Defervescence anti-inflammatory and anti-infection medicine with immunization function, preparation and application thereof

An immune function and anti-infection technology, applied in the field of medicine, to achieve the effect of easy storage and transportation, good water solubility

Active Publication Date: 2010-01-20
刘力
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] The current published literature has only reported 14-dehydroxyl-13-dehydroandrographolide-12-sodium sulfonate without crystal water [C 20 h 29 o 7 SNa molecular weight: 436.47] (such as: Meng Zhengmu. Pharmacological Journal. 1981,16 (8): 571-575.), so far, there is no open literature report at home and abroad to have antipyretic, anti-inflammatory, anti-inflammatory and anti-inflammatory drugs with immune effects. Infection drug andrographolide derivatives - 14-dehydroxy-13-dehydroandrographolide-12-sulfonic acid sodium salt hydrate or andrographolide sodium bisulfite hydrate [C 20 h 29 o 7 SNa·nH 2 O, n=0.88~3.5] and its preparation method and use

Method used

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  • Defervescence anti-inflammatory and anti-infection medicine with immunization function, preparation and application thereof
  • Defervescence anti-inflammatory and anti-infection medicine with immunization function, preparation and application thereof
  • Defervescence anti-inflammatory and anti-infection medicine with immunization function, preparation and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0070] Embodiment 1 Preparation of Andrographolide Sodium Bisulfite 2 Hydrate In a 1000ml three-necked flask, add ethanol 220ml, methyl alcohol 30ml and Andrographolide 100g, heat for dissolution, add 150ml of aqueous solution of Sodium Bisulfite (30g), heat Reflux for 30 minutes, concentrate under reduced pressure to dryness, add 400ml of distilled water to dissolve, filter after cooling, extract the filtrate with chloroform three times, 100ml each time, separate the chloroform layer, filter the water layer, concentrate the filtrate under reduced pressure to near dryness, add 1: 1 ethanol and isopropanol solution, heated to dissolve, cooled, filtered, the filtrate was concentrated under reduced pressure to near dryness, filtered, and then recrystallized with ethanol and diisopropyl ether as solvents, and the solid was dried at about 100°C for 2-4 Obtained 86.3g of off-white crystalline powder in 1 hour, melting point: 226.2-228.4°C decomposed (uncorrected), UV spectrum: λ H2O...

Embodiment 2

[0072] Example 2 Preparation of Andrographolide Sodium Bisulfite Trihydrate Get 100 g of Andrographolide, add 220 ml of ethanol, and 30 ml of isopropyl ether in a 1000 ml three-necked flask, heat, add dropwise 150 ml of 2M aqueous sodium sulfite solution, reflux for half an hour, reduce After concentrated under pressure, extract 3 times with chloroform and dichloromethane, 150ml each time, separate the organic layer, filter the water layer, concentrate the filtrate under reduced pressure, add ethanol, cool, filter, concentrate the filtrate under reduced pressure, and dry at room temperature to obtain a sample 82 grams, melting point: 215.5-218.6°C (uncorrected), UV spectrum: λ H2O max 203nm (ε, 10500), ESI-MS: m / z: 436; Infrared spectrum: v KBr max cm -1 3446, 2939, 2870, 1756, 1644, 1200, 1143, 898; Karl Fischer's method measures moisture to be 12.26%, thermal analysis TG-DTA: platform weight loss is about 11.31%, which is consistent with the result that the sample contain...

Embodiment 3

[0073] Example 3 Preparation of andrographolide sodium bisulfite 2.5 hydrate In a three-necked flask, add 20 g of andrographolide, 55 ml of ethanol, and 5 ml of methanol, heat to dissolve, add 30 ml of 2M aqueous sodium sulfite solution under stirring, heat, and reflux for 0.6 h , concentrated under reduced pressure, extracted 3 times with chloroform and dichloromethane, 100ml each time, separated the organic layer, filtered the water layer, concentrated under reduced pressure to near dryness, crystallized with ethanol and isopropanol mixed solvent (1: 2), filtered, Dry at about 72°C to obtain 16g of off-white powder, easily soluble in water; melting point: 219.3-222.6°C decomposition (uncorrected); UV spectrum: λ H2O max 203nm (ε, 10500), ESI: m / z: 436; Infrared spectrum: v KBr max cm -1 3446, 2939, 2870, 1756, 1644, 1200, 1143, 898, moisture (Karl Fischer method): 9.26%, thermal analysis TG-DTA: about 9.82% of the platform weight loss, which is the same as the result that...

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Abstract

The invention relates to a defervescence anti-inflammatory and anti-infection medicine with immunization function, a preparation and an application thereof. Andrographolidume derivant is andrographolidume sodium bisulfite hydrate, and the molecular formula of the andrographolidume sodium bisulfite hydrate is C20H29O7SNa.nH2O, wherein n is equal to a number between 0.88 and 3.5. The derivant has better water solubility and better storage stability, and is suitable to prepare treatment or prevention medicines for reducing fever and relieving internal heat of fever, resisting bacteria and diminishing inflammation, resisting virus and allaying fever, and adjusting immunologic function.

Description

technical field [0001] The present invention relates to the technical field of medicine, and specifically provides an antipyretic, anti-inflammatory, and anti-infection drug with immune effects-andrographolide derivatives and its preparation and application, that is, dehydroxydehydroandrographolide sulfonate sodium salt Compounds and their preparation and use. Background technique [0002] The current published literature has only reported 14-dehydroxyl-13-dehydroandrographolide-12-sodium sulfonate without crystal water [C 20 h 29 o 7 SNa molecular weight: 436.47] (such as: Meng Zhengmu. Acta Pharmaceutica Sinica. 1981,16 (8): 571-575.), so far, there is no published literature report at home and abroad to have antipyretic, anti-inflammatory, anti-inflammatory and anti-inflammatory drugs with immune effects. Infection drug andrographolide derivatives - 14-dehydroxy-13-dehydroandrographolide-12-sulfonic acid sodium salt hydrate or andrographolide sodium bisulfite hydrate [...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D307/60A61K31/365A61K9/19A61K9/14A61K9/08A61P37/02A61P29/00A61P31/00A61P11/00A61P1/00A61P9/00
CPCY02A50/30
Inventor 刘力
Owner 刘力
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