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Novel passive target skin whitening efficacy nanoemulsion for night and daylight and method of preparing the same

A skin whitening and nanoemulsion technology, applied in skin care preparations, cosmetic preparations, pharmaceutical formulas, etc., can solve the problems of high irritation, difficult transdermal absorption, unreasonable formulations, etc., and achieves significant effects, physical and chemical A stable effect

Active Publication Date: 2009-04-08
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Although there are many kinds of skin whitening functional ingredients and skin whitening cosmetics, some of them do have certain skin whitening or whitening effects and effects, but they have many shortcomings and defects in practical application: ①The harm is great: such as using mercury-containing Whitening cosmetics made of similar compounds (mercuric chloride, aminomercuric chloride or mercuric iodide, etc.) are extremely harmful
②Large side effects: For example, the use of whitening cosmetics containing hydroquinone (hydroquinone) is more toxic, because hydroquinone, a traditional and effective whitening and freckle-removing ingredient, is not only extremely unstable in physical and chemical properties, but also easily oxidized and discolored in the air. And it has strong cytotoxicity, which can destroy melanocytes and cause permanent white spots on the skin.
Not only is kojic acid poor in stability, it is easy to oxidize and decompose and make the preparation darker, and because the pyran in its molecular structural formula is the same directional compound as benzene, it has the same carcinogenicity as benzene in theory; not only that , the hydroxyl group and hydrogen peroxide in the structure of kojic acid can also induce or accumulate a large number of free radicals, and its peroxidation reaction and its products have certain mutagenic and carcinogenic possibilities
③High irritation: If you use whitening cosmetics containing retinoic acid and fruit acid, it will be very irritating
Because vitamin A acid (Tretinoin) is also called tretinoin or retinoic acid and fruit acid is also called α-hydroxy acid. If the concentration is too large and the use period is too long, it is easy to cause irritation to skin tissue, acid allergy, phototoxicity. , contact dermatitis, and even cause gene mutations, etc.
Moreover, if the application concentration of retinoic acid and fruit acid is not well grasped and the application method is improper, direct skin burns (such as skin congestion, edema, flushing, burning pain, running water, scaling, etc.) and indirect skin burns (mainly Refers to the stimulation of sunlight on the skin in the treatment area, increasing the skin's absorption of ultraviolet rays and the skin's defense against ultraviolet rays)
④ Poor stability: whether it is hydroquinone, kojic acid, vitamin C or phenolic compounds, etc., due to their unstable physical and chemical properties, especially resistance to external environmental factors such as light, oxygen, pH, and temperature Poor resistance, so that the content and function of the functional components are significantly reduced
Moreover, because of its unstable physical and chemical properties, it is easy to oxidize or autoxidize the functional components to make the product color continue to deepen, which seriously affects the appearance and internal quality of the product.
⑤ Poor transdermal absorption: Most of the commonly used skin whitening ingredients and skin whitening active substances are water-soluble, even if some are alcohol-soluble or oil-soluble, but due to the tight barrier structure of the skin epidermis and the inherent whitening ingredients The physical and chemical properties of the skin determine that its transdermal absorption effect and effect are general or difficult to transdermal absorption, so its skin whitening effect is naturally limited; ⑥ unreasonable formula: some skin whitening preparations or products currently have unreasonable or even unreasonable formulas phenomenon, such as the use of arbutin and vitamin C, but did not take into account the impact of PH value
Usually, the optimal pH value of arbutin is above 6.0, and the addition of vitamin C reduces the overall pH value to below 6.0, thus affecting the exertion of the two functional ingredients. In addition, the added functional ingredients are less synergistic , affecting the advantages of its functional ingredients
⑦The effect is not obvious: Many whitening ingredients currently used, whether they are chemically synthesized or semi-synthesized or modified, or extracted from natural plants or separated from animal organs, although in vitro tests have certain effects, but in actual use Sometimes its skin whitening or whitening effect is very general, especially some extracts from natural plants or herbs, although the side effects are small, but its effect is limited, and some even have little effect
⑧Prohibited by national cosmetics regulations: such as aminomercuric chloride, hydroquinone (hydroquinone), hydrogen peroxide (hydrogen peroxide) and other raw materials are prohibited in beauty cosmetics; The dosage has very strict restrictions; ⑨The dosage form is backward: at present, skin whitening cosmetics still adopt the dosage forms such as ointment, cream, emulsion, gel, and essence produced by traditional technology, which have general stability and are difficult to absorb through the skin. Insufficient dose, poor efficacy
The concentration or dosage of whitening functional ingredients per unit volume in skin whitening preparations is also very important. Whitening functional ingredients can only work when they have sufficient concentration or dosage, and it is difficult for the preparation technology of traditional dosage forms to achieve a certain curative effect. (Effective ingredient dosage and solubility)

Method used

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  • Novel passive target skin whitening efficacy nanoemulsion for night and daylight and method of preparing the same
  • Novel passive target skin whitening efficacy nanoemulsion for night and daylight and method of preparing the same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Embodiment one: skin whitening efficacy nanoemulsion for night use (taking the preparation of 100g as an example)

[0058] 1. Accurately weigh 0.688g of sodium hydroxide and 0.543g of citric acid with an analytical balance, place them in a decontaminated 100mL Erlenmeyer flask, add 33.15g of triple distilled water to fully dissolve, weigh and add 3.297g g L-ascorbic acid 2-glucoside, after completely dissolved, then add 3.080g β-raspberry ketone glucoside, 3.080g nicotinamide, 3.080g α-arbutin, 3.080g β-arbutin and 2.0mg cysteine Acid (*β-raspberry ketone glucoside, nicotinamide, α-arbutin, β-arbutin and cysteine ​​need to be dissolved in sequence and then added separately, not at the same time); the dissolution of the above substances can be placed Perform ultrasonic vibration in a CQ-10 ultrasonic oscillator to accelerate dissolution; after complete dissolution, measure the pH of the solution to be 6.2±0.2, if there is any deviation, adjust the pH to within this range...

Embodiment 2

[0066] Embodiment two: daily skin whitening efficacy nanoemulsion (taking the preparation of 100g as an example)

[0067] 1. Accurately weigh disodium ethylenediaminetetraacetic acid (EDTA-Na 2 ) 0.169g was placed in a decontaminated 100mL Erlenmeyer flask, then 31.78g of triple distilled water was added to fully dissolve, and then 0.676g of citric acid and 0.439g of NaOH were added in turn to fully dissolve, and then weighed and added 3.02g of N- Acetyl glucosamine, 2.7g L-ascorbic acid 2-glucoside, after completely dissolved, then add 3.074g β-raspberry ketone glucoside, 3.074g vitamin PP factor, the dissolution of the above substances can be placed in a CQ-10 ultrasonic oscillator Perform ultrasonic vibration to accelerate dissolution; then slowly add 5.068 g of glabridin application solution, after complete dissolution, measure the pH value of the solution to 4.7±0.2, if there is any deviation, adjust the pH to within this range. Clearly mark 50 g of the aqueous phase (I) w...

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Abstract

The invention relates to a novel passive targeting nano emulsion with skin whitening effect and a preparation method thereof. The invention uses a novel passive targeting transdermal delivery dosing system TDDS-nano emulsion as a carrier of a function component for whitening or lighting the skin, uses different physical and chemical properties, action mechanism and actual effect of each skin whitening function component, especially the action advantages of certain novel skin whitening function components, and provides skin whitening effect nano emulsion systems with two joint applications in morning and evening matched with each other. The two joint applied nano emulsion systems not only have minimum spherical grains, extremely even distribution of nano-scale grains, remarkable passive targeting function, good transdermal absorption and strong penetrability, but also have extremely even, exquisite, smooth and glossy texture of the nano emulsion, is quite comfortable after coating on the face or the skin, has no stimulus and good stability; and the nano is light yellow, beautiful in appearance, bright and transparent, clear and crystalline, has light opalescence, and is adhesive but not sticky, thick but not heavy, oily but not greasy.

Description

technical field [0001] The present invention relates to medical cosmetic health care products and new cosmetic preparation technology, in particular to a new type of passive targeted night-use and anti-inflammatory drug which can be successfully applied to skin whitening and skin pigmentation suppression and lighten or lighten skin pigmentation in human medical cosmetology. Nanoemulsion with skin whitening effect for daily use and preparation method thereof. Background technique [0002] (1) Background technology about skin whitening functional components: according to different action principles, current skin whitening agents can be divided into: tyrosinase activity inhibitors, melanocyte toxicity agents, melanin metabolism agents (melanin transport inhibitors) blocking agents), sunscreens (sunscreens), reducing agents, chemical exfoliants, endothelin antagonists, etc. Among them, tyrosinase activity inhibitors mainly include: mercury-containing compounds (such as mercurou...

Claims

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Application Information

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IPC IPC(8): A61K8/85A61K8/60A61K8/49A61K8/46A61K8/06A61Q19/02
Inventor 杨永鹏朱晓亮董萍丁宇丁克祥
Owner 董萍
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