Method for manufacturing a whitening composition
A whitening composition with eugenin, ellagic acid, and gallic acid, along with rose and papaya seed extracts, effectively inhibits tyrosinase to provide superior skin-whitening benefits by suppressing melanin production.
Patent Information
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- TOYO HAKKO
- Filing Date
- 2024-12-19
- Publication Date
- 2026-07-01
AI Technical Summary
Existing cosmetic compositions fail to provide sufficient skin-whitening effects to meet the growing consumer demand for effective whitening products.
A whitening composition containing eugenin, ellagic acid, and gallic acid, with specific mass ratios and concentrations, optionally including rose and papaya seed extracts, to inhibit tyrosinase activity and suppress melanin production.
The composition achieves superior skin-whitening effects by synergistically inhibiting tyrosinase activity, preventing darkening and freckles, with enhanced efficacy when specific component ratios and concentrations are met.
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Abstract
Description
[Technical Field]
[0001] This invention relates to a whitening composition. [Background technology]
[0002] Generally, adverse effects on the skin caused by ultraviolet (UV) radiation, such as tanning, dark spots, and freckles, are due to the production of melanin, a blackish-brown, amorphous pigment. Melanin is produced when UV radiation activates tyrosinase, an enzyme present in melanocytes in the skin, which oxidizes tyrosine, a protein-forming amino acid.
[0003] Therefore, it is expected that inhibiting the activity of tyrosinase, which is involved in melanin production, will have a skin-whitening effect. For this reason, as shown in Patent Document 1, for example, the incorporation of tyrosinase activity-inhibiting ingredients into cosmetics has been proposed. [Prior art documents] [Patent Documents]
[0004] [Patent Document 1] Japanese Patent Application Publication No. 1-85907 [Overview of the project] [Problems that the invention aims to solve]
[0005] However, the cosmetic composition described in Patent Document 1 was unable to provide sufficient whitening effects to meet the growing consumer interest in skin whitening and the increasing demand for whitening products in recent years. Therefore, there is a need to provide a whitening composition with superior whitening effects. [Means for solving the problem]
[0006] These objectives are achieved by the present invention as described in (1) to (7) below. (1) Contains eugenin, ellagic acid, and gallic acid, The ellagic acid content per 1 part by mass of eugeniin is 5 parts by mass or more and 15 parts by mass or less. A skin whitening composition characterized in that the content of gallic acid per 1 part by mass of eugenin is 10 parts by mass or more and 30 parts by mass or less.
[0007] (2) The amount of ellagic acid in the whitening composition is X EA [mass%], the gallic acid content is X GA When expressed as [mass %], 0.34 ≤ X EA / X GA A whitening composition as described in (1) above that satisfies the condition ≤ 0.80.
[0008] (3) The whitening composition according to (1) or (2) above, wherein the sum of the content of eugenin, the content of ellagic acid, and the content of gallic acid in the whitening composition is 1.41% by mass or more and 1.85% by mass or less.
[0009] (4) A whitening composition according to any one of (1) to (3) above, comprising rose extract.
[0010] (5) A whitening composition according to any one of (1) to (4) above, comprising papaya seed extract.
[0011] (6) The whitening composition is a liquid whitening composition as described in any of (1) to (5) above.
[0012] (7) The whitening composition according to (6) above, wherein the solid content in the whitening composition is 0.01% by mass or more and 1.00% by mass or less. [Effects of the Invention]
[0013] According to the present invention, it is possible to provide a whitening composition having excellent whitening effects. [Brief explanation of the drawing]
[0014] [Figure 1]Process diagram showing the configuration of the method for producing a whitening composition according to an embodiment.
Embodiments for Carrying Out the Invention
[0015] Hereinafter, an explanation will be given based on preferred embodiments of the present invention. [1] Whitening composition First, the whitening composition according to the embodiment will be described.
[0016] The whitening composition of the present invention contains eugenin, ellagic acid, and gallic acid, and is characterized in that the content of ellagic acid relative to 1 part by mass of eugenin is 5 parts by mass or more and 15 parts by mass or less, and the content of gallic acid relative to 1 part by mass of eugenin is 10 parts by mass or more and 30 parts by mass or less.
[0017] With such a configuration, a whitening composition having an excellent whitening effect can be provided.
[0018] More specifically, since the whitening composition of the present invention contains a component that suppresses the production of melanin, it can prevent the occurrence of darkening due to sunburn, spots, freckles, etc., and exhibit an excellent whitening effect. In addition, eugenin, ellagic acid, and gallic acid all have the effect of suppressing the production of melanin by inhibiting the activity of tyrosinase. However, when the contents of eugenin, ellagic acid, and gallic acid satisfy the above conditions, the synergistic effect due to the inclusion of the three components is more significantly exhibited, and an even more excellent whitening effect can be obtained.
[0019] The excellent effects as described above are obtained by satisfying all of the above conditions. If any one of the above conditions is not satisfied, the excellent effects as described above cannot be obtained.
[0020] For example, if the whitening composition does not contain any of eugenin, ellagic acid, and gallic acid, it does not have an excellent whitening effect.
[0021] Furthermore, while eugenin, ellagic acid, and gallic acid all have the effect of suppressing melanin production by inhibiting tyrosinase activity, if the content of eugenin, ellagic acid, and gallic acid does not meet the above conditions, the synergistic effect of including eugenin, ellagic acid, and gallic acid will not be fully realized.
[0022] Furthermore, as mentioned above, the content of ellagic acid per 1 part by mass of eugenin in the whitening composition is 5 parts by mass or more and 15 parts by mass or less, but preferably 6 parts by mass or more and 14 parts by mass or less, and more preferably 7 parts by mass or more and 13 parts by mass or less. This allows the aforementioned effects to be exhibited more significantly.
[0023] Furthermore, as mentioned above, the content of gallic acid per 1 part by mass of eugenin in the whitening composition is 10 parts by mass or more and 30 parts by mass or less, but preferably 11 parts by mass or more and 29 parts by mass or less, and more preferably 12 parts by mass or more and 28 parts by mass or less. This allows the aforementioned effects to be exhibited more significantly.
[0024] In this invention, "whitening" refers to a skin condition with less pigmentation such as darkening caused by sun exposure, blemishes, and freckles.
[0025] The components of the whitening composition of the present invention will be described in detail below. [1-1] Eugenine The whitening composition of the present invention contains eugenin. The content of eugenin in the whitening composition is preferably 0.02% by mass or more and 0.15% by mass or less, more preferably 0.03% by mass or more and 0.11% by mass or less, and even more preferably 0.04% by mass or more and 0.07% by mass or less. This allows the tyrosinase activity inhibitory effect of eugenin to be exerted more effectively, and the whitening effect of the whitening composition becomes more pronounced.
[0026] Furthermore, the sum of the content of eugenin, ellagic acid, and gallic acid in the whitening composition is preferably 0.01 parts by mass or more and 0.08 parts by mass or less per 1 part by mass of eugenin, more preferably 0.02 parts by mass or more and 0.07 parts by mass or less, and even more preferably 0.02 parts by mass or more and 0.06 parts by mass or less. This allows the synergistic effect of eugenin, ellagic acid, and gallic acid contained in the whitening composition of the present invention to be more pronounced, resulting in a superior whitening effect.
[0027] [1-2] Ellagic acid The whitening composition of the present invention contains ellagic acid. The ellagic acid content in the whitening composition is preferably 0.10% by mass or more and 2.25% by mass or less, more preferably 0.18% by mass or more and 1.54% by mass or less, and even more preferably 0.28% by mass or more and 0.91% by mass or less. This allows the tyrosinase activity inhibitory effect of ellagic acid to be more effectively exerted, resulting in a more pronounced whitening effect of the whitening composition.
[0028] Furthermore, the sum of the content of eugenin, ellagic acid, and gallic acid in the whitening composition is preferably such that the content of ellagic acid per 1 part by mass is 0.13 parts by mass or more and 0.58 parts by mass or less, more preferably 0.16 parts by mass or more and 0.54 parts by mass or less, and even more preferably 0.19 parts by mass or more and 0.50 parts by mass or less. This allows the synergistic effect of eugenin, ellagic acid, and gallic acid contained in the whitening composition of the present invention to be more pronounced, resulting in a superior whitening effect.
[0029] [1-3] Gallic acid The whitening composition of the present invention contains gallic acid. The content of gallic acid in the whitening composition is preferably 0.20% by mass or more and 4.50% by mass or less, more preferably 0.33% by mass or more and 3.19% by mass or less, and even more preferably 0.48% by mass or more and 1.96% by mass or less. Thereby, the inhibitory effect of gallic acid on tyrosinase activity is more effectively exerted, and the whitening effect of the whitening composition becomes more remarkable.
[0030] In addition, the sum of the content of eugenin, the content of ellagic acid, and the content of gallic acid in the whitening composition: the content of gallic acid per 1 part by mass is preferably 0.38 part by mass or more and 0.84 part by mass or less, more preferably 0.42 part by mass or more and 0.81 part by mass or less, and even more preferably 0.46 part by mass or more and 0.78 part by mass or less. Thereby, the synergistic effect due to the inclusion of eugenin, ellagic acid, and gallic acid in the whitening composition of the present invention is more remarkably exerted, and it can have a more excellent whitening effect.
[0031] In addition, when the content of ellagic acid in the whitening composition is X EA [% by mass] and the content of gallic acid is X GA [% by mass], it is preferable to satisfy the condition of 0.34 ≦ X EA / X GA ≦ 0.80, more preferably to satisfy the condition of 0.41 ≦ X EA / X GA ≦ 0.68, and even more preferably to satisfy the condition of 0.46 ≦ X EA / X GA ≦ 0.56. Thereby, the synergistic effect due to the inclusion of ellagic acid and gallic acid in the whitening composition of the present invention is more remarkably exerted, and it can have a more excellent whitening effect.
[0032] Furthermore, when the whitening composition is in solid form, the sum of the content of eugenin, ellagic acid, and gallic acid in the whitening composition is preferably 1.41% by mass or more and 1.85% by mass, more preferably 1.44% by mass or more and 1.82% by mass or less, and even more preferably 1.47% by mass or more and 1.79% by mass or less. This allows the synergistic effect of including eugenin and ellagic acid in the whitening composition of the present invention to be more pronounced, resulting in a superior whitening effect.
[0033] [1-4] Liquid media The whitening composition of the present invention may further include, as components other than those described above [1-1] to [1-3], a liquid medium that dissolves or disperses at least a portion of the components of the whitening composition of the present invention.
[0034] Examples of such liquid media include water, monohydric alcohols such as ethanol, and polyhydric alcohols such as 1,3-butylene glycol, 1,3-propanediol, glycerin, and ethylhexylglycerin.
[0035] In particular, the liquid medium preferably contains at least water. This improves the ease of handling of the whitening composition, for example, by improving its applicability and ease of spraying with a sprayer.
[0036] [1-5] Other ingredients The whitening composition of the present invention may contain ingredients other than those described above in [1-1] to [1-4]. Hereinafter, in this section, such ingredients will be referred to as "other ingredients".
[0037] Other ingredients include, for example, excipients, beauty ingredients other than whitening compositions, plant extracts, vitamins, vitamin-like substances, minerals, thickeners, pH adjusters, preservatives, surfactants, gelling agents, antioxidants, colorants, stabilizers such as lactose, solubilizers such as glutamic acid and aspartic acid, pH adjusters, humectants, emulsifiers, dispersants, emulsions, solutions, suspensions, elixirs, fragrances, scents, and other active ingredients (pharmaceutical ingredients).
[0038] Examples of thickening agents include xanthan gum. Examples of pH adjusters include citric acid and sodium citrate. Examples of preservatives include phenoxyethanol. Examples of surfactants include hydrogenated castor oil (PEG-4).
[0039] [1-6] Other conditions The whitening composition of the present invention may be in any state, such as liquid, solid, or semi-solid. Furthermore, the whitening composition of the present invention may be supported on a substrate. In this case, the substrate may be in any form, such as cotton or a sheet.
[0040] In particular, the whitening composition is preferably in liquid form. This improves the ease of handling of the whitening composition, for example, by making it easier to apply and spray using a sprayer.
[0041] When the whitening composition is in liquid form, the solid content in the whitening composition is preferably 0.01% by mass or more and 1.00% by mass or less, more preferably 0.05% by mass or more and 0.95% by mass or less, and even more preferably 0.1% by mass or more and 0.90% by mass or less. This allows for a sufficiently high whitening effect as a whole whitening composition while improving the ease of handling of the whitening composition, for example, improving the applicability of the whitening composition and the ease of spraying with a sprayer.
[0042] [1-7] Rose extract The whitening composition of the present invention preferably contains rose extract. The rose extract contains eugenin, ellagic acid, and gallic acid. Therefore, the inclusion of rose extract makes the whitening composition of the present invention easier to prepare. In addition, the rose extract contains trace components other than eugenin, ellagic acid, and gallic acid. This makes the whitening effect of the whitening composition of the present invention even better.
[0043] The roses included in the whitening composition are not particularly limited, but roses belonging to the genus Rosa of the family Rosaceae (Rosa spp.) are preferred. Specifically, examples include wild species such as Rosa gallica, Rosa centifolia, Rosa moschata, Rosa foetida, Rosa gigantea, Rosa multiflora, and Rosa wichuraiana, or horticultural varieties obtained by crossbreeding these.
[0044] [1-8] Papaya seed extract The whitening composition of the present invention preferably contains papaya seed extract. Papaya seed extract contains ellagic acid and gallic acid. Therefore, by including papaya seed extract, the whitening composition of the present invention can be prepared more easily. In addition, papaya seed extract contains trace components other than ellagic acid and gallic acid. This makes the whitening effect of the whitening composition of the present invention even better.
[0045] The papaya included in the whitening composition is not particularly limited, but papaya belonging to the genus Carica of the family Caricaceae (Carica spp.) is preferred, and specifically, examples include Carica papaya, Carica augusti, Carica glandulosa, and Carica aprica.
[0046] [1-9] Other extracts The whitening composition of the present invention may contain extracts other than rose and papaya seeds. Hereinafter, in this section, such components will be referred to as "other extracts." Examples of other extracts include African mango, pomegranate, sumac, blackberry, amla, kakadu plum, raspberry, tauric rock rose, mallow stem, acorn, Cistus albidus, long-lived spinach, Terminalia bellirica, green tea, galangal, guava leaves, and the like.
[0047] [1-10] Uses of whitening compositions The whitening composition may be, for example, an oral preparation or a parenteral preparation such as a topical preparation.
[0048] More specifically, examples include food; luxury goods; pharmaceuticals; quasi-drugs; soaps, body washes, hand soaps; skincare products such as lotions, creams, emulsions, serums, whitening agents, and facial cleansers (including facial cleansers); lip products such as lip balms and lipsticks; cosmetics such as makeup bases, blushes, foundation creams, and mascaras; nail care products such as polishes, polish removers, strengtheners, lengtheners, hardeners, cuticle removers, and softeners; hair removal-related products such as shaving creams and lotions, depilatory agents, and after-shave skin conditioners; and other products such as anti-aging agents, antiperspirants, sunscreens, perfumes, various waxes, bath additives, and cooling sprays.
[0049] Furthermore, the form of food includes solid, semi-solid (such as gels like jelly and pudding), and liquid forms, and the concept of food also includes beverages. In addition, seasonings, flavorings, food additives, and supplements (health supplements) are also included in the concept of food.
[0050] [2] Method for manufacturing a whitening composition Next, an example of a method for producing the aforementioned whitening composition will be described. Figure 1 is a process diagram showing the configuration for a method of manufacturing a whitening composition according to an embodiment.
[0051] The method for producing the whitening composition shown in Figure 1 comprises a preparation step S102 in which a rose extract is prepared, and a mixing step S104 in which the rose extract obtained in the preparation step S102 is mixed with other components.
[0052] [2-1] Preparation Steps In preparation step S102, rose extract is prepared. Rose extract can be prepared, for example, by the following method.
[0053] First, the components contained in the rose are extracted (extraction process). There are no particular limitations on the part of the rose used; any part such as the flower, petals, leaves, stems, roots, and seeds may be used, but the petals are preferred. The raw material for extraction may be unground, ground, or pre-treated. Examples of pre-treatment include washing, drying, freezing, heating, grinding, kneading, and fermentation.
[0054] Furthermore, the extraction method and conditions are not particularly limited. For example, as the extraction solvent, in addition to water, alcohols such as methanol and ethanol, organic solvents such as ethyl acetate, n-hexane or acetone, or mixed solvents of these organic solvents and water can be used. Among these, water is preferred as the extraction solvent. The extraction solvent may also contain acids or bases as pH adjusters.
[0055] Furthermore, the pH of the extraction solvent during extraction is preferably between 2 and 7, more preferably between 2.5 and 6.5, and even more preferably between 3 and 6. This effectively prevents unintended denaturation of the active ingredients and allows for the more efficient acquisition of extracts with a more favorable composition. Note that the pH values used in this invention are measured at 25°C.
[0056] Furthermore, as for the extraction method, for example, a heat extraction method in which roses and an extraction solvent are mixed and then heated to a degree that does not deactivate the activity of the active ingredients, or a supercritical fluid extraction method can be employed. In addition, an immersion extraction method in which roses are immersed in a predetermined amount of extraction solvent for batch processing, or a continuous extraction method in which roses are continuously supplied can be employed.
[0057] In particular, it is preferable to obtain rose extract by immersing roses in an extraction solvent (immersion extraction method). This allows for low cost, increased extraction efficiency of active ingredients, increased amount of active ingredients extracted per unit weight of raw material, and a more favorable balance of the content of multiple active ingredients contained in the extract. As a result, the aforementioned whitening effect is exhibited more significantly. Furthermore, while increasing the extraction efficiency of active ingredients, the extraction of unwanted components can be more effectively prevented.
[0058] Furthermore, while the extraction temperature is not particularly limited, heat extraction is preferred. In the case of heat extraction, the heating temperature is preferably 50°C to 100°C, more preferably 60°C to 90°C, and even more preferably 70°C to 85°C. This effectively prevents unintended denaturation of the active ingredients, allows for the efficient acquisition of an extract with a more suitable composition in a short time, and further improves productivity.
[0059] Furthermore, while there are no particular restrictions on the extraction time when heat extraction is performed by immersion extraction, it is preferably 15 minutes or more and 120 minutes or less, more preferably 20 minutes or more and 90 minutes or less, and even more preferably 40 minutes or more and 70 minutes or less. This effectively prevents unintended denaturation of the active ingredients, allows for the efficient acquisition of an extract with a more suitable composition in a shorter time, and further improves productivity.
[0060] Furthermore, while there are no particular restrictions on the extraction time when extracting at room temperature by immersion extraction, it is preferably between half a day and 10 days, more preferably between 1 day and 7 days, and even more preferably between 1 day and 5 days. This effectively prevents unintended denaturation of the active ingredients and allows for the acquisition of an extract with a more favorable composition. As a result, the aforementioned whitening effect is more pronounced.
[0061] Next, unwanted solid parts such as petals are removed from the obtained rose extract (removal step). While there are no particular limitations on the method of removing unwanted materials, filtration or centrifugation can be used. Among these, centrifugation is preferred for removing unwanted materials.
[0062] Next, the rose extract from which unwanted substances have been removed is concentrated (concentration step). Concentration methods include, for example, treatment using an evaporator, spray drying, vacuum drying, and freeze-drying.
[0063] [2-2]Mixing process In mixing step S104, the rose extract obtained in preparation step S102 is mixed with other components. Examples of other components include eugeniin, ellagic acid, gallic acid, papaya seed extract, the liquid media mentioned in [1-4], and the other components mentioned in [1-5]. One or more of these may be selected and used in combination. By mixing components other than the rose extract in mixing step S104, the composition of the rose extract obtained in preparation step S102 can be adjusted to be more suitable, and the whitening effect of the whitening composition of the present invention can be made even better.
[0064] When rose extract is mixed with eugenin, ellagic acid, gallic acid, etc., the balance of the active ingredients contained in the whitening composition can be made more favorable. Commercially available products may be used as eugenin, ellagic acid, and gallic acid.
[0065] When mixing rose extract with papaya seed extract, it is preferable to use papaya seed extract obtained by the following method.
[0066] First, prepare papaya seeds and extract their components (extraction step). It is preferable to use crushed papaya seeds. Alternatively, pre-treated papaya seeds may be used. Examples of pre-treatment include washing, drying, freezing, heating, crushing, kneading, and fermentation.
[0067] Furthermore, the extraction method and extraction conditions are not particularly limited. For example, as the extraction solvent, in addition to water, alcohols such as methanol and ethanol, organic solvents such as ethyl acetate, n-hexane, or acetone, or mixed solvents of these organic solvents and water can be used. Among these, ethanol is preferred.
[0068] Furthermore, as for extraction methods, for example, a heat extraction method in which papaya seeds and an extraction solvent are mixed and then heated to a degree that does not deactivate the activity of the active ingredients, or a supercritical fluid extraction method can be employed. In addition, an immersion extraction method in which papaya seeds are immersed in a predetermined amount of extraction solvent and processed in batches, or a continuous extraction method in which papaya seeds are continuously fed, can be employed.
[0069] In particular, it is preferable to obtain papaya seed extract by immersing papaya seeds in an extraction solvent (immersion extraction method). This allows for low cost, increased extraction efficiency of active ingredients, increased amount of active ingredients extracted per unit weight of raw material, and a more favorable balance of the content of multiple active ingredients contained in the extract. As a result, the aforementioned whitening effect is exhibited more significantly. Furthermore, while increasing the extraction efficiency of active ingredients, the extraction of unwanted components can be more effectively prevented.
[0070] Furthermore, while the extraction temperature is not particularly limited, heat extraction is preferred. In the case of heat extraction, the heating temperature is preferably 5°C to 70°C, more preferably 10°C to 60°C, and even more preferably 20°C to 40°C. This effectively prevents unintended denaturation of the active ingredients, allows for the efficient acquisition of an extract with a more suitable composition in a short time, and further improves productivity.
[0071] Furthermore, while there are no particular restrictions on the extraction time when heat extraction is performed by immersion extraction, it is preferably 15 minutes or more and 120 minutes or less, more preferably 20 minutes or more and 90 minutes or less, and even more preferably 40 minutes or more and 70 minutes or less. This effectively prevents unintended denaturation of the active ingredients, allows for the efficient acquisition of an extract with a more suitable composition in a shorter time, and further improves productivity.
[0072] Furthermore, while there are no particular restrictions on the extraction time when extracting at room temperature by immersion extraction, it is preferably between half a day and 10 days, more preferably between 1 day and 7 days, and even more preferably between 1 day and 5 days. This effectively prevents unintended denaturation of the active ingredients and allows for the acquisition of an extract with a more favorable composition. As a result, the aforementioned whitening effect is more pronounced.
[0073] Next, the unwanted solid portion is removed from the obtained papaya seed extract (removal step). The method for removing unwanted material is not particularly limited, but filtration or centrifugation can be used. Among these, it is preferable to remove unwanted material by filtration with filter paper.
[0074] Next, the rose extract from which unwanted substances have been removed is concentrated (concentration step). Concentration methods include, for example, treatment using an evaporator, spray drying, vacuum drying, and freeze-drying.
[0075] Although preferred embodiments of the present invention have been described above, the present invention is not limited thereto.
[0076] For example, the whitening composition of the present invention may be manufactured by any method, and is not limited to being manufactured by the method described in the embodiments above.
[0077] More specifically, for example, rose extract and papaya seed extract may be those manufactured without the removal or concentration steps. Also, the method for producing the whitening composition does not have to include a mixing step. Furthermore, for example, after the mixing or preparation steps, a purification step may be performed to remove at least some of the unwanted components contained in the extract, or a molding step may be performed to shape the obtained extract into a predetermined shape.
[0078] Furthermore, the whitening composition contains eugenin, ellagic acid, and gallic acid, and only the content of the three components mentioned above needs to meet the conditions described above; it may also be prepared without using extracts. [Examples]
[0079] Next, specific examples of the present invention will be described, but the present invention is not limited thereto. In the following examples, unless the temperature conditions are specified, the processing and measurements were performed at room temperature (25°C).
[0080] [4] Preparation of whitening compositions (Example 1) First, Rosa centifolia petals were prepared as the rose petals and contacted with hot water (80°C, pH 6) as the extraction solvent for 45 minutes to extract the components of the rose. Next, the solid components were removed by centrifugation, and then the extract was concentrated to obtain the rose extract.
[0081] Next, crushed papaya seeds were prepared and contacted with ethanol (30°C) as an extraction solvent for 24 hours to extract the components contained in the papaya seeds. Then, after removing the solids by filtration, the extract was concentrated to obtain a papaya seed extract.
[0082] Next, the obtained rose extract and papaya seed extract were mixed to obtain a powdered whitening composition.
[0083] (Examples 2-6) A powdered whitening composition was prepared in the same manner as in Example 1 described above, except that the types of ingredients and mixing ratios used in the preparation of the whitening composition were changed to achieve the composition shown in Table 1. Note that only in Example 6 was papaya seed extract not used.
[0084] (Comparative Examples 1-5) A powdered whitening composition was prepared in the same manner as in Example 1 described above, except that the types of ingredients and mixing ratios used in the preparation of the whitening composition were changed to achieve the composition shown in Table 1. In Comparative Example 5 only, the whitening composition was prepared using rose extract extracted under conditions where ethanol was used as the extraction solvent.
[0085] Table 1 summarizes the composition of the whitening compositions for each example and comparative example. In Table 1, the columns for ellagic acid and gallic acid show the content of ellagic acid and gallic acid per 1 part by mass of eugenin, respectively, and the unit of the numerical value is parts by mass. In Table 1, the column for the total of the three components shows the sum of the content of eugenin, ellagic acid, and gallic acid in the whitening composition, and the unit of the numerical value is mass%.
[0086] [5] Evaluation of whitening compositions [5-1] Tyrosinase inhibitory activity The whitening compositions of each example and comparative example were dissolved in pure water to a concentration of 2.0% by mass, and 20 μl of each was placed in each well of a 96-well microplate. Next, 100 μl of McIlbain buffer (pH 6.8) and 40 μl of 40 U / ml tyrosinase solution (derived from mushrooms, Sigma-Aldrich) were added to each well and mixed, and then pre-incubated at 25°C for 3 minutes. Next, 50 μl of 0.05% L-DOPA solution (Sigma-Aldrich) was added to each well and mixed, and incubated at 25°C for 10 minutes. The tyrosinase inhibition rate was then determined from the following formula by measuring the absorbance at 475 nm, the maximum absorption wavelength of dopachrome (an intermediate in melanin biosynthesis).
[0087] Tyrosinase inhibition rate (%) = {1 - (T - T0) / (C - C0)} × 100 T; Absorbance of each of the above samples added T0; Absorbance of the blank with each of the above samples added. C; Absorbance with the above control added C0; Absorbance of the blank with the above control added. In the formula, "control" represents the reaction system in which DMSO was added instead of the sample, and "blank" represents the reaction system in which McIlbain buffer was added instead of tyrosinase.
[0088] The absorbance was measured three times for each sample, and the average value was used as the measurement result. The tyrosinase inhibitory activity was evaluated according to the following evaluation criteria.
[0089] A: Tyrosinase inhibition rate of 48% or higher B: Tyrosinase inhibition rate is 44% or higher but less than 48% C: Tyrosinase inhibition rate is between 39% and 44% D: Tyrosinase inhibition rate is 37% or higher but less than 39% E: Tyrosinase inhibition rate less than 37%
[0090] These evaluation results, along with the composition of the whitening compositions for each of the above examples and comparative examples, are summarized in Table 1.
[0091] [Table 1]
[0092] As is clear from Table 1, the whitening compositions of each example exhibited excellent tyrosinase inhibitory activity and had excellent whitening effects. Furthermore, when powdered whitening compositions were prepared in the same manner as in Example 1, except that commercially available eugenin, ellagic acid, and gallic acid were used, and evaluated in the same manner as above, the same excellent results were obtained. In addition, when the whitening compositions of each example were diluted so that the solid content in the whitening composition was between 0.01% by mass and 1.00% by mass, and used by subjects, all received excellent evaluations regarding usability. In contrast, satisfactory results were not obtained for the whitening compositions of each comparative example. [Explanation of Symbols]
[0093] S102: Preparation process S104: Mixing process
Claims
1. It contains eugenin, ellagic acid, and gallic acid. The ellagic acid content per 1 part by mass of eugenin is 5 parts by mass or more and 15 parts by mass or less. A skin whitening composition characterized in that the content of gallic acid per 1 part by mass of eugenin is 10 parts by mass or more and 30 parts by mass or less.
2. The amount of ellagic acid in the whitening composition is X. EA [Mass %], the gallic acid content is X GA When expressed as [mass %], 0.34 ≤ X EA / X GA A skin-whitening composition according to claim 1 that satisfies the condition ≤ 0.
80.
3. The whitening composition according to claim 1 or 2, wherein the sum of the content of eugenin, the content of ellagic acid, and the content of gallic acid in the whitening composition is 1.41% by mass or more and 1.85% by mass or less.
4. A whitening composition according to claim 1 or 2, comprising rose extract.
5. A whitening composition according to claim 1 or 2, comprising papaya seed extract.
6. The whitening composition according to claim 1 or 2, wherein the whitening composition is in liquid form.
7. The whitening composition according to claim 6, wherein the solid content in the whitening composition is 0.01% by mass or more and 1.00% by mass or less.