New isoandrographolidume sulfonate, pharmaceutical composition containing sulfonate, preparation method and applications thereof

A technology of andrographolide and composition is applied to the new isoandrographolide sulfonated compound, the pharmaceutical composition containing the sulfonated compound and the fields of preparation and use thereof, which can solve the problem of affecting the clinical curative effect of the product, difficult to formulate product quality standards, etc. problem, to achieve the effect of simple composition, controllable quality and clear structure

Inactive Publication Date: 2009-10-21
YANTAI TARGET DRUG RES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, it is difficult to formulate product quality standards and affect the clinical efficacy of the product

Method used

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  • New isoandrographolidume sulfonate, pharmaceutical composition containing sulfonate, preparation method and applications thereof
  • New isoandrographolidume sulfonate, pharmaceutical composition containing sulfonate, preparation method and applications thereof
  • New isoandrographolidume sulfonate, pharmaceutical composition containing sulfonate, preparation method and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] This example discloses the preparation method of isoandrographolide and a composition containing isoandrographolide-19-sulfate, andrographolide sulfonate E, andrographolide, and andrographolide

[0038] (1) Preparation of total sulfonated andrographolide (refer to Chinese patent, patent authorization number CN1162420C):

[0039] Take 1000mL of absolute ethanol and place it in a reactor, slowly add 1000mL of concentrated sulfuric acid dropwise, stir well, add 1000g of andrographolide, stir well, and place it at room temperature for 72h. Add 1000mL of ethanol in a water bath, stir well, adjust the pH to 7.0, add ethanol until the alcohol content reaches 80%, let it stand for 24 hours, add a small amount of activated carbon, filter, recover ethanol from the filtrate, condense into a thick paste, and vacuum dry to obtain Andrographis paniculata Total sulfonates of lactones.

[0040] (2) The total sulfonates of andrographolide are separated by column chromatography to prepa...

Embodiment 2

[0066] Isoandrographolide-19-sulfate was prepared according to the method in Example 1, weighed 1g, dissolved in about 800mL of glucose isotonic solution, added 0.1% activated carbon and stirred for 10 minutes, filtered, added glucose isotonic solution to 1000mL, filtered , use 10% sodium hydroxide solution to adjust the pH value to 4.5-6.5, potting (injection solution with large capacity, specifications are 50mL / bottle, 100mL / bottle, 250mL / bottle, 500mL / bottle), sterilized at 100°C for 30 minutes , after the clarity inspection, the package is ready.

Embodiment 3

[0068] The composition is prepared according to Example 1. Weigh 25g of the composition, add 600mL of water for injection, stir to dissolve, add 25g of mannitol, stir to dissolve, add water for injection to 1000mL, mix well, and filter with a 0.22μm microporous membrane to obtain The solution was divided into 7mL vials, 2mL per vial, capped, put into a lyophilizer, and lyophilized according to the designed lyophilization curve to obtain a composition lyophilized powder injection (50 mg each).

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Abstract

The invention discloses a compound as a formula (1), a kalium salt, a sodium salt or an ammonium salt thereof and also discloses a pharmaceutical composition containing the compound as the formula (1), an isoandrographolidume sulfonate E, an andrographolic acid and andrographolidume and a preparation method thereof. The compound and the composition obtained by the method have favorable effects, such as an inflammatory factor resistant effect, an antibacterial effect, an analgesic effect and an antineoplastic effect. The invention also discloses a peroral preparation or an injection preparation prepared by using the compound and the composition.

Description

technical field [0001] The present invention relates to a novel andrographolide derivative, a composition containing the derivative, a preparation method thereof and an application in preparation of anti-inflammatory, anti-bacterial, anti-viral and anti-tumor drugs. Background technique [0002] Andrographolide is a diterpenoid in Andrographis paniculata (Burm.f.) Nees, molecular formula: C 20 h 30 o 5 , is a colorless square or rectangular crystal, m.p.230~232℃, [α] D 20 -126° (C=0.2, H 2 O). Very bitter taste, soluble in methanol, ethanol, propanol, pyridine, slightly soluble in chloroform, ether, hardly soluble in water and petroleum ether. Because andrographolide is insoluble in water, it brings difficulties to the preparation of injection. At present, there are many methods used to prepare various water-soluble derivatives of andrographolide to prepare injections, wherein Xiyanping injection is an injection made of total sulfonated andrographolide, Chinese patent...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D307/58A61K31/365A61P29/00A61P31/00A61P31/12A61P35/00
Inventor 刘珂许卉刘军锋邹晓丽于翠翠付颖颖邵萌李景源翟大伟
Owner YANTAI TARGET DRUG RES
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