L51/02C08L71/02C08L5/16
Inventor 蒋刚彪刘永林欧阳晓东袁进曾润萍
Owner SOUTH CHINA AGRI UNIV
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