A freckle-removing and skin-whitening composition and its application

Abstract

The present invention discloses a freckle-removing and whitening composition and its application. The composition comprises the following components in parts by weight: 5-30 parts of Rosa centifolia flower extract, 5-30 parts of Brussels sprout extract, 5-30 parts of spinach leaf extract, 1-30 parts of sesame sprout extract, 1-15 parts of Orchis maculata extract, and 1-15 parts of Malpighia emarginata extract. The composition of the present invention is mainly composed of active ingredients of plant extracts, has good safety, the components synergistically enhance the effect, inhibit the activity of tyrosinase, prevent or reduce the deposition of melanin in the skin, and can whiten and brighten the skin.

Description

Technical Field

[0001] The present invention relates to the technical field of cosmetics, and particularly relates to a freckle-removing and whitening composition and its application. Background Art

[0002] Whitening has always been an important part of consumers' skin care needs. According to the interpretation and claim guidelines of "freckle-removing and whitening" in the "Cosmetics Classification Rules and Classification Catalogue", except for physical covering forms, the freckle-removing and whitening effect mainly refers to helping to reduce or slow down skin pigmentation. The formation of skin spots is the result of pigment deposition on the skin under the influence of factors such as ultraviolet rays, hormones, genetics, and aging. Therefore, such products mainly achieve the purpose of freckle removal by adding effective ingredients that inhibit and reduce melanin in the cream matrix. However, the synthesis and metabolism of skin pigment is a very complex process involving multiple links, and many effective whitening products still require an organic combination of multiple freckle-removing and whitening ingredients.

[0003] Currently, consumers are becoming more rational. In addition to efficacy, they also pursue the safety and health of ingredients for whitening products. They pay more attention to the specific added ingredients when choosing cosmetics. Surveys show that among all freckle-removing and whitening ingredients, plant extracts account for as high as 45.7%, indicating consumers' preference for mild ingredients. Currently, commonly used freckle-removing additives include arbutin, kojic acid, vitamin C derivatives, fruit acids, and some traditional Chinese medicine extracts, etc.

[0004] However, the current whitening products on the market still have poor safety, or only play a whitening and freckle-removing role through a single approach. Therefore, it is very necessary to develop products that are mild, safe, and can play a whitening and freckle-removing role through multiple approaches. Summary of the Invention

[0005] The purpose of the present invention is to provide a freckle-removing and whitening composition and its application, which can effectively act on multiple paths of melanin formation, play a whitening and freckle-removing role, and are suitable for sensitive skin.

[0006] To this end, the first technical solution provided by the present invention is as follows:

[0007] A freckle-removing and whitening composition, characterized by comprising the following components in parts by weight: 5 - 30 parts of Rosa centifolia flower extract, 5 - 30 parts of Brassica oleracea var. gemmifera extract, 5 - 30 parts of spinach leaf extract, 1 - 30 parts of sesame sprout extract, 1 - 15 parts of Orchis maculata extract, and 1 - 15 parts of Malpighia emarginata extract.

[0008] Further, the freckle-removing and whitening composition further comprises 1 - 5 parts of Hydrastis canadensis extract.

[0009] Further, the freckle-removing and whitening composition further comprises 0.1 - 10 parts of diglucosyl gallic acid.

[0010] Furthermore, the freckle-removing and whitening composition further comprises 1-20 parts of niacinamide.

[0011] Furthermore, the Malpighia emarginata extract is Malpighia emarginata fruit extract and / or Malpighia emarginata seed extract.

[0012] Furthermore, the weight ratio of the Rosa centifolia flower extract: Brassica oleracea var. gemmifera extract: Orchis maculata extract: Malpighia emarginata extract is (5-20):(5-20):(2-10):(1-5).

[0013] Furthermore, the preparation method of the Orchis maculata extract is as follows:

[0014] S1, Take Orchis maculata, crush it with a pulverizer, and pass through a 10-50 mesh sieve to obtain Orchis maculata powder;

[0015] S2, Weigh an appropriate amount of Orchis maculata powder, add 5-10 times the volume of petroleum ether, and perform ultrasonic extraction for 1-3 h, then separate the filtrate and the filter residue;

[0016] S3, Reflux extract the filter residue separated in S2 with 5-30 times water at a temperature of 60-85 °C for 1-3 times, each time for 1-3 h, separate the filtrate and the filter residue, combine the filtrates obtained each time, and concentrate to 1 / 3-1 / 4 of the original volume;

[0017] S4, Extract the filter residue separated in S3 with 5-10 times ethanol at a temperature of 50-80 °C, perform ultrasonic treatment for 0.5-1 h, separate the filtrate and the filter residue, and concentrate the filtrate to 1 / 3-1 / 4 of the original volume;

[0018] S5, Combine the concentrated solutions of S3 and S4, mix them evenly, then perform vacuum filtration and drying to obtain the product.

[0019] The present invention also discloses an application of the freckle-removing and whitening composition in cosmetics. The cosmetics are skin external preparations prepared with the freckle-removing and whitening composition as the active ingredient, plus conventional pharmaceutical or cosmetic excipients or auxiliary components.

[0020] Furthermore, the cosmetics are one or more of lotion, essence, cream, mask, and gel.

[0021] Furthermore, the mass percentage of the freckle-removing and whitening composition in the cosmetics is 1-20%.

[0022] In the technical solution of the present application:

[0023] The extract of Rosa centifolia L. flower is rich in compounds, including organic acids, vitamins, carbohydrates, flavonoids, alkaloids, minerals, proteins, amino acids, fats, etc. Among them, organic acid compounds, as the main active ingredients, can promote the metabolism of skin cells, fade pigmentation such as black spots and freckles. Existing studies have shown that the extract of Rosa centifolia L. flower can promote the generation of ceramide, thus playing a role in repairing and softening the skin; it can quench free radicals and improve the dull and aging state of the skin.

[0024] The extract of sesame sprout can activate peroxisome proliferator-activated receptor, promote the proliferation of fibroblast cells, and has anti-inflammatory function; it also has an inhibitory effect on tyrosinase and has whitening effect.

[0025] The extract of Brussels sprout contains phenolic components such as flavonol, anthocyanin and chlorogenic acid, allyl isothiocyanate and sulfur-containing antithyroid substances, and has antioxidant, anti-wrinkle and anti-stress effects. It can detoxify and nourish the skin and help repair damaged skin.

[0026] The extract of spinach leaf is rich in various vitamins, among which the contents of vitamin C, vitamin E, vitamin K, etc. are relatively high, which can effectively delay aging, prevent internal oxidation of the body, and maintain the youthful state of the skin.

[0027] The extract of Ferocactus recurvus has a good promoting effect on the activity of epidermal cells, has skin-activating effect, and has antioxidant property.

[0028] The extract of Orchis maculata has antioxidant effect, enhances the hydration of the skin and the differentiation and proliferation of the stratum corneum of the skin, and can effectively slow down the aging speed of the skin and improve the skin state.

[0029] The extract of Hydrastis canadensis contains berberine and hydrastinine, and has antioxidant, antibacterial and anti-inflammatory effects.

[0030] Diglucosyl gallic acid can be used as an antioxidant, which can help inhibit the generation of free radicals and resist the damage of ultraviolet rays to the DNA of the skin. In terms of anti-inflammatory, it can prevent blood vessel dilation and redness. Diglucosyl gallic acid can control the MITF gene, hinder the transfer of melanin to the skin surface layer, and prevent the synthesis of melanin.

[0031] Compared with the prior art, the advantages of the present invention are:

[0032] The composition provided by the present invention can significantly inhibit the activity of tyrosinase and hinder melanogenesis by reasonably combining the ingredients of Rosa centifolia flower extract, Brussels sprout extract, spinach leaf extract, sesame sprout extract, Orchis maculata extract, Malpighia emarginata extract, diglucosyl gallic acid, niacinamide and Hydrastis canadensis extract. Specifically, the Rosa centifolia flower extract in the composition of the present invention is rich in vitamin C and organic acids, which can promote the metabolism of skin cells, fade pigmentation such as dark spots and freckles; the Brussels sprout extract has antioxidant and anti-wrinkle effects, detoxifies and nourishes the skin, repairs damaged skin, and can inhibit the transfer of melanosomes; the Orchis maculata extract enhances the hydration of the skin and the differentiation and proliferation of the stratum corneum of the skin, strengthens the skin barrier, and brightens the skin; the Malpighia emarginata extract can antioxidant and activate the skin, inhibit the activity of tyrosinase, thereby inhibiting the formation of new melanin. In particular, the Rosa centifolia flower extract, Brussels sprout extract, Orchis maculata extract and Malpighia emarginata extract in the composition of the present invention are combined in a specific ratio and act synergistically, which can effectively control multiple pathways of melanin formation, reduce the release of inflammatory factors produced by the skin, reduce the occurrence of allergies, and thus reduce the deposition of inflammatory pigments; it can inhibit the expression ability of P1 / P9 / neurotransmitter-related substance P, etc. through coordination, accelerate the metabolic shedding of melanocytes, fade acne marks, repair the skin barrier at the same time, reduce skin sensitivity, and improve skin brightness and reduce skin pigmentation through multiple pathways; by inhibiting the activity of tyrosinase, it can inhibit the activation of melanocytes and reduce the pigment deposition of the skin. Using diglucosyl gallic acid to prevent tyrosine from becoming melanin in advance can also reduce the content of ROS in the skin and reduce the level of protein carbonylation in human skin. Using niacinamide to reduce the transport of melanin to the stratum corneum of the skin, activate the skin metabolism ability, and promote melanin metabolism.

[0033] The ingredients in the composition provided by the present invention are mainly active ingredients of plant extracts. The plant extract components are natural, mild and safe. They contain a variety of similar structures, enabling them to exert their effects from multiple angles and through multiple channels, and achieving a good synergistic effect. When the components of the composition of the present invention are combined in a specific ratio, the extracts contain a variety of macromolecules and small molecules of different sizes that act together on the skin, penetrate from the skin surface layer by layer into different skin layers, and exert better efficacy. In short, through the synergistic effect under the different action mechanisms of several multi-components, a multi-faceted whitening and freckle-reducing effect is achieved. In addition, the present invention uses plant extracts as active ingredients, greatly reducing the dependence of the product on chemical synthetic products, and greatly improving the safety of the product. Sensitive skin can also use it with confidence. Detailed implementation mode

[0034] The following further describes the specific implementation modes of the technical solutions of this specification through specific embodiments. These embodiments are for the detailed description of the technical solutions and not for limiting the technical solutions. Based on the embodiments in this specification, all other embodiments obtained by those of ordinary skill in the art without creative efforts shall fall within the scope of protection of this specification.

[0035] Unless otherwise specified, the component raw materials in the following examples and comparative examples are all commercially available.

[0036] Example 1

[0037] A freckle-reducing and whitening composition comprises the following components: 30 parts of Rosa centifolia flower extract, 30 parts of Brussels sprout extract, 30 parts of spinach leaf extract, 30 parts of sesame sprout extract, 15 parts of Orchis maculata extract, and 15 parts of Malpighia emarginata extract.

[0038] Example 2

[0039] A freckle-reducing and whitening composition comprises the following components: 20 parts of Rosa centifolia flower extract, 20 parts of Brussels sprout extract, 20 parts of spinach leaf extract, 20 parts of sesame sprout extract, 15 parts of Orchis maculata extract, and 10 parts of Malpighia emarginata extract.

[0040] Example 3

[0041] A freckle-reducing and whitening composition comprises the following components: 10 parts of Rosa centifolia flower extract, 10 parts of Brussels sprout extract, 10 parts of spinach leaf extract, 10 parts of sesame sprout extract, 10 parts of Orchis maculata extract, and 10 parts of Malpighia emarginata extract.

[0042] Example 4

[0043] A freckle-reducing and whitening composition comprises the following components: 25 parts of Rosa centifolia flower extract, 25 parts of Brussels sprout extract, 20 parts of spinach leaf extract, 20 parts of sesame sprout extract, 15 parts of Orchis maculata extract, 10 parts of Malpighia emarginata extract, and 5 parts of diglucosyl gallic acid.

[0044] Example 5

[0045] A freckle-reducing and whitening composition comprises the following components: 20 parts of Rosa centifolia flower extract, 30 parts of Brussels sprout extract, 30 parts of spinach leaf extract, 15 parts of sesame sprout extract, 15 parts of Orchis maculata extract, 10 parts of Malpighia emarginata extract, and 10 parts of niacinamide.

[0046] Example 6

[0047] A freckle-reducing and whitening composition, comprising the following components: 30 parts of Rosa centifolia flower extract, 15 parts of Brussels sprout extract, 20 parts of spinach leaf extract, 20 parts of sesame sprout extract, 10 parts of Orchis maculata extract, 15 parts of Malpighia emarginata extract, 5 parts of diglucosyl gallic acid, and 10 parts of niacinamide.

[0048] Example 7

[0049] A freckle-reducing and whitening composition, comprising the following components: 25 parts of Rosa centifolia flower extract, 25 parts of Brussels sprout extract, 20 parts of spinach leaf extract, 20 parts of sesame sprout extract, 10 parts of Orchis maculata extract, 10 parts of Malpighia emarginata extract, 5 parts of Hydrastis canadensis extract, 5 parts of diglucosyl gallic acid, and 10 parts of niacinamide.

[0050] Comparative Example 1

[0051] Compared with Example 1, the difference lies in that it does not contain Rosa centifolia flower extract, and the other components are the same.

[0052] Comparative Example 2

[0053] Compared with Example 1, the difference lies in that it does not contain Brussels sprout extract, and the other components are the same.

[0054] Comparative Example 3

[0055] Compared with Example 1, the difference lies in that it does not contain spinach leaf extract, and the other components are the same.

[0056] Comparative Example 4

[0057] Compared with Example 1, the difference lies in that it does not contain sesame sprout extract, and the other components are the same.

[0058] Comparative Example 5

[0059] Compared with Example 1, the difference lies in that it does not contain Orchis maculata extract, and the other components are the same.

[0060] Comparative Example 6

[0061] Compared with Example 1, the difference lies in that it does not contain Malpighia emarginata extract, and the other components are the same.

[0062] Comparative Example 7

[0063] Compared with Example 1, the difference lies in that it does not contain Brussels sprout extract and Orchis maculata extract, and the other components are the same.

[0064] Comparative Example 8

[0065] Compared with Example 1, the difference lies in that it does not contain Rosa centifolia flower extract and Malpighia emarginata extract, and the other components are the same.

[0066] Comparative Example 9

[0067] Compared with Example 1, the difference lies in that it does not contain Rosa centifolia flower extract and Orchis maculata extract, and the other components are the same.

[0068] Comparative Example 10

[0069] Compared with Example 1, the difference lies in that it does not contain Brassica oleracea var. gemmifera extract and Malpighia emarginata extract, and the other components are the same.

[0070] Sample Example

[0071] The composition of the cosmetic is (wt%): 2.5% Tween 60, 1.5% acryloyldimethyltaurate / VP copolymer, 4% grape seed oil, 4% camellia seed oil, 4% jojoba seed oil, 7% glycerol, 5% butanediol, 5% sorbitol, 1.2% squalane, 2.5% allantoin, 1.8% aloe extract, 20% lightening and whitening composition, 1.2% xanthan gum, 1.0% sodium EDTA-2, 0.5% citric acid, 0.4% sodium benzoate and the balance water.

[0072] To better illustrate the advantages of the present invention, the following provides the efficacy experiments of the lightening and whitening composition provided by the present invention.

[0073] I. Human patch safety test

[0074] Sixty-eight volunteers aged 30 - 50 years were selected. The compositions of the examples and comparative examples were added to other cosmetic matrices to make emulsions, and then 20 μg was taken and placed in a qualified patch test chamber. The patch containing the test sample was applied to the flexor side of the forearm of the subject with a non-irritating tape, and gently pressed with the palm to make it evenly adhere to the skin for 24 h. After 24 h, the patch was removed, and the skin reaction was observed at 0.5 h, 24 h, and 48 h after the removal of the patch. The results showed that the compositions of Examples 1 - 7 and Comparative Examples 1 - 10 all showed negative reactions. According to the regulations in the "Technical Specifications for Cosmetics Safety" (2015 version), it can be determined that the test sample did not cause adverse reactions to the skin of this batch of subjects, and the composition of the present application has good use safety. The skin reaction grading standard for the skin closed patch test is shown in Table 1, and the specific test results are shown in Table 2.

[0075] Table 1. Skin reaction grading standard table for skin closed patch test

[0076]

[0077] Table 2. Patch test result table

[0078]

[0079]

[0080] As can be seen from Table 2, the composition obtained by the technical solution provided by the present invention is mild and safe, and has no irritation to the human body.

[0081] II. Efficacy Test

[0082] Test 1: Tyrosinase Activity Inhibition Experiment

[0083] The compositions of Examples 1-7 of the present invention and the compositions of Comparative Examples 1 to 10 were respectively taken to determine the tyrosinase activity inhibition rate. A tyrosinase solution (100 U / mL) was prepared with a pH 6.8 and 100 mmol / L PBS buffer solution, and then a L-tyrosine solution (0.01 mol / L) and a composition solution (1.0 mg / mL) were prepared; in a 96-well plate, 40 μL of 0.1 mg / mL tyrosine, 80 μL of PBS buffer solution, 60 μL of the composition solution, and 50 μL of 60 U / mL tyrosinase solution were added in sequence. After incubation at 37 °C for 30 min, it was detected with an enzyme-labeling instrument at a wavelength of 475 nm, and the PBS buffer solution was used as the blank group.

[0084] Calculation formula for tyrosinase inhibition rate: Tyrosinase inhibition rate = [(A1 - A2) - (A3 - A4)] / (A1 - A2) × 100%, where A1: absorbance of adding tyrosinase solution without adding the test sample solution; A2: absorbance of not adding tyrosinase solution without adding the test sample solution; A3: absorbance of adding tyrosinase solution with the test sample solution added; A4: absorbance of not adding tyrosinase solution with the test sample solution added. The test results are shown in Table 3:

[0085] Table 3 Influence of the composition on tyrosinase activity

[0086]

[0087]

[0088] From the test results in Table 3, it can be seen that for the composition with the ratio of the present invention, its tyrosinase inhibition rate is significantly higher than that of the composition without using its ratio components. It can be seen that the composition provided by the present invention can effectively inhibit the activity of tyrosinase.

[0089] Compared with Example 1, Comparative Examples 1-6 respectively do not contain one of the components, and their inhibition rates of tyrosinase activity are 60.29%-65.27%, significantly lower than the inhibition rate of 75.26% of the composition in Example 1. This shows that the raw materials of Rosa centifolia flower extract, Brussels sprout extract, spinach leaf extract, sesame sprout extract, Orchis maculata extract and Malpighia emarginata extract all have inhibitory effects on tyrosinase. In Examples 4-7, one, two or all of the components diglucosyl gallic acid, niacinamide and Hydrastis canadensis extract are further rationally configured, which can significantly improve the inhibitory effect on tyrosinase activity. Compared with the examples, Comparative Examples 7-10 do not contain at least two of the components of Rosa centifolia flower extract, Brussels sprout extract, Orchis maculata extract and Malpighia emarginata, and their inhibition rates of tyrosinase activity decrease significantly. This shows that the raw materials of Rosa centifolia flower extract, Brussels sprout extract, Orchis maculata extract and Malpighia emarginata extract are combined with each other and synergistically enhance the effect to better play the role of inhibiting tyrosinase activity.

[0090] Therefore, the raw materials of the composition provided by the present invention have a mutually promoting effect and are combined

[0091] to synergistically enhance

[0092] the inhibitory effect on tyrosinase activity.

[0093] Test 2: Melanin removal test

[0094] 170 volunteers aged 35-50 were selected and randomly divided into 17 groups, with 10 volunteers in each group, 5 males and 5 females. After washing their faces in the morning and evening every day, 0.25 g of the above-mentioned cosmetic products 1-17 was applied to the face, and it was continuously used for 30 days. Using the MX18 melanin measuring instrument of CK Company in Germany, the melanin content MI value (marked as A0) of the volunteers before using the cosmetic and the skin melanin content MI value on the 30th day (marked as A 30 ) were measured, and the reduction rate of melanin δ = 100%×(A0 - A 30 ) / A0 was calculated. The whitening effect of the products of the present invention was characterized by the melanin reduction rate δ, and the test results are shown in Table 4:

[0095] Table 4 Results of melanin removal test

[0096]

[0097]

[0098] The production of melanin by melanocytes in the skin is the main cause of skin darkening and the formation of age spots. From the test results in Table 4, it can be seen that the freckle-removing and whitening composition of the present invention, which consists of raw materials such as Rosa centifolia flower extract, Brassica oleracea var. gemmifera extract, Spinacia oleracea leaf extract, Sesamum indicum sprout extract, Orchis maculata extract, Malpighia emarginata extract, diglucosyl gallic acid, niacinamide, and Ranunculus acris extract, has excellent melanin-removing effect. The cosmetics prepared therefrom can reduce the proportion of melanin in the skin by 38.50% after 30 days of use.

[0099] From the comparison of the tests between the examples and the comparative examples, it can be seen that the Rosa centifolia flower extract of the present invention,

[0100] Brassica oleracea var. gemmifera extract,

[0101] Spinacia oleracea leaf extract, Sesamum indicum sprout extract, Orchis maculata extract, and Malpighia emarginata extract have a synergistic relationship of mutual promotion in enhancing the melanin-removing effect of cosmetics, and the compounding of the four can significantly increase the whitening and freckle-removing effect of the product.

[0102] Although the embodiments of the present specification have been shown and described, it will be understood by those of ordinary skill in the art that various changes, modifications, substitutions, and variations can be made to these embodiments without departing from the principles and spirit of the present specification, and the scope of the present specification is defined by the appended claims and their equivalents.

Claims

1. A spot-lightening and whitening composition, characterized in that: The invention comprises the following components in parts by weight: 5-30 parts of rosa centifolia flower extract, 5-30 parts of Brussels spore extract, 5-30 parts of spinach leaf extract, 1-30 parts of sesame sprout extract, 1-15 parts of spotted red gate orchid extract and 1-15 parts of concave-margin acerola extract; the preparation method of the spotted red gate orchid extract is as follows: S1, taking spotted red gate orchid, crushing it with a grinder, passing it through a 10-50 mesh sieve, and obtaining spotted red gate orchid powder; S2, weighing an appropriate amount of spotted red gate orchid powder, adding 5-10 times the volume of petroleum ether, ultrasonically extracting for 1-3 hours, and separating the filtrate and filter residue; S3, reflux extraction of the filter residue separated by S2 with 5-30 times of water, the temperature is 60-85°C, extraction 1-3 times, each time for 1-3h, separation of the filtrate and the filter residue, combination of the filtrate obtained from each separation, and concentration to 1 / 3-1 / 4 of the original volume; S4, extraction of the filter residue separated by S3 with 5-10 times of ethanol, the temperature is 50-80°C, ultrasonication for 0.5-1h, separation of the filtrate and the filter residue, and concentration of the filtrate to 1 / 3-1 / 4 of the original volume; S5, combination of the concentrated solutions of S3 and S4, mixing evenly, decompression filtering, and drying to obtain.

2. The spot-lightening and whitening composition according to claim 1, characterized in that: It also contains 1-5 parts of goldenseal extract.

3. The spot-lightening and whitening composition according to claim 1, characterized in that: It also contains 0.1-10 parts of diglucosyl gallic acid.

4. The spot-lightening and whitening composition according to claim 1, characterized in that: Also contains 1-20 parts of niacinamide.

5. The spot-lightening and whitening composition according to claim 1, characterized in that: The Acerola truncatum extract is Acerola truncatum fruit extract and / or Acerola truncatum seed extract.

6. The spot-lightening and whitening composition according to claim 1, characterized in that: The weight ratio of the Rosa centifolia flower extract: Brussels spore extract: Orchidaceae extract: Acer truncatum extract is (5-20): (5-20): (2-10): (1-5).

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