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Pharmaceutical composition, preparation method and application of huperzine in-situ gel spray

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: 2011-11-30
SHANGHAI INST OF PHARMA IND CO LTD
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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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  • Pharmaceutical composition, preparation method and application of huperzine in-situ gel spray
  • Pharmaceutical composition, preparation method and application of huperzine in-situ gel spray
  • Pharmaceutical composition, preparation method and application of huperzine in-situ gel spray

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 amount

[0037] Appropriate amount of ethanolamine

[0038] Add deionized water to 1000ml

[0039] Preparation method: Weigh the prescribed amount of mannitol, gellan gum, methylparaben and propylparaben, add 900ml of deionized water, and heat in a water bath at 90°C to dissolve completely. Dissolve Huperzine A with 30ml of 0.1mol / L hydrochloric acid, add it into the above solution under stirring, and mix well. Use 30% ethanolamine to adjust the pH to 6.5, add deionized water to reach the total amount, divide into white medical plastic bottles, and install a nasal cavity spray pump to obtain 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 amount

[0048] Appropriate amount of trishydroxymethyl aminomethane

[0049] Add deionized water to 1000ml

[0050] Preparation method: Weigh the prescribed amount of mannitol, gellan gum, methylparaben and propylparaben, add 900ml of deionized water, and heat in a water bath at 90°C to dissolve completely. Dissolve huperzine A with 50ml of 0.1mol / L hydrochloric acid, add it into the above solution under stirring, and mix well. Use 30% tris to adjust the pH to 5, add deionized water to make the total amount, divide into white medical plastic bottles, and install a nasal cavity spray pump to obtain 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 amount

[0059] Appropriate amount of trishydroxymethyl aminomethane

[0060] Add deionized water to 1000ml

[0061] Preparation method: Weigh the prescribed amount of mannitol, gellan gum, methylparaben and propylparaben, add 850ml of deionized water, and heat in a water bath at 90°C to dissolve completely. Dissolve Huperzine A with 100ml of 0.1mol / L hydrochloric acid, add it into the above solution under stirring, and mix well. Use 30% tris to adjust the pH to 8, add deionized water to reach the total amount, divide into white medical plastic bottles, and install a nasal cavity spray pump to obtain the product.

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Abstract

The invention discloses a composition for constituting the in-situ gel spray for huperzine turbinitis, as well as its preparation method and application. The preparation is a nasal preparation which is in a liquid state in vitro and becomes a gel state when sprayed into a nasal cavity. It uses huperzine A as the active ingredient, supplemented with in-situ gel forming agent, isotonic regulator, pH regulator, preservative, water, etc. It is a nasal in-situ gel spray, which is suitable for the prevention and treatment of elderly people Dementia and middle-aged and elderly memory impairment or improve the memory and learning ability of adolescents. The nasal preparation is in a liquid state in vitro, the dosage is easy to accurately control, and it is convenient to use. When sprayed into the nasal cavity, it can be evenly dispersed on the surface of the nasal mucosa, and diffuses with the nasal mucus to form a gel, which stays in the nasal cavity for a long time and is not easy to be lost. The bioavailability of cerebrospinal fluid, brain, and hippocampus is 2.2 to 2.7 times that of oral administration, and the drug effect is 2 to 4 times that of oral administration. It has small local irritation, low toxicity, and good biocompatibility.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to a composition for constituting the in-situ gel spray for huperzine turbinitis, as well as a preparation method and application of the composition. 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, an alkaloid obtained from the phenolic part extracted from the Chinese herbal medicine Melaleuca [Huperzia serrata(Thunb)Thev], is a highly efficient and reversible Acetylcholinesterase inhibitors. Studies have shown that huperzine A is effective in Alzheimer's disease. After retrieval, it is 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 inhi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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 CO LTD
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