CN116407462A - Whitening and freckle-removing composition and essence, cream and emulsion containing composition - Google Patents

Whitening and freckle-removing composition and essence, cream and emulsion containing composition Download PDF

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CN116407462A
CN116407462A CN202310078898.3A CN202310078898A CN116407462A CN 116407462 A CN116407462 A CN 116407462A CN 202310078898 A CN202310078898 A CN 202310078898A CN 116407462 A CN116407462 A CN 116407462A
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percent
whitening
phase
stirring
spot
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范开
李雪梅
杨黎
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Chongqing Fagen Biomedical Inc
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/67Vitamins
    • A61K8/676Ascorbic acid, i.e. vitamin C
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/40Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/44Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/60Sugars; Derivatives thereof
    • A61K8/602Glycosides, e.g. rutin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/67Vitamins
    • A61K8/673Vitamin B group
    • A61K8/675Vitamin B3 or vitamin B3 active, e.g. nicotinamide, nicotinic acid, nicotinyl aldehyde
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/02Preparations for care of the skin for chemically bleaching or whitening the skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/20Chemical, physico-chemical or functional or structural properties of the composition as a whole
    • A61K2800/30Characterized by the absence of a particular group of ingredients
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/59Mixtures
    • A61K2800/592Mixtures of compounds complementing their respective functions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/74Biological properties of particular ingredients
    • A61K2800/78Enzyme modulators, e.g. Enzyme agonists
    • A61K2800/782Enzyme inhibitors; Enzyme antagonists
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Animal Behavior & Ethology (AREA)
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  • Birds (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Cosmetics (AREA)

Abstract

The invention provides a whitening and freckle-removing composition and essence, face cream and emulsion containing the same. The whitening and spot-removing composition at least comprises the following components in percentage by weight: 4% -10% of nicotinamide; 3-5% of ascorbyl glucoside; 1% -3% of tranexamic acid; 1 to 2 percent of alpha-arbutin. The invention has synergistic whitening and freckle-removing effects, wherein nicotinamide inhibits the transfer of melanosomes to keratinocytes by inhibiting the generation of melanin particles; the tranexamic acid inhibits PAR-2 receptor activation in keratinocytes and plays roles in relieving pigmentation and whitening; alpha-arbutin can reduce melanin generation and pigmentation by inhibiting tyrosinase activity in vivo; the ascorbyl glucoside has reducing effect on existing melanin, and has effect of removing color spots. The invention combines a plurality of mechanisms, thereby realizing the effects of fading color spots, relieving pigmentation and improving skin brightness.

Description

Whitening and freckle-removing composition and essence, cream and emulsion containing composition
Technical Field
The invention relates to the technical field of cosmetics, in particular to a whitening and freckle-removing composition, and essence, face cream and emulsion containing the composition.
Background
With the pursuit of beauty, more and more people expect to have fair skin color, and whitening and freckle removing cosmetics are expected to have more active pharmacological effects. Pigmentation and various color spots are generated due to complex reasons, and generally, the generation of melanin in skin is accelerated due to factors such as ultraviolet irradiation, genetic factors, endocrine dyscrasia, environmental pollution, active oxygen and the like, so that the skin aging is accelerated, the skin is loose, the color spots are deposited, the skin color is dark yellow and has no luster, various fine lines and wrinkles are generated, and therefore, the main way of whitening and removing the color spots of the skin is to inhibit the generation of melanin.
Various active ingredients for whitening and removing freckles are added into cosmetics on the market, but the cosmetics have certain disadvantages. Firstly, the concentration of the single raw materials is too high or the ratio of the compound raw materials is improper, the efficacy is not clear, the generation of melanin can not be well inhibited, and skin irritation and allergy can be caused; secondly, a large amount of natural mixed extracts of plants or microorganisms and the like are adopted in cosmetics, and the cosmetics contain a large amount of inactive unknown ingredients although the natural extracts contain whitening and spot-lightening ingredients, the ingredients are complex, the natural ingredients cannot be controlled to be completely consistent in batches, the use experience is affected, and the effect and safety are uncontrollable due to the differences of extraction processes and production places of different manufacturers; thirdly, hydroquinone and its derivatives or corticoids are added, and although hydroquinone can cause melanocyte degeneration and apoptosis under a certain concentration, hydroquinone can not be used for a long time, and is not suitable for being made into cosmetics for daily use.
Patent CN202111186818.3 application discloses a whitening and anti-aging composition, a cosmetic and a preparation method thereof, wherein the whitening components in the composition are as follows: arbutin, ascorbyl glucoside, glutathione, nicotinamide and tranexamic acid; the anti-aging components are: dipeptide diamino Ding Xianbian-yl amide diacetate, acetyl tetrapeptide-2 and oligopeptide-4 as anti-aging agents. Although various whitening components are added, the proportion range of the five whitening components of arbutin, ascorbyl glucoside, glutathione, nicotinamide and tranexamic acid is too wide, the content is too low, the whitening effect cannot be displayed, and the addition purpose and the basis of combination are not described. In the examples, no effective formulation and related description were found, and the results of the comparative examples were found in the evaluation, and the data were not convincing.
Disclosure of Invention
Aiming at the defects existing in the prior art, the invention provides a whitening and freckle-removing composition, essence, cream and emulsion containing the composition, the composition has definite formula efficacy, and melanin generation and transportation distribution are inhibited through multiple ways.
In order to solve the technical problems, the invention provides the following technical scheme:
In a first aspect, a whitening and spot-fading composition is provided, wherein the preparation raw materials of the composition at least comprise the following components in percentage by weight:
Figure SMS_1
in a second aspect, a whitening and freckle-removing essence comprises the whitening and freckle-removing composition according to the first aspect.
Further, the essence for whitening and lightening spots comprises the following components in percentage by weight:
phase A: 65.93 to 89.4649 percent of pure water, 0.15 to 4 percent of glycerol, 0.1 to 2 percent of butanediol, 0.05 to 1 percent of sodium hyaluronate, 0.03 to 0.35 percent of sodium citrate and 0.0001 to 0.02 percent of citric acid;
and B phase: 0.8 to 4 percent of 1, 2-pentanediol and 0.15 to 0.7 percent of p-hydroxyacetophenone;
and C phase: 1 to 3 percent of tranexamic acid, 4 to 10 percent of nicotinamide, 3 to 5 percent of ascorbyl glucoside, 1 to 2 percent of alpha-arbutin, 0.25 to 1.5 percent of beta-glucan and 0.005 to 0.5 percent of sodium hydroxide.
Further, the preparation method of the whitening and freckle-removing essence comprises the following steps:
taking the phase A raw materials according to a proportion, sequentially adding pure water, glycerol, butanediol, sodium hyaluronate, sodium citrate and citric acid into a main pot, starting stirring, setting the rotating speed to be 20-25Hz, uniformly stirring, heating to 83-87 ℃ at the same time, and preserving heat for 20-30 minutes to obtain a phase A mixture;
Mixing the B-phase raw materials in other containers according to a proportion to obtain a B-phase mixture, adding the B-phase mixture into the A-phase mixture in the main pot after the temperature of the main pot is reduced to 63-67 ℃, setting the rotating speed to 20-25Hz, and uniformly stirring;
and (3) dissolving sodium hydroxide in the C phase by pure water according to a proportion, cooling the temperature of the main pot to 38-42 ℃, adding the C phase raw materials into the main pot according to the sequence of tranexamic acid, nicotinamide, ascorbyl glucoside, alpha-arbutin, beta-glucan and sodium hydroxide, and uniformly stirring to obtain the product.
In a third aspect, a whitening and spot-reducing cream comprises the whitening and spot-reducing composition of the first aspect.
Further, the whitening and freckle-removing face cream comprises the following components in percentage by weight:
phase A: 73.8495 to 24.585 percent of pure water, 3 to 5 percent of glycerol, 2.5 to 4.3 percent of 1, 2-pentanediol, 0.5 to 9 percent of hydroxypropyl tetrahydropyran triol, 0.1 to 1.8 percent of p-hydroxyacetophenone, 0.05 to 0.65 percent of hydrolyzed sodium hyaluronate and 0.1 to 0.35 percent of carbomer;
and B phase: 2% -5% of butter fruit, 3% -7% of glycerol tri (ethylhexanoate), 3% -5.8% of cetostearyl alcohol, 1.8% -5% of polydimethylsiloxane, 1% -3% of diisostearyl malate, 0.8% -3% of isostearyl isostearate, 2.3% -4.5% of MONTANOV-68 (emulsifying agent), 0.45% -1% of emulghos (phosphate emulsifying agent) and 0.1% -1% of vitamin E;
And C phase: 0.05 to 0.2 percent of carnosine, 0.0005 to 0.005 percent of palmitoyl pentapeptide-4, 0.1 to 0.36 percent of arginine, 1 to 3 percent of tranexamic acid, 2 to 5 percent of nicotinamide, 1 to 3 percent of ascorbyl glucoside, 0.5 to 2 percent of alpha-arbutin, 0.5 to 1.6 percent of kojic acid, 0.2 to 3 percent of saccharomyces cerevisiae extract and 0.1 to 0.85 percent of ceramide.
Further, the preparation method of the whitening and freckle-removing facial cream comprises the following steps:
proportionally adding the phase A raw materials into a main pot, starting stirring, setting the rotating speed to be 20-25Hz, uniformly stirring, heating to 85-90 ℃ at the same time, and preserving heat for 20-30 minutes to obtain a phase A mixture;
taking the B phase raw materials according to the proportion, sequentially adding the B phase raw materials into an oil pot according to the order of butter fruit tree fruit fat, glycerol tri (ethyl caproate), cetostearyl alcohol, polydimethylsiloxane, diisostearyl malate, isostearyl alcohol isostearate, MONTANOV-68 (emulsifying agent), emulsciphos (phosphate emulsifying agent) and vitamin E, starting stirring, setting the rotating speed to be 20-25Hz, uniformly stirring, and heating to 85-87 ℃ to obtain a B phase mixture;
pumping the B-phase mixture into the A-phase mixture while stirring, setting the rotating speed to be 15-18Hz, setting the rotating speed to be 30-35Hz after the adding is completed, and stirring and mixing for 5-8 minutes;
Taking the C-phase raw materials according to a proportion, mutually dissolving in other containers to obtain a C-phase mixture, adding the C-phase mixture into a main pot after the temperature of the main pot is reduced to below 40 ℃, setting the rotating speed to 20-25Hz, stirring and mixing for 5-8min, and uniformly stirring to obtain the product.
In a fourth aspect, a whitening and spot-reducing emulsion comprises the whitening and spot-reducing composition of the first aspect.
Further, the whitening and freckle-removing emulsion comprises the following components in percentage by weight:
a: 43.95 to 70.75 percent of water, 2 to 3.8 percent of glycerol, 2.5 to 4.2 percent of 1, 2-pentanediol, 0.05 to 0.7 percent of hydrolyzed sodium hyaluronate and 0.1 to 0.4 percent of carbomer;
b: 2% -3.2% of olive oil, 2% -4% of polydimethylsiloxane, 2.5% -3.5% of isostearyl isostearate, 2.4% -3.3% of isononyl isononanoate, 3.5% -5% of MONTANOV-68 (emulsifier) and 0.4% -1.2% of vitamin E;
c: 1.5 to 3 percent of tranexamic acid, 3 to 6 percent of nicotinamide, 1.3 to 2.75 percent of ascorbyl glucoside, 3 to 7 percent of alpha-arbutin and 3 to 8 percent of azelaic acid.
Further, the preparation method of the whitening and spot-fading emulsion comprises the following steps:
proportionally adding the phase A raw materials into a main pot, starting stirring, setting the rotating speed to be 15-18Hz, uniformly stirring, heating to 85-90 ℃ at the same time, and preserving heat for 20-30 minutes to obtain a phase A mixture;
Taking the B phase raw materials according to a proportion, sequentially adding olive oil, polydimethylsiloxane, isostearyl isostearate, isononyl isononanoate, MONTANOV-68 (emulsifier) and vitamin E into an oil pan, stirring while adding, setting the rotating speed to 20-25Hz, and simultaneously heating to 85-87 ℃ to obtain a B phase mixture;
pumping the mixture B into the mixture A while stirring, setting the rotating speed to be 15-18Hz, and stirring and mixing for 5-8 minutes;
taking the C-phase raw materials according to a proportion, mutually dissolving in other containers to obtain a C-phase mixture, adding the C-phase mixture into a main pot after the temperature of the main pot is reduced to below 40 ℃, setting the rotating speed to 20-25Hz, stirring and mixing for 5-8min, and uniformly stirring to obtain the product.
Compared with the prior art, the invention has the following beneficial effects:
1. the whitening and spot-fading composition comprises several main components of nicotinamide, tranexamic acid, alpha-arbutin and ascorbyl glucoside, and has synergistic whitening and spot-fading effects. Nicotinamide inhibits the transfer of melanosomes to keratinocytes by inhibiting the generation of melanin particles, and has a certain antioxidation effect to prevent spontaneous glycosylation reaction of proteins and sugar; tranexamic acid is a plasmin inhibitor and inhibits PAR-2 receptor activation in keratinocytes, so that the melanosomes are blocked from being phagocytosed and distributed by epidermal cells, and the effects of relieving pigmentation and whitening are achieved; alpha-arbutin can reduce melanin generation and pigmentation by inhibiting tyrosinase activity in vivo; the ascorbyl glucoside is a derivative of natural vitamin C, contains stable components of glucose, reduces the characteristics of easy oxidation and reduction of the natural vitamin C, maintains the antioxidant activity of the vitamin C, has the reduction effect on the existing melanin, and has the effect of fading color spots. Combines a plurality of mechanisms, thereby realizing the effects of lightening color spots, relieving pigmentation and improving skin brightness.
2. The whitening and freckle-removing composition comprises the following main components in percentage by weight: 4-10% of nicotinamide, 3-5% of ascorbyl glucoside, 1-3% of tranexamic acid and 1-2% of alpha-arbutin, and the main components are reasonable in proportion, proper in concentration and high in safety to human bodies, and when the composition is added into essence, face cream and emulsion, the effects of whitening and fading spots can be exerted to the greatest extent.
3. The formula of the whitening and spot-lightening essence, the face cream and the emulsion comprises four components of nicotinamide, tranexamic acid, alpha-arbutin and ascorbyl glucoside, and other components with the whitening and spot-lightening effect can be added through the prior art or the implementation means, including but not limited to kojic acid, azelaic acid, vitamin E and derivatives, acetylcysteine, glutathione, butyl or hexyl resorcinol, astaxanthin, nonapeptide-1, fruit acid, licoflavone and the like, so that the whitening and spot-lightening effect is further enhanced.
4. The invention provides a formula and a preparation method of whitening and spot-lightening essence, face cream and emulsion, which do not contain hydroquinone, corticoids, extracts of unknown functional components and components which are not listed in a cosmetic use catalog, have high component controllability and definite efficacy, and simultaneously provide safety and effectiveness of whitening and spot lightening in zebra fish tests and human body tests.
Drawings
FIG. 1 is a graph showing the results of experiments for reducing melanin content in B16 cells according to example 1 of the present invention
FIG. 2 is a graph showing the results of an experiment for reducing PAR-2 activation of epidermal cells according to example 1 of the present invention
FIG. 3 is a graph showing the whitening results in the zebra fish test according to example 1 of the present invention
Detailed Description
The technical solutions in the embodiments will be clearly and completely described below. It will be apparent that the embodiments described below are only some, but not all, embodiments of the invention. All other embodiments, which can be made by those skilled in the art based on the embodiments of the invention without making any inventive effort, are intended to be within the scope of the invention.
In a first aspect, the invention provides a whitening and spot-fading composition, which is prepared from the following components in percentage by weight:
Figure SMS_2
wherein, nicotinamide inhibits the transfer of melanosomes to keratinocytes by inhibiting the generation of melanin particles, and has a certain antioxidation effect at the same time, thus preventing spontaneous glycosylation reaction of protein and sugar; tranexamic acid is a plasmin inhibitor and inhibits PAR-2 receptor activation in keratinocytes, so that the melanosomes are blocked from being phagocytosed and distributed by epidermal cells, and the effects of relieving pigmentation and whitening are achieved; alpha-arbutin can reduce melanin generation and pigmentation by inhibiting tyrosinase activity in vivo; the ascorbyl glucoside is a derivative of natural vitamin C, contains stable components of glucose, reduces the characteristics of easy oxidation and reduction of the natural vitamin C, maintains the antioxidant activity of the vitamin C, has the reduction effect on the existing melanin, and has the effect of fading color spots. Combines a plurality of mechanisms, thereby realizing the effects of lightening color spots, relieving pigmentation and improving skin brightness.
In a second aspect, a whitening and freckle-removing essence comprises the whitening and freckle-removing composition according to the first aspect.
Further, the essence for whitening and lightening spots comprises the following components in percentage by weight:
phase A: 65.93 to 89.4649 percent of pure water, 0.15 to 4 percent of glycerol, 0.1 to 2 percent of butanediol, 0.05 to 1 percent of sodium hyaluronate, 0.03 to 0.35 percent of sodium citrate and 0.0001 to 0.02 percent of citric acid;
and B phase: 0.8 to 4 percent of 1, 2-pentanediol and 0.15 to 0.7 percent of p-hydroxyacetophenone;
and C phase: 1 to 3 percent of tranexamic acid, 4 to 10 percent of nicotinamide, 3 to 5 percent of ascorbyl glucoside, 1 to 2 percent of alpha-arbutin, 0.25 to 1.5 percent of beta-glucan and 0.005 to 0.5 percent of sodium hydroxide.
Further, the preparation method of the whitening and freckle-removing essence comprises the following steps:
step S1, taking the phase A raw materials according to a proportion, sequentially adding pure water, glycerol, butanediol, sodium hyaluronate, sodium citrate and citric acid into a main pot according to the sequence, starting stirring, setting the rotating speed to be 20-25Hz, uniformly stirring, heating to 83-87 ℃ at the same time, and preserving heat for 20-30 minutes to obtain a phase A mixture;
s2, mixing the B-phase raw materials in other containers according to a proportion to obtain a B-phase mixture, adding the B-phase mixture into the A-phase mixture in the main pot after the temperature of the main pot is reduced to 63-67 ℃, setting the rotating speed to 20-25Hz, and uniformly stirring;
And S3, proportionally taking sodium hydroxide in the C phase, dissolving the sodium hydroxide in pure water, cooling the temperature of the main pot to 38-42 ℃, adding the C phase raw materials into the main pot according to the sequence of tranexamic acid, nicotinamide, ascorbyl glucoside, alpha-arbutin, beta-glucan and sodium hydroxide, and uniformly stirring to obtain the product.
Further, in step S1, the temperature is raised to 83 ℃ to 87 ℃, wherein 85 ℃ is preferred; the incubation is for 20-30 minutes, with 30 minutes being preferred.
Further, in step S2, after the temperature of the main pot is reduced to 63 ℃ to 67 ℃, the temperature is preferably reduced to 65 ℃.
In a third aspect, a whitening and spot-reducing cream comprises the whitening and spot-reducing composition of the first aspect.
Further, the whitening and freckle-removing face cream comprises the following components in percentage by weight:
phase A: 73.8495 to 24.585 percent of pure water, 3 to 5 percent of glycerol, 2.5 to 4.3 percent of 1, 2-pentanediol, 0.5 to 9 percent of hydroxypropyl tetrahydropyran triol, 0.1 to 1.8 percent of p-hydroxyacetophenone, 0.05 to 0.65 percent of hydrolyzed sodium hyaluronate and 0.1 to 0.35 percent of carbomer;
and B phase: 2% -5% of butter fruit, 3% -7% of glycerol tri (ethylhexanoate), 3% -5.8% of cetostearyl alcohol, 1.8% -5% of polydimethylsiloxane, 1% -3% of diisostearyl malate, 0.8% -3% of isostearyl isostearate, 2.3% -4.5% of MONTANOV-68 (emulsifying agent), 0.45% -1% of emulghos (phosphate emulsifying agent) and 0.1% -1% of vitamin E;
And C phase: 0.05 to 0.2 percent of carnosine, 0.0005 to 0.005 percent of palmitoyl pentapeptide-4, 0.1 to 0.36 percent of arginine, 1 to 3 percent of tranexamic acid, 2 to 5 percent of nicotinamide, 1 to 3 percent of ascorbyl glucoside, 0.5 to 2 percent of alpha-arbutin, 0.5 to 1.6 percent of kojic acid, 0.2 to 3 percent of saccharomyces cerevisiae extract and 0.1 to 0.85 percent of ceramide.
Further, the preparation method of the whitening and freckle-removing facial cream comprises the following steps:
s1, proportionally adding the phase A raw materials into a main pot, starting stirring, setting the rotating speed to be 20-25Hz, uniformly stirring, heating to 85-90 ℃ at the same time, and preserving heat for 20-30 minutes to obtain a phase A mixture;
s2, taking the B phase raw materials according to a proportion, sequentially adding the B phase raw materials into an oil pan according to the sequence of the butter tree fruit fat, the triglyceride (ethyl caproic acid) ester, the cetostearyl alcohol, the polydimethylsiloxane, the diisostearyl alcohol malate, the isostearate, the MONTANOV-68 (emulsifying agent), the Emulsiformos (phosphate emulsifying agent) and the vitamin E, starting stirring, setting the rotating speed to be 20-25Hz, uniformly stirring, and simultaneously heating to 85-87 ℃ to obtain a B phase mixture;
s3, pumping the B-phase mixture into the A-phase mixture while stirring, setting the rotating speed to be 15-18Hz, setting the rotating speed to be 30-35Hz after the adding, and stirring and mixing for 5-8 minutes;
And S4, taking the C-phase raw materials according to a proportion, mutually dissolving in other containers to obtain a C-phase mixture, adding the C-phase mixture into a main pot after the temperature of the main pot is reduced to below 40 ℃, setting the rotating speed to be 20-25Hz, stirring and mixing for 5-8min, and uniformly stirring to obtain the product.
Further, in step S1, the temperature is raised to 85-90 ℃, wherein 85-87 ℃ is preferred; the incubation is for 20-30 minutes, with 25 minutes being preferred.
In a fourth aspect, a whitening and spot-reducing emulsion comprises the whitening and spot-reducing composition of the first aspect.
Further, the whitening and freckle-removing emulsion comprises the following components in percentage by weight:
a: 43.95 to 70.75 percent of water, 2 to 3.8 percent of glycerol, 2.5 to 4.2 percent of 1, 2-pentanediol, 0.05 to 0.7 percent of hydrolyzed sodium hyaluronate and 0.1 to 0.4 percent of carbomer;
b: 2% -3.2% of olive oil, 2% -4% of polydimethylsiloxane, 2.5% -3.5% of isostearyl isostearate, 2.4% -3.3% of isononyl isononanoate, 3.5% -5% of MONTANOV-68 (emulsifier) and 0.4% -1.2% of vitamin E;
c: 1.5 to 3 percent of tranexamic acid, 3 to 6 percent of nicotinamide, 1.3 to 2.75 percent of ascorbyl glucoside, 3 to 7 percent of alpha-arbutin and 3 to 8 percent of azelaic acid.
Further, the preparation method of the whitening and spot-fading emulsion comprises the following steps:
s1, proportionally adding the phase A raw materials into a main pot, starting stirring, setting the rotating speed to be 15-18Hz, uniformly stirring, heating to 85-90 ℃ at the same time, and preserving heat for 20-30 minutes to obtain a phase A mixture;
s2, taking the B-phase raw materials according to a proportion, sequentially adding olive oil, polydimethylsiloxane, isostearyl isostearate, isononyl isononanoate, MONTANOV-68 (emulsifying agent) and vitamin E into an oil pan, stirring while adding, setting the rotating speed to 20-25Hz, and simultaneously heating to 85-87 ℃ to obtain a B-phase mixture;
s3, pumping the mixture B into the mixture A while stirring, setting the rotating speed to be 15-18Hz, and stirring and mixing for 5-8 minutes;
and S4, taking the C-phase raw materials according to a proportion, mutually dissolving in other containers to obtain a C-phase mixture, adding the C-phase mixture into a main pot after the temperature of the main pot is reduced to below 40 ℃, setting the rotating speed to be 20-25Hz, stirring and mixing for 5-8min, and uniformly stirring to obtain the product.
Further, in step S1, the temperature is raised to 85-90 ℃, wherein 85 ℃ is preferred; the incubation is for 20-30 minutes, with 30 minutes being preferred.
The invention has been tested several times in succession, and the invention will now be described in further detail with reference to a few test results, which are described in detail below in connection with specific examples.
Example 1
The whitening and freckle-removing essence comprises the following components in percentage by weight:
phase A: 82.428% of pure water, 0.6% of glycerol, 0.5% of butanediol, 0.25% of sodium hyaluronate, 0.12% of sodium citrate and 0.002% of citric acid;
and B phase: 3.5% of 1, 2-pentanediol and 0.4% of p-hydroxyacetophenone;
and C phase: 3% of tranexamic acid, 5% of nicotinamide, 2% of ascorbyl glucoside, 1% of alpha-arbutin, 1% of beta-glucan and 0.2% of sodium hydroxide.
Further, the preparation method of the whitening and freckle-removing essence comprises the following steps:
step S1, taking phase A raw materials according to a proportion, sequentially adding pure water, glycerol, butanediol, sodium hyaluronate, sodium citrate and citric acid into a main pot according to the sequence, starting stirring, setting the rotating speed to be 20Hz, uniformly stirring, heating to 84 ℃ at the same time, and preserving heat for 30 minutes to obtain a phase A mixture;
s2, mixing the B-phase raw materials in other containers according to a proportion to obtain a B-phase mixture, adding the B-phase mixture into the A-phase mixture in the main pot after the temperature of the main pot is reduced to 65 ℃, setting the rotating speed to be 25Hz, and uniformly stirring;
and S3, proportionally taking sodium hydroxide in the C phase, dissolving the sodium hydroxide in pure water, and after the temperature of the main pot is reduced to 40 ℃, adding the C phase raw materials into the main pot according to the sequence of tranexamic acid, nicotinamide, ascorbyl glucoside, alpha-arbutin, beta-glucan and sodium hydroxide, and uniformly stirring to obtain the essence for whitening and lightening the spots.
Example 2
The whitening and freckle-removing face cream comprises the following components in percentage by weight:
phase A: 59.548% of pure water, 4% of glycerol, 3.5% of 1, 2-pentanediol, 1% of hydroxypropyl tetrahydropyran triol, 0.4% of p-hydroxyacetophenone, 0.2% of hydrolyzed sodium hyaluronate and 0.15% of carbomer;
and B phase: 3% of butter fruit, 6% of triglyceride (ethylhexanoate), 3.4% of cetostearyl alcohol, 3% of polydimethylsiloxane, 2% of diisostearyl malate, 1.2% of isostearyl isostearate, 2.6% of MONTANOV-68 (emulsifier), 0.8% of Emulsiformos (phosphate emulsifier) and 0.5% of vitamin E;
and C phase: carnosine 0.15%, palmitoyl pentapeptide-4.002%, arginine 0.15%, tranexamic acid 2.5%, nicotinamide 2.5%, ascorbyl glucoside 2%, alpha-arbutin 0.75%, kojic acid 0.65%, saccharomyces cerevisiae extract 0.5%, and ceramide 0.5%.
Further, the preparation method of the whitening and freckle-removing facial cream comprises the following steps:
s1, proportionally adding the phase A raw materials into a main pot, starting stirring, setting the rotating speed to be 20-25Hz, uniformly stirring, heating to 85 ℃, and preserving heat for 25 minutes to obtain a phase A mixture;
s2, taking phase B raw materials according to a proportion, sequentially adding the raw materials into an oil pan according to the order of butter fruit tree fruit fat, glycerol tri (ethyl hexanoate), cetostearyl alcohol, polydimethylsiloxane, diisostearyl alcohol malate, isostearyl alcohol isostearate, MONTANOV-68 (emulsifying agent), emulsiformos (phosphate emulsifying agent) and vitamin E, starting stirring, setting the rotating speed to be 25Hz, uniformly stirring, and simultaneously heating to 85 ℃ to obtain a phase B mixture;
S3, pumping the B-phase mixture into the A-phase mixture while stirring, setting the rotating speed to 18Hz, setting the rotating speed to 35Hz after the adding is completed, and stirring and mixing for 5 minutes;
and S4, taking the C-phase raw materials according to a proportion, mutually dissolving the C-phase raw materials in other containers to obtain a C-phase mixture, adding the C-phase mixture into the main pot after the temperature of the main pot is reduced to 40 ℃, setting the rotating speed to 20Hz, stirring and mixing for 8min, and uniformly stirring to obtain the whitening and freckle-removing face cream.
Example 3
The whitening and freckle-removing emulsion comprises the following components in percentage by weight:
a: 58.4% of water, 3% of glycerol, 3.5% of 1, 2-pentanediol, 0.15% of hydrolyzed sodium hyaluronate and 0.15% of carbomer;
b: 3% of olive oil, 3% of polydimethylsiloxane, 3% of isostearyl isostearate, 3% of isononyl isononanoate, 4% of MONTANOV-68 (emulsifier) and 0.8% of vitamin E;
c: 2% of tranexamic acid, 5% of nicotinamide, 2% of ascorbyl glucoside, 5% of alpha-arbutin and 4% of azelaic acid;
further, the preparation method of the whitening and spot-fading emulsion comprises the following steps:
s1, proportionally adding the phase A raw materials into a main pot, starting stirring, setting the rotating speed to be 15-18Hz, uniformly stirring, heating to 85 ℃, and preserving heat for 30 minutes to obtain a phase A mixture;
S2, taking the B-phase raw materials according to a proportion, sequentially adding olive oil, polydimethylsiloxane, isostearyl isostearate, isononyl isononanoate, MONTANOV-68 (emulsifying agent) and vitamin E into an oil pan, stirring while adding, setting the rotating speed to 20Hz, and simultaneously heating to 85 ℃ to obtain a B-phase mixture;
s3, pumping the mixture B into the mixture A while stirring, setting the rotating speed to be 15Hz, and stirring and mixing for 8 minutes;
and S4, taking the C-phase raw materials according to a proportion, mutually dissolving the C-phase raw materials in other containers to obtain a C-phase mixture, adding the C-phase mixture into the main pot after the temperature of the main pot is reduced to 40 ℃, setting the rotating speed to 20Hz, stirring and mixing for 5min, and uniformly stirring to obtain the whitening and spot-fading emulsion.
Effect verification experiment
1. Antioxidant experiment
Experimental principle: DPPH, also known as 1, 1-diphenyl-2-trinitrophenylhydrazine, is a very stable radical of the nitrogen center, whose stability is mainly due to steric hindrance of the 3 benzene rings of the resonance stabilization, so that unpaired electrons on the nitrogen atom clamped in between cannot exert their due electron pairing. DPPH can capture other free radicals and reflect the scavenging ability of the free radicals by observing the change in absorbance at 520nm wavelength in the reaction system after addition. If the antioxidant capacity exists in the measured object, the single electron of DPPH is captured, the maximum absorbance is reduced, and the maximum absorbance is obviously linear.
The experimental steps are as follows:
s1, weighing 0.002 g of DPPH sold in the market, dissolving in 50ml of ethanol, preserving in a dark place, preparing ascorbyl glucoside (0.5 mg/ml) as a positive control, taking 1-2ml of each of the examples 1 and 2 to be tested, diluting with 10 times of volume of double distilled water, shaking, dissolving, preparing, centrifuging, and taking the supernatant for measurement;
s2, dissolving DPPH in 0.1ml of 96-well plates, and adding 0.1ml of various samples to be tested prepared by dilution and samples with different dilution multiples of ascorbyl glucoside (0.5 mg/ml) positive control. The reaction was carried out at 37℃for 30min, and the absorbance at 517nm (average value of two wells) was measured;
s3, calculating the free radical clearance, wherein the free radical clearance (%) = [1- (A sample-A blank)/(A blank) DPPH Control]X 100% and the experimental data are shown in table 1.
Table 1 antioxidant test results:
experimental sample Radical (DPPH) clearance (%)
2.0% of the component of example 1 76.2
0.5% of the component of example 1 34.3
2.0% of example 2 component 84.5
0.5% of the component of example 2 37.6
2.0% of example 3 component 73.6
0.5% of the component of example 3 29.8
0.5mg/ml ascorbyl glucoside 62.1
As shown by the antioxidant experiment results in Table 1, the composition for whitening and lightening spots contains ascorbyl glucoside as a whitening and antioxidant component, has obvious effect of scavenging free radicals, and has stronger antioxidant synergistic effect at the concentration of 2% in the combined formula compared with the same concentration of positive 0.5mg/ml ascorbyl glucoside, so that the ascorbyl glucoside in the composition for whitening and lightening spots does not act independently, and the main components of nicotinamide, ascorbyl glucoside, tranexamic acid and alpha-arbutin can be further proved to mutually promote and synergistically increase.
2. Tyrosinase inhibition assay
The test was performed by selecting the powder of arbutin (control) as a whitening agent of example 1 and commercially available arbutin powder (control), wherein the control is 2% of alpha-arbutin, and the rest ingredients and preparation methods are the same.
The experimental steps are as follows:
s1, preparing a test sample and a solution, wherein the DMEM complete medium is prepared: DMEM basal medium 44.5ml,FBS 5ml,100X diabody 0.5ml;
DMEM complete medium formulation (dilution) with 2% fbs: DMEM basal medium 47.5ml,FBS 2ml,100X diabody 0.5ml;
diluting the example 1 and the diluent according to the proportion of 1:50, filtering and sterilizing the diluent by 0.2um, and preserving the diluent at the temperature of 2-8 ℃;
2% alpha-arbutin solution: dissolving a certain amount of alpha-arbutin dry powder into 2% solution with diluent, filtering with 0.2um for sterilization, and preserving at 2-8deg.C;
s2, selecting logarithmic phase B16 cells, paving 96-well plates, placing 100ul/5000 cells/well into a carbon dioxide incubator, and continuously culturing; after the cells are attached to the wall the next day, adding the corresponding reagent to be detected, putting the cells into a carbon dioxide incubator for further cultivation for 48 hours, sucking the culture solution, washing twice by PBS, adding 50ul of 1% TritonX-100 solution into each hole, rapidly putting the cells into a refrigerator at-80 ℃ for freezing for 60 minutes, and adding the cells into a water bath at 37 ℃ for 30 minutes. Adding 0.1% levodopa 50ul, reacting for 2 hours at 37 ℃, and measuring absorbance at 490nm by an enzyme-labeled instrument (DMEM with 2% FBS as control group);
S3, calculating tyrosinase activity, wherein the tyrosinase activity (%) = (experimental group-blank group)/(control group-blank group) ×100%, and experimental data are shown in table 2.
Table 2 tyrosinase inhibition assay results:
Figure SMS_3
note that: no difference is found between the cell viability of the arbutin positive group and 0.5%, 1% and 2% of the whitening and freckle-removing essence by the CC-K8 method.
The experimental results in table 2 show that the example 1 and 2% of alpha-arbutin have good inhibition effect on tyrosinase, and the essence containing nicotinamide, tranexamic acid, alpha-arbutin and ascorbyl glucoside has synergistic inhibition effect on tyrosinase.
3. Experiments for reducing melanin content in B16 cells
And (3) in the selected antioxidant experiment, 0.5-2% of the solution prepared in the step S2 and 2% of alpha-arbutin are added into B16 cells, and the experimental result is observed.
The experimental steps are as follows:
s1, using B16 cells, paving 96-well plates, placing 100ul/5000 cells/well into a carbon dioxide incubator, and continuously culturing; the next day, after the cells adhere to the wall, the supernatant is sucked and removed, and then the solution prepared in the step S2 and 0.5 to 2 percent of the solution prepared in the example 1 and 2 percent of the alpha-arbutin are added into the cells, and the cells are cultured in an incubator for 24 hours;
s2, observing under a microscope after 24 hours, photographing and preserving, digesting cells by using pancreatin, centrifuging the culture supernatant for 1000r/6min, discarding the supernatant after centrifugation, re-suspending cell sediment by using 0.5ml DMEM, taking 200ul of the supernatant after centrifugation, adding 10mol/L NaOH solution of 10% DMSO to dissolve melanin in a water bath at 80 ℃, wherein the solution still presents black;
S3, taking 100ul of the dissolved liquid, adding the dissolved liquid into a 96-well plate, measuring an OD value at 490nm, and calculating a formula (a control group is DMEM (2% FBS)) of melanin content reduction: melanin content (%) = (experimental group-blank group)/(control group-blank group) ×100%, calculated results are shown in table 3, and a map of the change in melanin content in B16 cells is shown in fig. 1.
Table 3B16 results of experiments for reduced melanin content in cells:
Figure SMS_4
the experimental results in Table 3 show that 0.5-2% of the whitening and freckle-removing essence can obviously reduce the generation of melanin content in melanocytes. As shown in FIG. 1, the whitening and freckle-removing essence has a remarkable effect of reducing the melanin content in B16 cells. By the combined action of the main components of nicotinamide, tranexamic acid, alpha-arbutin and ascorbyl glucoside, which are obtained by the comparison of 2% alpha-arbutin, the melanin content in B16 cells can be further reduced.
4. Epidermal cell PAR-2 activation test
After the sample of example 1 was treated, the sample was added to cells, and the results of the expression of cellular fluorescence were observed.
The experimental steps are as follows:
s1, preparing a solution: 1ml of the sample 1 was diluted 50-fold with DMEM culture medium containing 2% FBS to obtain a 2% solution to be tested;
S2, cell culture: inoculating HACAT cells and B16 cells respectively into DMEM medium containing 10% FBS under aseptic condition, standing at 37deg.C, and 5% CO 2 Culturing at constant temperature in an incubator, and changing liquid for 1 time for 2 days. Taking HACAT cells and B16 cells in logarithmic growth phase, respectively using 0.25% trypsin to digest and collect the cells, and using the HACAT cells: b16 cells were 4:1, setting HACAT cell independent culture group, and adjusting cell concentration to 2×10 4 Inoculating 100ul of each hole into a 96-well plate, culturing in an incubator for 24 hours, discarding supernatant, adding 2% of the liquid to be tested respectively, adding the same volume of DMEM culture solution containing 2% FBS into a blank control group, arranging 2 compound holes in each group, and culturing in a carbon dioxide incubator for 24 hours;
s3, fluorescence detection: the HACAT and B16 cell co-culture groups and HACAT cell individual culture groups were fixed with cells in 4% paraformaldehyde for 10 minutes at room temperature. Cells were washed 3 times with ice PBS, incubated with PBST (PBS+0.1% Tween 20, 1% BSA, 22.52mg/mL glycine) for 30 min, blocking non-specific binding of antibodies. The solution was aspirated at room temperature, and rabbit monoclonal antibody Anti-PAR2 (cat# ab 180953) diluted 500-fold with PBST was added, and cells were incubated in a dark environment for 1 hour, or overnight at 4 ℃. The solution was aspirated and the cells were washed 3 times for 5 minutes with PBS. FITC-labeled goat polyclonal antibody secondary anti-rabbit IgG (cat# ab 150077) was diluted 1500-fold with 1% BSA solution at room temperature, cells were incubated for 1 hour in the dark, washed 3 times in PBS in the dark for 5 minutes each, immediately observed under a fluorescence microscope (Nikon: TS 2R) and photographed to give FIG. 2.
As shown in fig. 2, 2% of the cells treated in example 1 were less fluorescent than the control untreated cells, indicating that the protease activated receptor (PAR-2) was inhibited and the whitening and spot-lightening essence reduced the transport of melanosomes to epidermal cells via PAR-2.
5. Maximum concentration evaluation of whitening and freckle-removing essence in zebra fish
The product of example 1 was selected and commissioned to the Hangzhou Cyclotte Biotechnology Co., ltd.
Experimental principle:
zebra fish is one of the alternative species currently used in human health and ecological hazard assessment, zebra fish has 87% high similarity with human genes, and is the third largest model organism except for rats and mice. Zebra fish are subject to environmental and chemical effects and present death and developmental toxicity. The maximum detection concentration (MTC) of the sample can thus be determined by the death and toxicity of the zebra fish.
The experimental steps are as follows:
s1, randomly selecting zebra fish in a 6-hole plate, wherein 15 tails are arranged in each hole;
s2, taking samples of the embodiment 1, respectively dissolving the samples with pure water to obtain samples with the concentration of 0.5%, 1%, 2%, 4% and 8% of the embodiment 1, and simultaneously setting a normal control group, wherein the capacity of each hole is 3mL;
s3, incubating for 45h at 28 ℃ in a dark place;
S4, determining MTC of the sample to normal zebra fish according to the death condition and the toxicity condition of the zebra fish, and recording experimental results, wherein the experimental results are shown in Table 4.
TABLE 4 evaluation results of maximum concentration of whitening and freckle-removing essence in zebra fish
Figure SMS_5
The results in table 4 can obtain that under the test condition, the MTC of the whitening and freckle-fading essence to normal zebra fish is 1%, so that the whitening and freckle-fading essence is safe in components and reasonable in proportion.
6. Evaluation of whitening efficacy of essence for whitening and lightening spots in zebra fish
The essence product of example 1 for whitening and lightening spots was selected and entrusted to Hangzhou Cyclots biotechnology Co., ltd.
Experimental principle:
zebra fish were transparent throughout their body at the beginning of development, and melanin began to grow from retinal epithelium when embryos developed to 24 h. Pigment cells originate from a population of cells differentiated by the dorsal ectoderm-neural crest cells, and then proliferate, migrate, differentiate into pigment blast cells. Intervention during melanin formation can inhibit melanin formation. Therefore, whether the sample has whitening efficacy is evaluated by zebra fish skin whiteness.
The experimental steps are as follows:
s1, randomly selecting zebra fish in a 6-hole plate, wherein 15 tails are arranged in each hole;
s2, water-soluble administration was performed to the diluted 0.5% concentration of example 1, and a normal control group was set at a capacity of 3mL per well. Incubating for 45h at 28 ℃ in dark;
S3, randomly selecting 10 zebra fish from each experimental group, photographing under an dissecting microscope, analyzing and collecting data by using advanced image processing software to obtain a graph 3 (the dotted line part is a quantitative area), analyzing the melanin signal intensity (S) of the zebra fish head, calculating the whitening efficacy of the sample according to a formula, and recording the result as shown in the table 5. Whitening efficacy (%) = [ S (normal control group) -S (sample group)/S (normal control group) ]x100%.
Table 5 evaluation results of whitening efficacy of whitening and spot-lightening essence in zebra fish:
detecting items Concentration of detection (%) Efficacy (%) p value Detection result
Whitening efficacy 0.5 65 <0.001 Effective and effective
As can be seen from the data in table 5 and fig. 3, the head melanin signal intensity of the whitening and spot-lightening essence is significantly reduced compared with that of the normal control group, which proves the whitening ability of the whitening and spot-lightening composition and the formulation of the composition, and reveals the whitening efficacy.
7. Skin whitening and freckle fading essence liquid human body skin patch test
Example 1 was selected as a sample and was submitted to the dermatological institute of hospitals in Chongqing.
The experimental steps are as follows:
s1, selecting experimental samples as the whitening and spot-fading essence and the reference substance prepared in the first embodiment, wherein the reference substance is blank filter paper;
s1, selecting a total of 30 subjects, wherein 10 men and 20 women are aged 40 to 59 years, and the average age is 53.8+/-4.2 years, and the total number of the subjects meets the volunteer inclusion standard of the subjects;
S3, selecting qualified spot test equipment, sucking 0.020-0.025 mL of the sample of the example 1 and the reference sample by using a pipettor by using a closed spot test method, dripping the sample onto a filter paper sheet in the spot test device, applying a hyposensitization adhesive tape to the back of a subject, removing the sample after 2 hours, observing skin reactions after 0.5, 24 and 48 hours respectively, and recording the results according to the skin reaction grading standard in the current effective technical specifications, wherein the results are shown in the table 6.
Table 6 skin Patch test results of whitening and freckle-removing essence
Figure SMS_6
Figure SMS_7
As can be seen from the data in table 6, the skin patch test results of human body show that adverse skin reactions occur in 0 cases among 30 persons, so that the essence for whitening and lightening the spots is not easy to be allergic, the ingredients are safe, and the proportion of the composition for whitening and lightening the spots is proper.
8. Whitening effect test of whitening and freckle-removing essence on human skin
Example 1 was selected as a sample and was submitted to the dermatological institute of hospitals in Chongqing.
The experimental steps are as follows:
s1, preparing a test product: whitening and spot-lightening essence prepared in example 1, negative control: blackened area blank, positive control: 7% ascorbic acid (vitamin C) preparation was prepared according to the standard method annex formulation.
S2, selecting a subject: completing the test for 30 total subjects, wherein men 12, women 18, ages 24 to 58, average ages 37.37 ±9.52, meet the subject's volunteer inclusion and exclusion criteria;
S3, performing an experiment: the test is carried out according to the specific requirements of the current effective technical specification method.
And (3) establishing an ultraviolet blackening model: first testing the minimum erythema dose (Minimal erythema does, MED) at the test site (back) of the group of eligible subjects, then selecting 3 areas at the test site of not less than 6cm 2 The test product areas are respectively a negative control area and a positive control area, the interval between each test area is not less than 1.0cm, and the selected area in each test area is not less than 0.5cm 2 Is irradiated with an ultraviolet ray solar simulator 1 time a day at a dose of 0.75 times MED for 4 days. The skin color of each darkened test area was visually assessed and instrumentally detected every other week after application of the test article and recorded as shown in table 7.
Cosmetic freckle removing and whitening efficacy test (first method) is adopted:
minimum erythema dose (Minimal erythema dose, MED): causing a clearly visible erythema of the skin in a range reaching the minimum dose m 2) or for a minimum time of uv irradiation required for most of the area of the irradiation spot;
individual type angle (individual type angle ITA °): measuring skin L x a x b x color space data by a skin colorimeter or a reflectance spectrophotometer to characterize parameters of human skin color;
Melanin Index (MI): parameters of melanin content in skin are characterized by measuring the absorption of a specific wavelength spectrum by the skin surface.
TABLE 7 visual skin tone grade score difference results for each test zone before and after product use [ median (minimum, maximum) ]
Figure SMS_8
Figure SMS_9
The data of the oil table 7 can be compared with negative control, and the score difference of the visual skin color grade of the test product after 1 week, 2 weeks, 3 weeks and 4 weeks of use is obviously improved (P < 0.05); compared with a negative control, the skin blackening of the test product group is obviously improved (P is less than 0.05) through the integral judgment of the visual skin color grade score regression coefficient analysis, so that the product has obvious whitening effect on skin, the components of the whitening and spot-fading composition are safe and reasonable in proportion, the efficacy of each main component can be exerted to the greatest extent, the essence, the face cream and the emulsion added with the whitening and spot-fading composition have obvious whitening effect, and the whitening and spot-fading composition is safe and free of stimulation on human bodies and is not easy to be allergic.
Finally, it is noted that the above embodiments are only for illustrating the technical solution of the present invention and not for limiting the same, and although the present invention has been described in detail with reference to the preferred embodiments, it should be understood by those skilled in the art that modifications and equivalents may be made thereto without departing from the spirit and scope of the technical solution of the present invention, which is intended to be covered by the scope of the claims of the present invention.

Claims (10)

1. The whitening and freckle-removing composition is characterized by comprising the following raw materials in percentage by weight:
Figure FDA0004066931750000011
2. a whitening and spot-lightening essence, characterized by comprising the whitening and spot-lightening composition according to claim 1.
3. The whitening and freckle-removing essence as claimed in claim 2, wherein the whitening and freckle-removing essence comprises the following components in percentage by weight:
phase A: 65.93 to 89.4649 percent of pure water, 0.15 to 4 percent of glycerol, 0.1 to 2 percent of butanediol, 0.05 to 1 percent of sodium hyaluronate, 0.03 to 0.35 percent of sodium citrate and 0.0001 to 0.02 percent of citric acid;
and B phase: 0.8 to 4 percent of 1, 2-pentanediol and 0.15 to 0.7 percent of p-hydroxyacetophenone;
and C phase: 1 to 3 percent of tranexamic acid, 4 to 10 percent of nicotinamide, 3 to 5 percent of ascorbyl glucoside, 1 to 2 percent of alpha-arbutin, 0.25 to 1.5 percent of beta-glucan and 0.005 to 0.5 percent of sodium hydroxide.
4. The whitening and freckle-removing essence as claimed in claim 3, wherein the preparation method of the whitening and freckle-removing essence comprises the following steps:
taking the phase A raw materials according to a proportion, sequentially adding pure water, glycerol, butanediol, sodium hyaluronate, sodium citrate and citric acid into a main pot, starting stirring, setting the rotating speed to be 20-25Hz, uniformly stirring, heating to 83-87 ℃ at the same time, and preserving heat for 20-30 minutes to obtain a phase A mixture;
Mixing the B-phase raw materials in other containers according to a proportion to obtain a B-phase mixture, adding the B-phase mixture into the A-phase mixture in the main pot after the temperature of the main pot is reduced to 63-67 ℃, setting the rotating speed to 20-25Hz, and uniformly stirring;
and (3) dissolving sodium hydroxide in the C phase by pure water according to a proportion, cooling the temperature of the main pot to 38-42 ℃, adding the C phase raw materials into the main pot according to the sequence of tranexamic acid, nicotinamide, ascorbyl glucoside, alpha-arbutin, beta-glucan and sodium hydroxide, and uniformly stirring to obtain the product.
5. A whitening and spot-reducing cream comprising the whitening and spot-reducing composition of claim 1.
6. The whitening and freckle-removing facial cream according to claim 5, wherein the whitening and freckle-removing facial cream comprises the following components in percentage by weight:
phase A: 73.8495 to 24.585 percent of pure water, 3 to 5 percent of glycerol, 2.5 to 4.3 percent of 1, 2-pentanediol, 0.5 to 9 percent of hydroxypropyl tetrahydropyran triol, 0.1 to 1.8 percent of p-hydroxyacetophenone, 0.05 to 0.65 percent of hydrolyzed sodium hyaluronate and 0.1 to 0.35 percent of carbomer;
and B phase: 2% -5% of butter fruit, 3% -7% of glycerol tri (ethylhexanoate), 3% -5.8% of cetostearyl alcohol, 1.8% -5% of polydimethylsiloxane, 1% -3% of diisostearyl malate, 0.8% -3% of isostearyl isostearate, 2.3% -4.5% of MONTANOV-68 (emulsifying agent), 0.45% -1% of emulghos (phosphate emulsifying agent) and 0.1% -1% of vitamin E;
And C phase: 0.05 to 0.2 percent of carnosine, 0.0005 to 0.005 percent of palmitoyl pentapeptide-4, 0.1 to 0.36 percent of arginine, 1 to 3 percent of tranexamic acid, 2 to 5 percent of nicotinamide, 1 to 3 percent of ascorbyl glucoside, 0.5 to 2 percent of alpha-arbutin, 0.5 to 1.6 percent of kojic acid, 0.2 to 3 percent of saccharomyces cerevisiae extract and 0.1 to 0.85 percent of ceramide.
7. The whitening and spot-removing facial cream according to claim 6, wherein the preparation method of the whitening and spot-removing facial cream comprises the following steps:
proportionally adding the phase A raw materials into a main pot, starting stirring, setting the rotating speed to be 20-25Hz, uniformly stirring, heating to 85-90 ℃ at the same time, and preserving heat for 20-30 minutes to obtain a phase A mixture;
taking the B phase raw materials according to the proportion, sequentially adding the B phase raw materials into an oil pot according to the order of butter fruit tree fruit fat, glycerol tri (ethyl caproate), cetostearyl alcohol, polydimethylsiloxane, diisostearyl malate, isostearyl alcohol isostearate, MONTANOV-68 (emulsifying agent), emulsciphos (phosphate emulsifying agent) and vitamin E, starting stirring, setting the rotating speed to be 20-25Hz, uniformly stirring, and heating to 85-87 ℃ to obtain a B phase mixture;
pumping the B-phase mixture into the A-phase mixture while stirring, setting the rotating speed to be 15-18Hz, setting the rotating speed to be 30-35Hz after the adding is completed, and stirring and mixing for 5-8 minutes;
Taking the C-phase raw materials according to a proportion, mutually dissolving in other containers to obtain a C-phase mixture, adding the C-phase mixture into a main pot after the temperature of the main pot is reduced to below 40 ℃, setting the rotating speed to 20-25Hz, stirring and mixing for 5-8min, and uniformly stirring to obtain the product.
8. An emulsion for whitening and lightening spots, comprising the composition for whitening and lightening spots according to claim 1.
9. The whitening and spot-fading emulsion as set forth in claim 8, wherein the whitening and spot-fading emulsion comprises the following components in percentage by weight:
a: 43.95 to 70.75 percent of water, 2 to 3.8 percent of glycerol, 2.5 to 4.2 percent of 1, 2-pentanediol, 0.05 to 0.7 percent of hydrolyzed sodium hyaluronate and 0.1 to 0.4 percent of carbomer;
b: 2% -3.2% of olive oil, 2% -4% of polydimethylsiloxane, 2.5% -3.5% of isostearyl isostearate, 2.4% -3.3% of isononyl isononanoate, 3.5% -5% of MONTANOV-68 (emulsifier) and 0.4% -1.2% of vitamin E;
c: 1.5 to 3 percent of tranexamic acid, 3 to 6 percent of nicotinamide, 1.3 to 2.75 percent of ascorbyl glucoside, 3 to 7 percent of alpha-arbutin and 3 to 8 percent of azelaic acid.
10. The whitening and spot-fading emulsion as set forth in claim 9, wherein the preparation method of the whitening and spot-fading emulsion comprises the following steps:
Proportionally adding the phase A raw materials into a main pot, starting stirring, setting the rotating speed to be 15-18Hz, uniformly stirring, heating to 85-90 ℃ at the same time, and preserving heat for 20-30 minutes to obtain a phase A mixture;
taking the B phase raw materials according to a proportion, sequentially adding olive oil, polydimethylsiloxane, isostearyl isostearate, isononyl isononanoate, MONTANOV-68 (emulsifier) and vitamin E into an oil pan, stirring while adding, setting the rotating speed to 20-25Hz, and simultaneously heating to 85-87 ℃ to obtain a B phase mixture;
pumping the mixture B into the mixture A while stirring, setting the rotating speed to be 15-18Hz, and stirring and mixing for 5-8 minutes;
taking the C-phase raw materials according to a proportion, mutually dissolving in other containers to obtain a C-phase mixture, adding the C-phase mixture into a main pot after the temperature of the main pot is reduced to below 40 ℃, setting the rotating speed to 20-25Hz, stirring and mixing for 5-8min, and uniformly stirring to obtain the product.
CN202310078898.3A 2023-01-19 2023-01-19 Whitening and freckle-removing composition and essence, cream and emulsion containing composition Pending CN116407462A (en)

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN117100640A (en) * 2023-08-23 2023-11-24 宁波伯通伟达生物医药有限公司 Composition with skin multi-target whitening and freckle-removing effects and preparation method thereof
CN117224419A (en) * 2023-11-14 2023-12-15 山东第一医科大学(山东省医学科学院) Application of sennoside C in preparing skin whitening and spot-fading skin care product and related product

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN117100640A (en) * 2023-08-23 2023-11-24 宁波伯通伟达生物医药有限公司 Composition with skin multi-target whitening and freckle-removing effects and preparation method thereof
CN117100640B (en) * 2023-08-23 2024-02-09 宁波伯通伟达生物医药有限公司 Composition with skin multi-target whitening and freckle-removing effects and preparation method thereof
CN117224419A (en) * 2023-11-14 2023-12-15 山东第一医科大学(山东省医学科学院) Application of sennoside C in preparing skin whitening and spot-fading skin care product and related product
CN117224419B (en) * 2023-11-14 2024-01-30 山东第一医科大学(山东省医学科学院) Application of sennoside C in preparing skin whitening and spot-fading skin care product and related product

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