CN117100640A - Composition with skin multi-target whitening and freckle-removing effects and preparation method thereof - Google Patents

Composition with skin multi-target whitening and freckle-removing effects and preparation method thereof Download PDF

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CN117100640A
CN117100640A CN202311075726.7A CN202311075726A CN117100640A CN 117100640 A CN117100640 A CN 117100640A CN 202311075726 A CN202311075726 A CN 202311075726A CN 117100640 A CN117100640 A CN 117100640A
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parts
skin
composition
whitening
test
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CN117100640B (en
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郑宇强
王婷婷
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Ningbo Botong Weida Biomedical Co ltd
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Ningbo Botong Weida Biomedical Co ltd
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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
    • A61K8/72Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/84Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions otherwise than those involving only carbon-carbon unsaturated bonds
    • A61K8/89Polysiloxanes
    • A61K8/891Polysiloxanes saturated, e.g. dimethicone, phenyl trimethicone, C24-C28 methicone or stearyl dimethicone
    • 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
    • A61K8/31Hydrocarbons
    • 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
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34Alcohols
    • A61K8/345Alcohols containing more than one hydroxy group
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K8/00Cosmetics or similar toiletry preparations
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    • 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
    • A61K8/49Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/494Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
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    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/4973Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom
    • A61K8/498Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom having 6-membered rings or their condensed derivatives, e.g. coumarin
    • 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
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K8/67Vitamins
    • A61K8/676Ascorbic acid, i.e. vitamin C
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K8/84Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions otherwise than those involving only carbon-carbon unsaturated bonds
    • A61K8/89Polysiloxanes
    • A61K8/891Polysiloxanes saturated, e.g. dimethicone, phenyl trimethicone, C24-C28 methicone or stearyl dimethicone
    • A61K8/894Polysiloxanes saturated, e.g. dimethicone, phenyl trimethicone, C24-C28 methicone or stearyl dimethicone modified by a polyoxyalkylene group, e.g. cetyl dimethicone copolyol
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    • 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
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    • A61K2800/40Chemical, physico-chemical or functional or structural properties of particular ingredients
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    • 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
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    • A61K2800/782Enzyme inhibitors; Enzyme antagonists

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Abstract

The invention belongs to the field of cosmetics, and particularly relates to a composition with skin multi-target whitening and freckle-removing effects and a preparation method thereof. The composition with the skin multi-target whitening and freckle-removing effects is prepared from the following raw materials in parts by weight: 5 to 20 parts of nicotinamide, 0.5 to 4 parts of alpha-arbutin, 1 to 7 parts of tranexamic acid, 0.5 to 4 parts of hydroxyethyl piperazine ethane sulfonic acid, 0.1 to 4 parts of ascorbyl tetraisopalmitate, 0.5 to 4 parts of nano-coated glabridin, 1 to 10 parts of polydimethylsiloxane, 0.5 to 4 parts of phenyl trimethicone, 0.5 to 4 parts of bis-PEG-15 methyl ether polydimethylsiloxane, 0.05 to 2 parts of caprylyl glycol, 1 to 6 parts of isohexadecane, 0.5 to 5 parts of cetylstearyl olivate and 40 to 80 parts of purified water. The composition performs whitening link design from different stages of generation, inhibition, transportation, metabolism and the like of melanocytes, has multi-target whitening and spot-fading effects, can efficiently whiten and lighten skin, and has no toxicity to skin.

Description

Composition with skin multi-target whitening and freckle-removing effects and preparation method thereof
Technical Field
The invention belongs to the field of cosmetics, and particularly relates to a composition with skin multi-target whitening and freckle-removing effects and a preparation method thereof.
Background
Pigmentation is a common skin problem that becomes more pronounced with age, affecting appearance and quality of life to a great extent, and smooth, white and shiny skin is an important sign of aesthetic assessment, particularly in some countries of asia. Whereas acne, trauma, chemical stripping or laser treatment of inflammation may leave pigmentation behind. Wherein, the irradiation of ultraviolet rays is an important cause of pigments such as chloasma, sunburn, freckle and the like.
In the past, the difficulty of treating acquired (acquired) pigmentation disorders has been great, often without achieving the desired effect. Chinese patent application CN110974720a discloses a whitening and skin brightening composition, which comprises the following components in parts by weight: 0.1 to 1.5 parts of hydroxytyrosol, 0.1 to 1.5 parts of tranexamic acid, 0.1 to 3.0 parts of nicotinamide, 0.01 to 2.0 parts of carnosine and 0.01 to 1.0 part of encapsulated salicylic acid. However, it only exerts a whitening effect from one aspect, has a weak whitening and spot-lightening effect on skin, and requires the simultaneous use of other whitening products.
In addition, many of the whitening products currently on the market are irritating to the skin, sticky feel is generated after the whitening products are coated on the skin, the whitening mechanism is unknown, the effectiveness is low, and the whitening products need to be used regularly for several months continuously to have some effects. Meanwhile, ultraviolet rays are required to be avoided in the process of using the whitening agent, high-power (SPF) sun cream is used, the steps are extremely complicated, and the whitening effect is unstable.
Disclosure of Invention
Based on the technical background, aiming at the situation that modern urban females have continuous pursuit of skin whitening, but the existing skin whitening agent has an unknown technical mechanism and low effectiveness, the invention provides a composition with skin multi-target spot whitening and spot fading effects and a preparation method thereof. The composition can also solve the problem that most whitening combinations are poor in stability in different systems because of incompatibilities of raw material characteristics. Meanwhile, the composition has no light toxicity to skin, can be quickly absorbed by the skin after being coated on the skin, and is fresh and free of sticky feel.
The first aspect of the invention provides a composition with skin multi-target whitening and spot-fading effects, which is prepared from the following raw materials in parts by weight:
preferably, the composition is prepared from the following raw materials in parts by weight:
more preferably, the composition is prepared from the following raw materials in parts by weight:
in a second aspect, the present invention provides a method for preparing the composition with skin multi-target whitening and spot-lightening effects according to the first aspect, the method comprising the following steps:
step 1, heating isohexadecane under the stirring condition, and then preserving heat until the isohexadecane is completely melted to obtain a material A;
step 2, under the condition of stirring, placing cetostearyl alcohol olive oleate, polydimethylsiloxane, phenyl trimethicone and bis-PEG-15 methyl ether polydimethylsiloxane into purified water, heating and preserving heat until the materials are completely dissolved to obtain a material B;
and 3, after heating, slowly adding the material A into the material B, stirring to be emulsion, then cooling, adding nicotinamide, alpha-arbutin, tranexamic acid, hydroxyethyl piperazine ethane sulfonic acid, ascorbyl tetraisopalmitate and nano-coated glabridin and octaethylene glycol into the mixture, stirring until the system is milky white liquid, and aging at room temperature to obtain the composition with the skin multi-target whitening and freckle-fading effects.
Preferably, in the step 1, the isohexadecane is heated to 50-70 ℃ and is kept for 0.5-2 h.
Preferably, in the step 2, the temperature is raised to 45-60 ℃, the temperature is kept for 0.3-1.5 h, and then the temperature is lowered to 35-45 ℃.
Preferably, in the step 3, the temperature is raised to 50-65 ℃, the material A is slowly added into the material B, stirred for 0.5-2 h, and then cooled to 35-45 ℃.
Stirring for 0.2-2 h until the system is milky white liquid.
Aging for 10-25 h at room temperature.
The invention has the beneficial effects that:
(1) The combination of the polydimethylsiloxane, the phenyl trimethicone and the bis-PEG-15 methyl ether polydimethylsiloxane in the composition can play a role in increasing the smoothness and reducing the viscosity, and improve the sticky and greasy skin feel of the whitening and freckle-removing composition mainly comprising high-concentration nicotinamide. Nicotinamide is a general whitening agent which can achieve a whitening effect by inhibiting the transport of melanin, and is mild and not allergic to most people, so that it is widely used in cosmetics. However, high concentrations of nicotinamide give very sticky skin feel and reduced spreadability can also lead to skin allergies which are not applicable in cosmetics. The invention solves the problem of sticky skin feel caused by high-concentration nicotinamide, improves the refreshing skin feel of the application system product, and can be absorbed by skin quickly when being coated on the skin surface; the details are as follows:
in a plurality of experiments, the methyl siloxane composition composed of the polydimethylsiloxane, the phenyl trimethyl polysiloxane and the bis-PEG-15 methyl ether dimethyl siloxane in the composition can not only relieve the sticky feel of cream skin care products, but also eliminate the sticky feel of polyamino application system products mainly containing high-concentration nicotinamide within 3-5 minutes after the application of the skin, and can also obviously improve the irritation reaction of the residual nicotinic acid brought by the production process to the skin, but also avoid wrapping the whitening and freckle-fading properties of whitening and freckle-fading active substances.
(2) The invention creatively detects that the skin whitening needs to be performed by all paths and multiple targets, and the whitening effect of single target effect is weak, and the skin is easy to turn black, and the main reasons for blackening and darkening of the skin are the generation, transportation and deposition of melanin. First, three factors affecting melanin synthesis are tyrosinase inhibitors, signaling pathways, and tyrosine-related protein-2, respectively. Since tyrosinase is a key enzyme for synthesizing melanin through melanin production, tyrosinase becomes the most critical target for directly inhibiting melanin production inhibitors, including the use of copper ion complexing agents or inhibition of catalytic activity by binding to the active moiety of tyrosinase copper ion; competitive inhibition is achieved with substances similar to tyrosinase or the structure of the polybar. Secondly, the regulation of the melanin metabolic pathways, the melanocyte signaling pathway is affected by a variety of cytokines, such as basic fibroblast growth factor (bFGF) and endothelin-1 (ET-1), which affect melanocyte proliferation and pigmentation, and may stimulate tyrosinase activity, which highly color melanocytes. Another important exogenous factor is ultraviolet light and active oxygen, both of which affect the physiological process of melanin formation. After melanin production, melanocytes transport melanin granules to basal cells and acanthocytes via dendrites. After melanin production, it is transferred to the stratum corneum where it is deposited, and the skin "darkens" and these also fall off with the metabolism of the stratum corneum.
The invention skillfully combines different whitening and freckle-removing mechanisms and whitening agents with different action targets, not only simply obtains simple material superposition, but also plays roles around the mechanism of melanin generation and the regulation and control of a signal transduction pathway, and the full-link action whitens.
(3) According to the invention, different whitening agents are needed for detecting different whitening targets, and the whitening link design is carried out from different stages of generation, inhibition, transportation and metabolism of melanocytes: 1. intracellular inhibition of melanocytes: the activity of tyrosinase is inhibited by arbutin and glycyrrhiza glabra, the synthesis of melanin is reduced, and the deposition amount of melanin on skin is reduced. The VC-IP (ascorbate tetraisopalmitate) is used for reducing the melanin intermediate, scavenging oxygen free radicals, reducing the stimulation of the free radicals on melanocytes and reducing the generation of melanocytes. 2. Extracellular inhibition of melanocytes: modulation of melanin by paracrine factors is reduced by tranexamic acid (tranexamic acid), thereby reducing melanin synthesis. 3. Inhibiting melanin transport: the nicotinamide is used for blocking the melanin transmission path, inhibiting the transfer of melanosomes and reducing the melanin content of epidermal cells. 4. Accelerating melanin metabolism: HEPES (hydroxyethylpiperazine ethane sulfonic acid) is used for promoting metabolism of keratinocytes, accelerating exfoliation of pigmented keratinocytes, and reducing pigmentation on skin epidermis. Therefore, the skin-whitening and freckle-removing cream has the effects of multi-target whitening and freckle-removing, has the effects of high-efficiency whitening and skin-brightening, and has no toxicity to skin.
Drawings
FIG. 1 is a bar graph showing the inhibition effect of a methylsiloxane composition comprising polydimethylsiloxane, phenyl trimethicone, bis-PEG-15 methyl ether polydimethylsiloxane on greasy feel of oil and glycerin;
FIG. 2 is a bar graph showing the results of skin gloss difference tests before and after use of the composition with skin multi-target whitening and spot-lightening efficacy according to the present invention;
FIG. 3 is a bar graph showing the results of melanin MI value difference testing at various time points after use of the compositions of the present invention;
fig. 4 shows a bar graph of the results of skin brightness L x value difference tests at various time points after use of the composition according to the invention;
fig. 5 shows a bar graph of the results of skin color a difference measurements at various time points after application of the composition according to the invention;
fig. 6 shows a bar graph of skin color b x value difference test results after 14 days using the composition of the present invention;
figure 7 shows a bar graph of the results of the ITA deg. value difference test at various time points after use of the composition according to the invention.
Detailed Description
The features and advantages of the present invention will become more apparent and evident from the following detailed description of the invention.
The first aspect of the invention provides a composition with skin multi-target whitening and spot-fading effects, which is prepared from the following raw materials in parts by weight:
preferably, the composition is prepared from the following raw materials in parts by weight:
more preferably, the composition is prepared from the following raw materials in parts by weight:
when the amount of each raw material in the composition is in the above range, the composition can not only play a role in whitening and lightening spots, but also can not cause skin allergy. The methyl siloxane composition composed of the polydimethylsiloxane, the phenyl trimethyl polysiloxane and the bis-PEG-15 methyl ether dimethyl polysiloxane in the composition can inhibit the sticky feel and has obvious viscosity reducing effect.
Nicotinamide is a water-soluble vitamin, and can be used for preventing and treating nicotinic acid deficiency, brown leather disease, stomatitis, glossitis, sick sinus syndrome, atrioventricular block, etc.
Alpha-arbutin is a novel whitening raw material. Alpha-arbutin can be quickly absorbed by skin, and tyrosinase activity is selectively inhibited, so that melanin synthesis is blocked, but normal growth of epidermal cells is not affected, and self-expression of tyrosinase is not inhibited. Meanwhile, the alpha-arbutin can promote the decomposition and excretion of melanin, thereby avoiding the deposition of skin pigment and eliminating the color spots and freckles. The alpha-arbutin can not produce hydroquinone in the action process, and can not produce toxic and irritant side effects such as allergy and the like on skin.
The main effect of tranexamic acid on the skin is to whiten and lighten spots. The tranexamic acid is named as tranexamic acid, and the tranexamic acid can quickly whiten and lighten spots, so that the skin presents a white, soft, bright and transparent perfect skin and has a stable effect.
The hydroxyethyl piperazine ethane sulfonic acid has a certain effect of softening cutin and has the effect of assisting whitening; in cosmetics, it is a kind of hydrogen ion buffering agent, and can be controlled in stable pH range for a long time.
The ascorbyl tetraisopalmitate, the alias fat-soluble vitamin C, which mainly comprises vitamin C derivatives, can inhibit the activity of tyrosinase, is mainly used as an antioxidant and a humectant in cosmetics and skin care products, has the effects of whitening and removing spots, has a risk factor of 1, is safer, is suitable for pregnant women, and has no acne.
The nano-coated glabridin has strong whitening effect, is praised as whitening gold, can eliminate free radicals and myobasal melanin, and is a whitening and anti-aging holy thing of skin.
The polydimethylsiloxane is nontoxic and odorless, has physiological inertia, good chemical stability, good electrical insulation, weather resistance and hydrophobicity, and has very high shearing resistance, and can be used for a long time at-50-200 ℃.
Phenyl trimethicone has excellent film forming, lubricating, antistatic, dispersing and adsorbing properties.
bis-PEG-15 methyl ether polydimethylsiloxane as a surfactant and emulsifier can help regulate the viscosity and texture of the product in cosmetics, making it easier to push and spread. It also provides moisturizing effect, giving the skin a soft and smooth feel. The effect of this ingredient on the skin is relatively mild and beneficial.
The octaethylene glycol has the property of conditioning skin and hair, and is mainly used as a skin conditioner, a hair conditioner, a humectant and a preservative in cosmetics.
Isohexadecane is used in cosmetics as a emollient and solvent to add texture to the product, is insoluble in water, and forms a barrier to water loss on the skin like paraffin wax. Meanwhile, the isohexadecane is easy to biodegrade, has no residual feel, fresh and cool skin feel and stable property, has silky and smooth skin feel, and is suitable for skin care and sun protection products. Because of the multi-branched structure, the spreadability is obviously increased, the water retention is good, the product is more fresh and cool than the skin feel of the product using paraffin oil, the greasy feel of cream and emulsion products is greatly reduced, the cream and emulsion is especially suitable for water-in-oil systems, the chemical reactivity of isocetyl acid is extremely low, the stability is better, and the compatibility is extremely good.
The cetyl stearyl olive oleate is mainly used as an emulsifier in cosmetics and skin care products, has a risk factor of 1, is safer, can be used safely, has no influence on pregnant women generally, and has no acne-causing property.
In a second aspect, the present invention provides a method for preparing the composition with skin multi-target whitening and spot-lightening effects according to the first aspect, the method comprising the following steps:
step 1, heating isohexadecane under the stirring condition, and then preserving heat until the isohexadecane is completely melted to obtain a material A;
step 2, under the condition of stirring, placing cetostearyl alcohol olive oleate, polydimethylsiloxane, phenyl trimethicone and bis-PEG-15 methyl ether polydimethylsiloxane into purified water, heating and preserving heat until the materials are completely dissolved to obtain a material B;
and 3, after heating, slowly adding the material A into the material B, stirring to be emulsion, then cooling, adding nicotinamide, alpha-arbutin, tranexamic acid, hydroxyethyl piperazine ethane sulfonic acid, ascorbyl tetraisopalmitate and nano-coated glabridin and octaethylene glycol into the mixture, stirring until the system is milky white liquid, and aging at room temperature to obtain the composition with the skin multi-target whitening and freckle-fading effects.
The above steps are specifically described below.
In step 1, the stirring speed is 10 to 15r/min, preferably 15r/min.
Heating the isohexadecane to 50-70 ℃, and preserving heat for 0.5-2 h; preferably, the temperature is raised to 60-65 ℃ and the heat preservation is carried out for 0.5-1 h.
In step 2, the stirring speed is 30 to 45r/min, preferably 40r/min.
Heating to 45-60 ℃, preserving heat for 0.3-1.5 h, and then cooling to 35-45 ℃; preferably, the temperature is raised to 45-55 ℃, the temperature is kept for 0.5-1 h, and then the temperature is lowered to 40-45 ℃.
In the step 3, the temperature is raised to 50-65 ℃, the material A is slowly added into the material B, stirred for 0.5-2 h, and then cooled to 35-45 ℃.
The stirring speed is 50-60 r/min, preferably 55r/min.
Preferably, the temperature is raised to 55-60 ℃, the material A is slowly added into the material B, stirred for 0.5-1 h, and then cooled to 40-45 ℃.
Stirring for 0.2-2 h until the system is in a milky liquid, and stirring for 0.5-1 h until the system is in a milky liquid.
Aging for 10-25 h at room temperature, preferably 15-20 h at room temperature.
Examples
The invention is further illustrated by the following specific examples, which are intended to be illustrative of the invention and are not intended to limit the scope of the invention.
Example 1
The weight amounts of niacinamide 12 parts, alpha-arbutin 2 parts, tranexamic acid 4 parts, hydroxyethyl piperazine ethane sulfonic acid 2 parts, ascorbyl tetraisopalmitate 2 parts, nano-coated glabridin 2 parts, polydimethylsiloxane 6 parts, phenyl trimethicone 2 parts, bis-PEG-15 methyl ether polydimethylsiloxane 2 parts, octyl glycol 0.5 parts, isohexadecane 4 parts, cetostearyl oleate 2 parts, and purified water 60 parts were measured.
And (3) under the stirring speed of 15r/min, pouring the weighed isohexadecane into an oil phase pot, heating to 60 ℃, and preserving heat for 1h until the isohexadecane is completely melted to obtain a material A.
And (3) placing the weighed cetyl stearyl oleate, polydimethylsiloxane, phenyl trimethicone and bis-PEG-15 methyl ether polydimethylsiloxane into purified water at a stirring speed of 40r/min, heating to 50 ℃ and preserving heat for 1h until the cetyl stearyl oleate, polydimethylsiloxane, phenyl trimethicone and bis-PEG-15 methyl ether polydimethylsiloxane are completely dissolved in the purified water, and then cooling to 40 ℃ to obtain the material B.
Heating to 60 ℃ at a stirring speed of 55r/min, slowly adding the material A into the material B under the heat preservation condition, stirring for 1h until the system is emulsion, then cooling to 40 ℃, adding nicotinamide, alpha-arbutin, tranexamic acid, hydroxyethylpiperazine ethane sulfonic acid, ascorbyl tetraisopalmitate, nano-coated glabridin and octanediol into the system at a temperature of 40 ℃ and stirring for 1h until the system is milk white liquid, and then aging for 20h at room temperature to obtain the composition with the skin multi-target whitening and spot-lightening effects.
Example 2
The preparation of a composition with skin multi-target whitening and spot-lightening efficacy was carried out in a similar manner to example 1, except that: the weight amounts of nicotinamide 10 parts, alpha-arbutin 1 part, tranexamic acid 2 parts, hydroxyethyl piperazine ethane sulfonic acid 1 part, ascorbyl tetraisopalmitate 0.5 part, nano-coated glabridin 1 part, polydimethylsiloxane 2 parts, phenyl trimethicone 1 part, bis-PEG-15 methyl ether polydimethylsiloxane 1 part, caprylyl glycol 0.1 part, isohexadecane 3 parts, cetylstearyl oleate 1 part, and purified water 75 parts were measured.
Example 3
The preparation of a composition with skin multi-target whitening and spot-lightening efficacy was carried out in a similar manner to example 1, except that: 15 parts of nicotinamide, 3 parts of alpha-arbutin, 5 parts of tranexamic acid, 3 parts of hydroxyethyl piperazine ethane sulfonic acid, 3 parts of ascorbyl tetraisopalmitate, 3 parts of nano-coated glabridin, 8 parts of polydimethylsiloxane, 3 parts of phenyl trimethicone, 3 parts of bis-PEG-15 methyl ether polydimethylsiloxane, 1 part of octaethylene glycol, 5 parts of isohexadecane, 3 parts of cetylstearyl olivetoate and 50 parts of purified water.
Comparative example
Comparative example 1
The preparation of a composition with skin multi-target whitening and spot-lightening efficacy was carried out in a similar manner to example 1, except that: the weight amounts of 21 parts of nicotinamide, 5 parts of alpha-arbutin, 8 parts of tranexamic acid, 5 parts of hydroxyethyl piperazine ethane sulfonic acid, 5 parts of ascorbyl tetraisopalmitate, 5 parts of nano-coated glabridin, 11 parts of polydimethylsiloxane, 5 parts of phenyl trimethicone, 5 parts of bis-PEG-15 methyl ether polydimethylsiloxane, 3 parts of octaethylene glycol, 7 parts of isohexadecane, 6 parts of cetostearyl olive oleate and 60 parts of purified water are measured.
Experimental example
Experimental example 1 sticky feeling suppression test
Mixing 6 parts of polydimethylsiloxane, 2 parts of phenyl trimethicone and 2 parts of bis-PEG-15 methyl ether polydimethylsiloxane to obtain a methyl siloxane composition, mixing the methyl siloxane composition with glycerin and grease respectively, wherein the addition amount of the methyl siloxane composition in the glycerin and grease is 0.5%, 1% and 2%, and the specific test method is as follows, wherein the glycerin and grease without methyl siloxane are used as a control group: the testing steps are as follows: 1. the containers containing the test samples (test group samples and control group samples) are placed in a constant-temperature water bath, the temperature is set to be 25 ℃, and the temperature is kept uniform. 2. The power supply of the viscometer is turned on, and the power supply is zeroed. 3. And selecting a rotor 3, wherein the rotating speed is 30 revolutions. 4. The rotor was mounted to a viscometer and lowered into the sample, immersed in the spindle at the scribe line position, placed in the center of the cup and the test was started. 5. And stably reading the numerical value by the reading, and recording data. The test results are shown in FIG. 1.
As can be seen from FIG. 1, compared with the blank control group, the methyl siloxane composition has obvious viscosity reducing effect on glycerin and grease.
Experimental example 2 efficacy test
(1) Test group: the test product is the composition with skin multi-target whitening and freckle fading effects, which is prepared in the example 1;
blank (blank control): no skin care product is used;
the using method comprises the following steps: after face cleaning, a proper amount of the product prepared in the embodiment 1 is smeared on the face and the neck, and the product is tapped until being absorbed;
test part: forehead and cheek.
(2) Test purpose: at least 30 subjects meeting the criteria were recruited and the results of the product of example 1 on improving skin pigmentation, skin lightening, lightening efficacy, etc. were tested by the instrument using the test product.
(3) The test method is based on: the tests were carried out according to the "cosmetic pigmentation improvement efficacy test method", the "cosmetic skin gloss improvement efficacy test method" and the "cosmetic lightening efficacy test method".
(4) Test instrument: skin elasticity tester MPA580 (self-contained elasticity and grease probe, corneometer probe, colorimeter probe, mexameter probe, cutometer probe, glossemeter probe), skin surface texture analysis System Visioscan VC20plus, analytical balance.
(5) The test indexes are as follows: efficacy tests are shown in table 1.
TABLE 1 efficacy test
(6) Data statistics:
statistical analysis of the data was performed using statistical analysis software. The metering data are expressed as: the mean value is +/-standard deviation, normal distribution inspection is carried out, normal distribution requirements are met, paired t inspection is adopted for comparison before and after use, and otherwise, two related sample rank sum inspection is adopted; comparing the grade data before and after use, and adopting two related sample ranks and tests; comparison between test product and control group used independent sample t-test or rank-sum test. The above statistical analysis was a two-tailed test with a significance level of α=0.05.
(7) The testing process comprises the following steps: as shown in table 2.
TABLE 2
(8) Test results:
8.1 skin gloss test results are shown in table 3:
TABLE 3 results of skin gloss at various time points (mean.+ -. Standard deviation)
Group of Before use (D0) After 14 days of application of the product (D14) After 28 days of application of the product (D28)
Test sample 8.16±1.10 11.67±2.78 11.63±2.41
Blank control 8.25±1.29 8.61±1.60 8.23±1.27
The skin gloss change rate is shown in table 4 and fig. 2:
TABLE 4 Table 4
Group of After 14 days of application of the product (D14) After 28 days of application of the product (D28)
Test sample 43.01% 42.52%
Blank control 4.36% -0.24%
The skin gloss difference test results of the test products before and after use are shown in table 5:
TABLE 5
Note that: "n.s." means no statistical difference, P > 0.05; "represents a significant difference, P0.01.ltoreq.p < 0.05; "X" indicates that there is a very significant difference, 0.001.ltoreq.P < 0.01; ", P < 0.001 indicates a very significant difference. "N" means the number of users=30.
As can be seen from tables 3-5 and fig. 2, the skin gloss difference in the test product area of the subjects was very significantly different from that in the blank area using the test product for 14 days, and the change rate in the test product area was 43.01%. The skin gloss difference in the test product area of the subject was significantly different from that in the blank area for 28 days using the test product, and the change rate in the test product area was 42.52%, indicating that the composition of the present invention can improve skin gloss in a short period of time.
8.2 melanin MI values test results are shown in Table 6:
TABLE 6
Group of Before use (D0) After 14 days of application of the product (D14) After 28 days of application of the product (D28)
Test sample 158.08±33.52 132.01±36.32 128.80±29.66
Blank control 156.41±35.71 152.84±38.64 156.93±32.76
The rate of change of the MI values of melanin is shown in Table 7 and FIG. 3:
TABLE 7
Group of After 14 days of application of the product (D14) After 28 days of application of the product (D28)
Test sample -16.49% -18.52%
Blank control -2.28% 0.33%
The melanin MI value difference test results are shown in Table 8:
TABLE 8
Note that: "n.s." means no statistical difference, P > 0.05; "represents a significant difference, P0.01.ltoreq.p < 0.05; "X" indicates that there is a very significant difference, 0.001.ltoreq.P < 0.01; ", P < 0.001 indicates a very significant difference. "N" means the number of users=30.
As can be seen from tables 6-8 and fig. 3, the test product area of the subjects showed a very significant difference in melanin MI difference from the blank area for 14 days of continuous use of the test product, and the test product area variation rate was-16.49%. The test product is continuously used for 28 days, the MI difference of melanin in the test product area of a subject is extremely obviously different from that of a blank control area, and the change rate of the test product area is-18.52%, so that the composition can inhibit melanin deposition in a short time and improve the whiteness.
8.3 skin brightness L values test results are shown in table 9:
table 9 skin brightness L data (mean ± standard deviation) at different time points
Group of Before use (D0) After 14 days of application of the product (D14) After 28 days of application of the product (D28)
Test sample 61.26±2.80 63.10±2.52 63.62±2.67
Blank control 61.39±2.68 61.42±2.56 61.90±2.75
The skin brightness L x value change rate test results are shown in table 10 and fig. 4:
table 10
Group of After 14 days of application of the product (D14) After 28 days of application of the product (D28)
Test sample 3.00% 3.85%
Blank control 0.05% 0.83%
The skin brightness L-value difference test results are shown in table 11:
TABLE 11
Note that: "n.s." means no statistical difference, P > 0.05; "represents a significant difference, P0.01.ltoreq.p < 0.05; "X" indicates that there is a very significant difference, 0.001.ltoreq.P < 0.01; ", P < 0.001 indicates a very significant difference. "N" means the number of users=30.
As can be seen from tables 9-11 and fig. 4, the skin brightness difference in the test product area of the subjects was very significantly different from that in the blank area for 14 days of continuous use of the test product, and the change rate in the test product area was 3.00%. The test product was used for 28 days continuously, and the difference in skin brightness L values in the test product area of the subject was very significantly different from that in the blank area, and the change rate in the test product area was 3.85%, indicating that the composition of the present invention can improve skin brightness.
8.4 skin color a value test results are shown in table 12:
table 12 skin color a test data at various time points
Group of Before use (D0) After 14 days of application of the product (D14) After 28 days of application of the product (D28)
Test sample 13.06±1.41 12.12±1.39 11.58±1.96
Blank control 13.01±1.39 13.01±1.33 12.38±1.25
The rate of change of the skin color a values is shown in table 13 and fig. 5:
TABLE 13
Group of After 14 days of application of the product (D14) After 28 days of application of the product (D28)
Test sample -7.20% -11.33%
Blank control 0.00% -4.84%
Skin color a differential test results are shown in table 14:
TABLE 14
Note that: "n.s." means no statistical difference, P > 0.05; "represents a significant difference, P0.01.ltoreq.p < 0.05; "X" indicates that there is a very significant difference, 0.001.ltoreq.P < 0.01; ", P < 0.001 indicates a very significant difference. "N" means the number of users=30.
As can be seen from tables 12-14 and fig. 5, the skin color a values of the test product areas of the subjects were significantly different from those of the blank areas for 14 days of continuous use of the test product, and the rate of change of the test product areas was-7.20%. The test product was used continuously for 28 days, and the difference of the skin color a values of the test product areas of the subjects was significantly different from that of the blank control areas, and the change rate of the test product areas was-11.33%, which indicates that the composition of the invention has significant whitening efficacy.
8.5 skin color b value test results are shown in table 15:
table 15 test data for skin colour b values at different time points
Group of Before use (D0) After 14 days of application of the product (D14)
Test sample 14.29±2.05 13.90±1.93
The rate of change of the skin color b values is shown in table 16:
table 16
Group of After 14 days of application of the product (D14)
Test sample -2.73%
Skin color b value difference test results are shown in table 17 and fig. 6:
TABLE 17
Note that: "n.s." means no statistical difference, P > 0.05; "represents a significant difference, P0.01.ltoreq.p < 0.05; "X" indicates that there is a very significant difference, 0.001.ltoreq.P < 0.01; ", P < 0.001 indicates a very significant difference. "N" means the number of users=30.
As can be seen from tables 15-17 and fig. 6, the skin color b values of the test product areas of the subjects were significantly different from the blank areas after 14 days of continuous use of the test product, and the rate of change of the test product areas was-2.73%.
8.6ITA value (skin brightness) test results
Test data for various time points for ITA ° values are shown in table 18:
TABLE 18
Group of Before use (D0) After 14 days of application of the product (D14) After 28 days of application of the product (D28)
Test sample 37.91±7.88 43.13±6.84 43.52±6.72
Blank control 38.77±7.69 38.76±7.63 39.16±7.61
The ita° value change rate is shown in table 19 and fig. 7:
TABLE 19
Group of After 14 days of application of the product (D14) After 28 days of application of the product (D28)
Test sample 13.77% 14.80%
Blank control -0.03% 1.01%
The ita° value difference test results are shown in table 20:
table 20
Note that: "n.s." means no statistical difference, P > 0.05; "represents a significant difference, P0.01.ltoreq.p < 0.05; "X" indicates that there is a very significant difference, 0.001.ltoreq.P < 0.01; ", P < 0.001 indicates a very significant difference. "N" means the number of users=30.
As can be seen from tables 18-20 and fig. 7, the test sample areas of the subjects were tested for 14 days with a very significant difference in ITA ° difference from the blank area, and the test sample area variation rate was 13.77%. The test product was used continuously for 28 days, and the ITA degree difference of the test sample area of the subject was very significantly different from that of the blank control area, and the change rate of the test sample area was 14.80%, which indicates that the composition of the invention can effectively improve skin brightness.
Experimental example 3 skin phototoxicity test
(1) Test group product: the composition with the skin multi-target whitening and freckle-fading effects prepared in the example 1 is white emulsion;
control group products: 8-methoxy fructus Psoraleae, lot number: p1624916, manufacturer: adamas-beta. The solvent is corn oil. The product concentration was 0.05g/mL. The dosage is as follows: 0.2mL was used in the test area.
(2) Experimental animals and feeding environment:
experimental animals: hartley guinea pigs, grade: common stage, number: test group 6 (male and female halves), control group 6 (male and female halves). Weight of: 200g-300g. The source is as follows: the experimental animal fine-breed field limited company in the Songjiang area of Shanghai city. Experimental animal production license number: SCXK (Shanghai) 2022-0001, quality certificate number: 20220001000733.
feeding environment: temperature: 20-26 ℃, relative humidity: 40% -70% of experimental animal environment use license number: SYXK (Shanghai) 2022-0005.
Feed information: and (3) feed sources: the feed qualification is proved by the Xiaohe science and technology development limited company in the city of the third party: QC20230505201401.
Instrument: manufacturing factories of light source instruments: tianjin development district is combined with general industry and trade company, model: HOPE-MED 8130C.
(3) The test methods for the test group and the control group were as follows:
determination of light intensity: the back irradiation area of the experimental animal was set with 6 points of test light intensity (mW/cm) before skin phototoxicity test 2 ) Calculated as an average. Under the experimental conditions, the average value of the light intensity is measuredAbout 6.150mW/cm 2
Calculation of irradiation time: the irradiation dose was 10J/cm 2 The calculation is performed according to the following formula:
irradiation time (sec) =irradiation dose (10000 mJ/cm) 2 ) Light intensity (mJ/cm 2/sec).
The irradiation time was calculated to be 1626 seconds under the present experimental conditions.
Animals are acclimatized in the laboratory for at least 3d-5d time prior to testing.
The skin on two sides of the animal backbone is dehaired 18-24 hours before the formal phototoxicity test, and the skin on the test part needs to be intact and free from damage and abnormality. According to the cosmetic safety Specification (2015 edition) (hereinafter, abbreviated as Specification) P501 FIG. 1, 4 zones of dehairing were prepared, each zone having a dehairing area of about 2cm. Times.2 cm. Animals were fixed, 0.2mL of test product was applied to animal dehairing areas 1 and 2 as shown in table 1 of code P501, after 30min, the left side (dehairing areas 1 and 3) was covered with aluminum foil, tape fixed, and the right side (dehairing areas 2 and 4) was irradiated with UVA.
Skin reactions were observed at 1, 24, 48 and 72h, respectively, after the end, and skin reaction scores were determined for each animal according to the specifications P501-P502, table 2. And judging that the test product has phototoxicity when only the test product is coated and the non-irradiated area has no skin reaction, and the sum of the skin reaction scores of the irradiated area after the test product is coated is 2 or more and the number of animals which is more than 2 is 1 or more.
(4) Test results: the test results of the control group and the test group are shown in tables 21 and 22, respectively;
table 21 results of skin phototoxicity test of guinea pigs in control group
Table 22 results of the skin phototoxicity test of guinea pigs of the test group
Note that: the heads 1, 2, 3 and 4 are test areas shown in figure 1 of the skin phototoxicity test in chapter 7 of cosmetic safety Specification (2015).
From tables 21 and 22, the test results of the test groups show that the composition with the skin multi-target whitening and spot-fading effects disclosed by the invention has no phototoxicity to the skin, and is safe to use.
The invention has been described in detail in connection with the specific embodiments and exemplary examples thereof, but such description is not to be construed as limiting the invention. It will be understood by those skilled in the art that various equivalent substitutions, modifications or improvements may be made to the technical solution of the present invention and its embodiments without departing from the spirit and scope of the present invention, and these fall within the scope of the present invention. The scope of the invention is defined by the appended claims.

Claims (9)

1. The composition with the skin multi-target whitening and freckle-removing effects is characterized by being prepared from the following raw materials in parts by weight:
2. the composition with the skin multi-target whitening and spot-fading effects according to claim 1, wherein the composition is prepared from the following raw materials in parts by weight:
3. the composition with the skin multi-target whitening and spot-fading effects according to claim 2, wherein the composition is prepared from the following raw materials in parts by weight:
4. a method for preparing the composition with skin multi-target whitening and spot-lightening efficacy according to any one of claims 1 to 3, characterized in that the method comprises the following steps:
step 1, heating isohexadecane under the stirring condition, and then preserving heat until the isohexadecane is completely melted to obtain a material A;
step 2, under the condition of stirring, placing cetostearyl alcohol olive oleate, polydimethylsiloxane, phenyl trimethicone and bis-PEG-15 methyl ether polydimethylsiloxane into purified water, heating and preserving heat until the materials are completely dissolved to obtain a material B;
and 3, after heating, slowly adding the material A into the material B, stirring to be emulsion, then cooling, adding nicotinamide, alpha-arbutin, tranexamic acid, hydroxyethyl piperazine ethane sulfonic acid, ascorbyl tetraisopalmitate and nano-coated glabridin and octaethylene glycol into the mixture, stirring until the system is milky white liquid, and aging at room temperature to obtain the composition with the skin multi-target whitening and freckle-fading effects.
5. The method according to claim 4, wherein, in step 1,
heating the isohexadecane to 50-70 ℃, and preserving the heat for 0.5-2 h.
6. The method according to claim 4, wherein, in step 2,
heating to 45-60 ℃, preserving heat for 0.3-1.5 h, and then cooling to 35-45 ℃.
7. The method according to claim 4, wherein, in step 3,
heating to 50-65 ℃, slowly adding the material A into the material B, stirring for 0.5-2 h, and then cooling to 35-45 ℃.
8. The method according to claim 4, wherein, in step 3,
stirring for 0.2-2 h until the system is milky white liquid.
9. The method according to claim 4, wherein, in step 3,
aging for 10-25 h at room temperature.
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CN110101588A (en) * 2019-04-12 2019-08-09 广州市茗妍化妆品有限公司 A kind of whitening and spot-eliminating composition and its shin moisturizer and preparation method
CN111265445A (en) * 2020-03-25 2020-06-12 配方化妆品科技(广州)有限公司 Light sensation whitening essence and preparation method thereof
CN114588068A (en) * 2022-03-29 2022-06-07 上海新高姿化妆品有限公司 Composition with skin whitening and spot lightening effects
CN115154383A (en) * 2022-07-08 2022-10-11 泉后(广州)生物科技研究院有限公司 Mild whitening composition and whitening cream thereof
CN115227608A (en) * 2022-05-09 2022-10-25 广州妍医生物科技有限公司 Repair moisturizing spray and preparation method thereof
CN116407462A (en) * 2023-01-19 2023-07-11 重庆富进生物医药有限公司 Whitening and freckle-removing composition and essence, cream and emulsion containing composition

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110101588A (en) * 2019-04-12 2019-08-09 广州市茗妍化妆品有限公司 A kind of whitening and spot-eliminating composition and its shin moisturizer and preparation method
CN111265445A (en) * 2020-03-25 2020-06-12 配方化妆品科技(广州)有限公司 Light sensation whitening essence and preparation method thereof
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