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Nasal cavity administrated huperzine prepn

A nasal drug delivery preparation, huperzine technology, applied in the direction of drug combination, nervous system diseases, active ingredients of heterocyclic compounds, etc., can solve problems such as liver toxicity, achieve fast onset of action, convenient use, and high bioavailability Effect

Inactive Publication Date: 2002-12-11
ZHEJIANG ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At the same time, clinical trials have also shown that oral administration of huperzine A tablets and capsules has certain gastrointestinal reactions, and long-term use has certain toxicity to the liver.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Huperzine A 0.3g

[0019] Sodium carboxymethylcellulose 0.5g

[0020] Laurocaprazine 0.5ml

[0021] Propylene glycol 0.5ml

[0022] Ethylparaben 0.1g

[0023] Distilled water to 100ml

[0024] Preparation method: Soak carboxymethylcellulose sodium in water to swell, add huperzine A, propylene glycol, laurocapram and ethylparaben in sequence, stir well to dissolve all, and finally add distilled water to a sufficient amount. .

[0025] The above-mentioned preparation was administered to 5 rats at 1.5 mg / kg nasal cavity respectively, and the changes of brain acetylcholinesterase activity and acetylcholine level were observed. The results showed that the inhibition of acetylcholinesterase in the whole brain reached the peak value (45%) after 45 minutes of administration. Within 4 hours after administration, the inhibition rate of acetylcholinesterase in the brain was maintained at about 40%, and it was still 35% by 6 hours. 60 minutes after administration, the level ...

Embodiment 2

[0029] Huperzine A 0.3g

[0030] Carbopol 934 1.5g

[0031] Glycerin 10g

[0032] Sodium Lauryl Sulfate 1.5g

[0033] Distilled water to 100ml

[0034] Preparation method: Mix and swell Carbopol934 with sodium lauryl sulfate and 30ml of distilled water, then add huperzine A and glycerin and stir well to obtain a transparent gel.

[0035] The result of in vitro permeation test of sheep nasal mucosa shows that the permeation amount of the above preparation reaches 150-350 micrograms after each administration.

Embodiment 3

[0037] Huperzine A 0.08g

[0038] Polyvinyl alcohol 0486 0.6g

[0039] Sodium hydroxymethylcellulose 0.6g

[0040] Tween 80 0.6ml

[0041] Sorbitol 0.8g

[0042] Appropriate amount of distilled water

[0043] Film making about 200cm 2

[0044]Preparation method: Take polyvinyl alcohol and soak it in water to make it swell, heat it on a water bath to dissolve it into a gel, add sodium hydroxymethyl cellulose and stir to dissolve it for later use. Dissolve huperzine A and sorbitol in water. Mix and grind the above two solutions, add water to an appropriate amount, keep warm, remove air bubbles, and form a film on flat glass. After drying, calculate the single-dose area according to the content of the main drug, and cut it into small pieces.

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Abstract

The nasal cavity administrated huperzine preparation consists of huperzine as effective medicine component, lauryl azatroketone and other infiltration promoter and other assistants. It is used for treating senile dementia and memory dysfunction and raising memory and learning capacity. It has high mucous membrane penetrating property and high brain targeting property and each administration can lead 80-500 microgram of huperzine into body.

Description

technical field [0001] The present invention is a preparation for administration, especially a novel nasal cavity administration preparation of huperzine for treating senile dementia and middle-aged and elderly memory impairment or improving memory and learning ability of teenagers. Background technique [0002] The world's population has entered an aging stage, and the incidence of Alzheimer's disease (AD) is increasing day by day. Studies on the etiology of Alzheimer's disease have shown that its onset is closely related to the death of cholinergic neurons in the brain, leading to the failure of the cholinergic system and memory dysfunction. It is known that the cholinergic system in the brain is involved in the learning and memory processes. Studies have now confirmed that huperzine A can inhibit the activity of acetylcholinesterase in the brain and increase the level of acetylcholine. Its remarkable advantage is that the inhibition of cholinesteras...

Claims

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Application Information

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IPC IPC(8): A61K31/44A61P25/28
Inventor 陈国神叶金翠王俏
Owner ZHEJIANG ACAD OF MEDICAL SCI
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