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Compound quinhydrone liposome and preparation method thereof

A technology of hydroquinone lipids and plastids, applied in liposome delivery, active ingredients of hydroxyl compounds, skin diseases, etc., can solve the problems of poor patient compliance, reduce skin roughness, limit clinical application, etc., and meet clinical requirements Use requirements, reduce adverse reactions, and enhance the effect of curative effect

Inactive Publication Date: 2015-04-08
AFFILIATED YONGCHUAN HOSPITAL OF CHONGQING MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Hydroquinone is the first-choice drug for topical administration of facial skin pigmentation recommended by experts from the Dermatology Branch of the Chinese Medical Association. It is clinically used to treat chloasma, freckles and post-inflammatory hyperpigmentation spots. It is extremely unstable, easily oxidized and discolored, and becomes ineffective. It is a photosensitive substance, especially under light and alkaline conditions, which limits its clinical application.
[0003] Retinoic acid is the metabolic intermediate of vitamin A. By regulating the mitosis of epidermal cells and the renewal of epidermal cells, it can eliminate fine wrinkles, reduce skin roughness, and reduce pigmentation, but it is relatively irritating and patient compliance is not good , which limits its clinical application

Method used

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Examples

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Effect test

Embodiment 1

[0015] Solution A: Add 0.06g of hydroquinone, 10mg of retinoic acid, and 10mg of sodium bisulfate into 4ml of absolute ethanol and 2ml of chloroform to fully dissolve;

[0016] Solution B: Add 1.6g of phospholipids and 0.4g of cholesterol into 6ml of absolute ethanol and 1ml of chloroform and mix well;

[0017] Solution C: Mix solution A and solution B, reduce the pressure under vacuum at 40°C, remove the organic solvent, and obtain a uniform dry film. Add 50ml of preheated 0.2M phosphate buffer (pH5.7), wash the membrane with spin, sonicate for 30min, and pass through a 0.8μm filter membrane to obtain compound hydroquinone liposomes, which are stored at 4°C for use.

Embodiment 2

[0019] Solution A: Add 0.06g of hydroquinone, 10mg of retinoic acid, and 10mg of sodium bisulfate into 4ml of absolute ethanol and 2ml of chloroform to fully dissolve;

[0020] Solution B: Add 1.5g of phospholipids and 0.5g of cholesterol into 6ml of absolute ethanol and 1ml of chloroform and mix well;

[0021] Solution C: Mix solution A and solution B, reduce the pressure under vacuum at 40°C, remove the organic solvent, and obtain a uniform dry film. Add 50ml of preheated 0.2M phosphate buffer (pH5.7), wash the membrane with spin, sonicate for 30min, and pass through a 0.8μm filter membrane to obtain compound hydroquinone liposomes, which are stored at 4°C for use.

[0022] The liposome prepared by the invention is stable for 12 months in a refrigerator at 4° C., and has good effects in treating chloasma, freckles and post-inflammatory hyperpigmentation spots. 10 patients with chloasma participated in this study. Compound hydroquinone liposome and hydroquinone cream were ap...

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Abstract

The invention discloses compound quinhydrone liposome and a preparation method thereof. The compound quinhydrone liposome comprises drug active components such as retinoic acid and quinhydrone, and accessory materials. The compound quinhydrone liposome comprises, by weight, 1.0-6.0% of quinhydrone, 0.1-1.0% of retinoic acid, 70.0-85.0% of phosphatide, 15.0-25.0% of cholesterol and 0.1-1.0% of sodium bisulfate. The preparation method comprises the following steps of adding waterless ethanol and chloroform into quinhydrone, retinoic acid and sodium hydrogen sulfate for full dissolution, mixing the obtained solution and a waterless ethanol-chloroform solution of phosphatide and cholesterol to obtain a uniform mixed solution, carrying out vacuum pressure reduction, removing the organic solvent so that a uniform dry film is obtained, adding a preheated 0.2M phosphoric acid buffer into the uniform dry film, carrying out rotary evaporation washing on the film and carrying out ultrasonic treatment to obtain the compound quinhydrone liposome. The compound quinhydrone liposome has a stable structure, oxidation resistance and no irritation, has clear effects of treating chloasma, freckle and hyperpigmentation after inflammation, can promote skin targeting penetration, improves curative effects and has good effects.

Description

technical field [0001] The invention relates to the technical field of medicines, in particular to a compound hydroquinone liposome and a preparation method thereof. Background technique [0002] Hydroquinone is the first-choice drug for topical administration of facial skin pigmentation recommended by experts from the Dermatology Branch of the Chinese Medical Association. It is clinically used to treat chloasma, freckles and post-inflammatory hyperpigmentation spots. It is extremely unstable, easily oxidized and discolored, and becomes ineffective. It is a photosensitive substance, especially under light and alkaline conditions, which limits its clinical application. [0003] Retinoic acid is the metabolic intermediate of vitamin A. By regulating the mitosis of epidermal cells and the renewal of epidermal cells, it can eliminate fine wrinkles, reduce skin roughness, and reduce pigmentation, but it is relatively irritating and patient compliance is not good , limiting its c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/203A61K9/127A61P17/00A61K31/05
Inventor 刘娟金梅
Owner AFFILIATED YONGCHUAN HOSPITAL OF CHONGQING MEDICAL UNIV
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