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Lemon acid berbamine salt, preparation method and application thereof

A technology of berberine salt and citric acid, applied in the field of chemistry, can solve problems such as affecting the anti-tumor effect, and achieve the effects of improving bioavailability, high safety and high success rate

Inactive Publication Date: 2009-05-13
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The hydrophobicity of berbamine and the low water solubility of berbamine hydrochloride will undoubtedly affect its antitumor effect

Method used

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  • Lemon acid berbamine salt, preparation method and application thereof
  • Lemon acid berbamine salt, preparation method and application thereof
  • Lemon acid berbamine salt, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Embodiment 1: preparation of berbamine citrate monohydrate

[0034] At room temperature, weigh 20 grams of berbamine, put into a glass beaker, then add 200 milliliters of 2.5% citric acid monohydrate (C 6 h 5 o 7 .H 2 (0) solution, stirring, until the berbamine is completely dissolved, and the solution is completely transparent, then the berbamine citrate salt solution is dried to obtain slightly yellow or white berbamine citrate crystallization.

[0035] Reaction formula:

[0036]

[0037] Berbamine Citrate Monohydrate Berbamine Salt

[0038] Experimental results show: the berbamine citrate monohydrate salt prepared by applying this method not only has a high success rate (100%); moreover, the required reagents are few, only citric acid and water are needed, and the operation steps are few and simple, which is easy to use in ordinary laboratories. to operate.

Embodiment 2

[0039] Embodiment 2: preparation of anhydrous berbamine citrate

[0040] At room temperature, weigh 20 grams of berbamine, put it into a glass beaker, then add 200 milliliters of 2.5% anhydrous citric acid (C 6 h 5 o 7 ) solution, stirring, until the berbamine is completely dissolved and the solution is completely transparent, then the berbamine citrate solution is dried to obtain slightly yellow or white berbamine citrate crystals.

[0041]

[0042] Berbamine Citrate Anhydrous Berbamine Salt

[0043] Experimental results show: the anhydrous berbamine citrate salt prepared by applying this method not only has a high success rate (100%); moreover, the required reagents are few, only citric acid and water are needed, and the operation steps are few and simple, which is easy to use in ordinary laboratories. to operate.

Embodiment 3

[0044] Embodiment 3: Solubility comparison of berbamine citrate and berbamine hydrochloride

[0045] Weigh 0.1 g of berbamine citrate and berbamine hydrochloride respectively at room temperature, put them into 10ml test tubes, then slowly add deionized water, shake well while adding, until the added berbamine salt is fully dissolved , until the solution becomes completely transparent. Then, the water required to completely dissolve the berbamine salt was measured, and the solubility of the berbamine salt in water was calculated.

[0046] Experimental results show that: the solubility of berbamine citrate in water is about 500mg / ml, and the solubility of berbamine hydrochloride in water is about 30mg / ml. The water solubility of berbamine citrate is 16.6 times that of berbamine hydrochloride.

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Abstract

The invention provides berbamine citrate. Berbamine free alkali is taken as a raw material, and edible strong organic acid is applied to substitute the prior commonly-used inorganic acid to perform a salt-forming reaction according to certain proportion at room temperature to obtain the berbamine citrate. The berbamine citrate has remarkable killing effect on various hematological tumor cells cultured in vitro such as human leukemia, multiple myeloma, lymphoma and so on, and also has remarkable inhibition effect on the growth of human hematological tumor cells in the bodies of nude mice, but the berbamine citrate with the same concentration has no remarkable effect on the cell growth of normal persons and has no remarkable toxic side effect on the nude rice; and the berbamine citrate can form a pharmaceutical composition with other optional known anti-tumor medicines with one or more therapeutically effective amounts to achieve the synergistic effect. Therefore, the berbamine citrate can be applied to the preparation of medicines for treating hematological tumor diseases.

Description

technical field [0001] The invention belongs to the field of chemistry, and relates to berbamine citrate and its preparation, as well as a drug combination containing them and their application in preparation and treatment of hematological tumor diseases. Background technique [0002] According to the report of the World Health Organization: in 2007, about 25 million people in the world suffered from various cancers, and 7.9 million people died of these cancers (accounting for about 13% of all deaths). Cancer deaths are projected to continue to increase worldwide, with an estimated 12 million deaths from cancer in 2030. Cancer claimed nearly 1.8 million lives in China in 2006, about 300,000 more than in 2005. The 2006 Statistical Bulletin on the Development of China's Health Care, produced by the Health Statistics Center of the Ministry of Health, indicated that cancer "topped the list" for the first time among the causes of death among urban and rural residents in 2006. A...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D491/18A61K31/4748A61P35/00
Inventor 徐荣臻黄文栋张旭照古莹干小仙
Owner ZHEJIANG UNIV
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