A nano-brain-targeted drug for intranasal administration of ricolamin and its preparation method

A nasal and brain-targeting technology of Likolamin, which is applied in the field of medicine, can solve problems such as the inability of drugs to enter, and achieve the effects of improving brain targeting, good biosorption, and bioavailability

Active Publication Date: 2020-01-17
深圳市锦泰医药科技合伙企业有限合伙 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] 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 nasal administration of nicolamin, 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

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  • A nano-brain-targeted drug for intranasal administration of ricolamin and its preparation method
  • A nano-brain-targeted drug for intranasal administration of ricolamin and its preparation method
  • A nano-brain-targeted drug for intranasal administration of ricolamin and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1 Recoilamine Nasally Administered Nano-brain Targeted Drug

[0039] This example provides a preparation method of the nanobrain-targeted drug for intranasal administration of Licolamine of the present invention, which specifically includes the following steps:

[0040] 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 48 hours to remove impurities, and the final product was freeze-dried to obtain formaldehyde chitosan (CS-CHO);

[0041] 2) Dissolve 1 mol formaldehyde chitosan (CS-CHO) in 3 mol DMSO, then add 1 mol sodium chlorite, stir and react for 24 hours, the product is concentrated by rotary evaporation and then dialyzed in 1 mol / L NaCl aqueou...

Embodiment 2

[0043] The in vitro drug release research of embodiment 2 chitosan-loaded diuretics

[0044] 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.

[0045] The result is as figure 1As shown, the release rate of Ricosylamine hydrobromide solution is relatively fast, and it is basically completely released ...

Embodiment 3

[0046] Example 3 Evaluation of Brain Targeting

[0047] Get healthy rats, be divided into 4 groups at random, be respectively Licolamine original drug group (original drug group); Nano drug-loaded micelles group (experimental group); Blank carrier micelles (blank group); control group). No food or water was allowed 24 hours before the experiment.

[0048] 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.

[0049] 30 minutes after the rat operation, the nasal administration group was administered with a micro-s...

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Abstract

The invention provides a lycoramine intranasal medicated nano-brain-targeting medicine and a preparation method thereof. The preparation method comprises the following steps: firstly, oxidizing chitosan by utilizing periodate to obtain hydroformylated chitosan which has a different molecular weight and has a o-dialdehyde functional group on the chitosan chain; and further oxidizing the o-dialdehyde functional group by using DMSO as a solvent and chlorous acid as an oxidant to prepare o-dicarboxyl chitosan; performing an esterification reaction between carboxylated chitosan and lycoramine to prepare the targeting medicine. The medicine can reach cerebrospinal fluid or brain through olfactory mucosa along the conjunctive tissue enveloping the periphery of the olfactory tract or the axon of olfactory receptor neurons, can bypass the blood-brain barrier to enter the central nervous system, and is directly absorbed by the brain. The medicine has the characteristics of quick response, no injection administration and liver first-pass effect prevention, and is convenient to use due to application of a quantitative device.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a nanobrain-targeted drug for nasal administration of Recoilamine and a preparation method thereof. Background technique [0002] Alzheimer's disease (AD) is an senile neurodegenerative disease with memory impairment and cognitive impairment as the main clinical manifestations, and its pathological feature is a large amount of extracellular amyloid peptide (β-Amyloid peptide, Aβ) deposition Senile plaques (Senileplaques, SP), intracellular phosphorylated tau protein-based neurofibrillary tangles (Neurofibrillary tangles, NFT) and a large number of degeneration and loss of central nervous cells dominated by cholinergic neurons. Although the pathogenesis of AD has not been fully elucidated, the cholinergic hypothesis and the Aβ hypothesis have received the most attention. [0003] At present, anti-acetylcholinesterase preparations are still the mainstay of AD drug tre...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/61A61K31/55A61P25/28C08B37/08A61K36/88
CPCA61K9/0043A61K9/19A61K31/55A61K36/88C08B37/003
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
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