CN114569499B - Mild and efficient whitening composition and preparation method thereof - Google Patents
Mild and efficient whitening composition and preparation method thereof Download PDFInfo
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- CN114569499B CN114569499B CN202111339094.1A CN202111339094A CN114569499B CN 114569499 B CN114569499 B CN 114569499B CN 202111339094 A CN202111339094 A CN 202111339094A CN 114569499 B CN114569499 B CN 114569499B
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/92—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
- A61K8/922—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof of vegetable origin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/34—Alcohols
- A61K8/347—Phenols
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/55—Phosphorus compounds
- A61K8/553—Phospholipids, e.g. lecithin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/63—Steroids; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/67—Vitamins
- A61K8/678—Tocopherol, i.e. vitamin E
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
- A61Q19/02—Preparations for care of the skin for chemically bleaching or whitening the skin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/20—Chemical, physico-chemical or functional or structural properties of the composition as a whole
- A61K2800/30—Characterized by the absence of a particular group of ingredients
- A61K2800/33—Free of surfactant
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
- A61K2800/41—Particular ingredients further characterized by their size
- A61K2800/413—Nanosized, i.e. having sizes below 100 nm
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
- A61K2800/59—Mixtures
- A61K2800/592—Mixtures of compounds complementing their respective functions
- A61K2800/5922—At least two compounds being classified in the same subclass of A61K8/18
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/74—Biological properties of particular ingredients
- A61K2800/78—Enzyme modulators, e.g. Enzyme agonists
- A61K2800/782—Enzyme inhibitors; Enzyme antagonists
-
- Y—GENERAL 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
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Abstract
The invention discloses a mild and efficient whitening composition, which comprises the following preparation raw materials in parts by weight: 50-80 parts of water-soluble components, 5-10 parts of whitening agents, 7.5-25 parts of oil-soluble components and 10-30 parts of water. The invention adopts the synergistic combination of the phospholipid, the hydrogenated phosphatidylcholine and the 4-butylresorcinol to improve the problems of indissolvable and easy oxidative discoloration of the 4-butylresorcinol, so that the effective components are easier to be absorbed by skin, the whitening and spot-lightening effect is improved, and the combination of the cholest-5-ene-3 beta-ol, the alpha-tocopherol and the sunflower seed oil reduces the irritation of the 4-butylresorcinol to the skin, so that the mildness of the final product is greatly improved, and meanwhile, the liposome has good stability without surfactant by the combination of the phospholipid, the hydrogenated phosphatidylcholine and the cholest-5-ene-3 beta-ol, so that the use skin feel of the product is greatly improved, and the skin is fine and loose.
Description
Technical Field
The invention relates to a mild and efficient whitening composition, relates to A61K, and particularly relates to the field of cosmetic preparations.
Background
Whitening and freckle removing are always pursued effects of beauty lovers, skin darkening is that melanin generated by melanocytes is deposited into skin, and whitening products achieve whitening effects by inhibiting generation of melanin. Many whitening products are available on the market, but the whitening components have the defects of easy oxidative discoloration and unstable performance, and the high concentration of the whitening components can generate irritation to skin and influence the balance of the surface of the skin.
Chinese patent No. 201310414407.4 discloses a microcapsule composition coated with whitening liposome, which is prepared by coating whitening components, so that the stability of the whitening components is improved, and the irritation is reduced, but a surfactant is added in the preparation process, so that the product can generate dry hand feeling after being used, and the skin feel effect is poor. Chinese patent No. 201910083518.9 discloses a cream for removing freckle, whitening and resisting aging, which increases compatibility of whitening components and other components by adding retinol wrapped by liposome, but active components only can react on the surface of skin and are not easy to enter the skin substrate, so that the whitening and moisturizing effects are poor.
Disclosure of Invention
In order to improve the effect of the whitening composition on the skin and reduce the irritation to the skin, the first aspect of the invention provides a mild and efficient whitening composition, which is prepared from the following raw materials in parts by weight: 50-80 parts of water-soluble components, 5-10 parts of whitening agents, 7.5-25 parts of oil-soluble components and 10-30 parts of water.
As a preferred embodiment, the water-soluble component is glycerol.
As a preferred embodiment, the oil-soluble component is selected from one or a combination of several of phospholipids, choline, phosphoric acid, fatty acids, cholest-5-en-3 beta-ol, tocopherol, vegetable oil and fat.
As a preferred embodiment, the oil-soluble component comprises phospholipids, choline, cholest-5-en-3 beta-ol, tocopherol, vegetable oil and fat.
As a preferred embodiment, the phospholipid is selected from one or a combination of several of lecithin, soybean phospholipid, inositol phospholipid, cephalin and cardiolipin.
As a preferred embodiment, the phospholipid is lecithin.
As a preferred embodiment, the choline is selected from one or a combination of several of phosphorylcholine, acetylcholine, glycerophosphorylcholine, hydrogenated phosphatidylcholine, citicoline, glycerophosphorylcholine.
As a preferred embodiment, the choline is hydrogenated phosphatidylcholine.
As a preferred embodiment, the vegetable oil is selected from one or more of coconut oil, shea butter, jojoba oil, palm oil, almond oil, wheat germ oil, avocado oil, alglycerol, cactus oil, and sunflower seed oil.
As a preferred embodiment, the vegetable oil is sunflower seed oil.
As a preferred embodiment, the tocopherol is selected from one or a combination of several of alpha-tocopherol, beta-tocopherol, gamma-tocopherol and delta-tocopherol.
As a preferred embodiment, the tocopherol is α -tocopherol.
As a preferred embodiment, the whitening agent is selected from one or more of arbutin, licorice extract, phyllanthus emblica fruit extract, alkyl resorcinol, butyl resorcinol, hexyl resorcinol.
As a preferred embodiment, the whitening agent is butyl resorcinol, and more preferably, the whitening agent is 4-butyl resorcinol.
As a preferred embodiment, the preparation raw material further comprises 5-10 parts by weight of a thickener, preferably, the thickener is selected from one or a combination of several of xanthan gum, carbomer, glycerol oleate and high molecular cellulose.
As a preferred embodiment, the thickener is glycerol oleate.
As a preferred embodiment, the weight ratio of the phospholipid, choline and whitening agent is (5-10): (1-5): (5-10).
As a preferred embodiment, the weight ratio of the phospholipid, choline and whitening agent is (7-9): (1.5-3): (5-6).
As a preferred embodiment, the weight ratio of the phospholipid, the choline and the whitening agent is 8:2:5.
the applicant finds that the phospholipid, the hydrogenated phosphatidylcholine and the 4-butyl resorcinol are combined and compounded in the experimental process, so that the problems of indissolvable and easy discoloration of the 4-butyl resorcinol can be greatly improved, the 4-butyl resorcinol can be efficiently transferred to a dermis layer, and the effect of remarkably improving the skin state is generated. The possible reasons for the guess are: 4-butyl resorcinol is insoluble in aqueous solvent and is easy to oxidize and discolor, a layer of coating layer is formed on the surface of 4-butyl resorcinol by lecithin and hydrogenated phosphatidylcholine to isolate oxygen, and a fat-soluble surface is provided to generate liposome particles with the particle size of 55-60nm, so that the coated 4-butyl resorcinol can permeate into the muscle bottom more easily, inhibit the activity of tyrosinase, prevent the generation of melanin, and further achieve the effects of whitening and lightening spots.
As a preferred embodiment, the weight ratio of the cholest-5-en-3 beta-ol, the tocopherol and the vegetable oil and fat is (1-5): (0.1-1): (0.1-1).
As a preferred embodiment, the weight ratio of the cholest-5-en-3 beta-ol, the tocopherol and the vegetable oil and fat is (1.5-3): (0.3-0.8): (0.3-0.8).
As a preferred embodiment, the weight ratio of the cholest-5-en-3 beta-ol, the tocopherol and the vegetable oil and fat is 2:0.5:0.5.
the applicant further found that high concentrations of 4-butylresorcinol have a strong skin irritation, and that the use of low concentrations of 4-butylresorcinol has no significant effect on skin lightening and spot lightening, and that the combination of tocopherols and sunflower seed oil can effectively reduce the skin irritation of 4-butylresorcinol by the addition of cholesterol, presumably because: cholesterol, tocopherol and sunflower seed oil have synergistic effect similar to the components of skin cells, and reduce the specific reaction of the skin cells to 4-butylresorcinol, so that the mildness of the product is improved.
As a preferred embodiment, the whitening composition has a pH of 6.0 to 7.0 at 25 ℃ at a mass fraction of 1%.
The second aspect of the invention provides a method for preparing a mild and efficient whitening composition, which comprises the following steps:
(1) Mixing the oil-soluble component with the thickener, and stirring at 55-65deg.C to form phase A;
(2) Mixing water-soluble components, water and whitening agent at 55-65deg.C, and stirring to form phase B;
(3) Adding phase B into phase A, and homogenizing;
(4) Extruding the homogenized material obtained in the step 3 by using an ester extruder.
As a preferred embodiment, the liposome particle size obtained by the ester extruder is 55-60nm.
Compared with the prior art, the invention has the following beneficial effects:
(1) According to the mild and efficient whitening composition, the problems of indissolvable and easy oxidative discoloration of 4-butylresorcinol are solved by adopting the synergistic compounding of the phospholipid, the hydrogenated phosphatidylcholine and the 4-butylresorcinol, so that the active ingredients are easier to be absorbed by skin, and the whitening and freckle-removing effects are improved.
(2) According to the mild and efficient whitening composition, the irritation of 4-butyl resorcinol to skin is reduced by adopting the combination and compounding of cholest-5-ene-3 beta-alcohol, alpha-tocopherol and sunflower seed oil, so that the mildness of a final product is greatly improved.
(3) According to the mild and efficient whitening composition, the liposome has good stability through the compounding of the phospholipid, hydrogenated phosphatidylcholine and cholest-5-ene-3 beta-alcohol, and the whitening composition does not contain a surfactant, so that the skin feel of a product is greatly improved, and the skin is fine and smooth and is not tight.
Detailed Description
The present invention will be specifically described below by way of examples. It is noted herein that the following examples are given solely for the purpose of further illustration and are not to be construed as limitations on the scope of the invention, as will be apparent to those skilled in the art in light of the foregoing disclosure.
In addition, the raw materials used are commercially available unless otherwise indicated.
Example 1
A mild and efficient whitening composition is prepared from the following raw materials in parts by weight: 55 parts of glycerin, 5 parts of whitening agent, 13 parts of oil-soluble component, 20 parts of water and 6 parts of thickener.
The oil soluble components comprise lecithin, hydrogenated phosphatidylcholine, cholest-5-ene-3 beta-alcohol, alpha-tocopherol and sunflower seed oil, wherein the lecithin is purchased from Korean Fangshan group and has the model DS-SUN PC65;the hydrogenated phosphatidylcholine was purchased from the Korean Fangshan group under the model DS-Soya HPC90; the cholest-5-en-3β -ol was purchased from japan refinement corporation; the alpha-tocopherol is purchased from Royal Dissman company; the sunflower seed oil is available from Hallstar Inc., USA under the trade designationSunflower Oil REF。
The weight ratio of the cholest-5-alkene-3 beta-alcohol to the alpha-tocopherol to the sunflower seed oil is 2:0.5:0.5.
the whitening agent is 4-butyl resorcinol, and the weight ratio of lecithin, hydrogenated phosphatidylcholine and 4-butyl resorcinol is 8:2:5.
the thickener is glycerol oleate, available from Sanshi biotechnology Co.
The whitening composition has a pH value of 6.5 at 25 ℃ and a mass fraction of 1%.
A preparation method of a mild and efficient whitening composition comprises the following steps:
(1) Mixing the oil-soluble component with the thickener, and stirring at 55-65deg.C to form phase A;
(2) Mixing water-soluble components, water and whitening agent at 55-65deg.C, and stirring to form phase B;
(3) Adding phase B into phase A, and homogenizing;
(4) Extruding the homogenized material obtained in the step 3 by using an ester extruder.
The liposome particle size obtained by the ester extruder was 58.55nm.
Example 2
The specific steps of the mild and efficient whitening composition are the same as those of the embodiment 1, and the difference is that the weight ratio of the cholest-5-ene-3 beta-alcohol, alpha-tocopherol and sunflower seed oil is 0.8:1.2:1.5.
example 3
A mild and efficient whitening composition and a preparation method thereof are characterized in that the specific steps are the same as those of the embodiment 1, and the weight ratio of lecithin, hydrogenated phosphatidylcholine and 4-butylresorcinol is 4:1:8.
example 4
A commercially available whitening composition is different in that it comprises tween-20 with a mass fraction of 1.3% and span-80 with a mass fraction of 1.5%.
Performance testing
1. Stability test: the prepared composition is added into water to prepare an aqueous solution with the mass fraction of 5 percent, so as to form the limit stability condition. The precipitation time of the active ingredient in the composition was observed.
2. And (3) defoaming effect test: adding the prepared composition into water to prepare an aqueous solution with the mass fraction of 5%, vigorously shaking for 10-20min to generate bubbles, and observing the time required for the bubbles to disappear.
3. Skin absorption effect test: 30mg of the composition of examples 1-4 was applied to the backs of 50 volunteers, and after rubbed until absorbed, the skin surface feeling of the volunteers was inquired, and at least 48 volunteers considered that the skin feeling was smooth, fine and free from irritation, and marked as excellent; the number of the volunteers is more than 35 and less than 48, and the skin feel smooth, fine and smooth, and has no slight tight stimulus, and the skin feel is recorded as good; less than or equal to 35 volunteers think that the skin feel smooth, fine and smooth without tension and stimulus, and the skin feel bad.
Examples 1-4 were tested according to the criteria described above and the test results are shown in Table 1.
TABLE 1
Claims (4)
1. The mild and efficient whitening composition is characterized by comprising the following preparation raw materials in parts by weight: 50-80 parts of water-soluble components, 5-10 parts of whitening agents, 7.5-25 parts of oil-soluble components and 10-30 parts of water;
the oil-soluble components comprise phospholipid, choline, cholest-5-ene-3 beta-alcohol, tocopherol and vegetable oil;
the weight ratio of the phospholipid, the choline and the whitening agent is (7-9): (1.5-3): (5-6);
the phospholipid is lecithin;
the choline is hydrogenated phosphatidylcholine;
the whitening agent is 4-butyl resorcinol;
the weight ratio of the cholest-5-alkene-3 beta-alcohol to the tocopherol to the vegetable oil is 2:0.5:0.5;
the vegetable oil is sunflower seed oil.
2. The mild and high-potency whitening composition according to claim 1, wherein said tocopherol is selected from one or a combination of several of α -tocopherol, β -tocopherol, γ -tocopherol, δ -tocopherol.
3. The mild and high-efficient whitening composition according to claim 1, wherein the raw materials for preparing the whitening composition further comprise 5-10 parts by weight of a thickening agent selected from one or more of xanthan gum, carbomer, glycerol oleate and high-molecular cellulose.
4. A method of preparing the mild and high-efficiency whitening composition according to claim 3, comprising the steps of:
(1) Mixing the oil-soluble component with the thickener, and stirring at 55-65deg.C to form phase A;
(2) Mixing water-soluble components, water and whitening agent at 55-65deg.C, and stirring to form phase B;
(3) Adding phase B into phase A, and homogenizing;
(4) Extruding the homogenized material obtained in the step 3 by using an ester extruder.
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Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
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KR100827678B1 (en) * | 2006-12-19 | 2008-05-07 | 주식회사 동부하이텍 | 4-n-butylresorcinol complex, preparation and cosmetic composition containing as an active ingredient |
CN103432009A (en) * | 2013-09-12 | 2013-12-11 | 广东轻工职业技术学院 | Whitening agent liposome coating micro-capsule composition as well as preparation method and application thereof |
CN111658585A (en) * | 2020-06-24 | 2020-09-15 | 珠海美逸生物科技有限公司 | Whitening and spot-fading composition and preparation method thereof |
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Publication number | Priority date | Publication date | Assignee | Title |
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KR100827678B1 (en) * | 2006-12-19 | 2008-05-07 | 주식회사 동부하이텍 | 4-n-butylresorcinol complex, preparation and cosmetic composition containing as an active ingredient |
CN103432009A (en) * | 2013-09-12 | 2013-12-11 | 广东轻工职业技术学院 | Whitening agent liposome coating micro-capsule composition as well as preparation method and application thereof |
CN111658585A (en) * | 2020-06-24 | 2020-09-15 | 珠海美逸生物科技有限公司 | Whitening and spot-fading composition and preparation method thereof |
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