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Dehydroandrographolide derivative composition and preparation method as well as application thereof

A technology of dehydrated Andrographis paniculata and composition, applied in the field of medicine, can solve the problems of affecting purity, poor recrystallization effect, affecting the stability of ester bonds, etc., and achieve the effects of cardiovascular protection, stability improvement, and good curative effect.

Inactive Publication Date: 2014-01-01
HARBIN ZHENBAO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Chuanhuning (dehydroandrographolide succinate half-ester monopotassium salt) increases its water solubility after salting the free carboxyl group, and mostly forms potassium and sodium salts; however, the potassium salt is highly alkaline, which affects the stability of the ester bond, and The recrystallization effect is not good, affecting the purity

Method used

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  • Dehydroandrographolide derivative composition and preparation method as well as application thereof
  • Dehydroandrographolide derivative composition and preparation method as well as application thereof
  • Dehydroandrographolide derivative composition and preparation method as well as application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Example 1 Preparation of Dehydroandrographolide Glycine Half Ester Hydrochloride

[0053] 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;

[0054] 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 palladium carbon wa...

Embodiment 2

[0055] Example 2 Dehydroandrographolide derivative composition freeze-dried powder injection

[0056] 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;

[0057] 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;

[0058] 3) Freeze-dry the liquid medicine, press the plug, and seal it to obtain the product.

Embodiment 3

[0059] Example 3 Dehydroandrographolide derivative composition freeze-dried powder injection

[0060] 1) Dissolve 0.5 g of edetate calcium sodium in 600 ml of water for injection, add 100 g of dehydrated andrographolide glycine half ester hydrochloride prepared in Example 1, stir to dissolve, and obtain a solution;

[0061] 2) Add 20g of lactose to the solution to dissolve it, adjust the pH value to 7.0, add water for injection to 1000ml, filter the resulting liquid deeply, divide the liquid into vials, 1ml per bottle, and transfer to freeze-drying Inside the machine;

[0062] 3) Freeze-dry the liquid medicine, press the plug, and seal it to obtain the product.

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Abstract

The invention provides a dehydroandrographolide glycine semi-ester hydrochloride derivative composition. The composition comprises dehydroandrographolide glycine semi-ester hydrochloride, a metal complexing agent and / or other pharmaceutically acceptable carriers. The invention also provides a preparation method as well as application of the composition. The composition can be used for adjusting the nonspecific immunity function, and has anti-tumor, anti-pyretic, anti-inflammatory, anti-virus, liver protection, cholagogic, anti-diabetic, anti-fertility and cardiovascular protection effects. The purity of the active ingredient of the composition is high, and the risk of adverse effect caused by impurities is avoided; the composition is in a scientific proportion, so that the stability of the medicament is greatly improved and other serious adverse events caused by degradation and polymer formation occurring in manufacturing and storage of the medicament are avoided; the composition has a better curative effect and an excellent effect on the adjustment of the nonspecific immunity function.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to a dehydroandrographolide derivative composition and its preparation method and application, in particular to a dehydroandrographolide glycine half ester hydrochloride composition and its preparation method and application. Background technique [0002] Andrographolide is a diterpene lactone compound extracted from Andrographis paniculata, a plant of the Acanthaceae family. It is one of the main active ingredients of the traditional Chinese medicine Andrographis paniculata. It has the functions of clearing away heat and detoxification, cooling blood and reducing swelling. Andrographolide is insoluble in water, and different hydrophilic groups need to be introduced into the lactone structure to enhance its water solubility, so as to exert corresponding pharmacological effects. A large number of andrographolide derivatives such as Xiyanping injection, Chuanhuning injection, Yanhuning ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/365A61P35/00A61P29/00A61P31/12A61P1/16A61P3/10A61P15/00A61P9/00A61P31/16C07D307/58
Inventor 方同华周广红董雪婷朱自力高丽
Owner HARBIN ZHENBAO PHARMA
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