Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Preparation method of nanoparticles with functions of inhibiting histamine release and histamine receptor antagonism

A technology of histamine receptors and nanoparticles, applied in the field of biomedical materials, can solve problems such as limiting feasibility

Inactive Publication Date: 2019-04-09
OCEAN UNIV OF CHINA
View PDF5 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the excessively large particle size (1.0-1.3 μm) limits its feasibility for mucosal administration

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0013] Weigh 40 mg of hydroxybutyl chitosan with a molecular weight of 600 KDa, dissolve it in 1 mL of distilled water, and add 4 mL of methanol to dilute; weigh 40 mg of cetirizine hydrochloride, dissolve it in 16 mL of dimethyl sulfoxide , add 36 mL triethylamine, and react for 120 min in the dark; add 74.7 mg EDC and 45.0 mg NHS to the reaction solution, and keep stirring for 5 h at room temperature to activate γ-COOH in cetirizine; The cetirizine solution activated by -COOH was added dropwise to the hydroxybutyl chitosan solution, and after reacting for 48 h at 4°C, it was transferred to a dialysis bag and dialyzed in a solution with a ratio of methanol to water of 4:1. After 24 h, transfer to distilled water and continue dialysis for 24 h; freeze-dry the dialyzed solution to obtain cetirizine-hydroxybutyl chitosan; mix 20 mg cetirizine-hydroxybutyl chitosan and 40 mg of ketotifen was co-dissolved in 10 mL of dimethyl sulfoxide. After fully dissolving, it was added dropwis...

Embodiment 2

[0015] Weigh 40 mg of hydroxybutyl chitosan with a molecular weight of 700 KDa, dissolve it in 2 mL of distilled water, and add 6 mL of methanol to dilute; weigh 40 mg of cetirizine hydrochloride, dissolve it in 4 mL of dimethyl sulfoxide , add 12 mL triethylamine, and react for 20 min in the dark; add 24.9 mg EDC, 15.0 mg NHS to the reaction solution, and keep stirring at room temperature for 1.5 h to activate γ-COOH in cetirizine; The cetirizine solution activated by -COOH was added dropwise to the hydroxybutyl chitosan solution, and after reacting for 24 h at 0°C, it was transferred to a dialysis bag and dialyzed in a solution with a ratio of methanol to water of 4:1. After 24 h, transfer to distilled water and continue dialysis for 24 h; freeze-dry the dialyzed solution to obtain cetirizine-hydroxybutyl chitosan; mix 20 mg cetirizine-hydroxybutyl chitosan and 8 mg of ketotifen was co-dissolved in 5 mL of dimethyl sulfoxide. After fully dissolved, it was added dropwise to 1...

Embodiment 3

[0017] Weigh 40 mg of hydroxybutyl chitosan with a molecular weight of 1700 KDa, dissolve it in 4 mL of distilled water, and add 16 mL of methanol to dilute; weigh 160 mg of cetirizine hydrochloride, dissolve it in 4 mL of dimethyl sulfoxide , add 12 mL of triethylamine, and react for 60 min in the dark; add 124.5 mg of EDC and 75.0 mg of NHS to the reaction solution, and keep stirring for 1 h at room temperature to activate the γ-COOH in cetirizine; -COOH-activated cetirizine solution was added dropwise to hydroxybutyl chitosan solution, reacted at 8 °C for 24 h, transferred to a dialysis bag, and dialyzed in a solution with a ratio of methanol to water of 3:1 After 24 h, transfer to distilled water and continue dialysis for 24 h; freeze-dry the dialyzed solution to obtain cetirizine-hydroxybutyl chitosan; mix 20 mg cetirizine-hydroxybutyl chitosan and 20 mg of ketotifen was co-dissolved in 20 mL of dimethyl sulfoxide. After fully dissolved, it was added dropwise to 20 mL of ...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
molecular weightaaaaaaaaaa
Login to View More

Abstract

The invention discloses a preparation method of nanoparticles with the functions of inhibiting histamine release and histamine receptor antagonism. The preparation method comprises the following steps: synthesizing hydroxybutyl chitosan (patent number ZL201110214776.X); grafting desalinated cetirizine to the hydroxybutyl chitosan by carbodiimide reaction to obtain cetirizine-hydroxybutyl chitosan;dissolving the cetirizine-hydroxybutyl chitosan and ketotifen into dimethyl sulfoxide; dropwise adding a mixed solution into distilled water under the stirring condition to obtain ketotifen: cetirizine-hydroxybutyl chitosan. A preparation process of the nanoparticles has the advantages of simplicity, short cycle and low cost; the nanoparticles have the effects of inhibiting the histamine releaseand histamine H1 receptor antagonism, can effectively relieve typical allergy symptoms and have a good development and application prospect on treatment aspect of allergic rhinitis.

Description

technical field [0001] The invention belongs to the field of biomedical materials and relates to a method for preparing nanoparticles with the functions of inhibiting histamine release and histamine receptor antagonism. Background technique [0002] Chitosan (CS) is a high-molecular-weight aminopolysaccharide obtained by deacetylation of chitin in shrimp skin crab shells. Some enzymes (such as: lysozyme) degradation. Due to the large number of amino groups and hydroxyl groups distributed on the molecular chain of chitosan, which can form intramolecular and intermolecular hydrogen bonds, it is almost insoluble in water or alkaline solutions, which limits its application in neutral environments in vivo. Hydroxybutyl chitosan is a modified product of chitosan etherification. The hydroxybutyl modification endows it with good water solubility, which effectively improves the limitation that chitosan can only be dissolved in acidic solution. Hydroxybutyl chitosan has good biocomp...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/61A61K31/495A61K31/4535A61P37/08
CPCA61P37/08A61K9/5161A61K31/4535A61K31/495A61K2300/00
Inventor 刘雅孙梦杰陈西广程晓杰孔明冯超
Owner OCEAN UNIV OF CHINA
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com