Composition for improving whitening effect of alpha-arbutin, preparation method and application

Abstract

The invention relates to the technical field of biological medicine, and particularly discloses a composition for improving the whitening effect of alpha-arbutin, a preparation method and application. The composition is prepared from alpha-arbutin, lecithin, ethyoxyl diethylene glycol, a surface active agent and water. Researches show that lecithin and ethyoxyl diethylene glycol are simultaneously added into the composition, so that the whitening effect of alpha-arbutin can be synergistically improved; the composition disclosed by the invention is applied to a specific skin external preparation, the dosage of alpha-arbutin can be greatly reduced, and the composition has an important application value.

Description

Technical Field

[0001] The invention relates to the technical field of biomedicine, and in particular to a composition for increasing the whitening effect of alpha-arbutin, a preparation method and use thereof. Background Art

[0002] α-Arbutin Chemical Formula C 12 H 16 O7 is an ingredient extracted from the leaves of the Ericaceae plant Uva ursi. It is a classic whitening agent commonly used in the cosmetics market. It is characterized by significant whitening effect and high safety, but it also has the disadvantage of requiring a higher dose to achieve a significant whitening effect.

[0003] Through the study of the whitening kinetics of α-arbutin, it was found that its target in the human body is tyrosinase. α-arbutin needs to penetrate the cell membrane to enter the melanocytes to inhibit tyrosinase activity, block the melanin production chain and inhibit melanin production to achieve a whitening effect.

[0004] α-Arbutin is a water-soluble whitening raw material that is difficult to penetrate the cell membrane easily. The arbutin products on the market currently need to increase the addition to 3% to allow α-arbutin to enter the cell through the osmotic pressure difference to achieve the ideal whitening effect; but the price of α-arbutin is relatively high, and a high addition amount will increase the cost of the product. Therefore, a raw material compounding system is developed to increase the effect of α-arbutin at a low addition amount, thereby improving product effects and reducing product costs. Summary of the invention

[0005] In order to overcome at least one of the technical problems existing in the prior art, the present invention provides a composition for increasing the whitening effect of α-arbutin, a preparation method and use thereof.

[0006] The technical solution of the present invention is as follows:

[0007] The invention first provides a composition comprising alpha-arbutin, lecithin, ethoxydiglycol, a surfactant and water.

[0008] Preferably, the composition comprises the following components in percentage by weight:

[0009] α-Arbutin 8-12%; lecithin 1-3%; ethoxydiglycol 5-8%; surfactant 1-3%; water 60-80%.

[0010] The inventors surprisingly found in their research that, in the composition of the present invention, adding lecithin and ethoxydiglycol at the same time can synergistically improve the whitening effect of α-arbutin; the degree of improvement in the whitening effect of α-arbutin is much higher than that of the composition obtained by adding only lecithin or only ethoxydiglycol.

[0011] Preferably, the lecithin is soybean lecithin.

[0012] Preferably, the surfactant is Tween 80.

[0013] Preferably, the composition further comprises dipotassium glycyrrhizinate and trehalose.

[0014] Preferably, the composition comprises the following components in percentage by weight:

[0015] α-arbutin 8-12%; lecithin 1-3%; ethoxydiglycol 5-8%; surfactant 1-3%; dipotassium glycyrrhizinate 2-4%; trehalose 4-6%; water 60-80%.

[0016] Most preferably, the composition comprises the following components in percentage by weight:

[0017] α-Arbutin 10%; Lecithin 2%; Ethoxydiglycol 6%; Surfactant 2%; Dipotassium glycyrrhizinate 3%; Trehalose 5%; Water 72%.

[0018] Preferably, the composition is a composition that increases the whitening effect of α-arbutin.

[0019] The present invention also provides a method for preparing the above composition, which comprises the following steps:

[0020] Melting soybean lecithin and ethoxydiglycol to obtain a molten mixture;

[0021] α-arbutin, Tween 80, dipotassium glycyrrhizinate, trehalose and water are mixed and stirred to obtain a mixed solution;

[0022] Injecting mixed solution B into the molten mixture and mixing uniformly to obtain a mixed emulsion;

[0023] The mixed emulsion is sheared and emulsified to obtain a micron-sized dispersion, and then the micron-sized dispersion is homogenized and filtered through a microporous filter membrane to obtain the composition for increasing the whitening effect of α-arbutin.

[0024] The present invention also provides a use of the composition in preparing a skin external preparation.

[0025] Preferably, the skin topical preparation includes but is not limited to face cream, eye cream, neck cream, lotion, toner, essence, facial mask and sunscreen.

[0026] Beneficial effects: The present invention provides a new composition; studies have shown that adding lecithin and ethoxydiglycol to the composition can synergistically improve the whitening effect of α-arbutin; the composition of the present invention is applied to a specific skin external preparation, which can greatly reduce the amount of α-arbutin used, and has important application value.

[0027] In addition, by adding dipotassium oxalate and trehalose to the composition of the present invention, it can also prevent the α-arbutin composition from causing damage to the skin when opening the cell membrane channel, thereby reducing the irritation of α-arbutin to the skin. DETAILED DESCRIPTION

[0028] The present invention is further explained below in conjunction with specific examples, but the examples do not limit the present invention in any form.

[0029] Example 1 Preparation of the composition

[0030] The components of the composition in mass percentage are: 10% α-arbutin; 2% soybean lecithin; 6% ethoxydiglycol; 2% Tween 80; 3% dipotassium glycyrrhizate; 5% trehalose; and 72% water.

[0031] Preparation method:

[0032] S1. Melting soybean lecithin and ethoxydiglycol in a water bath at 60°C to obtain a molten mixture;

[0033] S2. α-arbutin, Tween 80, dipotassium glycyrrhizinate, trehalose and water were mixed in a 30°C water bath and stirred to obtain a mixed solution;

[0034] S3. The mixed solution is injected into the molten mixture and mixed to obtain a mixed emulsion;

[0035] S4. The mixed emulsion is high-speed sheared and emulsified at a rotation speed of 7000 rpm for 2 minutes to obtain a micron-sized dispersion, and then the micron-sized dispersion is placed in a high-pressure homogenizer and homogenized for 2 cycles at a pressure of 600 bar, and then filtered with a 0.45 μm microporous filter membrane to obtain the composition for increasing the whitening effect of α-arbutin.

[0036] Example 2 Preparation of the composition

[0037] The components of the composition by mass percentage are: 8% of α-arbutin; 3% of soybean lecithin; 5% of ethoxydiglycol; 3% of Tween 80; 2% of dipotassium glycyrrhizinate; 6% of trehalose; and 73% of water.

[0038] The preparation method is the same as Example 1.

[0039] Example 3 Preparation of the composition

[0040] The components of the composition in mass percentage are: 12% of α-arbutin; 1% of soybean lecithin; 8% of ethoxydiglycol; 1% of Tween 80; 4% of dipotassium glycyrrhizinate; 4% of trehalose; and 70% of water.

[0041] The preparation method is the same as Example 1.

[0042] Comparative Example 1 Preparation of the composition

[0043] The components of the composition by mass percentage are: α-arbutin 10%, soybean lecithin 8%, Tween 80 2%, dipotassium glycyrrhizinate 3%, trehalose 5%, and water 72%.

[0044] Preparation method:

[0045] S1. Melting soybean lecithin in a water bath at 60°C to obtain a molten mixture;

[0046] S2. α-arbutin, Tween 80, dipotassium glycyrrhizinate, trehalose and water were mixed in a 30°C water bath and stirred to obtain a mixed solution;

[0047] S3. The mixed solution is injected into the molten mixture and mixed to obtain a mixed emulsion;

[0048] S4. The mixed emulsion is high-speed sheared and emulsified at a rotation speed of 7000 rpm for 2 minutes to obtain a micron-sized dispersion, and then the micron-sized dispersion is placed in a high-pressure homogenizer and homogenized for 2 cycles at a pressure of 600 bar, and then filtered with a 0.45 μm microporous filter membrane to obtain the composition for increasing the whitening effect of α-arbutin.

[0049] The difference between Comparative Example 1 and Example 1 is that Comparative Example 1 does not contain ethoxydiglycol.

[0050] Comparative Example 2 Preparation of the composition

[0051] The components of the composition in mass percentage are: 10% α-arbutin; 8% ethoxydiglycol; 2% Tween 80; 3% dipotassium glycyrrhizinate; 5% trehalose; and 72% water.

[0052] Preparation method:

[0053] S1. melting ethoxydiglycol in a water bath at 60° C. to obtain a molten mixture;

[0054] S2. α-arbutin, Tween 80, dipotassium glycyrrhizinate, trehalose and water were mixed in a 30°C water bath and stirred to obtain a mixed solution;

[0055] S3. The mixed solution is injected into the molten mixture and mixed to obtain a mixed emulsion;

[0056] S4. The mixed emulsion is high-speed sheared and emulsified at a rotation speed of 7000 rpm for 2 minutes to obtain a micron-sized dispersion, and then the micron-sized dispersion is placed in a high-pressure homogenizer and homogenized for 2 cycles at a pressure of 600 bar, and then filtered with a 0.45 μm microporous filter membrane to obtain the composition for increasing the whitening effect of α-arbutin.

[0057] The difference between Comparative Example 1 and Example 1 is that Comparative Example 1 does not contain soybean lecithin.

[0058] Experimental Example 1: Zebrafish Model Body Surface Black Area Measurement Experiment

[0059] 1. Using the zebrafish model, compare the differences in whitening activity of monomeric α-arbutin and the test composition at various concentrations. The monomeric α-arbutin and the test composition were configured to the concentrations in Table 1. The experiment was set up with 3 replicate wells, with no less than 10 zebrafish embryos in each well. 1 mL of diluent was added to each well. After 48 hours, the embryos were fixed on a glass slide using methylcellulose fixative and the melanin on the back of the zebrafish embryos was photographed using a fluorescent upright microscope. The melanin area was calculated using ImageJ software.

[0060] 2. Experimental results

[0061] Table 1 Whitening efficacy data of monomeric α-arbutin and its combination on zebrafish

[0062]

[0063]

[0064] Table 1 shows that the monomer α-arbutin has a significant whitening effect when the addition amount is 2%, and the α-arbutin composition has a significant whitening effect when the addition amount is 0.4%, that is, it actually contains 0.04% of the monomer α-arbutin, which is equivalent to the effect of adding 4% of the monomer α-arbutin. It can be seen that the effective concentration of the composition of the present invention is much lower than that of the monomer α-arbutin, and only 1 / 100 of the addition amount of the monomer α-arbutin is needed to achieve a comparable effect; an unexpected technical effect is achieved.

[0065] In addition, it can be seen from the experimental results of Comparative Examples 1 and 2 that when the concentration of α-arbutin is low (≤0.1%), adding lecithin alone or ethoxydiglycol alone cannot effectively improve the whitening effect of α-arbutin; when the concentration of α-arbutin is low (≤0.1%), only by adding lecithin and ethoxydiglycol at the same time can the whitening effect of α-arbutin be greatly improved. When the concentration of α-arbutin is low (≤0.1%), adding lecithin and ethoxydiglycol at the same time can synergistically improve the whitening effect of α-arbutin.

[0066] Experimental Example 2: Zebrafish Model Body Surface Black Area Measurement Experiment

[0067] 1. Configure the basic formula according to Table 2

[0068] Table 2 Basic formula details

[0069]

[0070] Note: The whitening ingredients in the table are monomeric α-arbutin or α-arbutin composition.

[0071] 2. The experimental method is the same as that of Experimental Example 1.

[0072] 3. Experimental results

[0073] The experimental results are shown in Table 3.

[0074] Table 3 Whitening efficacy data of monomer α-arbutin and basic formula of the combination on zebrafish

[0075]

[0076]

[0077] Table 3 shows that in the formula with an addition amount of 4% of monomeric α-arbutin and α-arbutin combination, when the actual concentration of monomeric α-arbutin is the same, the whitening effect of adding the α-arbutin combination is significantly better than that of adding the monomeric α-arbutin. It can be seen that the effective concentration of the α-arbutin combination in the formula system is much lower than that of the monomeric α-arbutin.

Claims

1. A composition, characterized in that Contains alpha-arbutin, lecithin, ethoxydiglycol, surfactants and water.

2. The composition according to claim 1, characterized in that Contains the following components in mass percentage: α-Arbutin 8-12%; lecithin 1-3%; ethoxydiglycol 5-8%; surfactant 1-3%; water 60-80%.

3. The composition according to claim 1, characterized in that The lecithin is soybean lecithin.

4. The composition according to claim 1, characterized in that The surfactant is Tween 80.

5. The composition according to claim 1, characterized in that Also includes dipotassium glycyrrhizinate and trehalose.

6. The composition according to claim 5, characterized in that Contains the following components in mass percentage: α-arbutin 8-12%; lecithin 1-3%; ethoxydiglycol 5-8%; surfactant 1-3%; dipotassium glycyrrhizinate 2-4%; trehalose 4-6%; water 60-80%.

7. The method for preparing the composition according to any one of claims 1 to 6, characterized in that: The following steps are included: Melting soybean lecithin and ethoxydiglycol to obtain a molten mixture; α-arbutin, Tween 80, dipotassium glycyrrhizinate, trehalose and water are mixed and stirred to obtain a mixed solution; injecting the mixed solution into the molten mixture and mixing them uniformly to obtain a mixed emulsion; The mixed emulsion is sheared and emulsified to obtain a micron-sized dispersion, and then the micron-sized dispersion is homogenized and filtered through a microporous filter membrane to obtain the composition for increasing the whitening effect of α-arbutin.

8. Use of the composition according to any one of claims 1 to 7 in the preparation of an external skin preparation.

9. The use according to claim 8, characterized in that The skin topical preparations include, but are not limited to, facial creams, eye creams, neck creams, lotions, toners, essences, facial masks, and sunscreens.

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