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Novel application of dehydroandrographolide derivative

A technology for dehydrating andrographis paniculata and derivatives, applied in the field of medicine, can solve the problems such as the application of andrographolide and its derivatives for senile dementia, which has not yet been seen, and achieve the effect of good development prospects.

Active Publication Date: 2014-05-07
HARBIN ZHENBAO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The application of andrographolide and its derivatives for senile dementia has not been seen

Method used

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  • Novel application of dehydroandrographolide derivative
  • Novel application of dehydroandrographolide derivative
  • Novel application of dehydroandrographolide derivative

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Embodiment 1: the preparation method of dehydroandrographolide glycine half ester hydrochloride

[0027] 1) Dissolve 6.64g dehydroandrographolide, 10.5g N-benzyloxycarbonyl-glycine in 100ml N,N-dimethylformamide, then add 10.3g dicyclohexylcarbodiimide and 0.24g4 -Dimethylaminopyridine, warmed to room temperature and stirred for 8h, filtered, and the filtrate was evaporated to dryness under reduced pressure; the residue was separated by silica gel column chromatography, and eluted with a mixed solvent of ethyl acetate:petroleum ether (1:3 by volume) , collected the target components, and concentrated to dryness under reduced pressure to obtain 8.8 g of 3,19-0-bis-(N-benzyloxycarbonylglycyl)-dehydroandrographolide;

[0028] 2) Dissolve 8.8 g of 3,19-0-bis-(N-benzyloxycarbonylglycyl)-dehydroandrographolide in 100 ml of ethanol, add 1.2 g of 10% palladium carbon, and store at room temperature under a hydrogen atmosphere of 1 atmosphere After stirring for 3 hours, the pall...

Embodiment 2

[0029] Embodiment 2: Dehydroandrographolide derivative composition freeze-dried powder injection

[0030] 1) Dissolve 0.3 g of disodium edetate in 500 ml of water for injection, add 40 g of dehydrated andrographolide glycine half ester hydrochloride prepared in Example 1, stir to dissolve, and obtain a solution;

[0031] 2) Add 30g of mannitol to the solution to dissolve it, adjust the pH value to 7.5, add water for injection to 1000ml, filter the resulting liquid deeply, divide the liquid into vials, 1ml per bottle, and transfer to the freezer in the dryer;

[0032] 3) Freeze-dry the liquid medicine, press the plug, and seal it to obtain the product.

Embodiment 3

[0033] Embodiment 3: dehydroandrographolide derivative aqueous injection

[0034] 1) Dissolve 0.1 g of calcium sodium edetate in 400 ml of water for injection, add 10 g of dehydrated andrographolide glycine half ester hydrochloride prepared in Example 1, stir to dissolve, and obtain a solution;

[0035] 2) Add 40g of fructose to the solution to dissolve it, adjust the pH value to 6.8, add water for injection to 1000ml, filter the resulting liquid in depth, wait for the liquid to cool to 30°C, fill it, 2ml per bottle, and extinguish at 115°C Bacteria for 40 minutes, that is.

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PUM

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Abstract

The invention relates to application of a dehydroandrographolide derivative in preparation of a medicine for treating dementia. Experiments discover that the dehydroandrographolide derivative, such as dehydroandrographolide glycine semi-ester hydrochloride, has a remarkable dose-effect relationship on the aspect of treating dementia. The novel application of the dehydroandrographolide derivative provides a brand-new thought in treating alzheimer disease, and has a good development prospect.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to a new application of dehydroandrographolide derivatives, in particular to the therapeutic effect of dehydroandrographolide glycine half ester hydrochloride on Alzheimer's disease (AD). Background technique [0002] Andrographis paniculata (Burm.f.) Nees is the whole grass or leaf of the Acanthaceae plant Andrographis paniculata (Burm.f.) Nees. Also known as spring lotus and autumn willow, happy at first sight, elemi, bitter gall grass, golden vanilla, golden ear hook, Indian grass, bitter grass and so on. The main active ingredients are flavonoids and Andrographolide, Neoandrographolide, Dehydroandrographolide, 14-Deoxyandrographolide (DA) and 14-Deoxy-11,12- Didehydroandrographolide (DDA), etc., lactones are collectively referred to as total andrographolide. [0003] Dehydroandrographolide (dehydroandrographolide), also known as andrographolide. Andrographolide is the main acti...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/365A61P25/28
Inventor 方同华周广红董雪婷李振宇
Owner HARBIN ZHENBAO PHARMA
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