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Oil-in-water type hydroquinone emulsion, and preparation method and application thereof

An oil-in-water, hydroquinone emulsion technology, applied in the field of medicine, can solve the problems of skin irritation, low transdermal absorption rate, poor stability, etc.

Pending Publication Date: 2020-12-08
广东人人康药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Hydroquinone preparations have defects such as skin irritation, poor stability and low transdermal absorption rate

Method used

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  • Oil-in-water type hydroquinone emulsion, and preparation method and application thereof
  • Oil-in-water type hydroquinone emulsion, and preparation method and application thereof
  • Oil-in-water type hydroquinone emulsion, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0098] Example 1 Preparation of hydroquinone present invention

[0099] Preparation hydroquinone, comprising the steps of:

[0100] 1) The MnO 2280g, 98% sulfuric acid 430g, 2.0L of water added to the reaction flask, at at 5-10 deg.] C, was slowly added dropwise aniline 100g, stirred, gradually warming to about 25 ℃, until the reaction was complete. The reaction mixture was steam distillation at 60-90 deg.] C, the collected condensate was introduced benzoquinone another reaction flask;

[0101] 2) Under light shielding, nitrogen blanket, collected in the condensate of p-benzoquinone added iron powder 42g, at 90-100 deg.] C, the reaction was stirred for 3-4 hours to complete the reaction, filtered and the filtrate was collected concentrated to hydroquinone in 35% concentrate;

[0102] 3) Add the concentrated solution of sodium metabisulphite 550mg, activated carbon 2.2g, 330 mg of zinc powder, and heated to 95 deg.] C, filtered hot, the filtrate was collected, cooled to 5 ℃, stirr...

Embodiment 2

[0103] Example 2 Preparation of hydroquinone present invention

[0104] Preparation hydroquinone, comprising the steps of:

[0105] 1) The MnO 2 350g, 98% 500g sulfuric acid, the reaction flask was added 2.0L of water, at 5 ℃ -8 ℃, aniline was slowly added dropwise 100g, stirred, gradually warming to about 25 ℃, until the reaction was complete. The reaction solution was distilled under steam conditions of 60-90 ℃, the collected reaction flask was introduced p-benzoquinone another condensate;

[0106] 2) Under light shielding, nitrogen blanket, collected in the condensate of p-benzoquinone added iron powder 60g, at 90-100 deg.] C, the reaction was stirred for 2-3 hours, until the reaction was complete, filtered, and the filtrate was concentrated under reduced pressure to collect to concentrate the hydroquinone content of 25%;

[0107] 3) Add the concentrated solution 750 mg of sodium metabisulfite, activated carbon 3.1g, iron 500mg, heated to 90 ℃, filtered, and the filtrate was c...

Embodiment 3

[0108] Example 3 Preparation of hydroquinone present invention

[0109] Preparation hydroquinone, comprising the steps of:

[0110] 1) The MnO 2 250g, 98% 370g sulfuric acid, the reaction flask was added 2.5L of water, at 6-10 deg.] C, was slowly added dropwise aniline 100g, stirred, gradually warming to about 25 ℃, until the reaction was complete. The reaction mixture was steam distillation at 70-95 deg.] C, the collected condensate was introduced benzoquinone another reaction flask;

[0111] 2) Under light shielding, nitrogen blanket, 31g of iron powder was added in the collected condensate of p-benzoquinone and stirred reaction at 90-100 deg.] C for 2-3 hours, until the reaction was complete, filtered, and the filtrate was concentrated under reduced pressure to collect concentrate hydroquinone content of 30%;

[0112] 3) Add the concentrated solution of sodium metabisulphite 550mg, 2.20 g of activated carbon, zinc 350mg, heated to 90 ℃, filtered, and the filtrate was cooled to...

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Abstract

The invention aims to provide an oil-in-water type hydroquinone emulsion. The emulsion comprises 10-40% (w / w) of an oil phase, 1-5% (w / w) of an oil-in-water type emulsifier, 50-80% (w / w) of a water phase and a pharmaceutically acceptable carrier. The hydroquinone emulsion in the invention has the advantages of high transdermal absorption rate, high bioavailability and the like.

Description

Technical field [0001] The present invention belongs to the field of medical technology, and more particularly to an oil-in-oil hydroquinone emulsion and a preparation method thereof and its application thereof. Background technique [0002] Hydroquinone (also known as terephiol) as tyrosinase inhibitors, inhibit tyrosine enzyme activity, regulates melanin cell metabolism by complexation, so that the number of positive melanocytes in the epidermis is significantly reduced, resulting in reverse Sexual skin fades. Oettel presented the role of hydroquinone with whitening skin in 1936. Since the 1960s, many countries used hydroquinone to use the whitening agents and dermatology of cosmetics for therapeutic preparations such as pigmentation, freckle. However, the amount of hydroquinone must be strictly controlled. [0003] Oxidative degradation reactions occur in the effect of hydroquinone instability, susceptible to light, temperature and other environmental factors. Hydroquinone is ...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/05A61K47/10A61K47/22A61K47/46A61K47/69A61P17/00A61K8/06A61K8/34A61K8/49A61K8/73A61K8/9789A61Q19/02
CPCA61K9/107A61K31/05A61K47/6951A61K47/10A61K47/46A61K47/22A61P17/00A61K8/347A61K8/34A61K8/4906A61K8/738A61K8/9789A61K8/062A61Q19/02
Inventor 苏冠荣尹贝立
Owner 广东人人康药业有限公司
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