CN114569491B - Composition for inhibiting grease generation and application thereof - Google Patents
Composition for inhibiting grease generation and application thereof Download PDFInfo
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- A61Q19/008—Preparations for oily skin
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Abstract
The application provides a composition for inhibiting grease generation, which comprises zinc hyaluronate and ectoin or derivatives thereof. The application also provides a skin care product comprising the composition for inhibiting grease generation and application of the composition comprising zinc hyaluronate and ectoin or derivatives thereof in preparing skin care products or medicines for inhibiting grease. The composition comprising zinc hyaluronate and ectoin or derivatives thereof can inhibit skin grease generation, reduce acne generation, and is very suitable for preparing cosmetics and cleaning products and medical appliances with the functions of controlling oil or resisting acne, treating seborrheic dermatitis, inhibiting acne and inhibiting closed mouth and blackhead generation.
Description
Technical Field
The application belongs to the field of biological medicine, and in particular relates to a composition for inhibiting grease generation and application thereof.
Background
With the improvement of the economic level and living standard of the human society, the pursuit of beauty is increasingly promoted. Acne is also known as acne, a common skin condition. Facial acne is frequently found in teenagers, and not only has certain harm to facial skin health, but also can cause the spelt mental condition of patients to damage the physical and mental health of the patients.
The occurrence of acne is closely related to the factors such as hypersecretion of sebum, blockage of the pilosebaceous ducts, bacterial infection and inflammatory reaction. Research in literature at home and abroad shows that excessive secretion of grease by sebaceous gland cells can be one of the important factors causing acne. SZ95 is an immortalized sebaceous gland cell line, commonly used for the assessment of in vitro lipid production. Arachidonic acid is one of the common inflammatory factors, and the stimulation of SZ95 cells by arachidonic acid to generate grease can well simulate the occurrence of acne.
Disclosure of Invention
In view of the above problems of the prior art, the present application provides a composition for inhibiting the formation of grease and its use.
In particular, the application relates to the following aspects:
1. a composition for inhibiting the formation of grease, the composition comprising zinc hyaluronate and ectoin or a derivative thereof.
2. The composition for inhibiting the formation of fat and oil according to item 1, wherein the molecular weight of the zinc hyaluronate is 1 ten thousand Da or more, preferably 3 ten thousand Da to 130 ten thousand Da.
3. The composition for inhibiting the formation of oil and fat according to item 1, wherein the mass ratio of the zinc hyaluronate to the ectoin or its derivative is 1:0.1-3, preferably 1:1-3.
4. The composition for inhibiting the formation of oil and fat according to item 1, which consists of zinc hyaluronate and exendin or a derivative thereof.
5. The composition for inhibiting the formation of fat and oil according to item 1, wherein the exendin or a derivative thereof is one or more selected from the group consisting of exendin, exendin methyl ester and hydroxyexendin.
6. A skin care product, characterized in that the skin care product comprises the composition for inhibiting the formation of oils as described in any one of items 1 to 4.
7. The skin care product according to item 6, wherein the content of the fat-production-inhibiting composition in the skin care product is 0.01 to 1% by weight.
8. Use of a composition comprising zinc hyaluronate and ectoin or a derivative thereof in the manufacture of a skin care product or medicament for inhibiting grease.
9. The use according to item 1, wherein the molecular weight of the zinc hyaluronate is 1 Da or more, preferably 3 Da to 130 Da.
10. The use according to item 1, wherein the mass ratio of zinc hyaluronate to ectoin or its derivative is 1:0.1-3, preferably 1:1-3.
The composition comprising zinc hyaluronate and ectoin or derivatives thereof can inhibit skin grease generation, reduce acne generation, and is very suitable for preparing cosmetics and cleaning products and medical appliances with the functions of controlling oil or resisting acne, treating seborrheic dermatitis, inhibiting acne and inhibiting closed mouth and blackhead generation.
Drawings
FIG. 1 is a graph showing the relative oil content (%) of the samples.
Detailed Description
The application will be further illustrated with reference to the following examples, which are to be understood as merely further illustrating and explaining the application and are not to be construed as limiting the application.
Unless defined otherwise, technical and scientific terms used in this specification 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 the practice or testing of the present application, the materials and methods are described herein below. In case of conflict, the present specification, including definitions therein, will control and materials, methods, and examples, will control and be in no way limiting. The application is further illustrated below in connection with specific examples, which are not intended to limit the scope of the application.
The application provides a composition for inhibiting grease generation, which comprises zinc hyaluronate and ectoin or derivatives thereof.
Among them, HYALURONIC ACID (HA) is a mucopolysaccharide substance composed of disaccharide repeating units of N-acetamido glucose and glucuronic ACID, and commercial HYALURONIC ACID is usually in the form of its sodium salt, called sodium hyaluronate. Hyaluronic acid plays multiple physiological functions on human body due to its special molecular composition structure and physicochemical properties. The hyaluronic acid has special water-retaining effect, and the high molecular weight hyaluronic acid rapidly forms a layer of breathable hydration film on the skin surface, and hydrates and softens the skin cuticle. The hyaluronic acid with low molecular weight can directly permeate into the dermis layer, so that the physiological characteristics of skin are effectively improved, a good external environment is provided for synthesis of dermis collagen and elastic fibers, effective supply of nutrient substances is facilitated, and the function of nourishing skin is generated. The zinc hyaluronate is zinc salt of hyaluronic acid and is prepared by ion exchange of zinc ions and sodium ions on sodium hyaluronate carboxyl. The medicine is mainly applied to healing of skin wounds, peptic ulcers, antioxidation and the like, and has the characteristics of good safety, good curative effect and the like.
In the present application, the molecular weight of zinc hyaluronate is not limited. In a specific embodiment, the molecular weight of the zinc hyaluronate is 1 ten thousand Da or more, for example, 1 ten thousand Da, 3 ten thousand Da, 5 ten thousand Da, 10 ten thousand Da, 20 ten thousand Da, 30 ten thousand Da, 40 ten thousand Da, 50 ten thousand Da, 60 ten thousand Da, 70 ten thousand Da, 80 ten thousand Da, 90 ten thousand Da, 100 ten thousand Da, 110 ten thousand Da, 120 ten thousand Da, 130 ten thousand Da, 140 ten thousand Da, 150 ten thousand Da, 160 ten thousand Da, 170 ten thousand Da, 180 ten thousand Da, 190 ten thousand Da, 200 ten thousand Da, 300 ten thousand 500 Da, preferably 3 ten thousand Da to 130 ten thousand Da.
Epidendole (Ectoine), also known as tetrahydropyrimidine (chemical name 1,4,5,6-tetrahydro-2-methyl-4-pyrimidinecarboxylic acid, english name 1,4,5, 6-tetrahydroo-2-methyl-4-pyrimidinecarboxylic acid), is a cyclic amino acid derivative. The osmotic pressure compensation solute is synthesized by extreme environment microorganisms under osmotic pressure stress, is compatible with metabolism in cells, and has good protection effect on cells and biological macromolecules under the stimulation of high temperature, high salt, freezing, drying, radiation and other adverse environments. The exendin derivative may be hydroxy exendin, exendin methyl ester or other exendin derivatives.
In the composition for inhibiting the formation of fat, the zinc hyaluronate and the ectoin or the derivative thereof may be present in any mass ratio. In a specific embodiment, the mass ratio of zinc hyaluronate to ectoin or its derivative is 1:0.1-3, for example, 1:0.1, 1:0.2, 1:0.3, 1:0.4, 1:0.5, 1:0.6, 1:0.7, 1:0.8, 1:0.9, 1:1, 1:1.1, 1:1.2, 1:1.3, 1:1.4, 1:1.5, 1:1.6, 1:1.7, 1:1.8, 1:1.9, 1:2, 1:2.1, 1:2.3, 1:2.4, 1:2.5, 1:2.6, 1:2.7, 1:2.8, 1:2.9, 1:3, preferably 1:1-3.
In a specific embodiment, the composition for inhibiting oil production comprises zinc hyaluronate and exendin, wherein the molecular weight of the zinc hyaluronate is 90 Da, and the mass ratio of the zinc hyaluronate to the exendin is 1:1.5.
In a specific embodiment, the composition for inhibiting oil production comprises zinc hyaluronate and ectoin, wherein the molecular weight of the zinc hyaluronate is 90 Da, and the mass ratio of the zinc hyaluronate to the ectoin is 1:1.3.
In a specific embodiment, the composition for inhibiting oil production comprises zinc hyaluronate and ectoin, wherein the molecular weight of the zinc hyaluronate is 130 Da, and the mass ratio of the zinc hyaluronate to the ectoin is 1:2.2.
In a specific embodiment, the composition for inhibiting oil production comprises zinc hyaluronate and ectoin, wherein the molecular weight of the zinc hyaluronate is 90 Da, and the mass ratio of the zinc hyaluronate to the ectoin is 1:2.5.
In a specific embodiment, the composition for inhibiting oil production comprises zinc hyaluronate and ectoin, wherein the molecular weight of the zinc hyaluronate is 4 kiloDa, and the mass ratio of the zinc hyaluronate to the ectoin is 1:2.2.
In a specific embodiment, the composition for inhibiting oil production comprises zinc hyaluronate and ectoin, wherein the molecular weight of the zinc hyaluronate is 130 Da, and the mass ratio of the zinc hyaluronate to the ectoin is 1:2.2.
In a specific embodiment, the composition for inhibiting the formation of oil comprises zinc hyaluronate and ectoin methyl ester, wherein the molecular weight of the zinc hyaluronate is 90 ten thousand Da, and the mass ratio of the zinc hyaluronate to the ectoin is 1:2.2.
In a specific embodiment, the composition for inhibiting oil production comprises zinc hyaluronate and exendin, wherein the molecular weight of the zinc hyaluronate is 90 Da, and the mass ratio of the zinc hyaluronate to the exendin is 1:0.5.
In a specific embodiment, the composition for inhibiting the formation of oil comprises zinc hyaluronate and exendin, wherein the molecular weight of the zinc hyaluronate is 90 ten thousand Da, and the mass ratio of the zinc hyaluronate to the exendin is 1:2.2.
In a specific embodiment, the composition for inhibiting the formation of oil comprises zinc hyaluronate and ectoin or a derivative thereof.
The application also provides a skin care product which comprises the composition for inhibiting grease generation. The skin care product can be added with other components according to different product types or product performances.
In a specific embodiment, the grease-formation-inhibiting composition in the skin care product may be present in an amount of 0.01 to 1wt%, for example, 0.01wt%, 0.05wt%, 0.1wt%, 0.2wt%, 0.3wt%, 0.4wt%, 0.5wt%, 0.6wt%, 0.7wt%, 0.8wt%, 0.9wt%, 1wt%.
The application also provides the use of a composition comprising zinc hyaluronate and ectoin or a derivative thereof in the manufacture of a skin care product or medicament for inhibiting grease.
In a specific embodiment, in the above-mentioned use, the molecular weight of the zinc hyaluronate is 1 ten thousand Da or more, preferably 3 ten thousand Da to 130 ten thousand Da.
In a specific embodiment, in the above use, the mass ratio of the zinc hyaluronate and the ectoin or its derivative is 1:0.1-3, preferably 1:1-3.
The composition provided by the application comprises zinc hyaluronate and ectoine or derivatives thereof. Wherein, zinc hyaluronate provides certain effect of controlling grease generation, and simultaneously, the ectoin or the derivative thereof can protect sebaceous gland cells and prevent the sebaceous gland cells from being stimulated by inflammatory factors, and the use of the ectoin or the derivative thereof and the zinc hyaluronate can play a role of synergistic interaction and enhance the effect of the zinc hyaluronate on inhibiting grease generation.
Examples
The experimental methods used in the following examples are conventional methods, if no special requirements are imposed.
Materials, reagents, and the like used in the following examples were obtained commercially, and zinc hyaluronate and escitalopram or derivatives thereof were purchased from the same company as Huaxi biotechnology Co., ltd unless otherwise specified.
Example 1
10g of zinc hyaluronate having an average molecular weight of 90 Da was weighed out, and ectoin (trade name: xi An Yan) TM 15g of ectoine) and evenly mixing.
Example 2
10g of zinc hyaluronate having an average molecular weight of 90 Da was weighed out, and ectoin (trade name: xi An Yan) TM Ricketing) 13g, and mixing uniformly.
Example 3
10g of zinc hyaluronate having an average molecular weight of 90 Da was weighed out, and ectoin (trade name: xi An Yan) TM Escidodine) 25g, and mixing uniformly.
Example 4
10g of zinc hyaluronate having an average molecular weight of 90 Da was weighed out, and ectoin (trade name: xi An Yan) TM Ricketing) 22g, and mixing uniformly.
Example 5
10g of zinc hyaluronate having an average molecular weight of 90 Da was weighed out, and ectoin (trade name: xi An Yan) TM Escidodine) 50g, and mixing uniformly.
Example 6
10g of zinc hyaluronate having an average molecular weight of 90 Da was weighed out, and ectoin (trade name: xi An Yan) TM Elkeduoine) 44g, and mixing uniformly.
Example 7
10g of zinc hyaluronate having an average molecular weight of 130 Da was weighed out, and ectoin (trade name: xi An Yan) TM Ricketing) 22g, and mixing uniformly.
Example 8
10g of zinc hyaluronate having an average molecular weight of 4 Da was weighed out, and ectoin (trade name: xi An Yan) TM Ricketing) 22g, and mixing uniformly.
Example 9
10g of zinc hyaluronate having an average molecular weight of 200W Da was weighed out, and ectoin (trade name: xi An Yan) TM Ricketing) 22g, and mixing uniformly.
Example 10
Weighing 10g of zinc hyaluronate with the average molecular weight of 90 ten thousand Da, and 15g of ectoin methyl ester, and uniformly mixing.
Example 11
10g of zinc hyaluronate having an average molecular weight of 90 Da was weighed out, and ectoin (trade name: xi An Yan) TM 5g of ectoine) and evenly mixing.
Comparative example 1
10g of zinc hyaluronate having a molecular weight of 130 ten thousand Da was weighed.
Comparative example 2
Weighing 10g of ectoin (trade name: xi An Yan) TM Rickettsien).
The composition for inhibiting the grease generation comprises zinc hyaluronate and exendin or derivatives thereof, can inhibit the skin grease generation, and has obvious synergistic effect especially when the mass ratio of the zinc hyaluronate to the exendin or derivatives thereof is 1:1-3. The composition of the application reduces acne generation, and can be used for preparing cosmetics and cleaning products and medical appliances with the functions of controlling oil or resisting acne, treating seborrheic dermatitis, inhibiting acne and inhibiting closed mouth and blackhead generation.
Test examples
The efficacy of the composition containing zinc hyaluronate and ectoin or derivatives thereof is verified by using an arachidonic acid-induced SZ95 cell-based lipid generation model.
1. Sample preparation
The compositions obtained in examples and comparative examples were diluted with DMEM medium to obtain different samples. Sample information corresponding to each sample is shown in table 1. Specifically, the composition prepared in example 1 was diluted to a mass concentration of 0.05% to obtain sample 1. The composition prepared in example 2 was diluted to a mass concentration of 0.525% to obtain sample 2. The composition prepared in example 3 was diluted to a mass concentration of 0.042% to obtain sample 3. The composition prepared in example 3 was diluted to a mass concentration of 0.07% to give sample 4. The composition prepared in example 4 was diluted to a mass concentration of 0.0725% to give sample 5. The composition prepared in example 5 was diluted to a mass concentration of 0.12% to obtain sample 6. The composition prepared in example 6 was diluted to a mass concentration of 0.1225% to obtain sample 7. The composition prepared in example 7 was diluted to a mass concentration of 0.0725% to give sample 8-1. The composition prepared in example 8 was diluted to a mass concentration of 0.0725% to give sample 8-2. The composition prepared in example 9 was diluted to a mass concentration of 0.0725% to give sample 8-3. The composition prepared in example 10 was diluted to a mass concentration of 0.0725% to give sample 9. The composition prepared in example 11 was diluted to a mass concentration of 0.03% to obtain sample 10. The composition prepared in comparative example 1 was diluted to a mass concentration of 0.012%, to give sample 11-1. The composition prepared in comparative example 1 was diluted to a mass concentration of 0.02% to obtain sample 11-2. The composition prepared in comparative example 1 was diluted to a mass concentration of 0.0225% to obtain a sample 11-3. The composition prepared in comparative example 2 was diluted to a mass concentration of 0.03% to obtain sample 12-1. The composition prepared in comparative example 2 was diluted to a mass concentration of 0.05% to obtain sample 12-2. The composition prepared in comparative example 2 was diluted to a mass concentration of 0.1% to obtain sample 12-3.
TABLE 1
2. Dosing treatment and detection
SZ95 cells were seeded at a density of 6 ten thousand per well in 24 well plates and placed in an incubator for 24h. The supernatant was discarded, and the sample prepared in step 1 was added to the well plate while 50. Mu.M arachidonic acid was added per well, 500. Mu.L per well. The control group contained only 50 μ arachidonic acid without the addition of sample. Placed in an incubator for 48h of incubation. After the incubation, the supernatant was discarded, washed once with PBS, and fixed with 4% paraformaldehyde for 10min. After fixation, the cells were stained with oil red staining kit by washing twice with PBS. After the dyeing is finished, the grease is washed once by PBS, 300 mu L of isopropanol is added to extract the dyed grease, and 100 mu L of the grease is taken to read absorbance at 550nm after the extraction.
3. Statistical analysis
The relative oil content is calculated from the following formula:
relative oil content (%) = experimental oil absorbance/control oil content × 100%
Comparisons between groups were analyzed using t-test statistics, where p <0.05 was considered statistically different. * P <0.01 is considered to have significant statistical differences, p <0.001 is considered to have very significant statistical differences, and n.s is no statistical differences.
4. Results display
As shown in FIG. 1, samples 1,4 and 11-2 each had an effect of inhibiting the formation of oil, and sample 6 had no effect of inhibiting the formation of oil. The t-test was performed on sample 1 and sample 4, respectively, with sample 11-2, resulting in a statistical difference between both samples and sample 11-2.
Samples 2, 5 and 11-3 all had the effect of inhibiting the formation of oil, and sample 7 had no effect of inhibiting the formation of oil. The t-test was performed on sample 2 and sample 5, respectively, with sample 11-3, resulting in a statistical difference between both samples and sample 11-3.
Sample 3 has an effect of inhibiting the formation of oil, and sample 11-1 has no effect of inhibiting the formation of oil. The t-test was performed on sample 3 and sample 11-1 to obtain a statistical difference between the two samples.
Sample 5, sample 8-1, sample 8-2, sample 8-3, sample 9 and sample 10 all have the effect of inhibiting the formation of grease.
Samples 12-1, 12-2 and 12-3 all had no effect of inhibiting the formation of grease.
The above results illustrate that in zinc hyaluronate: the ratio of the ectoin or the salt thereof is 1:1.3-1:2.5, compared to zinc hyaluronate alone, there was a statistical difference, whereas zinc hyaluronate: the ratio of the ectoin is 1:4.4 and 1: there were no statistical differences compared to zinc hyaluronate at 5, nor even to the control group, indicating that zinc hyaluronate: the ratio of the ectoin is 1:4.4 and 1:5, the effect of suppressing the formation of fat is not exhibited. Meanwhile, the zinc hyaluronate has no obvious difference between the oil control effect of the combination of the zinc hyaluronate and the ectoin when the molecular weight is 4 ten thousand and 130 ten thousand and the oil control effect of the zinc hyaluronate and the molecular weight of the zinc hyaluronate when the molecular weight is 90 ten thousand.
5. Golden's formula test
5.1 calculating relative oil and fat inhibition Rate
The relative oil inhibition rate was calculated from the following formula, and the results are shown in table 2:
relative oil and fat inhibition ratio=1-relative oil and fat content
TABLE 2
Relative oil inhibition rate | |
Sample 1 | 0.327 |
Sample 2 | 0.345 |
Sample 3 | 0.330 |
Sample 4 | 0.345 |
Sample 5 | 0.380 |
Sample 6 | 0.062 |
Sample 7 | 0.080 |
Sample 8-1 | 0.340 |
Sample 8-2 | 0.390 |
Sample 8-3 | 0.175 |
Sample 9 | 0.342 |
Sample 10 | 0.297 |
Sample 11-1 | 0.205 |
Sample 11-2 | 0.265 |
Sample 11-3 | 0.260 |
Sample 12-1 | 0.012 |
Sample 12-2 | -0.002 |
Sample 12-3 | -0.003 |
5.2 checking formulas and principles:
q=E a+b /(E a +E b -E a *E b )
wherein E is the same as E when the synergy between the sample 11-2 and the sample 12-1 is examined a+b 、E a And E is b The relative oil and fat inhibition rates of sample 1, sample 11-2 and sample 12-1 were respectively shown.
E when the synergy between samples 11-3 and 12-1 is examined a+b 、E a And E is b The relative oil and fat inhibition rates of sample 2, sample 11-3 and sample 12-1 were respectively shown.
E when the synergy between the sample 11-1 and the sample 12-1 is examined a+b 、E a And E is b The relative oil and fat inhibition rates of sample 3, sample 11-1 and sample 12-1 were respectively shown.
E when the synergy between the sample 11-2 and the sample 12-2 is examined a+b 、E a And E is b The relative oil and fat inhibition rates of sample 4, sample 11-2 and sample 12-2 were respectively.
E when the synergy between samples 11-3 and 12-2 is examined a+b 、E a And E is b The relative oil and fat inhibition rates of sample 5, sample 11-3 and sample 12-2 were respectively.
When q is 0.85-1.15, the simple addition is performed; more than 1.15-20.
5.3 test results of the King's formula
The relative oil inhibition rates of sample 1, sample 11-2, and sample 12-1 were brought into the gold equation to give q=1.19, indicating that in zinc hyaluronate: ricketiness = 1:1.5, the final concentration of the mixture is 0.05 percent.
The relative oil inhibition rates of sample 2, sample 11-3, and sample 12-1 were taken into the gold equation to give q=1.23, indicating that in zinc hyaluronate: ricketiness = 1:1.3, the final concentration of the mixture is 0.0525 percent.
Bringing the relative oil inhibition rates of sample 3, sample 11-1, sample 12-1 into the gold equation yields q=1.53, indicating that in zinc hyaluronate: ricketiness = 1:2.5, the final concentration of the mixture is 0.042 percent.
Bringing the relative oil inhibition rates of sample 4, sample 11-2, sample 12-2 into the gold equation yields q=1.31, indicating that in zinc hyaluronate: ricketiness = 1:2.5, the final concentration of the mixture is 0.07 percent.
The relative oil inhibition rates of sample 5, sample 11-3, and sample 12-2 were taken into the gold equation to give q=1.47, indicating that in zinc hyaluronate: ricketiness = 1:2.2, the final concentration of the mixture is 0.0725 percent, and the synergistic effect is achieved.
The above results illustrate that in zinc hyaluronate: ricketiness = 1:1.3-1:2.5 has synergistic effect.
Claims (12)
1. A composition for inhibiting the formation of oil, comprising zinc hyaluronate and ectoin or a derivative thereof, wherein the mass ratio of zinc hyaluronate to ectoin or a derivative thereof is 1:0.1-3.
2. The composition for inhibiting the formation of fat according to claim 1, wherein the zinc hyaluronate has a molecular weight of 1 ten thousand Da or more.
3. The composition for inhibiting the formation of fat according to claim 1, wherein the zinc hyaluronate has a molecular weight of 3 to 130 Da.
4. The grease-producing inhibiting composition according to claim 1, wherein the mass ratio of zinc hyaluronate to ectoin or its derivative is 1:1-3.
5. The composition for inhibiting the formation of oil and fat according to claim 1, wherein the composition comprises zinc hyaluronate and ectoine or a derivative thereof.
6. The composition for inhibiting the formation of fat or oil according to claim 1, wherein the exendin or the derivative thereof is one or more selected from the group consisting of exendin, exendin methyl ester and hydroxyexendin.
7. A skin care product comprising the lipid production inhibiting composition according to any one of claims 1 to 6.
8. The skin care product according to claim 7, wherein the content of the fat-production-inhibiting composition in the skin care product is 0.01 to 1wt%.
9. Use of a composition comprising zinc hyaluronate and exendin or a derivative thereof in the manufacture of a skin care product or medicament for inhibiting fat, said zinc hyaluronate to exendin or a derivative thereof having a mass ratio of 1:0.1-3.
10. The use according to claim 9, wherein the molecular weight of the zinc hyaluronate is greater than 1 kiloda.
11. The use according to claim 10, characterized in that the molecular weight of the zinc hyaluronate is 3-130 Da.
12. The use according to claim 9, wherein the mass ratio of zinc hyaluronate to ectoin or its derivative is 1:1-3.
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