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Salt of gambogicacid class compound, its preparation method, and medication combination with salt as active ingredient

A technology of gambogic acid and compound, applied in the field of salts of gambogic acid compounds, can solve problems such as failure to publish experimental data and solubility, and achieve the effect of improving anti-cancer effect and high medicinal value

Inactive Publication Date: 2004-05-26
杭州博大药物研究所
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] People such as You Qidong of China Pharmaceutical University have proposed a compound (publication number CN1309125A, Chinese invention patent application on August 22, 2001) with arginine, lysine and gambogic acid compounds, thinking Can improve the water solubility of gambogic acid compounds, but failed to publish the experimental data and solubility

Method used

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  • Salt of gambogicacid class compound, its preparation method, and medication combination with salt as active ingredient
  • Salt of gambogicacid class compound, its preparation method, and medication combination with salt as active ingredient
  • Salt of gambogicacid class compound, its preparation method, and medication combination with salt as active ingredient

Examples

Experimental program
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Effect test

example 1

[0027] The preparation of example 1. sodium gambogic acid

[0028] Take 10g of gambogic acid in a beaker, add an appropriate amount of distilled water, stir, and slowly add a sodium carbonate-sodium bicarbonate buffer solution with a pH of 9-11 until the gambogic acid is completely dissolved at a temperature below 10°C. After stirring evenly, filter and the filtrate Freeze-dry to obtain 11g of sodium gambogic acid.

example 2

[0029] Example 2. The preparation of new sodium gambogic acid

[0030] Take 10g of new gambogic acid in a beaker, add an appropriate amount of distilled water, stir, below 10°C, add a small amount of sodium carbonate-sodium bicarbonate buffer solution with a pH of 9-11, then slowly add 1 N NaOH solution until the new gambogic acid is completely dissolved, filter , The filtrate was freeze-dried to obtain 11g of sodium gambogic acid.

example 3

[0031] Example 3. The preparation of potassium gambogic acid

[0032] Take 10g of gambogic acid in a beaker, add an appropriate amount of 50% ethanol, stir, below 10°C, slowly add potassium carbonate-potassium bicarbonate buffer with pH 9-11, and then slowly add 1 NKOH solution until the gamboge After the acid was completely dissolved, it was filtered, and the filtrate was freeze-dried to obtain 11 g of potassium gambogic acid.

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Abstract

The salt of garcinolic acid kind of compounds is disclosed, which isa stable compound with a single structure and high feasibility and safety in medicinal research. Said salt, especially the neogarcinolate, has higher solubility in water and high anticancer effect. Its preparing process, the antineoplastic medicines using said salt as its active component, and the application of said antineoplastic medicines in treating liver cancer, intestinal cancer, lung cancer, gastric cancer, etc are also disclosed.

Description

technical field [0001] The present invention relates to a novel salt of gambogic acid compound, a preparation method thereof, a pharmaceutical composition containing the salt as an active ingredient, and their application in the preparation of antitumor drugs. Background technique [0002] Studies have shown that gambogic acid compounds have an inhibitory effect on tumors, but the solubility of gambogic acid compounds in water is extremely small, thus affecting their medicinal value. [0003] In recent years, academic circles have devoted themselves to improving the water solubility of gambogic acid compounds. Because gambogic acid compounds are unstable under alkaline conditions, especially when the pH value is greater than 12, the research direction of the academic circles is focused on finding suitable organic bases among the weaker organic bases to combine with vines. Flavonoids are compounded to increase its water solubility. [0004] People such...

Claims

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Application Information

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IPC IPC(8): A61K31/35A61P35/00C07D493/04
Inventor 金彪乔林沈国伟陈炜
Owner 杭州博大药物研究所
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