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Method for preparing andrographolide derivatives and preparation thereof

A technology of andrographolide and derivatives is applied in the field of medicine and achieves the effects of stable drug quality and simple preparation process

Inactive Publication Date: 2009-09-16
北京天恒永康医药科技有限责任公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, the adamantane salt of andrographolide has not been reported for the treatment of upper respiratory tract infection, pneumonia, bronchitis, influenza, etc.

Method used

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  • Method for preparing andrographolide derivatives and preparation thereof
  • Method for preparing andrographolide derivatives and preparation thereof
  • Method for preparing andrographolide derivatives and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016]

[0017] 30.3 (N-C-CH 2 - C h 2 ).

[0018] MW 187.7 C 10 h 17 N HCl

[0019] Physical and chemical properties: slightly soluble in water, soluble in chloroform. MP180~192℃. Hydrochloride was dissolved in 5 times ethanol, 18 times chloroform, 2.5 times water. Ph3.5-5, 1.87g amantadine hydrochloride (0.01mol) + 5ml distilled water dissolved, 25% NaOH (1.6ml, theoretical amount) to adjust Ph9-10, a large amount of solid precipitated, washed with water and dried. MP215~225℃

[0020] Yanhuning

[0021]

[0022] MW C 28 h 34 KNaO 10 h 2 O 610.6 Ph6.0-8.0 unstable.

[0023]

[0024] Andrographolide Disuccinate Half Ester MW C 28 h 36 o 10 532.5 MP Measured at 102-110°C (137-140°C literature) andrographolide disuccinic acid half ester 2.67g (0.005mol) was added to 40ml of chloroform, slightly heated to dissolve. Add 1.51 g (0.01 mol) of amantadine into 30 ml of chloroform to dissolve. Under stirring at room temperature, the amantadine / chloroform so...

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Abstract

The invention relates to a method for preparing andrographolide derivatives, and a preparation thereof. The preparation is a salt which consists of Kalii Dethydroandrographolidi Succinas and Adamantanes and has the effect of synergistic interaction. The curative effect of the preparation is better than that of the independent use of Kalii Dethydroandrographolidi Succinas and Adamantanes.

Description

technical field [0001] The invention relates to a salt composed of 14-dehydroxy-11,12-didehydroandrographolide-3,19-disuccinic acid half esters and adamantanes for anti-infection, anti-virus and antipyretic A pain compound, and a preparation method and application thereof belong to the technical field of medicine. Background technique [0002] Andrographis paniculata is the dry aerial part of Andrographis Paniculata (Burm.f.) Nees, a plant of the Acanthaceae family. It has the functions of clearing heat and detoxifying, cooling blood, and reducing swelling. Its main active ingredient is andrographis lactone. Its derivatives after esterification, dehydration, and salt formation can inhibit early capillary permeability increase, inflammatory exudation, and edema, and can specifically stimulate the pituitary-adrenal cortex function, promote the release of ACTH, and increase the anterior pituitary gland. The biosynthesis of ACTH in the middle; it has the function of inactivatin...

Claims

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Application Information

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IPC IPC(8): C07D307/58C07C211/38A61K31/365A61K31/13A61P11/00A61P29/00
Inventor 谢开智谢开书李玲王浩罗振福
Owner 北京天恒永康医药科技有限责任公司
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