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4-(1-phenethyl)-1,3-dihydroxy benzene liposome and preparation method thereof

A technology of hydroxyphenyl ester and dihydroxybenzene, which is applied in the field of 4--1 to achieve the effect of improving stability and prolonging the action time

Active Publication Date: 2011-06-22
苏州工业园区黎姿化妆品有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, since 4-(1-phenylethyl)-1,3-dihydroxybenzene is a phenolic compound, its water solubility and fat solubility are poor, the skin penetration rate is low, and it is easily oxidized, which has certain irritation , so the application of 4-(1-phenylethyl)-1,3-dihydroxybenzene in transdermal preparations and cosmetics is limited
[0003] Liposomes are hydrophilic vesicles composed of phospholipid bilayers, which can improve the stability of encapsulated drugs, promote drug transdermal absorption, and prolong drug absorption. However, there are no reports of making 4-(1-phenylethyl)-1,3-dihydroxybenzene into liposome dosage form so far.

Method used

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  • 4-(1-phenethyl)-1,3-dihydroxy benzene liposome and preparation method thereof
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  • 4-(1-phenethyl)-1,3-dihydroxy benzene liposome and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0025] Example 1: Preparation of 4-(1-phenylethyl)-1,3-dihydroxyphenyl liposomes

[0026] Get 4-(1-phenylethyl)-1,3-dihydroxybenzene 1g, soybean lecithin 3.8g, cholesterol 1.2g, put in the round bottom flask of 1000ml, add 50ml chloroform and methanol mixed solution (chloroform:methanol =1:1), dissolved at 55°C, placed in a constant temperature water bath at 55°C for rotary film evaporation to form a lipid film; then add 994ml of distilled water preheated to 55°C, hydrate, shake, and obtain colostrum; colostrum Perform secondary emulsification with a high-pressure homogenizer to obtain 1000 g of 4-(1-phenylethyl)-1,3-dihydroxyphenyl liposome.

Embodiment 2

[0027] Embodiment 2: Preparation of 4-(1-phenylethyl)-1,3-dihydroxyphenyl liposome

[0028] Take 80g of 4-(1-phenylethyl)-1,3-dihydroxybenzene, 20g of soybean lecithin, and dissolve it with 100ml of ethanol under heating in a water bath at 75°C to obtain a lipid solution; take 700g of glycerin and 100ml of distilled water, Mix well, and heat in a water bath to 75°C to obtain an aqueous phase. Inject the lipid solution into the water phase at 75°C and shake evenly to obtain colostrum. Place the colostrum in a high-pressure homogenizer for secondary emulsification to obtain 1000 g of 4-(1-phenylethyl)-1,3-dihydroxyphenyl liposome.

Embodiment 3

[0029] Example 3: Preparation of 4-(1-phenylethyl)-1,3-dihydroxyphenyl liposomes

[0030] Take 100g of 4-(1-phenylethyl)-1,3-dihydroxybenzene, 50g of egg yolk lecithin, 50g of cholesterol, and 20g of ceramide in a spinner bottle, add 200ml of dichloromethane, and dissolve it under heating at 50°C , placed in a constant temperature water bath at 50°C to rotate the film to evaporate to form a lipid film; then add 780ml of distilled water preheated to 65°C, hydrate, shake, and obtain colostrum; use ultrasonic emulsification to perform secondary emulsification on the colostrum. 1000 g of 4-(1-phenylethyl)-1,3-dihydroxyphenyl liposome was obtained.

[0031] Example 4: Preparation of 4-(1-phenylethyl)-1,3-dihydroxyphenyl liposomes

[0032] Take 30g of 4-(1-phenylethyl)-1,3-dihydroxybenzene, 30g of distearoylphosphatidylcholine, 50g of dipalmitoylphosphatidylcholine, and 10g of cholesterol, and heat it in a water bath at 70°C with 200ml of ethanol Dissolve it under pressure to obta...

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Abstract

The invention relates to the technical field of medicine and cosmetics, in particular to lipidosome preparation formulation of 4-(1- phenethyl)-1 and 3-dihydroxy benzene and a preparation method thereof. The invention prepares the 4-(1- phenethyl)-1, 3-dihydroxy benzene into lipidosome, overcomes the defects of the insufficient application of existing 4-(1- phenethyl)-1 and 3-dihydroxy benzene inpercutaneous administration preparation and cosmetics, improves the stability and percutaneous performance of the 4-(1- phenethyl)-1and 3-dihydroxy benzene and reduces the acrimony of the 4-(1- phenethyl)-1 and 3-dihydroxy benzene for the skin, thus better exerting the healing effect.

Description

technical field [0001] The invention relates to the technical field of medicine and cosmetics, and relates to a liposome dosage form of 4-(1-phenylethyl)-1,3-dihydroxybenzene and a preparation method thereof. Background technique [0002] 4-(1-phenylethyl)-1,3-dihydroxybenzene is a tyrosinase inhibitor, which has the effect of brightening skin and hair and anti-age spots. At present, 4-(1-phenylethyl) )-1,3-Dihydroxybenzene is used as a tyrosinase inhibitor for cosmetics or anti-freckle drugs ("Use of Diphenylmethane Derivatives as Tyrosinase Inhibitors", Patent Application No. 200480014939.8). However, since 4-(1-phenylethyl)-1,3-dihydroxybenzene is a phenolic compound, its water solubility and fat solubility are poor, the skin penetration rate is low, and it is easily oxidized, which has certain irritation , Therefore, the application of 4-(1-phenylethyl)-1,3-dihydroxybenzene in the field of transdermal preparations and cosmetics is limited. [0003] Liposomes are hydro...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/05A61K8/33A61K47/24A61Q19/00A61P17/00
Inventor 李成亮柳郁高保安
Owner 苏州工业园区黎姿化妆品有限公司
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