Nasal administration type nano-sized brain-targeting drug for galanthamine and preparation method of nasal administration type nano-sized brain-targeting drug for galanthamine

A galantamine and brain-targeting technology, which is applied in the field of medicine, can solve problems such as inaccessibility of drugs, achieve protection and promote regeneration, have good biosorption, and improve brain-targeting effects

Active Publication Date: 2016-06-01
深圳市锦泰医药科技合伙企业有限合伙 +1
View PDF0 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The present invention aims at the shortcomings of the blood-brain barrier in existing drugs for treating senile dementia, and aims to provide a nano-brain-targeted drug for galantamine administered through the nose, so as to eliminate the problem that the drug cannot enter the brain tissue due to the existence of the blood-brain barrier. shortcoming

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
  • Nasal administration type nano-sized brain-targeting drug for galanthamine and preparation method of nasal administration type nano-sized brain-targeting drug for galanthamine
  • Nasal administration type nano-sized brain-targeting drug for galanthamine and preparation method of nasal administration type nano-sized brain-targeting drug for galanthamine
  • Nasal administration type nano-sized brain-targeting drug for galanthamine and preparation method of nasal administration type nano-sized brain-targeting drug for galanthamine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Preparation of nanobrain-targeted drug for nasal administration of galantamine

[0044] This example provides a preparation method for nasally administered anti-senile dementia targeted drug of the present invention, which specifically includes the following steps:

[0045] 1) Under nitrogen atmosphere, 10 mol chitosan acetic acid-sodium acetate buffer solution and 1 mol potassium periodate were stirred and reacted at 4°C for 48 hours, then 1 mol ethylene glycol solution was added to the solution to stop the reaction, and the product was concentrated by rotary evaporation Dialyzed in 1mol / L NaCl aqueous solution and deionized water for 48h to remove impurities, and the final product was freeze-dried to obtain formaldehyde chitosan (CS-CHO);

[0046] 2) Dissolve 1 mol of formylated chitosan (CS-CHO) in 3 mol of DMSO, then add 1 mol of sodium chlorite, and stir for 24 hours. Impurities, the final product is freeze-dried to obtain ortho-dicarboxylated chitosan (CS-COOH);

...

Embodiment 2

[0049] In Vitro Drug Release Study of Chitosan Loaded Galantamine Drug

[0050] The drug is placed in a dialysis bag, and samples are taken from the release medium at regular intervals to analyze the drug content. The specific process is to freeze-dry the obtained drug solution, accurately weigh a certain amount, re-disperse it in 10ml of artificial cerebrospinal fluid by ultrasonic, put it into a dialysis bag (MWCO=12,000) and place it in a 100ml Erlenmeyer flask, add 40ml of artificial cerebrospinal fluid at a constant temperature In the shaker (setting temperature 37°C, rotation speed 60r / min), sample 2ml at intervals, and supplement the same amount of release medium. This method can ensure that the polymer micelles remain in the dialysis bag, making the determination of the drug content more accurate.

[0051] The result is as figure 1 As shown, the release rate of the galantamine hydrobromide solution is relatively fast, and it is basically completely released within 12...

Embodiment 3

[0052] Example 3 Evaluation of Brain Targeting

[0053] Take healthy rats and divide them into 4 groups at random, namely galantamine original drug group (original drug group); nanometer drug-loaded micelles group (experimental group); blank carrier micelles (blank group); normal saline (negative group). control group). No food or water was allowed 24 hours before the experiment.

[0054] Rats were anesthetized by intraperitoneal injection of 2% pentobarbital sodium solution (40m / kg), fixed on the rat board in a supine position, cut the neck skin and muscles, separated the trachea, esophagus, esophagus, and trachea, and performed tracheal intubation, esophagus The upper segment is ligated to prevent the loss of drug solution to the gastrointestinal tract after nasal administration. During the whole experiment, the anesthesia was supplemented timely to ensure that the rats were always under anesthesia.

[0055] 30 minutes after the rat operation, the nasal administration gro...

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

No PUM Login to view more

Abstract

The invention provides a nasal administration type nano-sized brain-targeting drug for galanthamine and a preparation method of the nasal administration type nano-sized brain-targeting drug for the galanthamine. The preparation method includes subjecting chitosan to oxidation by periodate so as to obtain different molecular weights of CS-CHO with chitosan chains containing o-dialdehyde functional groups, further, taking a DMSO (dimethyl sulfoxide) as a solvent and chlorous acid as an oxidizing agent to oxidize the o-dialdehyde functional groups into CS-COOH, and subjecting the CS-COOH and the galanthamine to esterification reaction so as to obtain the nano-sized brain-targeting drug. The nasal administration type nano-sized brain-targeting drug for the galanthamine has the advantages that the drug can envelop connecting tissues surrounding olfactory tracts or axons of olfactory receptor neurons through olfactory region mucous membranes to reach cerebral spinal fluid or the brain and can bypass blood-brain barriers to enter a central nervous system to be absorbed into the brain directly, and accordingly the drug is quick in action, needs no parenteral administration, avoids hepatic first-pass effect and is convenient to use by applying a dosing device.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a nano-brain-targeted drug for nasal administration of galantamine and a preparation method thereof. Background technique [0002] Alzheimer's disease (AD) is the most common type of senile dementia, ranking first among degenerative diseases of the central nervous system. It is characterized by progressive cognitive impairment and memory loss, abnormal mental behavior and life Decreased ability is the main performance. With the aging of the age structure of human society, the incidence of Alzheimer's disease is increasing day by day, and it has become the third largest health killer after cardiovascular and cerebrovascular diseases and tumors. According to the 2010 dementia report data, there are about 35.6 million AD patients in the world, and it is increasing at a rate of doubling every 20 years. By 2030, it will reach 65 million people, and most of them are in de...

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): A61K47/48A61K31/55A61K9/51A61K47/36A61P25/28
CPCA61K9/0043A61K9/5161A61K31/55
Inventor 吴正治段丽红
Owner 深圳市锦泰医药科技合伙企业有限合伙
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