Composition for improving skin or composition for improving hair, and containing urolithins
A urolithin-containing composition addresses the inefficacies of existing products by providing effective skin and hair improvements through controlled intake amounts and concentrations, enhancing elasticity, luster, thickness, and promoting growth, even at lower doses.
Patent Information
- Application Number
- PCT/JP2024/034320
- Authority / Receiving Office
- WO · WO
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2023-09-29
- Filing Date
- 2024-09-26
- Publication Date
- 2025-04-03
AI Technical Summary
Existing skincare and haircare products do not effectively improve skin elasticity, luster, thickness, firmness, and reduce wrinkles, and promote hair growth or regrowth without requiring large doses of urolithins.
A composition containing urolithins, specifically urolithin A and urolithin C, is formulated to achieve skin and hair improvements, with daily intake amounts between 1 mg and 250 mg and peak blood concentrations of 0.1 μM to 3.3 μM, utilizing natural sources like pomegranates and chemical synthesis.
The composition achieves skin improvements such as enhanced elasticity, luster, thickness, and reduced wrinkles, and promotes hair growth and regrowth, even at lower doses than conventional products, using urolithins derived from ellagitannins.
Smart Images

Figure JPOXMLDOC01-APPB-C000001 
Figure JPOXMLDOC01-APPB-T000002 
Figure JPOXMLDOC01-APPB-T000003
Abstract
Description
Skin-improving composition or hair-improving composition containing urolithins
[0001] The present disclosure relates to a skin improving composition or a hair improving composition containing urolithins.
[0002] Urolithins, represented by urolithin A and urolithin C, are known as intestinal metabolites of ellagic acid, which is derived from ellagitannins found in berries such as pomegranates, raspberries, blackberries, cloudberries, strawberries, and walnuts. As an example of the use and dosage of urolithins, it has been reported that muscle function improved when humans were given urolithin A produced by chemical synthesis at doses of 250 mg / day, 500 mg / day, or 1,000 mg / day for 28 days (Patent Document 1, Patent Document 2).
[0003] Special table 2020-510678 publication Special table 2020-514338 publication
[0004] An object of the present disclosure is to provide at least a technique for improving skin or hair.
[0005] The present inventors conducted extensive research to solve the above-mentioned problems and found that the above-mentioned problems can be solved by using urolithins.
[0006] The present disclosure can provide a skin improvement composition containing urolithins. The skin improvement of the composition is preferably one or more selected from the group consisting of improved skin elasticity, skin beautification, skin gloss improvement, whitening, improved skin thickness, improved skin firmness, and wrinkle reduction. The total daily intake of the urolithins of the composition is preferably 1 mg to 250 mg. The composition is preferably ingested so that the maximum blood concentration of the urolithins is 0.1 μM to 3.3 μM. The present disclosure can also provide a hair improvement composition containing urolithins. The hair improvement of the composition is preferably one or more selected from the group consisting of hair growth and hair regeneration. The total daily intake of the urolithins of the composition is preferably 1 mg to 250 mg. The composition is preferably ingested so that the maximum blood concentration of the urolithins is 0.1 μM to 3.3 μM.
[0007] The present disclosure may at least provide an effect of providing a technique for improving skin or hair. Furthermore, in a preferred embodiment of the present disclosure, skin or hair improvement can be achieved even when the intake amount is smaller than that of conventional products, thereby eliminating the need to ingest large amounts of urolithins.
[0008] The configurations and combinations thereof in each embodiment are merely examples, and additions, omissions, substitutions, and other modifications of the configurations are possible as appropriate without departing from the spirit of the present disclosure. The present disclosure is not limited by the embodiments, but is limited only by the scope of the claims. Furthermore, each aspect of the present disclosure can be combined with any feature of the present disclosure.
[0009] <Urolithins> Urolithins are represented by the following general formula (1): (In the formula, R1 to R6 each independently represent a hydroxyl group, a hydrogen atom, or a methoxy group.) One or more of R1 to R6 in the formula may be a hydroxyl group, or all of them may be hydrogen atoms. Examples of urolithins include all compounds included in the compound represented by general formula (1). Specific examples include urolithin A, urolithin B, urolithin C, urolithin D, urolithin E, urolithin M3, urolithin M4, urolithin M5, urolithin M6, urolithin M7, urolithin M8, isourolithin A, and 6H-dibenzo[b,d]pyran-6-one. Urolithins can be used singly or in any combination of two or more.
[0010] Note that, although the term "class" is sometimes used in the present disclosure, such as "urolithins," this is merely a formal notation for classification. For example, "urolithins" is a concept that includes urolithin A, urolithin B, etc., which are included in "urolithins," and "urolithins" is sometimes simply referred to as "urolithin" as a generic term that represents urolithin A, urolithin B, etc.
[0011] The method for obtaining urolithins is not particularly limited, and commercially available products may be used, or urolithins may be synthesized by chemical synthesis. Examples of commercially available urolithins include urolithin A, urolithin B, urolithin C, urolithin D, and urolithin E (manufactured by Dalton Pharma). Chemical synthesis can be performed according to conventional methods, such as synthesizing urolithin A using 2-bromo-5-methoxybenzoic acid and aluminum chloride as raw materials, as described in the Examples section of this specification.
[0012] Alternatively, punicalagin, a type of ellagitannin, may be extracted from a plant, hydrolyzed to ellagic acid, or ellagic acid may be extracted and then converted to urolithins using a microorganism. The type of plant is not particularly limited, and examples include pomegranate, raspberry, blackberry, cloudberry, boysenberry, strawberry, walnut, and Geranium herb. Among these, pomegranate, boysenberry, and Geranium herb are preferred, with pomegranate being more preferred, due to their high content of ellagitannins and / or ellagic acid. These plants may be used alone or in combination with two or more species. The extraction method and conditions from the plant are not particularly limited, and may be conventional. For example, known extraction methods such as water extraction, hot water extraction, warm water extraction, alcohol extraction, and supercritical extraction may be used.
[0013] When solvent extraction is performed, examples of the solvent include water; alcohols (whether anhydrous or hydrous) such as lower alcohols such as methanol and ethanol, and polyhydric alcohols such as propylene glycol and 1,3-butylene glycol; ketones such as acetone; esters such as diethyl ether, dioxane, acetonitrile, and ethyl acetate; and xylene, with water and ethanol being preferred. These solvents may be used alone or in combination. The method for hydrolyzing the extracted ellagitannins such as punicalagin to ellagic acid is not particularly limited, and examples include hydrolysis using acids, enzymes, and microorganisms. The method for converting ellagic acid into urolithins using microorganisms is not particularly limited, and a known method such as that described in Food Funct., 5, 8, 1779-1784 (2014) can be used.
[0014] The obtained urolithins can be used as is, or may be dried and used in powder form. Furthermore, if necessary, the obtained urolithins may be subjected to purification, concentration, or other treatments. Purification treatments include filtration, adsorption using ion exchange resins or activated carbon columns, and decolorization. Concentration treatments can be performed using conventional methods such as an evaporator.
[0015] Alternatively, the obtained urolithins (or purified or concentrated products) may be powdered according to known methods, such as freeze-drying to obtain a powder, or adding an excipient such as dextrin, corn starch, or gum arabic and then spray-drying to obtain a powder. The resulting product may then be dissolved in pure water, ethanol, or the like, as needed, for use.
[0016] <Skin-improving composition> One aspect of the present disclosure is a skin-improving composition containing urolithins. The composition according to this aspect may contain urolithins alone, or may contain other components as long as it can improve skin. When the composition according to this aspect contains other components, the composition according to this aspect may be a mixture of urolithins and other components, and these components may be homogeneous or heterogeneous.
[0017] The composition according to this embodiment is intended to be ingested by a human, and the human may be a male (male human) or a female (female human).
[0018] The age of the person ingesting the composition according to this embodiment is not particularly limited as long as the skin is improved by ingestion of the composition according to this embodiment, and may be, for example, 12 years or older, 18 years or older, 25 years or older, 30 years or older, 40 years or older, etc., or 100 years or younger, 75 years or younger, 60 years or younger, 50 years or younger, 40 years or younger, etc., or any compatible combination thereof. Specifically, for example, 12 years or older and 100 years or younger, 18 years or older and 75 years or older, 25 years or older and 60 years or older, 30 years or older and 50 years or older, 40 years or older and 50 years or older, 18 years or older and 40 years or younger, etc.
[0019] In this embodiment, skin improvement may be "improvement of skin condition" or "improvement of skin symptoms." In this embodiment, skin improvement is preferably one or more selected from the group consisting of improvement of skin elasticity, beautiful skin, improvement of skin luster, whitening, improvement of skin thickness, improvement of skin firmness, and improvement of wrinkles. "Beautiful skin" may mean "making the skin beautiful" or "beautifying the skin" of the person who consumes the product. "Whitening" may mean "whitening" or "whitening" the skin of the person who consumes the product.
[0020] The composition of this embodiment may be used for non-therapeutic purposes. "Non-therapeutic purposes" are purposes that do not include medical procedures. In other words, purposes that do not include therapeutic treatment of a subject. Furthermore, the "skin condition" and "skin symptom" may be "skin conditions caused by factors other than disease, etc." and "skin symptoms caused by factors other than disease, etc.", respectively. Therefore, when the composition of this embodiment is, for example, a food or drink composition (e.g., a health food or drink), it may be intended for "skin conditions caused by factors other than disease, etc." or "skin symptoms caused by factors other than disease, etc." Furthermore, the composition of this embodiment may be intended for healthy individuals.
[0021] The "improvement of skin elasticity," a preferred aspect of this embodiment, can be determined based on indicators measured (or determined) using a measurement method (or determination method) commonly used in the art. For example, the "R7 value" measured by a cutometer, the "skin thickness (μm)" measured by a DermaLab, and the "Low Echogenic Band (LEB) (μm)" measured by a DermaLab can be used as indicators. Specifically, the "improvement of skin elasticity," a preferred aspect of this embodiment, corresponds to an improvement in one or more of the following: the "R7 value," "skin thickness (μm)," and the "Low Echogenic Band (LEB) (μm)." The more desirable the "R7 value," the more desirable it is. The higher the "skin thickness (μm)," the more desirable it is, and the lower the "Low Echogenic Band (LEB) (μm)."
[0022] "Beautiful skin," a preferred aspect of this embodiment, can be determined based on an index measured (or determined) by a measurement method (or determination method) commonly used in the art. For example, it can be determined using an index such as "Gloss Value" measured by a gloss meter or "Diffuse Scattering Correction" measured by a gloss meter. Specifically, "beautiful skin," a preferred aspect of this embodiment, corresponds to a desirable state in which one or more of the following selected from the group consisting of "Gloss Value" and "Diffuse Scattering Correction" are favorable, and more desirable states are more favorable. The higher the "Gloss Value," the more favorable the "Diffuse Scattering Correction."
[0023] The "improvement of skin gloss," which is a preferred aspect of this embodiment, can be determined based on an index measured (or determined) by a measurement method (or determination method) commonly used in the art. For example, it can be determined using an index such as "Gloss Value" measured by a gloss meter or "Diffuse Scattering Correction" measured by a gloss meter. Specifically, the "improvement of skin gloss," which is a preferred aspect of this embodiment, corresponds to a favorable increase in one or more selected from the group consisting of "Gloss Value" and "Diffuse Scattering Correction," and it is more preferable if more of them are favorable. The larger the "Gloss Value," the more preferable the "Diffuse Scattering Correction."
[0024] "Whitening," a preferred aspect of this embodiment, can be determined based on an index measured (or determined) by a measurement method (or determination method) commonly used in the art. For example, it can be determined using an index such as a "melanin value" measured by a mexameter or an "erythema value" measured by a mexameter. Specifically, "whitening," a preferred aspect of this embodiment, corresponds to a favorable state of one or more values selected from the group consisting of "melanin value" and "erythema value," and more favorable states of more values are preferred. The smaller the "melanin value," the more preferable the "erythema value."
[0025] The "improvement of skin thickness," which is a preferred aspect of this embodiment, can be determined based on an index measured (or determined) by a measurement method (or determination method) commonly used in the art. For example, it can be determined using indices such as "Skin Thickness (μm)" measured by Derma Lab and "Low Echogenic Band (LEB) (μm)" measured by Derma Lab. Specifically, the "improvement of skin thickness," which is a preferred aspect of this embodiment, corresponds to an improvement in one or more of the following selected from the group consisting of "Skin Thickness (μm)" and "Low Echogenic Band (LEB) (μm)," with the improvement being more preferable. The larger the "Skin Thickness (μm)," the more preferable the "Low Echogenic Band (LEB) (μm)."
[0026] The "improvement of skin firmness," which is a preferred aspect of this embodiment, can be determined based on an index measured (or determined) by a measurement method (or determination method) commonly used in the art. For example, it can be determined using indices such as "Skin Thickness (μm)" measured by Derma Lab and "Low Echogenic Band (LEB) (μm)" measured by Derma Lab. Specifically, the "improvement of skin firmness," which is a preferred aspect of this embodiment, corresponds to an improvement in one or more of the following: "Skin Thickness (μm)" and "Low Echogenic Band (LEB) (μm)." The more the number of improvements, the more preferable it is. The larger the "Skin Thickness (μm)," the more preferable it is, and the smaller the "Low Echogenic Band (LEB) (μm)."
[0027] "Improvement of wrinkles," which is a preferred aspect of this embodiment, can be determined based on an index measured (or determined) by a measurement method (or determination method) commonly used in the art. For example, it can be determined using an index such as a "wrinkle grade" determined by wrinkle grade determination. Specifically, "improvement of wrinkles," which is a preferred aspect of this embodiment, corresponds to a case where the "wrinkle grade" becomes favorable. The "wrinkle grade" is more favorable when the sum of positive ranks is smaller than the sum of negative ranks.
[0028] The form of the composition according to this embodiment is not particularly limited. Examples of the form of the composition according to this embodiment include powder, granules, paste, pellets, capsules (hard capsules, soft capsules), tablets, etc. Furthermore, the composition according to this embodiment may be a solution or dispersion using water or the like as a solvent, or may be an emulsion composition.
[0029] The total content of urolithins relative to the total amount of the composition according to this embodiment may be, for example, 0.001% by weight or more, 0.01% by weight or more, 0.1% by weight or more, or 10% by weight or less, 5% by weight or less, 1% by weight or less, or any compatible combination thereof. Specifically, for example, 0.001% by weight or more and 10% by weight or less, 0.01% by weight or more and 5% by weight or less, 0.1% by weight or more and 1% by weight or less, etc.
[0030] The effective intake amount of the composition according to this embodiment may be appropriately determined depending on the person's age, body weight, skin condition, skin symptoms, intake route, intake schedule, formulation, etc., but is not particularly limited as long as skin is improved by ingestion of the composition according to this embodiment. The effective intake amount of the composition according to this embodiment may be, for example, 1 mg or more, 5 mg or more, 10 mg or more, 15 mg or more, 20 mg or more, etc., per day as the total amount of urolithins, or 500 mg or less, 250 mg or less, 200 mg or less, 150 mg or less, 100 mg or less, 50 mg or less, 30 mg or less, 20 mg or less, etc., or a compatible combination thereof. Specifically, the effective intake amount is 1 mg or more and 500 mg or less, 5 mg or more and 250 mg or less, 10 mg or more and 200 mg or less, 15 mg or more and 150 mg or more, 20 mg or more and 100 mg or more, 20 mg or more and 50 mg or less, 20 mg or more and 30 mg or less, 10 mg or more and 20 mg or less, etc.
[0031] Furthermore, the composition according to this embodiment has a maximum blood concentration (C max) may be ingested to a concentration of, for example, 0.1 μM or more, 0.2 μM or more, 0.6 μM or more, 0.7 μM or more, 0.8 μM or more, 1.7 μM or more, etc., or 3.3 μM or less, 1.7 μM or less, 1.6 μM or less, 0.7 μM or less, 0.6 μM or less, etc., or any compatible combination thereof. In this case, "urolithins" includes glucuronide conjugates. Specifically, the concentration may be 0.1 μM or more and 3.3 μM or less, 0.2 μM or more and 1.7 μM or less, 0.6 μM or more and 1.6 μM or less, 0.7 μM or more and 1.6 μM or less, 0.8 μM or more and 1.7 μM or less, 1.7 μM or more and 3.3 μM or less, 0.2 μM or more and 0.7 μM or less, 0.1 μM or more and 0.6 μM or less, etc.
[0032] Furthermore, the composition according to this embodiment has a maximum blood concentration (t max ) may be ingested for, for example, 0.5 hours or more, 2 hours or more, 4.65 hours or more, 5 hours or more, 6 hours or more, 7.2 hours or more, or for 12 hours or less, 7.2 hours or less, 6 hours or less, 5 hours or less, 4.65 hours or less, 3 hours or less, or the like, or any compatible combination thereof. In this case, "urolithins" includes glucuronide conjugates. Specifically, the urolithins may be ingested for 0.5 hours or more and 12 hours or less, 2 hours or more and 7.2 hours or less, 4.65 hours or more and 6 hours or less, 5 hours or more and 6 hours or less, 6 hours or more and 7.2 hours or less, 7.2 hours or more and 12 hours or less, 0.5 hours or more and 5 hours or less, 2 hours or more and 4.65 hours or less, 2 hours or more and 3 hours or less, etc.
[0033] Furthermore, the composition according to this embodiment has a plasma concentration-area under the curve (AUC) for up to 24 hours as the total amount of urolithins. 0-24時間) may be ingested to a concentration of, for example, 1 μM or more, 2.36 μM or more, 4.3 μM or more, 7.86 μM or more, 18 μM or more, 24.61 μM or more, or 34 μM or less, 24.61 μM or less, 15 μM or less, 7.86 μM or less, 3.2 μM or less, 2.36 μM or less, or any compatible combination thereof. In this case, "urolithins" includes glucuronide conjugates. Specifically, it may be 1 μM or more and 34 μM or less, 2.36 μM or more and 24.61 μM or less, 4.3 μM or more and 15 μM or less, 7.86 μM or more and 15 μM or less, 18 μM or more and 24.61 μM or less, 24.61 μM or more and 34 μM or less, 4.3 μM or more and 7.86 μM or less, 2.36 μM or more and 3.2 μM or less, or 1 μM or more and 2.36 μM or less, etc.
[0034] The composition according to this embodiment may be taken once a day, or in divided doses per day, or once every few days or weeks, but daily intake is preferred.
[0035] The intake period of the composition according to this embodiment may be, for example, 4 weeks or more, 8 weeks or more, 12 weeks or more, etc. On the other hand, there is no upper limit to the intake period, and a longer period is preferable, but examples include until death, 1 year or less, 6 months or less, etc. Specifically, it is 4 weeks or more until death, 8 weeks or more and 1 year or less, 12 weeks or more and 6 months or less, etc.
[0036] A preferred embodiment of the composition according to this aspect is a food or beverage product (including a supplement). That is, a preferred embodiment that can be provided by the present disclosure is a food or beverage product containing urolithins as an active ingredient.
[0037] When urolithins are used as ingredients in foods and beverages, they can be used in general foods and beverages, as well as in foods for specified health uses, nutritional supplements, functional foods, foods for the sick, food additives, etc. (These include beverages.) As for the form of the food and beverage, for example, after adding appropriate auxiliary agents, they can be formed into an edible form, such as granules, particles, tablets, capsules, or pastes, using conventional means, and then provided for consumption. They can also be added to various foods, for example, processed meat foods such as ham and sausage, processed seafood foods such as kamaboko and chikuwa, bread, confectionery, butter, powdered milk, fermented dairy products, or beverages such as water, fruit juice, milk, and soft drinks.
[0038] The food and beverage products according to this embodiment may contain, as their main ingredients, water, proteins, carbohydrates, lipids, vitamins, minerals, organic acids, organic bases, fruit juice, flavors, etc. Examples of proteins include animal and vegetable proteins such as whole milk powder, skim milk powder, partially skim milk powder, casein, soy protein, egg protein, and meat protein, as well as hydrolysates thereof, and butter. Examples of carbohydrates include sugars, modified starch (dextrin, soluble starch, British starch, oxidized starch, starch ester, starch ether, etc.), and dietary fiber. Examples of lipids include vegetable oils and fats such as lard, safflower oil, corn oil, rapeseed oil, palm oil, fractionated oils thereof, hydrogenated oils, and interesterified oils. Examples of vitamins include vitamin A, carotenes, B vitamins, vitamin C, D vitamins, vitamin E, K vitamins, vitamin P, vitamin Q, niacin, nicotinic acid, pantothenic acid, biotin, inositol, choline, and folic acid. Examples of minerals include calcium, potassium, magnesium, sodium, copper, iron, manganese, zinc, selenium, and whey minerals. Examples of organic acids include malic acid, citric acid, lactic acid, and tartaric acid. Two or more of these components may be used in combination, and synthetic products and / or foods and beverages containing large amounts of these may also be used.
[0039] The food and beverage product according to this embodiment can be produced according to conventional methods. The amount, method, and timing of incorporation of urolithins can be selected as appropriate. Furthermore, the product can be packaged in an appropriate container such as a bottle, bag, can, box, or pack, as needed.
[0040] The total content of urolithins relative to the total amount of the food or beverage according to this embodiment may be, for example, 0.001% by weight or more, 0.01% by weight or more, 0.1% by weight or more, or 10% by weight or less, 5% by weight or less, 1% by weight or less, or any compatible combination thereof. Specifically, for example, 0.001% by weight or more and 10% by weight or less, 0.01% by weight or more and 5% by weight or less, 0.1% by weight or more and 1% by weight or less, etc.
[0041] The effective intake amount of the food or beverage according to this embodiment may be appropriately determined based on a person's age, body weight, skin condition, skin symptoms, intake route, intake schedule, formulation, etc., but is not particularly limited as long as skin is improved by ingestion of the food or beverage according to this embodiment. The effective intake amount of the food or beverage according to this embodiment may be, for example, 1 mg or more, 5 mg or more, 10 mg or more, 15 mg or more, 20 mg or more, etc., per day as the total amount of urolithins, or 500 mg or less, 250 mg or less, 200 mg or less, 150 mg or less, 100 mg or less, 50 mg or less, 30 mg or less, 20 mg or less, etc., or a compatible combination thereof. Specifically, the effective intake amount is 1 mg or more and 500 mg or less, 5 mg or more and 250 mg or less, 10 mg or more and 200 mg or less, 15 mg or more and 150 mg or more, 20 mg or more and 100 mg or more, 20 mg or more and 50 mg or less, 20 mg or more and 30 mg or less, 10 mg or more and 20 mg or less, etc.
[0042] Furthermore, the food and drink according to this embodiment has a maximum blood concentration (C max) may be ingested to a concentration of, for example, 0.1 μM or more, 0.2 μM or more, 0.6 μM or more, 0.7 μM or more, 0.8 μM or more, 1.7 μM or more, etc., or 3.3 μM or less, 1.7 μM or less, 1.6 μM or less, 0.7 μM or less, 0.6 μM or less, etc., or any compatible combination thereof. In this case, "urolithins" includes glucuronide conjugates. Specifically, the concentration may be 0.1 μM or more and 3.3 μM or less, 0.2 μM or more and 1.7 μM or less, 0.6 μM or more and 1.6 μM or less, 0.7 μM or more and 1.6 μM or less, 0.8 μM or more and 1.7 μM or less, 1.7 μM or more and 3.3 μM or less, 0.2 μM or more and 0.7 μM or less, 0.1 μM or more and 0.6 μM or less, etc.
[0043] Furthermore, the food and drink according to this embodiment has a maximum blood concentration reaching time (t max ) may be ingested for, for example, 0.5 hours or more, 2 hours or more, 4.65 hours or more, 5 hours or more, 6 hours or more, 7.2 hours or more, or for 12 hours or less, 7.2 hours or less, 6 hours or less, 5 hours or less, 4.65 hours or less, 3 hours or less, or the like, or any compatible combination thereof. In this case, "urolithins" includes glucuronide conjugates. Specifically, the urolithins may be ingested for 0.5 hours or more and 12 hours or less, 2 hours or more and 7.2 hours or less, 4.65 hours or more and 6 hours or less, 5 hours or more and 6 hours or less, 6 hours or more and 7.2 hours or less, 7.2 hours or more and 12 hours or less, 0.5 hours or more and 5 hours or less, 2 hours or more and 4.65 hours or less, 2 hours or more and 3 hours or less, etc.
[0044] Furthermore, the food and drink according to this embodiment has a plasma concentration-area under the curve (AUC) for up to 24 hours as a total amount of urolithins. 0-24時間) may be ingested to a concentration of, for example, 1 μM or more, 2.36 μM or more, 4.3 μM or more, 7.86 μM or more, 18 μM or more, 24.61 μM or more, or 34 μM or less, 24.61 μM or less, 15 μM or less, 7.86 μM or less, 3.2 μM or less, 2.36 μM or less, or any compatible combination thereof. In this case, "urolithins" includes glucuronide conjugates. Specifically, it may be 1 μM or more and 34 μM or less, 2.36 μM or more and 24.61 μM or less, 4.3 μM or more and 15 μM or less, 7.86 μM or more and 15 μM or less, 18 μM or more and 24.61 μM or less, 24.61 μM or more and 34 μM or less, 4.3 μM or more and 7.86 μM or less, 2.36 μM or more and 3.2 μM or less, or 1 μM or more and 2.36 μM or less, etc.
[0045] The food and drink according to this embodiment may be taken once a day or in divided doses per day, or once every few days or weeks, but daily intake is preferred.
[0046] The intake period of the food or beverage according to this embodiment may be, for example, 4 weeks or more, 8 weeks or more, 12 weeks or more, etc. On the other hand, the upper limit of the intake period is not limited, and a longer period is preferable, but examples include until death, 1 year or less, 6 months or less, etc. Specifically, it is 4 weeks or more until death, 8 weeks or more and 1 year or less, 12 weeks or more and 6 months or less, etc.
[0047] When urolithins are used as ingredients in foods and beverages for the above-mentioned uses, the foods and beverages may state the respective uses, or may state uses that are associated with the respective uses.
[0048] <Hair Improvement Composition> One aspect of the present disclosure is a hair improvement composition containing urolithins. With regard to this aspect, the explanation of the skin improvement composition according to the previous aspect is basically applicable, but differences will be described below.
[0049] In this embodiment, "hair" refers to "scalp hair." Therefore, "hair improvement" in this embodiment may be "scalp hair improvement." Hair improvement in this embodiment may be "improvement of hair condition" or "improvement of hair symptoms." Hair improvement in this embodiment is preferably one or more selected from the group consisting of hair growth and hair regeneration. "Hair growth" may be "inhibition of hair loss" or "prevention of hair loss."
[0050] "Hair growth," which is a preferred aspect of this embodiment, can be determined based on an index measured (or determined) by a measurement method (or determination method) commonly used in the art. For example, "hair density ( / cm)" measured by Trichoscan 2 ")" and "Sabin scale" determined by Sabin scale assessment can be used as indicators. In this case, specifically, "hair growth," which is a preferred aspect of this aspect, can be determined by using "hair density ( / cm 2 ") and "Sabin scale." It corresponds to a case where one or more selected from the group consisting of "hair density ( / cm 2 )" and "Sabin scale" are preferred, and it is more preferable when more of them are preferred. 2 The larger the "Sabin scale," the more preferable it is, and the smaller the sum of positive ranks relative to the sum of negative ranks, the more preferable it is.
[0051] "Hair growth," which is a preferred embodiment of this embodiment, can be determined based on an index measured (or determined) by a measurement method (or determination method) commonly used in the art. For example, "hair density ( / cm)" measured by Trichoscan 2 ")" and the "Sabin scale" determined by the Sabin scale assessment can be used as indicators. In this case, specifically, "hair growth," which is a preferred aspect of this aspect, can be determined by the "hair density ( / cm 2 ") and "Sabin scale." It corresponds to a case where one or more selected from the group consisting of "hair density ( / cm 2 )" and "Sabin scale" are preferred, and it is more preferable when more of them are preferred. 2 The larger the "Sabin scale," the more preferable it is, and the smaller the sum of positive ranks relative to the sum of negative ranks, the more preferable it is.
[0052] The effective intake of the composition according to this embodiment may be determined as appropriate based on a person's age, body weight, hair condition, hair symptoms, intake route, intake schedule, formulation, etc., but is not particularly limited as long as hair is improved by ingestion of the composition according to this embodiment. The effective intake of the composition according to this embodiment may be, for example, 1 mg or more, 5 mg or more, 10 mg or more, 15 mg or more, 20 mg or more, etc., per day as the total amount of urolithins, or 500 mg or less, 250 mg or less, 200 mg or less, 150 mg or less, 100 mg or less, 50 mg or less, 30 mg or less, 20 mg or less, etc., or a compatible combination thereof. Specifically, the effective intake may be 1 mg or more and 500 mg or less, 5 mg or more and 250 mg or less, 10 mg or more and 200 mg or less, 15 mg or more and 150 mg or more, 20 mg or more and 100 mg or more, 20 mg or more and 50 mg or less, 20 mg or more and 30 mg or less, 10 mg or more and 20 mg or less, etc.
[0053] The effective intake amount of the food or beverage according to this embodiment may be appropriately determined based on a person's age, body weight, hair condition, hair symptoms, intake route, intake schedule, formulation, etc., but is not particularly limited as long as hair is improved by ingestion of the food or beverage according to this embodiment. The effective intake amount of the food or beverage according to this embodiment may be, for example, 1 mg or more, 5 mg or more, 10 mg or more, 15 mg or more, 20 mg or more, etc., per day as the total amount of urolithins, or 500 mg or less, 250 mg or less, 200 mg or less, 150 mg or less, 100 mg or less, 50 mg or less, 30 mg or less, 20 mg or less, etc., or a compatible combination thereof. Specifically, the effective intake amount is 1 mg or more and 500 mg or less, 5 mg or more and 250 mg or less, 10 mg or more and 200 mg or less, 15 mg or more and 150 mg or more, 20 mg or more and 100 mg or more, 20 mg or more and 50 mg or less, 20 mg or more and 30 mg or less, 10 mg or more and 20 mg or less, etc.
[0054] When urolithins are used as ingredients in foods and beverages for the above-mentioned uses, the foods and beverages may state the respective uses, or may state uses that are associated with the respective uses.
[0055] The present disclosure can provide, for example, the following aspects: Use of urolithins for producing a composition for improving skin; Use of urolithins for improving skin; Use of a composition containing urolithins for improving skin; A method for improving skin, comprising administering an effective amount of urolithins to a subject in need of skin improvement; A method for improving skin, comprising administering an effective amount of a composition containing urolithins to a subject in need of skin improvement.
[0056] Use of urolithins for producing a hair improvement composition. Use of urolithins for improving hair. Use of a composition containing urolithins for improving hair. A method for improving hair, comprising administering an effective amount of urolithins to a subject in need of improvement. A method for improving hair, comprising administering an effective amount of a composition containing urolithins to a subject in need of improvement.
[0057] The following examples are provided, but none of the examples should be construed as limiting.
[0058] Example 1 The ingredients in Table 1 were formulated into No. 2 HMPC hard capsules.
[0059] Example 2 Thirty healthy Japanese men and women aged 40 years or older were used as subjects, and divided into three groups of 10 subjects each (Group A, Group B, Group C) for a study (open-label, randomized, single-dose, parallel-group comparison). Subjects took hard capsules to achieve the following urolithin A intake amounts: Group A: 1 capsule (10 mg of urolithin A) / day; Group B: 5 capsules (50 mg of urolithin A) / day; Group C: 25 capsules (250 mg of urolithin A) / day. Blood samples were taken before and 0.5, 1, 2, 3, 6, 12, 24, and 48 hours after intake, and blood urolithin A (including glucuronide conjugates) concentrations were measured by HPLC under the following conditions. From the measurement results, the maximum blood concentration (C max ), time to reach maximum blood concentration (t max ), the area under the plasma concentration-time curve up to 24 hours (AUC 0-24時間The results are shown in Table 2.
[0060] [HPLC conditions] Column: COSMOSIL Packed Column 5C18-AR II (inner diameter 4.6 mm x length 150 mm, manufactured by Nacalai Tesque) Eluent: ultrapure water (MilliQ water) / acetonitrile / formic acid = 80:20:1 Column temperature: 40°C Flow rate: 1.0 mL / min Detector: PDA (photodiode array)
[0061]
[0062] Example 3 A study was conducted on 59 healthy Japanese women aged 18 years or older, divided into two groups of 29 and 30 subjects (open-label, randomized parallel group comparison). The subjects took the following urolithin A intake amounts for 12 weeks: Test Food Group 1 (29 subjects): 1 capsule (10 mg of urolithin A) / day Test Food Group 2 (30 subjects): 2 capsules (20 mg of urolithin A) / day The evaluation items listed in Table 3 were evaluated using each measuring device before and after 12 weeks of intake. Each measurement was performed according to the manual for each measuring device.
[0063] The evaluation items in the table correspond to the applications described in the corresponding lines. For example, "improvement of skin elasticity" corresponds to a favorable condition in which one or more evaluation items selected from the group consisting of "R7 value," "Skin Thickness (μm)," and "Low Echogenic Band (LEB) (μm)" are favorable, and it is more preferable if more evaluation items are favorable. Furthermore, "beautiful skin" corresponds to a favorable condition in which one or more evaluation items selected from the group consisting of "Gloss Value" and "Diffuse Scattering Correction" are favorable, and it is more preferable if more evaluation items are favorable. This also applies to other applications. Specifically, the closer the R7 value is to 1.00, the more preferable it is; the larger the Skin Thickness (μm), the smaller the Low Echogenic Band (LEB) (μm), the more preferable it is; the larger the Gloss Value, the more preferable it is; the larger the Diffuse Scattering Correction, the more preferable it is; the smaller the melanin value, the more preferable it is; the smaller the erythema value, the more preferable it is; the smaller the sum of the positive ranks relative to the sum of the negative ranks for the wrinkle grade, the more preferable it is; and the hair density ( / cm 2 ) is more preferable, and the Sabin scale is more preferable when the sum of positive ranks is smaller than the sum of negative ranks.
[0064]
[0065] (Result 1) In test food group 1, the evaluation items R7 value, Skin Thickness (μm), Low Echogenic Band (LEB) (μm), Gloss Value, Diffuse Scattering Correction, Melanin value, Erythema value, Hair density ( / cm 2 The results of the t-test (p value) were obtained by testing the data before and after 12 weeks of intake.
[0066]
[0067] (Result 2) The results of the wrinkle grade and Sabin scale evaluation items for test food group 1 are shown in the table below (n=29). The t-test results (p-values) were obtained by testing before intake and after 12 weeks of intake.
[0068]
[0069]
[0070]
[0071] (Result 3) In test food group 2, the evaluation items R7 value, Skin Thickness (μm), Low Echogenic Band (LEB) (μm), Gloss Value, Diffuse Scattering Correction, Melanin value, Erythema value, Hair density ( / cm 2 The results of the t-test (p value) were obtained by testing the data before and after 12 weeks of intake.
[0072]
[0073] (Result 4) The results of the wrinkle grade and Sabin scale evaluation items for test food group 2 are shown in the table below (n=30). The t-test results (p-values) were obtained by testing before intake and after 12 weeks of intake.
[0074]
[0075]
[0076]
Claims
1. A skin improving composition containing urolithins.
2. The composition according to claim 1, wherein the skin improvement is one or more selected from the group consisting of improvement of skin elasticity, beautiful skin, improvement of skin luster, whitening, improvement of skin thickness, improvement of skin firmness, and improvement of wrinkles.
3. The composition according to claim 1 or 2, wherein the total daily intake amount of the urolithins is 1 mg or more and 250 mg or less.
4. The composition described in claim 1 or 2, which is ingested so that the maximum blood concentration of urolithins is 0.1 μM or more and 3.3 μM or less.
5. A hair improving composition containing urolithins.
6. The composition according to claim 5, wherein the hair improvement is one or more selected from the group consisting of hair growth and hair regrowth.
7. The composition described in claim 5 or 6, wherein the total daily intake amount of the urolithins is 1 mg or more and 250 mg or less.
8. The composition described in claim 5 or 6, which is ingested so that the maximum blood concentration of urolithins is 0.1 μM or more and 3.3 μM or less.
Citation Information
Patent Citations
Hair tonics containing urolithins, and 5α-reductase activity inhibitors containing urolithins
JP2016216443A
Photoaging inhibitor comprising urolithin
JP2017007951A
Anti-wrinkle agent, collagen production promoter, MMP-1 production inhibitor, and elastase activity inhibitor that contain urolithin
JP2017031108A
Sirtuin 6 activator
WO2022114152A1
Composition for enhancing SIRT3 gene expression
WO2023228994A1