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Lysine aescin saponin, its preparation and use

A technology of lysine and aescin, which is applied in the direction of pharmaceutical formulations, medical preparations containing active ingredients, pill delivery, etc., and can solve problems such as small compounds

Active Publication Date: 2007-01-17
WUHAN AIMIN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] At present, there is still a lack of a solution that can produce less toxic and less irritating compounds on the basis of ensuring the activity of aescin

Method used

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  • Lysine aescin saponin, its preparation and use
  • Lysine aescin saponin, its preparation and use
  • Lysine aescin saponin, its preparation and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] The preparation of embodiment 1β-escin and different-escin

[0024] 1. Cholesterol precipitation method

[0025] Sala seed powder, with 5 times the amount of dilute ethanol with a concentration of 50% to 70v / v%, stirred and extracted three times, each time for 4 hours, collected and combined extracts, vacuum recovered ethanol to a certain volume, and determined by high performance liquid chromatography Extract the content of β-escin in the concentrated solution, then add cholesterol with β-escin: cholesterol 1: 1.2 ratio under stirring, stir for 2 hours after adding, leave overnight, collect the cholesterol precipitate the next day, use Wash with water until colorless, collect by centrifuge and dry at 60°C. After the precipitate is dried, it is treated with chloroform or toluene to dissolve the cholesterol into the solvent, while the salts of aescin (sodium and potassium salts) still exist in solid form. After wiping off the residual solvent, dissolve it in water, pas...

Embodiment 2

[0039] The preparation of embodiment 2 lysine β-escin and lysine iso-escin

[0040] (1) Preparation of lysine β-escin

[0041] Grind β-escin crystals, take 56.55g (0.05mol) of fine powder, put 500ml of distilled water in a 1000ml three-necked bottle, slowly add L-lysine solution under stirring [50ml of distilled water contains 7.31g L-lysine (0.05mol)], after β-escin is completely dissolved, adjust the pH of the solution to 5.5-7.5 with the remaining lysine solution (total consumption of L-lysine 0.049mol), then add the solution without Water ethanol, so that the alcohol content reaches 80%, vacuum-concentrate to about 100ml below 50°C, add 500ml of anhydrous alcohol, then vacuum-concentrate to 200ml, and refrigerate to obtain lysine β-escin 57.95g, yield It is 90.7%, and its content is 99.5% as determined by liquid chromatography. Physical and chemical characteristics:

[0042] mp.217~219.5℃

[0043] 13 C-NMR (δ / ppm): 91.2 (C 3 ), 122.5 (C 12 ), 142.8 (C 13 ), 79.1 (C...

Embodiment 3

[0055] Lysine Aescin 10mg

[0056] Appropriate amount of water for injection

[0057] The total lysine aescin is dissolved in water for injection, and freeze-dried according to the conventional process of freeze-dried powder injection.

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PUM

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Abstract

A lysine escin, its compound, production and use are disclosed. The compound consists of beta-escin lysine salt, isoescin lysine salt or their mixture and / or the other accepted carriers. It has better anti-inflammatory and anti-exudative performances, better suppressant for brain edema and medicinal safety. It can also improve blood circulation increase venous tension.

Description

technical field [0001] The invention relates to an aescin lysine salt with low toxicity and low irritation, a preparation method and an application thereof. Background technique [0002] Sodium aescinate is the sodium salt of total saponins extracted from the seeds of Aescinaceae Aesculus. Total aescin (Totalescin) sodium is used clinically and contains 4 main components. According to the national standard of our country, it is named as aescin A (that is, escin I in Japan) according to the peak sequence of liquid chromatography. a ), aescin B (escin I b ), Aescin C (isoescin I a ) and aescin D (isoescin I a ). Aescin A and B are β-type aescins, their structure is basically the same, but with C 21 -Hydroxyl ester-forming organic acids are different, which are crotonoleic acid or angelic acid, which are anti-isomers of each other, so aescin A and B can be combined and represented by structural formula (1). Aescin C and D are the C of aescin A and B, respectively 21 Tran...

Claims

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Application Information

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IPC IPC(8): C07J63/00A61K31/704A61K9/08A61K9/10A61K9/12A61K9/14A61K9/16A61K9/20A61K9/48A61K9/70A61K9/00A61P7/10A61P17/02A61P1/00
Inventor 李信炯林范天张丽新马全发刘伟冯宇董元伟陈伯安程正达赵云霞施冬梅段术生陈平燕英
Owner WUHAN AIMIN PHARMA
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