Targeted preparation via nose to brain of Huperzine and its derivant or its salt

A technology of huperzine A and derivatives, which is applied in the field of nasal-brain targeting preparations, can solve problems such as large systemic toxicity, and achieve the advantages of improving brain selectivity, improving memory and learning ability, and reducing systemic side effects. Effect

Inactive Publication Date: 2005-06-01
SHANGHAI INST OF PHARMA IND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] Chinese patent CN 1383824A discloses a kind of huperzine A nasal cavity administration preparation, it uses huperzine as medicine, adopts the permeation enhancer such as laurocaprone to increase the absorption of medicine through the nasal mucosa, and the in vitro penetration test of sheep nasal mucosa proves that every 80-500 micrograms of huperzine can enter the body in a single administration. Like oral preparations, injections or transdermal preparations, it exerts its curative effect after being absorbed into the blood through the mucosa, so it will also have greater systemic toxicity.

Method used

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  • Targeted preparation via nose to brain of Huperzine and its derivant or its salt
  • Targeted preparation via nose to brain of Huperzine and its derivant or its salt

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Huperzine A 0.1g

[0048] Medicinal absolute ethanol 20g

[0049] Distilled water up to 100g

[0050] Preparation method: dissolve huperzine A with medicinal ethanol, and add distilled water to a sufficient amount. It can be directly made into nasal administration dosage forms such as nasal drops and nasal sprays.

Embodiment 2

[0052] Huperzine A 0.1g

[0053] Hydroxypropyl-β-cyclodextrin 10g

[0054] Distilled water up to 100g

[0055] Preparation method: Dissolve 10g of hydroxypropyl-β-cyclodextrin in 40g of distilled water, then add huperzine A, heat and stir in a water bath at 50°C to dissolve the drug completely, then add distilled water to a sufficient amount. It can be directly made into nasal administration dosage forms such as nasal drops and nasal sprays. Or freeze-dry, and then add an appropriate amount of 0.9% sodium chloride solution to the prepared sterile powder, suspend it and use it as nasal drops or spray nasal spray; or add an appropriate amount of sterile powder to a carrier with good fluidity, such as lactose, mannitol One or more than one of , starch or β-cyclodextrin, mixed evenly, filled, and inhaled through nasal powder inhalation device.

Embodiment 3

[0057] Huperzine A 0.1g

[0058] Polyoxyethylene hydrogenated castor oil condensate (Cremophor RH40) 8.1g

[0059] Medicinal absolute ethanol 3g

[0060] Polyglycerol Linoleate 1.25g

[0061] Distilled water up to 100g

[0062] Preparation method: first dissolve huperzine A with medicinal absolute ethanol, then add polyoxyethylene hydrogenated castor oil condensate (Cremophor RH40) and linoleic acid polyethylene glycol glyceride to dissolve, and slowly add distilled water to a sufficient Get what you need. The particle size of the microemulsion is between 2 and 18nm. It can be directly made into nasal administration dosage forms such as nasal drops and nasal sprays.

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Abstract

The present invention discloses one kind of nasal administrated brain-targeting preparation of hyperzine An and its derivative or salt. The preparation of the present invention is conveyed directly to brain via nasal cavity and olfactory passage to prevent and treat senile dementian and dysmnesian or to raise the memory and learning capacity of teenage. The preparation of the present invention has raised bioavailability in brain and thus lowered dosage and reduced toxic side effect. The preparation of the present invention is convenient in use and has raised patient compliance.

Description

technical field [0001] The present invention relates to nasal and brain targeting preparations of huperzine A and its derivatives or salts thereof. Background technique [0002] Huperzine A (Huperzine A), chemical name: (5R,9R,11E)-5-amino-11-ethylene-5,6,9,10-tetrahydro-7-methyl-5,9 -Methylene cycloaryl octane-2(1H)-pyridone, which is an alkaloid obtained from the phenolic part extracted from the Chinese herbal medicine Melaleuca [Huperzia serrata(Thunb)Thev], is a high-efficiency, low-toxicity and reversible acetylcholinesterase inhibitors (AChEI). Studies have shown that huperzine A is effective in Alzheimer's disease. The study also found that some derivatives of huperzine A have similar curative effect. The present invention relates to following huperzine A and derivatives thereof: [0003] [0004] X Y Z [0005] I H H NH 2 [0006] II H H [0007] III H CH 3 NH 2 [0008] IV CH 3 H NH 2 [0009] V CH 3 CH 3 NH ...

Claims

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Application Information

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IPC IPC(8): A61K9/72A61K31/438A61P25/28
Inventor 陶涛顾玉兰岳鹏赵雁陈庆华
Owner SHANGHAI INST OF PHARMA IND
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