Composition, cosmetic containing same and application of composition

Abstract

The invention discloses a composition, a cosmetic containing the composition and application of the composition, and relates to the technical field of cosmetics. The composition is prepared from the following raw materials: a coffee seed extract, a saccharomycetes fermentation product, a lactobacillus fermentation product, dihydric alcohol and water, the preparation method comprises the following steps: carrying out ultrasonic microfluid nano dispersion treatment on a mixture of the preparation raw materials to obtain the composition. The composition subjected to ultrasonic microfluid nano dispersion treatment has a good anti-oxidation effect, is mild and non-irritant, can also significantly improve the percutaneous permeability of ascorbic acid and water-soluble / fat-soluble derivatives thereof, and promotes the biological utilization of an organism on ascorbic acid and the derivatives thereof.

Description

Technical Field

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

[0002] Ascorbic acid is a common water-soluble vitamin with functions such as antioxidant and whitening. Ester derivatives, salt derivatives, ether derivatives, etc. of ascorbic acid also have good skin care effects. For example, the ascorbate derivative sodium ascorbyl phosphate has the effects of whitening and promoting collagen production; the ascorbic acid ester derivative ascorbyl tetraisopalmitate can prevent skin aging by promoting the growth of human fibroblasts; the ascorbic acid ether derivative 3-O-ethyl ascorbic acid has more stable chemical properties than ascorbic acid and has functions such as antioxidant and whitening. Ascorbic acid and its derivatives also have the advantages of being safe and non-toxic, and are very valuable cosmetic raw materials. However, the transdermal delivery effect of ascorbic acid and its derivatives is poor, it is difficult to penetrate to the basal layer to exert its effects, and the bioavailability is low. Therefore, it is necessary to develop a composition that can promote the penetration of ascorbic acid and its derivatives through the epidermis and reach the basal layer to exert its effects, so as to improve its bioavailability. Summary of the Invention

[0003] The present invention aims to solve at least one of the technical problems existing in the prior art. For this purpose, the present invention provides a composition that can effectively improve the transdermal penetration rate of ascorbic acid and its derivatives and promote the bioavailability of ascorbic acid and its derivatives by organisms.

[0004] The present invention also provides the application of the composition.

[0005] The present invention also provides a cosmetic.

[0006] The present invention also provides a method for promoting the transdermal penetration and absorption of ascorbic acid and / or ascorbic acid derivatives.

[0007] The composition according to the first aspect embodiment of the present invention comprises the following preparation raw materials:

[0008] Extract of Coffea arabica seeds, yeast fermentation product, Lactobacillus fermentation product, diol and water;

[0009] The preparation method of the composition comprises the following steps:

[0010] Performing ultrasonic microfluidic nanodispersion treatment on the mixture of each preparation raw material to obtain the composition.

[0011] The composition according to the embodiment of the present invention has at least the following beneficial effects:

[0012] The extract of Coffea arabica seeds is rich in phenolic acids and alkaloid components. The various organic acids, amino acids, and nitrogen-containing substances in the yeast fermentation products and lactic acid bacteria fermentation products can promote the penetration of active ingredients by increasing the gaps between skin cells through hydration. In addition, the phenolic acids and alkaloids in the extract of Coffea arabica seeds can covalently bind with some active substances to improve the solubility and stability of the active ingredients, which is beneficial for the active ingredients to penetrate through the stratum corneum of the skin. In the ultrasonic microfluidic channel, the ultrasonic cavitation bubbles and the composition collide frequently and efficiently in a narrow space. At the same time, the high-speed jets generated by the oscillation and collapse of the cavitation bubbles themselves can quickly disperse all the preparation raw materials, making the active substances and prebiotics in the extract of Coffea arabica seeds, yeast fermentation products, and lactic acid bacteria fermentation products disperse more evenly, forming stable and uniform nanoscale droplets, which can significantly improve the penetration-promoting effect of the composition.

[0013] After the composition of the embodiment is processed by ultrasonic microfluidic nanodispersion, it has good antioxidant efficacy, is mild and non-irritating, and can also improve the percutaneous penetration rate of ascorbic acid and its derivatives, promoting the utilization of ascorbic acid and its derivatives by organisms.

[0014] According to some embodiments of the present invention, by mass, the composition comprises:

[0015]

[0016] According to some embodiments of the present invention, by mass, the composition comprises:

[0017]

[0018] According to some embodiments of the present invention, by mass, the composition comprises:

[0019]

[0020] According to some embodiments of the present invention, by mass, the composition comprises:

[0021]

[0022] According to some embodiments of the present invention, the mass ratio of the extract of Coffea arabica seeds, yeast fermentation products, lactic acid bacteria fermentation products, diol, and water is (0.05 - 0.9):(0.15 - 1.8):(0.3 - 1.8):(0.8 - 1.2):1.

[0023] According to some embodiments of the present invention, the mass ratio of the extract of Coffea arabica seeds, yeast fermentation products, lactic acid bacteria fermentation products, diol, and water is (0.1 - 0.25):(0.2 - 0.45):(0.35 - 0.6):(0.9 - 1.1):1.

[0024] According to some embodiments of the present invention, the mass ratio of the Coffea arabica seed extract, yeast fermentation product, Lactobacillus fermentation product, diol, and water is (0.15 - 0.25):(0.35 - 0.45):(0.35 - 0.45):(0.9 - 1.1):1.

[0025] According to some embodiments of the present invention, the diol includes C3 - C8 diol.

[0026] According to some embodiments of the present invention, the diol includes at least one of 1,3 - propanediol, 1,2 - pentanediol, 1,2 - propanediol, butanediol, methylpropanediol, and hexanediol.

[0027] According to some embodiments of the present invention, the diol includes 1,2 - propanediol and butanediol. The mass ratio of the 1,2 - propanediol and butanediol is 1:(0.8 - 1.2).

[0028] According to some embodiments of the present invention, the ultrasonic microfluidic nanodispersion treatment is carried out by an ultrasonic microfluidic nanodisperser.

[0029] According to some embodiments of the present invention, the ultrasonic power of the ultrasonic microfluidic nanodispersion treatment is 200W - 800W. For example: it can be 200W, 250W, 300W, 350W, 400W, 450W, 500W, 550W, 600W, 650W, 700W, 750W, or 800W.

[0030] According to some embodiments of the present invention, the dispersion time of the ultrasonic microfluidic nanodispersion treatment is 1min - 3min. For example: it can be 1min, 1.1min, 1.2min, 1.3min, 1.4min, 1.5min, 1.6min, 1.7min, 1.8min, 1.9min, 2min, 2.1min, 2.2min, 2.3min, 2.4min, 2.5min, 2.6min, 2.7min, 2.8min, 2.9min, or 3min.

[0031] According to some embodiments of the present invention, the treatment temperature of the ultrasonic microfluidic nanodispersion treatment is 30°C - 45°C. For example: it can be 30°C, 31°C, 32°C, 33°C, 34°C, 35°C, 36°C, 37°C, 38°C, 39°C, 40°C, 41°C, 42°C, 43°C, 44°C, or 45°C.

[0032] Use of the above - mentioned composition according to the embodiments of the second aspect of the present invention in any one of A1) - A4):

[0033] A1) Promote the percutaneous permeation and absorption of ascorbic acid and / or ascorbic acid derivatives;

[0034] A2) Prepare products for promoting the percutaneous permeation and absorption of ascorbic acid and / or ascorbic acid derivatives;

[0035] A3) Antioxidant;

[0036] A4) Prepare antioxidant products.

[0037] According to some embodiments of the present invention, the application is for non-disease diagnosis and treatment purposes.

[0038] According to some embodiments of the present invention, the ascorbic acid derivatives include at least one of water-soluble ascorbic acid derivatives and lipid-soluble ascorbic acid derivatives.

[0039] According to some embodiments of the present invention, the water-soluble ascorbic acid derivatives include ascorbate derivatives.

[0040] According to some embodiments of the present invention, the ascorbate derivatives include at least one of sodium ascorbyl phosphate, magnesium ascorbyl phosphate, sodium ascorbate, magnesium ascorbate, and calcium ascorbate.

[0041] According to some embodiments of the present invention, the lipid-soluble ascorbic acid derivatives include at least one of ascorbyl ester derivatives and ascorbyl ether derivatives.

[0042] According to some embodiments of the present invention, the ascorbyl ester derivatives include at least one of ascorbyl tetraisopalmitate, ascorbyl palmitate, ascorbyl stearate, and ascorbyl dipalmitate.

[0043] According to some embodiments of the present invention, the ascorbyl ether derivatives include at least one of 2-O-ethyl ascorbic acid and 3-O-ethyl ascorbic acid.

[0044] According to some embodiments of the present invention, the products are selected from reagents, drugs, reagent kits, and cosmetics.

[0045] The cosmetics according to the embodiments of the third aspect of the present invention include the composition and active ingredients described in the embodiments of the first aspect;

[0046] The active ingredients include ascorbic acid and / or ascorbic acid derivatives.

[0047] According to some embodiments of the present invention, the addition amount of the composition in the cosmetic is 0.01% - 80% by mass fraction. For example, it can be 0.01%, 0.05%, 0.1%, 0.5%, 1%, 5%, 10%, 15%, 20%, 25%, 30%, 35%, 40%, 45%, 50%, 55%, 60%, 65%, 70%, 75% or 80%.

[0048] According to some embodiments of the present invention, the addition amount of the active ingredient in the cosmetic is 0.01% - 10% by mass fraction. For example, it can be 0.01%, 0.05%, 0.1%, 0.5%, 1%, 1.5%, 2%, 2.5%, 3%, 3.5%, 4%, 4.5%, 5%, 5.5%, 6%, 6.5%, 7%, 7.5%, 8%, 8.5%, 9%, 9.5% or 10%.

[0049] According to some embodiments of the present invention, the mass ratio of the composition to the active ingredient is (0.5 - 10):1. For example, it can be 0.5:1, 1:1, 1.5:1, 2:1, 2.5:1, 3:1, 3.5:1, 4:1, 4.5:1, 5:1, 5.5:1, 6:1, 6.5:1, 7:1, 7.5:1, 8:1, 8.5:1, 9:1, 9.5:1 or 10:1.

[0050] According to some embodiments of the present invention, the dosage form of the cosmetic is cream, lotion, aqueous solution, spray, essence, gel, facial mask or lotion.

[0051] According to some embodiments of the present invention, the cosmetic further comprises a cosmetically acceptable excipient.

[0052] A method for promoting the transdermal permeation and absorption of ascorbic acid and / or ascorbic acid derivatives according to the embodiments of the fourth aspect of the present invention includes the following steps:

[0053] Prepare a mixture containing the composition described in the embodiments of the first aspect and the ascorbic acid and / or ascorbic acid derivatives.

[0054] Other features and advantages of the present invention will be described in the subsequent specification, and, in part, will be obvious from the specification, or will be understood by implementing the present invention. Detailed Embodiments

[0055] The concept of the present invention and the resulting technical effects will be clearly and completely described below in conjunction with embodiments to fully understand the purpose, features, and effects of the present invention. Obviously, the described embodiments are only a part of the embodiments of the present invention, rather than all embodiments. Based on the embodiments of the present invention, other embodiments obtained by those skilled in the art without creative efforts shall fall within the scope of protection of the present invention.

[0056] For those not specified in the embodiments, they are carried out according to conventional conditions or conditions recommended by the manufacturer. For reagents or instruments without indicating the manufacturer, they are all conventional products that can be obtained through commercial purchase.

[0057] When a numerical range is disclosed herein, the above range is considered continuous and includes the minimum and maximum values of the range, as well as each value between such minimum and maximum values. Further, when the range refers to integers, it includes each integer between the minimum and maximum values of the range. In addition, when multiple ranges are provided to describe features or characteristics, the ranges can be combined. In other words, unless otherwise specified, all ranges disclosed herein should be understood to include any and all sub-ranges subsumed therein.

[0058] "Parts by mass" refers to the basic measurement unit representing the mass ratio relationship of multiple components. 1 part can represent any unit mass, such as 1 g or 2.689 g, etc. If we say that the mass fraction of component A is a parts and the mass fraction of component B is b parts, it means the mass ratio of component A to component B is a:b. Or, it means the mass of component A is aK and the mass of component B is bK (K is any number representing a multiple factor). It should not be misunderstood that, different from mass fraction, the sum of the mass fractions of all components is not limited to 100 parts.

[0059] "And / or" is used to indicate that either one or both of the described situations may occur. For example, A and / or B includes (A and B) and (A or B).

[0060] Unless otherwise specified, Coffea arabica seed extract, yeast fermentation product, Lactobacillus fermentation product, black tea extract, Streptococcus thermophilus fermentation product are all purchased from Guangzhou Noway Biotechnology Co., Ltd.; ascorbic acid and sodium ascorbyl phosphate are purchased from Aladdin Reagent (Shanghai) Co., Ltd., and 3-O-ethyl ascorbic acid is purchased from Nanjing Specco Biochemical Industry Co., Ltd.; ascorbyl tetraisopalmitate is purchased from Shanghai Macklin Reagent Co., Ltd.

[0061] Embodiment

[0062] This example provides a total of five compositions, namely Embodiment 1 - Embodiment 5. By mass, the composition of the composition is shown in Table 1.

[0063] Table 1

[0064]

[0065]

[0066] The specific steps of the preparation method of the composition are as follows:

[0067] Mix the Coffea arabica seed extract, yeast fermentation product, Lactobacillus fermentation product, deionized water, and diol, and then pump them into an ultrasonic microfluidic nano-dispersing machine (the instrument is purchased from Moge Microfluidic Technology Co., Ltd., model is Jizi No. 1) for ultrasonic microfluidic nano-dispersing treatment. The ultrasonic power is 600 W, the dispersing time is 2 min, and the treatment temperature is 35 °C to obtain the composition.

[0068] Application Example 1

[0069] This example provides an eye cream. In terms of mass fraction, the composition of the composition is shown in Table 2.

[0070] Table 2

[0071]

[0072]

[0073] This example also provides a preparation method of the eye cream. The steps are as follows:

[0074] 1) Put the oil-phase raw materials into an oil pan and heat up to 85 °C, then stir and disperse evenly;

[0075] 2) Put the water-phase raw materials into a water-phase pan and heat up to 85 °C, then stir and homogenize until completely swollen.

[0076] 3) Keep at 85 °C, pump the water phase into the emulsifying pan, then pump the oil phase and emulsify for 30 minutes, stir evenly, and keep the temperature at 85 °C during the emulsification process.

[0077] 4) After the emulsification is completed, cool down to 45 °C, add the active ingredient (tetraisopalmitate ascorbate), stir evenly, (evacuate and defoam), and then cool down to 37 °C, stir evenly and finely.

[0078] Comparative Example 1

[0079] This example provides a composition, which is basically the same as the composition in Example 1, except that: the yeast fermentation product and the Lactobacillus fermentation product are replaced with an equal amount of Coffea arabica seed extract.

[0080] In terms of mass parts, the composition is composed of the following preparation raw materials:

[0081] Coffea arabica seed extract 100 parts;

[0082] 100 parts of deionized water;

[0083] 1,3-Propanediol 100 parts.

[0084] The preparation method of the composition is the same as that of Example 1.

[0085] Comparative Example 2

[0086] This example provides a composition, which is substantially the same as the composition of Example 1, except that the Arabica coffee seed extract and the lactobacillus fermentation product are replaced with an equal amount of yeast fermentation product.

[0087] The composition is composed of the following raw materials by weight:

[0088] 100 parts of yeast fermentation products;

[0089] 100 parts of deionized water;

[0090] 1,3-Propanediol 100 parts.

[0091] The preparation method of the composition is the same as that of Example 1.

[0092] Comparative Example 3

[0093] This example provides a composition that is substantially the same as the composition of Example 1, except that the Arabica coffee seed extract and the yeast fermentation product are replaced with an equal amount of lactobacillus fermentation product.

[0094] The composition is composed of the following raw materials by weight:

[0095] 100 parts of lactobacillus fermentation product;

[0096] 100 parts of deionized water;

[0097] 1,3-Propanediol 100 parts.

[0098] The preparation method of the composition is the same as that of Example 1.

[0099] Comparative Example 4

[0100] This example provides a composition, which is substantially the same as the composition of Example 1, except that the Arabica coffee seed extract is replaced with an equal amount of black tea extract.

[0101] The composition is composed of the following raw materials by weight:

[0102] 20 parts of black tea extract;

[0103] 40 parts of yeast fermentation products;

[0104] 40 parts of lactobacillus fermentation products;

[0105] 100 parts of deionized water;

[0106] 100 parts of 1,3 - propanediol.

[0107] The preparation method of this composition is the same as that of Example 1.

[0108] Comparative Example 5

[0109] This example provides a composition, which is basically the same as the composition of Example 1, except that: the yeast fermentation product is replaced with an equal amount of Streptococcus thermophilus fermentation product.

[0110] Calculated by mass parts, this composition is composed of the following raw materials for preparation:

[0111] 20 parts of Coffea arabica seed extract;

[0112] 40 parts of Streptococcus thermophilus fermentation product;

[0113] 40 parts of Lactobacillus fermentation product;

[0114] 100 parts of deionized water;

[0115] 100 parts of 1,3 - propanediol.

[0116] The preparation method of this composition is the same as that of Example 1.

[0117] Comparative Example 6

[0118] This example provides a composition, which is basically the same as the composition of Example 1, except that: the Lactobacillus fermentation product is replaced with an equal amount of Streptococcus thermophilus fermentation product.

[0119] Calculated by mass parts, this composition is composed of the following raw materials for preparation:

[0120]

[0121] The preparation method of this composition is the same as that of Example 1.

[0122] Comparative Example 7

[0123] This example provides a composition, which is basically the same as the composition of Example 1, except that: there are differences in the preparation method.

[0124] Calculated by mass parts, this composition is composed of the following raw materials for preparation:

[0125]

[0126] The specific steps of the preparation method of this composition are as follows:

[0127] After mixing small-fruited coffee seed extract, yeast fermentation product, lactobacillus fermentation product, deionized water, and diol, ultrasonic dispersion treatment is carried out with an ultrasonic power of 600 W and a dispersion time of 2 min to obtain the composition.

[0128] Comparative Example 8

[0129] This example provides a composition, which is basically the same as the composition of Example 1, except that the small-fruited coffee seed extract, yeast fermentation product, and lactobacillus fermentation product are replaced with an equal amount of deionized water.

[0130] Calculated by mass parts, the composition is composed of the following preparation raw materials:

[0131] Deionized water 200 parts;

[0132] 1,3-propanediol 100 parts.

[0133] The preparation method of this composition is the same as that of Example 1.

[0134] Comparative Example 9

[0135] This example provides a composition, which is basically the same as the composition of Example 1, except that 1,3-propanediol is replaced with an equal amount of deionized water.

[0136] Calculated by mass parts, the composition is composed of the following preparation raw materials:

[0137]

[0138] The preparation method of this composition is the same as that of Example 1.

[0139] Comparative Example 10

[0140] This example provides a penetration enhancer, which is deionized water.

[0141] Application of Comparative Example 1

[0142] This example provides an eye cream, which is basically the same as the eye cream of Application Example 1, except that the composition of Example 1 is replaced with an equal amount of the composition of Comparative Example 1.

[0143] The preparation method of this eye cream is the same as that of Application Example 1.

[0144] Experimental Example 1

[0145] This experimental example respectively tests the DPPH free radical scavenging ability and total antioxidant ability of the compositions of Examples 1-5 and Comparative Examples 1-10.

[0146] 1. IC 50 value represents the amount of the test substance required to scavenge half of the DPPH free radicals, IC 50The lower the value, the better the scavenging effect of the test substance on DPPH free radicals.

[0147] Samples obtained by gradient dilution of the compositions of Examples 1-5 and Comparative Examples 1-10 with deionized water were used as test substances (the concentration was expressed as the mass percentage of the composition in the test substance). Precisely pipette 2 mL of ethanol and 2 mL of DPPH solution (0.0414 mg / mL) into a 10 mL EP tube in sequence. After mixing, shake well, and let stand for 30 min. Then measure the absorbance (A1) at 517 nm. Precisely pipette 2 mL of ethanol and 2 mL of the test substance into a 10 mL EP tube in sequence. After mixing, shake well, and let stand for 30 min. Then measure the absorbance (A2) at 517 nm. Precisely pipette 2 mL of DPPH solution (0.0414 mg / mL) and 2 mL of the test substance into a 10 mL stoppered test tube in sequence. After mixing, shake well, and let stand for 30 min. Then measure the absorbance (A3) at 517 nm. Measure in parallel 2 times. After calculating the scavenging rate, calculate the IC 50 value.

[0148] Scavenging rate = (1 - (A3 - A2) / A1) × 100%.

[0149] The experimental results are shown in Table 3 below.

[0150] Table 3

[0151]

[0152]

[0153] The compositions of Examples 1-5 all had good DPPH free radical scavenging ability and good antioxidant activity. When any one of the small fruit coffee seed extract, yeast fermentation product, and lactic acid bacteria fermentation product was missing, or the composition was not subjected to ultrasonic microfluidic nanodispersion treatment, the DPPH free radical scavenging ability would be significantly deteriorated. Therefore, the combination of small fruit coffee seed extract, yeast fermentation product, and lactic acid bacteria fermentation product with ultrasonic microfluidic nanodispersion treatment could synergistically improve its DPPH free radical scavenging ability.

[0154] 2. Under low pH conditions, ferrous ions react with TPTZ (tripyridyltriazine) to form a blue-violet complex, which can thus be used to evaluate the antioxidant ability of the test substance.

[0155] Add 200 μL of the test substance (the compositions of Examples 1-5 and Comparative Examples 1-10) into a reaction tube, and then add 6 mL of FRAP working solution (obtained by mixing 30 mL of 300 mmol / L acetate buffer (pH 3.6), 3 mL of 10 mmol / L TPTZ solution and 3 mL of 20 mmol / L FeCl3·6H2O solution). Mix well, react at 37 °C for 15 min, measure the absorbance at 593 nm, and repeat each experiment three times. Use a standard solution of FeSO4 with a concentration of 0.1 mmol / L - 1.6 mmol / L to replace the test substance for testing, draw a standard curve, substitute the absorbance value of the test substance into the standard curve, and express its total antioxidant capacity (FRAP value) in terms of the equivalent concentration of FeSO4 (unit: mmol / L).

[0156] The experimental results are shown in Table 4 below.

[0157] Table 4

[0158] Sample FRAP value (mmol) Sample FRAP value (mmol) Sample FRAP value (mmol) Example 1 183.61 Comparative Example 1 95.86 Comparative Example 6 100.33 Example 2 175.95 Comparative Example 2 92.22 Comparative Example 7 112.16 Example 3 169.26 Comparative Example 3 102.17 Comparative Example 8 90.56 Example 4 163.85 Comparative Example 4 113.40 Comparative Example 9 116.63 Example 5 141.16 Comparative Example 5 107.51 Comparative Example 10 85.47

[0159] The compositions of Examples 1-5 all have good total antioxidant capacity. When any one of the small fruit coffee seed extract, yeast fermentation product, and lactic acid bacteria fermentation product is absent, or the composition is not subjected to ultrasonic microfluidic nanodispersion treatment, the total antioxidant capacity of the composition will be significantly deteriorated. Therefore, the combination of small fruit coffee seed extract, yeast fermentation product, and lactic acid bacteria fermentation product with ultrasonic microfluidic nanodispersion treatment can synergistically improve its total antioxidant capacity.

[0160] Experimental Example 2

[0161] This experimental example respectively tests the effects of the compositions of Examples 1-5 and Comparative Examples 1-10 on the transdermal absorption of active ingredients (ascorbic acid, sodium ascorbyl phosphate, 3-O-ethyl ascorbic acid, ascorbyl tetraisopalmitate).

[0162] An osmosis experiment was carried out using a Franz vertical double-chamber osmosis diffusion cell, and the effective osmosis area was 1.77 cm 2, the receiving pool had a volume of 12 mL, and a PBS buffer solution containing 20% (v / v) ethanol was prepared as the receiving solution. The excised porcine skin was cut into an appropriate size, with the stratum corneum facing up, and placed between the two half-cells of the diffusion chamber and the receiving chamber of the Franz vertical diffusion cell, and fixed with clips. The receiving chamber was filled with the receiving solution so that the liquid level just contacted the skin, ensuring that there were no bubbles between the receiving solution and the porcine skin, and a magnetic stirring rotor was added to the receiving pool. After accurately weighing 0.1 g of the test substance (obtained by mixing 3 wt% active ingredient, 10 wt% composition, and 87 wt% deionized water) and placing it in the diffusion chamber, the receiving pool was heated in a constant temperature water bath at 32 ± 0.5 °C. The magnetic stirrer was turned on and stirred at a speed of 300 rpm. 1 mL of the receiving solution was aspirated at 1, 2, 4, 6, 8, 10, and 24 h respectively. After each sampling, 1 mL of blank receiving solution at the same temperature was immediately added. The HLPC-DAD method was used to measure the concentration of the active ingredient in the receiving solution at different time periods, and the cumulative permeability was calculated.

[0163] Q = [C n ×V + ∑C i ×V0] / S (i = 1···n - 1);

[0164] Q: Cumulative permeation amount (μg); V: Volume of the receiving solution in the receiving chamber; V0: Volume of each sampling; C i : Concentration of the active ingredient in the receiving solution from the first sampling to the previous sampling; C n : Concentration of the active ingredient measured at the nth sampling point; S: Effective permeation area (1.77 cm 2 ).

[0165] Cumulative permeability = Q × S / M × 100%;

[0166] Q: Cumulative permeation amount (μg / cm 2 ); S: Effective permeation area (1.77 cm 2 ); M: Added amount of the active ingredient (μg).

[0167] The detection conditions for ascorbic acid, sodium ascorbyl phosphate, and 3 - O - ethyl ascorbic acid were as follows: Agilent 1260 high - performance liquid chromatograph, Agilent Zorbox EC - C18 column (4.6 × 150 mm, 2.7 μm); ultraviolet spectrophotometric detector; injection volume was 10 μL, flow rate was 0.5 mL / min, and detection wavelength was 245 nm. The mobile phase was 0.1% (v / v) acetic acid aqueous solution (solution A) and methanol (solution B). The gradient elution conditions were: 0 - 5 min (B 5%), 5 - 7 min (B 5 - 80%), 8 - 15 min (B 80%).

[0168] The detection conditions for ascorbyl tetraisopalmitate are as follows: Agilent 1260 high performance liquid chromatograph, Agilent Zorbox EC-C18 column (4.6×150mm, 2.7μm); ultraviolet spectrophotometric detector; injection volume is 10 μL, flow rate is 0.5 mL / min, detection wavelength is 236 nm. The mobile phase is isopropanol (solution A) and methanol (solution B). The isocratic elution conditions are: 0 - 12 min (B 25%).

[0169] 1. The effects of the compositions of Examples 1 - 5 and Comparative Examples 1 - 10 on the transdermal absorption of the active ingredient ascorbic acid.

[0170] The experimental results are shown in Table 5 below.

[0171] Table 5

[0172]

[0173] 2. The effects of the compositions of Examples 1 - 5 and Comparative Examples 1 - 10 on the transdermal absorption of the active ingredient sodium ascorbyl phosphate. The experimental results are shown in Table 6 below.

[0174] Table 6

[0175]

[0176]

[0177] 3. The effects of the compositions of Examples 1 - 5 and Comparative Examples 1 - 10 on the transdermal absorption of the active ingredient 3 - O - ethyl ascorbic acid. The experimental results are shown in Table 7 below.

[0178] Table 7

[0179]

[0180]

[0181] 4. The effects of the compositions of Examples 1 - 5 and Comparative Examples 1 - 10 on the transdermal absorption of the active ingredient ascorbyl tetraisopalmitate.

[0182] The experimental results are shown in Table 8 below.

[0183] Table 8

[0184]

[0185]

[0186] The compositions of Examples 1-5 have good percutaneous absorption enhancing effects on ascorbic acid, water-soluble ascorbic acid derivatives (sodium ascorbyl phosphate), and lipid-soluble ascorbic acid derivatives (3-O-ethyl ascorbic acid, ascorbyl tetraisopalmitate). When any one of the coffee arabica seed extract, yeast fermentation product, and lactobacillus fermentation product is absent, or the composition is not subjected to ultrasonic microfluidic nanodispersion treatment, the percutaneous absorption enhancing effect will be greatly deteriorated. Therefore, the combined ultrasonic microfluidic nanodispersion treatment of coffee arabica seed extract, yeast fermentation product, and lactobacillus fermentation product can synergistically improve the percutaneous penetration rate of ascorbic acid and its derivatives and enhance their bioavailability.

[0187] Experimental Example 3

[0188] This experimental example respectively tested the irritation of the compositions of Examples 1-5 and Comparative Examples 1-10 to the chorioallantoic membrane of chicken embryos.

[0189] Select chicken embryos at 9 days old with a mass of 50 g - 60 g. Mark the position of the air chamber on the eggshell surface, remove part of the eggshell to expose the white egg membrane, and after wetting the egg membrane with physiological saline, remove it with forceps. Take 0.3 mL of the composition and directly apply it to the chorioallantoic membrane (CAM) to ensure that the coverage area reaches at least 50%. Immediately observe the reaction of the CAM until 5 min and stop, record the observation results and make a judgment. Each sample is repeated 3 times, and physiological saline is used as a negative control. Calculate the irritation score (IS) according to the HET-CAM test score.

[0190]

[0191] where; sec H (bleeding time) - the average time when bleeding is observed on the CAM, in seconds;

[0192] sec L (vascular lysis time) - the average time when vascular lysis is observed on the CAM, in seconds;

[0193] sec C (coagulation time) - the average time when coagulation is observed on the CAM, in seconds;

[0194] Evaluation criteria: IS < 1 is non-irritating, 1 ≤ IS < 5 is slightly irritating, and 5 ≤ IS < 10 is moderately irritating.

[0195] The experimental results are shown in Table 9 below.

[0196] Table 9

[0197] Sample Irritation level Sample Irritation level Sample Irritation level Example 1 Non-irritating Comparative Example 1 Non-irritating Comparative Example 6 Non-irritating Example 2 Non-irritating Comparative Example 2 Non-irritating Comparative Example 7 Non-irritating Example 3 Non-irritating Comparative Example 3 Non-irritating Comparative Example 8 Non-irritating Example 4 Non-irritating Comparative Example 4 Slight irritation Comparative Example 9 Non-irritating Example 5 Non-irritating Comparative Example 5 Non-irritating Comparative Example 10 Non-irritating

[0198] The compositions of Examples 1-5 are all non-irritating and have good mildness. When the coffee arabica seed extract is replaced with an equal amount of black tea extract, there is slight irritation.

[0199] Experimental Example 4

[0200] In this experimental example, the transdermal effects of tetraisopalmitate ascorbate in the eye creams of Application Example 1 and Application Comparative Example 1 were respectively tested. The testing method was the same as that in Experimental Example 3.

[0201] The experimental results are shown in Table 10 below.

[0202] Table 10

[0203] Sample 24h cumulative permeability Application Example 1 4.92％ Application Comparative Example 1 3.43％

[0204] The 24-hour cumulative penetration rate of tetraisopalmitate ascorbate in the eye cream of Application Example 1 was significantly higher than that of Application Comparative Example 1. The composition of the present invention can effectively promote the transdermal absorption of tetraisopalmitate ascorbate in cosmetics.

[0205] Experimental Example 5

[0206] In this experimental example, the brightening and dark circle improvement effects of the eye creams of Application Example 1 and Application Comparative Example 1 were respectively tested.

[0207] Sixty volunteers (aged 30 - 55 years) with obvious dark circles and rough and dull facial skin were recruited and randomly divided into 2 groups, and the eye creams of Application Example 1 and Application Comparative Example 1 were used respectively. It was applied around the eye area morning and evening every day, about 2 mg / cm 2 , gently pressed and massaged until absorbed, and used continuously for 14 days. At D0 (before use), D7 (on the 7th day of use), and D14 (on the 14th day of use), under the conditions of temperature 21 ± 1 °C and humidity 50 ± 10%, after the subjects cleaned their faces and waited for 20 min, the skin lightness L* value and skin melanin content (MI value) were measured, and the average values of each group of data were calculated. The larger the skin lightness L* value, the brighter the skin color. The smaller the MI value, the lower the skin melanin content.

[0208] The experimental results are shown in Table 11 below.

[0209] Table 11

[0210]

[0211] Among the 30 volunteers using the eye cream of Application Example 1, at the 7th day and 14th day, the skin lightness L* values were higher than those of the Application Comparative Example 1 group, and the skin melanin MI values were lower than those of the Application Comparative Example 1 group. This shows that using the eye cream of Application Example 1 can effectively brighten the skin color and reduce the skin melanin content.

[0212] The embodiments of the present invention have been described in detail above in conjunction with the embodiments, but the present invention is not limited to the above embodiments. Within the scope of knowledge possessed by those of ordinary skill in the art, various changes can be made without departing from the gist of the present invention.

Claims

1. A composition, characterized in that The preparation includes the following raw materials: Arabica coffee seed extract, saccharomyces ferment, lactobacillus ferment, glycols and water; The preparation method of the composition comprises the following steps: The mixture of each prepared raw material is subjected to ultrasonic microfluidic nano-dispersion treatment to obtain the composition.

2. The composition according to claim 1, characterized in that In parts by mass, the composition comprises: 10-40 parts of Arabica coffee seed extract; 20-85 parts of yeast fermentation products; 35-85 parts of lactobacillus fermentation products; 40-110 parts of diol; 40-110 parts of water; Preferably, the composition comprises, by weight: 13-20 parts of Arabica coffee seed extract; 24-40 parts of yeast fermentation products; 40-54 parts of lactobacillus fermentation product; 98-102 parts of diol; Water 98-102 parts; Preferably, the composition comprises, by weight: 18-22 parts of Arabica coffee seed extract; 38-42 parts of yeast fermentation products; 38-42 parts of lactobacillus fermentation products; 98-102 parts of diol; 98-102 parts of water.

3. The composition according to claim 1, characterized in that The diol includes at least one of 1,3-propylene glycol, 1,2-pentanediol, 1,2-propylene glycol, butanediol, methylpropanediol, and hexanediol; And / or, the ultrasonic power of the ultrasonic microfluidic nanodispersion treatment is 200W-800W; And / or, the dispersion time of the ultrasonic microfluidic nanodispersion treatment is 1 min-3 min; And / or, the processing temperature of the ultrasonic microfluidic nano-dispersion treatment is 30°C-45°C.

4. Use of the composition according to any one of claims 1 to 3 in any one of A1) to A4): A1) promoting the percutaneous permeation and absorption of ascorbic acid and / or ascorbic acid derivatives; A2) preparing a product for promoting the percutaneous permeation and absorption of ascorbic acid and / or ascorbic acid derivatives; A3) Antioxidant; A4) Preparation of antioxidant products.

5. The use according to claim 4, characterized in that: The ascorbic acid derivative includes at least one of a water-soluble ascorbic acid derivative and a fat-soluble ascorbic acid derivative.

6. The use according to claim 5, characterized in that: The water-soluble ascorbic acid derivatives include ascorbate derivatives; Preferably, the ascorbate derivatives include at least one of sodium ascorbyl phosphate, magnesium ascorbyl phosphate, sodium ascorbate, magnesium ascorbate, and calcium ascorbate.

7. The use according to claim 5, characterized in that: The fat-soluble ascorbic acid derivative includes at least one of an ascorbic acid ester derivative and an ascorbic acid ether derivative; Preferably, the ascorbyl ester derivatives include at least one of ascorbyl tetraisopalmitate, ascorbyl palmitate, ascorbyl stearate, and ascorbyl dipalmitate; Preferably, the ascorbic acid ether derivative includes at least one of 2-o-ethyl ascorbic acid and 3-o-ethyl ascorbic acid.

8. A cosmetic, characterized in that: include: The composition and active ingredient according to any one of claims 1 to 3; The active ingredient includes ascorbic acid and / or ascorbic acid derivatives.

9. The cosmetic according to claim 8, characterized in that: Calculated by mass fraction, the added amount of the active ingredient in the cosmetic is 0.01%-10%.

10. A method for promoting the percutaneous permeation and absorption of ascorbic acid and / or ascorbic acid derivatives, characterized in that: The following steps are involved: A mixture comprising the composition according to any one of claims 1 to 3 and the ascorbic acid and / or ascorbic acid derivative is prepared.

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