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Amino butanetriol aescin and its prepn process

A technique for escin and tromethamine, which is applied to pharmaceutical formulations, medical preparations containing active ingredients, steroids, etc., can solve the hidden dangers of unsafe medicines, poor stability of arginine escin, and formulation molding. Problems such as difficulties in drug storage and transportation

Inactive Publication Date: 2007-06-06
陈文展
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, during use, it was found that the stability of arginine aescin was relatively poor, and the content of arginine was determined to decrease by about 10% after one month of accelerated test. The liquid chromatography analysis showed that there were more impurity peaks compared with the original sample. The analysis was because Arginine is easy to oxidize, resulting in poor stability of arginine aescin, which causes great difficulties for preparation molding, storage and transportation of medicines, and brings unsafe hidden dangers of medicines

Method used

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  • Amino butanetriol aescin and its prepn process
  • Amino butanetriol aescin and its prepn process

Examples

Experimental program
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Effect test

Embodiment 1

[0016] Embodiment 1: Preparation of tromethamine aescin

[0017] Get commercially available escin 113.1g (0.1mol), tromethamine 12.1g (0.1mol) and 1000ml distilled water, stir to react to a clear liquid, evaporate the solvent to dryness under reduced pressure, filter, and wash with absolute ethanol until no It was turbid and dried under reduced pressure at 80°C to obtain 100.2 g of off-white solid with a yield of 80.0%.

[0018] Aescin was used as the reference substance for content determination, and the product content was 99.6%.

Embodiment 2

[0019] Embodiment 2: Preparation of tromethamine aescin

[0020] Get commercially available aescin 11 3.1g (0.1mol), tromethamine 12.1g (0.1mol) and 1000ml distilled water, stir to react to a clear liquid, evaporate the solvent under reduced pressure, add 300ml acetone and no A mixed solvent of water and ethanol (1:1) was ground to obtain an off-white precipitate, which was filtered and dried under reduced pressure at 80° C. to obtain 92.2 g of off-white solid with a yield of 73.6%.

[0021] Aescin was used as the reference substance for content determination, and the product content was 99.3%.

Embodiment 3

[0022] Embodiment 3: Preparation of tromethamine aescin

[0023] Take commercially available escin 113.1g (0.1mol), tromethamine 12.1 (0.1mol) and 1000ml of distilled water, stir the reaction to a clear liquid, and freeze-dry to obtain 122.8g of off-white solid with a yield of 98.1%.

[0024] Aescin sodium was used as the reference substance for content determination, and the product content was 98.9%.

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Abstract

The present invention relates to amino butanetriol aescin and its isomer for relieving swelling, diminishing inflammation and improving blood circulation. The amino butanetriol aescin is prepared with amino butanetriol and aescin, and has the structural formula as shown. The amino butanetriol aescin has high water solubility, lowered possibility of resulting in vasospasm and raised administrating safety.

Description

Technical field: [0001] The invention belongs to the field of pharmacy, and relates to tromethamine aescin for reducing swelling, anti-inflammation and improving blood circulation, corresponding isomers and a preparation method. Background technique: [0002] Aescin (Sodium Aescinate) is a triterpene saponin extracted from the dried ripe fruit of the traditional Chinese medicine Su Luozi recorded in the first part of the Chinese Pharmacopoeia. Abroad, the crude drug Aesculus hippocastanum L. (English name horse chestnut) is extracted from the mature fruit of the crude drug Aesculus hippocastanum L., which is recorded in the German Pharmacopoeia. The German Dr. Madaus Pharmaceutical Factory conducted in-depth research on it and found that it has anti-inflammatory, anti-exudation , It has a significant effect on reducing swelling, can restore the normal permeability of capillaries, increase venous tension, and improve microcirculation. After long-term clinical observation of ...

Claims

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Application Information

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IPC IPC(8): C07J63/00A61K31/704A61K9/00A61P29/00
Inventor 陈文展
Owner 陈文展
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