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Crystal forms of asiatic acid tromethamine salt and preparation methods thereof

A technology of tromethamine and salt crystals is applied in the field of a class of tromethamine asiatica crystal forms and the preparation thereof, and can solve the problems that there is no tromethamine crystalline form of asiatic acid, and achieves The preparation method is simple, the operation is simple, and the effect of good stability

Active Publication Date: 2012-12-19
安徽林宇新创医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the asiatic acid tromethamine salt in the prior art exists in a semi-crystalline or amorphous state, and there is no report on the crystal form of the asiatic acid tromethamine salt

Method used

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  • Crystal forms of asiatic acid tromethamine salt and preparation methods thereof
  • Crystal forms of asiatic acid tromethamine salt and preparation methods thereof
  • Crystal forms of asiatic acid tromethamine salt and preparation methods thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-15

[0035] Example 1-15 Preparation of asiatic acid tromethamine salt crystal form A

Embodiment 1

[0037] Put 1g of amorphous asiatic acid tromethamine salt in a stirred container, add 100ml of acetonitrile into it at 20°C, start stirring for 72 hours, filter the suspension with suction, and dry the filter cake. After testing, the product It is crystal form A of asiatic acid tromethamine salt.

Embodiment 2

[0039] Put 1g of amorphous asiatic acid tromethamine salt in a stirred container, add 100ml of butanone at 20°C, start stirring for 72 hours, filter the suspension with suction, and dry the filter cake. After testing, the The product is asiatic acid tromethamine salt crystal form A.

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PUM

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Abstract

The invention discloses a crystal form A of asiatic acid tromethamine salt, which has main peaks at angles of diffraction 2theta being equal to 5.98, 6.87, 9.12, 10.38, 12.00, 12.47, 12.93, 13.42, 14.72, 15.10, 17.01 and 18.14 degrees, and which has minor peaks at 2theta being equal to 3.44, 13.87, 15.89, 19.04, 19.64, 20.17, 20.94, 21.75, 22.56, 23.33, 24.18, 26.38, 26.98 and 27.75 degrees. The invention also discloses a crystal form B of asiatic acid tromethamine salt, which has main peaks at angles of diffraction 2theta being equal to 3.54, 7.05, 10.04, 11.88, 13.38, 14.29 and 15.18 degrees; and which has minor peaks at 2theta being equal to 9.28, 9.59, 12.43, 16.68, 17.03, 17.57, 18.16, 18.91, 19.24, 20.07, 20.68, 22.46, 24.84, 25.20, 26.86, 27.73, 28.30, 28.85, 30.43, 30.83 and 33.93 degrees. Further, the invention discloses preparation methods of the crystal forms A and B. The crystal forms A and B of asiatic acid tromethamine salt are brand new crystal forms and have excellent stability. The methods provided by the invention have the advantages of simple operation and ease of implementation.

Description

technical field [0001] The invention relates to asiatic acid tromethamine salt crystal forms A and B, and a preparation method thereof. Background technique [0002] Asiatic acid (2α, 3β, 23-trihydroxyurea-12-ene-28-acid), also known as Asiatic acid, was first isolated from Centella asiatica by Bondmonds et al., and its pharmacological It has a wide range of effects, and is often used to treat burns or chronic ulcers, skin deformation caused by tuberculosis or leprosy, and has certain curative effects on cardiovascular diseases and liver poisoning. In addition, studies have shown that asiatic acid has anti-depressant, anti-fibrosis, anti-bacterial, anti-tumor and anti-oxidative effects. [0003] Although there are 4 hydrophilic groups (3 alcoholic hydroxyl groups and 1 carboxyl group) in the molecular structure of asiatic acid, its wettability is relatively poor and it is almost insoluble in water. Formulation, especially hydrophilic formulations, requires the use of uniqu...

Claims

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Application Information

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IPC IPC(8): C07J63/00C07C215/10C07C213/10
CPCC07B2200/13C07J63/00C07C215/10C07J63/008
Inventor 任国宾刘英陈金瑶黄晓玲齐明辉刘珉宇张瑱肖璘吴学军邓轶方陈仁海汤生荣刘全海
Owner 安徽林宇新创医药科技有限公司
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