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Aescin medicine composition and its prepn process and use

The technology of aescin and its composition is applied in the pharmaceutical composition of aescin and its preparation field, which can solve the problems of complex preparation process, etc., and achieve the effects of simple production process, improved curative effect, and excellent synergistic effect

Active Publication Date: 2007-03-21
WUHAN AIMIN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] In May 2005, our factory submitted a patent application for lysine aescin to the State Intellectual Property Office (the application number is 2005101055854), which disclosed that lysine aescin compared with sodium aescin, has Better anti-inflammatory, anti-exudation and blood circulation improvement activities, and can effectively reduce the irritation of aescin on blood vessels and muscles, improve the safety and therapeutic index of the drug, but its preparation process is relatively complicated

Method used

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  • Aescin medicine composition and its prepn process and use
  • Aescin medicine composition and its prepn process and use
  • Aescin medicine composition and its prepn process and use

Examples

Experimental program
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Effect test

Embodiment 1

[0054] Example 1 Preparation of Aescin Potassium Sodium Mixed Salt by Cholesterol Precipitation

[0055] Use 5 times of the amount of 5 times the amount of ethanol solution with a concentration of 50v / v%-70v / v% to stir and extract for 4 hours each time, collect and combine the extracts, recover ethanol in a vacuum to 1 / 5 of the volume of the extract, and use Determine the content of β-escin in the extract concentrate by high-performance liquid chromatography, then add cholesterol under stirring conditions with the mass ratio of β-escin and cholesterol as 1:1.2, stir for 2 hours after the addition, and place Overnight, collect the cholesterol precipitate by centrifugation the next day, wash it with water until it is colorless, dry it at 60°C, and treat it with chloroform or toluene to dissolve the cholesterol into the solvent, while the salt of aescin (sodium, potassium salt) still exists in solid form , recrystallized twice with 90%-95% ethanol to obtain white aescin salt (sod...

Embodiment 2

[0056] Example 2 Preparation of β-escin and isoescin

[0057] 1. Cholesterol precipitation method

[0058] Sala seed fine powder, use 5 times the amount of dilute ethanol with a concentration of 50v / v% to 70v / v% to stir and extract three times, each time for 4 hours, collect and combine the extracts, recover ethanol in a vacuum to 1 / 5 of the volume of the extract, Measure the content of β-escin in the extract concentrate by high-performance liquid chromatography, then add the cholesterol under the stirring condition with the mass ratio of β-escin and cholesterol as 1: 1.2, and stir for 2 hours after adding. Leave it overnight, and collect the cholesterol precipitate by centrifugation the next day, wash it with water until it is colorless, dry it at 60°C, and treat the precipitate with chloroform or toluene after drying to dissolve the cholesterol in the solvent, and the salt of aescin (sodium, potassium salt) still exists in solid form. After wiping away the residual solvent...

Embodiment 3

[0072] Example 3 Preparation of high-purity sodium aescinate

[0073] 1. Aescin salt (potassium, sodium salt) with a purity of 98.5% is dissolved in distilled water to obtain an aqueous solution with a concentration of about 2%. The aqueous solution passes through a hydrogen-type cation exchange column, and the weight ratio of aescin salt to resin is about 0.8-1.2: 1.2-0.8, to obtain a solution with a pH of about 2.0-2.8, which can be placed in a cold place or refrigerated to precipitate crystals. Redissolve the crystals in 95v / v% ethanol, add an equivalent amount of sodium hydroxide ethanol solution, place in a cold place or refrigerated to precipitate crystals, and obtain sodium aescinate crystals with a purity of 99.0%.

[0074] 2. Dissolve aescin salt (potassium, sodium salt) with a purity of 97.5% in distilled water to obtain an aqueous solution with a concentration of about 2%, add 2 mol of sulfuric acid or hydrochloric acid, adjust the pH of the solution to 1-3, and pla...

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Abstract

The present invention relates to aescin medicine composition and its preparation process and use. The aescin product of purity over 90 % may be compounded with medicine carrier to form composition with obvious synergistic effect, reduced stimulation of aescin on blood vessels and muscles, and obviously raised effects of diminishing inflammation, antagonizing effusion, improving blood circulation, etc. The composition features its less stimulation, high safety, high treating index, etc.

Description

technical field [0001] The invention belongs to the field of medicaments, and in particular relates to a escin pharmaceutical composition, a preparation method and an application thereof. Background technique [0002] Aescin, also known as aescinic acid, is a general term for total saponins, β-aescin or isoescin, which are extracted from the seeds of Aesculus in the family Aesculus. At present, total aescin sodium (Totalescin) sodium is mostly used clinically, mainly containing 4 main components. According to the national standard of my 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 ...

Claims

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Application Information

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IPC IPC(8): A61K31/704A61K9/00A61K9/08C07J53/00C07J63/00A61P29/00A61P3/12A61P7/10A61P9/10A61P9/14A61P17/02
Inventor 李信炯林范天张丽新马全发冯宇陈伯安程正达赵云霞
Owner WUHAN AIMIN PHARMA
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