Irritation-mitigating agent, external composition for mitigating irritation, and method for mitigating irritation

1-kestose and raffinose effectively alleviate irritation from surfactants, preservatives, and plant extracts in topical compositions, improving product safety and formulation flexibility.

JP2026014427APending Publication Date: 2026-01-29KISHO
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Patent Information

Application Number
JP2024115477
Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
Filing Date
2024-07-19
Publication Date
2026-01-29

AI Technical Summary

Technical Problem

Existing products that come into contact with the skin, eyes, and mucous membranes often cause irritation due to ingredients like surfactants, preservatives, and plant extracts, with existing irritation alleviators not effectively reducing symptoms such as skin erythema.

Method used

The use of 1-kestose and raffinose as active ingredients to suppress irritation caused by surfactants, preservatives, and plant extracts, formulated in topical compositions for direct application to the skin, eyes, and mucous membranes.

Benefits of technology

Reduces irritation symptoms by suppressing the effects of these irritants, enhancing product safety and formulation flexibility while maintaining consumer safety and confidence.

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Abstract

To provide a technique capable of mitigating irritation caused by a component blended in a cosmetic, a medicated cosmetic, a cleanser or the like.SOLUTION: The irritation-mitigating agent comprises 1-kestose and / or raffinose as an active ingredient for mitigating irritation to the skin, eyes and / or mucous membranes. According to the present invention, it is possible to suppress irritation to the skin, eyes, and mucous membranes due to surfactants, preservatives, preservative aids, plant extracts, and the like. Therefore, it is possible to contribute to the production of cosmetics, medicated cosmetics, cleansers, and the like that can be used more safely.SELECTED DRAWING: Figure 1
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Description

[Technical Field]

[0001] The present invention relates to an agent for alleviating irritation to the skin, eyes, and / or mucous membranes, which contains 1-kestose and / or raffinose as active ingredients, as well as an external composition for alleviating irritation and a method for alleviating irritation that uses the same. [Background technology]

[0002] Many cosmetics, medicated cosmetics, cleansers, and other products that come into direct contact with the skin, eyes, and mucous membranes (such as the oral cavity, lips, genitals, nasal cavities, and conjunctiva) contain surfactants and preservatives. While these ingredients play a role in maintaining product stability, they can also irritate the skin, eyes, and mucous membranes, posing a challenge. Other ingredients in products for external application to the skin, eyes, and mucous membranes, such as ultraviolet absorbers, lower alcohols, colorants, fragrances, and peeling agents, are known to cause irritation. Therefore, research and development has been conducted into technologies to reduce irritation in such products. For example, Patent Document 1 discloses an irritation-reducing agent containing, as an active ingredient, at least one plant extract selected from the group consisting of cardamom, Sophora flavescens, Peucedanum japonicum, Zedoary, chamomile, guarana, pueraria, Panax notoginseng, Tartary buckwheat, nutmeg, pepper, ginger, and peach kernel. [Prior art documents] [Patent documents]

[0003] [Patent Document 1] Japanese Patent Application Laid-Open No. 2003-155246 Summary of the Invention [Problem to be solved by the invention]

[0004] However, although the irritation alleviator described in Patent Document 1 has been confirmed to increase cell viability in cultured human epidermal keratinocytes when exposed to sodium lauryl sulfate, it is unclear whether it can actually reduce symptoms such as skin erythema caused by contact with an irritant. In other words, even in light of this patent document, it cannot be said that a technology capable of alleviating irritation to the skin, eyes, or mucous membranes has been adequately provided. The present invention has been made to solve this problem, and aims to provide a technology capable of alleviating irritation caused by ingredients in products applied externally to the skin, eyes, or mucous membranes. [Means for solving the problem]

[0005] As a result of extensive research, the present inventors have found that 1-kestose and raffinose can suppress irritation caused by various irritants such as surfactants, preservatives, preservative aids, and plant extracts. Based on this finding, the present inventors have completed the following inventions.

[0006] (1) The irritation-reducing agent according to the present invention contains 1-kestose and / or raffinose as active ingredients for reducing irritation to the skin, eyes, and / or mucous membranes.

[0007] (2) In the present invention, examples of the stimulation include stimulation by a surfactant, a preservative, an antiseptic aid, and / or a plant extract.

[0008] (3) The topical composition for alleviating irritation according to the present invention is a composition for alleviating irritation to the skin, eyes and / or mucous membranes, which is used externally and contains 1-kestose and / or raffinose as active ingredients for alleviating irritation.

[0009] (4) The method for alleviating irritation according to the present invention is a method for alleviating irritation to the skin, eyes and / or mucous membranes, characterized by using 1-kestose and / or raffinose in combination with a irritant. [Effects of the Invention]

[0010] According to the present invention, irritation to the skin, eyes, and mucous membranes caused by surfactants, preservatives, preservative aids, plant extracts, etc. can be suppressed. This contributes to the production of products such as cosmetics, medicated cosmetics, and cleansers that can be used with greater peace of mind. Furthermore, because the irritation to the skin, eyes, and mucous membranes caused by substances that may cause irritation can be reduced, the degree of freedom in product formulation design can be increased regarding the blending or blending amount of the substance.

[0011] Furthermore, both 1-kestose and raffinose are sugars naturally contained in vegetables and fruits, and have been ingested as foods or food components since ancient times, so they are highly safe and provide a sense of security to consumers. Therefore, according to the present invention, it is possible to claim that products have the effect of reducing irritation to the skin, eyes, and mucous membranes without raising concerns about safety or allergic reactions. [Brief explanation of the drawings]

[0012] [Figure 1] 1 is a bar graph showing the rate of change in the erythema index of skin that was contacted with an aqueous solution of an irritant (sodium lauryl sulfate) after applying an aqueous solution of the test substance (1-kestose, raffinose, xylitol, glycosyltrehalose / hydrogenated starch hydrolysate mixture, or hydrogenated starch hydrolysate). [Figure 2] 1 is a bar graph showing the rate of change in the erythema index of skin that was contacted with an aqueous solution containing an irritant (sodium lauryl sulfate) and a test substance (1-kestose, glycosyltrehalose / hydrolyzed hydrogenated starch mixture, dipotassium glycyrrhizinate, or glucose). [Figure 3] 1 is a line graph showing the rate of change in the erythema index of skin contacted with an aqueous solution containing an irritant (sodium lauryl sulfate) and a test substance (1-kestose). [Figure 4] 1 is a line graph showing the rate of change in the erythema index of skin contacted with an aqueous solution containing an irritant (methylparaben) and a test substance (1-kestose or sucrose). [Figure 5]1 is a line graph showing the rate of change in the erythema index of skin contacted with an aqueous solution containing an irritant (methylparaben) and 2%, 5%, or 10% by mass of the test substance (1-kestose). [Figure 6] 1 is a line graph showing the rate of change in the erythema index of skin contacted with an aqueous solution containing an irritant (phenoxyethanol) and 2%, 5%, or 10% by mass of the test substance (1-kestose). [Figure 7] 1 is a line graph showing the rate of change in the erythema index of skin contacted with an aqueous solution containing an irritant (ethylhexylglycerin) and 2% by mass or 10% by mass of the test substance (1-kestose). [Figure 8] 1 is a line graph showing the rate of change in the erythema index of skin contacted with an aqueous solution containing an irritant (capsicum tincture) and a test substance (1-kestose). [Figure 9] This is a bar graph showing the cell viability of a corneal epithelial model exposed to PBS(-) (sample solution A), an irritant (sodium lauryl sulfate) only (sample solution B), or an irritant (sodium lauryl sulfate) and a test substance (1-kestose) together (sample solution C). DETAILED DESCRIPTION OF THE INVENTION

[0013] The present invention will be further described below.

[0014] In the present invention, "irritation" refers to irritation caused by contact of an irritant with the skin, eyes, or mucous membranes. Examples of symptoms include redness or erythema, dryness, itching, keratinization, rash, hot flashes, pain, swelling, stiffness, etc. at the site of contact with the irritant.

[0015] In the present invention, "alleviating irritation" includes not only eliminating irritation caused by contact of an irritant with the skin, eyes, or mucous membranes, but also reducing the severity of the irritation. Whether or not irritation has been alleviated can be confirmed, for example, by comparing the severity of the above-mentioned symptoms between when the agent of the present invention is used and when it is not used.

[0016] In the present invention, "topical composition" refers to a composition used in a form that can come into direct contact with the skin, eyes, or mucous membranes (such as the oral cavity, lips, genitals, nasal cavity, or conjunctiva). Specific examples of topical compositions include cosmetics, quasi-drugs, and pharmaceuticals that are directly applied, attached, or sprayed onto the skin, eyes, or mucous membranes, as well as hygiene products that can come into contact with the skin, eyes, or mucous membranes. More specific examples include various cosmetics, cleansers, shampoos, facial cleansers, products for delicate areas, face masks, bath additives, toothpastes, mouthwashes, disinfectants, and germicides.

[0017] Examples of substances that can cause irritation to the skin, eyes, and mucous membranes (irritants) include surfactants, preservatives, preservative aids, plant extracts, ultraviolet absorbers, lower alcohols, pigments, fragrances, peeling agents, retinoids, antibacterial agents, hair dyes, acids, and alkalis.

[0018] More specific examples of "surfactants" include anionic surfactants, nonionic surfactants, cationic surfactants, amphoteric surfactants, etc., which are used in compositions for external application to the skin and mucous membranes.

[0019] More specific examples of the "preservative" include phenoxyethanol, benzoic acid and its salts, salicylic acid and its salts, phenol, sorbic acid and its salts, dehydroacetic acid and its salts, paraoxybenzoic acid esters (e.g., methylparaben, ethylparaben, butylparaben, etc.), chlorcresol, hexachlorophene, resorcinol, isopropylmethylphenol, o-phenylphenol, benzalkonium chloride, chlorhexidine hydrochloride, chlorphenesin, hinokitiol, butylcaprylamide ... Examples include propynyl iodide carbamate, benzalkonium chloride, polyaminopropyl biguanide, chlorhexidine gluconate, alkylisoquinolium bromide, trichloricarbanilide, halocarban, photosensitizer No. 201, trichlorohydroxydiphenyl ether (triclosan), methylchloroisothiazolinone, methylisothiazolinone, bisabolol, alkyldiaminoethylglycine hydrochloride, trichloro salicylanilide (TCSA), tribromo salicylanilide (TBS), and the like.

[0020] More specific examples of the "antiseptic aid" include diols (1,2-hexanediol, 1,2-pentanediol, 1,3-butylene glycol, dipropylene glycol, propylene glycol, propanediol, caprylyl glycol, etc.), glyceryl caprylate, glyceryl caprate, glycerin fatty acid esters, caprylhydroxamic acid, capryloylglycine, N-octanoylglycine, anisic acid and its salts, ethanol, denatured alcohol, levulinic acid and its salts, ethylhexylglycerin, phenylethyl alcohol, glycerin mono-2-ethylhexyl ether, cocoyl arginine ethyl PCA, linalyl acetate denatured alcohol, bisabolol, and hydroxyacetophenone.

[0021] "Plant extract" refers to an extract from a plant body such as a flower, skin, leaf, or bark, and may contain a solvent (water, BG, ethanol, oil, etc.). More specific examples of plant extracts include capsicum tincture and capsicum fruit extract.

[0022] More specific examples of "acids" include citric acid, tartaric acid, lactic acid, glycolic acid, hydrochloric acid, nitric acid, citric acid, succinic acid, acetic acid, fumaric acid, sulfuric acid, malic acid, phosphoric acid, ascorbic acid, adipic acid, potassium phosphate, sodium phosphate, sodium dihydrogen phosphate, and potassium dihydrogen phosphate.

[0023] More specific examples of the "alkali" include alkali metal hydroxides such as sodium hydroxide, potassium hydroxide, calcium hydroxide, magnesium hydroxide, sodium citrate, sodium lactate, sodium acetate, disodium succinate, 2-amino-2-methyl-1,3-propanediol, 2-amino-2-hydroxymethyl-1,3-propanediol, 2-amino-2-methyl-1-propanol, arginine, sodium carbonate, sodium bicarbonate, guanidine carbonate, ammonium carbonate, ammonia, aqueous ammonia, dimethylamine, diethylamine, trimethylamine, triethylamine, triisopropanolamine, disodium phosphate, trisodium phosphate, disodium hydrogen phosphate, dipotassium hydrogen phosphate, monoethanolamine, diethanolamine, isopropanolamine, diisopropanolamine, and triethanolamine; alkaline earth metal hydroxides; primary, secondary, or tertiary alkylamines; and primary, secondary, or tertiary alkanolamines.

[0024] As shown in the Examples below, 1-kestose and raffinose were confirmed to reduce irritation caused by substances with various structures in skin and corneal epithelium models. That is, 1-kestose and raffinose are thought to exert an irritation-reducing effect by acting on epithelial cells of the skin, eyes, and mucous membranes exposed to irritants and / or on the irritants themselves.

[0025] "1-kestose" is a trisaccharide oligosaccharide consisting of one glucose molecule and two fructose molecules. 1-kestose may be produced according to methods known to those skilled in the art, or commercially available 1-kestose may be used for convenience. Commercially available products include purified products containing 1-kestose at high purity (mass % of the sugar when the total amount of sugars is taken as 100%), and mixtures of fructooligosaccharides containing 1-kestose at a relatively low purity of about 30 to 70 mass%, and either of these may be used.

[0026] "Raffinose" is a trisaccharide oligosaccharide consisting of one glucose molecule, one galactose molecule, and one fructose molecule. It is widely present in higher plants such as beets (sugar beets), sugarcane, cabbage, legume seeds, and corn. Raffinose hydrates are commercially available as a cosmetic ingredient, and it is also sold as a health food and reagent. Beet oligosaccharides containing highly purified raffinose extracted and purified from beets are also commercially available, and these commercially available products can be used in the present invention.

[0027] 1-kestose and raffinose are used by contacting the target skin, eye, or mucous membrane area together with or before exposure to an irritant. 1-kestose and raffinose may be used as is (in the form of powder or aqueous solution) or in a form mixed with an irritant or other ingredients.

[0028] That is, the present invention also provides a method for alleviating irritation. This method is a method for alleviating irritation to the skin, eyes, and / or mucous membranes, and is characterized by using an active ingredient (1-kestose and / or raffinose) in combination with a irritant. Here, "combined use" may mean, as described above, using the active ingredient and the irritant simultaneously, or using them with a certain time interval between them. Furthermore, the active ingredient and the irritant may be used in combination, or may be used separately.

[0029] The irritation alleviator and topical composition for alleviating irritation of the present invention can contain, in addition to the active ingredients 1-kestose and raffinose, an irritant substance and can further contain other ingredients within a range that does not impair the effects of the present invention. Examples of other ingredients include raw materials commonly used in cosmetics, quasi-drugs, pharmaceuticals, and hygiene products (e.g., oily bases, aqueous bases, surfactants, alcohols, preservatives, chelating agents, antioxidants, thickeners, excipients, fragrances, vitamins, anti-inflammatory agents, UV absorbers, UV scattering agents, polymeric compounds, animal and plant extracts, disinfectants, antioxidants, anti-aging ingredients, anti-inflammatory ingredients, whitening ingredients, cell activating ingredients, blood circulation promoting ingredients, moisturizing ingredients, ingredients that prevent and repair DNA damage, anti-glycation ingredients, peptides or derivatives thereof, amino acids or derivatives thereof, hydroquinone glycosides and esters thereof, etc.).

[0030] That is, the irritation alleviator and topical composition for alleviating irritation of the present invention can be in the form of cosmetics, quasi-drugs, pharmaceuticals, and also hygiene products such as cleansers, bath additives, disinfectants, germicides, etc. More specific dosage forms of these products include, for example, creams, sheets, lotions, emulsions, gels, aerosols, roll-ons, sticks, powders, tablets, etc.

[0031] The content of 1-kestose when other components are contained can be appropriately set depending on the product form and application. Specific examples of the content include 0.001% by mass or more, 0.01% by mass or more, 0.1% by mass or more, 1% by mass or more, 100% by mass or less, 90% by mass or less, 80% by mass or less, 70% by mass or less, 60% by mass or less, 50% by mass or less, 40% by mass or less, 35% by mass or less, and 30% by mass or less.

[0032] The raffinose content when other components are contained can also be appropriately set depending on the product form and application. Specific examples of the raffinose content include 0.001% by mass or more, 0.01% by mass or more, 0.1% by mass or more, 1% by mass or more, and 100% by mass or less, 90% by mass or less, 80% by mass or less, 70% by mass or less, 60% by mass or less, 50% by mass or less, 40% by mass or less, 35% by mass or less, and 30% by mass or less.

[0033] The present invention will be described below based on examples, but the technical scope of the present invention is not limited to the features shown by these examples. [Example]

[0034] <Test Method> The examples were carried out in the following manner unless otherwise specified.

[0035] (1) Test materials Eight types of test substances (all commercially available products) shown in Table 1 were used to evaluate the irritation-reducing effect. Five types of irritating substances (all commercially available products) shown in Table 1 were used. Sodium lauryl sulfate is an anionic surfactant commonly used in detergents, etc. Methylparaben and phenoxyethanol are preservatives commonly used in cosmetics, etc. Ethylhexylglycerin is a preservative aid commonly used in cosmetics, etc. Capsicum tincture is a plant extract commonly used in cosmetics, pharmaceuticals, and quasi-drugs for purposes such as promoting blood circulation. In this example, the concentrations (mass%) of the test substances and irritating substances are the concentrations of the products shown in Table 1. [Table 1]

[0036] (2) Evaluation of skin irritation [2-1] Patch test The patch test was performed using Finn Chamber (registered trademark) (Smart Practice Japan) according to the following procedures (i) to (iv). (i) A test area of ​​a size that matched the size of the gold plate of the Finn chamber was set on the outer side of the left forearm, and erythema measurements were made by placing marks on the area to obtain an erythema index (measurement before the test). (ii) Pre-application only: The test substance solution was prepared. 15 μl of the test substance solution was applied to each test area, and then air-dried for 20 minutes. (iii) The sample solution was prepared. The filter paper attached to the Finn chamber was fixed inside the chamber with white petrolatum, and then the sample solution was dropped onto the filter paper and attached to the test area. (iv) Two hours after application, the Finn chamber was removed, and the moisture in the test area was gently removed using tissue paper. (v) After a predetermined time (30 minutes, 1 hour or 2 hours) had elapsed since the Finn Chamber peeling, erythema measurements were carried out to obtain an erythema index (post-test measurement). (vi) Regarding the "erythema index measured after the test," a conversion value was calculated by setting the "erythema index measured before the test" at 100%, and this was used as the rate of change in the erythema index.

[0037] [2-2] Erythema measurement When skin irritation is severe, the skin surface usually turns red and erythema occurs.For this reason, in this embodiment, the erythema index of the test group is obtained using a measuring instrument Mexameter (registered trademark) MX18 (Courage+Khazaka Co., Ltd.), and is used as an index of the degree of skin irritation.Since skin erythema is mainly caused by vasodilation and local increase in hemoglobin concentration, this measuring instrument measures the hemoglobin concentration of the skin based on the principle of absorptiometry, and calculates the erythema index based on this.That is, the light of two wavelengths (568nm, 660nm) including the wavelength with the highest absorption by hemoglobin is irradiated onto the skin, and the amount of reflected light is measured, and the hemoglobin concentration or erythema index is calculated.

[0038] Therefore, the higher the erythema index value, the greater the skin irritation. Furthermore, the "rate of change in the erythema index," where the "erythema index measured before the test" is taken as 100%, can be considered a value that correlates with the intensity of the redness of the skin after the test, with the redness of the skin before the test being used as the standard. In other words, if the rate of change exceeds 100%, the higher the value, the greater the degree of redness compared to the skin before the test.

[0039] Example 1: Effect of alleviating skin irritation caused by sodium lauryl sulfate Patch tests were conducted using sodium lauryl sulfate as the irritant according to the method described in Test Method (2) [2-1]. A total of seven test areas were set up. The test substance solutions were aqueous solutions containing 1-kestose, raffinose, xylitol, a glycosyltrehalose / hydrolyzed hydrogenated starch mixture, or hydrolyzed hydrogenated starch, each dissolved at 5% by mass. The sample solution was either an aqueous solution containing 2% by mass of sodium lauryl sulfate or water. Erythema measurements were performed for each test area according to the method described in Test Method (2) [2-2], and the percentage change was obtained. The post-test erythema measurement was performed 2 hours after peeling. Table 2 shows an overview of the treatments and the percentage change in the erythema index for each test area. A bar graph of the percentage change is shown in Figure 1. [Table 2]

[0040] As shown in Table 2 and Figure 1, groups 5 to 7 showed a change rate equal to or greater than that of group 2, whereas groups 3 and 4 showed a smaller change rate than group 2. In particular, the change rate in group 3 was significantly smaller. That is, in the test groups in which a 1-kestose aqueous solution or a raffinose aqueous solution was pre-applied and then contacted with sodium lauryl sulfate, the degree of erythema was smaller than in the test groups in which neither pre-application nor contact was made with sodium lauryl sulfate aqueous solution alone. In particular, the degree of erythema was significantly smaller in the test group in which a 1-kestose aqueous solution was pre-applied. These results demonstrate that 1-kestose and raffinose can mitigate the irritation caused by surfactants.

[0041] Example 2: Effect of alleviating skin irritation caused by sodium lauryl sulfate The test substance solution was not applied beforehand. The test substances (1-kestose, glycosyl trehalose / hydrolyzed hydrogenated starch mixture, dipotassium glycyrrhizinate, and glucose) were dissolved in the test solution along with an irritant (sodium lauryl sulfate) and used in a patch test according to the method described in Test Method (2) [2-1]. A total of six test sections were set up. The concentrations of each substance in the test solution were 2% by mass for sodium lauryl sulfate, 5% by mass for 1-kestose, 6.76% by mass for the glycosyl trehalose / hydrolyzed hydrogenated starch mixture, 0.05% by mass for dipotassium glycyrrhizinate, and 5% by mass for glucose. Water was used as the test solution for Section 1. Erythema measurements were performed for each test section according to the method described in Test Method (2) [2-2], and the percentage change was obtained. The post-test erythema measurement was performed 30 minutes after removal. Table 3 shows the treatment summary and percentage change in the erythema index for each test section. A bar graph of the rate of change is shown in Figure 2. [Table 3]

[0042] As shown in Table 3 and Figure 2, the change rates in groups 4 to 6 were greater than in group 2, whereas the change rate in group 3 was smaller than in group 2 and was comparable to that in group 1. In other words, the test group exposed to 1-kestose in addition to sodium lauryl sulfate showed a smaller degree of erythema than the test group exposed to sodium lauryl sulfate alone. These results demonstrate that 1-kestose can alleviate the irritation caused by surfactants.

[0043] Example 3: Effect of alleviating skin irritation caused by sodium lauryl sulfate The test substance solution was not applied beforehand. The test substance (1-kestose) was dissolved in the sample solution together with an irritant (sodium lauryl sulfate), and patch tests were conducted using the method described in Test Method (2) [2-1]. Three test sections were set up in total. The concentrations of each substance in the sample solution were 2% by mass for sodium lauryl sulfate and 2% by mass for 1-kestose. Water was used as the sample solution for the first section. Erythema measurements were performed for each test section using the method described in Test Method (2) [2-2], and the percentage change was obtained. The post-test erythema measurements were performed 30 minutes and 2 hours after removal. Table 4 shows an overview of the treatments for each test section, along with the percentage change in the erythema index. A line graph of the percentage change is shown in Figure 3. [Table 4]

[0044] As shown in Table 4 and Figure 3, the rate of change in Group 3 was smaller than that in Group 2 at both 30 minutes and 2 hours after peeling. In other words, the test group exposed to 2% by mass of 1-kestose in addition to sodium lauryl sulfate showed a smaller degree of erythema than the test group exposed to sodium lauryl sulfate alone. These results demonstrate that 1-kestose can alleviate surfactant irritation regardless of its concentration.

[0045] <Example 4> Effect of alleviating skin irritation caused by methylparaben The test substance solution was not applied beforehand. The test substances (1-kestose, sucrose) were dissolved in the sample solution together with an irritant (methylparaben), and patch tests were conducted using the method described in Test Method (2) [2-1]. A total of four test sections were set up. The concentrations of each substance in the sample solution were 0.1% by mass for methylparaben, 5% by mass for 1-kestose, and 5% by mass for sucrose. Water was used as the sample solution for Section 1. Erythema measurements were performed for each test section using the method described in Test Method (2) [2-2], and the percentage change was obtained. The post-test erythema measurements were performed 1 and 2 hours after removal. Table 5 shows an overview of the treatments for each test section, along with the percentage change in the erythema index. A line graph of the percentage change is shown in Figure 4. [Table 5]

[0046] As shown in Table 5 and Figure 4, the rate of change in Group 3 was smaller than that in Group 2 at both 1 and 2 hours after peeling. In other words, the test group exposed to 1-kestose in addition to methylparaben showed a smaller degree of erythema than the test group exposed to methylparaben alone. These results demonstrate that 1-kestose can alleviate the irritation caused by preservatives.

[0047] Example 5: Examination of 1-kestose concentration The test substance solution was not applied beforehand. The test substance (1-kestose) was dissolved in the sample solution together with the irritant (methylparaben), and patch tests were conducted using the method described in Test Method (2) [2-1]. Five test sections were set up in total. The concentrations of each substance in the sample solution were 0.1% by mass for methylparaben and 2%, 5%, or 10% by mass for 1-kestose. Water was used as the sample solution for the first section. Erythema measurements were performed for each test section using the method described in Test Method (2) [2-2], and the percentage change was obtained. The post-test erythema measurements were performed 1 and 2 hours after removal. Table 6 shows the treatment summary and percentage change in the erythema index for each test section. A line graph of the percentage change is shown in Figure 5. [Table 6]

[0048] As shown in Table 6 and Figure 5, the change rates in Groups 3, 4, and 5 were smaller than that in Group 2 at both 1 hour and 2 hours after peeling. In other words, the test groups exposed to a 2-10% by mass 1-kestose aqueous solution in addition to methylparaben showed a smaller degree of erythema than the test group exposed to methylparaben alone. These results demonstrate that 1-kestose can mitigate the irritation caused by preservatives, regardless of the concentration.

[0049] Example 6: Effect of mitigating skin irritation caused by phenoxyethanol The test substance solution was not applied beforehand. Instead, the test substance (1-kestose) was dissolved in the sample solution together with the irritant (phenoxyethanol), and patch tests were conducted using the method described in Test Method (2) [2-1]. Five test sections were set up in total. The concentrations of each substance in the sample solution were 1.0% by mass for phenoxyethanol and 2%, 5%, or 10% by mass for 1-kestose. Water was used as the sample solution for the first section. Erythema measurements were performed for each test section using the method described in Test Method (2) [2-2], and the percentage change was obtained. The post-test erythema measurements were performed 30 minutes and 2 hours after removal. Table 7 shows the treatment summary and percentage change in the erythema index for each test section. A line graph of the percentage change is shown in Figure 6. [Table 7]

[0050] As shown in Table 7 and Figure 6, the change rates in Groups 3, 4, and 5 were smaller than that in Group 2 at both 30 minutes and 2 hours after peeling. That is, the test groups exposed to a 2-10% by mass aqueous solution of 1-kestose in addition to phenoxyethanol showed a smaller degree of erythema than the test group exposed to phenoxyethanol alone. These results demonstrate that 1-kestose can mitigate the irritation caused by preservatives, regardless of the concentration.

[0051] Example 7: Effect of ethylhexylglycerin on skin irritation The test substance solution was not applied beforehand. Instead, the test substance (1-kestose) was dissolved in the sample solution together with an irritant (ethylhexylglycerin), and patch tests were conducted using the method described in Test Method (2) [2-1]. A total of four test sections were set up. The concentrations of each substance in the sample solution were 0.18% by mass for ethylhexylglycerin and 2% or 10% by mass for 1-kestose. Water was used as the sample solution for Section 1. Erythema measurements were performed for each test section using the method described in Test Method (2) [2-2], and the percentage change was obtained. The post-test erythema measurements were performed 30 minutes and 2 hours after removal. Table 8 shows the treatment summary and percentage change in the erythema index for each test section. A line graph of the percentage change is shown in Figure 7. [Table 8]

[0052] As shown in Table 8 and Figure 7, the change rates in Groups 3 and 4 were smaller than that in Group 2 at both 30 minutes and 2 hours after peeling. That is, the test group exposed to a 2-10% by mass aqueous solution of 1-kestose in addition to ethylhexylglycerin showed a smaller degree of erythema than the test group exposed to ethylhexylglycerin alone. These results demonstrate that 1-kestose can mitigate the irritation of preservative aids, regardless of their concentration.

[0053] Example 8: Effect of reducing skin irritation caused by capsicum tincture The test substance solution was not applied in advance. The test substance (1-kestose) was dissolved in the sample solution together with the irritant (capsicum tincture) and used for patch testing according to the method described in Test Method (2) [2-1]. A total of three test sections were set up. The concentrations of each substance in the sample solution were 2% by mass for capsicum tincture and 5% by mass for 1-kestose. Water was used as the sample solution for Section 1. Erythema measurements were performed for each test section according to the method described in Test Method (2) [2-2], and the percentage change was obtained. The post-test erythema measurements were performed 30 minutes and 2 hours after removal. Table 9 shows an overview of the treatments for each test section and the percentage change in the erythema index. A line graph of the percentage change is shown in Figure 8. [Table 9]

[0054] As shown in Table 9 and Figure 8, the rate of change in Group 3 was smaller than that in Group 2 at both 30 minutes and 2 hours after peeling. In other words, the test group exposed to 1-kestose in addition to capsicum tincture showed a smaller degree of erythema than the test group exposed to capsicum tincture alone. These results demonstrate that 1-kestose can alleviate the irritation caused by plant extracts.

[0055] Example 9: Eye irritation relief effect The effect of test substances on ocular irritation was evaluated using the Reconstructed Human Cornea-like Epithelium Test Method (RhCE test method) (OECD test guideline TG492), which uses a three-dimensional cultured corneal epithelium model in which normal human corneal epithelial cells are cultured in layers. After exposing the corneal epithelium model (RhCE tissue) to the irritant and test substances, cell viability was determined by quantifying the formazan dye produced by the reduction of tetrazolium dye by viable cells using absorbance measurement.

[0056] Specifically, the test was carried out according to the following procedures 1) to 8). 1) Sample solutions A to C were prepared. Sample solution A was a negative control, and Mg2+ / Ca 2+ The sample solution was a phosphate-buffered saline solution (PBS(-)). Sample solution B was an aqueous solution (SLS) in which sodium lauryl sulfate was dissolved to a concentration of 5% by mass. Sample solution C was an aqueous solution (SLS+Kes) in which sodium lauryl sulfate and 1-kestose were each dissolved to a concentration of 5% by mass. 2) The human 3D cultured corneal epithelial model "LabCyte CORNEA-MODEL" (J-TEC) was cultured in the attached assay medium for 15 to 30 hours. 3) 50 μL each of sample solution A, B, or C was added to the corneal surface of three corneal epithelial models and allowed to stand for 1 minute. 4) The corneal epithelium model was removed and washed with PBS(-) at least 10 times. 5) The corneal epithelial model was transferred to a well of a culture plate containing 500 μL of fresh assay medium and cultured for 24 hours. 6) The corneal epithelium model was washed twice with 20 mL of PBS(-) and then cultured in a WST-8 (tetrazolium salt) reaction solution for 4 hours. 7) The WST-8 reaction solution was thoroughly stirred, and 200 μL of each was transferred to a microplate. The absorbance at 450 nm and 650 nm was measured using a microplate reader. The measured absorbance at 450 nm minus the absorbance at 650 nm was used as the measured value. The average of the measured values ​​for the samples using each of sample solutions A to C was calculated. 8) The cell viability of the corneal epithelium model exposed to sample solution A (negative control) was set at 100%, and the cell viability when exposed to sample solutions B and C was calculated using the following formula 1. Equation 1: Cell viability (%) = (average of measured values ​​of sample solution B or sample solution C / average of measured values ​​of sample solution A) * 100

[0057] Figure 9 shows the cell viability of the corneal epithelium model exposed to sample solutions A to C. As shown in Figure 9, the cell viability was 94.3% for sample solution B, while it was 99.9% for sample solution C. In other words, the number of surviving cells was greater in the corneal epithelium model exposed to 1-kestose in addition to sodium lauryl sulfate than in the model exposed to sodium lauryl sulfate alone. These results demonstrate that 1-kestose can alleviate irritation caused by irritating substances not only in skin tissue but also in eye tissue.

Claims

1. An irritation-relieving agent containing 1-kestose and / or raffinose as an active ingredient for relieving irritation to the skin, eyes and / or mucous membranes.

2. The agent according to claim 1, which is used to alleviate irritation caused by surfactants, preservatives, preservative aids and / or plant extracts.

3. An external composition for alleviating irritation to the skin, eyes and / or mucous membranes, comprising the agent according to claim 1 or 2.

4. A method for alleviating irritation to the skin, eyes and / or mucous membranes, comprising using the agent according to claim 1 or 2 in combination with an irritant.

Citation Information

Patent Citations

  • Abirritant composition

    JP2003155246A