Slow-release small pill prparation containing huperzine A and method for making same

A technology of Huperzine A and sustained-release pellets, applied in the field of pharmaceutical preparations, can solve problems such as unfavorable treatment of patients, inconvenient dosage forms of Huperzine A, and achieve the effects of reducing toxic side effects, improving bioavailability, and completely releasing

Inactive Publication Date: 2007-12-05
上海特敏生物医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] The object of the present invention is to provide a kind of sustained-release pellet preparation containing huperzine A, described this sustained-release pell...

Method used

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  • Slow-release small pill prparation containing huperzine A and method for making same
  • Slow-release small pill prparation containing huperzine A and method for making same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Embodiment 1 0.044% (weight) huperzine A sustained-release pellet preparation

[0040] All of the various substances described below are expressed in grams of dry matter for a final amount of 5000 g sustained release pellet formulation.

[0041] composition

[0042] Neutral ball core 4432.62

[0043] Active layer:

[0044] Huperzine A 2.22

[0045] Polyacrylic resin RS 4.43

[0046] Slow release layer:

[0047] Ethyl cellulose 443.26

[0048] Dibutyl sebacate 106.38

[0049] Talc powder 11.08

[0050] Steps:

[0051] A. Dissolve huperzine A, or the acid salt of pharmaceutically acceptable huperzine A and binding agent—polyacrylic acid resin RS in the aqueous ethanol solution, in the described aqueous ethanol solution, the The mass percentage concentration of ethanol is 50~95%;

[0052] B. Prepare the neutral ball core, spray the solution prepared above onto the neutral ball core and dry it, forming an active layer on the outside of the neutral ball core;

[0...

Embodiment 2

[0055] Embodiment 2 0.008% (weight) huperzine A sustained-release pellet preparation

[0056] All of the various substances described below are expressed in g of dry matter for a final amount of 5000 g sustained release pellet formulation (preparation as above).

[0057] composition

[0058] Neutral ball core 4440.0

[0059] Active layer:

[0060] Huperzine A 0.4

[0061] Polyvinylpyrrolidone 2.0

[0062] Slow release layer:

[0063] Polyacrylic resin RS type 491.0

[0064] Triethyl citrate 49.1

[0065] Talc 17.5

Embodiment 3

[0066] Embodiment 3 0.015% (weight) huperzine A sustained-release pellet preparation

[0067] All of the various substances described below are expressed in g of dry matter for a final amount of 5000 g sustained release pellet formulation (preparation as above).

[0068] composition

[0069] Neutral ball core 4500.0

[0070] Active layer:

[0071] Huperzine A 0.75

[0072] Methylcellulose 3.0

[0073] Slow release layer:

[0074] Ethyl cellulose 360.3

[0075] Talc powder 135.95

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Abstract

The slow released Huperzine A pillet comprising one neutral core, one active layer containing Huperzine A and coating the core, and one slow releasing layer coating the active layer. It is prepared through a solvent dispersing process to coat the Huperzine A medicine onto the neutral core and subsequent coating the slow releasing layer. The present invention has raised medicine content homogeneity, ensures the stable, slow and complete release of the medicine, makes Huperzine A be absorbed in stomach, small intestine and colon to maintain the treating concentration of Huperzine A in blood and raises the compliance of the patient greatly.

Description

Technical field: [0001] The invention relates to a pharmaceutical preparation, in particular to a sustained-release pill preparation, in particular to a sustained-release pellet preparation containing huperzine A and a preparation method thereof. Background technique: [0002] The chemical name of huperzine A is (5R,9R,11E)-5-amino-11ethylene-5,8,9,10-tetrahydro-7-methyl-5,9-methylenecyclooctyl Tetraeno"b"pyridin-2(1H)-ones having the following structure: [0003] [0004] Huperzine A can be isolated from the natural Chinese herbal medicine Huperzia serrata. It is a reversible inhibitor of acetylcholinesterase. It has the characteristics of high selectivity, low toxicity and long drug effect time. It is an ideal treatment for senile dementia in the world so far. Outlook drug. [0005] The active ingredient huperzine A extracted from the Chinese herbal medicine Huperzia serrata is currently the most potent and selective acetylcholinesterase inhibitor in nature. A series ...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K31/439A61K47/30A61P25/28
Inventor 周菊珍林益华潘俊芳李莉胡英伟俞晓燕徐峥
Owner 上海特敏生物医药科技有限公司
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