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Uses of dehydroandrographolide derivatives

A technology of dehydrating andrographolide and its derivatives, applied in the field of medicine, can solve problems such as the application of andrographolide and its derivatives to senile dementia, and achieve good development prospects

Active Publication Date: 2016-03-02
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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  • Uses of dehydroandrographolide derivatives
  • Uses of dehydroandrographolide derivatives
  • Uses of dehydroandrographolide derivatives

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 of dehydroandrographolide and 10.5g of N-benzyloxycarbonyl-glycine in 100ml of N,N-dimethylformamide, then add 10.3g of dicyclohexylcarbodiimide and 0.24g of 4-bis Aminopyridine, 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, eluted with a mixed solvent of ethyl acetate:petroleum ether (volume ratio: 1:3), and collected The target component was 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 ...

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 is the whole grass or leaves of 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 active ingredient of the natural plant ...

Claims

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Application Information

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Patent Type & Authority Patents(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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