Whitening composition as well as application and cosmetic thereof

By combining nicotinamide, 4-butyl resorcinol, citrus peel extract, Tokyo cherry blossom leaf extract and rosea flower fermentation filtrate, the problem of adverse reactions in the inhibition of melanin production has been solved, and more effective whitening effect and safety have been achieved.

CN119632871APending Publication Date: 2025-03-18GUANGZHOU MEIZI BIOTECHNOLOGY CO LTD
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Patent Information

Application Number
CN202411978172.6
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2024-12-31
Publication Date
2025-03-18

AI Technical Summary

Technical Problem

Existing whitening products are prone to adverse reactions when inhibiting melanin production and lack a composition with good whitening ability unlike the prior art.

Method used

The combined action of nicotinamide, 4-butyl resorcinol, citrus peel extract, Tokyo cherry blossom leaf extract and rosea flower fermentation filtrate is enhanced to enhance the inhibition ability of tyrosinase, thereby enhancing the whitening effect.

Benefits of technology

The composition significantly inhibits the activity of tyrosinase, reduces the production of melanin, improves skin tone unevenness, fades the spots, and reduces the risk of adverse reactions to use.

✦ Generated by Eureka AI based on patent content.

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Abstract

The invention belongs to the technical field of cosmetic production, and discloses a whitening composition which is prepared from the following components in parts by mass: 10 to 35 parts of nicotinamide, 12 to 25 parts of 4-butylresorcinol, 0.005 to 0.1 part of citrus peel extract, 0.005 to 0.1 part of oriental cherry leaf extract and 0.005 to 0.1 part of roselle flower fermentation filtrate. According to the whitening composition, the inhibition capability on tyrosinase is further enhanced to reduce the generation of melanin, so that the whitening effect of the composition is enhanced, and in addition, the invention further discloses application of the whitening composition and a cosmetic.
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Description

Technical Field

[0001] The present invention relates to the technical field of cosmetic production, and in particular to a whitening composition and application thereof, and cosmetics. Background Art

[0002] Skin color is affected by a variety of internal and external factors, and actually depends on the amount of melanin and its dispersion in the skin. The skin whitening effect is mainly closely related to the melanin production inhibition activity and free radical scavenging ability. It can also achieve whitening effects by accelerating skin metabolism and stratum corneum shedding. The most important way is to inhibit the production of melanin. Traditional whitening drugs generally reduce the production of melanin by inhibiting the maturation of melanocytes, but they are prone to adverse reactions, including stinging, contact dermatitis, etc. Therefore, most of the whitening products studied in the cosmetics field over the years are to reduce the deposition of melanin by selectively inhibiting the activity of tyrosinase (TYR), while avoiding toxicity to normal mature melanocytes and reducing adverse reactions to use.

[0003] The three main signaling pathways involved in regulating melanogenesis are: (1) melanocortin 1 receptor (Mc1R); (2) Wnt / β-catenin signaling pathway; and (3) tyrosinase receptor KIT / SCF pathway. In the process of melanin formation, the hydroxylation of L-tyrosine to produce L-3,4-dihydroxyphenylalanine (L-DOPA) is the rate-limiting step of the entire process and is catalyzed by tyrosinase. Tyrosinase is the key enzyme in the synthesis of melanin through melanin, and it has become the most significant target for melanin synthesis inhibitors that directly inhibit the catalytic activity of tyrosinase.

[0004] Chinese patent application 201910684895.8 discloses a customized whitening inkjet ink, including a solvent and a whitening and lightening functional substance, wherein the suspension rate of the customized whitening inkjet ink is 50%-100%, preferably 70%-100%, and the particle size of the whitening and lightening functional substance is ≤5μm, preferably ≤1μm. The whitening and lightening functional substance includes one or more of compound whitening and lightening functional substances, extract whitening and lightening functional substances, peptide and enzyme whitening and lightening functional substances, pearl powder, titanium dioxide or silica in any proportion.

[0005] The droplets of this customized whitening inkjet ink are uniform, smooth, delicate and stable. The ink is in solution or evenly dispersed state, and has good adhesion to the membrane cloth. It is used in skin care, repair, beauty or medicinal patches;

[0006] Further observation of paragraph 77 of the specification of the scheme shows that, although the scheme discloses the use of niacinamide and citrus peel extract as whitening ingredients, the scheme does not attempt to use raw materials such as roselle flower fermentation filtrate together with the above ingredients.

[0007] The problem to be solved in this scheme is: how to provide a composition different from the prior art and having good whitening ability. Summary of the invention

[0008] The purpose of the present application is to provide a composition with good whitening ability, and through the combined action of niacinamide, 4-butylresorcinol, citrus peel extract, Tokyo cherry leaf extract, and roselle flower fermentation filtrate, the tyrosinase inhibitory ability of the composition is further enhanced, thereby enhancing the whitening effect of the composition.

[0009] To achieve the above object, the present application provides a whitening composition, which comprises at least the following components by weight:

[0010]

[0011] Niacinamide and 4-butylresorcinol can inhibit the activity of tyrosinase, a key enzyme in the synthesis of melanin. By reducing the activity of tyrosinase, niacinamide reduces the production of melanin, thereby helping to reduce skin spots and improve the uniformity of skin tone;

[0012] Certain components in tangerine peel extract (such as flavonoids) reduce the production of melanin, thereby improving uneven skin tone and fading spots;

[0013] Tokyo Sakura leaf extract is rich in antioxidant ingredients, especially polyphenols and flavonoids. These ingredients not only have good antioxidant capacity, but also reduce the production of melanin, thereby improving uneven skin tone and fading spots.

[0014] Roselle flower is rich in plant polyphenols and anthocyanins, which can inhibit the activity of tyrosinase, thereby reducing the production of melanin. By reducing the synthesis of melanin, Roselle flower ferment filtrate helps to even out skin tone and reduce dark spots.

[0015] Preferably, the composition comprises at least the following components by weight:

[0016]

[0017] Preferably, the roselle flower fermentation filtrate is a fermentation filtrate obtained by fermenting roselle flowers with microorganisms, and the microorganism is lactobacillus.

[0018] Preferably, the method for preparing the roselle flower fermentation filtrate comprises the following steps:

[0019] Step 1: crushing the roselle flowers and performing enzymatic hydrolysis to obtain an enzymatic hydrolyzate;

[0020] Step 2: Mix the enzymatic hydrolysate with peptone, glucose, sodium dihydrogen phosphate and pure water to obtain a culture medium;

[0021] Step 3: inoculate lactobacillus into the culture medium for fermentation, sterilize after fermentation, and centrifuge to obtain the supernatant to obtain the roselle flower fermentation filtrate.

[0022] Preferably, the mass ratio of the enzyme used in step 1 to the roselle flower is 2-8:100, and the enzyme is a mixture of cellulase and lipase, and the mass ratio of cellulase to lipase is 6-8:1.

[0023] Preferably, the lactobacillus used in step 3 is added in the form of a lactobacillus bacterial liquid, and the number of viable bacteria in the lactobacillus bacterial liquid is not less than 1×10 6 CFU / g, and the mass ratio of lactobacillus liquid to enzymatic hydrolysate is 1-3:10.

[0024] In addition, the present application also discloses the use of the whitening composition as described above for preparing cosmetics.

[0025] In addition, the present application also discloses a cosmetic containing 1 to 10 wt % of the whitening composition described above.

[0026] Preferably, the dosage form of the daily chemical product is a patch, an ointment, a liquid, a spray, a gel, an emulsion, or a cream.

[0027] The beneficial effects of the present application are: the nicotinamide and 4-butylresorcinol used in the present application can inhibit the activity of tyrosinase, which is a key enzyme in the synthesis of melanin. By reducing the activity of tyrosinase, nicotinamide reduces the production of melanin, thereby helping to lighten skin spots and improve skin tone uniformity;

[0028] Certain components in tangerine peel extract (such as flavonoids) reduce the production of melanin, thereby improving uneven skin tone and fading spots;

[0029] Tokyo Sakura leaf extract is rich in antioxidant ingredients, especially polyphenols and flavonoids. These ingredients not only have good antioxidant capacity, but also reduce the production of melanin, thereby improving uneven skin tone and fading spots.

[0030] Roselle flower contains rich plant polyphenols and anthocyanins, which can inhibit the activity of tyrosinase, thereby reducing the production of melanin. By reducing the synthesis of melanin, Roselle flower ferment filtrate helps to even out skin tone and reduce dark spots;

[0031] When the above raw materials are used together, the inhibitory ability to tyrosinase is further enhanced and the production of melanin can be further reduced, thereby enhancing the whitening effect of the composition. DETAILED DESCRIPTION

[0032] The present invention will be described clearly and completely below in conjunction with the embodiments of the present invention. In the description of the present invention, it should be noted that, if no specific conditions are specified in the embodiments, the conditions are carried out according to conventional conditions or conditions recommended by the manufacturer. If the manufacturer of the reagents or instruments used is not specified, they are all conventional products that can be purchased commercially.

[0033] Supplier information and / or product information

[0034] Nicotinamide was purchased from Hangzhou Weibolai Biotechnology Co., Ltd., with an active substance content of ≥99%, and the raw material trade name is nicotinamide;

[0035] 4-Butylresorcinol was purchased from Kumar Organic Products Limited, with an active substance content of ≥99%, and the raw material trade name is kopcino l;

[0036] Citrus peel extract was purchased from Ichimaru Natural Beauty Co., Ltd., Japan, with an active substance content of 3%, the trade name is transparent muscle, and the complete formula is 3% by mass of citrus peel extract, 67.9% by mass of butylene glycol, and 29.1% by mass of water;

[0037] Tokyo cherry leaf extract was purchased from Ichimaru Natural Beauty Co., Ltd. of Japan, with an active substance content of 2%. The trade name is Tokyo cherry leaf extract, and the complete formula is 49% by mass of butylene glycol, 49% by mass of water, and 2% by mass of Tokyo cherry leaf extract;

[0038] Cellulase was purchased from Kangdisi Chemical (Hubei) Co., Ltd., with an effective substance content of 99%, and the trade name is cellulase;

[0039] Lipase was purchased from Kangdisi Chemical (Hubei) Co., Ltd., with an effective substance content of 99%, and the trade name is lipase;

[0040] Lactobacillus was purchased from Guangzhou Huayang Biotechnology Co., Ltd., with an effective substance content of 25%. The complete formula is 73% by mass of water, 25% by mass of lactobacillus, and 2% by mass of Leuconostoc / radish (RAPHANUS SATIVUS) root fermentation product filtrate.

[0041] The preparation method of roselle flower fermentation filtrate is as follows (unless otherwise specified, the roselle flower fermentation filtrate used in the examples is the roselle flower fermentation filtrate prepared by this method):

[0042] Step 1: crushing the roselle flowers and performing enzymatic hydrolysis to obtain an enzymatic hydrolyzate;

[0043] Step 2: The enzymatic hydrolysate is mixed with peptone, glucose, sodium dihydrogen phosphate and pure water to obtain a culture medium, wherein the mass fraction of the enzymatic hydrolysate is 20%, the mass fraction of peptone is 3%, the mass fraction of glucose is 2%, the mass fraction of disodium hydrogen phosphate is 15%, and the mass fraction of pure water is 60%;

[0044] Step 3: inoculate the activated lactobacillus into the culture medium and ferment for 12 hours, sterilize after fermentation, and centrifuge to obtain the supernatant to obtain the roselle flower fermentation filtrate.

[0045] The mass ratio of the enzyme used in step 1 to the roselle flower is 3:100, and the enzyme is cellulase;

[0046] The lactobacillus used in step 3 is added in the form of lactobacillus bacterial liquid, and the mass ratio of the lactobacillus bacterial liquid to the enzymatic hydrolysate is 1:10;

[0047] The activation method of lactobacillus liquid is as follows: add the purchased lactobacillus to an activation medium consisting of 3% peptone, 2% glucose, 15% sodium dihydrogen phosphate and 80% pure water, and culture until the number of viable bacteria reaches 1.3x10 6 (±0.2x10 6 )CFU / g.

[0048] Preparation method of whitening composition:

[0049] Nicotinamide, 4-butylresorcinol, citrus peel extract, Tokyo cherry leaf extract, and roselle flower fermentation filtrate are mixed according to a mass ratio and uniformly dispersed to obtain a whitening composition.

[0050] Examples 1-6

[0051] A whitening composition, the formula of which is shown in Table 1:

[0052] Table 1

[0053]

[0054] Example 7

[0055] The method is basically the same as Example 1, except that commercially available roselle flower fermentation filtrate is used to replace the roselle flower fermentation filtrate in Example 1. The commercially available roselle flower fermentation filtrate in this example is purchased from Technobao Co., Ltd. under the trade name (TECHNOLONG HIBISCUS FLOWER-FF Roselle Fermentation Broth).

[0056] Example 8

[0057] The method is basically the same as Example 1, except that, in the preparation process of the roselle flower fermentation filtrate, galactosyl yeast is used to replace lactobacillus in step 3.

[0058] Example 9

[0059] The method is substantially the same as Example 1, except that, in the preparation process of the roselle flower fermentation filtrate, Lactococcus lactis is used in step 3 to replace Lactobacillus.

[0060] Example 10

[0061] The method is basically the same as Example 1, except that, in the preparation process of the roselle flower fermentation filtrate, lipase is used to replace cellulase in step 1.

[0062] Embodiment 11

[0063] The method is basically the same as Example 1, except that, in the preparation process of roselle flower fermentation filtrate, a mixed enzyme of cellulase and lipase is used to replace cellulase in step 1, and the mass ratio of cellulase to lipase is 7:1.

[0064] Comparative Examples 1-5

[0065] A composition, the formula is shown in Table 2:

[0066] Table 2

[0067]

[0068]

[0069] Comparative Examples 6-10

[0070] A composition, the formula is shown in Table 3:

[0071] Table 3

[0072]

[0073]

[0074] Performance Test:

[0075] 1 Experimental materials and methods

[0076] 1.1 Instruments and Equipment

[0077] BSA224S Analytical Balance

[0078] RT-6100 ELISA Analyzer

[0079] 1.2 Reagents

[0080] Polyphenol oxidase (mushroom), BR

[0081] Levodopa, BR

[0082] 1.3 Test methods

[0083] (1) Treatment of control and test samples

[0084] Sample group: diluted with pure water to a concentration of 5.003% of the composition prepared in the examples and comparative examples;

[0085] Negative control: pure water.

[0086] (2) Test operation steps

[0087] Set up sample tubes, sample background tubes, enzyme reaction tubes, and solvent background tubes. Set up 3 parallel tubes for each group. Add different reagent solutions to the four groups, shake gently, and let stand at room temperature for 5 minutes. Transfer each group of reaction solutions into a 1 cm cuvette and measure the absorbance at 475 nm.

[0088] (3) Calculation formula

[0089]

[0090] Where: T—absorbance of sample tube, i.e. absorbance of solution after sample reacts with tyrosinase;

[0091] T0—sample background absorbance;

[0092] C—the average value of the absorbance of the enzyme reaction tube three times, that is, the absorbance of the reaction of tyrosinase and DOPA when no sample is added;

[0093] C0—Solvent background absorbance.

[0094] (4) Data analysis

[0095] The statistical analysis software was SPSS, and the comparison between the tyrosinase inhibition rate of the test sample and the negative control was performed using an independent sample t test. The above statistical analyses were all two-tailed tests, with a significance level of α=0.05.

[0096] P>0.05 indicates that there is no significant difference between the two groups; P<0.05 indicates that there is a significant difference between the two groups.

[0097] The test results are shown in Table 4:

[0098] Table 4

[0099]

[0100]

[0101] Results Analysis

[0102] 1. It can be seen from Examples 1-6 that when the amount of raw materials added is changed, the tyrosinase inhibition rate of Examples 1-6 fluctuates. It can be seen that the tyrosinase inhibition ability in Examples 1-6 is different. Further observation shows that Example 1 has a more excellent tyrosinase inhibition ability. It can be seen that the tyrosinase inhibition ability under this formula can be maximized.

[0103] 2. It can be seen from Examples 1 and 7 that when the roselle flower fermentation filtrate obtained by the specific preparation method in the examples was replaced with the commercially available roselle flower fermentation filtrate, the tyrosinase inhibition ability of Example 7 relative to Example 1 showed a certain downward trend. Further observation of Examples 8-9 showed that when the lactobacillus used in Example 1 was replaced with other strains, the tyrosinase inhibition abilities of Examples 8-9 all showed a downward trend to varying degrees. It can be seen that the lactobacillus produced a fermentation product with tyrosinase inhibition ability that was more suitable for synergizing with other substances during the fermentation process of roselle flowers.

[0104] 3. It can be seen from Example 1 and Examples 10-11 that when Example 10 uses lipase to replace the cellulase in Example 1, the tyrosinase inhibition rate of Example 10 has a certain degree of downward trend relative to Example 1. Further observation of Example 11 shows that when Example 11 uses a mixed enzyme composed of the cellulase and lipase in Examples 1 and 10, the tyrosinase inhibition ability obtained by Example 11 should theoretically be between Examples 1 and 10, but the tyrosinase inhibition ability actually obtained by Example 11 is better than either of Examples 1 and 10; it can be seen that when cellulase and lipase are mixed and used, the two are more conducive to providing lactobacilli with a fermentation substrate with good fermentation efficiency or can be more easily fermented by lactobacilli into a fermentation substrate with tyrosinase inhibition ability;

[0105] 4. It can be seen from Example 1 and Comparative Examples 1-5 that when any one of nicotinamide, 4-butylresorcinol, citrus peel extract, Tokyo cherry leaf extract, and roselle flower fermentation filtrate is missing from the composition, the tyrosinase inhibition ability of Comparative Examples 1-5 shows a significant downward trend relative to Example 1. It can be seen that nicotinamide, 4-butylresorcinol, citrus peel extract, Tokyo cherry leaf extract, and roselle flower fermentation filtrate are indispensable in the composition;

[0106] And through further calculation of the tyrosinase inhibition ability of comparative examples 1-5, we surprisingly found that the above five raw materials produced a synergistic effect, thereby making the composition have excellent tyrosinase inhibition ability;

[0107] The reason is that, by observing comparative examples 1-5, it can be seen that the tyrosinase inhibition rates thereof are 56.238%, 55.199%, 56.231%, 56.187%, and 56.731%, respectively; and comparative examples 1-5 respectively use only four raw materials, so the average theoretical tyrosine inhibition rate of each raw material is calculated to be 14.029%, while the theoretical value of embodiment 1 which uses five raw materials at the same time should be 70.146%, but by observing Table 4, it can be seen that the actual value of embodiment 1 reaches 76.361%, which shows that the tyrosinase inhibition ability obtained by embodiment 1 exceeds the simple superposition of each raw material;

[0108] 5. Further observation of Example 1 and Comparative Examples 6-10 shows that when any of the above raw materials is replaced with a substitute having similar efficacy to niacinamide, 4-butylresorcinol, citrus peel extract, Tokyo cherry leaf extract, and roselle flower fermentation filtrate, the tyrosinase inhibition ability of Comparative Examples 6-10 shows a significant downward trend, which shows that none of the above raw materials is replaceable.

Claims

1. A whitening composition, characterized in that: Calculated by mass, it includes at least the following components:

2. The whitening composition according to claim 1, characterized in that Calculated by mass, it includes at least the following components:

3. The whitening composition according to claim 1, characterized in that The roselle flower fermentation filtrate is a fermentation filtrate obtained by fermenting roselle flowers with microorganisms, and the microorganisms are lactobacilli.

4. The whitening composition according to claim 3, characterized in that The preparation method of the roselle flower fermentation filtrate comprises the following steps: Step 1: crushing the roselle flowers and performing enzymatic hydrolysis to obtain an enzymatic hydrolyzate; Step 2: Mix the enzymatic hydrolysate with peptone, glucose, sodium dihydrogen phosphate and pure water to obtain a culture medium; Step 3: inoculate lactobacillus into the culture medium for fermentation, sterilize after fermentation, and centrifuge to obtain the supernatant to obtain the roselle flower fermentation filtrate.

5. The whitening composition according to claim 4, characterized in that The mass ratio of the enzyme used in step 1 to the roselle flower is 2-8:100, and the enzyme is a mixture of cellulase and lipase, and the mass ratio of cellulase to lipase is 6-8:

1.

6. The whitening composition according to claim 4, characterized in that The lactobacillus used in step 3 is added in the form of a lactobacillus bacterial liquid, and the number of live bacteria in the lactobacillus bacterial liquid is not less than 1×10 6 CFU / g, and the mass ratio of lactobacillus liquid to enzymatic hydrolysate is 1-3:

10.

7. Use of the whitening composition according to any one of claims 1 to 6 for preparing cosmetics.

8. A cosmetic, characterized in that: Contains 1 to 10 wt % of the whitening composition according to any one of claims 1 to 6.

9. The cosmetic according to claim 8, characterized in that: The dosage forms of the daily chemical product are patches, ointments, liquids, sprays, gels, emulsions, and creams.

Citation Information

Patent Citations

  • Customized whitening inkjet ink and preparing method and application thereof

    CN110464663A