Curcumin micelle nasal solution and preparation method thereof

A technology of nasal administration and curcumin, which is applied in the field of curcumin micellar nasal administration solution and its preparation, can solve the problems of low trigeminal ganglion targeting, side effects, and effective stability of only 3 months. Controllable micellar particle size, improved targeting, and good storage stability

Active Publication Date: 2015-10-28
SHANDONG EYE INST
View PDF11 Cites 10 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The invention patent "A Cyclosporine A Micellar Eye Drops and Its Preparation Method" (ZL201210529616.9) applied and authorized by the Shandong Provincial Institute of Ophthalmology is mainly based on polyethylene caprolactam-polyvinyl acetate-polyethylene glycol Copolymers are used to construct high-efficiency preparations for eye drops, but in the subsequent development process, research by the Shandong Provincial Institute of Ophthalmology found that the particle size of micelles based on polyethylene caprolactam-polyvinyl acetate-polyethylene glycol copolymers is mainly in the range of 50~ 90nm, simple polyethylene caprolactam-polyvinyl acetate-polyethylene glycol copolymer-constructed micelles are not highly targeted to the trigeminal ganglion after nasal administration, and the drug is widely distributed in the olfactory nerve and brain tissue after nasal administration , has potential risk of side effects, and during the storage of its aqueous solution, cyclosporin A will gradually dissociate from the micelles, and the effective stability of its aqueous solution at room temperature is only 3 months

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

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Curcumin micelle nasal solution and preparation method thereof
  • Curcumin micelle nasal solution and preparation method thereof
  • Curcumin micelle nasal solution and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Put 50 mg curcumin, 30 mg four-arm-polyethylene glycol-maleimide (molecular weight 1000) and 900 mg polyethylene caprolactam-polyvinyl acetate-polyethylene glycol (molecular weight 118000) in a 100 mL round bottom flask, Add 20mL of absolute ethanol, after fully dissolved, evaporate the absolute ethanol in a 40°C water bath in a rotary vacuum to obtain a uniformly dispersed film of drug and copolymer, then add 10mL of phosphate buffer, wash the film thoroughly, and ultrasonicate in a 300w water bath for 10 minutes to obtain gel Beam solution. Cool the micellar solution to 4°C, add 10 mg of RGD peptide to the micellar solution, and continue to incubate at 4°C for 30 minutes after fully dissolving, add preservative benzalkonium chloride, isotonic regulator sodium chloride, and adjust the pH to 7.4. After the micellar solution passes through a 0.22 μm microporous membrane, it can be aseptically dispensed. The average particle size of curcumin micelles measured by laser pa...

Embodiment 2

[0026] Put 50mg curcumin, 50mg four-arm-polyethylene glycol-maleimide (molecular weight 1000) and 1000mg polyethylene caprolactam-polyvinyl acetate-polyethylene glycol (molecular weight 118000) in a 100mL round bottom flask, Add 20mL of absolute ethanol, after fully dissolved, evaporate the absolute ethanol in a 40°C water bath in a rotary vacuum to obtain a uniformly dispersed film of the drug and the copolymer, then add 10mL of phosphate buffer, wash the film thoroughly, and ultrasonicate in a 300w water bath for 10 minutes to obtain gel Beam solution. Cool the micellar solution to 4°C, add 25 mg of RGD peptide to the micellar solution, and continue to incubate at 4°C for 30 minutes after fully dissolving, add preservative benzalkonium chloride, isotonic regulator sodium chloride, adjust the pH to 7.4, and After the micellar solution passes through a 0.22 μm microporous membrane, it can be aseptically dispensed. The average particle size of curcumin micelles measured by las...

Embodiment 3

[0028] Put 50 mg curcumin, 15 mg four-arm-polyethylene glycol-maleimide (molecular weight 1000) and 600 mg polyethylene caprolactam-polyvinyl acetate-polyethylene glycol (molecular weight 118000) in a 100 mL round bottom flask, Add 20mL of absolute ethanol, after fully dissolved, evaporate the absolute ethanol in a 40°C water bath in a rotary vacuum to obtain a uniformly dispersed film of the drug and the copolymer, then add 10mL of phosphate buffer, wash the film thoroughly, and ultrasonicate in a 300w water bath for 10 minutes to obtain gel Beam solution. Cool the micellar solution to 4°C, add 3.75mg RGD peptide to the micellar solution, fully dissolve and continue to incubate at 4°C for 30min, add preservative benzalkonium chloride, isotonic regulator sodium chloride, adjust pH to 7.4, After the micellar solution is passed through a 0.22 μm microporous membrane, it can be aseptically dispensed. The average particle size of curcumin micelles measured by laser particle size ...

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
particle diameteraaaaaaaaaa
particle diameteraaaaaaaaaa
Login to view more

Abstract

The invention discloses a curcumin micelle nasal solution which contains curcumin used as a main drug, a preservative and an isoosmotic adjusting agent. The curcumin micelle nasal solution is characterized by comprising a poly(N-vinylcaprolactam)-polyvinyl acetate-polyethylene glycol copolymer, a medicinal polyethylene glycol auxiliary material and RGD peptide which are used as medicinal excipients. The mass ratio of the main drug curcumin to the poly(N-vinylcaprolactam)-polyvinyl acetate-polyethylene glycol copolymer medicinal excipient is 1:12-1:20. The mass ratio of the medicinal polyethylene glycol auxiliary material to the poly(N-vinylcaprolactam)-polyvinyl acetate-polyethylene glycol copolymer medicinal excipient is 1:20-1:40. The mass ratio of RGD peptide to the medicinal polyethylene glycol auxiliary material is 1:2-1:4. According to the prepared curcumin micelle nasal solution, curcumin has good solubility in an aqueous solution. By a preparation method of the curcumin micelle nasal solution, water solubility of curcumin is solved, and molecular stability of curcumin is raised. Meanwhile, particle size of the micelle is adjusted to an appropriate particle size range (150-220 nm), and stability of the micelle aqueous solution is enhanced.

Description

technical field [0001] The invention relates to a curcumin nasal administration solution, in particular to a curcumin micellar nasal administration solution and a preparation method thereof. Background technique [0002] The prevalence of diabetes in my country has increased rapidly in recent years, and diabetes has become a major public health problem in my country. The patient's long-term hyperglycemia state leads to lesions in various tissues and organs throughout the body, causing serious diabetes-related complications, including diabetic keratopathy. In addition, diabetic patients are prone to delayed corneal epithelial healing or even non-healing during corneal trauma or corneal surgery. Blindness is difficult to treat, the prognosis is poor, and the patient's economic and mental burden is serious. At present, the clinical treatment methods for diabetic keratopathy are limited. Therefore, it is of great clinical significance to study new therapeutic targets and effec...

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): A61K9/08A61K31/12A61K47/34A61K47/42A61P25/00A61P3/10A61P27/02
Inventor 吴祥根郭传龙李梦双史伟云
Owner SHANDONG EYE INST
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap