Liquid oral composition

Abstract

A liquid oral composition comprising the following component (a): at least one component selected from tranexamic acid and salts thereof, and component (b): a perfume; and satisfies at least one of the following conditions 1 and 2. (Condition 1) The composition further contains the following component (c): a surfactant having an HLB value of 13.0-20.0, wherein the mass ratio (c) / ((a) + (b)) is 3.5 or more. (Condition 2) The color difference [Delta] E * is 0.0-2.5.

Description

Technical Field

[0001] The present invention relates to liquid oral compositions. Background Art

[0002] As a technique for adding a copper compound to a preparation for oral use, there is a technique described in Patent Document 1 (Japanese Patent Application Laid-Open No. 2010-189358).

[0003] This document describes, as a technology regarding an oral composition that is excellent in inhibiting periodontal disease and bad breath (paragraph 0001), an oral composition containing specific amounts of copper gluconate and / or copper sulfate or hydrates thereof, allantoin or a derivative thereof, and a nonionic surfactant having an HLB value of 6 to 20 (claim 1).

[0004] Prior art literature

[0005] Patent Literature

[0006] Patent Document 1: Japanese Patent Application Laid-Open No. 2010-189358 Summary of the Invention

[0007] The present inventors have studied and found that a liquid oral composition containing a flavoring agent undergoes discoloration over time.

[0008] Therefore, the present invention provides a technique for suppressing the discoloration of a liquid oral composition over time.

[0009] According to the present invention, the following liquid oral composition and method for suppressing discoloration of the liquid oral composition are provided.

[0010] [1] A liquid oral composition comprising:

[0011] (a) at least one selected from tranexamic acid and its salt, and

[0012] (b) spices;

[0013] At least one of the following conditions 1 and 2 is satisfied.

[0014] (Condition 1)

[0015] Further containing the following ingredient (c):

[0016] (c) surfactants with an HLB value of 13.0 to 20.0,

[0017] The mass ratio (c) / ((a)+(b)) of the content of the above-mentioned component (c) to the total content of the above-mentioned components (a) and (b) is 3.5 or more,

[0018] (Condition 2)

[0019] The color difference ΔE was measured by the following method and obtained using the following formula (I): * 0.0~2.5,

[0020] (method)

[0021] The chromaticity coordinates of each sample of the liquid oral composition after storage at 25°C and 60°C for 4 weeks were measured using a spectrocolorimeter under the following conditions in accordance with JIS Z 8722, and CIE 1976L was obtained based on the measured values. * a * b * The chromaticity coordinates specified in the color system are used to calculate the color difference ΔE * .

[0022] Type of measurement method: Spectrophotometric method

[0023] Types of color functions: X, Y, and Z values

[0024] Type of standard illuminant for color measurement: D65 light source / viewing angle 10°

[0025] Geometric conditions of illumination and light reception: Transmission (0°: 0°)

[0026] Wavelength: Measurement wavelength 380nm ~ 780nm, measurement interval: 5nm

[0027] ΔE * ={(L * 2-L * 1) 2 +(a * 2-a * 1) 2 +(b * 2-b * 1) 2} 1 / 2 (I)

[0028] (In the above formula (I), (L * 1.a * 1.b * 1) and (L * 2.a * 2. b * 2) CIE1976L of the above sample after being stored at 25°C for 4 weeks and at 60°C for 4 weeks * a * b * Chromaticity coordinates specified in the colorimetric system.)

[0029] [2] The liquid oral composition according to [1], which satisfies the above condition 1.

[0030] [3] The liquid oral composition according to [1] or [2], further comprising component (d): a copper compound.

[0031] [4] The liquid oral composition according to any one of [1] to [3], wherein when the liquid oral composition contains ethanol, the content of ethanol in the liquid oral composition is 30% by mass or less.

[0032] [5] The liquid oral composition according to any one of [1] to [4], wherein the liquid oral composition does not contain ethanol, or the liquid oral composition contains ethanol and the content of ethanol in the liquid oral composition is 5% by mass or less.

[0033] [6] The liquid oral composition according to any one of [1] to [5], wherein the component (b) comprises one or more selected from lavender oil, peppermint oil, and bergamot oil.

[0034] [7] The liquid oral composition according to any one of [1] to [6], wherein the component (c) comprises one or more selected from polyoxyethylene hydrogenated castor oil, polyoxyethylene cetyl ether, polyoxyethylene behenyl ether, and polyethylene glycol fatty acid ester.

[0035] [8] The liquid oral composition according to [1] or [2], satisfying the above condition 2.

[0036] [9] The liquid oral composition according to [8], wherein Δb is measured by the above method and obtained by the following formula (II) * It is 0 to 3.0.

[0037] Δb * =b * 2-b * 1(II)

[0038]

[10] The liquid oral composition according to [8] or [9], further comprising ethanol,

[0039] The content of the ethanol in the liquid oral composition is 15% by mass or less based on the entire liquid oral composition.

[0040]

[11] The liquid oral composition according to any one of [8] to

[10] , wherein the component (b) is peppermint oil.

[0041]

[12] The liquid oral composition according to any one of [8] to

[11] , further comprising component (c): a surfactant having an HLB value of 13.0 to 20.0.

[0042]

[13] The liquid oral composition according to any one of [8] to

[12] , further comprising component (d): a copper compound.

[0043]

[14] A method for inhibiting discoloration of a liquid oral composition, comprising: adding a component (c): a surfactant having an HLB value of 13.0 to 20.0 to a liquid oral composition containing (a) at least one selected from tranexamic acid and its salts and (b) a flavoring, so that the mass ratio (c) / ((a)+(b)) of the content of the above component (c) relative to the total content of the above components (a) and (b) is 3.5 or more.

[0044] According to the present invention, discoloration over time of a liquid oral composition can be suppressed. DETAILED DESCRIPTION

[0045] The following describes embodiments of the present invention. In this embodiment, the composition may contain each component alone or in combination of two or more components.

[0046] In this specification, "to" indicating a numerical range means above and below, and both numerical values ​​at both ends are included.

[0047] In the present embodiment, the liquid oral composition contains the following components (a) and (b), and satisfies at least one of the following conditions 1 and 2.

[0048] (a) at least one selected from tranexamic acid and its salt

[0049] (b) Spices

[0050] (Condition 1)

[0051] Further containing component (c): a surfactant having an HLB value of 13.0 to 20.0, wherein the mass ratio (c) / ((a)+(b)) of the content of the above component (c) to the total content of components (a) and (b) is 3.5 or more

[0052] (Condition 2)

[0053] The color difference ΔE was measured by the following method and obtained using the following formula (I): * 0.0~2.5

[0054] (method)

[0055] The chromaticity coordinates of each sample of the liquid oral composition after storage at 25°C and 60°C for 4 weeks were measured using a spectrocolorimeter under the following conditions in accordance with JIS Z 8722, and CIE 1976L was obtained based on the measured values. * a * b *The chromaticity coordinates specified in the color system are used to calculate the color difference ΔE * .

[0056] Type of measurement method: Spectrophotometric method

[0057] Types of color functions: X, Y, and Z values

[0058] Type of standard illuminant for color measurement: D65 light source / viewing angle 10°

[0059] Geometric conditions of illumination and light reception: Transmission (0°: 0°)

[0060] Wavelength: Measurement wavelength 380nm ~ 780nm, measurement interval: 5nm

[0061] ΔE * ={(L * 2-L * 1) 2 +(a * 2-a * 1) 2 +(b * 2-b * 1) 2} 1 / 2 (I)

[0062] (In the above formula (I), (L * 1.a * 1.b * 1) and (L * 2.a * 2. b * 2) CIE1976L of the above sample after being stored at 25°C for 4 weeks and at 60°C for 4 weeks * a * b * Chromaticity coordinates specified in the colorimetric system.)

[0063] The liquid oral composition contains components (a) and (b) and satisfies at least one of conditions 1 and 2. Thus, even when the component (b) is added, discoloration over time can be appropriately suppressed.

[0064] From the viewpoint of suppressing discoloration over time, the liquid oral composition only needs to satisfy either one of conditions 1 and 2, and preferably satisfies both conditions.

[0065] The compositions satisfying the conditions are described in detail below. The configurations described in the following embodiments can be combined as appropriate.

[0066] (First embodiment)

[0067] In this embodiment, the composition is used in the oral cavity, specifically a liquid oral composition.

[0068] (Liquid oral composition)

[0069] In this embodiment, the liquid oral composition contains the following components (a) to (c). That is, the liquid oral composition in this embodiment satisfies the above-mentioned condition 1.

[0070] (a) at least one selected from tranexamic acid and its salt

[0071] (b) Spices

[0072] (c) Surfactants with HLB values ​​of 13.0 to 20.0

[0073] Furthermore, the mass ratio (c) / ((a)+(b)) of the content of the component (c) to the total content of the components (a) and (b) in the liquid oral composition is 3.5 or more.

[0074] Since the liquid oral composition in this embodiment contains the above-mentioned components (a) to (c) in combination at a specific ratio, discoloration with time can be appropriately suppressed.

[0075] Each component is described below.

[0076] (ingredient (a))

[0077] Component (a) is at least one selected from tranexamic acid and its salts. Component (a) is a known compound and can be produced by a known method or a commercially available product can be used.

[0078] Component (a) is disclosed as tranexamic acid in the 18th revised edition of the Japanese Pharmacopoeia, for example.

[0079] Specific examples of the salt of tranexamic acid include one or two or more selected from acid addition salts, metal salts, amine salts, and salts with amino acids.

[0080] Among them, as an acid addition salt, for example, one or more salts selected from the following can be mentioned:

[0081] Hydrohalides such as hydrofluoride, hydrochloride, hydrobromide, and hydroiodide;

[0082] Inorganic acid salts such as nitrates, perchlorates, sulfates, and phosphates;

[0083] Methanesulfonate, trifluoromethanesulfonate, ethanesulfonate and other lower (carbon number 1 to 3) alkane sulfonates;

[0084] Aryl sulfonates such as benzenesulfonate and p-toluenesulfonate; and

[0085] Organic acid salts such as acetate, malate, fumarate, succinate, citrate, ascorbate, tartrate, oxalate, maleate, etc.

[0086] Examples of the metal salt include alkali metal salts selected from sodium salts, potassium salts, and the like; and

[0087] One or more alkaline earth metal salts such as calcium salts and magnesium salts.

[0088] Examples of the amine salt include organic amine salts such as N-methylmorpholine salt, triethylamine salt, tributylamine salt, diisopropylethylamine salt, dicyclohexylamine salt, N-methylpiperidinium salt, pyridinium salt, 4-pyrrolidinylpyridinium salt, and picolinium salt.

[0089] Examples of the salt with an amino acid include one or two or more selected from glycine salts, lysine salts, arginine salts, ornithine salts, glutamate salts, and aspartate salts.

[0090] From the viewpoint of more stably suppressing discoloration of the liquid oral composition, component (a) is preferably tranexamic acid.

[0091] From the viewpoint of exhibiting superior anti-inflammatory and anti-hemostatic effects, the content of component (a) in the liquid oral composition is preferably 0.01% by mass or more, more preferably 0.02% by mass or more, and even more preferably 0.03% by mass or more, based on the entire liquid oral composition.

[0092] Furthermore, from the viewpoint of reducing the influence of taste and the like on the feel during use, the content of component (a) in the liquid oral composition is preferably 1% by mass or less, more preferably 0.5% by mass or less, even more preferably 0.1% by mass or less, and even more preferably 0.08% by mass or less, relative to the entire liquid oral composition.

[0093] (Component (b))

[0094] Ingredient (b) is fragrance.

[0095] Specific examples of component (b) include one or more selected from lavender oil, mint oil, bergamot oil, menthol, peppermint, spearmint, and fruit flavorings. From the perspective of more stably suppressing discoloration of the liquid oral composition, component (b) preferably contains one or more selected from lavender oil, mint oil, and bergamot oil.

[0096] From the viewpoint of providing a good feel during use, the content of component (b) in the liquid oral composition is preferably 0.01% by mass or more, more preferably 0.03% by mass or more, even more preferably 0.05% by mass or more, and even more preferably 0.08% by mass or more, based on the entire liquid oral composition.

[0097] In addition, from the perspective of reducing the impact of taste and the like on the feel of use, the content of component (b) in the liquid oral composition is preferably 1% by mass or less, more preferably less than 1% by mass, further preferably 0.5% by mass or less, and even more preferably 0.3% by mass or less, relative to the total liquid oral composition. On the other hand, from the perspective of imparting an appropriate flavor, the content of component (b) in the liquid oral composition is also preferably less than 1% by mass relative to the total liquid oral composition.

[0098] (ingredient (c))

[0099] Component (c) is a surfactant having an HLB value of 13.0 to 20.0. Specific examples of the surfactant include nonionic surfactants.

[0100] Examples of the nonionic surfactant include polyoxyethylene alkyl ethers such as polyoxyethylene cetyl ether and polyoxyethylene behenyl ether; polyoxyethylene-polyoxypropylene block copolymers; polyoxyethylene hydrogenated castor oil; polyoxyethylene ethers of glycerides; sucrose fatty acid esters; alkanolamides; fatty acid glycerides; and one or more polyoxyalkylene fatty acid esters such as polyethylene glycol fatty acid esters.

[0101] When the component (c) contains a polyoxyethylene chain, the average number of moles of ethylene oxide added is, for example, 50 to 100.

[0102] When component (c) contains an alkyl group or a fatty acid, the average number of moles of ethylene oxide added is, for example, 5 to 50, or preferably 9 to 50. The alkyl group or fatty acid has, for example, 4 to 34 carbon atoms, or preferably 12 to 22 carbon atoms.

[0103] From the viewpoint of more stably suppressing discoloration of the liquid oral composition, component (c) is preferably a nonionic surfactant, and more preferably comprises one or more selected from polyoxyethylene hydrogenated castor oil, polyoxyethylene cetyl ether, polyoxyethylene behenyl ether, and polyethylene glycol fatty acid esters.

[0104] Specifically, the HLB value of the component (c) is 13.0 or more, preferably 15.0 or more, from the viewpoint of improving solubility in water and more stably suppressing discoloration of the liquid oral composition.

[0105] Specifically, the HLB value of the component (c) is 20.0 or less, preferably 19.0 or less, and more preferably 17.0 or less.

[0106] Here, when the liquid oral composition contains two or more surfactants, the HLB value can be determined as the sum of the products of the HLB values ​​and the mass fractions of the respective surfactants.

[0107] From the viewpoint of more stably solubilizing the oily component and more stably suppressing discoloration of the liquid oral composition, the content of component (c) in the liquid oral composition is preferably 0.1% by mass or more, more preferably 0.5% by mass or more, even more preferably 0.8% by mass or more, even more preferably 1% by mass or more, and even more preferably 1.5% by mass or more, relative to the entire liquid oral composition.

[0108] From the viewpoint of suppressing bitterness and astringency and adjusting taste, the content of component (c) in the liquid oral composition is preferably 10% by mass or less, more preferably 7.5% by mass or less, and even more preferably 5% by mass or less, relative to the entire liquid oral composition.

[0109] From the viewpoint of suppressing discoloration over time of the liquid oral composition, the mass ratio (c) / ((a) + (b)) of the content of component (c) to the total content of components (a) and (b) is specifically 3.5 or more, preferably 4.0 or more, more preferably 4.5 or more, even more preferably 5.0 or more, and even more preferably 5.5 or more.

[0110] From the viewpoint of suppressing bitterness and astringency and adjusting taste, the mass ratio (c) / ((a)+(b)) is preferably 50 or less, more preferably 40 or less, further preferably 30 or less, and even more preferably 20 or less.

[0111] The liquid oral composition may contain components other than components (a) to (c).

[0112] For example, the liquid oral composition may further contain component (d): a copper compound.

[0113] (ingredient (d))

[0114] Component (d) is a copper compound. By further comprising component (d), the liquid oral composition can enhance the effect of suppressing bad breath, etc. Specific examples of component (d) include water-soluble copper salts.

[0115] Specifically, the water-soluble copper salt refers to a water-soluble copper salt among inorganic and organic copper salts. The water-soluble copper salt may be either an anhydrous form or a hydrate. The water-soluble copper salt may be any copper salt that can be used as a raw material for pharmaceuticals, foods, or cosmetics.

[0116] In addition, examples of water-soluble copper salts include one or more selected from copper gluconate, copper sulfate, copper citrate, copper chlorophyllin, and sodium copper chlorophyllin. From the perspective of further enhancing the effect of inhibiting bad breath, such as the effect of combining water-soluble copper salts, the water-soluble copper salt preferably includes at least one of copper gluconate and copper sulfate, and more preferably copper gluconate.

[0117] As the water-soluble copper salt, for example, a commercially available item can be used.

[0118] From the viewpoint of further enhancing the effect of incorporating the water-soluble copper salt, such as the effect of suppressing bad breath, the content of component (d) in the liquid oral composition is preferably 0.001% by mass or more, more preferably 0.01% by mass or more, further preferably 0.03% by mass or more, and even more preferably 0.08% by mass or more, relative to the entire liquid oral composition.

[0119] Furthermore, from the viewpoint of reducing an unpleasant feeling during use such as a metallic taste, the content of component (d) in the liquid oral composition is preferably 10% by mass or less, more preferably 1% by mass or less, even more preferably 0.5% by mass or less, even more preferably 0.3% by mass or less, and even more preferably 0.2% by mass or less, relative to the entire liquid oral composition.

[0120] Furthermore, from the viewpoint of further enhancing the effect of the addition of component (d), such as the effect of suppressing bad breath, the content of component (d) in the liquid oral composition is preferably 0.001% by mass or more, and more preferably 0.01% by mass or more, based on the amount of copper added.

[0121] From the viewpoint of reducing unpleasant sensations such as metallic taste, the content of component (d) in the liquid oral composition is preferably 0.06% by mass or less, more preferably 0.03% by mass or less, based on the amount of copper incorporated.

[0122] From the viewpoint of suppressing discoloration over time of the liquid oral composition, the mass ratio (c) / ((a) + (b) + (d)) of the content of component (c) to the total content of components (a), (b), and (d) is preferably 2.6 or more, more preferably 3.0 or more, and even more preferably 5.0 or more.

[0123] In addition, from the viewpoint of suppressing bitterness and astringency and adjusting taste, the mass ratio (c) / ((a)+(b)+(d)) is preferably 50 or less, more preferably 40 or less, further preferably 30 or less, and even more preferably 20 or less.

[0124] (water)

[0125] Liquid oral compositions specifically comprise water.

[0126] The content of water in the liquid oral composition may be, for example, the remainder obtained by removing components other than water from the liquid oral composition.

[0127] The water content in the liquid oral composition is preferably 50% by mass or more, more preferably 60% by mass or more, and even more preferably 70% by mass or more, and is preferably 99.88% by mass or less, more preferably 99.5% by mass or less, and even more preferably 99% by mass or less, relative to the entire liquid oral composition.

[0128] (Ethanol)

[0129] The liquid oral composition may further comprise ethanol.

[0130] From the viewpoint of appropriately imparting a refreshing and good feeling during use, the ethanol content in the liquid oral composition is preferably 0.1% by mass or more, more preferably 1% by mass or more, and even more preferably 2% by mass or more.

[0131] In addition, from the perspective of suppressing strong irritation in the oral cavity, the ethanol content in the liquid oral composition is preferably 30% by mass or less, more preferably 20% by mass or less, even more preferably 10% by mass or less, even more preferably 7.5% by mass or less, and even more preferably 5% by mass or less. From the same perspective, it is also preferred that the liquid oral composition does not contain ethanol, that is, the ethanol content is 0% by mass, or that the liquid oral composition contains ethanol and the content is 5% by mass or less.

[0132] (Other ingredients)

[0133] A composition such as a liquid oral composition may contain components other than the above components within a range not impairing the effects of the present invention.

[0134] Examples of such ingredients include pharmaceutical ingredients, binders, wetting agents, flavoring agents, preservatives, colorants, pH adjusters, solvents, solubilizers, bases, detergents, and adsorbents, which can be appropriately selected depending on the dosage form. Specific examples of the additives are shown below, but the ingredients that can be incorporated into the present invention are not limited to these.

[0135] Examples of the medicinal ingredients include one or more selected from antiseptics, anti-inflammatory agents, blood circulation enhancers, tartar deposit inhibitors, stain removers, anti-sensitivity agents, vitamins, and plaque-degrading enzymes. These medicinal ingredients are not limited as long as they can be used in pharmaceuticals.

[0136] Among the medicinal ingredients, examples of the bactericide include one or more selected from isopropylmethylphenol, cetylpyridinium chloride, benzalkonium chloride, benzethonium chloride, hinokitiol, chlorhexidine hydrochloride, alkylbis(aminoethyl)glycine hydrochloride, sodium lauroyl sarcosinate, and triclosan.

[0137] As anti-inflammatory agents, for example, one or more selected from the group consisting of β-glycyrrhetinic acid, glycyrrhetinic acid, glycyrrhizic acid, diammonium glycyrrhizate, disodium glycyrrhizate, trisodium glycyrrhizate, dipotassium glycyrrhizate, monoammonium glycyrrhizate, ε-aminocaproic acid, sodium azulenesulfonate hydrate, allantoin, aluminum dihydroxyallantoin, epidihydrocholesterol, dihydrocholesterol and lysozyme hydrochloride can be cited.

[0138] As a blood circulation promoting agent, sodium chloride is mentioned, for example.

[0139] Examples of dental calculus deposit inhibitors include one or more selected from disodium hydrogen phosphate, disodium dihydrogen pyrophosphate, sodium pyrophosphate, anhydrous sodium pyrophosphate, tetrasodium pyrophosphate (anhydrous), disodium hydrogen phosphate, sodium hydrogen phosphate hydrate, disodium hydrogen phosphate (crystalline), trisodium phosphate, and sodium polyphosphate.

[0140] Examples of the stain remover include one or more selected from MACROGOL (MACROGOL 200, MACROGOL 300, MACROGOL 400, MACROGOL 600, MACROGOL 1000, MACROGOL 1500, MACROGOL 1540, MACROGOL 4000, MACROGOL 6000, MACROGOL 20000, etc.), sodium polyphosphate, and polyvinyl pyrrolidone.

[0141] Examples of the anti-sensitizing agent include at least one selected from potassium nitrate and water-soluble aluminum salts.

[0142] Examples of vitamins include one or more selected from ascorbic acid, L-ascorbic acid, sodium ascorbate, sodium L-ascorbate, pyridoxine hydrochloride, DL-α-tocopheryl acetate, tocopheryl acetate, dl-α-tocopheryl nicotinate, and tocopheryl nicotinate.

[0143] Examples of plaque-decomposing enzymes include glucanase.

[0144] Examples of the binder include one or more selected from organic binders such as pullulan, gelatin, methylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, sodium carboxymethylcellulose, carrageenan, sodium alginate, xanthan gum, sodium polyacrylate, gum arabic, guar gum, locust bean gum, polyvinyl alcohol, and carboxyvinyl polymers, thickening anhydrous silicic acid, and bentonite.

[0145] Here, from the viewpoint of easy cleaning of the oral cavity, the liquid oral composition preferably does not contain xanthan gum, and more preferably does not contain a binder.

[0146] Here, the liquid oral composition containing no xanthan gum or binder specifically means that xanthan gum or binder is not intentionally added to the liquid oral composition, and more specifically means that the content of xanthan gum or binder is 0.001% by mass or less based on the entire liquid oral composition.

[0147] As the wetting agent, any wetting agent that can be sold as a raw material for medicines, foods, or cosmetics may be used, and examples thereof include polyols, and more specifically, one or more selected from sorbitol, glycerin, concentrated glycerin, ethylene glycol, propylene glycol, 1,3-butylene glycol, propylene glycol (1,3-propanediol), polyethylene glycol, polypropylene glycol, sodium hyaluronate, and hydrolyzed collagen.

[0148] From the viewpoint of reducing irritation to the oral cavity, the humectant is preferably at least one selected from glycerin and propylene glycol, and more preferably glycerin.

[0149] From the viewpoint of achieving a more appropriate viscosity of the liquid oral composition, the content of the humectant in the liquid oral composition is preferably 1% by mass or more, more preferably 3% by mass or more, and even more preferably 5% by mass or more, and is preferably 30% by mass or less, more preferably 25% by mass or less, and even more preferably 20% by mass or less.

[0150] Examples of flavoring agents include monosodium L-glutamate, saccharin, saccharin sodium, sucrose, glucose, fructose, lactose, honey, aspartame, stevia, sucralose, inositol, D-sorbitol, D-mannitol, arabitol, raffinose, lactulose, lactitol, xylitol, erythritol, reduced isomaltulose, isomaltulose, PALATINIT (registered trademark), acesulfame potassium, trehalose, maltose, stachyose or maltitol, neohesperidin dihydrochalcone, perilla frutescens, p-methoxycinnamaldehyde, and thaumatin.

[0151] From the viewpoint of having a strong sweet taste and being able to adjust the taste even in a small amount, the flavoring agent is preferably at least one selected from xylitol, sodium saccharin, and saccharin, and more preferably at least one selected from xylitol and sodium saccharin.

[0152] From the viewpoint of appropriately imparting a refreshing and good feeling during use, the content of the flavoring agent in the liquid oral composition is preferably 0.01% by mass or more, more preferably 0.05% by mass or more, and even more preferably 0.1% by mass or more, and is preferably 2% by mass or less, more preferably 1% by mass or less, and even more preferably 0.5% by mass or less.

[0153] Examples of preservatives include sodium benzoate, methyl parahydroxybenzoate, ethyl parahydroxybenzoate, butyl parahydroxybenzoate, isopropyl parahydroxybenzoate, propyl parahydroxybenzoate, isobutyl parahydroxybenzoate, benzyl parahydroxybenzoate and the like; alcohols such as phenoxyethanol; sorbic acid, benzoic acid, dehydroacetic acid, propionic acid and salts thereof; ethylenediaminetetraacetate and alkyldi(aminoethyl)glycine hydrochloride, or two or more thereof.

[0154] As coloring agents, for example, natural pigments selected from safflower red pigment, gardenia yellow pigment, gardenia blue pigment, perilla pigment, red yeast rice pigment, red cabbage pigment, carrot pigment, hibiscus pigment, cocoa pigment, spirulina blue pigment, coumarin pigment, etc.; legal pigments such as Red No. 3, Red No. 104, Red No. 105, Red No. 106, Yellow No. 4, Yellow No. 5, Green No. 3, Blue No. 1; one or more of riboflavin and titanium dioxide.

[0155] Examples of the pH adjuster include one or more selected from acids, bases, and buffers such as acetic acid, hydrochloric acid, sulfuric acid, nitric acid, citric acid, phosphoric acid, malic acid, gluconic acid, maleic acid, succinic acid, glutamic acid, pyrophosphoric acid, tartaric acid, acetic acid, sodium hydroxide, potassium hydroxide, sodium acetate, sodium carbonate, sodium citrate, sodium hydrogen citrate, phosphoric acid, sodium phosphate, disodium hydrogen phosphate, sodium dihydrogen phosphate, and potassium dihydrogen phosphate.

[0156] Examples of the solvent include water as described above and lower alcohols such as propanol.

[0157] In order to promote the dissolution of the above-mentioned additives or medicinal ingredients in water, a solubilizer may be added. Examples of such a solubilizer include polyols such as dipropylene glycol.

[0158] As a base, sodium bicarbonate is mentioned, for example.

[0159] As a cleaning agent, sodium polyphosphate is mentioned, for example.

[0160] Examples of the adsorbent include β-cyclodextrin.

[0161] Furthermore, in addition to the above-mentioned components, components suitable for the use of oral compositions such as liquid oral compositions may be appropriately blended within a range that does not impair the scope of the present invention.

[0162] (Viscosity)

[0163] In the present embodiment, from the viewpoint of easy cleaning of the oral cavity, the viscosity of the liquid oral composition is preferably 25 mPa·s or less, more preferably 10 mPa·s or less, and even more preferably 7.5 mPa·s or less.

[0164] The viscosity of the liquid oral composition may be, for example, 0.1 mPa·s or more.

[0165] Specifically, the viscosity of the liquid oral composition can be measured using a B-type viscometer (e.g., Brookfield Rotational Viscometer DV3T, manufactured by Brookfield) at room temperature of 25±3°C, Rotor LV-1, rotation speed of 200 rpm, and measurement time of 1 minute.

[0166] (Liquid preparation)

[0167] In addition, the liquid oral composition is specifically a liquid preparation. The liquid preparation is specifically an oral preparation.

[0168] Specific embodiments of the liquid oral composition include one selected from mouthwash, liquid toothpaste, and mouth freshener. The liquid oral composition is preferably mouthwash.

[0169] (Manufacturing Method)

[0170] In the present embodiment, the method for producing the liquid oral composition includes, for example, a step of blending components (a) to (c) and other appropriate components.

[0171] Since the liquid oral composition obtained in the present embodiment contains components (a) to (c) in combination at a specific ratio, discoloration over time can be appropriately suppressed.

[0172] (Method for suppressing discoloration)

[0173] In this embodiment, the method for suppressing discoloration of a liquid oral composition includes adding the component (c) to a liquid oral composition containing the components (a) and (b) described above, such that the mass ratio (c) of the content of the component (c) relative to the total content of the components (a) and (b) ((a) + (b)) is 3.5 or greater. In the method of this embodiment, since the components (a) to (c) are combined and added to the liquid oral composition at a specific ratio, discoloration of the liquid oral composition over time can be appropriately suppressed.

[0174] (Second embodiment)

[0175] In this embodiment, the composition is used in the oral cavity, specifically a liquid oral composition.

[0176] (Liquid oral composition)

[0177] In this embodiment, the liquid oral composition contains the following components (a) and (b).

[0178] (a) at least one selected from tranexamic acid and its salt

[0179] (b) Spices

[0180] The color difference ΔE of the liquid oral composition was measured by the following method and obtained using the following formula (I): * It is 0.0 to 2.5. That is, the liquid oral composition in this embodiment satisfies the above-mentioned condition 2.

[0181] (method)

[0182] The chromaticity coordinates of each sample of the liquid oral composition after storage at 25°C and 60°C for 4 weeks were measured using a spectrocolorimeter in accordance with JIS Z 8722 under the following conditions, and CIE 1976L was obtained based on the measured values. * a * b * Calculate the color difference ΔE from the chromaticity coordinates specified in the color system * .

[0183] Type of measurement method: Spectrophotometric method

[0184] Types of color functions: X, Y, and Z values

[0185] Type of standard illuminant for color measurement: D65 light source / viewing angle 10°

[0186] Geometric conditions of illumination and light reception: Transmission (0°: 0°)

[0187] Wavelength: Measurement wavelength 380nm ~ 780nm, measurement interval: 5nm

[0188] ΔE * ={(L * 2-L * 1) 2 +(a * 2-a * 1) 2 +(b * 2-b * 1) 2} 1 / 2 (I)

[0189] (In the above formula (I), (L * 1.a * 1.b *1) and (L * 2.a * 2. b * 2) CIE1976L of samples after storage at 25°C for 4 weeks and at 60°C for 4 weeks * a * b * Chromaticity coordinates specified in the colorimetric system.)

[0190] The present inventors have found for the first time that a liquid oral composition containing the above-mentioned components (a) and (b) and a color difference ΔE obtained by formula (I) * Specifically, as an indicator related to the presence or degree of discoloration over time, the color difference ΔE of the liquid oral composition after storage at 25°C and after the accelerated test can be used. * By setting the content in a specific range, discoloration of the liquid oral composition can be effectively suppressed.

[0191] Specifically, the color difference ΔE * It is 0.0 or more, and from the viewpoint of appropriately suppressing discoloration over time, it is preferably 0.01 or more, more preferably 0.05 or more, and even more preferably 0.1 or more.

[0192] In addition, from the viewpoint of appropriately suppressing discoloration over time, specifically, the color difference ΔE * 2.5 or less, preferably 2.0 or less, more preferably 1.5 or less, further preferably 1.0 or less, and further more preferably 0.8 or less. * More preferably, it is 0.5 or less.

[0193] From the same viewpoint, when the liquid oral composition does not contain a copper compound, the color difference ΔE * It can be 0.5 or less. When the liquid oral composition contains a copper compound, the color difference ΔE * It can be 2.5 or less.

[0194] Color difference ΔE * The measurement was performed using the method described above. More specifically, the liquid oral composition was dispensed into two 50 mL glass bottles, each containing 50 mL. One bottle was stored at 25°C and 60% RH, while the other was stored in a thermostatic chamber at 60°C and constant humidity. Here, constant humidity specifically refers to a relative humidity range of 45% to 85%.

[0195] Each composition after storage is returned to room temperature by, for example, storing it at room temperature for 3 to 4 hours. Thereafter, the color of each composition is measured under the above-mentioned conditions using a spectrocolorimeter (specifically, SE-7700, manufactured by Nippon Denshoku Industries Co., Ltd.).* a * b * The lightness specified in the color system (L * ) and chromaticity (a * 、b * ) Calculate the color difference ΔE according to formula (I) * .

[0196] In the liquid oral composition, from the viewpoint of appropriately suppressing discoloration over time, Δb is measured by the above method and obtained by the following formula (II): * It is preferably 0 or greater, preferably 0.01 or greater, more preferably 0.05 or greater, and further preferably 0.1 or greater.

[0197] In addition, from the viewpoint of appropriately suppressing discoloration over time, the color difference Δb * For example, it is 3.0 or less, preferably 2.5 or less, more preferably 2.0 or less, further preferably 1.5 or less, and further more preferably 1.0 or less. * More preferably, it is 0.5 or less.

[0198] Δb * =b * 2-b * 1(II)

[0199] Next, the components contained in the liquid oral composition will be described.

[0200] (ingredient (a))

[0201] Component (a) is at least one selected from tranexamic acid and its salts. Component (a) is a known compound and can be produced by a known method or a commercially available product can be used.

[0202] Component (a) is disclosed as tranexamic acid in the 18th revised edition of the Japanese Pharmacopoeia, for example.

[0203] Specific examples of the salt of tranexamic acid include one or two or more selected from acid addition salts, metal salts, amine salts, and salts with amino acids.

[0204] Among them, as an acid addition salt, for example, one or more salts selected from the following can be mentioned:

[0205] Hydrohalides such as hydrofluoride, hydrochloride, hydrobromide, and hydroiodide;

[0206] Inorganic acid salts such as nitrates, perchlorates, sulfates, and phosphates;

[0207] Methanesulfonate, trifluoromethanesulfonate, ethanesulfonate and other lower (carbon number 1 to 3) alkane sulfonates;

[0208] Aryl sulfonates such as benzenesulfonate and p-toluenesulfonate; and

[0209] Organic acid salts such as acetate, malate, fumarate, succinate, citrate, ascorbate, tartrate, oxalate, maleate, etc.

[0210] Examples of the metal salt include alkali metal salts selected from sodium salts, potassium salts, and the like; and

[0211] One or more alkaline earth metal salts such as calcium salts and magnesium salts.

[0212] Examples of the amine salt include organic amine salts such as N-methylmorpholine salt, triethylamine salt, tributylamine salt, diisopropylethylamine salt, dicyclohexylamine salt, N-methylpiperidinium salt, pyridinium salt, 4-pyrrolidinylpyridinium salt, and picolinium salt.

[0213] Examples of the salt with an amino acid include one or two or more selected from glycine salts, lysine salts, arginine salts, ornithine salts, glutamate salts, and aspartate salts.

[0214] From the viewpoint of more stably suppressing discoloration of the liquid oral composition, component (a) is preferably tranexamic acid.

[0215] From the viewpoint of exhibiting superior anti-inflammatory and anti-hemostatic effects, the content of component (a) in the liquid oral composition is preferably 0.01% by mass or more, more preferably 0.02% by mass or more, and even more preferably 0.03% by mass or more, based on the entire liquid oral composition.

[0216] Furthermore, from the viewpoint of reducing the influence of taste and the like on the feel during use, the content of component (a) in the liquid oral composition is preferably 1% by mass or less, more preferably 0.5% by mass or less, even more preferably 0.1% by mass or less, even more preferably less than 0.1% by mass, and even more preferably 0.08% by mass or less, relative to the entire liquid oral composition.

[0217] (Component (b))

[0218] Ingredient (b) is fragrance.

[0219] Specific examples of component (b) include one or more selected from lavender oil, mint oil, bergamot oil, menthol, peppermint, spearmint, and fruit flavorings. From the perspective of more stably suppressing discoloration of the liquid oral composition, component (b) preferably contains one or more selected from lavender oil, mint oil, and bergamot oil, and more preferably mint oil.

[0220] From the viewpoint of providing a good feel during use, the content of component (b) in the liquid oral composition is preferably 0.01% by mass or more, more preferably 0.03% by mass or more, even more preferably 0.05% by mass or more, even more preferably 0.1% by mass or more, and even more preferably 0.2% by mass or more, based on the entire liquid oral composition.

[0221] In addition, from the perspective of reducing the impact of taste and the like on the feel of use, the content of component (b) in the liquid oral composition is preferably 1% by mass or less, more preferably less than 1% by mass, further preferably 0.5% by mass or less, and even more preferably 0.3% by mass or less, relative to the total liquid oral composition. On the other hand, from the perspective of imparting an appropriate flavor, the content of component (b) in the liquid oral composition is also preferably less than 1% by mass relative to the total liquid oral composition.

[0222] The liquid oral composition may contain ingredients other than ingredients (a) and (b).

[0223] For example, the liquid oral composition may further contain at least one of the following components (c) and (d).

[0224] (c) Surfactants with HLB values ​​of 13.0 to 20.0

[0225] (d) Copper compounds

[0226] (ingredient (c))

[0227] Component (c) is a surfactant having an HLB value of 13.0 to 20.0. The liquid oral composition can be further stably inhibited from discoloring by further comprising component (c). Specific examples of the surfactant include nonionic surfactants.

[0228] Examples of the nonionic surfactant include polyoxyethylene alkyl ethers such as polyoxyethylene cetyl ether and polyoxyethylene behenyl ether; polyoxyethylene-polyoxypropylene block copolymers; polyoxyethylene hydrogenated castor oil; polyoxyethylene ethers of glycerides; sucrose fatty acid esters; alkanolamides; fatty acid glycerides; and one or more polyoxyalkylene fatty acid esters such as polyethylene glycol fatty acid esters.

[0229] When the component (c) contains a polyoxyethylene chain, the average number of moles of ethylene oxide added is, for example, 50 to 100.

[0230] When component (c) contains an alkyl group or a fatty acid, the average number of moles of ethylene oxide added is, for example, 5 to 50, or preferably 9 to 50. The alkyl group or fatty acid has, for example, 4 to 34 carbon atoms, or preferably 12 to 22 carbon atoms.

[0231] From the viewpoint of more stably suppressing discoloration of the liquid oral composition, component (c) is preferably a nonionic surfactant, more preferably comprises one or more selected from polyoxyethylene hydrogenated castor oil, polyoxyethylene cetyl ether, polyoxyethylene behenyl ether, and polyethylene glycol fatty acid esters, and even more preferably polyoxyethylene hydrogenated castor oil.

[0232] From the viewpoint of improving solubility in water and more stably suppressing discoloration of the liquid oral composition, the HLB value of component (c) is, for example, 13.0 or more, preferably 14.0 or more, and more preferably 15.0 or more.

[0233] The HLB value of the component (c) is, for example, 20.0 or less, preferably 19.0 or less, and more preferably 17.0 or less.

[0234] Here, when the liquid oral composition contains two or more surfactants, the HLB value can be determined as the sum of the products of the HLB values ​​and the mass fractions of the respective surfactants.

[0235] From the viewpoint of more stably solubilizing the oily component and more stably suppressing discoloration of the liquid oral composition, the content of component (c) in the liquid oral composition is preferably 0.1% by mass or more, more preferably 0.5% by mass or more, even more preferably 0.8% by mass or more, even more preferably 1.0% by mass or more, and even more preferably 1.5% by mass or more, relative to the entire liquid oral composition.

[0236] From the viewpoint of suppressing bitterness and astringency and adjusting taste, the content of component (c) in the liquid oral composition is preferably 10% by mass or less, more preferably 7.5% by mass or less, and even more preferably 5% by mass or less, relative to the entire liquid oral composition.

[0237] From the viewpoint of suppressing discoloration over time of the liquid oral composition, the mass ratio (c) / ((a) + (b)) of the content of component (c) to the total content of components (a) and (b) is preferably 3.5 or more, more preferably 4.0 or more, even more preferably 4.5 or more, even more preferably 5.0 or more, and even more preferably 5.5 or more.

[0238] From the viewpoint of suppressing bitterness and astringency and adjusting taste, the mass ratio (c) / ((a)+(b)) is preferably 50 or less, more preferably 40 or less, further preferably 30 or less, and even more preferably 20 or less.

[0239] (ingredient (d))

[0240] Component (d) is a copper compound. By further comprising component (d), the liquid oral composition can enhance the effect of suppressing bad breath, etc. Specific examples of component (d) include water-soluble copper salts.

[0241] Specifically, the water-soluble copper salt refers to a water-soluble copper salt among inorganic and organic copper salts. The water-soluble copper salt may be either an anhydrate or a hydrate. The water-soluble copper salt may be any copper salt that can be used as a raw material for pharmaceuticals, foods, or cosmetics, for example.

[0242] In addition, examples of water-soluble copper salts include one or more selected from copper gluconate, copper sulfate, copper citrate, copper chlorophyllin, and sodium copper chlorophyllin. From the perspective of further enhancing the effect of inhibiting bad breath, such as the effect of combining water-soluble copper salts, the water-soluble copper salt preferably includes at least one of copper gluconate and copper sulfate, and more preferably copper gluconate.

[0243] As the water-soluble copper salt, for example, a commercially available item can be used.

[0244] From the viewpoint of further enhancing the effect of incorporating the water-soluble copper salt, such as the effect of suppressing bad breath, the content of component (d) in the liquid oral composition is preferably 0.001% by mass or more, more preferably 0.01% by mass or more, further preferably 0.03% by mass or more, and even more preferably 0.08% by mass or more, relative to the entire liquid oral composition.

[0245] Furthermore, from the viewpoint of reducing an unpleasant feeling during use such as a metallic taste, the content of component (d) in the liquid oral composition is preferably 10% by mass or less, more preferably 1% by mass or less, even more preferably 0.5% by mass or less, even more preferably 0.3% by mass or less, and even more preferably 0.2% by mass or less, relative to the entire liquid oral composition.

[0246] Furthermore, from the viewpoint of further enhancing the effect of the addition of component (d), such as the effect of suppressing bad breath, the content of component (d) in the liquid oral composition is preferably 0.001% by mass or more, and more preferably 0.01% by mass or more, based on the amount of copper added.

[0247] From the viewpoint of reducing unpleasant sensations such as metallic taste, the content of component (d) in the liquid oral composition is preferably 0.06% by mass or less, more preferably 0.03% by mass or less, based on the amount of copper incorporated.

[0248] From the viewpoint of suppressing discoloration over time of the liquid oral composition, the mass ratio (c) / ((a) + (b) + (d)) of the content of component (c) to the total content of components (a), (b), and (d) is preferably 2.6 or more, more preferably 3.0 or more, and even more preferably 4.0 or more.

[0249] In addition, from the viewpoint of suppressing bitterness and astringency and adjusting taste, the mass ratio (c) / ((a)+(b)+(d)) is preferably 50 or less, more preferably 40 or less, further preferably 30 or less, and even more preferably 20 or less.

[0250] (water)

[0251] Liquid oral compositions specifically comprise water.

[0252] The content of water in the liquid oral composition may be, for example, the remainder obtained by removing components other than water from the liquid oral composition.

[0253] The water content in the liquid oral composition is preferably 50% by mass or more, more preferably 60% by mass or more, and even more preferably 70% by mass or more, relative to the entire liquid oral composition. For example, it is 99.98% by mass or less, preferably 99.88% by mass or less, more preferably 99.5% by mass or less, and even more preferably 99% by mass or less.

[0254] (Ethanol)

[0255] The liquid oral composition may further comprise ethanol.

[0256] From the viewpoint of appropriately imparting a refreshing and good feeling during use, the ethanol content in the liquid oral composition is preferably 0.1% by mass or more, more preferably 1% by mass or more, and even more preferably 2% by mass or more.

[0257] In addition, from the perspective of suppressing strong irritation in the oral cavity, the ethanol content in the liquid oral composition is preferably 30% by mass or less, more preferably 20% by mass or less, even more preferably 15% by mass or less, even more preferably 10% by mass or less, even more preferably 7.5% by mass or less, and even more preferably 5% by mass or less. From the same perspective, it is also preferred that the liquid oral composition does not contain ethanol, that is, the ethanol content is 0% by mass, or that the liquid oral composition contains ethanol and the content is 5% by mass or less.

[0258] (Other ingredients)

[0259] Compositions such as liquid oral compositions may contain components other than the above components within a range not impairing the effects of the present invention.

[0260] Examples of such ingredients include pharmaceutical ingredients, binders, wetting agents, flavoring agents, preservatives, colorants, pH adjusters, solvents, solubilizers, bases, detergents, adsorbents, and the like, which can be appropriately selected depending on the dosage form. Specific examples of the additives are shown below, but the ingredients that can be incorporated into the present invention are not limited to these.

[0261] Examples of the medicinal ingredients include one or more selected from antiseptics, anti-inflammatory agents, blood circulation enhancers, tartar deposit inhibitors, stain removers, anti-sensitivity agents, vitamins, and plaque-degrading enzymes. These medicinal ingredients are not limited as long as they can be used in pharmaceuticals.

[0262] Among the medicinal ingredients, examples of the bactericide include one or more selected from isopropylmethylphenol, cetylpyridinium chloride, benzalkonium chloride, benzethonium chloride, hinokitiol, chlorhexidine hydrochloride, alkylbis(aminoethyl)glycine hydrochloride, sodium lauroyl sarcosinate, and triclosan.

[0263] As anti-inflammatory agents, for example, one or more selected from the group consisting of β-glycyrrhetinic acid, glycyrrhetinic acid, glycyrrhizic acid, diammonium glycyrrhizate, disodium glycyrrhizate, trisodium glycyrrhizate, dipotassium glycyrrhizate, monoammonium glycyrrhizate, ε-aminocaproic acid, sodium azulenesulfonate hydrate, allantoin, aluminum dihydroxyallantoin, epidihydrocholesterol, dihydrocholesterol and lysozyme hydrochloride can be cited.

[0264] As a blood circulation promoting agent, sodium chloride is mentioned, for example.

[0265] Examples of dental calculus deposit inhibitors include one or more selected from disodium hydrogen phosphate, disodium dihydrogen pyrophosphate, sodium pyrophosphate, anhydrous sodium pyrophosphate, tetrasodium pyrophosphate (anhydrous), disodium hydrogen phosphate, sodium hydrogen phosphate hydrate, disodium hydrogen phosphate (crystalline), trisodium phosphate, and sodium polyphosphate.

[0266] Examples of the stain remover include one or more selected from MACROGOL (MACROGOL 200, MACROGOL 300, MACROGOL 400, MACROGOL 600, MACROGOL 1000, MACROGOL 1500, MACROGOL 1540, MACROGOL 4000, MACROGOL 6000, MACROGOL 20000, etc.), sodium polyphosphate, and polyvinyl pyrrolidone.

[0267] Examples of the anti-sensitizing agent include at least one selected from potassium nitrate and water-soluble aluminum salts.

[0268] Examples of vitamins include one or more selected from ascorbic acid, L-ascorbic acid, sodium ascorbate, sodium L-ascorbate, pyridoxine hydrochloride, DL-α-tocopheryl acetate, tocopheryl acetate, dl-α-tocopheryl nicotinate, and tocopheryl nicotinate.

[0269] Examples of plaque-decomposing enzymes include glucanase.

[0270] Examples of the binder include one or more selected from organic binders such as pullulan, gelatin, methylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, sodium carboxymethylcellulose, carrageenan, sodium alginate, xanthan gum, sodium polyacrylate, gum arabic, guar gum, locust bean gum, polyvinyl alcohol, and carboxyvinyl polymers, thickening anhydrous silicic acid, and bentonite.

[0271] Here, from the viewpoint of easy cleaning of the oral cavity, the liquid oral composition preferably does not contain xanthan gum, and more preferably does not contain a binder.

[0272] Here, the liquid oral composition containing no xanthan gum or binder specifically means that xanthan gum or binder is not intentionally added to the liquid oral composition. More specifically, it means that the content of xanthan gum or binder is 0.001% by mass or less based on the entire liquid oral composition.

[0273] As the wetting agent, any wetting agent that can be sold as a raw material for medicines, foods, or cosmetics may be used. For example, polyols can be mentioned, and more specifically, one or more selected from sorbitol, glycerin, concentrated glycerin, ethylene glycol, propylene glycol, 1,3-butylene glycol, isopropylene glycol (1,3-propanediol), polyethylene glycol, polypropylene glycol, sodium hyaluronate, and hydrolyzed collagen can be mentioned.

[0274] From the viewpoint of reducing irritation to the oral cavity, the humectant is preferably at least one selected from glycerin and propylene glycol, and more preferably glycerin.

[0275] From the viewpoint of achieving a more appropriate viscosity of the liquid oral composition, the content of the humectant in the liquid oral composition is preferably 1% by mass or more, more preferably 3% by mass or more, and even more preferably 5% by mass or more, and is preferably 30% by mass or less, more preferably 25% by mass or less, and even more preferably 20% by mass or less.

[0276] Examples of flavoring agents include monosodium L-glutamate, saccharin, saccharin sodium, sucrose, glucose, fructose, lactose, honey, aspartame, stevia, sucralose, inositol, D-sorbitol, D-mannitol, arabitol, raffinose, lactulose, lactitol, xylitol, erythritol, reduced isomaltulose, isomaltulose, PALATINIT (registered trademark), acesulfame potassium, trehalose, maltose, stachyose or maltitol, neohesperidin dihydrochalcone, perilla frutescens, p-methoxycinnamaldehyde, and thaumatin.

[0277] From the viewpoint of having a strong sweet taste and being able to adjust the taste even in a small amount, the flavoring agent is preferably at least one selected from xylitol, sodium saccharin, and saccharin, and more preferably at least one selected from xylitol and sodium saccharin.

[0278] From the viewpoint of appropriately imparting a refreshing and good feeling during use, the content of the flavoring agent in the liquid oral composition is preferably 0.01% by mass or more, more preferably 0.05% by mass or more, and even more preferably 0.1% by mass or more, and is preferably 2% by mass or less, more preferably 1% by mass or less, and even more preferably 0.5% by mass or less.

[0279] Examples of preservatives include sodium benzoate, methyl parahydroxybenzoate, ethyl parahydroxybenzoate, butyl parahydroxybenzoate, isopropyl parahydroxybenzoate, propyl parahydroxybenzoate, isobutyl parahydroxybenzoate, benzyl parahydroxybenzoate and the like; alcohols such as phenoxyethanol; sorbic acid, benzoic acid, dehydroacetic acid, propionic acid and salts thereof; ethylenediaminetetraacetate and alkyldi(aminoethyl)glycine hydrochloride, or two or more thereof.

[0280] As coloring agents, for example, natural pigments selected from safflower red pigment, gardenia yellow pigment, gardenia blue pigment, perilla pigment, red yeast rice pigment, red cabbage pigment, carrot pigment, hibiscus pigment, cocoa pigment, spirulina blue pigment, coumarin pigment, etc.; legal pigments such as Red No. 3, Red No. 104, Red No. 105, Red No. 106, Yellow No. 4, Yellow No. 5, Green No. 3, Blue No. 1; one or more of riboflavin and titanium dioxide.

[0281] Examples of the pH adjuster include one or more selected from acids, bases, and buffers such as acetic acid, hydrochloric acid, sulfuric acid, nitric acid, citric acid, phosphoric acid, malic acid, gluconic acid, maleic acid, succinic acid, glutamic acid, pyrophosphoric acid, tartaric acid, acetic acid, sodium hydroxide, potassium hydroxide, sodium acetate, sodium carbonate, sodium citrate, sodium hydrogen citrate, phosphoric acid, sodium phosphate, disodium hydrogen phosphate, sodium dihydrogen phosphate, and potassium dihydrogen phosphate.

[0282] Examples of the solvent include water as described above and lower alcohols such as propanol.

[0283] In order to promote the dissolution of the above-mentioned additives and medicinal ingredients in water, a solubilizing agent may be added. Examples of such a solubilizing agent include polyols such as dipropylene glycol.

[0284] As a base, sodium bicarbonate is mentioned, for example.

[0285] As a cleaning agent, sodium polyphosphate is mentioned, for example.

[0286] Examples of the adsorbent include β-cyclodextrin.

[0287] Furthermore, in addition to the above-mentioned components, components suitable for the use of oral compositions such as liquid oral compositions can be appropriately blended within a range that does not impair the scope of the present invention.

[0288] (Viscosity)

[0289] In the present embodiment, from the viewpoint of easy cleaning of the oral cavity, the viscosity of the liquid oral composition is preferably 25 mPa·s or less, more preferably 10 mPa·s or less, and even more preferably 7.5 mPa·s or less.

[0290] The viscosity of the liquid oral composition may be, for example, 0.1 mPa·s or more.

[0291] Specifically, the viscosity of the liquid oral composition can be measured using a B-type viscometer (e.g., Brookfield Rotational Viscometer DV3T, manufactured by Brookfield) at room temperature of 25±3°C, Rotor LV-1, rotation speed of 200 rpm, and measurement time of 1 minute.

[0292] (Liquid preparation)

[0293] In addition, the liquid oral composition is specifically a liquid preparation. The liquid preparation is specifically an oral preparation.

[0294] Specific embodiments of the liquid oral composition include one selected from mouthwash, liquid toothpaste, and mouth freshener. The liquid oral composition is preferably mouthwash.

[0295] (Manufacturing Method)

[0296] In the present embodiment, the method for producing the liquid oral composition includes, for example, a step of blending components (a) and (b) and other appropriate components.

[0297] Here, in order to obtain the color difference ΔE *To achieve a liquid oral composition within the above range, it is important to appropriately select the components and blending ratios contained in the liquid oral composition. Furthermore, it is also preferred to optimize the production process of the liquid oral composition.

[0298] For example, it is important to appropriately select the amounts of components (a) and (b) contained in the liquid oral composition and design the formulation in combination. In addition, it is preferred to further incorporate component (c) into the liquid oral composition, and it is also preferred to further incorporate components (c) and (d).

[0299] In addition, in the production process of the liquid oral composition, it is also preferred that a liquid containing component (a), as well as (d) as appropriate, and water is heated to, for example, about 80°C to obtain liquid 1, and a liquid containing component (b) and as appropriate (c) is separately heated and dissolved at, for example, about 80°C to obtain liquid 2, liquids 1 and 2 are mixed, and water is added as appropriate, and the mixture is further mixed to obtain the liquid oral composition.

[0300] The liquid oral composition obtained in this embodiment contains components (a) and (b), and the color difference ΔE * Within the specific range, discoloration with time can be appropriately suppressed.

[0301] In addition, in this embodiment, the method for suppressing discoloration of the liquid oral composition includes reducing the color difference ΔE of the liquid oral composition containing the above components (a) and (b) to * It is 0.0~2.5.

[0302] In addition, in the present embodiment, the method for suppressing discoloration of the oral composition may include adding peppermint oil to the oral composition containing at least one of the components (a) and (d).

[0303] While the embodiments of the present invention have been described above, these are merely examples of the present invention, and various configurations other than those described above may be employed.

[0304] For example, the present invention includes the following aspects.

[0305] [A1] A liquid oral composition comprising the following components (a) to (c):

[0306] (a) at least one selected from tranexamic acid and a salt thereof,

[0307] (b) spices, and

[0308] (c) surfactants with an HLB value of 13.0 to 20.0,

[0309] The mass ratio (c) / ((a)+(b)) of the content of the component (c) to the total content of the components (a) and (b) is 3.5 or more.

[0310] [A2] The liquid oral composition according to [A1], further comprising a component (d): a copper compound.

[0311] [A3] The liquid oral composition according to [A1] or [A2], wherein when the liquid oral composition contains ethanol, the content of ethanol in the liquid oral composition is 30% by mass or less.

[0312] [A4] The liquid oral composition according to any one of [A1] to [A3], wherein the liquid oral composition does not contain ethanol, or contains ethanol and the ethanol content in the liquid oral composition is 5% by mass or less.

[0313] [A5] The liquid oral composition according to any one of [A1] to [A4], wherein the component (b) comprises one or more selected from lavender oil, peppermint oil, and bergamot oil.

[0314] [A6] The liquid oral composition according to any one of [A1] to [A5], wherein the component (c) comprises one or more selected from polyoxyethylene hydrogenated castor oil, polyoxyethylene cetyl ether, polyoxyethylene behenyl ether, and polyethylene glycol fatty acid ester.

[0315] [A7] A method for inhibiting discoloration of a liquid oral composition, comprising: adding a component (c): a surfactant having an HLB value of 13.0 to 20.0 to a liquid oral composition containing (a) at least one selected from tranexamic acid and its salts and (b) a flavoring, so that the mass ratio (c) / ((a)+(b)) of the content of the above-mentioned component (c) relative to the total content of the above-mentioned components (a) and (b) is 3.5 or more.

[0316] [B1] A liquid oral composition comprising (a) at least one selected from tranexamic acid and its salts, and (b) a flavoring,

[0317] The color difference ΔE was measured by the following method and obtained using the following formula (I): * It is 0.0~2.5.

[0318] (method)

[0319] The chromaticity coordinates of each sample of the liquid oral composition after storage at 25°C and 60°C for 4 weeks were measured using a spectrocolorimeter under the following conditions in accordance with JIS Z 8722, and CIE 1976L was obtained based on the measured values. * a * b * The chromaticity coordinates specified in the color system are used to calculate the color difference ΔE* .

[0320] Type of measurement method: Spectrophotometric method

[0321] Types of color functions: X, Y, and Z values

[0322] Type of standard illuminant for color measurement: D65 light source / viewing angle 10°

[0323] Geometric conditions of illumination and light reception: Transmission (0°: 0°)

[0324] Wavelength: Measurement wavelength 380nm ~ 780nm, measurement interval: 5nm

[0325] ΔE * ={(L * 2-L * 1) 2 +(a * 2-a * 1) 2 +(b * 2-b * 1) 2} 1 / 2 (I)

[0326] (In the above formula (I), (L * 1.a * 1.b * 1) and (L * 2.a * 2. b * 2) CIE1976L of the above sample after being stored at 25°C for 4 weeks and at 60°C for 4 weeks * a * b * Chromaticity coordinates specified in the colorimetric system.)

[0327] [B2] The liquid oral composition according to [B1], wherein Δb is measured by the above method and obtained by the following formula (II): * It is 0 to 3.0.

[0328] Δb * =b * 2-b * 1(II)

[0329] [B3] The liquid oral composition according to [B1] or [B2], further comprising ethanol,

[0330] The content of the ethanol in the liquid oral composition is 15% by mass or less based on the entire liquid oral composition.

[0331] [B4] The liquid oral composition according to any one of [B1] to [B3], wherein the component (b) is peppermint oil.

[0332] [B5] The liquid oral composition according to any one of [B1] to [B4], further comprising component (c): a surfactant having an HLB value of 13.0 to 20.0.

[0333] [B6] The liquid oral composition according to any one of [B1] to [B5], further comprising component (d): a copper compound.

[0334] Example

[0335] The present embodiment will be described in detail below with reference to Examples and Comparative Examples, but the present embodiment is not limited to these Examples.

[0336] (Test Example 1)

[0337] (Examples A1 to A4, Comparative Example A1)

[0338] The components listed in Table 1 were mixed to prepare mouthwashes of each example, and the mouthwashes were evaluated by the method described below. Details of the components listed in each table are shown below.

[0339] (d) Copper gluconate: manufactured by Fuso Chemical Industry Co., Ltd.

[0340] (a) Tranexamic acid: manufactured by Kyowa Pharma Chemical Co., Ltd.

[0341] Polyoxyethylene (40) hydrogenated castor oil, NIKKOL HCO-40, manufactured by Nippon Surfactant Industries, HLB 12.5

[0342] (c) Polyoxyethylene (60) hydrogenated castor oil, NIKKOL HCO-60, manufactured by Nippon Surfactant Industries, Ltd., HLB14

[0343] (c) Polyoxyethylene (100) hydrogenated castor oil, NIKKOL HCO-100, manufactured by Nippon Surfactant Industries, HLB 16.5

[0344] (c) Polyoxyethylene cetyl ether BC-23, manufactured by Nippon Surfactant Industries, Ltd., HLB18

[0345] Ethanol: Made by FUJIFILM Wako Pure Chemical Co., Ltd.

[0346] Glycerin: Made by Kosakai Pharmaceutical Co., Ltd.

[0347] Saccharin sodium: Made by Junsei Chemical Co., Ltd.

[0348] (b) Bergamot oil: manufactured by FUJIFILM Wako Pure Chemical Co., Ltd.

[0349] (b) Lavender oil: manufactured by NacalaiTesque

[0350] (b) Peppermint oil: manufactured by Kosakai Pharmaceutical Co., Ltd.

[0351] (Method for preparing mouthwash)

[0352] Sodium saccharin, glycerin, and water were mixed to the amounts listed in Table 1 and dissolved by stirring in a beaker A. Tranexamic acid was added to the beaker A, and copper gluconate was added as needed to further dissolve the mixture.

[0353] In another beaker B, ethanol, fragrance, and surfactant were added and dissolved in a hot water bath at 80°C.

[0354] Beaker A was also heated to 80°C and placed in beaker B, which was stirred. Beaker B was removed from the hot water bath and further stirred with a stirrer. Water was added to a final volume of 100 g, and further stirred to obtain the mouthwash of each example.

[0355] (Determination of viscosity)

[0356] The viscosity of the mouthwash obtained in each example was measured using a B-type viscometer (Brookfield Rotational Viscometer DV3T, manufactured by Brookfield) at 23°C (room temperature), Rotor LV-1, a rotation speed of 200 rpm, and a measurement time of 1 minute. The measurement results are shown in Table 1.

[0357] (Evaluation method)

[0358] As an indicator of the temporal color change of the mouthwash obtained in each example, the color change after the accelerated test was evaluated by the following method.

[0359] (Evaluated by visual observation)

[0360] The mouthwash obtained in each example was stored at 25°C and 60°C for one month. The degree of discoloration of the sample stored at 60°C relative to the sample stored at 25°C was visually observed and evaluated according to the following criteria. The evaluation results are shown in Table 1.

[0361] ++: Severe discoloration

[0362] +: Discoloration (yellowing)

[0363] ±: There is discoloration but it is within the allowable range (the extent of discoloration can be confirmed by visual observation)

[0364] -: No discoloration (no discoloration was observed by visual observation)

[0365] (Evaluation using a colorimeter)

[0366] Each sample after storage used for evaluation by visual observation was measured using a colorimeter under the following conditions, and ΔE was obtained based on the following formula: * (ab) were evaluated according to the following criteria. The evaluation results are shown in Table 1.

[0367] (Measurement method and conditions)

[0368] (Color difference ΔE * Determination of

[0369] 50 mL of each mouthwash obtained in each example was dispensed into 50 mL glass bottles to obtain specimens 1 and 2. Specimen 1 was stored at 25°C and 60% RH for 4 weeks, and specimen 2 was stored in a thermostatic chamber at 60°C and constant humidity for 4 weeks.

[0370] After storage, each sample was returned to room temperature (25°C) and placed in a measuring cell (No. 1488 5×36×55 mm) of a spectrocolorimeter (SE-7700, manufactured by Nippon Denshoku Industries Co., Ltd.). The chromaticity coordinates (L * 1.a * 1.b * 1) and the chromaticity coordinates of specimen 2 (L * 2.a * 2. b * 2) The measurement was performed once for each sample.

[0371] Type of measurement method: Spectrophotometric method

[0372] Types of color functions: X, Y, and Z values

[0373] Type of standard illuminant for color measurement: D65 light source / viewing angle 10°

[0374] Geometric conditions of illumination and light reception: Geometric condition e, transmission (0°: 0°)

[0375] Wavelength: Measurement wavelength 380nm ~ 780nm, measurement interval: 5nm

[0376] Based on the obtained chromaticity coordinates, the color difference ΔE of each mouthwash was calculated using the following formula (I): * .

[0377] ΔE* (ab)={(L * 2-L * 1) 2 +(a * 2-a * 1) 2 +(b * 2-b * 1) 2} 1 / 2 (I)

[0378] (evaluate)

[0379] For the samples not containing copper compounds (Examples A1 and A2), the following case A was evaluated as acceptable. In addition, for the samples containing copper compounds (Examples A3, A4 and Comparative Example A1), the following cases A and B were evaluated as acceptable, considering the coloring from the copper compounds.

[0380] A: ΔE * (ab)=0~0.5

[0381] B: ΔE * (ab) = greater than 0.5 and less than 2.5

[0382] C:ΔE * (ab)=greater than 2.5

[0383] [Table 1]

[0384]

[0385] As can be seen from Table 1, in each Example, discoloration of the mouthwash after the accelerated test was appropriately suppressed.

[0386] (Test Example 2)

[0387] (Examples B1 to B3, Comparative Example B1)

[0388] The components listed in Table 2 were mixed to prepare mouthwashes of each example, and the mouthwashes were evaluated by the method described below. Details of the components listed in each table are shown below.

[0389] (d) Copper gluconate: manufactured by Fuso Chemical Industry Co., Ltd.

[0390] (a) Tranexamic acid: manufactured by Kyowa Pharma Chemical Co., Ltd.

[0391] (c) Polyoxyethylene (60) hydrogenated castor oil, NIKKOL HCO-60, manufactured by Nippon Surfactant Industries, Ltd., HLB14

[0392] (c) Polyoxyethylene (100) hydrogenated castor oil, NIKKOL HCO-100, manufactured by Nippon Surfactant Industries, HLB 16.5

[0393] Ethanol: Made by FUJIFILM Wako Pure Chemical Co., Ltd.

[0394] Glycerin: Made by Kosakai Pharmaceutical Co., Ltd.

[0395] Saccharin sodium: Made by Junsei Chemical Co., Ltd.

[0396] (b) Peppermint oil: manufactured by Kosakai Pharmaceutical Co., Ltd.

[0397] (Method for preparing mouthwash)

[0398] Sodium saccharin, glycerin, and water were mixed to the amounts shown in Table 2, and stirred and dissolved in beaker A. Tranexamic acid was added to beaker A, and copper gluconate was added as needed to further dissolve the mixture.

[0399] In another beaker B, ethanol, fragrance, and surfactant were added and dissolved in a hot water bath at 80°C.

[0400] Beaker A was also heated to 80°C and placed in beaker B, which was stirred. Beaker B was removed from the hot water bath and further stirred with a stirrer. Water was added to a final volume of 100 g, and further stirred to obtain the mouthwash of each example.

[0401] (Color difference ΔE * Determination of

[0402] 50 mL of each mouthwash obtained in each example was dispensed into 50 mL glass bottles to obtain specimens 1 and 2. Specimen 1 was stored at 25°C and 60% RH for 4 weeks, and specimen 2 was stored in a thermostatic chamber at 60°C and constant humidity for 4 weeks.

[0403] After storage, each sample was returned to room temperature (25°C) and placed in a measuring cell (No. 1488 5×36×55 mm) of a spectrocolorimeter (SE-7700, manufactured by Nippon Denshoku Industries Co., Ltd.). The chromaticity coordinates (L * 1.a * 1.b * 1) and the chromaticity coordinates of specimen 2 (L * 2.a * 2. b * 2) The measurement was performed once for each sample.

[0404] Type of measurement method: Spectrophotometric method

[0405] Types of color functions: X, Y, and Z values

[0406] Type of standard illuminant for color measurement: D65 light source / viewing angle 10°

[0407] Geometric conditions of illumination and light reception: Geometric condition e, transmission (0°: 0°)

[0408] Wavelength: Measurement wavelength 380nm ~ 780nm, measurement interval: 5nm

[0409] Based on the obtained chromaticity coordinates, the color difference ΔE of each mouthwash was calculated using the following formulas (I) and (II): * and Δb * .

[0410] ΔE * ={(L * 2-L * 1) 2 +(a * 2-a * 1) 2 +(b * 2-b * 1) 2} 1 / 2 (I)

[0411] Δb * =b * 2-b * 1 (II)

[0412] (Determination of viscosity)

[0413] The viscosity of the mouthwash obtained in each example was measured using a B-type viscometer (Brookfield Rotational Viscometer DV3T, manufactured by Brookfield) at 25°C (room temperature), Rotor LV-1, a rotation speed of 200 rpm, and a measurement time of 1 minute. The measurement results are shown in Table 2.

[0414] (Evaluation method)

[0415] The color change over time of the mouthwash obtained in each example was evaluated by the following method.

[0416] (Evaluated by visual observation)

[0417] The mouthwash obtained in each example was stored at room temperature (set to 23°C, with temperature and humidity adjusted as needed) for 10 months. The degree of discoloration of the samples after storage relative to the samples immediately after production was visually observed and evaluated according to the following criteria. The evaluation results are shown in Table 2.

[0418] ++: Severe discoloration

[0419] +: Discoloration (yellowing)

[0420] ±: There is discoloration but it is within the allowable range (the extent of discoloration can be confirmed by visual observation)

[0421] -: No discoloration (no discoloration was observed by visual observation)

[0422] [Table 2]

[0423]

[0424] As can be seen from Table 2, in each Example, the temporal discoloration of the mouthwash was appropriately suppressed.

[0425] This application claims priority based on Japanese patent application No. 2023-024143 and No. 2023-024144 filed on February 20, 2023, the disclosures of which are incorporated herein in their entirety.

Claims

1. A liquid oral composition comprising the following components (a) and (b): (a) at least one selected from tranexamic acid and a salt thereof, (b) spices; The liquid oral composition satisfies at least one of the following conditions 1 and 2, Condition 1: Further containing the following ingredient (c): (c) surfactants with an HLB value of 13.0 to 20.0, The mass ratio (c) / ((a)+(b)) of the content of the component (c) to the total content of the components (a) and (b) is 3.5 or more, Condition 2: The color difference ΔE was measured by the following method and obtained using the following formula (I): * 0.0~2.5, method: The chromaticity coordinates of each sample of the liquid oral composition after storage at 25°C and 60°C for 4 weeks were measured using a spectrocolorimeter under the following conditions in accordance with JIS Z 8722, and CIE 1976L was obtained based on the measured values. * a * b * The chromaticity coordinates specified in the color system are used to calculate the color difference ΔE * , Type of measurement method: Spectrophotometric method Types of color functions: X, Y, and Z values Type of standard illuminant for color measurement: D65 light source / viewing angle 10° Geometric conditions of illumination and light reception: Transmission (0°: 0°) Wavelength: Measurement wavelength 380nm ~ 780nm, measurement interval: 5nm ΔE * ={(L * 2-L * 1) 2 +(a * 2-a * 1) 2 +(b * 2-b * 1) 2 } 1 / 2 (I) In the formula (I), (L * 1.a * 1.b * 1) and (L * 2.a * 2. b * 2) CIE1976L of the sample after being stored at 25°C for 4 weeks and at 60°C for 4 weeks * a * b * Chromaticity coordinates specified in a colorimetric system. The liquid oral composition according to claim 1 , which satisfies condition 1.

3. The liquid oral composition according to claim 1 or 2, wherein Further comprising component (d): a copper compound.

4. The liquid oral composition according to any one of claims 1 to 3, wherein When the liquid oral composition contains ethanol, the content of ethanol in the liquid oral composition is 30% by mass or less.

5. The liquid oral composition according to any one of claims 1 to 4, wherein The liquid oral composition does not contain ethanol, or the liquid oral composition contains ethanol and the content of ethanol in the liquid oral composition is 5% by mass or less.

6. The liquid oral composition according to any one of claims 1 to 5, wherein The component (b) comprises one or more selected from lavender oil, peppermint oil and bergamot oil.

7. The liquid oral composition according to any one of claims 1 to 6, wherein The component (c) comprises one or more selected from polyoxyethylene hydrogenated castor oil, polyoxyethylene cetyl ether, polyoxyethylene behenyl ether and polyethylene glycol fatty acid ester. The liquid oral composition according to claim 1 or 2, which satisfies condition 2.

9. The liquid oral composition according to claim 8, wherein Δb is determined by the above method and obtained using the following formula (II): * 0 to 3.0, Δb * =b * 2-b * 1(II).

10. The liquid oral composition according to claim 8 or 9, wherein further comprising ethanol, The content of the ethanol in the liquid oral composition is 15% by mass or less based on the entire liquid oral composition.

11. The liquid oral composition according to any one of claims 8 to 10, wherein The component (b) is peppermint oil.

12. The liquid oral composition according to any one of claims 8 to 11, wherein The invention further comprises a component (c): a surfactant having an HLB value of 13.0 to 20.

0.

13. The liquid oral composition according to any one of claims 8 to 12, wherein Further comprising component (d): a copper compound.

14. A method for inhibiting discoloration of a liquid oral composition, comprising: A liquid oral composition containing (a) at least one selected from tranexamic acid and its salts and (b) a flavoring is blended with a component (c): a surfactant having an HLB value of 13.0 to 20.0, such that the mass ratio (c) / ((a) + (b)) of the content of the component (c) to the total content of the components (a) and (b) is 3.5 or more.

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