CN117717485A - Composition containing ectoine and raffinose and application thereof - Google Patents

Composition containing ectoine and raffinose and application thereof Download PDF

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Publication number
CN117717485A
CN117717485A CN202311638673.5A CN202311638673A CN117717485A CN 117717485 A CN117717485 A CN 117717485A CN 202311638673 A CN202311638673 A CN 202311638673A CN 117717485 A CN117717485 A CN 117717485A
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CN
China
Prior art keywords
raffinose
composition
retinol
ectoin
exendin
Prior art date
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Pending
Application number
CN202311638673.5A
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Chinese (zh)
Inventor
张亚
孙欣
王瑞妍
曲文杰
温亮亮
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Beijing Huaxi Rongxi Biotechnology Research Co ltd
Bloomage Biotech Co Ltd
Original Assignee
Beijing Huaxi Rongxi Biotechnology Research Co ltd
Bloomage Biotech Co Ltd
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Application filed by Beijing Huaxi Rongxi Biotechnology Research Co ltd, Bloomage Biotech Co Ltd filed Critical Beijing Huaxi Rongxi Biotechnology Research Co ltd
Priority to CN202311638673.5A priority Critical patent/CN117717485A/en
Publication of CN117717485A publication Critical patent/CN117717485A/en
Pending legal-status Critical Current

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Abstract

The present application provides a composition comprising ectoine and raffinose and its use in reducing retinol irritation, reducing the increase in the percutaneous water loss value due to retinol, or repairing retinol-induced skin barrier damage. The composition of the application comprises the ectoin and the raffinose, so that the irritation of retinol to skin can be reduced, and compared with the ectoin monomer and the raffinose monomer, the composition has obvious difference in statistical sense, which shows that the combination of the ectoin monomer and the raffinose monomer has synergistic effect, and the damage of skin barrier can be obviously improved.

Description

Composition containing ectoine and raffinose and application thereof
Technical Field
The application belongs to the technical field of cosmetics, and particularly relates to a composition containing ectoine and raffinose and application thereof in reducing retinol irritation, reducing increase of percutaneous water loss value or repairing skin barrier injury.
Background
The retinoid acid compound is a vitamin a derivative and comprises two sources of natural and synthetic, and has wide biological application prospects, including cancer treatment, cervical tumor and the like, wherein the most prominent application direction is skin disease treatment, and the treatment of actinic keratosis, psoriasis and ichthyosis has been reported since 1940s is used for acne treatment for the first time. Subsequently, retinoid substances, which mainly include retinol, retinol palmitate, retinol propionate, retinol acetate and the like, are increasingly used in the cosmetic field for anti-wrinkle efficacy. Although the above-mentioned substances have excellent anti-wrinkle effects, the irritation to the skin is not neglected, common irritation after application includes stinging, erythema, burning, allergy, and the like, and phototoxicity generated by decomposition through ultraviolet irradiation also causes strong irritation. The direct impact of these skin problems is an impaired skin barrier, such as an increased percutaneous water loss (TEWL) value, and a reduced expression of associated barrier-associated proteins.
Retinol is favored by consumers as a powerful anti-wrinkle ingredient in cosmetics, but is limited in application process because of great irritation to skin, causing problems of skin allergy, redness, stinging and the like, and further causing damage to skin barrier.
Disclosure of Invention
In response to the problems of the prior art, the present application provides a composition comprising ectoin and raffinose and its use in reducing retinol irritation, reducing the increase in transdermal water loss value, or repairing skin barrier damage.
In particular, the present application relates to the following:
1. a composition comprising ectoin and raffinose.
2. The composition according to item 1, wherein the mass ratio of the exendin to the raffinose is (0.1-10): 1.
3. The composition according to item 1 or 2, wherein the mass ratio of exendin to raffinose is (0.5-9): 1.
4. The composition according to any one of claims 1 to 3, wherein the content of ectoin in the composition is 0.05wt% to 5wt% and the content of raffinose is 0.05wt% to 5wt%.
5. The composition of any one of items 1-4, wherein the composition further comprises retinol.
6. The composition of item 5, wherein the composition further comprises one or more of a humectant, an emulsifier, a thickener, a pH adjustor, and a chelating agent.
7. Use of the composition of any one of items 1-6 to reduce retinol irritation, reduce the increase in transdermal water loss value, and/or repair skin barrier damage.
8. The use according to item 7, wherein the increase in the percutaneous water loss value is an increase in the percutaneous water loss value caused by retinol, and the skin barrier damage is a repair of a retinol-caused skin barrier damage.
9. Use of a combination of ectoin and raffinose for reducing retinol irritation, reducing the increase in transdermal water loss values, and/or repairing skin barrier damage.
10. The use according to item 9, wherein the increase in the percutaneous water loss value is an increase in the percutaneous water loss value caused by retinol, and the skin barrier damage is a repair of a retinol-caused skin barrier damage.
11. The use according to item 10, wherein the mass ratio of the exendin to the raffinose is (0.1-10): 1.
12. The use according to item 10 or 11, wherein the mass ratio of exendin to raffinose is (0.5-9): 1.
The composition of the application comprises the ectoin and the raffinose, so that the irritation of retinol to skin can be reduced, and compared with the ectoin monomer and the raffinose monomer, the composition has obvious difference in statistical sense, which shows that the combination of the ectoin monomer and the raffinose monomer has synergistic effect, and the damage of skin barrier can be obviously improved.
Drawings
FIG. 1 shows the TEWL differences for each monomer and different blend compositions.
Detailed Description
The present application is further illustrated below with reference to examples, it being understood that the examples are for further illustration and explanation of the application only and are not intended to limit 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 invention, 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 present application is further illustrated below in conjunction with specific examples, but is not intended to limit the scope of the present application.
The present application provides a composition comprising ectoin and raffinose.
In a specific embodiment, the mass ratio of ectoin to raffinose in the composition is (0.1-10): 1, the number of the components is 1, for example, 0.1:1 may be provided as 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, 1.4:1, 1.6:1, 1.7:1, 1.8:1, 1.9:1, 2:1, 2.1:2:1, 2.7:1, 2.8:1, 2.9:1, 2.1, 2.6:1, 2.7:1, 2.8:1, 2.1, 2:1, 2.9:1, 3:1, 3.1:1, 3.2:1, 3.4:1, 3.5:1, 3:1, 3.1, 3:1, 4:1, 6:1, 1.1, 6:1, 1, 1.1, 6:1, 1.1:1, 6:1, 1.1, 1:1, 6:1, 1.1, 6:1, 1, 1.1:1:1, 6:1, 1:1, 6:1, 1.1:1, 6:1, 1:1, 6:1, 9:1, 9:1:1, 6:1, 1, 6:1:1, 3:1, 3:1:1, 3:1 1, 3 21, 31, 31, 1, 1, 1 and any range between these values.
In a specific embodiment, the mass ratio of exendin to raffinose in the composition is (0.5-9): 1.
In a specific embodiment, the mass ratio of exendin to raffinose in the composition is (0.5-8.1): 1.
In a specific embodiment, the content of the ectoin in the composition is 0.05wt% to 5wt%, for example, it may be 0.05wt%, 0.06wt%, 0.07wt%, 0.08wt%, 0.09wt%, 0.1wt%, 0.2wt%, 0.3wt%, 0.4wt%, 0.5wt%, 0.6wt%, 0.7wt%, 0.8wt%, 0.9wt%, 1wt%, 1.1wt%, 1.2wt%, 1.3wt%, 1.4wt%, 1.5wt%, 1.6wt%, 1.7wt%, 1.8wt%, 1.9wt%, 2wt%, 2.1wt%, 2.2wt%, 2.3wt%, 2.4wt%, 2.5wt%, 2.6wt%, 2.7wt%, 2.8wt%, 2.9wt%, 3wt%, 3.1wt%, 3.2wt%, 3.3wt%, 3.4wt%, 3.5wt%, 3.6wt%, 3.7wt%, 3.8wt%, 3.9wt%, 4.1wt%, 4.2wt%, 4.3wt%, 4.4wt%, 4.5wt%, and any of these ranges; the raffinose content is 0.05wt% to 5wt%, and may be, for example, 0.05wt%, 0.06wt%, 0.07wt%, 0.08wt%, 0.09wt%, 0.1wt%, 0.2wt%, 0.3wt%, 0.4wt%, 0.5wt%, 0.6wt%, 0.7wt%, 0.8wt%, 0.9wt%, 1wt%, 1.1wt%, 1.2wt%, 1.3wt%, 1.4wt%, 1.5wt%, 1.6wt%, 1.7wt%, 1.8wt%, 1.9wt%, 2wt%, 2.1wt%, 2.2wt%, 2.3wt%, 2.4wt%, 2.5wt%, 2.6wt%, 2.7wt%, 2.8wt%, 2.9wt%, 3wt%, 3.1wt%, 3.2wt%, 3.3wt%, 3.5wt%, 3.6wt%, 3.7wt%, 3.8wt%, 3.9wt%, 4wt%, 4.4wt%, and any of these ranges between these values of 4.4wt%, 4wt%, 4.8wt%, 4wt%, and 3.8 wt%.
In a specific embodiment, the mass ratio of the exendin to the raffinose in the composition is (0.1-10): 1, the content of the exendin is 0.05wt% to 5wt%, and the content of the raffinose is 0.05wt% to 5wt%.
In a specific embodiment, the mass ratio of the exendin to the raffinose in the composition is (0.5-9): 1, the content of the exendin is 0.05wt% to 5wt%, and the content of the raffinose is 0.05wt% to 5wt%.
In a specific embodiment, the mass ratio of the exendin to the raffinose in the composition is (0.5-8.1): 1, the content of the exendin is 0.05-5 wt%, and the content of the raffinose is 0.05-5 wt%.
It will be appreciated by those skilled in the art that the compositions of the present application may further comprise other ingredients, such as solvents or other excipients, in addition to the exendin and raffinose.
In a specific embodiment, the composition consists of ectoin and raffinose.
In a specific embodiment, the composition consists of exendin and raffinose in a mass ratio of (0.1-10): 1.
In a specific embodiment, the composition consists of exendin and raffinose in a mass ratio of (0.5-9): 1.
In a specific embodiment, the composition consists of exendin and raffinose in a mass ratio of (0.5-8.1): 1.
The composition of any of the above may further comprise retinol.
One skilled in the art will appreciate that the composition may further comprise one or more of a humectant, an emulsifier, a thickener, a pH modifying agent, a chelating agent.
The present application also provides the use of any of the above compositions for reducing retinol irritation.
The present application also provides the use of any of the above compositions for reducing the increase in the transdermal water loss value.
Further, the percutaneous water loss value is a retinol-induced percutaneous water loss value.
The present application also provides the use of any of the above compositions in the repair of skin barrier damage.
Further, the skin barrier damage is retinol-induced skin barrier damage.
In the present application, the percutaneous Water loss (TEWL) value is measured by methods and apparatus known in the art, e.g., CK, germanyTM Hex or related instrument. The principle of Tewameter to determine TEWL value derives from Fick's law of diffusion:
dm/dt- -the amount of water evaporated per hour, D- -the diffusion constant, A- -the test area, dp/dx- -the pressure difference between the upper and lower sensors, mmHg.
The present application also provides the use of a combination of ectoin and raffinose in reducing retinol irritation.
In a specific embodiment, the mass ratio of exendin to raffinose in the use is (0.1-10): 1.
In a specific embodiment, the mass ratio of exendin to raffinose in the use is (0.5-9): 1.
In a specific embodiment, the mass ratio of exendin to raffinose in the use is (0.5-8.1): 1.
The present application also provides the use of a combination of ectoin and raffinose in decreasing the increase in the transdermal water loss value.
In a specific embodiment, the mass ratio of exendin to raffinose in the use is (0.1-10): 1.
In a specific embodiment, the mass ratio of exendin to raffinose in the use is (0.5-9): 1.
In a specific embodiment, the mass ratio of exendin to raffinose in the use is (0.5-8.1): 1.
The present application also provides the use of a combination of ectoin and raffinose in repairing skin barrier damage.
In a specific embodiment, the mass ratio of exendin to raffinose in the use is (0.1-10): 1.
In a specific embodiment, the mass ratio of exendin to raffinose in the use is (0.5-9): 1.
In a specific embodiment, the mass ratio of exendin to raffinose in the use is (0.5-8.1): 1.
The compositions of the present application are effective in reducing skin irritation by combining exendin and raffinose, especially in specific mass ratios, e.g., in a mass ratio of (0.1-10): 1, and are statistically significantly different from monomeric exendin and monomeric raffinose, indicating that the combination has a synergistic effect, which significantly improves skin barrier damage.
Examples
The reagents and apparatus used in the examples and comparative examples of the present application are shown in table 1.
TABLE 1
Example 1
The composition of this example comprises raffinose 0.67g and exendin 0.33g and is prepared by the following steps:
0.35g of carbomer U20 is weighed into a 200mL beaker, then 0.67g of raffinose powder, 0.33g of ectoin, 7.5g of glycerin and 0.1g of disodium ethylenediamine tetraacetate are weighed into the beaker, a certain amount of deionized water is continuously added into the beaker, and the mixture is stirred at 75-80 ℃ to obtain phase A. 0.5g of p-hydroxyacetophenone and 0.5g of 1, 2-hexanediol are weighed into a small beaker and stirred under heating at 60-70 ℃ until completely dissolved, thus obtaining phase B. 10g of retinol and 0.5g of LRI (PEG-40 hydrogenated castor oil, PPG-26 butanol polyether 26) are weighed, heated and stirred at 75-80 ℃ until dissolved, to obtain phase C. Adding the phase C into the phase A under the heating condition of 75-80 ℃, dispersing for 5-10 min by a dispersing machine, cooling to about 40 ℃, adding the phase B into the mixed solution, and regulating the pH of the system to about 6.1 by adopting a 1% NaOH aqueous solution to obtain emulsion. The mass of the emulsion finally obtained was 100g.
Examples 2 to 5
Examples 2-5 differ from example 1 only in the amounts of exendin and raffinose added, but the total amounts of exendin and raffinose are the same. In example 2, the amount of exendin was 0.5g and the amount of raffinose was 0.5g. In example 3, the amount of exendin was 0.89g and the amount of raffinose was 0.11g. In example 4, the amount of exendin was 0.09g and the amount of raffinose was 0.91g. In example 5, the amount of exendin was 0.91g and the amount of raffinose was 0.09g.
Comparative example 1
Comparative example 1 differs from example 1 only in that no ectoin and raffinose were added.
Comparative example 2
Comparative example 2 differs from example 1 only in that raffinose was not added and that the addition amount of exendin was 1g.
Comparative example 3
Comparative example 3 differs from example 1 only in that no ectoin was added and that the amount of raffinose added was 1g.
The contents of the respective components in the above examples and comparative examples are shown in Table 2.
TABLE 2
Test examples
In the test example, firstly, retinol and active substances are simultaneously added into basic emulsion at the inner side of the forearm of a human body, a barrier damage model is manufactured by continuously using an emulsion sample, and after the model is successfully manufactured, the change of TEWL (test wl) of each smearing part is monitored, wherein the increase of the TEWL value represents the increase of percutaneous water loss, which indicates that the barrier function is damaged; a decrease in TEWL value represents a decrease in transdermal water loss, indicating skin barrier repair. Since the TEWL values are different for each different part of the skin, background effects are subtracted by calculating the TEWL difference by subtracting the pre-use TEWL value from the post-use TEWL value and comparing the tewil difference to account for the significance of the differences between groups.
(1) Screening of retinol sensitive populations
1g of emulsion sample containing retinol only (i.e. the sample of comparative example 1) was applied to the forearm of the subject, and the application was performed uniformly for 20 times, 1 time each in the morning and at night, and 2 days in succession, subjects with tingling, burning and pain feedback were selected, wherein 8 subjects satisfying the standard were selected in total, 8 women were aged 21 to 31 years, and the average age was 25.88.+ -. 1.17 years.
(2) TEWL test
Firstly, the inner side of the forearm of a subject is washed by clean water, wiped clean by paper towels, and is kept for 30min in a constant temperature and constant humidity environment (the temperature is 20-22 ℃ and the humidity is 40-60%). The medial forearm score of the subject was divided into 7 square areas each 1.5cm x 1.5cm in size. Then useTM Hex test of TEWL values before applying samples to each area 7 areas were applied with 1g of the different samples of examples 1-5 and comparative examples 2-3, respectively, looped 20 times until complete absorption, each time in the morning and evening, 2 consecutive days, day 3, and each area TEWL value was tested.
The collected data are collated and the variability is analyzed by statistical methods. The test results are shown in table 3 and fig. 1, where x represents statistically significant differences (p < 0.05) from monomeric ectoin comparison, and statistically significant differences (p < 0.05) from monomeric raffinose comparison consistent with the above trend.
TABLE 3 Table 3

Claims (10)

1. A composition comprising ectoin and raffinose.
2. The composition according to claim 1, wherein the mass ratio of the exendin to the raffinose is (0.1-10): 1.
3. The composition according to claim 1 or 2, wherein the mass ratio of exendin to raffinose is (0.5-9): 1.
4. A composition according to any one of claims 1-3, wherein in the composition the content of ectoin is 0.05-5 wt% and the content of raffinose is 0.05-5 wt%.
5. The composition of any one of claims 1-4, wherein the composition further comprises retinol.
6. The composition of claim 5, wherein the composition further comprises one or more of a humectant, an emulsifier, a thickener, a pH adjuster, a chelating agent.
7. Use of the composition of any one of claims 1-6 for reducing retinol irritation, reducing the increase in transdermal water loss value, and/or repairing skin barrier damage.
8. Use of a combination of ectoin and raffinose for reducing retinol irritation, reducing the increase in transdermal water loss values, and/or repairing skin barrier damage.
9. The use according to claim 8, wherein the mass ratio of escin to raffinose is (0.1-10): 1.
10. Use according to claim 8 or 9, wherein the mass ratio of ectoin to raffinose is (0.5-9): 1.
CN202311638673.5A 2023-12-01 2023-12-01 Composition containing ectoine and raffinose and application thereof Pending CN117717485A (en)

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Application Number Priority Date Filing Date Title
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Publications (1)

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CN117717485A true CN117717485A (en) 2024-03-19

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