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Aescin A and B liposome gel and preparation method thereof

A technology of liposome gel and aescin, which is applied in liposome delivery, liquid delivery, pharmaceutical formulations, etc., can solve the problems of poor transdermal absorption effect and large skin irritation, and achieve good transdermal absorption effect , reduce the incidence, good safety effect

Inactive Publication Date: 2017-09-15
WUHAN AIMIN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to provide a liposome gel with aescin A and B as active components and a preparation method thereof for the problems of poor transdermal absorption effect and large skin irritation of the existing sodium aescinate external preparations

Method used

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  • Aescin A and B liposome gel and preparation method thereof
  • Aescin A and B liposome gel and preparation method thereof
  • Aescin A and B liposome gel and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Raw material prescription:

[0022]

[0023] Preparation Process:

[0024] 1) Preparation of liposomes: Take 6.8g of aescin A, 4.3g of aescin B, 20g of soybean lecithin and 5g of cholesterol, add 50g of absolute ethanol, stir at 60°C to dissolve, pass the resulting ethanol solution through a peristaltic pump Inject into 250g of purified water at constant temperature to 60°C at a speed of 15ml / min, stir for 30min to make a liposome suspension; then place the liposome suspension in a liposome extruder, and pass through PC filter membranes with a pore size of 200nm and 100nm were extruded 4 times each to obtain 305g of the extruded liquid; finally, the method of membrane dialysis was used to dilute the extruded liquid by adding 200g of purified water, and then dialyzed 3 times to remove the extruded liquid. The ethanol in, get aescin A, B liposome 414g;

[0025] The encapsulation efficiency and particle size of the liposomes were detected according to the literature m...

Embodiment 2

[0030] Raw material prescription:

[0031]

[0032] Preparation Process:

[0033] 1) Preparation of liposomes: Take 14g of aescin A, 4g of aescin B, 25g of soybean lecithin and 10g of cholesterol, add 100g of dehydrated ethanol, stir at 60°C to dissolve, pass the obtained ethanol solution through a peristaltic pump in 25ml The speed of / min is injected into 300g purified water with constant temperature to 60°C, and stirred for 30min to make a liposome suspension; The 200nm and 100nm PC filter membranes were extruded 4 times each to obtain 370g of the extruded liquid; finally, the method of membrane dialysis was used to dilute the extruded liquid by adding 300g of purified water, and then dialyzed 3 times to remove the extruded liquid. Ethanol, get aescin A, B liposome 505g;

[0034] The encapsulation efficiency and particle size of the liposomes were detected according to the literature method, and the encapsulation efficiency was 83%, and the average particle size was 39...

Embodiment 3

[0039] Raw material prescription:

[0040]

[0041]

[0042] Preparation Process:

[0043] 1) Preparation of liposomes: Take 3.2g of aescin A, 5.2g of aescin B, 15g of soybean lecithin and 4g of cholesterol, add 30g of absolute ethanol, stir at 60°C to dissolve, pass the resulting ethanol solution through a peristaltic pump Inject into 180g of purified water at constant temperature to 60°C at a speed of 5ml / min, stir for 30min to make a liposome suspension; then place the liposome suspension in a liposome extruder, and pass through PC filter membranes with a pore size of 200nm and 100nm were extruded 4 times each to obtain 195g of extruded liquid; finally, membrane dialysis was used to dilute the extruded liquid by adding 150g of purified water, and then dialyzed 3 times to remove the extruded liquid. The ethanol in, get aescin A, B liposome 320g;

[0044] The encapsulation efficiency and particle size of the liposomes were detected according to the literature method, ...

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Abstract

The invention discloses aescin A and B liposome gel which comprises aescin A, aescin B, soybean phospholipids, cholesterol, Carbomer, triethanolamine, EDTA (ethylene diamine tetraacetic acid)-2Na, menthol and the like. The invention further discloses a preparation method which includes the steps of liposome preparation and liposome gel preparation. Compared with common gel, the liposome gel has better transdermal absorption effects, has sustained and controlled release functions and can be slowly released at a certain rate, constant plasma concentration is formed in skins, drug therapy time can be prolonged, and the occurrence rate of skin irritation reaction can be decreased.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to a liposome gel with aescin A and B as active components and a preparation method thereof. Background technique [0002] Aescin, also known as aescinic acid, is a general term for total saponins, β-aescin or isoaescin, etc. extracted from the seeds of Aesculus in the family Aescinaceae, belonging to triterpenoid saponins. The water solubility of aescin is poor. In order to increase its solubility, it is often made into sodium salt. Studies have shown that the components with higher content in sodium aescin are aescin A, B, C, and D. Sodium aescinate can reduce the increase of pathological capillary permeability, increase venous tension, reduce the exudation of inflammatory substances, have anti-inflammation, detumescence, pain relief, improve blood circulation, and promote the recovery of acute blunt soft tissue injury. [0003] Oral bioavailability of sodium aescinate is not ...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K9/127A61K31/704A61K47/32A61K47/18A61K47/10A61P29/00
CPCA61K9/0002A61K9/0014A61K9/06A61K9/127A61K31/704A61K47/10A61K47/18A61K47/183A61K47/32A61K2300/00
Inventor 石召华关小羽李群叶利春张晓存杜文杰
Owner WUHAN AIMIN PHARMA
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