CN112402280B - Efficacy-promoting composition and application thereof - Google Patents

Efficacy-promoting composition and application thereof Download PDF

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CN112402280B
CN112402280B CN202011343249.4A CN202011343249A CN112402280B CN 112402280 B CN112402280 B CN 112402280B CN 202011343249 A CN202011343249 A CN 202011343249A CN 112402280 B CN112402280 B CN 112402280B
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hyaluronic acid
salt
weight
efficacy
composition
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CN112402280A (en
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蔺虓霄
阚洪玲
林伶俐
董建军
邵萌
王磊
田雪
郭学平
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Bloomage Biotech Co Ltd
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Bloomage Biotech Co Ltd
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Priority to PCT/CN2021/075783 priority patent/WO2022110550A1/en
Priority to KR1020237019821A priority patent/KR20230107323A/en
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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
    • A61K8/73Polysaccharides
    • A61K8/735Mucopolysaccharides, e.g. hyaluronic acid; 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
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34Alcohols
    • A61K8/345Alcohols containing more than one hydroxy group
    • 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
    • A61K8/49Cosmetics 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
    • A61K8/4946Imidazoles or their condensed derivatives, e.g. benzimidazoles
    • 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
    • A61K8/4953Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom containing pyrimidine ring derivatives, e.g. minoxidil
    • 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
    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9728Fungi, e.g. yeasts
    • 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
    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783Angiosperms [Magnoliophyta]
    • A61K8/9794Liliopsida [monocotyledons]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/007Preparations for dry 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
    • A61K2800/40Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/52Stabilizers
    • A61K2800/524Preservatives
    • 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
    • A61K2800/80Process related aspects concerning the preparation of the cosmetic composition or the storage or application thereof
    • A61K2800/85Products or compounds obtained by fermentation, e.g. yoghurt, beer, wine

Abstract

The invention provides an efficacy-promoting composition, which is characterized by comprising high molecular hyaluronic acid or a salt thereof, hydrolyzed hyaluronic acid or a salt thereof, acetylated hyaluronic acid or a salt thereof, tetrahydropyrimidine or a derivative thereof, ergothioneine, yeast/rice fermentation product filtrate and aminobutyric acid. The efficacy promoting composition disclosed by the invention can be used for moisturizing and repairing skin, so that on one hand, the stability of macromolecular efficacy components can be improved, and the contact time with the skin is increased, thereby improving the utilization rate of the macromolecular efficacy components, reducing the dosage of the efficacy components, saving the cost, and reducing the skin irritation caused by excessive dosage of some efficacy components; on the other hand, the transdermal absorption effect of the micromolecule functional components can be improved, and the utilization rate of the micromolecule functional components can be increased.

Description

Efficacy-promoting composition and application thereof
Technical Field
The invention belongs to the field of biological medicines, and particularly relates to an efficacy promoting composition and application thereof.
Background
The precondition for the maximum efficacy of the cosmetic is that the active ingredients have good permeability and activity, and the utilization rate of the active ingredients is improved.
Transdermal absorption of cosmetics refers to a process in which functional ingredients in cosmetics act on the skin surface or enter the epidermis or dermis according to the effectiveness of the product, and accumulate and act at that site. Transdermal absorption of cosmetic benefit agents does not require penetration through the skin into the systemic circulation, which is a major difference from drugs. For example, the whitening agent in a whitening product needs to act on the basal layer of the skin, blocking the production of melanin; the functional components of the anti-aging product need to act on fibroblasts in the dermis layer, so that the skin is elastic; the sunscreen agent in the sunscreen product needs to stay on the surface of the skin to absorb and reflect ultraviolet rays; some moisturizing products act on the epidermis or dermis according to different action mechanisms to improve the moisture content of the skin.
There are many factors that affect the transdermal absorption of cosmetics, mainly: skin factors, active ingredient structures, substance concentrations, cosmetic formulations, external environments and the like, at present, active ingredients similar to skin are mostly selected in the market, the cosmetic formulations are changed to improve the permeability of cosmetics, the effect is single, and the permeation promoting effect has certain limitations.
Therefore, there is an urgent need for an efficacy-enhancing composition, which can enhance the penetration and absorption of active ingredients, realize accurate positioning of the active ingredients, rapidly exert the skin-care effect, improve the stability of the active ingredients, and increase the contact time between the active ingredients and the skin according to the different positions where the different active ingredients act, thereby improving the utilization rate of the active ingredients.
Disclosure of Invention
The invention aims to provide an efficacy promoting composition which can effectively improve the penetration and absorption of efficacy components and the stability of the efficacy components while keeping moisture and replenishing water, thereby improving the utilization rate of the efficacy components and improving the skin condition. Specifically, the present invention relates to the following aspects:
1. an efficacy-promoting composition comprising a polymeric hyaluronic acid or salt thereof, a hydrolyzed hyaluronic acid or salt thereof, an acetylated hyaluronic acid or salt thereof, a tetrahydropyrimidine or derivative thereof, ergothioneine, yeast/rice fermentation product filtrate, and aminobutyric acid.
2. The composition according to item 1, wherein the composition comprises 1-30% by mass, preferably 1-10% by mass of the polymeric hyaluronic acid or the salt thereof, 2-50% by mass, preferably 2-10% by mass of the hydrolyzed hyaluronic acid or the salt thereof, 1-10% by mass, preferably 1-1.5% by mass of the acetylated hyaluronic acid or the salt thereof, 0.1-10% by mass, preferably 0.3-5% by mass of the tetrahydropyrimidine or the derivative thereof, 2-20% by mass, preferably 3-10% by mass of the ergothioneine, 10-50% by mass, preferably 15-40% by mass of the yeast/rice fermentation product filtrate, and 0.1-5% by mass of the aminobutyric acid, preferably 0.3 to 3%.
3. The composition according to item 1 or 2, wherein the amount of the polymeric hyaluronic acid or the salt thereof is 1 part by weight, the amount of the hydrolyzed hyaluronic acid or the salt thereof is 0.2 to 2 parts by weight, preferably 0.5 to 1 part by weight, and the amount of the acetylated hyaluronic acid or the salt thereof is 0.05 to 1.5 parts by weight, preferably 0.1 to 0.5 parts by weight.
4. The composition according to any of items 1 to 3, wherein the high molecular weight hyaluronic acid or salt thereof has a molecular weight of 1000-1800kDa, preferably 1000-1500 kDa.
5. The composition according to any one of items 1 to 4, wherein the hydrolyzed hyaluronic acid has a molecular weight of 1kDa to 10kDa, preferably 5kDa to 10 kDa.
6. The composition according to any one of items 1 to 5, wherein the acetylated hyaluronic acid or salt thereof has a molecular weight of 20kDa to 100kDa and a mass percentage of acetyl groups of 20 to 40%.
7. The composition according to any one of claims 1 to 6, wherein the tetrahydropyrimidine or derivative thereof is selected from one or both of a tetrahydropyrimidine carboxylic acid and a hydroxytetrahydropyrimidine carboxylic acid, preferably a tetrahydropyrimidine carboxylic acid.
8. The composition according to any one of items 1 to 7, further comprising a preservative, wherein the preservative is 0.1 to 5% by mass in the composition, and the preservative is selected from one or more of pentanediol, hexanediol, butanediol, and ethylhexylglycerin.
9. Use of the composition according to any one of items 1 to 8 in skin care or cosmetic products.
10. A skin care or cosmetic product comprising the composition of any one of items 1 to 8.
The invention has the following beneficial effects:
1. the acetylated hyaluronic acid is connected with high molecular hyaluronic acid and hydrolyzed hyaluronic acid with specific molecular weights according to a specific proportion, a stable I-shaped channel is constructed in a three-dimensional space, a long-acting water replenishing and moisturizing channel from a skin surface moisturizing and water locking layer to a skin deep layer moisturizing layer is formed, water is effectively replenished, and the water content of the skin is increased;
2. the tetrahydropyrimidine, the ergothioneine, the yeast/rice fermentation product filtrate and the aminobutyric acid have synergistic effect, so that the efficient operation of an I-shaped structure formed by the sodium hyaluronate and the derivatives thereof is ensured, the skin barrier is repaired more efficiently, the damage is repaired, and the skin surface condition is improved;
3. the I-shaped efficacy promoting system constructed by 7 components can improve the stability of macromolecular efficacy components and increase the contact time with skin while moisturizing and repairing the skin, thereby improving the utilization rate of the macromolecular efficacy components, reducing the dosage of the efficacy components, saving the cost and reducing the skin irritation caused by excessive dosage of certain efficacy components; on the other hand, the transdermal absorption effect of the small molecule functional components can be increased through the I-shaped channel, and the utilization rate of the small molecule functional components is increased.
Detailed Description
The present invention is further illustrated by the following examples, which are intended to be purely exemplary of the invention and are not intended to be limiting.
Unless defined otherwise, technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art. Although methods and materials similar or equivalent to those described herein can be used in experimental or practical applications, the materials and methods are described below. In case of conflict, the present specification, including definitions, will control, and the materials, methods, and examples are illustrative only and not intended to be limiting. The present invention is further illustrated by the following examples, which are not intended to limit the scope of the invention.
The invention provides an efficacy-promoting composition, which comprises high molecular hyaluronic acid or a salt thereof, hydrolyzed hyaluronic acid or a salt thereof, acetylated hyaluronic acid or a salt thereof, tetrahydropyrimidine or a derivative thereof, ergothioneine, yeast/rice fermentation product filtrate and aminobutyric acid.
In a specific embodiment, the mass percentage of the polymeric hyaluronic acid or the salt thereof is 1 to 30%, for example, 1%, 5%, 10%, 15%, 20%, 25%, 30%, preferably 1 to 10%. The mass percentage of the hydrolyzed hyaluronic acid or the salt thereof may be 2% to 50%, for example, 2%, 5%, 10%, 15%, 20%, 25%, 30%, 35%, 40%, 45%, 50%, preferably 2% to 10%, and the mass percentage of the acetylated hyaluronic acid or the salt thereof may be 1% to 10%, for example, 1%, 1.2%, 1.5%, 2%, 3%, 4%, 5%, 6%, 7%, 8%, 9%, 10%, preferably 1% to 1.5%. The percentage by mass of the tetrahydropyrimidine or a derivative thereof may be 0.1% to 10%, for example, 0.1%, 0.3%, 0.5%, 1%, 2%, 3%, 4%, 5%, 6%, 7%, 8%, 9%, 10%, preferably 0.3% to 5%. The ergothioneine accounts for 2-20% by mass, and can be 2%, 3%, 5%, 10%, 15%, 20%, preferably 3-10%. The mass percentage of the yeast/rice fermentation product filtrate is 10-50%, for example, 10%, 15%, 20%, 25%, 30%, 35%, 40%, 45%, 50%, preferably 15-40%. The aminobutyric acid may be 0.1 to 5% by mass, for example, 0.1%, 0.3%, 0.5%, 1%, 2%, 3%, 4%, 5%, preferably 0.3 to 3%.
The Hyaluronic Acid (HA) is a high molecular polysaccharide naturally existing in human interstitial tissue, is widely applied to the fields of medicines, skin care products, foods and the like, HAs various different molecular weights, HAs different effects and expressions of the HA with each molecular weight, HAs excellent film forming and water locking effects, can permeate the skin through low molecular hydrolyzed HA, deeply moisturizes the skin, can be used as a bridge for connecting the skin surface with the hydrolyzed HA through acetylation, and is a natural and effective moisturizing factor and water locking factor.
According to the invention, through the matching of three different HA, a skin surface moisturizing and moisturizing layer mainly comprising film-forming high-molecular HA, a deep water replenishing layer mainly comprising hydrolyzed HA and a water conveying layer connecting two parts of acetylated HA are formed in a space, and an I-shaped long-acting moisturizing channel is constructed in a three-dimensional space.
In a specific embodiment, the high molecular weight hyaluronic acid or salt thereof has a molecular weight of 1000-1800kDa, such as 1000kDa, 1100kDa, 1200kDa, 1300kDa, 1400kDa, 1500kDa, 1600kDa, 1700kDa, 1800kDa, preferably 1000-1500 kDa. The molecular weight of the hydrolyzed hyaluronic acid or a salt thereof is 1kDa to 10kDa, and may be, for example, 1kDa, 2kDa, 3kDa, 4kDa, 5kDa, 6kDa, 7kDa, 8kDa, 9kDa, 10kDa, and preferably 5kDa to 10 kDa. The acetylated hyaluronic acid or salt thereof has a molecular weight of 20kDa to 100kDa, and may be, for example, 20kDa, 30kDa, 40kDa, 50kDa, 60kDa, 70kDa, 80kDa, 90kDa, 100 kDa. The mass percentage of acetyl groups in the acetylated hyaluronic acid or salt thereof is 20-40%, and may be, for example, 20%, 25%, 30%, 35%, 40%.
In a specific embodiment, the amount of the polymeric hyaluronic acid or the salt thereof is 1 part by weight, the amount of the hydrolyzed hyaluronic acid or the salt thereof is 0.2 to 2 parts by weight, for example, it may be 0.2 parts by weight, 0.3 parts by weight, 0.4 parts by weight, 0.5 parts by weight, 0.6 parts by weight, 0.7 parts by weight, 0.8 parts by weight, 0.9 parts by weight, 1 part by weight, 1.1 parts by weight, 1.2 parts by weight, 1.3 parts by weight, 1.4 parts by weight, 1.5 parts by weight, 1.6 parts by weight, 1.7 parts by weight, 1.8 parts by weight, 1.9 parts by weight, 2 parts by weight, preferably 0.5 to 1 part by weight, and the acetylated hyaluronic acid or a salt thereof is 0.05 to 1.5 parts by weight, for example, it may be 0.05 part by weight, 0.1 part by weight, 0.2 part by weight, 0.3 part by weight, 0.4 part by weight, 0.5 part by weight, 1 part by weight, 1.1 part by weight, 1.2 parts by weight, 1.3 parts by weight, 1.4 parts by weight, 1.5 parts by weight, preferably 0.1 to 0.5 part by weight.
Tetrahydromethylpyrimidine carboxylic acid (ECTOIN) is the most widely distributed compatible solute in the bacterial community, is compatible with the metabolism in cells, does not influence the biomacromolecule function or physiological function of the cells, and is an important osmotic pressure compensation solute. The intensive charge distribution on the surface of the ectoine enables the ectoine to further strengthen the hydrogen bond effect between water molecules through the electrostatic interaction between the ectoine and the water molecules, reduces the water activity, complexes the water molecules and has the long-acting moisturizing effect. The hydrogen bond effect among water molecules is strengthened through the high-density charges of the water-based moisturizing agent, so that long-acting moisturizing is achieved; because of the excellent hydrophilicity, the skin barrier can be repaired with higher efficiency and the damage can be repaired through the I-shaped structure.
In a specific embodiment, the tetrahydropyrimidine or derivative thereof is selected from one or both of a tetrahydropyrimidine carboxylic acid and a hydroxytetrahydropyrimidine carboxylic acid, preferably a tetrahydropyrimidine carboxylic acid.
ERGOTHIONEINE (ERGOTHIONINE) is distributed in certain tissues and organs of mammal, is a natural antioxidant, can be produced by fermentation, can protect cells in human body, has UV protection effect, and is an important active substance in organism. Through the synergistic effect of the sodium hyaluronate and the ECTOIN, the skin barrier can be effectively protected, and the operation of an I-shaped structure formed by the sodium hyaluronate and derivatives thereof is ensured.
The yeast/rice fermentation product filtrate (Saccharomyces/RICE FERMENT FILTRATE) is a natural material produced by fermentation, and has effects of improving cell activity and promoting cell regeneration. The polymer HA can effectively stay on the skin surface for a long time through a film formed on the skin surface by the polymer HA, the regeneration of surface damaged cells is promoted, and the polymer HA, the ergothioneine and the ECTOIN have synergistic effect, so that the skin surface condition is improved more efficiently, and the moisturizing capability of the polymer HA is improved.
AMINOBUTYRIC ACID (Aminobtyric ACID) can promote epidermal cell proliferation and keratinocyte involucrin production, repair stratum corneum barrier, reduce ultraviolet injury to skin, and improve cell activity.
Tetrahydropyrimidine or derivatives thereof, ergothioneine, yeast/rice fermentation product filtrate and aminobutyric acid can effectively protect skin barriers and ensure the stability and durability of a film formed on the surface of the skin by high-molecular HA, thereby ensuring the efficient operation of an I-shaped structure formed by sodium hyaluronate and derivatives thereof.
The composition also comprises a preservative, wherein the preservative is one or more than two of pentanediol, hexanediol, butanediol and ethylhexyl glycerin, and the mass percentage of the preservative in the composition is 0.1-5%.
The present invention also provides an efficacy-promoting composition comprising a high molecular hyaluronic acid or a salt thereof, a hydrolyzed hyaluronic acid or a salt thereof, an acetylated hyaluronic acid or a salt thereof, a tetrahydropyrimidine or a derivative thereof, ergothioneine, yeast/rice fermentation product filtrate, aminobutyric acid, a preservative and water. The mass ratio of the components, and the properties such as molecular weight are as described above.
The invention also provides the application of the composition in skin care products or cosmetics.
The efficacy promoting composition comprises high molecular hyaluronic acid, hydrolyzed hyaluronic acid, acetylated hyaluronic acid, tetrahydropyrimidine, ergothioneine, yeast/rice fermentation product filtrate and aminobutyric acid in a specific ratio, and has an effective efficacy promoting function. For example, it is possible to remarkably promote water replenishment, improve the stability of active ingredients, improve the absorption of anti-aging ingredients, and the like. The reason is probably that on one hand, acetylated hyaluronic acid is connected with high molecular weight hyaluronic acid and hydrolyzed hyaluronic acid with specific molecular weights in a specific proportion, and a stable I-shaped channel is constructed in a three-dimensional space, and on the other hand, tetrahydropyrimidine, ergothioneine, yeast/rice fermentation product filtrate and aminobutyric acid are cooperated to ensure the efficient operation of an I-shaped structure formed by sodium hyaluronate and derivatives thereof.
Examples
The present invention is further illustrated by the following examples, which are intended to be purely exemplary of the invention and are not intended to be limiting.
The experimental methods used in the following examples are all conventional methods, unless otherwise specified.
Materials, reagents and the like used in the following examples are commercially available unless otherwise specified. Wherein the high molecular weight sodium hyaluronate, hydrolyzed sodium hyaluronate, acetylated sodium hyaluronate, tetrahydromethylpyrimidine carboxylic acid, ergothioneine, yeast/rice fermentation product filtrate, and aminobutyric acid are all from Huaxi Biotech Ltd.
Example 1
Adding 2.5g of high molecular weight sodium hyaluronate (1200kDa) into a proper amount of water, and stirring until the sodium hyaluronate is completely dissolved; then 2.5g of hydrolyzed sodium hyaluronate (5kDa) and 1g of acetylated sodium hyaluronate (molecular weight 4kDa, acetyl content 24%) are added, and the mixture is stirred uniformly until the mixture is completely dissolved; adding 3g of tetrahydro-methyl pyrimidine carboxylic acid, 7g of ergothioneine, 20g of yeast/rice fermentation product filtrate, 1.5g of aminobutyric acid and 5g of preservative (2.5 g of pentanediol and 2.5g of hexanediol) in sequence, supplementing water to 100g, and stirring uniformly until the preservative is completely dissolved to obtain the efficacy promoting composition.
Examples 2-8, comparative examples 1-8 differ from example 1 in the molecular weight or content of the high molecular weight sodium hyaluronate, hydrolyzed sodium hyaluronate, acetylated sodium hyaluronate, the content of the tetrahydro methyl pyrimidine carboxylic acid, ergothioneine, yeast/rice fermentation product filtrate, aminobutyric acid, as shown in table 1.
TABLE 1 examples and comparative examples the contents of the components
Figure BDA0002799138330000071
Test example 1 Water replenishing Effect
1. Skin hydration was tested in 17 different areas of the forearm (area numbers 1-17) and initial data was recorded.
2. Ceramide-3 was added to the efficacy-promoting compositions prepared in examples 1 to 8 and comparative examples 1 to 8 in an amount of 1% by mass, respectively, to obtain moisturizing compositions corresponding to examples 1 to 8 and comparative examples 1 to 8.
3. The same amount of moisturizing composition corresponding to examples 1-8 and comparative examples 1-8 was applied to 16 different areas of the forearm (area No. 1-16), and after 30 minutes the skin moisture content was measured and recorded using a skin moisture loss meter Tewameter TM300(Courage + Khazaka, germany). The moisturizing composition of the example 1 corresponds to the area No. 1, the moisturizing composition of the example 2 corresponds to the area No. 2, and the analogy is that the moisturizing composition of the example 8 corresponds to the area No. 8, the moisturizing composition of the comparative example 1 corresponds to the area No. 9, the moisturizing composition of the comparative example 2 corresponds to the area No. 10, and the moisturizing composition of the comparative example 8 corresponds to the area No. 16.
4. The same amount of moisturizing ingredient solution (1% by mass of ceramide-3) was applied to area 17 as a control, and after 30 minutes, the skin moisture content was measured and recorded.
5. The number of test persons was 10, and the water content was averaged.
The moisturizing effect of each moisturizing composition is shown in table 2.
TABLE 2 Water replenishing Effect of each example and comparative example
Water content (initial value) Water content (after application)
Region 1 36.71 45.33
Region 2 35.42 42.87
Region 3 36.34 44.76
Region 4 35.89 43.76
Region 5 36.03 40.22
Region 6 36.07 39.46
Region 7 36.12 40.21
Region 8 36.08 39.72
Region 9 36.11 37.00
Region 10 36.01 36.59
Region 11 35.98 36.91
Region 12 36.00 37.10
Region 13 36.01 37.23
Region 14 35.99 37.01
Region 15 36.02 37.34
Region 16 36.03 36.24
Region 17 36.07 36.11
And (4) conclusion: as can be seen from table 2, the moisturizing ability of the moisturizing ingredient is significantly increased after the composition prepared in the examples of the present invention is added, and particularly, the moisturizing effect of the compositions obtained in examples 1 to 4 is the best, which shows that the efficacy-enhancing composition of the present invention can effectively enhance moisturizing.
The comparative examples 1 to 3 only contain two of the three kinds of hyaluronic acid, so that the water replenishing effect is poor, and probably because the three kinds of hyaluronic acid can construct stable I-shaped channels in a three-dimensional space, long-acting water replenishing and moisturizing channels from a skin surface moisturizing and water locking layer to a skin deep layer moisturizing layer are formed, so that the water is effectively replenished, the water content of the skin is increased, meanwhile, the I-shaped channels can increase the transdermal absorption effect of the ceramide-3, increase the utilization rate of the ceramide-3 and enhance the water replenishing effect.
Comparative examples 4 to 8 are also poor in moisturizing effect, wherein the moisturizing effect achieved by comparative example 8 is the worst, and the difference in moisture content of the skin before and after use is only 0.21, which may be due to the synergistic effect of tetrahydropyrimidine, ergothioneine, yeast/rice fermentation product filtrate and aminobutyric acid, which can maintain the stability and durability of the membrane formed by the high molecular hyaluronic acid on the surface of the skin, thereby ensuring the efficient operation of the I-shaped structure formed by sodium hyaluronate and derivatives thereof.
Test example 2 protective action against active ingredients
Astaxanthin was added to the efficacy-promoting compositions prepared in examples 1 to 8 and comparative examples 1 to 8 so that the mass percentage of astaxanthin in the compositions was 0.01%, to obtain astaxanthin-containing compositions, which correspond to application examples 1 to 16, respectively. The astaxanthin composition obtained in example 1 corresponds to application example 1, the astaxanthin composition obtained in example 2 corresponds to application example 2, and so on, the astaxanthin composition obtained in example 8 corresponds to application example 8, the astaxanthin composition obtained in comparative example 1 corresponds to application example 9, the astaxanthin composition obtained in comparative example 2 corresponds to application example 10, and the astaxanthin composition obtained in comparative example 8 corresponds to application example 16.
An equal amount of the astaxanthin composition of application examples 1 to 16 was placed in a transparent container and left at room temperature for 2 hours while being stirred to contact with oxygen, the color change of the composition was observed, an appropriate amount of the composition was diluted with chloroform solvent to a solution having a concentration of 1. mu.g/mL, and the absorbance at 489nm was measured with a UV8500 UV spectrophotometer. The absorbance at 489nm was measured under the same conditions using astaxanthin at the same concentration and hermetically stored in the dark as a control. The results are shown in Table 3.
TABLE 3 protective action of the examples and comparative examples on active ingredients
Figure BDA0002799138330000091
Figure BDA0002799138330000101
And (4) conclusion: astaxanthin is easily oxidized to lighten the color, and the lighter the color, the more astaxanthin is oxidized, the poorer the efficacy of astaxanthin is. The astaxanthin color did not fade significantly upon addition of the compositions prepared in the examples of the invention, and the absorbance was only reduced 0.0391-0.0969 compared to the control stored in a light-tight and sealed condition, particularly with minimal color change in examples 1-4. However, the astaxanthin composition of the comparative example showed a large color change and a decrease in absorbance of 0.3 or more. This shows that the efficacy promoting system constructed by 7 components of the invention can improve the stability of macromolecular efficacy components such as astaxanthin, increase the contact time of astaxanthin and skin, and thus improve the utilization rate of astaxanthin.
Test example 3 promoting action of anti-aging component
1. The eyes and facial wrinkles were photographed by Visia, and skin age data was recorded.
2. In example 1, comparative example 1, and comparative example 8, 1% of wrinkle-removing component (anti-wrinkle complex peptide) was added to obtain anti-aging compositions, which correspond to application examples 18, 19, and 20, respectively.
3. The application examples 18, 19, 20 were applied by regional application twice daily for 12 weeks, photographed with Visia every 2 weeks, and skin age data was recorded.
4. The number of test persons was 10 persons each, and the skin ages were averaged.
Table 4 skin age data
Figure BDA0002799138330000102
Figure BDA0002799138330000111
And (4) conclusion: the efficacy-promoting composition prepared in the example of the present invention can well promote the efficacy of the anti-aging ingredient to be exerted, and as can be seen from the above table, the efficacy of the anti-aging ingredient of application example 18 is significantly increased, and after a certain period of use, the skin age is reduced by 6 years, whereas the skin age changes little or hardly after application examples 19 and 20 are used for a certain period of time.

Claims (12)

1. An efficacy-promoting composition comprising a polymeric hyaluronic acid or salt thereof, a hydrolyzed hyaluronic acid or salt thereof, an acetylated hyaluronic acid or salt thereof, a tetrahydropyrimidine or derivative thereof, ergothioneine, yeast/rice fermentation product filtrate, aminobutyric acid;
wherein the mass percent of the high molecular hyaluronic acid or the salt thereof is 1-10%, the mass percent of the hydrolyzed hyaluronic acid or the salt thereof is 2-10%, the mass percent of the acetylated hyaluronic acid or the salt thereof is 1-10%, the mass percent of the tetrahydropyrimidine or the derivative thereof is 0.1-10%, the mass percent of the ergothioneine is 2-20%, the mass percent of the yeast/rice fermentation product filtrate is 10-50%, and the mass percent of the aminobutyric acid is 0.1-5%;
the molecular weight of the high molecular hyaluronic acid or the salt thereof is 1000kDa-1800 kDa;
the molecular weight of the hydrolyzed hyaluronic acid is 1kDa-10 kDa.
2. The composition according to claim 1, wherein the mass percent of the acetylated hyaluronic acid or salt thereof is 1-1.5%, the mass percent of the tetrahydropyrimidine or derivative thereof is 0.3-5%, the mass percent of the ergothioneine is 3-10%, the mass percent of the yeast/rice fermentation product filtrate is 15-40%, and the mass percent of the aminobutyric acid is 0.3-3%.
3. The composition according to claim 1, wherein the amount of the polymeric hyaluronic acid or the salt thereof is 1 part by weight, the amount of the hydrolyzed hyaluronic acid or the salt thereof is 0.2 to 2 parts by weight, and the amount of the acetylated hyaluronic acid or the salt thereof is 0.05 to 1.5 parts by weight.
4. The composition according to claim 1, wherein the amount of the polymeric hyaluronic acid or the salt thereof is 1 part by weight, the amount of the hydrolyzed hyaluronic acid or the salt thereof is 0.5 to 1 part by weight, and the amount of the acetylated hyaluronic acid or the salt thereof is 0.1 to 0.5 part by weight.
5. The composition of claim 1, wherein the molecular weight of the polymeric hyaluronic acid or salt thereof is from 1000kDa to 1500 kDa.
6. The composition of claim 1, wherein the hydrolyzed hyaluronic acid has a molecular weight of 5kDa to 10 kDa.
7. The composition according to claim 1, wherein the acetylated hyaluronic acid or salt thereof has a molecular weight of 20-100 kDa and a mass percentage of acetyl groups of 20-40%.
8. The composition of claim 1, wherein the tetrahydropyrimidine or derivative thereof is selected from one or both of tetrahydropyrimidine carboxylic acid and hydroxytetrahydropyrimidine carboxylic acid.
9. The composition of claim 8, wherein the tetrahydropyrimidine or derivative thereof is a tetrahydropyrimidine carboxylic acid.
10. The composition according to claim 1, further comprising a preservative, wherein the preservative is 0.1-5% by mass of the composition, and the preservative is one or more selected from the group consisting of pentanediol, hexanediol, butanediol, and ethylhexylglycerin.
11. Use of a composition according to any one of claims 1 to 10 for the preparation of a skin care or cosmetic product.
12. A skin care or cosmetic product comprising the composition of any one of claims 1-10.
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