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A kind of pharmaceutical composition for treating and/or preventing Alzheimer's disease and use thereof

A technology for Alzheimer's disease and composition, applied in the field of pharmaceutical composition containing galantamine

Active Publication Date: 2016-02-17
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] There is no report of combining galantamine and lycorine oxide in the prior art

Method used

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  • A kind of pharmaceutical composition for treating and/or preventing Alzheimer's disease and use thereof
  • A kind of pharmaceutical composition for treating and/or preventing Alzheimer's disease and use thereof
  • A kind of pharmaceutical composition for treating and/or preventing Alzheimer's disease and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Evaluation of the Inhibitory Activity of Galantamine and Lycorine Oxide on Acetylcholinesterase by Modified Ellman Method

[0027] Instruments and materials

[0028] Instruments: BioTek Synergy2 multifunctional microplate reader (BioTek, USA), high-speed cryogenic centrifuge (SovallEvolutionRC, Kendro Corporation), vortex shaker (Vortex-Genie2, Scientific Industries, USA).

[0029] Reagents: acetylcholinesterase (AchE, from electric eel, enzyme activity: 687U / mg protein, Mr280kDa), acetylthiocholineiodide (AchE, AchE substrate, Mr289.2); 5,5'-di Thio-dithiobis(2-nitrobenzoic acid) (5,5-dithiobis(2-nitro)benzoic acid, DTNB) were purchased from Sigma–Aldrich (St. Louis, MO, USA); ultrapure water (Millipore, USA) , Tris-Hydroxymethylaminomethane Tris-base (Biosharp, Korea), and other reagents are of analytical grade.

[0030] Preparation of solution

[0031] Tris / HCl buffer: 20mM Tris buffer, containing 100mM NaCl, pH 7.5; AChE solution: take For AChE stock solution (...

Embodiment 2

[0053] Analysis on the effect of combined administration of galantamine and lycorine oxide

[0054] Based on the Median-effect Principle (moderate effect principle), the dose-response curve and the combination index curve (Fa-C curve) under different effects were drawn by using the CombiDrug statistical software. ,3,4,5 and figure 1 ,2,3,4,5) Quantitatively evaluate the synergistic, antagonistic or additive relationship between the two drugs. Specific steps are as follows:

[0055] The effect of the drug is the inhibition rate (fa)=1-(the reaction rate of the test sample solution / the reaction rate of the blank control sample) according to the intermediate effect equation fa / fu=(D / Dm) m , take the logarithm logfa / fu=mlogD-mlogDm on both sides, set a=-mlogDm, b=m, x=logD, y=logfa / fu, and substitute into the intermediate effect equation to get y=bx-a; where fa is the drug effect , fu=1-fa, D is the drug concentration, m is the slope, and Dm is the intermediate effect concentra...

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PUM

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Abstract

The invention discloses a medicament composition for preventing and / or treating alzheimer diseases. The composition is composed of galanthamine and lycobetaine. The two medicaments in combination have excellent synergistic effects on inhibition of acetylcholin esterase activity and can be used for treating alzheimer diseases. By using the composition, the administration dosage of galanthamine can be greatly reduced when being used for preventing and / or treating alzheimer diseases, therefore, the side effects of a medicament are avoided and the administration compliance is improved.

Description

technical field [0001] The invention relates to the field of natural medicines, in particular to a pharmaceutical composition containing galantamine for treating and / or preventing Alzheimer's disease and its application. Background technique [0002] Alzheimer's disease (Alzheimer's Disease, AD) is a degenerative disease of the central nervous system, clinically manifested as severe cognitive and memory dysfunction and decreased social adaptability. Its pathogenesis is complex, and its etiology has not yet been fully elucidated. Among them, acetylcholinesterase inhibitor (AChEI) is the most mature and successful method for the treatment of AD at present, and it is also the only type that has been approved by the US FDA for marketing. It is the earliest and most successful clinical application. It is the primary drug for AD treatment and is regarded as the standard treatment for mild to moderate AD patients. AChEIs mainly include donepezil, rivastigmine, tacrine and the alka...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/55A61P25/28A61K31/4745
Inventor 李萍李若倩石子琪郝海平陈君宋德芳王鼎乾
Owner CHINA PHARM UNIV