Composition and method
By adjusting the pH to 5.2 or less, the composition containing polyphenols and iron compounds prevents color changes, enabling their use in oral and external formulations.
Patent Information
- Application Number
- JP2024084936
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- Filing Date
- 2024-05-24
- Publication Date
- 2025-12-05
AI Technical Summary
Compositions containing polyphenols and iron compounds often experience changes in appearance color over time due to coordination between the two components, which is undesirable for oral and external compositions.
Adjusting the pH of the composition to 5.2 or less suppresses the change in appearance color by inhibiting the coordination between polyphenols and iron compounds.
The method effectively prevents color changes in compositions containing polyphenols and iron compounds, allowing their use in oral and external applications without discoloration.
Smart Images

Figure 2025177819000001_ABST
Abstract
Description
[Technical Field]
[0001] The present invention relates to a composition containing a polyphenol and an iron compound and having a pH of 5.2 or less, a method for using the composition, and a method for suppressing a change in the appearance color of a composition containing a polyphenol and an iron compound.The composition is preferably used as an oral composition such as a supplement or as an external composition such as a cosmetic. [Background technology]
[0002] BACKGROUND ART In oral compositions such as supplements and external compositions such as cosmetics, various components are blended into the compositions to achieve desired effects.
[0003] As an example of a composition, Patent Document 1 discloses a polyphenol preparation having excellent storage stability, which is characterized by comprising at least one type of polyphenol, at least one type of cyclodextrin, and one or more types of antioxidants dissolved in purified water at predetermined concentrations. [Prior art documents] [Patent documents]
[0004] [Patent Document 1] Japanese Patent Application Laid-Open No. 2010-168318 Summary of the Invention [Problem to be solved by the invention]
[0005] As shown in Patent Document 1, polyphenols are sometimes used as components incorporated into compositions. Polyphenols have been reported to have antioxidant functions, such as suppressing the generation of active oxygen and removing active oxygen. To achieve these functions, polyphenols are used in various compositions, such as oral compositions and topical compositions.
[0006] On the other hand, iron compounds may be used as another component incorporated into compositions. Iron compounds contain iron, a mineral, and are therefore sometimes incorporated into oral compositions for the purpose of iron supplementation. Iron compounds may also be incorporated into external compositions for the purpose of modifying or improving the condition of skin or hair.
[0007] In order to exert the functions of polyphenols and iron compounds in various compositions, polyphenols and iron compounds are sometimes combined and blended. However, in compositions blending polyphenols and iron compounds, the iron compounds may coordinate with the polyphenols in the composition, resulting in changes in the external color, such as blackening. Furthermore, although no changes in the external color of the composition are observed immediately after production, blackening may occur over time.
[0008] When a composition is intended for oral administration or topical administration, it is sometimes designed to have a subdued black appearance. In such cases, it is necessary to suppress the change in appearance color of the polyphenols and iron compounds in order to improve the quality of the composition.
[0009] In view of the above circumstances, an object of the present invention is to suppress changes in the appearance color of a composition containing a polyphenol and an iron compound. Another object of the present invention is to provide a method for using a composition containing a polyphenol and an iron compound, which has been suppressed from causing a change in appearance color, as an oral composition or an external composition. A further object of the present invention is to provide a method for suppressing a change in the external color of a composition containing a polyphenol and an iron compound. [Means for solving the problem]
[0010] The present inventors have conducted extensive research and have found that, in a composition containing polyphenols and an iron compound, the change in appearance color caused by the polyphenols and the iron compound can be suppressed by adjusting the pH to 5.2 or less. Furthermore, the present inventors have come up with a new idea for using the composition as an oral composition or an external composition.
[0011] The present invention includes the following inventions [1] to [9].
[0012] The composition [1] contains polyphenols and iron compounds and has a pH of 5.2 or less.
[0013] The composition [2] is the composition [1], which has a pH of less than 4.9.
[0014] The composition [3] is the composition [1] or [2], in which the polyphenol is a polyphenol having one or more 3,4-dihydroxyphenyl groups, and an amino acid is further added.
[0015] The composition [4] is any one of the compositions [1] to [3], which contains an amino acid other than a basic amino acid.
[0016] The composition [5] is any one of the compositions [1] to [4], in which a polyphenol having a molecular weight of 5000 or less is blended as the polyphenol.
[0017] The composition [6] is any one of the compositions [1] to [5] and is in a liquid or solid form.
[0018] The composition [7] is any one of the compositions [1] to [6], and is an oral composition or an external composition.
[0019] The method [8] is a method in which any of the compositions [1] to [7] is used as an oral composition or an external composition.
[0020] The method [9] is a method for suppressing a change in the appearance color of a composition containing a polyphenol and an iron compound, characterized by adjusting the pH to 5.2 or less. [Effects of the Invention]
[0021] According to the composition of the present invention, in a composition containing a polyphenol and an iron compound, changes in the appearance color can be suppressed. According to the method of the present invention, a method can be provided in which the composition of the present invention is used as an oral composition or an external composition. According to another method of the present invention, a method for suppressing changes in the appearance color of a composition containing a polyphenol and an iron compound can be provided. [Brief explanation of the drawings]
[0022] [Figure 1] Photographs of the appearance of the compositions of Examples 1a to 9a, Examples 1b to 3b, and Comparative Examples 1 to 4. [Figure 2] Photographs of the appearance of the compositions of Example 1a, Examples 10a to 16a, Example 1b, Examples 10b to 16b, Comparative Example 1, and Comparative Examples 5 to 11. [Figure 3] Photographs of the appearance of the compositions of Example 2a, Examples 17a to 23a, Example 2b, Examples 17b to 23b, Comparative Example 2, and Comparative Examples 12 to 18. [Figure 4] Photographs of the appearance of the compositions of Example 3a, Examples 24a to 28a, Example 3b, Examples 24b to 28b, Comparative Example 3, and Comparative Examples 19 to 23. DETAILED DESCRIPTION OF THE INVENTION
[0023] The present invention will be described below based on an embodiment of the present invention (hereinafter referred to as "the present embodiment").
[0024] First Embodiment The composition of this embodiment is a composition containing a polyphenol and an iron compound and having a pH of 5.2 or less (hereinafter, this composition will be referred to as the "composition of the first embodiment").
[0025] In a composition containing a polyphenol and an iron compound, as described above, the iron compound coordinates with the polyphenol, causing a change in the external color, such as blackening.
[0026] However, even when the composition of the first embodiment contains polyphenols and iron compounds, the change in appearance color caused by the polyphenols and iron compounds can be suppressed by adjusting the pH of the composition to 5.2 or less.
[0027] The "change in appearance color" in the composition of the first embodiment includes the following (1-1). (1-1) In a composition containing a polyphenol and an iron compound, the appearance color of the composition changes over time to a color including black (blackening due to coordination of the iron compound with the polyphenol).
[0028] [Polyphenols] The composition of the first embodiment contains one or more polyphenols.
[0029] Examples of polyphenols include polyphenols having two or more 4-hydroxyphenyl groups, polyphenols having one or more 3,4-dihydroxyphenyl groups, and polyphenols having one or more 3,4,5-trihydroxyphenyl groups.
[0030] The composition of the first embodiment may contain one or more polyphenols selected from polyphenols having two or more 4-hydroxyphenyl groups, polyphenols having one or more 3,4-dihydroxyphenyl groups, and polyphenols having one or more 3,4,5-trihydroxyphenyl groups.
[0031] The polyphenol having two or more 4-hydroxyphenyl groups, the polyphenol having one or more 3,4-dihydroxyphenyl groups, or the polyphenol having one or more 3,4,5-trihydroxyphenyl groups in the composition of the first embodiment includes those having only a 4-hydroxyphenyl group, those having only a 3,4-dihydroxyphenyl group, those having only a 3,4,5-trihydroxyphenyl group, those having a 4-hydroxyphenyl group and a 3,4-dihydroxyphenyl group, those having a 4-hydroxyphenyl group and a 3,4,5-trihydroxyphenyl group, those having a 3,4-dihydroxyphenyl group and a 3,4,5-trihydroxyphenyl group, and those having a 4-hydroxyphenyl group, a 3,4-dihydroxyphenyl group and a 3,4,5-trihydroxyphenyl group.
[0032] The polyphenols having two or more 4-hydroxyphenyl groups, one or more 3,4-dihydroxyphenyl groups, or one or more 3,4,5-trihydroxyphenyl groups are known as known polyphenols that belong to, for example, flavonoids (flavones, flavones, flavonols, etc.) and hydroxy derivatives of cinnamic acid (hydroxycinnamic acid derivatives, etc.), and are contained in plant extracts.
[0033] [Polyphenols having two or more 4-hydroxyphenyl groups] An example of a polyphenol having two or more 4-hydroxyphenyl groups in the composition of the first embodiment is tiliroside.
[0034] The composition of the first embodiment may contain tiliroside as a single component or a plant extract containing tiliroside, such as strawberry seed extract.
[0035] [Polyphenols having one or more 3,4-dihydroxyphenyl groups] The polyphenol having one or more 3,4-dihydroxyphenyl groups in the composition of the first embodiment may be a polyphenol having one 3,4-dihydroxyphenyl group or a polyphenol having two or more 3,4-dihydroxyphenyl groups.
[0036] Examples of the polyphenols having one 3,4-dihydroxyphenyl group include luteolin, catechin, quercetin, caffeoyl glucose, quercitrin, and rutin.
[0037] The composition of the first embodiment may contain any single component of luteolin, catechin, quercetin, caffeoyl glucose, quercitrin, or rutin, or may contain a plant extract containing any of these. Examples of plant extracts containing luteonin include perilla seed extract, chrysanthemum flower extract, and artichoke extract. Examples of plant extracts containing catechin include tea leaf extract. Examples of plant extracts containing quercetin include onion root extract. Examples of plant extracts containing caffeoyl glucose include cherry blossom extract. Examples of plant extracts containing quercitrin include kiwi seed extract. Examples of plant extracts containing rutin include buckwheat leaf extract.
[0038] Examples of the polyphenols having two or more 3,4-dihydroxyphenyl groups include rosmarinic acid, butterbur acid, chicoric acid, and echinacoside.
[0039] The composition of the first embodiment may contain any single component of rosmarinic acid, butterbur acid, chicoric acid, or echinacoside, or a plant extract containing any of these. Examples of plant extracts containing rosmarinic acid include rosemary leaf extract. Examples of plant extracts containing butterbur include butterbur leaf / stem extract. Examples of plant extracts containing chicoric acid include Echinacea purpurea extract. Examples of plant extracts containing echinacoside include Citrus tuberosa root extract.
[0040] [Polyphenols having one or more 3,4,5-trihydroxyphenyl groups] The polyphenol having one or more 3,4,5-trihydroxyphenyl groups in the composition of the first embodiment may be a polyphenol having one 3,4,5-trihydroxyphenyl group or a polyphenol having two or more 3,4,5-trihydroxyphenyl groups.
[0041] Examples of the polyphenol having one 3,4,5-trihydroxyphenyl group include gallic acid and delphinidin-3,5-glucoside.
[0042] The composition of the first embodiment may contain either gallic acid or delphinidin-3,5-glucoside as a single component, or a plant extract containing either of these. Examples of plant extracts containing gallic acid include evening primrose seed extract. Examples of plant extracts containing delphinidin-3,5-glucoside include Aristotelia chilensis fruit extract.
[0043] [Polyphenols having two or more 3,4,5-trihydroxyphenyl groups] Examples of the polyphenols having two or more 3,4,5-trihydroxyphenyl groups include GHG (1,2-di-galloyl-4,6-hexahydroxydiphenoyl-β-D-glucose) and hydrolyzable tannins (including tannic acid).
[0044] In the composition of the first embodiment, the GHG and hydrolyzable tannin (including tannic acid) may be a single component of GHG and hydrolyzable tannin (including tannic acid), or a plant extract containing GHG and hydrolyzable tannin (including tannic acid) may be used. Examples of the plant extract containing GHG include tea leaf extract. Examples of the plant extract containing hydrolyzable tannin (including tannic acid) include scutellaria extract.
[0045] The polyphenol to be blended in the composition of the first embodiment may be, for example, a polyphenol having a molecular weight of 5000 or less.
[0046] (Polyphenol content) The amount of polyphenols to be blended in the composition of the first embodiment is not particularly limited and may be set appropriately.
[0047] (Amount of polyphenols in oral compositions) When the composition of the first embodiment is intended for oral administration, the amount of polyphenols in the composition may be, for example, 0.1 mg or more, in terms of the daily polyphenol intake for an adult. From the viewpoint of further enhancing the antioxidant effect, an amount of 1 mg or more is preferred, and an amount of 10 mg or more is more preferred.
[0048] When the composition of the first embodiment is intended for oral administration, the amount of polyphenols in the composition may be, for example, 10 g or less, as the daily polyphenol intake for an adult. From the viewpoint of preventing a decrease in iron absorption, an amount of 5 g or less is preferred, and an amount of 1 g or less is more preferred.
[0049] When the composition of the first embodiment is intended for oral administration, the range of the amount of polyphenols in the composition may be, for example, 0.1 mg to 10 g, in terms of the daily polyphenol intake for an adult. From the viewpoint of the amount of polyphenols mentioned above, the range of 1 mg to 5 g is preferred, and the range of 10 mg to 1 g is more preferred.
[0050] (Amount of polyphenols in the composition for external use) When the composition of the first embodiment is used as a topical composition, the amount of polyphenol in the composition is, for example, 0.001% by mass or more, but from the viewpoint of further enhancing the antioxidant effect, 0.005% by mass or more is preferable, and 0.01% by mass or more is more preferable.
[0051] When the composition of the first embodiment is used as a topical composition, the amount of polyphenol in the composition is, for example, 10% by mass or less, but from the viewpoint of suppressing the risk of discoloration of the composition over time due to the polyphenol itself, it is preferably 5% by mass or less, more preferably 3% by mass or less. Note that the above-mentioned "discoloration of the composition over time due to the polyphenol itself" does not mean a change in appearance color due to the combination of the polyphenol and the iron compound, but rather refers to discoloration over time due to the polyphenol itself in the composition containing the polyphenol.
[0052] When the composition of the first embodiment is used as a composition for external use, the range of the amount of polyphenol in the composition is, for example, 0.001% by mass or more and 10% by mass or less. However, from the viewpoints described above, the amount of polyphenol in the composition is preferably 0.005% by mass or more and 5% by mass or less, and more preferably 0.01% by mass or more and 3% by mass or less.
[0053] [Iron compounds] The composition of the first embodiment contains one or more iron compounds.
[0054] The iron compound may be either a divalent iron compound or a trivalent iron compound. The iron compound may also be an organic or inorganic acid salt of divalent iron, an organic or inorganic acid salt of trivalent iron, or a metal oxide containing iron.
[0055] Examples of the iron compounds include iron citrate, ammonium iron citrate, sodium ferrous citrate, sodium iron succinate citrate, iron succinate, ferrous fumarate, ferrous gluconate, iron lactate, ammonium / iron pentetic acid, diammonium / iron pentetic acid, iron tetracarboxyphthalocyanine, iron ferritin, iron lactoferrin, iron dextran, Heme iron, chlorophyllin / iron complex, iron chlorophyllin, sodium iron chlorophyllin, sulfate / citric acid / hydroxide (Na / Al / iron), sulfate / oxalic acid / hydroxide (Na / Al / iron), sulfate / tartrate / hydroxide (Na / Al / iron), iron phosphate, ferrous pyrophosphate, ferric pyrophosphate, ferric chloride, ferric chloride, ammonium iron chloride, ferrous hydroxide, ferric hydroxide, ferrous sulfate, ferric sulfate, ammonium iron sulfate, iron fluoride, iron fluorosilicate, aluminum / iron silicate, aluminum / iron / calcium / magnesium / zirconium silicate, aluminum / zinc / iron oxide, iron / titanium oxide, iron oxide, and synthetic iron phlogopite.
[0056] (Iron Compounds for Oral Compositions) When the composition of the first embodiment is used as an oral composition, the iron compound may be, for example, one that can be used as a food additive, such as one or more selected from ferric chloride, sodium ferrous citrate, iron citrate, ammonium ferrous citrate, ferrous gluconate, sodium iron chlorophyllin, iron lactate, ferric pyrophosphate, potassium hexacyanoferrate(II), sodium hexacyanoferrate(II), heme iron, ferrous sulfate, ferrous oxide, and iron.
[0057] (Iron compounds when used in external compositions) When the composition of the first embodiment is used as a composition for external use, the iron compound to be used may be, for example, one that can be used in external cosmetics.
[0058] (Iron compound content) The amount of the iron compound blended in the composition of the first embodiment is not particularly limited and may be set appropriately.
[0059] (Amount of iron compound in oral composition) When the composition of the first embodiment is used as an oral composition, the amount of iron compound in the composition may be, for example, an amount that results in an iron compound intake of 1 mg or more per day for an adult. From the viewpoint of increasing iron intake, an amount of 1.5 mg or more is preferred, and an amount of 2 mg or more is more preferred.
[0060] When the composition of the first embodiment is used as an oral composition, the amount of iron compound in the composition may be, for example, an amount that results in an adult's daily intake of iron compound of 30 mg or less. From the viewpoint of preventing excessive iron intake, an amount that results in ...
[0061] When the composition of the first embodiment is an oral composition, the amount of iron compound in the composition may be, for example, in the range of 1 mg to 30 mg, in terms of the daily intake of iron compound for an adult. From the viewpoint of the amount of iron compound mentioned above, the amount is preferably in the range of 1.5 mg to 20 mg, and more preferably in the range of 2 mg to 15 mg.
[0062] (Amount of iron compound in the case of a topical composition) When the composition of the first embodiment is used as a topical composition, the amount of iron compound in the composition is, for example, 0.001% by mass or more, but from the viewpoint of better exerting the function of modifying and improving the condition of skin or hair, 0.005% by mass or more is preferable, and 0.01% by mass or more is more preferable.
[0063] When the composition of the first embodiment is used as a topical composition, the amount of iron compound in the composition is, for example, 1% by mass or less, but from the viewpoint of improving the feel of the skin or hair, 0.5% by mass or less is preferable, and 0.1% by mass or less is more preferable.
[0064] When the composition of the first embodiment is used as a topical composition, the range of the amount of iron compound in the composition is, for example, 0.001% by mass or more and 1% by mass or less. However, from the viewpoints mentioned above, the amount of iron compound in the composition is preferably 0.005% by mass or more and 0.5% by mass or less, and more preferably 0.01% by mass or more and 0.1% by mass or less.
[0065] (Polyphenol / iron compound mass ratio) In the composition of the first embodiment, the mass ratio of the amount of polyphenol to the amount of iron compound (hereinafter, sometimes referred to as "mass ratio of polyphenol / iron compound") may be set appropriately.
[0066] The composition of the first embodiment has a mass ratio of polyphenol / iron compound of, for example, 0.1 or more, but from the viewpoint of further suppressing changes in appearance color due to polyphenol and iron compound, it is preferably 0.5 or more, and more preferably 1 or more.
[0067] In the composition of the first embodiment, the mass ratio of polyphenol / iron compound may be, for example, 10,000 or less, 5,000 or less, or 1,000 or less.
[0068] In the composition of the first embodiment, the range of the polyphenol / iron compound mass ratio is, for example, 0.1 or more and 10,000 or less, but may also be 0.5 or more and 5,000 or less, or 1 or more and 1,000 or less.
[0069] (Total amount of polyphenols and iron compounds) The total amount of polyphenol and iron compound in the composition of the first embodiment may be set as appropriate, and is, for example, from 0.01% by mass to 50% by mass.
[0070] (optional ingredient) The composition of the first embodiment may contain ingredients other than polyphenols and iron compounds. The types and amounts of ingredients other than polyphenols and iron compounds can be appropriately determined depending on the formulation of the composition. Examples of ingredients other than polyphenols and iron compounds include surfactants, higher alcohols, lower alcohols, polyhydric alcohols, sugars, oily ingredients, synthetic polymer compounds, semi-synthetic polymer compounds, natural polymer compounds, proteins, animal and plant extracts, microbial-derived substances, inorganic compounds, fragrances, preservatives, UV absorbers, acids, alkalis, and pigments.
[0071] (acid) The composition of the first embodiment preferably contains one or more acids to prevent the pH of the composition from exceeding 5.2 over time. Examples of the acids that can be used include organic acids (citric acid, lactic acid, glycolic acid, malic acid, succinic acid, etc.) and inorganic acids (phosphoric acid, etc.).
[0072] (Amount of Acid to be Added When Forming Oral Composition) When the composition of the first embodiment is used as an oral composition, the amount of acid in the composition may be set to an amount that results in a pH of 5.2 or less depending on the other ingredients, for example, 0.01% by mass or more and 30% by mass or less.
[0073] (Amount of Acid in the Composition for External Use) When the composition of the first embodiment is used as a topical composition, the amount of acid in the composition may be set to an amount that results in a pH of 5.2 or less depending on the other ingredients, for example, 0.01% by mass or more and 30% by mass or less.
[0074] (alkali) The composition of the first embodiment may contain one or more alkalis. The pH of the composition of the first embodiment can be adjusted by adding the alkali. Examples of the alkali that can be used include inorganic alkalis (potassium hydroxide, sodium hydroxide, phosphates (dipotassium monohydrogen phosphate, disodium monohydrogen phosphate, magnesium oxide, etc.), sodium tripolyphosphate, etc.) and organic alkalis (aminoethylpropanol, arginine, triethanolamine, potassium carbonate, sodium carbonate, sodium bicarbonate, salts, etc.).
[0075] (Amount of alkali to be added when preparing an oral composition) When the composition of the first embodiment is used as an oral composition such as a supplement, the amount of alkali in the composition may be set to an amount that will result in a pH of 5.2 or less depending on the other ingredients, for example, 0.01% by mass or more and 30% by mass or less.
[0076] (Amount of alkali to be added when preparing a composition for external use) When the composition of the first embodiment is used as a composition for external use such as a cosmetic, the amount of alkali in the composition may be set to an amount that will result in a pH of 5.2 or less depending on the other ingredients, and is, for example, 0.01% by mass or more and 30% by mass or less.
[0077] [pH] The pH of the composition of the first embodiment is 5.2 or less.
[0078] In this specification, the pH of a composition is a value measured with a known pH meter for a composition at 25° C. If the composition is solid or contains a relatively small amount of water, making it difficult to measure the pH of the composition itself, the pH value measured for a dilution obtained by diluting the composition 20 times with purified water is used.
[0079] For example, when the composition of the first embodiment is a solid composition such as a tablet or powder, the pH can be measured by the following procedure: 19 parts by mass of purified water is added to 1 part by mass of the solid composition to dissolve it, and a 20-fold diluted product is obtained. The pH of the diluted product is measured at 25°C using a known pH meter.
[0080] In order to further suppress the suppression of blackening caused by polyphenols and iron compounds, the pH of the composition of the first embodiment is preferably less than 4.9, more preferably 4.8 or less, even more preferably less than 4.5, even more preferably 4.3 or less, and particularly preferably 4.2 or less. The pH of the composition of the first embodiment is, for example, 2.0 or higher, but is preferably 3.0 or higher from the viewpoint of reducing the sourness when used as an oral composition or reducing the risk of skin irritation when used as an external composition.
[0081] The pH range of the composition of the first embodiment is, for example, 2.0 or more and 5.2 or less, but from the above-mentioned viewpoint, it is preferably 3.0 or more and less than 4.9, more preferably 3.0 or more and less than 4.8, even more preferably 3.0 or more and less than 4.5, even more preferably 3.0 or more and less than 4.3, and particularly preferably 3.0 or more and less than 4.2.
[0082] [Dosage form] The composition of the first embodiment may be, for example, a liquid composition or a solid composition. Note that a liquid composition is one that has fluidity when left standing at 25°C, and a solid composition is one that does not have fluidity when left standing at 25°C.
[0083] Examples of the liquid composition include compositions in liquid, gel, and cream forms. Examples of solid compositions include compositions in the form of powder, granules, spheres, discs, and pills.
[0084] [Application] The composition of the first embodiment is used, for example, as an oral composition such as a supplement, or as an external composition such as a cosmetic.
[0085] [Oral Composition] The composition of the first embodiment may be, for example, an oral composition. The oral composition may be used, for example, as a pharmaceutical product, a quasi-drug, or a food (including general foods, foods with nutrient function claims, foods with functional claims, foods for specified health uses, and supplements).
[0086] When the composition of the first embodiment is used as an oral composition, it may be in the form of a food product, such as a supplement, dairy product, beverage, frozen dessert, ice cream, confectionery, seasoning, cream, jelly, jam, syrup, fish paste product, processed meat product, retort food, or frozen food.
[0087] The composition of the first embodiment may be used as a supplement for supplying polyphenols and iron, for example.
[0088] When the composition of the first embodiment is an oral composition, its dosage form may be, for example, tablets, granules, fine granules, fine granules, powders, capsules, soft capsules, pills, liquids, syrups, beverages, jellies, syrups, dry syrups, tablets, chewable tablets, troches, effervescent tablets, drops, suspensions, or orally disintegrating tablets.
[0089] [External composition] The composition of the first embodiment may be, for example, a composition for external use. In this specification, the term "composition for external use" refers to a composition for external use that is applied to an external part of the human body (hair, skin (including the scalp), etc.) by a method such as coating or application.
[0090] When the composition of the first embodiment is used as a composition for external use, it may be, for example, a cosmetic (a composition for treating the human body for the purposes of beautifying, cleansing, protecting, or deodorizing.) The cosmetic may be classified as a drug, a quasi-drug, or a cosmetic.
[0091] Examples of cosmetics include hair cosmetics, scalp cosmetics, and skin cosmetics.
[0092] (Hair cosmetics) The composition of the first embodiment may be used as, for example, a hair cosmetic. Examples of hair cosmetic include hair care cosmetic (e.g., hair treatment, hair treatment with styling function, one component of a multi-agent hair treatment, hair treatment for pre-treatment of perm, hair treatment for post-treatment of perm, hair treatment for pre-treatment of hair coloring, hair treatment for post-treatment of hair coloring, hair treatment for pre-treatment of bleaching, hair treatment for post-treatment of bleaching, etc.), hair styling cosmetic (e.g., hair styling agent), hair coloring cosmetic (e.g., temporary hair dye, semi-permanent hair dye, permanent hair dye (non-oxidative hair dye, oxidative hair dye, etc.), bleach, bleaching agent), permanent wave cosmetic, straight perm cosmetic (e.g., hair straightener, straightener, relaxer, etc.), hair care or hair growth cosmetic (e.g., hair growth agent, hair growth agent, etc.), etc.). The hair treatment may be a leave-in hair treatment or a rinse-off hair treatment.
[0093] (scalp cosmetics) The composition of the first embodiment may be used as, for example, a scalp cosmetic. Examples of scalp cosmetic products include scalp treatments (for example, leave-in scalp treatments, rinse-off scalp treatments, and one component of a multi-ingredient scalp treatment).
[0094] (Skin cosmetics other than scalp) The composition of the first embodiment may be used as, for example, a skin cosmetic for skin other than the scalp. Examples of skin cosmetic for skin other than the scalp include serums, emulsions, creams, packs, and masks.
[0095] The composition of the first embodiment may, for example, serve as both a hair cosmetic and a scalp cosmetic, or may serve as both a scalp cosmetic and a skin cosmetic other than the scalp, or may serve as both a hair cosmetic, a scalp cosmetic, and a skin cosmetic other than the scalp.
[0096] When the composition of the first embodiment is a cosmetic, its form may be selected as appropriate, and examples thereof include liquid, emulsion, cream, wax, solid, foam, and mist.
[0097] The product form of the composition of the first embodiment may be, for example, a product form that can be normally used as a cosmetic or quasi-drug.
[0098] [Manufacturing method] The composition of the first embodiment can be produced by a known method for producing oral compositions (such as foods) or topical compositions (such as cosmetics and quasi-drugs), depending on the dosage form. The composition of the first embodiment can be produced, for example, by mixing a polyphenol and an iron compound (other components such as a solvent or excipient may be added as necessary) and adjusting the pH to 5.2 or less.
[0099] The composition of the first embodiment may be produced, for example, by the following (Production Method 1) or (Production Method 2). (Production Method 1) A method of producing a composition having a pH of 5.2 or less by mixing a polyphenol, an iron compound, and an acid. (Production Method 2) A method for producing a composition by mixing a polyphenol with an iron compound and adjusting the pH of the composition to 5.2 or less after mixing.
[0100] [How to use] The method of using the composition of the first embodiment may be a conventional method for the intended use of the composition of the first embodiment.
[0101] When the composition of the first embodiment is used as an oral composition, for example, it may be taken or eaten as is, or may be taken or eaten after being dissolved or dispersed in a beverage such as water or hot water.
[0102] When the composition of the first embodiment is used as an external composition to treat at least one of hair, scalp, and skin other than the scalp, a known method for treating cosmetics for hair, scalp, and skin other than the scalp may be adopted.
[0103] Second Embodiment The composition of this embodiment is the composition of the first embodiment, which further contains a polyphenol having one or more 3,4-dihydroxyphenyl groups as the polyphenol, and further contains an amino acid or a salt thereof (hereinafter, this composition will be referred to as the "composition of the second embodiment"). That is, the composition of the second embodiment contains a polyphenol having one or more 3,4-dihydroxyphenyl groups, an iron compound, and an amino acid or a salt thereof, and has a pH of 5.2 or less.
[0104] The composition of the second embodiment contains a polyphenol having one or more 3,4-dihydroxyphenyl groups (hereinafter sometimes referred to as a "specific polyphenol") and an iron compound. By adjusting the pH of the composition to 5.2 or less, the change in appearance color caused by the polyphenols (including the specific polyphenols) and iron compounds described in the composition of the first embodiment can be suppressed.
[0105] In a composition containing a polyphenol (including a specific polyphenol) and an amino acid or a salt thereof, crosslinking between the polyphenol and the amino acid or the salt thereof can cause a change in appearance color, such as blackening, over time. Furthermore, this change in appearance color due to crosslinking is likely to occur more rapidly when iron compounds act as a catalyst.
[0106] However, even when the composition of the second embodiment contains a specific polyphenol, an iron compound, and an amino acid or its salt, the change in appearance color caused by the specific polyphenol and the amino acid or its salt catalyzed by the iron compound can be suppressed by setting the pH of the composition to 5.2 or less.
[0107] The "change in appearance color" in the composition of the second embodiment includes both of the following (1-2) and (2-1). (1-2) In a composition containing a specific polyphenol and an iron compound, the appearance color of the composition changes over time to a color including black (blackening due to coordination of the iron compound with the specific polyphenol). (2-1) In a composition containing a specific polyphenol, an iron compound, and an amino acid or a salt thereof, the color changes over time to a color that includes black (blackening due to cross-linking of the specific polyphenol with the amino acid or a salt thereof, catalyzed by the iron compound).
[0108] [Specific polyphenols (polyphenols having one or more 3,4-dihydroxyphenyl groups)] The composition of the second embodiment contains one or more specific polyphenols (polyphenols having one or more 3,4-dihydroxyphenyl groups).
[0109] As the specific polyphenol in the composition of the second embodiment, the same polyphenol having one or more 3,4-dihydroxyphenyl groups as described above in the composition of the first embodiment can be used.
[0110] The specific polyphenol to be blended in the composition of the second embodiment may have a molecular weight of 200 or more and 1500 or less, for example.
[0111] The amount of the specific polyphenol contained in the composition of the second embodiment is not particularly limited and may be set appropriately.
[0112] (Amount of specific polyphenols in oral compositions) When the composition of the second embodiment is intended for oral administration, the amount of specific polyphenol in the composition may be, for example, 0.1 mg or more, as the daily intake of specific polyphenol for an adult. From the viewpoint of further enhancing the antioxidant effect, an amount of 1 mg or more is preferred, and an amount of 10 mg or more is more preferred.
[0113] When the composition of the second embodiment is an oral composition, the amount of the specific polyphenol in the composition may be, for example, 10 g or less, as the daily intake of the specific polyphenol for an adult. From the viewpoint of suppressing the risk of discoloration of the composition over time due to the specific polyphenol itself, an amount of 5 g or less is preferred, and an amount of 1 g or less is more preferred. Note that the "discoloration of the composition over time due to the specific polyphenol itself" does not refer to a change in appearance color due to the combination of the specific polyphenol and the iron compound, but rather to discoloration over time due to the polyphenol itself in the composition containing the specific polyphenol.
[0114] When the composition of the second embodiment is intended for oral administration, the range of the amount of specific polyphenol contained in the composition may be, for example, a range of 0.1 mg to 10 g, in terms of the daily intake of specific polyphenol by an adult. From the viewpoint of the amount of polyphenol contained as described above, a range of 1 mg to 5 g is preferred, and a range of 10 mg to 1 g is more preferred.
[0115] (Amount of polyphenols in the composition for external use) When the composition of the second embodiment is used as a topical composition, the amount of the specific polyphenol in the composition is, for example, 0.001% by mass or more, but from the viewpoint of further enhancing the antioxidant effect, 0.005% by mass or more is preferable, and 0.01% by mass or more is more preferable.
[0116] When the composition of the second embodiment is used as a topical composition, the amount of the specific polyphenol in the composition is, for example, 10% by mass or less, but from the viewpoint of suppressing the risk of discoloration of the composition over time due to the specific polyphenol itself, 5% by mass or less is preferred, and 3% by mass or less is more preferred.
[0117] When the composition of the second embodiment is used as a topical composition, the range of the amount of the specific polyphenol in the composition is, for example, 0.001% by mass or more and 10% by mass or less. However, from the viewpoints mentioned above, the amount of the specific polyphenol in the composition is preferably 0.005% by mass or more and 5% by mass or less, and more preferably 0.01% by mass or more and 3% by mass or less.
[0118] [Iron compounds] The composition of the second embodiment contains one or more iron compounds. The types and amounts of the iron compounds contained in the composition of the second embodiment, including examples and preferred examples, are the same as those of the iron compounds in the composition of the first embodiment, and therefore will not be described here.
[0119] [Amino acid or its salt] The composition of the second embodiment contains one or more amino acids or salts thereof. The "amino acid" contained in the composition of the second embodiment means a compound having an amino group (-NH2) and a carboxyl group (-COOH) in the molecule. The amino acids in the composition of the second embodiment include "amino acids other than basic amino acids" in the composition of the third embodiment, which will be described later.
[0120] The amino acid or salt thereof to be incorporated into the composition of the second embodiment may be, for example, an amino acid or salt thereof selected from the amino acids represented by the following general formula (1) and salts thereof.
[0121] NH2-R 1 -COOH (1) [In the above general formula (1), R 1represents a group having a branched or linear chain or cyclic structure composed of 1 to 15 carbon atoms and an atom selected from hydrogen atoms, oxygen atoms, nitrogen atoms, and sulfur atoms.
[0122] In the above general formula (1), R 1 may have, for example, a hydroxyl group (-OH), a ketone group (-CO-), an aldehyde group (-CHO), a carboxyl group (-COO-), an amine group (-NH-), an amide group (-NHCO-), an acyl group (acetyl group, benzoyl group, etc.), or a thiol group (-SH).
[0123] The amino acid or salt thereof to be incorporated into the composition of the second embodiment may have an α-amino acid, β-amino acid, γ-amino acid, δ-amino acid, or ε-amino acid structure, for example.
[0124] The amino acid or a salt thereof to be incorporated into the composition of the second embodiment may have any of a D-, L- or DL-amino acid structure.
[0125] The amino acid to be blended in the composition of the second embodiment may have, for example, 1 to 15 carbon atoms.
[0126] The amino acid to be incorporated into the composition of the second embodiment may have a molecular weight of, for example, 300 or less.
[0127] Examples of amino acid salts include inorganic acid salts of amino acids (such as hydrochlorides, sulfates, and phosphates), organic acid salts of amino acids (such as acetates, propionates, succinates, glycolates, lactates, malates, tartrates, citrates, maleates, and fumarates), alkali metal salts of amino acids (such as sodium salts and potassium salts), alkaline earth metal salts of amino acids (such as calcium salts and magnesium salts), inorganic base salts of amino acids (such as ammonium salts), and organic base salts of amino acids (such as alkanolamine salts).
[0128] Examples of amino acids or salts thereof include glycine, alanine, leucine, isoleucine, valine, tyrosine, phenylalanine, tryptophan, serine, threonine, methionine, cysteine, glutamine, asparagine, glutamic acid, aspartic acid, lysine, arginine, histidine, ornithine, citrulline, theanine, β-aminobutyric acid, γ-aminobutyric acid, hydroxylysine, homoserine, cystine, argininosuccinic acid, tranexamic acid, lanthionine, 3-aminopropanoic acid, β-methyllanthionine, cystathionine, felinine, aminomalonic acid, glutathione, ε-aminocaproic acid, glycylglycine, and salts thereof.
[0129] The composition of the second embodiment may contain, as the amino acid or salt thereof, one or more selected from acidic amino acids or salts thereof, neutral amino acids or salts thereof, and basic amino acids or salts thereof.
[0130] Acidic amino acids include, for example, glutamic acid and aspartic acid. Examples of neutral amino acids include glycine, alanine, leucine, isoleucine, valine, tyrosine, phenylalanine, tryptophan, serine, threonine, methionine, cysteine, glutamine, asparagine, citrulline, theanine, β-aminobutyric acid, γ-aminobutyric acid, homoserine, cystine, tranexamic acid, lanthionine, 3-aminopropanoic acid, and ε-aminocaproic acid. Examples of basic amino acids include lysine, arginine, histidine, ornithine, and hydroxylysine.
[0131] In the composition of the second embodiment, the amino acid or salt thereof is preferably an acidic amino acid, a neutral amino acid, or a salt thereof, from the viewpoint of further suppressing blackening caused by polyphenols and amino acids or salts thereof catalyzed by iron compounds.
[0132] The amino acid or salt thereof to be incorporated into the composition of the second embodiment is more preferably one or more selected from glycine, alanine, leucine, isoleucine, valine, tyrosine, phenylalanine, tryptophan, serine, threonine, methionine, cysteine, glutamine, asparagine, glutamic acid, aspartic acid, lysine, arginine, histidine, and salts thereof.
[0133] (Amount of amino acid or its salt) The amount of the amino acid or salt thereof in the composition of the second embodiment is not particularly limited and may be set appropriately.
[0134] (Amount of amino acid or its salt when used as an oral composition) When the composition of the second embodiment is intended as an oral composition, the amount of amino acid or a salt thereof in the composition may be, for example, an amount that provides an adult with a daily intake of amino acid of 1 mg or more. From the viewpoint of increasing the intake of amino acid, an amount that provides ...
[0135] When the composition of the second embodiment is used as an oral composition, the amount of amino acid or a salt thereof in the composition may be, for example, 5 g or less as the daily intake of amino acid for an adult. From the viewpoint of preventing excessive intake of amino acid, an amount of 3 g or less is preferred, and an amount of 2 g or less is more preferred.
[0136] When the composition of the second embodiment is an oral composition, the range of the amount of amino acid or a salt thereof in the composition may be, for example, 1 mg to 5 g, in terms of the daily intake of amino acid for an adult. From the viewpoints described above regarding the amount of amino acid or a salt thereof, the range of the amount of amino acid is preferably 5 mg to 3 g, and more preferably 10 mg to 2 g.
[0137] (Amount of amino acid or its salt when used as a topical composition) When the composition of the second embodiment is used as a topical composition, the amount of amino acid or its salt in the composition is, for example, 0.01% by mass or more, but from the viewpoint of further enhancing the moisturizing effect on the skin or hair, 0.05% by mass or more is preferable, and 0.1% by mass or more is more preferable.
[0138] When the composition of the second embodiment is used as a topical composition, the amount of amino acid or its salt in the composition is, for example, 10% by mass or less, but from the viewpoint of improving the stability of the composition over time, 5% by mass or less is preferable, and 1% by mass or less is more preferable.
[0139] When the composition of the second embodiment is used as a composition for external use, the range of the amount of amino acid or its salt in the composition is, for example, 0.01% by mass or more and 10% by mass or less. However, from the viewpoints mentioned above, the amount of amino acid or its salt is preferably 0.05% by mass or more and 5% by mass or less, and more preferably 0.1% by mass or more and 1% by mass or less.
[0140] (mass ratio of specific polyphenols to iron compounds) In the composition of the second embodiment, the mass ratio of the blended amount of the specific polyphenol to the blended amount of the iron compound (hereinafter referred to as the "mass ratio of the specific polyphenol / iron compound") may be set appropriately.
[0141] In the composition of the second embodiment, the mass ratio of the specific polyphenol to the iron compound is, for example, 0.1 or more, but from the viewpoint of further suppressing changes in the appearance color due to the polyphenol and the iron compound, it is preferably 0.5 or more, and more preferably 1 or more.
[0142] In the composition of the second embodiment, the mass ratio of the specific polyphenol to the iron compound may be, for example, 10,000 or less, 5,000 or less, or 1,000 or less.
[0143] In the composition of the second embodiment, the range of the mass ratio of the specific polyphenol to the iron compound is, for example, 0.1 or more and 10,000 or less, but may also be 0.5 or more and 5,000 or less, or 1 or more and 1,000 or less.
[0144] (Total amount of specific polyphenols and iron compounds) The total amount of the specific polyphenol and the iron compound in the composition of the second embodiment may be set as appropriate, and is, for example, 0.1% by mass or more and 50% by mass or less.
[0145] (mass ratio of specific polyphenols + amino acids or their salts / iron compounds) In the composition of the second embodiment, the mass ratio of the total amount of the specific polyphenol and the amino acid or its salt to the amount of the iron compound (hereinafter referred to as the "mass ratio of specific polyphenol + amino acid or its salt / iron compound") may be set appropriately.
[0146] In the composition of the second embodiment, the mass ratio of specific polyphenol + amino acid or its salt / iron compound is, for example, 0.1 or more, but from the viewpoint of further suppressing the change in external color caused by the specific polyphenol and amino acid or its salt catalyzed by the iron compound, it is preferably 0.5 or more, and more preferably 1 or more.
[0147] In the composition of the second embodiment, the mass ratio of specific polyphenol+amino acid or salt thereof / iron compound may be, for example, 10,000 or less, 5,000 or less, or 1,000 or less.
[0148] In the composition of the second embodiment, the mass ratio of specific polyphenol+amino acid or its salt / iron compound is, for example, in the range of 0.1 to 10,000, but may also be 0.5 to 5,000, or 1 to 1,000.
[0149] (Total amount of specific polyphenols, amino acids or their salts, and iron compounds) The total amount of the specific polyphenol, amino acid or a salt thereof, and iron compound in the composition of the second embodiment may be set as appropriate, and is, for example, 0.1% by mass or more and 50% by mass or less.
[0150] (optional ingredient) The composition of the second embodiment may contain ingredients other than the specific polyphenol, iron compound, and amino acid or salt thereof. The types and amounts of the ingredients other than the specific polyphenol, iron compound, and amino acid or salt thereof can be appropriately determined depending on the dosage form, etc. The ingredients other than the specific polyphenol, iron compound, and amino acid or salt thereof may be the same as those of the composition of the first embodiment except for the polyphenol and iron compound, but excluding the amino acid or salt thereof.
[0151] (acid) The composition of the second embodiment preferably contains one or more acids from the viewpoint of preventing the pH of the composition from exceeding 5.2 over time. When an acid is contained in the composition of the second embodiment, the acid can be of the same type and in the same amount as the acid described above for the composition of the first embodiment.
[0152] (alkali) The composition of the second embodiment may contain one or more alkalis. When an alkali is contained in the composition of the second embodiment, the alkali may be of the same type and in the same amount as the alkali described above in the composition of the first embodiment.
[0153] [pH] The pH of the composition of the second embodiment is 5.2 or less, and may be measured in the same manner as the pH of the composition of the first embodiment.
[0154] The pH of the composition of the second embodiment is preferably less than 4.9, more preferably 4.8 or less, even more preferably less than 4.5, even more preferably 4.3 or less, and particularly preferably 4.2 or less, from the viewpoint of further suppressing blackening caused by polyphenols and amino acids or salts thereof catalyzed by iron compounds. The pH of the composition of the second embodiment is, for example, 2.0 or higher, but is preferably 3.0 or higher from the viewpoint of reducing the sourness when used as an oral composition or reducing the risk of skin irritation when used as an external composition.
[0155] The pH range of the composition of the second embodiment is, for example, 2.0 or more and 5.2 or less, but from the above-mentioned viewpoint, it is preferably 3.0 or more and less than 4.9, more preferably 3.0 or more and less than 4.8, even more preferably 3.0 or more and less than 4.5, even more preferably 3.0 or more and less than 4.3, and particularly preferably 3.0 or more and less than 4.2.
[0156] [Dosage form] The dosage form of the composition of the second embodiment may be the same as the dosage form described above for the composition of the first embodiment.
[0157] [Application] The composition of the second embodiment has the same uses as those described above for the composition of the first embodiment (oral composition, external composition).
[0158] [Manufacturing method] The composition of the second embodiment can be produced by a known method for oral compositions (such as foods) or topical compositions (such as cosmetics and quasi-drugs), depending on the dosage form. The composition of the second embodiment can be produced, for example, by mixing a specific polyphenol, an iron compound, and an amino acid or a salt thereof (other components such as a solvent or excipient may be added as necessary), and adjusting the pH to 5.2 or less.
[0159] The composition of the second embodiment may be produced, for example, by the following (Production Method 3) or (Production Method 4). (Production Method 3) A method for producing a composition having a pH of 5.2 or less by mixing a specific polyphenol, an iron compound, an amino acid or a salt thereof, and an acid. (Production Method 4) A method for producing a composition by mixing a specific polyphenol, an iron compound, and an amino acid or a salt thereof, and adjusting the pH of the composition to 5.2 or less after mixing.
[0160] [How to use] The composition of the second embodiment can be used in the same manner as described above for the composition of the first embodiment.
[0161] Third Embodiment The composition of this embodiment is the composition of the first embodiment further containing one or more amino acids selected from amino acids other than basic amino acids or salts thereof (hereinafter, this composition will be referred to as the "composition of the third embodiment"). That is, the composition of the third embodiment contains a polyphenol, an iron compound, and an amino acid other than basic amino acids or salts thereof, and has a pH of 5.2 or less. In the following description, the amino acid other than basic amino acids or salts thereof may be referred to as "specific amino acids, etc."
[0162] The composition of the third embodiment contains a polyphenol and an iron compound, and by adjusting the pH of the composition to 5.2 or less, the change in appearance color caused by the polyphenol and iron compound described in the composition of the first embodiment can be suppressed.
[0163] As described above in the composition of the second embodiment, in a composition containing a polyphenol and an amino acid or a salt thereof, crosslinking between the polyphenol and the amino acid or the salt thereof may cause a change in appearance color, such as blackening, over time. Furthermore, this change in appearance color due to crosslinking is likely to occur at an accelerated rate when the iron compound acts as a catalyst.
[0164] However, even when the composition of the third embodiment contains polyphenols, iron compounds, specific amino acids, etc., the change in appearance color caused by the polyphenols and specific amino acids, etc. catalyzed by the iron compounds can be suppressed by setting the pH of the composition to 5.2 or less.
[0165] The "change in appearance color" in the composition of the third embodiment includes both of the following (1-1) and (2-2). (1-1) In a composition containing a polyphenol and an iron compound, the appearance color of the composition changes over time to a color including black (blackening due to coordination of the iron compound with a specific polyphenol). (2-2) In a composition containing polyphenols, an iron compound, and a specific amino acid, etc., the color changes over time to a color including black (blackening due to cross-linking of polyphenols and the specific amino acid, etc., catalyzed by the iron compound).
[0166] [Polyphenols] The composition of the third embodiment contains one or more polyphenols. The types and amounts of polyphenols contained in the composition of the third embodiment, including exemplified and preferred ones, are the same as those in the composition of the first embodiment.
[0167] The polyphenol blended in the composition of the third embodiment may be the specific polyphenol (a polyphenol having one or more 3,4-dihydroxyphenyl groups) in the composition of the second embodiment described above.
[0168] [Iron compounds] The composition of the third embodiment contains one or more iron compounds. The iron compounds contained in the composition of the third embodiment are the same as those in the composition of the first embodiment, and therefore will not be described here.
[0169] (Polyphenol / iron compound mass ratio) In the composition of the third embodiment, the mass ratio of the amount of polyphenol to the amount of iron compound is the same as the mass ratio of polyphenol / iron compound in the composition of the first embodiment, and therefore will not be repeated.
[0170] (Total amount of polyphenols and iron compounds) In the composition of the third embodiment, the total amount of polyphenol and iron compound blended is the same as the total amount of polyphenol and iron compound blended in the composition of the first embodiment, and therefore will not be repeated here.
[0171] [Specific amino acids, etc. (amino acids other than basic amino acids or their salts)] The composition of the third embodiment contains one or more specific amino acids etc. (amino acids other than basic amino acids or salts thereof).
[0172] Here, "amino acids other than basic amino acids" refers to amino acids (compounds having an amino group (-NH2) and a carboxyl group (-COOH) in the molecule) excluding basic amino acids (amino acids having two or more amino groups (-NH2) and an isoelectric point (pI) of 7 or more). The isoelectric point (pI) can be measured by isoelectric focusing.
[0173] Examples of specific amino acids include inorganic acid salts (hydrochloride, sulfate, phosphate, etc.) of amino acids other than basic amino acids, organic acid salts (acetate, propionate, succinate, glycolate, lactate, malate, tartrate, citrate, maleate, fumarate, etc.), alkali metal salts (sodium salt, potassium salt, etc.), alkaline earth metal salts (calcium salt, magnesium salt, etc.), inorganic base salts (ammonium salt, etc.), and organic base salts (alkanolamine salt, etc.).
[0174] The specific amino acid may be selected from the following general formula (2) or (3).
[0175] NH2-CHR 2 -COOH (2) [In the above general formula (2), R 2 represents a branched or linear chain group composed of atoms selected from carbon atoms, hydrogen atoms, oxygen atoms, nitrogen atoms, and sulfur atoms, a hydrogen group, a phenyl group, a phenol group, or an indole group, provided that R 2 is a chain group, the chain group contains 1 to 15 carbon atoms. In addition, in the above general formula (2), those having two or more amino groups (-NH2) in the molecule and having an isoelectric point (pI) of 7 or more are excluded.
[0176] In the above general formula (2), R 2may have, for example, a hydroxyl group (-OH), a ketone group (-CO-), an aldehyde group (-CHO), a carboxyl group (-COO-), an amine group (-NH-), an amide group (-NHCO-), an acyl group (acetyl group, benzoyl group, etc.), or a thiol group (-SH).
[0177] NH2-(CH2) a -R 3 -(CH2) b -COOH (3) [In the above general formula (3), R 3 represents a group having a branched or straight chain structure or a cyclic structure composed of 1 to 15 carbon atoms and atoms selected from hydrogen atoms, oxygen atoms, nitrogen atoms, and sulfur atoms. In addition, a and b are integers of 0 or more, and the sum of a and b is 1 or more. However, in the above general formula (3), those having two or more amino groups (-NH2) in the molecule and having an isoelectric point (pI) of 7 or more are excluded.
[0178] In the above general formula (2), R 3 may have, for example, a hydroxyl group (-OH), a ketone group (-CO-), an aldehyde group (-CHO), a carboxyl group (-COO-), an amine group (-NH-), an amide group (-NHCO-), an acyl group (acetyl group, benzoyl group, etc.), or a thiol group (-SH).
[0179] The specific amino acids and the like to be incorporated into the composition of the third embodiment may have, for example, an α-amino acid, a β-amino acid, a γ-amino acid, a δ-amino acid, or an ε-amino acid structure.
[0180] The specific amino acid etc. to be blended in the composition of the third embodiment may have any of the D-, L- or DL-amino acid structures.
[0181] The specific amino acid etc. to be blended in the composition of the third embodiment may have, for example, 1 to 15 carbon atoms.
[0182] The specific amino acid etc. to be blended in the composition of the third embodiment may have a molecular weight of 300 or less, for example.
[0183] Examples of specific amino acids include glycine, alanine, leucine, isoleucine, valine, tyrosine, phenylalanine, tryptophan, serine, threonine, methionine, cysteine, glutamine, asparagine, glutamic acid, aspartic acid, citrulline, theanine, β-aminobutyric acid, γ-aminobutyric acid, homoserine, cystine, argininosuccinic acid, tranexamic acid, lanthionine, 3-aminopropanoic acid, β-methyllanthionine, cystathionine, felinine, aminomalonic acid, glutathione, ε-aminocaproic acid, glycylglycine, and salts thereof.
[0184] The specific amino acids and the like to be incorporated into the composition of the third embodiment are preferably one or more selected from glycine, alanine, leucine, isoleucine, valine, tyrosine, phenylalanine, tryptophan, serine, threonine, methionine, cysteine, glutamine, asparagine, glutamic acid, aspartic acid, and salts thereof.
[0185] (Amount of specific amino acids, etc.) The amount of the specific amino acid and the like blended in the composition of the third embodiment is not particularly limited and may be set appropriately.
[0186] (Amount of specific amino acids, etc. when used as an oral composition) When the composition of the third embodiment is used as an oral composition, the amount of the specific amino acid, etc. in the composition may be, for example, an amount that provides an adult with a daily intake of amino acids other than basic amino acids of 1 mg or more. From the viewpoint of increasing the intake of the specific amino acid, etc., an amount that provides 5 mg or more is preferred, and an amount that provides 10 mg or more is more preferred.
[0187] When the composition of the third embodiment is used as an oral composition, the amount of the specific amino acid, etc. in the composition may be, for example, an amount that results in an adult's daily intake of amino acids other than basic amino acids of 5 g or less. From the viewpoint of preventing excessive intake of amino acids, an amount that results in ...
[0188] When the composition of the third embodiment is an oral composition, the range of the amount of the specific amino acid, etc. in the composition may be, for example, a range of 1 mg to 5 g, in terms of the daily intake of amino acids other than basic amino acids for an adult. From the above-mentioned viewpoint of the amount of the specific amino acid, etc., a range of 5 mg to 3 g is preferred, and a range of 10 mg to 2 g is more preferred.
[0189] (Amount of amino acid or its salt when used as a topical composition) When the composition of the third embodiment is used as a topical composition, the amount of the specific amino acid, etc. in the composition is, for example, 0.01% by mass or more, but from the viewpoint of further enhancing the moisturizing effect on the skin or hair, 0.05% by mass or more is preferable, and 0.1% by mass or more is more preferable.
[0190] When the composition of the third embodiment is used as a topical composition, the amount of the specific amino acid, etc. in the composition is, for example, 10% by mass or less, but from the viewpoint of improving the stability of the composition over time, 5% by mass or less is preferable, and 1% by mass or less is more preferable.
[0191] When the composition of the third embodiment is used as a topical composition, the range of the amount of specific amino acids, etc. in the composition is, for example, 0.01% by mass or more and 10% by mass or less. However, from the viewpoints mentioned above, the amount of specific amino acids, etc. in the composition is preferably 0.05% by mass or more and 5% by mass or less, and more preferably 0.1% by mass or more and 1% by mass or less.
[0192] (mass ratio of polyphenols + specific amino acids etc. / iron compounds) In the composition of the third embodiment, the mass ratio of the total amount of polyphenols and specific amino acids, etc. to the amount of iron compounds (hereinafter referred to as the "mass ratio of polyphenols + specific amino acids, etc. / iron compounds") may be set appropriately.
[0193] In the composition of the third embodiment, the mass ratio of polyphenols + specific amino acids, etc. to iron compounds is, for example, 0.1 or more, but from the viewpoint of further suppressing changes in external color due to polyphenols and specific amino acids, etc. catalyzed by iron compounds, the mass ratio is preferably 0.5 or more, and more preferably 1 or more.
[0194] In the composition of the third embodiment, the mass ratio of polyphenol+specific amino acid etc. / iron compound may be, for example, 10,000 or less, 5,000 or less, or 1,000 or less.
[0195] In the composition of the third embodiment, the mass ratio of polyphenol+specific amino acid etc. / iron compound is, for example, in the range of 0.1 to 10,000, but may also be 0.5 to 5,000, or 1 to 1,000.
[0196] (Total amount of specific polyphenols, amino acids or their salts, and iron compounds) The total amount of the specific polyphenol, amino acid or a salt thereof, and iron compound in the composition of the third embodiment may be set as appropriate, and is, for example, 0.1% by mass or more and 50% by mass or less.
[0197] (optional ingredient) The composition of the third embodiment may contain ingredients other than polyphenols, iron compounds, specific amino acids, etc. The types and amounts of ingredients other than polyphenols, iron compounds, specific amino acids, etc. can be appropriately determined depending on the dosage form, etc. The ingredients other than salts of polyphenols, iron compounds, specific amino acids, etc. may be the same as those of the composition of the first embodiment except for the polyphenols and iron compounds described above, excluding the specific amino acids, etc.
[0198] (acid) The composition of the third embodiment preferably contains one or more acids from the viewpoint of preventing the pH of the composition from exceeding 5.2 over time. When an acid is contained in the composition of the third embodiment, the acid can be of the same type and in the same amount as the acid described above for the composition of the first embodiment.
[0199] (alkali) The composition of the third embodiment may contain one or more alkalis. When an alkali is contained in the composition of the third embodiment, the alkali may be of the same type and in the same amount as the alkali described above in the composition of the first embodiment.
[0200] [pH] The pH of the composition of the third embodiment is 5.2 or less, and can be measured in the same manner as the pH of the composition of the first embodiment.
[0201] The pH of the composition of the third embodiment is preferably less than 4.9, more preferably 4.8 or less, even more preferably less than 4.5, even more preferably 4.3 or less, and particularly preferably 4.2 or less, from the viewpoint of further suppressing blackening due to polyphenols and specific amino acids catalyzed by iron compounds. The pH of the composition of the third embodiment is, for example, 2.0 or higher, but is preferably 3.0 or higher from the viewpoint of reducing the sourness when used as an oral composition or reducing the risk of skin irritation when used as an external composition.
[0202] The pH range of the composition of the third embodiment is, for example, 2.0 or more and 5.2 or less, but from the above-mentioned viewpoint, it is preferably 3.0 or more and less than 4.9, more preferably 3.0 or more and less than 4.8, even more preferably 3.0 or more and less than 4.5, even more preferably 3.0 or more and less than 4.3, and particularly preferably 3.0 or more and less than 4.2.
[0203] [Dosage form] The dosage form of the composition of the third embodiment may be the same as the dosage form described above for the composition of the first embodiment.
[0204] [Application] The composition of the third embodiment has the same uses as those described above for the composition of the first embodiment (oral composition, external composition).
[0205] [Manufacturing method] The composition of the third embodiment can be produced by a known method for producing oral compositions (such as foods) or topical compositions (such as cosmetics and quasi-drugs), depending on the dosage form. The composition of the third embodiment can be produced, for example, by mixing polyphenols, iron compounds, specific amino acids, etc. (other components such as solvents and excipients may be added as necessary), and adjusting the pH to 5.2 or less.
[0206] The composition of the third embodiment may be produced, for example, by the following (Production Method 5) or (Production Method 6). (Production Method 5) A method of producing a composition having a pH of 5.2 or less by mixing polyphenols, an iron compound, specific amino acids, etc., and an acid. (Production Method 6) A method for producing a composition by mixing a polyphenol, an iron compound, a specific amino acid, etc., and adjusting the pH of the composition to 5.2 or less after mixing.
[0207] [How to use] The composition of the third embodiment can be used in the same manner as described above for the composition of the first embodiment.
[0208] <Method of use as an oral composition or topical composition> The method of use of this embodiment is a method of using any composition selected from the composition of the first embodiment, the composition of the second embodiment, and the composition of the third embodiment as an oral composition or an external composition (hereinafter, this method will be referred to as the "method of the fourth embodiment").
[0209] The method of the fourth embodiment may be carried out in the same manner as the above-described method for using any composition selected from the composition of the first embodiment, the composition of the second embodiment, and the composition of the third embodiment.
[0210] <Method for suppressing changes in the appearance color of a composition> The method of this embodiment is a method for suppressing changes in the external color of a composition containing polyphenols and an iron compound, characterized by adjusting the pH to 5.2 or less (hereinafter, this method will be referred to as the "method of the fifth embodiment").
[0211] According to the method of the fifth embodiment, even when a polyphenol and an iron compound are blended into the composition, the change in appearance color due to the polyphenol and the iron compound can be suppressed by adjusting the pH of the composition to 5.2 or less. The pH of the composition can be adjusted by blending an acid or alkali as needed. The types and amounts of the acid and alkali are the same as those described above for the composition of the first embodiment.
[0212] The method of the fifth embodiment is a method for suppressing a change in the external color of a composition containing a polyphenol and an iron compound by adjusting the pH of the composition to 5.2 or less. The types and amounts of the polyphenol and iron compound used in the method of the fifth embodiment, including examples and preferred examples, are the same as those of the polyphenol and iron compound in the composition of the first embodiment.
[0213] The method of the fifth embodiment may involve adjusting the pH of a composition containing a specific polyphenol as the polyphenol and an iron compound and an amino acid to 5.2 or less. Even when the composition contains a specific polyphenol, an iron compound, and an amino acid, adjusting the pH of the composition to 5.2 or less can suppress changes in appearance color due to the specific polyphenol and the iron compound while also suppressing changes in appearance color due to the specific polyphenol and the amino acid or a salt thereof catalyzed by the iron compound. In this case, the types and amounts of the specific polyphenol and amino acid, including examples and preferred ones, are the same as those of the specific polyphenol and amino acid in the composition of the second embodiment.
[0214] Furthermore, the method of the fifth embodiment may involve further blending a specific amino acid or the like into a composition containing a polyphenol and an iron compound, and adjusting the pH to 5.2 or less. Even when a specific polyphenol, an iron compound, and an amino acid are blended into the composition, adjusting the pH of the composition to 5.2 or less can suppress changes in appearance color due to the polyphenol and the iron compound while also suppressing changes in appearance color due to the polyphenol and the specific amino acid or the like catalyzed by the iron compound. In this case, the types and amounts of the specific amino acids or the like, including exemplary and preferred ones, are the same as those of the specific amino acids or the like in the composition of the third embodiment. [Example]
[0215] The present invention will be described in detail below based on examples, but the present invention should not be construed as being limited by the descriptions in these examples.
[0216] <Test 1: Inhibition of changes in appearance color by polyphenols and iron compounds>
[0217] [Examples 1a to 9a, Examples 1b to 3b, Comparative Examples 1 to 4]
[0218] (Production of compositions of Examples 1a to 9a, Examples 1b to 3b, and Comparative Examples 1 to 4) The compositions of Examples 1a to 9a, Examples 1b to 3b, and Comparative Examples 1 to 4 were produced as follows using any of the following components.
[0219] (Ingredients used (1)) Polyphenols Gallic acid (a polyphenol with one 3,4,5-trihydroxyphenyl group) Tannic acid (a polyphenol with two or more 3,4,5-trihydroxyphenyl groups) Rosmarinic acid (a polyphenol with two or more 3,4-dihydroxyphenyl groups) Iron compounds Sodium ferrous citrate Other ingredients Citric acid Malic acid purified water
[0220] The compositions of Examples 1a to 9a were produced according to the following steps so as to have the compositions shown in Tables 1 and 2. 0.01 g of either gallic acid, tannic acid, or rosmarinic acid, 0.1 g of ferrous sodium citrate, a predetermined amount of citric acid or malic acid, and 10 g of purified water were placed in a 15 mL polypropylene centrifuge tube manufactured by Corning Incorporated (product number 430791; colorless and transparent appearance) (hereinafter simply referred to as a centrifuge tube) and mixed in a conventional manner to obtain a mixture (Part A). This mixture (Part A) was designated as the composition of Examples 1a to 9a.
[0221] The compositions of Examples 1b to 3b were produced according to the following steps so as to have the compositions shown in Table 1. 0.01 g of either gallic acid, tannic acid, or rosmarinic acid was placed in a 0.1 g centrifuge tube and mixed in a conventional manner to obtain a mixture (Part A). After 24 hours, Part B (0.1 g of citric acid) was added to the centrifuge tube containing this mixture (Part A) and mixed in a conventional manner to obtain the compositions of Examples 1b, 2b, and 3b.
[0222] The compositions of Comparative Examples 1 to 4 were produced to have the compositions shown in Tables 1 and 2 in the same manner as the compositions of Examples 1a to 9a, except that neither citric acid nor malic acid was added.
[0223] The pH of each of the compositions produced in Examples 1a to 9a, Examples 1b to 3b, and Comparative Examples 1 to 4 at 25° C. was measured one day after production.
[0224] In Tables 1 and 2, the numerical values in the composition column are in parts by mass, and the notation "-" indicates that the component is not blended. Similarly, in Tables 3 to 10 shown below, the numerical values in the composition column are in parts by mass, and the notation "-" indicates that the component is not blended.
[0225] (Evaluation method) The appearance (appearance color, transparency) of each composition contained in a centrifuge tube was evaluated visually within 12 hours after production for the compositions of Examples 1a to 9a, Examples 1b to 3b, and Comparative Examples 1 to 4. The evaluation was performed by one evaluator who routinely evaluates the appearance color of oral compositions and topical compositions. The evaluation of transparency and appearance color was performed according to the following evaluation criteria. After the appearance evaluation, the centrifuge tubes containing the compositions of Examples 1a to 9a, Examples 1b to 3b, and Comparative Examples 1 to 4 were photographed. For the compositions of Examples 1b to 3b, the appearance color of part A before mixing with part B during the production process (the appearance color of part A immediately before adding part B to part A during the production process) was also evaluated.
[0226] (Evaluation criteria: transparency) Transparent: When the surrounding scenery is observed through a centrifuge tube containing the composition, the surrounding scenery can be clearly seen. Slightly transparent: When the surrounding scenery is observed through the centrifuge tube containing the composition, the surrounding scenery can be seen in a slightly blurred state. Slightly opaque: When observing the surrounding scenery through the centrifuge tube containing the composition, the surrounding scenery is very blurred and not very visible. Opaque: When the surrounding scenery is observed through the centrifuge tube containing the composition, the surrounding scenery cannot be seen.
[0227] (Evaluation criteria: appearance color) ⊚: No black tint is observed in the appearance color of the composition. ◯: A very faint black tint is observed in the appearance color of the composition. Δ: A slightly faint black tint was observed in the appearance color of the composition. ×: A distinct dark black color is observed in the appearance color of the composition.
[0228] (Evaluation results of Examples 1a to 3a, Examples 1b to 3b, and Comparative Examples 1 to 3) Table 1 shows the evaluation results for the compositions of Examples 1a to 3a, Examples 1b to 3b, and Comparative Examples 1 to 3. Also, Figure 1 shows photographs of the appearance of the compositions of each Example and Comparative Example.
[0229] [Table 1]
[0230] The results shown in Table 1 indicate that the compositions of Examples 1a to 3a and 1b to 3b contain either gallic acid, tannic acid, or rosmarinic acid (polyphenols) and sodium ferrous citrate (iron compound). However, the pH was adjusted by adding citric acid to keep the pH below 5.2, resulting in a pale yellow appearance and no apparent black color. On the other hand, the compositions of Comparative Examples 1 to 3 contain either gallic acid, tannic acid, or rosmarinic acid (polyphenols) and sodium ferrous citrate (iron compound), but the pH exceeded 5.2, resulting in a distinctly black appearance. Therefore, the compositions of Examples 1a to 3a and 1b to 3b performed better in the evaluation of appearance color than the compositions of Comparative Examples 1 to 3, demonstrating that the blackening caused by polyphenols and iron compounds was suppressed.
[0231] In the production of the compositions of Examples 1b to 3b, the mixture (Part A) obtained by mixing gallic acid, tannic acid, or rosmarinic acid (polyphenol), sodium ferrous citrate, and water had a black appearance. However, when citric acid (Part B) was added to the black-appearing Part A to adjust the pH to 5.2 or less, the color of the composition turned pale yellow, and the black color disappeared. This result demonstrates that, regardless of the pH adjustment step used in the production process, adjusting the pH to 5.2 or less can suppress blackening caused by polyphenols and iron compounds. It also demonstrates that blackening caused by polyphenols and iron compounds can be reversibly suppressed by adjusting the pH.
[0232] (Evaluation results of Examples 3a to 9a and Comparative Examples 3 and 4) Table 2 shows the evaluation results for the compositions of Examples 3a to 9a and Comparative Examples 3 and 4. Also, Figure 1 shows photographs of the appearance of the compositions of each Example and Comparative Example.
[0233] [Table 2]
[0234] The results shown in Table 2 indicate that the compositions of Examples 3a to 9a had a pale yellow, pale yellowish brown, or pale brown appearance, whereas the compositions of Comparative Examples 3 and 4 had a distinct black appearance. Therefore, the compositions of Examples 3a to 9a either had no black appearance or only a lighter black appearance than the compositions of Comparative Examples 3 and 4, and thus had superior appearance color evaluation results. Therefore, it can be seen that the compositions of Examples 3a to 9a, which contain rosmarinic acid (a polyphenol) and sodium ferrous citrate (an iron compound), were able to suppress blackening due to the polyphenol and iron compound by adjusting the pH to 5.2 or less. The composition of Example 4a containing malic acid had a lighter, pale yellow appearance color than the composition of Example 3a containing citric acid.
[0235] The results shown in Table 2 indicate that the compositions of Examples 3a to 7a, which had a pH of less than 4.9 (light yellow or light yellowish brown), either showed no black tint or exhibited a lighter black tint, and had better evaluation results for appearance color than the compositions of Examples 8a to 9a, which had a pH of more than 4.8 (light brown). These results demonstrate that the compositions of Examples 3a to 7a, which have a pH of less than 4.9, are able to more effectively suppress blackening due to rosmarinic acid (polyphenol) and iron compounds. Furthermore, the compositions of Examples 3a to 5a, which had a pH of 4.2 or less (light yellow appearance), showed no black tint in their appearance and had better appearance color evaluation results than the compositions of Examples 6a to 7a, which had a pH of more than 4.2 but less than 4.9 (light yellow-brown appearance). These results demonstrate that the compositions of Examples 3a to 5a, which have a pH of 4.2 or less, are able to further suppress blackening due to rosmarinic acid (polyphenol) and iron compounds.
[0236] <Test 2: Inhibition of changes in appearance color by polyphenols, iron compounds, and amino acids or their salts>
[0237] [Examples 10a to 28a, Examples 10b to 28b, Comparative Examples 5 to 23]
[0238] (Production of compositions of Examples 10a to 28a, Examples 10b to 28b, and Comparative Examples 5 to 23) The compositions of Examples 10a to 28a, Examples 10b to 28b, and Comparative Examples 5 to 23 were produced as follows using the above-mentioned component (1) and also one of the following components (2).
[0239] (Ingredients used (2)) Amino acids or their salts Glycine, alanine, leucine, tyrosine, methionine, glutamic acid, histidine
[0240] The compositions of Examples 10a to 28a were produced according to the following steps so as to have the compositions shown in Tables 3 to 10. 0.01 g of gallic acid, tannic acid, or rosmarinic acid, 0.1 g of ferrous sodium citrate, 0.1 g of glycine, alanine, leucine, tyrosine, methionine, glutamic acid, or histidine, 0.1 g of citric acid, and 10 g of purified water were placed in a centrifuge tube and mixed by a conventional method to obtain a mixture (Part A). This mixture (Part A) was designated as the compositions of Examples 10a to 28a.
[0241] The compositions of Examples 10b to 28b were produced according to the following steps so as to have the compositions shown in Tables 3 to 10. 0.01 g of any one of gallic acid, tannic acid, or rosmarinic acid, 0.1 g of ferrous sodium citrate, 0.1 g of any one of glycine, alanine, leucine, tyrosine, methionine, glutamic acid, or histidine, and 10 g of purified water were placed in a centrifuge tube and mixed by a standard method to obtain a mixture (Part A). After 24 hours, Part B (0.1 g of citric acid) was added to the centrifuge tube containing this mixture (Part A) and mixed by a standard method to obtain the compositions of Examples 10b to 28b.
[0242] The compositions of Comparative Examples 5 to 23 were produced to have the compositions shown in Tables 3 to 10 in the same manner as the compositions of Examples 10a to 28a, except that citric acid was not added.
[0243] The pH of each of the compositions produced in Examples 10a to 28a, Examples 10b to 28b, and Comparative Examples 5 to 23 was measured at 25° C. one day after production.
[0244] (Evaluation method) The produced compositions of Examples 10a to 28a, Examples 10b to 28b, and Comparative Examples 5 to 23 were evaluated using the same evaluation method and criteria as in the above-mentioned Test 1. For the compositions of Examples 10b to 28b, the appearance color of Part A before mixing Part B in the production process (the appearance color of Part A immediately before adding Part B to Part A in the production process) was also evaluated.
[0245] [2-1: Suppression of changes in external color caused by gallic acid (a polyphenol having one 3,4,5-trihydroxyphenyl group), iron compounds, and amino acids or their salts]
[0246] (Evaluation results of Examples 10a to 16a, Examples 10b to 16b, and Comparative Examples 5 to 11) Tables 2 to 4 show the evaluation results for the compositions of Examples 10a to 16a, Examples 10b to 16b, and Comparative Examples 5 to 11. Table 3 also shows the evaluation results for the compositions of Examples 1a, 1b, and Comparative Example 1 in Test 1 for reference. Figure 2 shows photographs of the appearance of the compositions of each Example and Comparative Example.
[0247] [Table 3]
[0248] [Table 4]
[0249] [Table 5]
[0250] (Evaluation results of the compositions of Examples 10a to 15a, Examples 10b to 15b, and Comparative Examples 5 to 10) From the results shown in Tables 3 to 5, the compositions of Examples 10a to 15a were blended with gallic acid (a polyphenol), any of glycine, alanine, leucine, tyrosine, methionine, and glutamic acid (an amino acid other than a basic amino acid), and ferrous sodium citrate (an iron compound). However, the pH was adjusted by adding citric acid to a pH of 5.2 or less, resulting in a pale yellow appearance and no black tint in the composition. Furthermore, the compositions of Examples 10b to 15b were blended with gallic acid (a polyphenol), an amino acid other than a basic amino acid, and an iron compound, and then the pH was adjusted by adding citric acid to a pH of 5.2 or less, resulting in a pale yellow, pale yellowish brown, or pale brown appearance. The compositions of Examples 10a to 15a had similar results in appearance color evaluation to Example 1a (no amino acid added), and the compositions of Examples 10b to 15b had similar results in appearance color evaluation to Example 1b (no amino acid added), or the appearance color of the compositions was light yellowish brown or light brown, and compared to Example 1b, a very light or slightly lighter black color was observed (evaluation results: ○ or △). On the other hand, the compositions of Comparative Examples 5 to 10 contained gallic acid (polyphenol), an amino acid other than basic amino acids, and ferrous sodium citrate (iron compound), but had a pH greater than 5.2 and a distinct black color was observed in appearance. The compositions of Comparative Examples 5 to 10 had similar results in appearance color evaluation to Comparative Example 1 (no amino acid added). Therefore, the compositions of Examples 5a to 10a and Examples 5b to 10b had superior evaluation results for appearance color compared to the compositions of Comparative Examples 5 to 10, and it can be seen that they are able to suppress blackening caused by polyphenols and iron compounds, while also suppressing blackening caused by polyphenols catalyzed by iron compounds and amino acids other than basic amino acids.
[0251] In the preparation of the compositions of Examples 10b to 15b, the mixtures (Part A) obtained by mixing gallic acid (polyphenol), amino acids other than basic amino acids, ferrous citrate sodium, and water were black. However, when citric acid (Part B) was added to each of these Parts A to adjust the pH to 5.2 or less, the color of the compositions turned pale yellow, pale yellowish brown, or pale brown, and the black color disappeared. These results demonstrate that the blackening caused by gallic acid (polyphenol) and amino acids other than basic amino acids, catalyzed by iron compounds, can be reversibly suppressed by adjusting the pH.
[0252] (Evaluation results of the compositions of Example 16a, Example 16b, and Comparative Example 11) From the results shown in Table 5, the composition of Example 16a contains gallic acid (a polyphenol), histidine (a basic amino acid), and ferrous citrate (an iron compound). However, the pH was adjusted by adding citric acid, resulting in a pH of 5.2 or less, and therefore the composition had a pale yellow appearance and no black color. However, the composition of Example 16b, in which gallic acid (a polyphenol), histidine (a basic amino acid), and an iron compound were mixed and then the pH was adjusted by adding citric acid, resulting in a pH of 5.2 or less, had a black appearance similar to the composition of Comparative Example 11 (an example with a pH greater than 5.2). In the production of the composition of Example 16b, the mixture (part A) obtained by mixing gallic acid (a polyphenol), histidine (a basic amino acid), ferrous citrate (a sodium ferrous citrate), and water was black. Citric acid (Part B) was added to Part A to adjust the pH to 5.2 or less, but the composition remained black and the color remained unchanged. This result indicates that the blackening caused by gallic acid (polyphenol) and basic amino acids catalyzed by iron compounds is irreversible, and that once blackening has occurred, it cannot be suppressed by adjusting the pH.
[0253] The results shown in Tables 3 and 5 indicate that the evaluation results for the composition of Example 16b were similar to those for the composition of Comparative Example 1, in which the pH exceeded 5.2. Regarding the evaluation results for the composition of Example 16b, the results of Test 1 indicate that, regardless of the pH adjustment step used in the production, adjusting the pH to 5.2 or less can suppress blackening caused by polyphenols and iron compounds (see Examples 1a and 1b and Comparative Example 1 in Tables 1 and 3). Furthermore, the composition of Example 16a shown in Table 5 had a pale yellow appearance and no black color was observed. This indicates that adjusting the pH to 5.2 or less suppresses blackening caused by polyphenols and iron compounds, while also suppressing blackening caused by polyphenols and amino acids other than basic amino acids catalyzed by iron compounds. Therefore, based on the results of Test 1 and Example 16a, it can be said that adjusting the pH to 5.2 or less for the composition of Example 16b can suppress blackening caused by polyphenols and iron compounds, but it was found that adjusting the pH to 5.2 or less does not suppress blackening caused by polyphenols and basic amino acids catalyzed by iron compounds.
[0254] [2-2: Suppression of changes in external color caused by tannic acid (a polyphenol having two or more 3,4,5-trihydroxyphenyl groups), iron compounds, and amino acids or their salts]
[0255] (Evaluation results of Examples 17a to 23a, Examples 17b to 23b, and Comparative Examples 12 to 18) Tables 6 to 8 show the evaluation results for the compositions of Examples 17a to 23a, Examples 17b to 23b, and Comparative Examples 12 to 18. Table 6 also shows the evaluation results for the compositions of Examples 2a, 2b, and Comparative Example 2 in Test 1 for reference. Also, FIG. 3 shows photographs of the appearance of the compositions of each Example and Comparative Example. Furthermore, when Part A was mixed with Part B during the production of Example 23b, black precipitate was observed, and therefore the transparency evaluation column for Example 23b in Table 8 is indicated by a diagonal line.
[0256] [Table 6]
[0257] [Table 7]
[0258] [Table 8]
[0259] (Evaluation results of the compositions of Examples 17a to 22a, Examples 17b to 22b, and Comparative Examples 12 to 17) From the results shown in Tables 6 to 8, the compositions of Examples 17a to 22a were blended with tannic acid (a polyphenol), any of glycine, alanine, leucine, tyrosine, methionine, and glutamic acid (an amino acid other than a basic amino acid), and ferrous citrate sodium (an iron compound), but because the pH was adjusted to 5.2 or less by adding citric acid, the appearance was pale yellow and no black was observed. Furthermore, the compositions of Examples 17b to 22b were blended with tannic acid (a polyphenol), an amino acid other than a basic amino acid, and an iron compound, and then the pH was adjusted by adding citric acid, resulting in a pH of 5.2 or less, so all of them had a pale yellow or pale yellowish brown appearance. The compositions of Examples 17a to 22a had similar results in appearance color evaluation to Example 2a (no amino acid added), and the compositions of Examples 17b to 22b had similar results in appearance color evaluation to Example 2b (no amino acid added), or the appearance color of the compositions was light yellowish brown, and a very light black hue was observed in the appearance color of the compositions compared to Example 2b (evaluation result: ○). On the other hand, the compositions of Comparative Examples 12 to 17 contained tannic acid (polyphenol), an amino acid other than basic amino acids, and ferrous sodium citrate (iron compound), but had a pH greater than 5.2, and a distinct black color was observed in the appearance. The compositions of Comparative Examples 12 to 17 had similar results in appearance color evaluation to Comparative Example 2 (no amino acid added). Therefore, the compositions of Examples 17a to 22a and Examples 17b to 22b had superior evaluation results for appearance color compared to the compositions of Comparative Examples 12 to 17, and it can be seen that they are able to suppress blackening caused by polyphenols and iron compounds, while also suppressing blackening caused by polyphenols catalyzed by iron compounds and amino acids other than basic amino acids.
[0260] In the preparation of the compositions of Examples 17b to 22b, the mixtures (Part A) obtained by mixing tannic acid (polyphenols), amino acids other than basic amino acids, ferrous citrate sodium, and water were black. However, when citric acid (Part B) was added to each of the Part A compositions to adjust the pH to 5.2 or less, the color of the composition turned pale yellow or pale yellowish brown, and the black color disappeared. This result demonstrates that the blackening caused by polyphenols and amino acids other than basic amino acids, catalyzed by iron compounds, can be reversibly suppressed by adjusting the pH.
[0261] (Evaluation results of the compositions of Example 23a, Example 23b, and Comparative Example 18) From the results shown in Table 8, the composition of Example 23a contains tannic acid (a polyphenol), histidine (a basic amino acid), and ferrous citrate (an iron compound). However, the pH was adjusted by adding citric acid, resulting in a pH of 5.2 or less, and therefore the composition had a pale yellow appearance and no black color. However, the composition of Example 23b, after mixing tannic acid (a polyphenol), histidine (a basic amino acid), and an iron compound, was adjusted by adding citric acid. Although the pH was 5.2 or less, black precipitates were observed on the appearance. Furthermore, the composition of Comparative Example 11, which had a pH greater than 5.2, had a black appearance. Here, in the production of the composition of Example 23b, the mixture (part A) obtained by mixing tannic acid (a polyphenol), histidine (a basic amino acid), ferrous citrate (a basic amino acid), and water was black. To Part A, citric acid (Part B) was added to adjust the pH to 5.2 or less, but a black precipitate was observed on the outside of the composition. This result shows that the blackening caused by the polyphenols and basic amino acids catalyzed by iron compounds is irreversible, and once blackening has occurred, it cannot be suppressed even by adjusting the pH.
[0262] The results shown in Tables 6 and 8 indicate that the evaluation results for the composition of Example 23b were nearly identical to those for the composition of Comparative Example 2, which had a pH greater than 5.2, except for the presence or absence of precipitation. The evaluation results for the composition of Example 23b are discussed below. The results of Test 1 indicate that, regardless of the pH adjustment step used in the production process, maintaining a pH of 5.2 or less can suppress blackening caused by polyphenols and iron compounds (see Examples 2a and 2b and Comparative Example 2 in Tables 1 and 6). Furthermore, the composition of Example 23a shown in Table 8 had a pale yellow appearance and no black color was observed. This indicates that maintaining a pH of 5.2 or less suppresses blackening caused by polyphenols and iron compounds, while also suppressing blackening caused by polyphenols and amino acids other than basic amino acids, which are catalyzed by iron compounds. Therefore, taking into account the results of Test 1 and Example 23a, it can be said that the composition of Example 23b can suppress blackening caused by polyphenols and iron compounds by setting the pH at 5.2 or less, but it was found that it cannot suppress blackening caused by polyphenols and basic amino acids catalyzed by iron compounds.
[0263] [2-3: Suppression of changes in external color caused by rosmarinic acid (a polyphenol having two or more 3,4-dihydroxyphenyl groups), iron compounds, and amino acids or their salts]
[0264] (Evaluation results of Examples 24a to 28a, Examples 24b to 28b, and Comparative Examples 19 to 23) Tables 9 and 10 show the evaluation results for the compositions of Examples 24a to 28a, Examples 24b to 28b, and Comparative Examples 19 to 23. In Table 9, the evaluation results for the compositions of Examples 3a, 3b, and Comparative Example 3 in Test 1 are shown for reference. Also, Figure 4 shows photographs of the appearance of the compositions of each Example and Comparative Example.
[0265] [Table 9]
[0266] [Table 10]
[0267] (Evaluation results of the compositions of Examples 24a to 27a, Examples 24b to 27b, and Comparative Examples 19 to 22) The results shown in Tables 9 and 10 indicate that the compositions of Examples 24a to 27a contain rosmarinic acid (a polyphenol), glycine, alanine, leucine, or glutamic acid (an amino acid other than a basic amino acid), and ferrous citrate (an iron compound). However, the pH was adjusted by adding citric acid to a pH of 5.2 or less, resulting in a pale yellow appearance and no black tint. The compositions of Examples 24b to 27b contain rosmarinic acid (a polyphenol), an amino acid other than a basic amino acid, and an iron compound, and then the pH was adjusted by adding citric acid. Since the pH was 5.2 or less, the compositions all had a pale yellow appearance. The compositions of Examples 24a to 27a were comparable in appearance color to those of Example 3a (no amino acid added), and the compositions of Examples 24b to 27b were comparable in appearance color to those of Example 3b (no amino acid added). On the other hand, the compositions of Comparative Examples 24 to 27, which contained rosmarinic acid (a polyphenol), an amino acid other than basic amino acids, and ferrous sodium citrate (an iron compound), had a pH greater than 5.2 and exhibited a distinct black appearance. The compositions of Comparative Examples 19 to 22 had similar appearance color evaluation results to Comparative Example 3 (containing no amino acid). Therefore, it can be seen that the compositions of Examples 24a to 27a and 24b to 27b were able to suppress blackening caused by polyphenols and iron compounds, while also suppressing blackening caused by polyphenols and amino acids other than basic amino acids, which are catalyzed by iron compounds, compared to the compositions of Comparative Examples 19 to 22.
[0268] In the preparation of the compositions of Examples 24b to 27b, the mixtures (Part A) obtained by mixing rosmarinic acid (polyphenol), amino acids other than basic amino acids, sodium ferrous citrate, and water were black. However, when citric acid (Part B) was added to each of the Part A mixtures to adjust the pH to 5.2 or less, the color of the composition turned pale yellow, and the black color disappeared. This result demonstrates that the blackening caused by polyphenols and amino acids other than basic amino acids, catalyzed by iron compounds, can be reversibly suppressed by adjusting the pH.
[0269] (Evaluation results of the compositions of Example 28a, Example 28b, and Comparative Example 23) From the results shown in Table 10, the composition of Example 28a contained rosmarinic acid (a polyphenol), histidine (a basic amino acid), and ferrous citrate (an iron compound). However, the pH was adjusted by adding citric acid, resulting in a pH of 5.2 or less, and therefore the composition had a pale yellow appearance and no black color. The composition of Example 28b had a brown appearance despite the pH being 5.2 or less, after mixing rosmarinic acid (a polyphenol), histidine (a basic amino acid), and an iron compound, and then adding citric acid. The composition of Comparative Example 23, which had a pH greater than 5.2, had a black appearance. Here, in the preparation of the composition of Example 28b, the mixture (Part A) obtained by mixing rosmarinic acid (a polyphenol), histidine (a basic amino acid), ferrous citrate (a basic amino acid), and water was black. When citric acid (Part B) was added to Part A to adjust the pH to 5.2 or less, the composition turned brown and its appearance changed color. This result indicates that the blackening caused by rosmarinic acid (polyphenol) and basic amino acids, catalyzed by iron compounds, can be reversibly suppressed.
[0270] The results shown in Tables 9 and 10 indicate that the composition of Example 28b had a superior color appearance compared to the composition of Comparative Example 23, which had a pH greater than 5.2. The results of the composition of Example 28b are discussed below. The results of Test 1 indicate that, regardless of the pH adjustment step used in the production process, maintaining a pH of 5.2 or less can suppress blackening caused by polyphenols and iron compounds (see Examples 3a and 3b and Comparative Example 3 in Tables 1 and 9). Furthermore, the composition of Example 28a shown in Table 10 had a pale yellow appearance and no black color was observed. This indicates that maintaining a pH of 5.2 or less not only suppresses blackening caused by polyphenols and iron compounds, but also suppresses blackening caused by polyphenols and amino acids other than basic amino acids, which are catalyzed by iron compounds. Therefore, taking into account the results of Test 1 and Example 28a, it was found that the composition of Example 28b, by setting the pH at 5.2 or less, was able to suppress blackening caused by polyphenols and iron compounds, and furthermore, was able to suppress blackening caused by polyphenols and basic amino acids catalyzed by iron compounds.
[0271] <Test 3: Preparation of solid composition (powder form) and pH> The compositions (powder-form solid compositions) of Examples 29 and 30 below were prepared, and their pH values at 25°C were measured.
[0272] Example 29 0.01 g of rosmarinic acid, 0.1 g of ferrous sodium citrate, and 0.1 g of citric acid were mixed to produce the composition of Example 29 (a powdered solid composition). The composition of Example 29 was white, with no noticeable black tint in appearance. 3.99 g of purified water was then added to and dissolved in the composition of Example 29 to obtain a 20-fold diluted version of the composition of Example 29. The pH of this 20-fold diluted version at 25°C was measured to be 3.7.
[0273] Example 30 0.01 g of rosmarinic acid, 0.1 g of ferrous sodium citrate, 0.1 g of citric acid, and 0.1 g of glycine were mixed to produce the composition of Example 30 (a solid composition in powder form). The composition of Example 30 was white, with no noticeable black tint in appearance. 5.89 g of purified water was then added to and dissolved in the composition of Example 30 to obtain a 20-fold diluted version of the composition of Example 30. The pH of this 20-fold diluted version at 25°C was measured to be 3.7.
[0274] <Prescription example> Formulation examples A1 to A3 for oral compositions and formulation examples B1 to B4 for external use compositions are shown below.
[0275] (Formulation Example A1: Oral Composition (Tablets)) Rosemary leaf extract (containing rosmarinic acid) 100mg Sodium ferrous citrate 10mg Glycine 15mg Zinc gluconate 1mg Vitamin B2 1mg Vitamin B6 1mg Crystalline cellulose 100mg Hydroxypropyl cellulose 5mg Dextrin 50mg Silicon dioxide 10mg Citric acid (appropriate amount) Magnesium stearate 10mg
[0276] (Formulation Example A2: Oral Composition (Hard Capsule)) The following content (1) is filled into a commercially available HPMC capsule to produce a hard capsule in a conventional manner. ·Contents (1) Rosemary leaf extract (containing rosmarinic acid) 100mg Sodium ferrous citrate 10mg Glycine 15mg Zinc gluconate 1mg Vitamin B2 1mg Vitamin B6 1mg Starch 100mg Silicon dioxide 30mg Citric acid (appropriate amount) Magnesium stearate 10mg
[0277] (Formulation Example A3: Oral Composition (Beverage)) Rosemary leaf extract (containing rosmarinic acid) 100mg Sodium ferrous citrate 1mg Glycine 15mg Zinc gluconate 1mg Vitamin B2 1mg Vitamin B6 1mg Vitamin C 10mg Glucose-sweetened liquid sugar 50mg Fragrance 1mg Purified water 100mg
[0278] (Formulation Example B1: Composition for external use (hair shampoo or body cleanser)) Echinacea purpurea extract (contains chicoric acid) 0.1% by mass Sodium ferrous citrate 0.001% by mass Glycine 0.1% by mass Sodium laureth sulfate 12% by mass Cocamidopropyl betaine 3% by mass Polyquaternium-10 0.1% by mass Methylparaben 0.2% by mass Citric acid (amount to achieve pH 4) Fragrance 0.1% by mass Purified water Amount to make the total 100% by mass
[0279] (Formulation Example B2: External Composition (Hair Cream)) Echinacea purpurea extract (contains chicoric acid) 0.1% by mass Sodium ferrous citrate 0.001% by mass Glycine 0.1% by mass Stearyltrimonium chloride 2% by mass Cetyl alcohol 3% by mass Stearyl alcohol 3% by mass Olive oil 2% by mass Dimethicone 2% by mass Phenoxyethanol 0.2% by mass Glycerin 3% by mass Citric acid (amount to achieve pH 4) Fragrance 0.1% by mass Purified water Amount to make the total 100% by mass
[0280] (Formulation Example B3: Composition for external use (liquid for hair or liquid for skin)) Echinacea purpurea extract (contains chicoric acid) 0.1% by mass Sodium ferrous citrate 0.001% by mass Glycine 0.1% by mass PEG-60 hydrogenated castor oil 0.5% by mass Methylparaben 0.2% by mass Glycerin 3% by mass Citric acid (amount to achieve pH 4) Fragrance 0.1% by mass Purified water Amount to make the total 100% by mass
[0281] (Formulation Example B4: External Composition (Hair Gel or Skin Gel)) Echinacea purpurea extract (contains chicoric acid) 0.1% by mass Sodium ferrous citrate 0.001% by mass Glycine 0.1% by mass Carbomer 0.5% by mass Hydroxyethyl cellulose 0.1% by mass Sodium hydroxide 0.1% by mass Glycerin 3% by mass PEG-60 hydrogenated castor oil 0.2% by mass Methylparaben 0.1% by mass Citric acid (amount to achieve pH 4) Fragrance 0.1% by mass Purified water Amount to make the total 100% by mass
Claims
1. A composition containing polyphenols and an iron compound and having a pH of 5.2 or less.
2. 10. The composition of claim 1, wherein the pH is less than 4.
9.
3. The polyphenol is a polyphenol having one or more 3,4-dihydroxyphenyl groups, The composition according to claim 1 or claim 2, further comprising an amino acid.
4. The composition according to claim 1 or claim 2, further comprising an amino acid other than a basic amino acid.
5. The composition according to claim 1 or 2, wherein the polyphenol is a polyphenol having a molecular weight of 5,000 or less.
6. 3. The composition according to claim 1 or claim 2, which is an oral composition or an external composition.
7. 3. The composition according to claim 1 or claim 2, which is in liquid or solid form.
8. A method for using the composition according to claim 1 or 2 as an oral composition or an external composition.
9. A method for suppressing a change in the appearance color of a composition containing a polyphenol and an iron compound, characterized by adjusting the pH of the composition to 5.2 or less.
Citation Information
Patent Citations
Polyphenols preparation excellent in preservation stability
JP2010168318A