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Method for preparing chitosan grafted cetirizine nano-micelles

A cetirizine and nanomicelle technology, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve the problems of poor stability of cataplasm and complicated preparation process, etc. It can achieve the effect of good research and development application prospects, simple preparation technology, and convenient operation.

Active Publication Date: 2016-12-14
OCEAN UNIV OF CHINA
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AI Technical Summary

Problems solved by technology

At present, the external preparation of cetirizine has the report of cataplasm, but the cataplasm also has the disadvantages of poor stability and complicated preparation process.

Method used

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  • Method for preparing chitosan grafted cetirizine nano-micelles
  • Method for preparing chitosan grafted cetirizine nano-micelles

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preparation example Construction

[0015] 3. Preparation of chitosan grafted cetirizine

[0016] Weigh chitosan and dissolve in dilute acid solution, wherein the concentration of dilute acid solution is controlled at 0.5-2% (v / v), the concentration of chitosan solution is 0.2-1%, and chitosan solution is added drop by drop into the carboxyl-activated cetirizine solution and stirred evenly, wherein the molar ratio of chitosan to cetirizine is 1:0.5-2, and the reaction is continued for 12-48h.

[0017] 4. Purification of the product

[0018] The reaction product is dialyzed in deionized water, and the light yellow solid obtained by drying is the chitosan cetirizine graft.

[0019] 5. Preparation of chitosan-grafted cetirizine nanomicelles

[0020] Dissolve the chitosan cetirizine graft in dilute acid solution, where the concentration of dilute acid is controlled at 1-2% (v / v), and perform ultrasonication (750W, 20-40%, 6-24min) , that is, chitosan grafted cetirizine nano-micelle.

[0021] The dilute acid solu...

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Abstract

The invention relates to a method for preparing chitosan grafted cetirizine nano-micelles in the field of biotechnologies. Chitosan and cetirizine hydrochloride are used as raw materials, chitosan and cetirizine grafted materials are synthesized by the aid of carbodiimide processes, and ultrasonic treatment is carried out on chitosan and cetirizine grafted material solution to obtain the chitosan grafted cetirizine nano-micelles. The method includes carrying out desalting treatment on the cetirizine hydrochloride; adding carboxyl activators into the cetirizine hydrochloride, activating carboxyl and then mixing the cetirizine hydrochloride with chitosan solution; carrying out continuous reaction to obtain reaction products; sufficiently dialyzing and drying the reaction products to obtain chitosan grafted cetirizine; carrying out ultrasonic treatment on chitosan grafted cetirizine solution to obtain the chitosan grafted cetirizine nano-micelles. The method has the advantages that the substitution degree of the chitosan grafted cetirizine nano-micelles is 2.8-5.6%, the chitosan grafted cetirizine nano-micelles are regularly spherical, the particle sizes of the chitosan grafted cetirizine nano-micelles are 80.6-320.1 nm, and the method has excellent research and development application prospects in the aspects of chronic rhinitis and asthma treatment and the like.

Description

technical field [0001] The invention belongs to the field of biotechnology, and relates to a preparation method of chitosan grafted cetirizine nano micelles. Background technique [0002] Cetirizine, the active carboxylic acid metabolite of hydroxyzine, is a potent second-generation antihistamine with anti-inflammatory properties and high specific affinity for histamine H1 receptors, which is not metabolized by the liver and is currently used It is the first choice drug for the treatment of allergic diseases in the treatment of year-round or seasonal skin, respiratory system and eye allergic diseases. In existing research reports, chitosan cross-linked sodium tripolyphosphate has been used as an oral carrier of cetirizine hydrochloride, and the prepared drug-loaded nanoparticles are in a regular spherical shape with good uniformity and can obtain relatively The high encapsulation rate and encapsulation capacity can be used for the controlled release of cetirizine hydrochlor...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K47/36A61K47/48A61K31/495A61P37/08
CPCA61K9/1075A61K31/495
Inventor 陈西广于晓萍程晓杰孔明刘雅冯超
Owner OCEAN UNIV OF CHINA
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