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Pharmaceutical composition for nose administered in-situ gel spray of Huperzine A, preparation process and use thereof

A technology of huperzine A and in-situ gel, applied in the field of pharmacy, can solve the problems of toxic and side effects of the human body and low brain selectivity, and achieve the effects of less irritation, good compatibility and improving brain selectivity.

Inactive Publication Date: 2007-05-16
SHANGHAI INST OF PHARMA IND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] In order to overcome the shortcoming that the brain selectivity is not high when using huperzine A to treat senile dementia at present, it is easy to produce toxic and side effects on the human body while achieving the therapeutic effect, and taking into account that huperzine A is more suitable for being applied to the human body, the present invention is proposed

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Preparation formula and preparation method:

[0031] Huperzine A 0.5g

[0032] Gellan Gum 5g

[0033] Mannitol 50g

[0034] Methylparaben 1.8g

[0035] Propylparaben 0.2g

[0036] Hydrochloric acid appropriate amount

[0037] Ethanolamine appropriate amount

[0038] Add deionized water to 1000ml

[0039] Preparation method: Weigh the prescribed amounts of mannitol, gellan gum, methylparaben and propylparaben, add 900ml of deionized water, and heat in a 90°C water bath to dissolve completely. Huperzine A was dissolved in 30 ml of 0.1 mol / L hydrochloric acid, added to the above solution under stirring, and thoroughly mixed. Adjust the pH to 6.5 with 30% ethanolamine, add deionized water to the total amount, divide into white medical plastic bottles, and install a nasal spray pump to get the product.

Embodiment 2

[0041] Preparation formula and preparation method:

[0042] Huperzine A 1g

[0043] Gellan Gum 5g

[0044] Mannitol 50g

[0045] Methylparaben 1.8g

[0046] Propylparaben 0.2g

[0047] Hydrochloric acid appropriate amount

[0048] Tris(hydroxymethylaminomethane)

[0049] Add deionized water to 1000ml

[0050] Preparation method: Weigh the prescribed amounts of mannitol, gellan gum, methylparaben and propylparaben, add 900ml of deionized water, and heat in a 90°C water bath to dissolve completely. Huperzine A was dissolved in 50 ml of 0.1 mol / L hydrochloric acid, added to the above solution under stirring, and thoroughly mixed. Adjust pH to 5 with 30% tris(hydroxymethyl)aminomethane, add deionized water to the total amount, pack in white medical plastic bottles, and install a nasal spray pump to get the product.

Embodiment 3

[0052] Preparation formula and preparation method:

[0053] Huperzine A 2g

[0054] Gellan Gum 6g

[0055] Glucose 50g

[0056] Methylparaben 1.8g

[0057] Propylparaben 0.2g

[0058] Hydrochloric acid appropriate amount

[0059] Tris(hydroxymethylaminomethane)

[0060] Add deionized water to 1000ml

[0061] Preparation method: Weigh the prescribed amounts of mannitol, gellan gum, methylparaben and propylparaben, add 850ml of deionized water, and heat in a 90°C water bath to dissolve completely. Huperzine A was dissolved in 100 ml of 0.1 mol / L hydrochloric acid, added to the above solution under stirring, and thoroughly mixed. Adjust the pH to 8 with 30% tris(hydroxymethyl)aminomethane, add deionized water to the total amount, pack in white medical plastic bottles, and install a nasal spray pump to get the product.

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PUM

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Abstract

The invention relates to a compound of original gel atomizer of Huperzine nose, and relative preparation, wherein it is external liquid, which can be atomized into nose as gel state. The invention use Huperzine as active component, assisted with original gel agent, pH adjuster, water, etc. The invention can treat senile dementia, and improve memory level of children. The invention has simple application, while it can be atomized into nose. And its cerebrospinal fluid and jordonet snyder utilization is 2.2-2.7 times of oral agent, and its effect is 2-4 times of oral agent, with low toxic.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to a composition for forming Huperzine A nasal in-situ gel spray, a preparation method of the composition and the use 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 ring aromatic octano-2(1H)-pyridone, an alkaloid obtained from the phenolic fraction extracted from Chinese herbal medicine Huperzia serrata (Thunb) Thev, is a highly efficient and reversible Acetylcholinesterase inhibitors. Studies have shown that Huperzine A is effective against Alzheimer's disease. After searching, it was found that the preparations of Huperzine A include tablets, capsules, transdermal preparations (including transdermal controlled-release patches), injections and sustained-release microspheres for injection. Since Huperzine A is a non-brain-selective acetylcholinesterase inhibitor, the existing p...

Claims

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Application Information

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IPC IPC(8): A61K31/435A61K9/12A61P25/28A61P25/00
Inventor 陶涛赵雁岳鹏张春娜吴金金陈庆华
Owner SHANGHAI INST OF PHARMA IND
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