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Asiaticoside liposome and its use

A technology of asiaticoside and glucoside, which is applied in the field of asiaticoside liposome and its preparation of pharmaceutical preparations and cosmetics, can solve the limitations of asiaticoside development and application, asiaticoside fat solubility and Problems such as poor water solubility and large molecular weight can achieve the effect of avoiding systemic adverse reactions, improving skin penetration, and promoting skin penetration

Inactive Publication Date: 2003-07-23
SHANGHAI JAHWA UNITED
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Madecassoside is a triterpene saponin. In practical application, it is found that asiaticoside has a large molecular weight (about 936), and its fat-soluble and water-soluble characteristics make it difficult to penetrate the skin; The characteristics of madecassoside's own structure make it unstable in air or solution, easy to oxidize and degrade, and affect the preparation of stable pharmaceutical preparations and cosmetic formulations; in addition, due to the poor fat solubility and water solubility of asiaticoside characteristics, which affect its mixing with other ingredients in pharmaceutical preparations or cosmetics, and bring difficulties to the preparation process
These unfavorable factors limit the further development and application of asiaticoside in the field of transdermal drug delivery preparations and cosmetics

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Take madecassoside 30g, soybean lecithin 20g, cholesterol 30g, poloxamer F 68 40g, ceramide 10g, chloroform 200mL, ethanol 100mL, pH 7.4 phosphate buffer to 1000mL.

[0017] The above-mentioned asiaticoside, soybean lecithin, poloxamer F 68 , cholesterol, and ceramide were added to a 10,000mL round-bottomed flask, and the above-mentioned lipid components were dissolved with a mixed solution of chloroform and ethanol, and placed in a constant temperature water bath at 25-40°C for rotary film evaporation, so that the lipid formed a thin film at the bottom of the round-bottomed flask ,spare. Pour 800mL of pH7.4 phosphate buffer solution into the above-mentioned flask, hydrate, shake, add the mixed liquid to 1000mL with pH7.4 phosphate buffer solution, and perform ultrasonic treatment (output 4, duty cycle 50%, time 20mins) to obtain the product Madecassoside liposomes.

Embodiment 2

[0019] Take 50g of asiaticoside, 50g of egg yolk lecithin, 50g of cholesterol, 20g of ceramide, and add pH7.4 phosphate buffer to 1000mL.

[0020] Put the above-mentioned asiaticoside, egg yolk lecithin, cholesterol and ceramide in a Erlenmeyer flask, heat to melt or add the organic solvent to heat and dissolve, prepare a lipid solution, and put it in a constant temperature water bath at 80°C for later use. Put 800mL of pH7.4 phosphate buffer in a water bath, heat to the same temperature as the lipid solution, shake and mix the aqueous solution and lipid solution, cool, add the mixed liquid to 1000mL with pH7.4 phosphate buffer, and homogenize under high pressure Treatment (high pressure 60MPa, low pressure 10MPa), homogenization 6 times to obtain asiaticoside liposomes.

Embodiment 3

[0022] Take 20g of asiaticoside, 20g of dipalmitoylphosphatidylcholine, 30g of polyoxyethylene cetyl ether, 40g of cholesterol, 40g of ceramide, 200mL of dichloromethane, 200mL of ethanol, and add pH7.4 phosphate buffer to 1000mL.

[0023] Add the above-mentioned asiaticoside, dipalmitoylphosphatidylcholine, polyoxyethylene cetyl ether, ceramide, and cholesterol into a 10000mL round-bottomed flask, and dissolve the above-mentioned lipids with a mixed solution of dichloromethane and ethanol. Heat the ingredients to dissolve, place in a constant temperature water bath at 25-40°C for rotary thin-film evaporation, and make the lipid form a thin film at the bottom of the round-bottomed flask for later use. Pour 800 mL of pH 7.4 phosphate buffer into the above-mentioned flask, hydrate, shake, and add the mixed liquid to 1000 mL with pH 7.4 phosphate buffer. Squeeze and filter the above mixed lipid aqueous solution through a polycarbonate fiber membrane to obtain asiaticoside liposo...

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PUM

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Abstract

An asiaticoside lipoid is prepared from asiaticoside and lipoid component through thermal fusing or dissolving in organic solvent, rotating film evaporation, hydrating in aqueous solution, oscillating, emulsifying, and filter. It can be used for preparing percutaneous medicines and medicines due to its high percutaneous nature, stability and hydrophilicity.

Description

technical field [0001] The invention belongs to the field of chemistry, relates to the field of pharmaceutical preparations and cosmetics, in particular to asiaticoside liposome and its application in the preparation of pharmaceutical preparations and cosmetics. Background technique [0002] Centella asiatica (L.) Urban.] is a plant of the genus Centella asiatica of the Umbelliferae family. The whole herb is used as medicine, and has the effects of clearing heat and dampness, detoxifying and reducing swelling. In the application of traditional Chinese medicine in my country for two thousand years, centella asiatica extract is mainly used to treat diseases such as damp-heat jaundice, carbuncle sores, bruises and persistent skin ulcers. Existing data show that the triterpenoid saponins extracted from Centella asiatica can significantly promote wound healing, stimulate granulation growth, promote epidermal keratinization, and contribute to the generation of new connective tissu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K8/14A61K8/63A61K9/127A61K31/704A61P17/00A61Q19/00
CPCA61Q19/00A61K8/14A61K8/63A61K31/704A61K9/127A61P17/00A61P17/02
Inventor 陈建明吕洛高申林惠芬魏少敏张仰眉李慧良钟延强史青郭奕光管斐王巍马来记顾娟
Owner SHANGHAI JAHWA UNITED
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