A whitening composition, use and cosmetic product suitable for sensitive skin

Abstract

The present invention belongs to the field of new daily chemical materials, and discloses a whitening composition suitable for sensitive skin and its application. The whitening composition is added to the application formula in a proportion of 1-30 wt%, and the whitening composition includes a whitening component and an anti-allergic component; the whitening component is composed of tranexamic acid and diglucosyl gallic acid; the anti-allergic component is composed of β-glucan, Illicium lanceolatum A. C. Smith leaf extract, and oat kernel extract. The composition includes a whitening component and an anti-allergic component. The whitening component is mainly mild tranexamic acid, and by compounding with diglucosyl gallic acid, it can prevent the generation and transfer of melanin and prevent pigmentation. At the same time, the present invention adopts an anti-allergic component containing Illicium lanceolatum A. C. Smith leaf extract, β-glucan, and oat kernel extract to achieve functions such as anti-allergy and anti-inflammation; more importantly, when these two components are compounded together, it will not weaken the efficacy of the whitening component, but on the contrary, it will significantly promote the efficacy of the whitening component. At the same time, the present invention also provides the uses and cosmetics of the composition.

Description

Technical Field

[0001] The present invention relates to the field of new daily chemical materials, and specifically to a composition, uses, and cosmetics. Background Art

[0002] Whitening cosmetics suitable for sensitive skin are a very challenging product in the industry; although there are many products on the market that claim to be suitable for sensitive skin and have whitening functions, many products are either not mild enough or have poor whitening effects.

[0003] In fact, the root cause of the above problems is that due to the characteristics of sensitive skin itself, it is more likely to cause pigment deposition due to factors such as infection and irritation; at the same time, sensitive skin itself is intolerant to most whitening active ingredients; embarrassingly, the stronger the efficacy of the whitening active ingredients, the stronger the irritation; so the final result is the extensive use of anti-allergic active ingredients, and the excessive use of anti-allergic active ingredients often inhibits the performance of whitening active ingredients.

[0004] In some extreme cases, the whitening process of sensitive skin will become darker instead of lighter.

[0005] CN113576933A discloses a composition with whitening efficacy, its preparation method and applications, which specifically includes the following components: α-hydroxy acid, resorcinol derivatives, ascorbic acid and its derivatives, tranexamic acid, and gallic acid and its derivatives; the gallic acid and its derivatives include at least one of diglucosyl gallic acid, gallic acid, propyl gallate, ethylhexyl gallate, and ellagic acid.

[0006] The problems of the above solution are: the amount of whitening active ingredients used is too much, and there are as many as 5 kinds of whitening active ingredients, namely α-hydroxy acid, resorcinol derivatives, ascorbic acid and its derivatives, tranexamic acid, and gallic acid and its derivatives;

[0007] Except for tranexamic acid which has mildness, the irritation of other substances is generally stronger than that of tranexamic acid.

[0008] Therefore, the technical problem to be solved in this case is: how to develop a composition suitable for sensitive skin with good whitening effect. Summary of the Invention

[0009] The object of the present invention is to provide a whitening composition suitable for sensitive skin and its application. The addition ratio of the composition formula is 1-30 wt%, and the composition includes a whitening component and an anti-allergy component. The whitening component is mainly mild tranexamic acid, and by compounding with diglucosyl gallic acid, it can prevent the transfer and generation of melanin and prevent pigmentation. At the same time, the present invention adopts an anti-allergy component containing Illicium lanceolatum A. C. Smith extract, β-glucan, and oat kernel extract to achieve functions such as anti-allergy and anti-inflammation. More importantly, when these two components are compounded together, it will not weaken the efficacy of the whitening component. On the contrary, it will significantly promote the efficacy of the whitening component.

[0010] At the same time, the present invention also provides the use and cosmetics of the composition.

[0011] To achieve the above object, the present invention provides the following technical solutions:

[0012] A whitening composition suitable for sensitive skin, which is added to the application formula at a ratio of 1-30 wt%, and the whitening composition includes a whitening component and an anti-allergy component;

[0013] The whitening component is composed of tranexamic acid and diglucosyl gallic acid;

[0014] The anti-allergy component is composed of β-glucan, Illicium lanceolatum A. C. Smith extract, and oat kernel extract;

[0015] The contents of each component in the whitening composition are as follows:

[0016] Tranexamic acid 0.2-20 wt%;

[0017] Diglucosyl gallic acid solution with a concentration of 1-4.99 wt% 0.1-10 wt%;

[0018] β-glucan solution with a concentration of 1 wt% 0.05-5 wt%;

[0019] Illicium lanceolatum A. C. Smith extract solution with a concentration of 0.4-2 wt% 0.1-10 wt%;

[0020] Oat kernel extract solution with a concentration of 5 wt% 0.02-2 wt%;

[0021] The balance is water.

[0022] Tranexamic acid prevents ultraviolet-induced pigmentation by interfering with the structure of plasminogen and preventing the binding of plasminogen to the lysine site of keratinocytes, thereby achieving the effect of lightening age spots. Tranexamic acid has high safety, few adverse reactions, good curative effect, and has a good treatment effect on chloasma.

[0023] Diglucosyl gallic acid: Trihydroxybenzoic acid is a natural and potent tyrosinase inhibitor with excellent antioxidant effects. Using biotechnology, diglucosyl gallic acid converts unstable trihydroxybenzoic acid into highly stable and water-soluble diglucosyl gallic acid. In the skin, it can cleave the glucose bond through α-glucosidase to release trihydroxybenzoic acid, achieving a whitening effect. Diglucosyl gallic acid has multiple functions, including reducing free radicals, inhibiting the generation of Nf-KB, inhibiting PEG2, preventing DNA damage, inhibiting tyrosinase activity, preventing melanin transfer, and inhibiting MITF activity. It is an effective ingredient that can prevent skin allergies and whiten the skin. When applied to sensitive skin, its dosage needs to be carefully controlled.

[0024] In the formulation of the present invention, the dosage of diglucosyl gallic acid is as low as 1‰ or less. By using a large amount of tranexamic acid, the whitening effect can be maximized, and at the same time, it will not show irritation after the appropriate use of anti-allergic agents.

[0025] β-Glucan has good moisturizing, anti-inflammatory, and antioxidant abilities.

[0026] The extract of Illicium lanceolatum A. C. Smith mainly contains various active ingredients such as flavonoids and phenolic acids, and has good moisturizing, antioxidant, anti-inflammatory, soothing and other effects.

[0027] The extract of oat kernel is a natural active ingredient derived from oat kernel, and has all-round activities such as strong anti-inflammatory and antipruritic, antihistamine, anti-erythema, and reducing inflammatory factors IL-6 and IL-8. It is an excellent skin anti-allergic agent.

[0028] All of the above three have good anti-inflammatory and antioxidant functions, and are active ingredients of cosmetics with anti-allergic functions commonly used in the art.

[0029] After experiments, it was found that when the above three components are used in combination, the risk of skin allergy caused by the large amount of tranexamic acid can be reduced. Compared with other anti-allergic agents, the combination of the above three anti-allergic agents can still achieve an inhibition rate of more than 30% on the activity of hyaluronidase even at the lowest addition amount of the composition. At the same time, the composition can increase the melanin generation inhibition rate by 2-10%.

[0030] In the above-mentioned whitening composition, the trade name of the diglucosyl gallic acid solution with a concentration of 1-4.99 wt% is Brightenyl.

[0031] The trade name of the β-glucan solution with a concentration of 1 wt% is Hydrasensyl Glucan Green.

[0032] The trade name of the extract of Illicium lanceolatum A. C. Smith with a concentration of 0.4-2 wt% is TAZMAN PEPPER TM C.

[0033] In the above-mentioned whitening composition, the contents of the components in the whitening composition are as follows:

[0034] Tranexamic acid: 0.5 - 10 wt%;

[0035] Diglucosyl gallic acid solution with a concentration of 1 - 4.99 wt%: 0.2 - 5 wt%;

[0036] β-Glucan solution with a concentration of 1 wt%: 0.1 - 4 wt%;

[0037] Illicium lanceolatum A. C. Smith extract solution with a concentration of 0.4 - 2 wt%: 0.5 - 6 wt%;

[0038] Oat kernel extract solution with a concentration of 5 wt%: 0.1 - 1 wt%;

[0039] The balance is water.

[0040] Meanwhile, the present invention also discloses the use of the whitening composition described above in any one of the preceding paragraphs for preparing cosmetics.

[0041] Finally, the present invention also discloses a whitening cosmetic suitable for sensitive skin, containing the whitening composition described above in any one of the preceding paragraphs. Preferably, the whitening cosmetic is one of aqueous solution, essence, emulsion, cream, and facial mask.

[0042] Compared with the prior art, the beneficial effects of the present invention are as follows:

[0043] The composition formula of the present invention is applied at an addition ratio of 1 - 30 wt%. The composition includes a whitening component and an anti-allergic component. The whitening component is mainly mild tranexamic acid. By compounding diglucosyl gallic acid, it realizes preventing the transfer and generation of melanin and preventing pigmentation. At the same time, the present invention adopts an anti-allergic component containing Illicium lanceolatum A. C. Smith extract, β-glucan, and oat kernel extract to realize functions such as anti-allergy and anti-inflammation; more importantly, when these two components are compounded together, it does not weaken the efficacy of the whitening component. On the contrary, it significantly promotes the efficacy of the whitening component. Detailed implementation mode

[0044] The following will clearly and completely describe the technical solutions of the present invention in conjunction with the embodiments of the present invention. Obviously, the described embodiments are only a part of the embodiments of the present invention, rather than all of the embodiments. All other embodiments obtained by those of ordinary skill in the art based on the embodiments of the present invention without making creative efforts shall fall within the protection scope of the present invention.

[0045] Description of raw material sources:

[0046] Raw material 1: Hydrasensyl Glucan Green

[0047] Composition: water 96.5 wt%; 1,2-pentanediol 2 wt%; β-glucan 1 wt%; octyldecanol 0.5 wt%;

[0048] Raw material 2: Tranexamic acid

[0049] Composition: tranexamic acid 100%;

[0050] Raw material 3: Brightenyl

[0051] Composition: glycerol 50 - 100 wt%; water 25 - 49.99 wt%; diglucosyl gallic acid 1 - 4.99 wt%, total 100%;

[0052] Raw material 4: TAZMAN PEPPER TM C

[0053] Composition: glycerol 65 - 75 wt%; water 27.8 - 29.8 wt%; leaf extract of Tasmannia lanceolata 0.4 - 2 wt%, total 100%;

[0054] Raw material 5: Avena sativa alkaloids

[0055] Composition: extract of Avena sativa kernel 5 wt%; butanediol 25 wt%; 1,2-pentanediol 20 wt%; water 50 wt%.

[0056] Among the above components, taking the products represented by the trade names as the standard, the above component ranges are only the data recorded in the specifications provided by the supplier.

[0057] Screening of the first part of whitening components

[0058] In the previous experiments, a combination screening was carried out for various whitening components. Considering that tranexamic acid itself has the characteristic of being non-irritating when used in large amounts, tranexamic acid was selected as the main whitening active ingredient. Combining the addition ratio of the composition in the formula, by compounding different types and dosages of whitening components, a combination with better whitening effect was screened;

[0059] The specific preparation method is: adding the selected whitening ingredients into deionized water (some raw materials that are not easy to dissolve can be pretreated first), and mixing evenly.

[0060] The specific formula refers to Table 1; in Table 1, the dosage of tranexamic acid is 1 wt%, and the dosages (net content) of other components are all 0.1 wt‰, and the balance is water; √ in Table 1 indicates that this example contains this substance.

[0061] Table 1 Formula table

[0062]

[0063]

[0064] Performance test: In vitro test of B16 cell melanin synthesis inhibition for cosmetics, T / SHRH 027-2019;

[0065] In this test, the positive control was kojic acid (200 μg / mL).

[0066] Samples The samples of each embodiment of the present invention were diluted 100,000 times.

[0067] The test results are shown in Table 2 below;

[0068] Table 2 Test Results

[0069] Inhibition rate ± standard deviation (%) Example 1 7.23±1.28 Example 2 12.41±1.54 Example 3 7.46±2.24 Example 4 6.96±2.11 Example 5 13.12±1.85 Example 6 8.56±1.13 Example 7 14.05±1.66 Example 8 7.14±1.27 Example 9 9.17±1.2 Example 10 13.82±0.78 Example 11 6.43±0.83 Example 12 6.41±0.78 NC 0±2.19 PC 30.1±1.23

[0070] Result analysis:

[0071] Through the above experiments, it was found that Examples 2, 5, 7, and 10 had good effects; in the subsequent third part, further experiments were carried out using the above 4 combinations.

[0072] Second part Screening of anti-allergic components

[0073] In the previous experiments, it has been verified that β-glucan and the solution containing more β-glucan and oat kernel extract have the basic functions of anti-inflammatory, anti-allergic and building skin barrier as anti-allergic components. In order to further improve the anti-allergic ability of these two, a variety of anti-allergic components were screened, and the performance trend of the composition was judged by detecting the inhibition rate of hyaluronidase activity.

[0074] Its specific formula refers to Table 3; in Table 3, the dosage of Hydrasensyl Glucan Green is 1 wt%, the dosage of oat alkaloid is 0.5 wt%, the dosage of other anti-allergic components is 0.5 wt%, and the balance is water; √ in Table 3 indicates that this example contains this substance.

[0075] Its specific preparation method is: add the selected anti-allergic components to deionized water and mix evenly.

[0076] Table 3 Formulation table

[0077]

[0078] The test method for the inhibition rate of hyaluronidase activity is: T / JSRH003~2023;

[0079] Dilute the sample 10 times with acetate buffer solution and then test.

[0080] The test results are shown in Table 4 below;

[0081] Table 4 Test Results

[0082]

[0083]

[0084] Result analysis:

[0085] From the tests in Table 4 above, it can be seen that Examples 13, 15, and 16 have good effects; in the subsequent third part, further experiments will be carried out using the above 3 combinations.

[0086] Screening of the Optimal Combinations in the Third Part

[0087] Fix tranexamic acid (1 wt%), Hydrasensyl Glucan Green (1 wt%), and avenanthramides (0.5 wt%) in the formula, and add additional whitening ingredients (0.1 wt‰, net content) (some poorly soluble raw materials can be pretreated first) and anti-allergy ingredients (0.5 wt%) to the formula, with the balance being water. For the specific formula, refer to Table 5; a tick in Table 5 indicates that the example contains the substance.

[0088] Table 5 Formula Table

[0089]

[0090]

[0091] Performance test: In vitro test of the cosmetic on B16 cell melanin synthesis inhibition experiment (refer to the first part)

[0092] The test results are shown in Table 6;

[0093] Table 6 Test Results

[0094] Inhibition rate ± standard deviation (%) Example 19 12.21±1.19 Example 20 13.04±1.27 Example 21 11.95±1.86 Example 22 17.02±2.03 Example 23 14.27±1.2 Example 24 13.68±1.62 Example 25 15.12±1.48 Example 26 14.22±0.87 Example 27 13.63±1.43 Example 28 12.96±0.88 Example 29 14.28±2.21 Example 30 14.8±1.82 NC 0±1.77 PC 30.32±1.42

[0095] Result analysis:

[0096] 1. From Examples 2, 19 to 21, it can be seen that Hydrasensyl Glucan Green, avenanthramides, and Illicium lanceolatum A. C. Smith extract or Portulaca oleracea L. extract or dipotassium glycyrrhizinate have no promoting effect on the inhibition of cell melanin synthesis by whitening ingredients;

[0097] 2. From Examples 5, 22 to 24, it can be seen that Illicium lanceolatum A. C. Smith extract and Portulaca oleracea L. extract have a promoting effect on the inhibition of cell melanin synthesis by the combination of tranexamic acid and diglucosyl gallic acid.

[0098] 3. As can be seen from Example 7, Examples 25 to 27, the extract of Illicium lanceolatum A. C. Smith has a promoting effect on inhibiting the synthesis of cellular melanin for the combination of tranexamic acid and arbutin.

[0099] 4. As can be seen from Example 10, Examples 28 to 30, the extract of Portulaca oleracea L. and dipotassium glycyrrhizinate has a promoting effect on inhibiting the synthesis of cellular melanin for the combination of tranexamic acid and resveratrol.

[0100] Based on the above results, the extract of Illicium lanceolatum A. C. Smith has the largest promoting amplitude on inhibiting the synthesis of cellular melanin for the combination of tranexamic acid and diglucosyl gallic acid. Therefore, this combination is used for subsequent experiments.

[0101] Part Four: Functional Verification of Example 21

[0102] Based on the above functional verification, further extended performance experiments are carried out for Example 22 to verify the effectiveness of Example 22. Considering the production cost - benefit, the inhibition rate of melanin synthesis and the inhibitory effect on hyaluronidase are compared for the highest 30% addition amount of all components in the composition (Example 31), higher proportion addition amounts of different components in the composition (Examples 32 - 35), and the lowest 1% addition amount of all components in the composition (Example 36).

[0103] Use the formula shown in Table 7;

[0104] Table 7 Formula Table Unit: g

[0105]

[0106]

[0107] The above Table 7 is tested for the inhibition rate of hyaluronidase activity and the in - vitro test of inhibiting melanin synthesis in B16 cells of cosmetics; to judge its performance changes, the specific results are shown in Table 8;

[0108] Table 8 Test Results

[0109]

[0110] Result Analysis:

[0111] Examples 34 and 35 showed the best inhibitory effect on cell melanin synthesis. Although the test product in Comparative Example 36 had an inhibitory effect on melanin synthesis and hyaluronidase activity, the values were relatively low. The possible reasons are as follows: 1. The dosage of tranexamic acid / Brightenyl (diglucosyl gallic acid) in Examples 34 and 35 was relatively large, which increased the inhibition rate; 2. As can be seen from Examples 22 and 25 above, the extract of Illicium lanceolatum A. C. Smith had a certain synergistic effect on inhibiting cell melanin synthesis for some whitening components. At the same time, in Example 34, the dosage of the extract of Illicium lanceolatum A. C. Smith was the largest, so it showed the best inhibitory effect. Of course, due to the existence of multiple variables in Examples 31 to 36 above, the above explanation is only an inference.

[0112] Although there were performance differences in Example 22 and Examples 31 to 35, excessive pursuit of the hyaluronidase inhibition rate was not conducive to the screening of whitening performance; from a research and development perspective, we hoped to have a better whitening effect under the condition of ensuring low irritation. Example 31 had achieved an ideal effect in terms of overall performance. Therefore, based on the experimental results of Examples 31 to 36 and combined with the market positioning, the formula performance protected by the present invention had comprehensive performance advantages and was an optimal combination choice. Moreover, the optimal application addition ratio of the composition formula was 1-30 wt%.

[0113] Fifth part: Application formula

[0114] One application direction of the composition of the present invention is water, essence, lotion, cream, and mask. The application addition ratio of the composition formula is 1-30 wt%. The formula of the essence can be referred to Table 9;

[0115] Table 9: Formula table

[0116]

[0117]

[0118] Its preparation method is as follows:

[0119] (1) Inject accurately weighed water into a clean and disinfected production tank, turn on the homogenizer, add the materials in the first process, homogenize until completely dissolved without fine particles, turn on the stirrer, and start heating. During this period, perform multiple homogenizations to ensure that the material is completely dissolved.

[0120] (2) Add the materials in the second process to an oil phase pot, start heating, turn on the stirrer, and stir and heat to 83-85 °C until completely dissolved, and set aside.

[0121] (3) Open the vacuum in the production tank, turn on the homogenizer, pump the materials in the second process into the production tank, homogenize for 8-15 min, stir and keep warm for 20-30 min, and then start cooling.

[0122] (4) When the temperature is lowered to 45 °C, start stirring. Use a clean container to stir the materials of the third process until they are completely dissolved and transparent, then add them to the production tank, stir for 10 min, and continue to lower the temperature;

[0123] (5) Add the materials of the fourth process to the production tank, stir for 10 - 20 min until evenly mixed, take samples for inspection, and after passing the inspection, filter and discharge the materials.

[0124] For those skilled in the art, it is obvious that the present invention is not limited to the details of the above exemplary embodiments, and without departing from the spirit or basic characteristics of the present invention, the present invention can be implemented in other specific forms. Therefore, from any point of view, the embodiments should be regarded as exemplary and non-restrictive. The scope of the present invention is defined by the appended claims rather than the above description. Therefore, all changes falling within the meaning and scope of the equivalent elements of the claims are intended to be embraced within the present invention.

Claims

1. A whitening composition suitable for sensitive skin, characterized in that, The whitening composition is added to the application formula at a ratio of 1-30 wt%, and the whitening composition includes a whitening component and an anti-allergy component; The whitening component consists of tranexamic acid and diglucosyl gallic acid; The anti-allergy component consists of β-glucan, Illicium lanceolatum A. C. Smith extract, and oat kernel extract; The contents of each component in the whitening composition are as follows: Tranexamic acid 0.5-10 wt%; Diglucosyl gallic acid solution with a concentration of 1-4.99 wt% 0.2-5 wt%; β-glucan solution with a concentration of 1 wt% 0.1-4 wt%; Illicium lanceolatum A. C. Smith extract solution with a concentration of 0.4-2 wt% 0.5-6 wt%; Oat kernel extract solution with a concentration of 5 wt% 0.1-1 wt%; The balance is water; The commodity name of the diglucosyl gallic acid solution with a concentration of 1-4.99 wt% is Brightenyl; The commodity name of the β-glucan solution with a concentration of 1 wt% is Hydrasensyl Glucan Green; The commodity name of the Illicium lanceolatum A. C. Smith extract with a concentration of 0.4-2 wt% is TAZMAN PEPPER™ C.

2. Use of the whitening composition as claimed in claim 1 for preparing cosmetics.

3. A whitening cosmetic suitable for sensitive skin, characterized in that, Containing the whitening composition as claimed in claim 1.

4. The whitening cosmetic according to claim 3, wherein The whitening cosmetic is one of an aqueous solution, essence, emulsion, cream, and facial mask.

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