Compositions, whitening complexes and cosmetic products inhibiting the activity of tyrosinase

Abstract

The present application relates to the technical field of skin care products, in particular to a composition for inhibiting tyrosinase activity, a whitening compound and a daily chemical product. The composition for inhibiting tyrosinase activity comprises 0.5-2.0 parts of hydroxytyrosol and 0.8-2.0 parts of resveratrol by weight. The composition can effectively inhibit the activity of tyrosinase and reduce the formation of melanin. Meanwhile, the compound provided by the present application can effectively reduce the occurrence of various skin diseases, has better biological activities such as whitening, antioxidant, anti-inflammatory, anti-aging, moisturizing and emollient, and has a good application prospect in the daily chemical market.

Description

Technical Field

[0001] This invention relates to the field of skincare technology, and more specifically, to compositions that inhibit tyrosinase activity, whitening complexes, and daily chemical products. Background Technology

[0002] In recent years, with the development of society and the economy and the change in people's aesthetic concepts, healthy and fair skin has become a desired skin condition for many people, especially women. The content and distribution of melanin in the skin are one of the main factors affecting skin color. Melanin is an amino acid-derived biological pigment, belonging to polyphenol polymers. It can inhibit damage to skin cells from external stimuli such as ultraviolet rays and free radicals. However, excessive synthesis and accumulation not only hinder the pursuit of a beautiful skin tone but may also lead to freckles, melasma, age spots, and even malignant melanoma. Therefore, ingredients that reduce melanin synthesis are often added to daily chemical products to prevent excessive melanin accumulation and achieve a whitening effect.

[0003] The distribution of melanin in the body can be roughly divided into four stages: (1) melanosome formation; (2) melanosome maturation; (3) melanin synthesis; and (4) transport of melanosomes containing large amounts of melanin. Melanin synthesis is the process by which the non-essential amino acid L-tyrosine is converted step-by-step from dopaquinone into a mixture of eumelanin and pheomelanin under the action of oxidases such as tyrosinase. Therefore, to achieve the goals of reducing melanin synthesis and whitening the skin, research can be advanced from two directions: inhibiting the activity of tyrosinase and hindering the transport of melanin within the body. Currently, domestic and international scholars primarily focus on the inhibition of tyrosinase activity, researching the effects of various natural, harmless, and multi-biologically active ingredients on tyrosinase inhibition. This provides a theoretical basis for developing corresponding daily chemical products. For example, domestic scholars such as Chen Jing et al. explored the mechanism by which oleuropein, derived from olive leaf extract, inhibits tyrosinase activity and melanin production. They found that while oleuropein significantly inhibits tyrosinase and exhibits a good dose-dependent relationship, its inhibitory effect is still lower than that of kojic acid, the positive control, resulting in limited market application value. Therefore, exploring an economical and efficient novel tyrosinase-activating agent and developing corresponding whitening formulas based on it is an effective way to expand the daily chemical market.

[0004] In view of this, the present invention is proposed. Summary of the Invention

[0005] The purpose of this invention is to provide compositions that inhibit tyrosinase activity, whitening complexes, and daily chemical products. The compositions provided in the embodiments of this invention can effectively inhibit tyrosinase activity and reduce melanin formation. Furthermore, the complexes provided in the embodiments of this invention not only have excellent whitening effects but also possess various biological activities such as antioxidant, anti-inflammatory, anti-aging, moisturizing, and skin-nourishing properties, showing promising application prospects in the daily chemical market.

[0006] This invention is implemented as follows:

[0007] In a first aspect, the present invention provides a composition for inhibiting tyrosinase activity, wherein the raw materials comprise, by weight, 0.5-2.0 parts of hydroxytyrosol and 0.8-2.0 parts of resveratrol.

[0008] In an optional embodiment, the hydroxytyrosol is 0.8-2.0 parts by weight;

[0009] Preferably, the amount of resveratrol is 1.0-2.0 parts.

[0010] Secondly, the present invention provides a whitening complex, the raw materials of which include the composition for inhibiting tyrosinase activity as described in the foregoing embodiments.

[0011] In an optional embodiment, the raw materials further include at least one of whitening agents, moisturizers, emulsifiers, viscosity modifiers, pH modifiers, a matrix, and water.

[0012] In an optional embodiment, the raw materials, by weight percentage, include 0.5-2.0% hydroxytyrosol, 0.8-2.0% resveratrol, 0.1-3.0% whitening agent, 0.1-5.0% moisturizer, 0.1-2.0% emulsifier, 0.1-0.5% viscosity modifier, 0.05-0.1% pH adjuster, with the remainder being a matrix or water.

[0013] In an optional embodiment, the content of hydroxytyrosol is 0.8-2.0% by mass percentage;

[0014] Preferably, the resveratrol content is 1.0-2.0%;

[0015] Preferably, the content of the whitening agent is 1.0-3.0%;

[0016] Preferably, the content of the humectant is 0.5% to 3.0%;

[0017] Preferably, the content of the emulsifier is 1.0 to 2.0%;

[0018] Preferably, the content of the viscosity modifier is 0.3-0.5%.

[0019] In an optional embodiment, the moisturizer is selected from one or more mixtures of ceramides, squalane, hyaluronic acid and its salts, and cholesterol;

[0020] Preferably, the ceramide substance is selected from any one or a combination of two of ceramide 3 and ceramide 3B.

[0021] Preferably, the whitening agent is selected from niacinamide and / or α-arbutin;

[0022] Preferably, the emulsifier is selected from one or more mixtures of hydrogenated lecithin, glyceryl stearate, rhamnolipin, and sophorolipid;

[0023] Preferably, the viscosity modifier is selected from carbomer and / or xanthan gum;

[0024] Preferably, the pH adjuster is selected from citric acid and / or triethanolamine;

[0025] Preferably, the matrix is ​​selected from glycerol and / or ethanol.

[0026] Thirdly, the present invention provides a method for preparing the whitening complex described in the foregoing embodiments, comprising: mixing the raw materials.

[0027] In an optional implementation, it includes:

[0028] Hydroxytyrosol and resveratrol are mixed according to the specified ratio to form mixture A;

[0029] Mix the moisturizer, whitening agent, emulsifier and base according to the formula to form mixture B;

[0030] Mix the mixture A and the mixture B to form mixture C;

[0031] Mix mixture C with water, viscosity modifier, and pH modifier;

[0032] Preferably, the conditions for forming the mixture A include a temperature of 40-50°C;

[0033] The conditions for forming the mixture B include: a temperature of 50-60°C;

[0034] The conditions for forming the mixture C include: a temperature of 40-50℃, a homogenization speed of 2000-4500 rpm, a time of 10-20 min, and 1-3 cycles.

[0035] The mixing conditions for the mixture C, the viscosity modifier, and the pH modifier include: a temperature of 40-50°C, a homogenization speed of 7000-10000 rpm, and a time of 5-10 min.

[0036] Fourthly, the present invention provides a daily chemical product comprising the whitening complex described in the foregoing embodiments;

[0037] Preferably, the daily chemical products include skin care products, preferably any one of lotion, cream, facial cleanser, serum and mask.

[0038] This invention offers the following advantages: It innovatively selects hydroxytyrosol and resveratrol as active ingredients, which exhibit a good synergistic effect, effectively enhancing the composition's efficacy in inhibiting tyrosinase activity. In addition to inhibiting tyrosinase activity, the complex provided by this invention also possesses good antioxidant and free radical scavenging bioactivities, effectively reducing the occurrence of various skin diseases while further achieving a whitening effect. Furthermore, this complex has good transdermal absorption properties, maximizing the efficacy of each component. Simultaneously, the components forming this complex are mostly natural products, unlikely to cause harm to the human body, environmentally friendly, mild and non-irritating, and have a wide range of applications; moreover, the preparation process does not introduce harmful substances, is green and environmentally friendly, and the preparation process is simple and low-cost. Detailed Implementation

[0039] To make the objectives, technical solutions, and advantages of the embodiments of the present invention clearer, the technical solutions in the embodiments of the present invention will be clearly and completely described below. Where specific conditions are not specified in the embodiments, conventional conditions or conditions recommended by the manufacturer shall apply. Reagents or instruments whose manufacturers are not specified are all conventional products that can be purchased commercially.

[0040] This invention provides a composition for inhibiting tyrosinase activity, comprising, by weight, 0.5-2.0 parts hydroxytyrosol and 0.8-2.0 parts resveratrol.

[0041] In the composition provided by the embodiments of the present invention, hydroxytyrosol and resveratrol work together to exert a synergistic effect, enabling the composition to effectively inhibit tyrosine kinase activity.

[0042] The amount of hydroxytyrosol can be any value between 0.5 and 2 parts, or any range formed by any two values, such as 0.5 parts, 0.8 parts, 1 part, 1.2 parts, 1.5 parts, and 2 parts, for example, preferably 0.8 to 2.0 parts.

[0043] The amount of resveratrol can be any value between 0.8 and 2 parts, such as 0.8 parts, 1 part, 1.2 parts, 1.5 parts, and 2 parts, or any range formed by any two values, for example, preferably 1.0 to 2.0 parts.

[0044] Secondly, the present invention provides a whitening complex, the raw materials of which include the composition for inhibiting tyrosinase activity as described in the foregoing embodiments. It also includes at least one of a whitening agent, a moisturizer, an emulsifier, a viscosity modifier, a pH adjuster, a matrix, and water.

[0045] The whitening complex described above not only exerts the effects of the above-mentioned composition, but also, in combination with other substances, gives the complex better whitening, antioxidant, anti-inflammatory, anti-aging, moisturizing, and skin-nourishing effects, and can therefore be widely used in the field of skin care products.

[0046] Specifically, by weight percentage, its raw materials include 0.5–2.0% hydroxytyrosol, 0.8–2.0% resveratrol, 0.1–3.0% whitening agent, 0.1–5.0% moisturizer, 0.1–2.0% emulsifier, 0.1–0.5% viscosity modifier, 0.05–0.1% pH adjuster, with the remainder being matrix or water.

[0047] Specifically, the amount of hydroxytyrosol used is any value between 0.5% and 2.0%, or any range formed by any two values, such as 0.5%, 0.8%, 1.0%, 1.2%, 1.5%, and 2.0%. Preferably, it is 0.8% to 2.0%.

[0048] The amount of resveratrol used is any value between 0.8% and 2.0%, or any range formed by any two values, such as 0.8%, 1.0%, 1.2%, 1.5%, and 2.0%, preferably 1.0% to 2.0%.

[0049] The content of the whitening agent is any value or a range formed by any two values ​​between 0.1% and 3%. It is preferably 1.0% to 3.0%.

[0050] The content of the humectant is any value between 0.1% and 5.0, or any range formed by any two values, such as 0.1%, 0.5%, 0.8%, 1.0%, 1.2%, 1.5%, 2.0%, 2.5%, 3%, 3.5%, 4%, 4.5%, and 5%, preferably 0.5% to 3.0%.

[0051] The emulsifier content is any value between 0.1% and 2.0%, or any range formed by any two values, such as 0.1%, 0.5%, 0.8%, 1.0%, 1.2%, 1.5%, and 2.0%, preferably 1.0% to 2.0%.

[0052] The viscosity modifier content is any value between 0.1% and 0.5%, or any range formed by any two values, such as 0.1%, 0.2%, 0.3%, 0.4%, and 0.5%, preferably 0.3% to 0.5%.

[0053] The pH adjuster content is any value between 0.05% and 0.1%, or any range formed by any two values, such as 0.05%, 0.06%, 0.07%, 0.08%, 0.09%, and 0.1%.

[0054] The moisturizer is selected from one or more of the following: ceramides, squalane, hyaluronic acid and its salts, and cholesterol; the ceramide is selected from any one or a combination of two of ceramide 3 and ceramide 3B; the whitening agent is selected from niacinamide and / or α-arbutin; the emulsifier is selected from one or more of the following: hydrogenated lecithin, glyceryl stearate, rhamnolipid, and sophorolipid; the viscosity modifier is selected from carbomer and / or xanthan gum; the pH adjuster is selected from citric acid and / or triethanolamine; and the matrix is ​​selected from glycerin and / or ethanol.

[0055] Thirdly, the present invention provides a method for preparing the whitening complex described in the foregoing embodiments, comprising: mixing the raw materials.

[0056] Specifically, refer to the table below to roughly classify the raw materials:

[0057]

[0058]

[0059] Weigh out hydroxytyrosol and resveratrol according to the ratio, and mix and dissolve them in a water bath at 40℃~50℃ to form mixture A;

[0060] Weigh out the moisturizer, whitening agent, emulsifier and matrix according to the formula, and mix and dissolve them under a water bath condition of 50℃~60℃ to form mixture B;

[0061] Mixture B is added dropwise to phase A under stirring at 40-50℃. Then, it is homogenized using a high-speed stirring mill disperser at a speed of 2000-4500 rpm for 10-20 minutes, and 1-3 cycles are performed to form mixture C.

[0062] Mixture C was added dropwise to deionized water while stirring at 40–50°C. The viscosity and pH of the mixture were adjusted using viscosity modifier and pH modifier, respectively. The mixture was then homogenized using a high-speed stirring mill disperser at a speed of 7000 rpm–10000 rpm for 5–10 minutes.

[0063] After homogenization, the mixture was left to stand at room temperature for 5 to 10 minutes to obtain a whitening complex containing a composition that inhibits tyrosinase activity.

[0064] Fourthly, the present invention provides a daily chemical product comprising the whitening complex described in the foregoing embodiments;

[0065] Preferably, the daily chemical products include skin care products, preferably any one of lotion, cream, facial cleanser, serum and mask.

[0066] The features and performance of the present invention will be further described in detail below with reference to embodiments.

[0067] Example 1

[0068] This invention provides a whitening complex, the raw materials and dosages of which are shown in the table below.

[0069]

[0070]

[0071] This embodiment provides a method for preparing the above-mentioned whitening complex, including:

[0072] (1) Weigh out the raw materials of the above mass percentages, with 100g as the total mass of the raw materials forming the complex.

[0073] After the A phase raw materials are added and mixed according to the proportions in the table above, they are stirred and dissolved under a 45℃ water bath to obtain mixture A for later use; the B phase raw materials are dissolved in the matrix under a 50℃ water bath to obtain mixture B for later use.

[0074] (2) Mixture B is added to mixture A while stirring at 45°C. Then, a high-speed stirring mill disperser is used to homogenize the mixture at 4500 rpm for 15 min. Two cycles are performed to form mixture C.

[0075] (3) Mixture C was added dropwise to deionized water while stirring at 45°C. The viscosity and pH of the mixture were adjusted by viscosity modifier and pH modifier respectively. Then, it was homogenized by high-speed stirring mill dispersion at 8000 rpm for 5 min.

[0076] (4) The homogenized solution was left to stand at room temperature for 10 minutes to obtain a whitening complex solution containing a composition that inhibits tyrosinase activity.

[0077] Example 2

[0078] This invention provides a whitening complex, the raw materials and dosages of which are shown in the table below.

[0079]

[0080]

[0081] This embodiment provides a method for preparing the above-mentioned whitening complex, including:

[0082] (1) Weigh out the raw materials of the above mass percentages, with 100g as the total mass of the raw materials forming the complex.

[0083] After the A phase raw materials are added and mixed according to the proportions in the table above, they are stirred and dissolved under a 50℃ water bath to obtain mixture A for later use; the B phase raw materials are dissolved in the matrix under a 60℃ water bath to obtain mixture B for later use.

[0084] (2) Mixture B is added to mixture A while stirring at 50°C. Then, a high-speed stirring mill disperser is used to homogenize the mixture at 3000 rpm for 15 min. Three cycles are performed to form mixture C.

[0085] (3) Mixture C was added dropwise to deionized water while stirring at 50°C. The viscosity and pH of the mixture were adjusted by viscosity modifier and pH modifier, respectively. Then, it was homogenized by high-speed stirring mill dispersion at 10,000 rpm for 5 min.

[0086] (4) The homogenized solution was left to stand at room temperature for 10 minutes to obtain a whitening complex solution containing a composition that inhibits tyrosinase activity.

[0087] Example 3

[0088] This invention provides a whitening complex, the raw materials and dosages of which are shown in the table below.

[0089]

[0090]

[0091] This embodiment provides a method for preparing the above-mentioned whitening complex, including:

[0092] (1) Weigh out the raw materials of the above mass percentages, with 100g as the total mass of the raw materials forming the complex.

[0093] After the A phase raw materials are added and mixed according to the proportions in the table above, they are stirred and dissolved under a 50°C water bath to obtain mixture A for later use; the B phase raw materials are dissolved in the matrix under a 50°C water bath to obtain mixture B for later use.

[0094] (2) Mixture B is added to mixture A while stirring at 50°C. Then, a high-speed stirring mill disperser is used to homogenize the mixture at 4500 rpm for 20 min. Two cycles are performed to form mixture C.

[0095] (3) Mixture C was added dropwise to deionized water while stirring at 50°C. The viscosity and pH of the mixture were adjusted by viscosity modifier and pH modifier respectively. Then, it was homogenized by high-speed stirring mill dispersion at 10,000 rpm for 10 min.

[0096] (4) The homogenized solution was left to stand at room temperature for 10 minutes to obtain a whitening complex solution containing a composition that inhibits tyrosinase activity.

[0097] Example 4

[0098] This invention provides a whitening complex, the raw materials and dosages of which are shown in the table below.

[0099]

[0100]

[0101] This embodiment provides a method for preparing the above-mentioned whitening complex, including:

[0102] (1) Weigh out the raw materials of the above mass percentages, with 100g as the total mass of the raw materials forming the complex.

[0103] After the A phase raw materials are added and mixed according to the proportions in the table above, they are stirred and dissolved under a 40℃ water bath to obtain mixture A for later use; the B phase raw materials are dissolved in the matrix under a 60℃ water bath to obtain mixture B for later use.

[0104] (2) Mixture B is added to mixture A while stirring at 40°C. Then, a high-speed stirring mill disperser is used to homogenize the mixture at 2000 rpm for 20 min. Three cycles are performed to form mixture C.

[0105] (3) Mixture C was added dropwise to deionized water while stirring at 40°C. The viscosity and pH of the mixture were adjusted by viscosity modifier and pH modifier respectively. Then, it was homogenized by high-speed stirring mill dispersion at 7000 rpm for 10 min.

[0106] (4) The homogenized solution was left to stand at room temperature for 10 minutes to obtain a whitening complex solution containing a composition that inhibits tyrosinase activity.

[0107] Example 5

[0108] This invention provides a whitening complex, the raw materials and dosages of which are shown in the table below.

[0109]

[0110]

[0111] This embodiment provides a method for preparing the above-mentioned whitening complex, including:

[0112] (1) Weigh out the raw materials of the above mass percentages, with 100g as the total mass of the raw materials forming the complex.

[0113] After the A phase raw materials are added and mixed according to the proportions in the table above, they are stirred and dissolved under a 45℃ water bath to obtain mixture A for later use; the B phase raw materials are dissolved in the matrix under a 50℃ water bath to obtain mixture B for later use.

[0114] (2) Mixture B is added to mixture A while stirring at 45°C. Then, a high-speed stirring mill disperser is used to homogenize the mixture at 3000 rpm for 15 min. Three cycles are performed to form mixture C.

[0115] (3) Mixture C was added dropwise to deionized water while stirring at 45°C. The viscosity and pH of the mixture were adjusted by viscosity modifier and pH modifier respectively. Then, it was homogenized by high-speed stirring mill dispersion at 9000 rpm for 10 min.

[0116] (4) The homogenized solution was left to stand at room temperature for 10 minutes to obtain a whitening complex solution containing a composition that inhibits tyrosinase activity.

[0117] Example 6

[0118] This invention provides a whitening complex, the raw materials and dosages of which are shown in the table below.

[0119]

[0120] This embodiment provides a method for preparing the above-mentioned whitening complex, including:

[0121] (1) Weigh out the raw materials of the above mass percentages, with 100g as the total mass of the raw materials forming the complex.

[0122] After the A phase raw materials are added and mixed according to the proportions in the table above, they are stirred and dissolved under a 45℃ water bath to obtain mixture A for later use; the B phase raw materials are dissolved in the matrix under a 50℃ water bath to obtain mixture B for later use.

[0123] (2) Mixture B is added to mixture A while stirring at 45°C. Then, a high-speed stirring mill disperser is used to homogenize the mixture at 4500 rpm for 15 min. Two cycles are performed to form mixture C.

[0124] (3) Mixture C was added dropwise to deionized water while stirring at 45°C. The viscosity and pH of the mixture were adjusted by viscosity modifier and pH modifier respectively. Then, it was homogenized by high-speed stirring mill dispersion at 8000 rpm for 5 min.

[0125] (4) The homogenized solution was left to stand at room temperature for 10 minutes to obtain a whitening complex solution containing a composition that inhibits tyrosinase activity.

[0126] Comparative Example 1

[0127] This comparative example provides a whitening complex, which differs from Example 1 only in that resveratrol is omitted while maintaining the total amount added in phase A. The raw materials and amounts are shown in the table below.

[0128]

[0129] This embodiment provides a method for preparing the above-mentioned whitening complex, including:

[0130] (1) Weigh out the raw materials of the above mass percentages, with 100g as the total mass of the raw materials forming the complex.

[0131] Phase B raw material is dissolved in the matrix under a 50°C water bath to obtain mixture B for later use.

[0132] (2) Mixture B is added to mixture A while stirring at 45°C. Then, a high-speed stirring mill disperser is used to homogenize the mixture at 4500 rpm for 15 min. Two cycles are performed to form mixture C.

[0133] (3) Mixture C was added dropwise to deionized water while stirring at 45°C. The viscosity and pH of the mixture were adjusted by viscosity modifier and pH modifier respectively. Then, it was homogenized by high-speed stirring mill dispersion at 8000 rpm for 5 min.

[0134] (4) The homogenized solution was left to stand at room temperature for 10 minutes to obtain a whitening complex solution containing a composition that inhibits tyrosinase activity.

[0135] Comparative Example 2

[0136] This comparative example provides a whitening complex, which differs from Example 1 only in that it lacks the addition of tyrosol while maintaining the total amount added in phase A. The raw materials and amounts are shown in the table below.

[0137]

[0138] This embodiment provides a method for preparing the above-mentioned whitening complex, including:

[0139] (1) Weigh out the raw materials of the above mass percentages, with 100g as the total mass of the raw materials forming the complex.

[0140] Phase B raw material is dissolved in the matrix under a 50°C water bath to obtain mixture B for later use.

[0141] (2) Mixture B is added to mixture A while stirring at 45°C. Then, a high-speed stirring mill disperser is used to homogenize the mixture at 4500 rpm for 15 min. Two cycles are performed to form mixture C.

[0142] (3) Mixture C was added dropwise to deionized water while stirring at 45°C. The viscosity and pH of the mixture were adjusted by viscosity modifier and pH modifier respectively. Then, it was homogenized by high-speed stirring mill dispersion at 8000 rpm for 5 min.

[0143] (4) The homogenized solution was left to stand at room temperature for 10 minutes to obtain a whitening complex solution containing a composition that inhibits tyrosinase activity.

[0144] Comparative Example 3

[0145] This comparative example provides a whitening complex, which differs from Example 1 in that it contains ceramide 3B. The raw materials and dosages are shown in the table below.

[0146]

[0147]

[0148] This embodiment provides a method for preparing the above-mentioned whitening complex, including:

[0149] (1) Weigh out the raw materials of the above mass percentages, with 100g as the total mass of the raw materials forming the complex.

[0150] After the A phase raw materials are added and mixed according to the proportions in the table above, they are stirred and dissolved under a 45℃ water bath to obtain mixture A for later use; the B phase raw materials are dissolved in the matrix under a 50℃ water bath to obtain mixture B for later use.

[0151] (2) Mixture B is added to mixture A while stirring at 45°C. Then, a high-speed stirring mill disperser is used to homogenize the mixture at 4500 rpm for 15 min. Two cycles are performed to form mixture C.

[0152] (3) Mixture C was added dropwise to deionized water while stirring at 45°C. The viscosity and pH of the mixture were adjusted by viscosity modifier and pH modifier respectively. Then, it was homogenized by high-speed stirring mill dispersion at 8000 rpm for 5 min.

[0153] (4) The homogenized solution was left to stand at room temperature for 10 minutes to obtain a whitening complex solution containing a composition that inhibits tyrosinase activity.

[0154] Comparative Example 4

[0155] The whitening complex provided in this comparative example has the same formulation as that in Example 1, except that the preparation method is different. This comparative example lacks the homogenization step. The specific process is as follows:

[0156] (1) Weigh out the raw materials of the above mass percentages, with 100g as the total mass of the raw materials forming the complex.

[0157] After the A phase raw materials are added and mixed according to the proportions in the table above, they are stirred and dissolved under a 45℃ water bath to obtain mixture A for later use; the B phase raw materials are dissolved in the matrix under a 50℃ water bath to obtain mixture B for later use.

[0158] (2) Mixture B is added dropwise to mixture A while stirring at 45°C to form mixture C.

[0159] (3) Mixture C was added dropwise to deionized water while stirring at 45°C. The viscosity and pH of the mixture were adjusted by viscosity modifier and pH modifier, respectively. The mixture was then allowed to stand at room temperature for 10 minutes to obtain a whitening complex solution containing a composition that inhibits tyrosinase activity.

[0160] Comparative Example 5

[0161] This comparative example provides a whitening complex, which differs from Example 1 only in that, while maintaining the total amount added in phase A, resveratrol is replaced with an equal amount of another natural product with tyrosinase inhibitory activity, luteolin. The raw materials and amounts are shown in the table below.

[0162]

[0163] The preparation method of this whitening complex is the same as that in Example 1.

[0164] Comparative Example 6

[0165] This invention provides a whitening complex, which differs from Example 1 in that it uses the conventional emulsifier sorbitan monostearate instead of rhamnolipid, and its preparation method is the same as that of Example 1.

[0166] Test 1: Stability Test

[0167] (1) Heat resistance test

[0168] Take a portion of the whitening complex solution obtained in the above examples and comparative examples as a sample, and pour it into two test tubes with specifications of 20mm×120mm, so that the liquid level is about 80mm. Then, stopper the tubes with clean corks. Place one of the test tubes in a constant temperature incubator that has been pre-adjusted to the specified temperature ±1℃. After 24 hours, remove the tube, allow it to return to room temperature, and then visually compare it with the sample in the other test tube.

[0169] (2) Cold resistance test

[0170] Take a portion of the whitening complex solution obtained in the above examples and comparative examples as a sample, and pour it into two test tubes with specifications of 20mm×120mm, so that the liquid level is about 80mm. Then, stopper the tubes with clean corks. Place one of the test tubes to be tested in a refrigerator that has been pre-adjusted to a specified temperature ±2℃. After 24 hours, take it out, allow it to return to room temperature, and then visually compare it with the sample in the other test tube.

[0171] (3) Alternating heat and cold resistance test

[0172] After completing the heat resistance test (or cold resistance test), perform the cold resistance test (or heat resistance test) next. This is called a hot-cold cycle. Repeat this process until the tested sample shows phenomena such as oil-water separation, color change, or oil seepage. Record the number of cycles, and according to the book "7 Steps to Cosmetic Formulation Design" published by Chemical Industry Press, 7 cycles are the minimum standard for a qualified cosmetic formulation composition.

[0173] (4) Centrifugation test

[0174] Take a portion of the whitening complex solution obtained in the above examples and comparative examples as a sample. Pour the sample into a centrifuge tube to about two-thirds of its height and fill it tightly. Seal the tube with a cork. Then place it in an electric thermostatic incubator that has been pre-adjusted to (38±1)℃. After keeping it warm for 1 hour, immediately transfer it to a centrifuge and adjust the centrifugation speed to 2000 rpm. Rotate for 30 minutes and then take it out for observation.

[0175] The test results are shown in the table below:

[0176]

[0177]

[0178] Based on the above results, it can be seen that changing the preparation method and formulation of the whitening complex in this application (e.g., changing the emulsifier) ​​may affect the stability of the formed whitening complex, which also shows that the whitening complex provided in the embodiments of the present invention has good stability.

[0179] Test 2: Tyrosinase activity inhibition ability test

[0180] The tyrosinase activity inhibition ability of the whitening complexes provided in the embodiments and comparative examples of this invention was tested in accordance with "T / SHRH 015-2018 Cosmetics - Experimental Method for Inhibition of Tyrosinase Activity" and other relevant literature.

[0181] The required reagents include PBS disodium hydrogen phosphate-citrate buffer (pH 6.8, solvent), L-tyrosinase solution, levodopa solution, kojic acid solution (positive control sample), and complex solutions (samples) obtained from each example and comparative example. When levodopa reacts with tyrosinase to generate a colored substance, the absorbance of the solution after adding each sample is measured to calculate the tyrosinase activity inhibition rate.

[0182] Using 10 g / L kojic acid solution as a positive control sample, four groups were set up to test the tyrosinase activity inhibition ability of the complex solutions obtained in each example and comparative example. The concentration of each complex was prepared as a 10 g / L solution based on the total content of tyrosinase inhibitors.

[0183] T: Solvent background group, without L-tyrosine substrate solution or sample solution.

[0184] T0: Solvent reaction group, with substrate L-tyrosine solution added but sample solution not added.

[0185] C: Background sample group, without L-tyrosine solution as substrate.

[0186] C0: Sample reaction group, which includes both the substrate L-tyrosine solution and the sample solution.

[0187] The formula for calculating the tyrosinase activity inhibition rate is:

[0188] Where: Y—Tyrosinase activity inhibition rate; T—Absorbance of sample reaction wells; T0—Absorbance of sample background wells; C—Average absorbance of solvent reaction wells; C0—Average absorbance of solvent background wells.

[0189] The test results are as follows:

[0190] Example 1 66.54 Example 2 65.31 Example 3 67.43 Example 4 66.85 Example 5 68.27 Example 6 64.85 Control group (kojic acid) 51.43 Comparative Example 1 52.67 Comparative Example 2 48.31 Comparative Example 3 61.74 Comparative Example 4 60.28 Comparative Example 5 60.89 Comparative Example 6 62.31

[0191] According to the table above, (1) changing or replacing resveratrol or hydroxytyrosol in the composition will reduce the ability to inhibit tyrosine kinase activity, indicating that the two play a synergistic role.

[0192] (2) The preparation method and formulation provided by the embodiments of the present invention can effectively ensure the ability of the whitening complex to inhibit the activity of tyrosine kinase.

[0193] (3) The compositions of Comparative Example 4 and Comparative Example 6 could not be well miscible in the complex, resulting in uneven distribution of hydroxytyrosol and other enzyme-inhibiting components in the complex solution, which in turn reduced the overall concentration of hydroxytyrosol in the complex solution, thus reducing the enzyme-inhibiting ability.

[0194] Test 3: Free radical scavenging ability test

[0195] Following the experimental procedures for "DPPH free radical scavenging capacity determination" in the Chinese literature "Preparation and Antioxidant Activity Study of Hydroxytyrosol from Olive Leaves" (DOI: 10.27345 / d.cnki.gsnyu.2020.001087), the antioxidant effects of the whitening complexes obtained in the above examples and comparative examples were determined. The absorbance of the reaction solution was measured every 10 minutes, for a total of 3 measurements, and the DPPH free radical scavenging rate was calculated. The results are as follows:

[0196]

[0197] Based on the above results, it can be seen that changing the preparation method and formulation of the whitening complex in this application (e.g., changing the emulsifier) ​​may affect the ability of the formed whitening complex to scavenge free radicals, which also shows that the whitening complex provided in the embodiments of the present invention has good antioxidant capacity, that is, it has a good anti-aging effect.

[0198] Test 4: Absorption Effect Test

[0199] According to the relevant experiments in "2.4.3 Permeation Experiment Step" of the literature "Experimental Study on Transdermal Absorption of Neomycin Sulfate Ointment through Rat Ex vivo Burned Skin" published by Chen Yuebin et al., the transdermal absorption effect of the whitening complexes obtained in the above examples and comparative examples was measured by HPLC six times every 10 minutes, and the cumulative permeation amount of the complex in this scheme (calculated as the cumulative permeation amount of hydroxytyrosol / resveratrol) was calculated. The results are as follows:

[0200]

[0201] As can be seen from the table above, the whitening complex provided in this embodiment of the invention has excellent transdermal absorption performance and can maximize the efficacy of each ingredient.

[0202] The above description is merely a preferred embodiment of the present invention and is not intended to limit the invention. Various modifications and variations can be made to the present invention by those skilled in the art. Any modifications, equivalent substitutions, improvements, etc., made within the spirit and principles of the present invention should be included within the scope of protection of the present invention.

Claims

1. A composition for inhibiting tyrosinase activity, characterized in that, By weight, its active ingredient consists of 0.5-2.0 parts hydroxytyrosol and 0.8-2.0 parts resveratrol.

2. The composition for inhibiting tyrosinase activity according to claim 1, characterized in that, The hydroxytyrosol is 0.8-2.0 parts by weight.

3. The composition for inhibiting tyrosinase activity according to claim 1, characterized in that, The resveratrol is 1.0-2.0 parts by weight.

4. A whitening complex, characterized in that, The raw materials include the composition for inhibiting tyrosinase activity as described in any one of claims 1-3.

5. The whitening complex according to claim 4, characterized in that, The raw materials also include at least one of the following: whitening agent, moisturizer, emulsifier, viscosity modifier, pH modifier, matrix, and water.

6. The whitening complex according to claim 5, characterized in that, By weight percentage, its raw materials include 0.5-2.0% hydroxytyrosol, 0.8-2.0% resveratrol, 0.1-3.0% whitening agent, 0.1-5.0% moisturizer, 0.1-2.0% emulsifier, 0.1-0.5% viscosity modifier, 0.05-0.1% pH adjuster, and the remainder is matrix or water.

7. The whitening complex according to claim 6, characterized in that, The content of hydroxytyrosol is 0.8 to 2.0% by mass percentage.

8. The whitening complex according to claim 6, characterized in that, The resveratrol content is 1.0 to 2.0% by mass.

9. The whitening complex according to claim 6, characterized in that, The content of the whitening agent is 1.0 to 3.0% by mass percentage.

10. The whitening complex according to claim 6, characterized in that, The content of the humectant is 0.5 to 3.0% by mass percentage.

11. The whitening complex according to claim 6, characterized in that, The emulsifier content is 1.0 to 2.0% by mass percentage.

12. The whitening complex according to claim 6, characterized in that, The viscosity modifier content is 0.3 to 0.5% by mass percentage.

13. The whitening complex according to any one of claims 6-12, characterized in that, The moisturizer is selected from any one or more of the following: ceramides, squalane, hyaluronic acid and its salts, and cholesterol.

14. The whitening complex according to any one of claims 6-12, characterized in that, The ceramides are selected from any one or a combination of two of ceramide 3 and ceramide 3B.

15. The whitening complex according to any one of claims 6-12, characterized in that, The whitening agent is selected from niacinamide and / or α-arbutin.

16. The whitening complex according to any one of claims 6-12, characterized in that, The emulsifier is selected from one or more mixtures of hydrogenated lecithin, glyceryl stearate, rhamnolipin and sophorolipid.

17. The whitening complex according to any one of claims 6-12, characterized in that, The viscosity modifier is selected from carbomer and / or xanthan gum.

18. The whitening complex according to any one of claims 6-12, characterized in that, The pH adjuster is selected from citric acid and / or triethanolamine.

19. The whitening complex according to any one of claims 6-12, characterized in that, The matrix is ​​selected from glycerol and / or ethanol.

20. A method for preparing the whitening complex according to claim 4, characterized in that, include: Mix the raw materials.

21. The preparation method according to claim 20, characterized in that, include: Hydroxytyrosol and resveratrol are mixed according to the specified ratio to form mixture A; Mix the moisturizer, whitening agent, emulsifier and base according to the formula to form mixture B; Mix the mixture A and the mixture B to form mixture C; Mix mixture C with water, viscosity modifier and pH modifier.

22. The preparation method according to claim 21, characterized in that, The conditions for forming the mixture A include a temperature of 40-50°C; The conditions for forming the mixture B include: a temperature of 50-60°C; The conditions for forming the mixture C include: a temperature of 40-50℃, a homogenization speed of 2000-4500 rpm, a time of 10-20 min, and 1-3 cycles. The mixing conditions for the mixture C, the viscosity modifier, and the pH modifier include: a temperature of 40-50°C, a homogenization speed of 7000-10000 rpm, and a time of 5-10 min.

23. A daily chemical product, characterized in that, It includes the whitening complex as described in claim 4.

24. The daily chemical product according to claim 23, characterized in that, The aforementioned daily chemical products include skincare products.

25. The daily chemical product according to claim 23, characterized in that, The daily chemical products mentioned are any one of lotion, face cream, facial cleanser, serum and face mask.

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