Oral composition
By adding sodium fluoride and sodium monofluorophosphate to the oral composition, controlling their content, and combining them with a specific anionic surfactant, the problems of enzyme inactivation and reduced foaming properties caused by anionic surfactants were solved, achieving enzyme activity stability and good foaming properties.
Patent Information
- Application Number
- CN202511105738.9
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Priority Date
- 2024-08-26
- Filing Date
- 2025-08-08
- Publication Date
- 2026-02-10
AI Technical Summary
When anionic surfactants and enzymes are used together in oral compositions, it is difficult to balance the activity stability and foaming properties of the enzyme, especially since anionic surfactants can lead to enzyme inactivation and reduced foaming properties.
By adding sodium fluoride and/or sodium monofluorophosphate to the oral composition, controlling their content to be 3000ppm to 20000ppm, the activity stability of the enzyme is ensured, and good foaming properties are maintained by combining anionic surfactants such as alkyl sulfates and tetradecene sulfonates.
It achieves enzyme activity stability and good foaming properties in the presence of anionic surfactants, thus improving the user experience.
Smart Images

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Abstract
Description
Technical Field
[0001] This invention relates to a composition for oral use. Background Technology
[0002] Previously, various enzymes have been incorporated into oral care compositions from the perspectives of preventing and inhibiting the development of dental caries, preventing halitosis, and improving the aesthetics of teeth. Among the enzymes that can be incorporated into oral care compositions, dextranase is known to achieve a caries-preventing effect by breaking down dental plaque.
[0003] On the other hand, from the viewpoint of improving the user experience and usability, surfactants are usually incorporated into oral care compositions. Examples of surfactants incorporated into oral care compositions include anionic surfactants, which are formulated to ensure adequate foaming properties.
[0004] However, anionic surfactants incorporated into oral compositions may modify or deactivate enzymes.
[0005] Therefore, techniques for stabilizing enzyme activity, especially in cases where anionic surfactants and enzymes are used together, are indispensable.
[0006] In the past, when dextranase was incorporated into oral compositions as an enzyme, it was known to incorporate specific amphoteric surfactants or nonionic surfactants from the viewpoint of ensuring the stabilization of dextranase activity.
[0007] Specifically, for example, Patent Document 1 describes a compound carboxylic acid type amphoteric surfactant, Patent Document 2 describes a compound polyoxyethylene alkyl ether, Patent Document 3 describes a compound glycerol fatty acid ester, and Patent Document 4 describes a compound fatty acid diethanolamide. Existing technical documents Patent documents
[0008] Patent Document 1: Japanese Patent Application Publication No. 58-225007 Patent Document 2: Japanese Patent Application Publication No. 61-176518 Patent Document 3: Japanese Patent Application Publication No. 03-181413 Patent Document 4: Japanese Patent Application Publication No. 08-12543 Summary of the Invention The technical problem that the invention aims to solve
[0009] However, when anionic surfactants and enzymes are used together, if a large amount of surfactants disclosed in the aforementioned patent documents, such as nonionic surfactants, are added, the excellent foaming properties brought about by anionic surfactants may be reduced.
[0010] Therefore, the object of the present invention is to provide an oral composition that, even when used in combination with anionic surfactants and enzymes, ensures, in particular, the stability of enzyme activity and excellent user experience such as foaming properties. Technical solutions for solving technical problems
[0011] That is, the present invention provides the following [1] to [9]. [1] An oral composition, characterized in that it contains: Component (A) is one or both of sodium fluoride and sodium monofluorophosphate. Component (B) enzymes, and Component (C) is an anionic surfactant. The content of component (A), converted to fluoride ion concentration, is 3000ppm to 20000ppm. [2] According to the oral composition described in [1], wherein component (B) is one or both of glucanase and protease. [3] The oral composition according to [1] or [2], wherein component (B) comprises one or more selected from dextranase, mutagenase, kiwi protease, papain and bromelain. [4] An oral composition according to any one of [1] to [3], wherein component (C) is one or both of alkyl sulfate and tetradecene sulfonate. [5] An oral composition according to any one of [1] to [4], wherein component (A) is sodium fluoride and the content of sodium fluoride is 0.6% to 4.5% by mass. [6] An oral composition according to any one of [1] to [4], wherein component (A) is sodium monofluorophosphate and the content of sodium monofluorophosphate is 2.2% to 15.2% by mass. [7] The oral composition described in any one of [1] to [6], wherein the content of component (A) is 4,000 ppm to 15,000 ppm in terms of fluoride ion concentration. [8] The oral composition according to any one of [1] to [7], wherein the ratio of the concentration of fluoride ions corresponding to the content of component (A) to the content of component (C) (A) / (C) is 1,500 to 50,000. [9] The oral composition described in any one of [1] to [8], wherein the oral composition is a dental cleaning agent. Invention Effects
[0012] According to the present invention, an oral composition can be provided in which the stability of enzyme activity can be ensured even when anionic surfactants and enzymes are used in the oral composition, by adding a specified amount of sodium fluoride and / or sodium monofluorophosphate, and it has good foaming properties, or in other words, excellent user experience such as good foaming. Detailed Implementation
[0013] The present invention will now be described in detail. The oral composition of the present invention contains one or both of sodium fluoride and sodium monofluorophosphate (A), an enzyme (B), and an anionic surfactant (C). The content of component (A) is 3,000 ppm to 20,000 ppm when converted from fluoride ion concentration.
[0014] First, the components (A), (B), and (C) contained in the oral composition of this embodiment will be described.
[0015] [Ingredient (A) Sodium fluoride and / or sodium monofluorophosphate] In the embodiments of the present invention, “(A) component” is sodium fluoride and / or sodium monofluorophosphate.
[0016] In this embodiment, component (A) is a component that provides stability to impart enzyme activity to the oral composition, even when used in combination with anionic surfactants and enzymes.
[0017] In this embodiment, from the viewpoint of ensuring the stability of enzyme activity and good foaming properties (i.e., foaming) during use, the content of component (A), calculated in terms of fluoride ion concentration, is preferably 3000 ppm or more, more preferably 4000 ppm or more, preferably 20000 ppm or less, more preferably 15000 ppm or less, preferably 3000 ppm to 20000 ppm, more preferably 3000 ppm to 15000 ppm, and even more preferably 4000 ppm to 15000 ppm.
[0018] More specifically, for example, when component (A) is sodium fluoride, from the viewpoint of ensuring the stability of enzyme activity and further improving shape retention, when the total amount of the oral composition is set to 100% by mass, the content of sodium fluoride is preferably 0.6% by mass or more, more preferably 0.8% by mass or more, preferably 4.5% by mass or less, more preferably 3.4% by mass or less, preferably 0.6% by mass to 4.5% by mass, more preferably 0.8% by mass to 3.4% by mass.
[0019] Furthermore, for example, when component (A) is sodium monofluorophosphate, from the viewpoint of ensuring the stability of enzyme activity and further improving shape retention, when the total amount of the oral composition is set to 100% by mass, the content of sodium monofluorophosphate is preferably 2.2% by mass or more, more preferably 3.0% by mass or more, preferably 15.2% by mass or less, more preferably 11.4% by mass or less, preferably 2.2% by mass to 15.2% by mass, more preferably 3.0% by mass to 11.4% by mass.
[0020] [Component (B) Enzyme] Component (B) is an enzyme. In this embodiment, the enzyme may have activities that are useful to the oral composition, such as aiding in the decomposition and removal of dental plaque (biofilm) on the tooth surface, in periodontal pockets, and on the tongue, preventing tooth decay, and inhibiting its development. There are no particular limitations on these activities.
[0021] As component (B) enzyme in this embodiment, glucanase and / or protease are preferred, that is, glucanase that can decompose glucans contained in dental plaque, which may be the cause of tooth decay, or that is the cause of dental plaque formation, and / or protease that can decompose proteins contained in tongue coating and stains in addition to dental plaque.
[0022] More specifically, the enzyme component (B) in this embodiment is more preferably selected from one or more of dextranase, mutagenase, actinidin, papain and bromelain.
[0023] In this embodiment, when component (B) is dextranase, from the viewpoint of effectively preventing tooth decay and inhibiting its development by decomposing dental plaque, and further suppressing the astringent taste during use, the amount of component (B), when measured by enzyme activity, is preferably 2 U / g or more, more preferably 10 U / g or more, preferably 200 U / g or less, more preferably 100 U / g or less, preferably 2 U / g to 200 U / g, and more preferably 10 U / g to 100 U / g. More specifically, for example, when using dextranase with an enzyme activity of 4000 U / g, and setting the total amount of the oral composition to 100% by mass, it is preferably 0.05% by mass to 5% by mass.
[0024] In this embodiment, when component (B) is papain, from the viewpoint of effectively breaking down tongue coating and stains and further suppressing the generation of astringent taste during use, the amount of component (B), when measured by enzyme activity, is preferably 400 U / g or more, more preferably 2000 U / g or more, preferably 40000 U / g or less, more preferably 10000 U / g or less, preferably 400 U / g to 40000 U / g, and more preferably 2000 U / g to 10000 U / g. More specifically, for example, when using papain with an enzyme activity of 800000 U / g, and setting the total amount of the oral composition to 100% by mass, it is preferably set to 0.05% by mass to 5% by mass.
[0025] [Component (C) Anionic surfactant] In this embodiment, "Component (C)" is an anionic surfactant. Anionic surfactants can impart foaming properties (i.e., foaming) to oral compositions that are liquid (gel) or paste-like dental cleaning compositions, thereby improving the user experience when brushing teeth with a toothbrush or similar device.
[0026] In this embodiment, as component (C), anionic surfactants include, for example, α-olefin sulfonates such as tetradecene sulfonate, N-acyl sulfonates, alkyl sulfates, N-acyl taurate such as sodium methyl lauroyl taurate, N-acyl amino acid salts such as sodium lauroyl sarcosinate and sodium lauroyl glutamate, and sulfates of glycerol fatty acid esters.
[0027] In this embodiment, as component (C), an anionic surfactant, specifically, one or both of alkyl sulfate and tetradecene sulfonate are preferably used.
[0028] In this embodiment, the amount of the anionic surfactant in component (C) is not particularly limited, provided that it does not impair the effect of the present invention.
[0029] From the viewpoint of ensuring the stability of enzyme activity and further ensuring good foaming properties (i.e., foaming) during use to improve the user experience, when the total amount of the oral composition is set to 100% by mass, the amount of the anionic surfactant in component (C) is preferably 0.1% by mass or more, more preferably 0.5% by mass or more, preferably 3.0% by mass or less, more preferably 1.5% by mass or less, preferably 0.1% to 3.0% by mass, and more preferably 0.5% to 1.5% by mass.
[0030] [Contains ratio] -Ingredient (A) / Ingredient (C)- From the viewpoint of ensuring the stability of enzyme activity and further ensuring good foaming properties during use to improve the user experience, the ratio of fluoride ion concentration corresponding to the content of component (A) to the content of component (C) (component (A) / component (C)) is preferably 1,500 to 50,000, more preferably 3,000 to 20,000.
[0031] [Any ingredients] The oral composition of this embodiment may contain any component other than components (A) to (C) already described, without impairing the effects of the present invention. Detailed description will follow.
[0032] As any component, when the oral composition is a dental cleaning composition (liquid dental cleaning agent, gel dental cleaning agent, and toothpaste), examples include solvents, surfactants, sweeteners, flavorings, pharmaceutical ingredients, oily ingredients, preservatives, humectants, abrasives, binders, pH adjusters, and colorants (pigments). When the oral composition is a mouthwash, examples include solvents, humectants, surfactants, sweeteners, preservatives, pH adjusters, and flavorings. Specific details will be provided below.
[0033] It should be noted that the content of each component in this specification is based on the amount of each component added when manufacturing the oral composition.
[0034] -solvent- The oral composition of this embodiment may further include a solvent. Water (purified water) or ethanol are preferred as solvents.
[0035] -surfactant- The oral composition of this embodiment may further include a surfactant. Examples of surfactants that can be used in oral compositions include nonionic surfactants and amphoteric surfactants.
[0036] Examples of nonionic surfactants include polyoxyethylene alkyl ethers, polyoxyethylene hydrogenated castor oil, sorbitan fatty acid esters, polyoxyethylene sorbitan fatty acid esters (e.g., polyoxyethylene sorbitan monostearate), alkanolamides, polyoxyethylene fatty acid esters, polyoxyethylene alkenyl ethers, glycerol fatty acid esters, sucrose fatty acid esters (e.g., maltose fatty acid esters), sugar alcohol fatty acid esters (e.g., maltitol fatty acid esters, lactitol fatty acid esters), fatty acid diethanolamides (e.g., lauric acid mono- or diethanolamides), polyoxyethylene polyoxypropylene copolymers, and polyoxyethylene polyoxypropylene fatty acid esters. The alkyl chain of polyoxyethylene alkyl ethers typically has 14 to 18 carbon atoms, and the average molar number of ethylene oxide addition is typically 5 to 30 moles. The average molar number of ethylene oxide addition in polyoxyethylene hydrogenated castor oil is typically 20 to 100 moles, preferably 20 to 60 moles. The fatty acids in sorbitan fatty acid esters typically have 12 to 18 carbon atoms. The fatty acids in polyoxyethylene sorbitan fatty acid esters typically have 16 to 18 carbon atoms, and the average molar number of ethylene oxide additions is typically 10 to 40 moles. The alkyl chains of alkanolamides typically have 12 to 14 carbon atoms. As nonionic surfactants, polyoxyethylene hydrogenated castor oil, polyoxyethylene sorbitan fatty acid esters, and polyoxyethylene alkyl ethers are preferred.
[0037] Examples of amphoteric surfactants include: alkyl dimethylaminoacetic acid betaine (e.g., lauryl dimethylaminoacetic acid betaine), fatty acid amide propyl dimethylaminoacetic acid betaine (e.g., cocamidopropyl betaine), and other betaine-type amphoteric surfactants; N-fatty acyl-N-carboxymethyl-N-hydroxyethyl ethylenediamine salts (e.g., N-cocofatty acyl-N-carboxymethyl-N-hydroxyethyl imidazoline betaine), coconut fatty acid imidazoline betaine, 2-alkyl-N-carboxymethyl-N-hydroxyethyl imidazoline betaine, and other imidazoline-type amphoteric surfactants; and alkyl betaines such as lauryl dimethylaminoacetic acid betaine.
[0038] When the total amount of the oral composition is set to 100% by mass, the content of any surfactant, except for the content of the anionic surfactant already described (C), is generally 0.001% by mass or more, preferably 0.1% by mass or more, more preferably 0.5% by mass or more, generally 10% by mass or less, preferably 5% by mass or less, more preferably 3% by mass or less, generally 0.001% by mass to 10% by mass, preferably 0.1% by mass to 5% by mass, more preferably 0.5% by mass to 3% by mass.
[0039] -Sweeteners- The oral composition of this embodiment can contain any suitable sweetener known in the prior art in any suitable amount. By including a sweetener in the oral composition, the user experience can be further improved.
[0040] Examples of sweeteners include saccharin, sodium saccharin, aspartame, steviol glycosides, stevia extract, p-methoxycinnamonaldehyde, neohesperidin dihydrochalcone, perilla stigma, thaumatin, and aspartyl-phenylalanine methyl ester. As sweeteners, one of the above-mentioned examples can be used alone, or two or more can be used in combination.
[0041] -spices- The oral composition of this embodiment can contain any suitable fragrance known in the prior art in any suitable amount. By including fragrance in the oral composition, the user experience can be further improved.
[0042] As spices, examples include peppermint oil, spearmint oil, Japanese peppermint oil, fennel oil, cinnamon oil, eucalyptus oil, wintergreen oil, frankincense oil, orange flower oil, lemongrass oil, jasmine oil, rose oil, iris oil, clove oil, thyme oil, sage oil, cardamom oil, rosemary oil, laurel oil, chamomile oil, caraway oil, basil oil, oregano oil, lemon oil, orange oil, white lemon oil, yuzu oil, nutmeg oil, lavender oil, chamomile oil, vanilla oil, cinnamon oil, allspice oil, bay leaf oil, perilla oil, wintergreen oil, and other natural essential oils; menthol, carvone, cinnamaldehyde, anethole, 1,8-cineole, methyl salicylate, eugenol, thymol, linalool, limonene, menthone, menthyl acetate, citral, decanal, and camphor. The fragrance components contained in the above-mentioned natural essential oils, including borneol, pinene, citronellol, n-decyl alcohol, citronellol, α-terpineol, citronellol acetate, eucalyptol, ethyl linalool, and vanillin; fragrance components such as ethyl acetate, ethyl butyrate, isoamyl acetate, hexanal, hexenal, methyl anthranilate, ethyl methyl phenyl glycidyl ester, benzaldehyde, vanillin, ethyl vanillin, furanol, N-ethyl-p-menthane-3-carboxamide, menthyl lactate, and ethylene glycol-l-menthyl carbonate; and various blended fragrances such as peppermint, fruit, and herbal fragrances composed of several fragrance components and natural essential oils. In addition, other fragrances that can also function as cooling agents include, for example, N-ethyl-p-menthane-3-carboxamide, menthyl lactate, menthyl succinate, isoprene alcohol, menthone glyceryl ketal, N-(4-cyanomethylphenyl)-p-menthane-carboxamide, 3-l-menthoxy-1,2-propanediol, 5-methyl-2-propane-2-yl-N-(2-pyridin-2-ylethyl)cyclohexane-1-carboxamide, ethyl 3-(p-menthane-3-carboxamide)acetate, and 2-isopropyl-N,2,3-trimethylbutyramide. As a flavoring agent, one of the flavoring agents exemplified above may be used alone, or two or more may be used in combination. When the oral composition contains a flavoring agent, and the total amount of the oral composition is set to 100% by mass, its content is typically 0.000001% by mass to 1% by mass, preferably 0.01% by mass to 1% by mass. When the oral composition contains a flavoring agent that can also function as a cooling agent, and the total amount of the oral composition is set to 100% by mass, its content is preferably 0.00001% by mass to 0.01% by mass.
[0043] -Medicinal ingredients- Examples of medicinal ingredients include: tranexamic acid, ε-aminocaproic acid, allantoin, allantoin chlorohydrin aluminum, azulene, glycyrrhizic acid or its salts (e.g., dipotassium glycyrrhizate), glycyrrhetinic acid or its salts (e.g., stearyl glycyrrhetinate), and other anti-inflammatory agents; sodium chloride, vitamins, and other cell activators; isopropyl methylphenol, hexadecylpyridine chloride, benzalkonium chloride, benzyl chloride, physalicylic acid, thymol, lysozyme chloride, chlorhexidine, triclosan, zinc gluconate, zinc citrate, and other bactericides or antibacterial agents; chlorophyll Water-soluble copper compounds such as copper sulfate and copper gluconate; tartar prevention agents such as zeolite, ethane hydroxybisphosphonate, and polyphosphates; vitamins such as vitamin C (e.g., ascorbic acid), vitamin E (e.g., tocopheryl acetate, tocopheryl nicotinate, tocopherol), and pyridoxine; astringents such as sodium chloride, alum, and lysozyme chloride; sensory hypersensitivity inhibitors such as potassium nitrate, aluminum lactate, and strontium chloride; amino acids such as alanine, glycine, and proline; and peptides such as caropeptide. When the oral composition contains a pharmaceutical ingredient, its content can be set to an effective amount within a range that does not impair the effects of the present invention (a range that is pharmacologically acceptable).
[0044] -Oily ingredients- Examples of oily components include: hydrocarbons such as squalane, (light) liquid paraffin, petrolatum, and microcrystalline wax; higher alcohols (e.g., alcohols with 8 to 22 carbon atoms such as lauryl alcohol, cetyl alcohol, cetearyl alcohol, oleyl alcohol, and isostearyl alcohol); higher fatty acids (e.g., fatty acids with 8 to 22 carbon atoms such as lauric acid, myristic acid, oleic acid, and isostearic acid); vegetable oils such as olive oil, castor oil, and coconut oil; and fatty acid esters such as isopropyl myristate.
[0045] -preservative- The oral composition of this embodiment can contain any suitable preservative known in the prior art in any suitable amount. By including a preservative in the oral composition, the preservative effect of the oral composition can be ensured.
[0046] Examples of preservatives that may be included in oral compositions include parabens (such as methylparaben, ethylparaben, and butylparaben), sodium benzoate, etc. Preservatives may be used alone or in combination of two or more.
[0047] -Wetting agent- The oral composition of this embodiment can contain any suitable humectant known in the prior art in any suitable amount. By including any humectant in the oral composition, the user experience can be further improved.
[0048] As a humectant, sugar alcohols and polyols other than sugar alcohols are preferred. Examples of sugar alcohols include sorbitol, erythritol, maltitol, lactitol, xylitol, and reduced starch saccharides; glycerol; and polyols such as ethylene glycol, propylene glycol, dipropylene glycol, butylene glycol, and polyethylene glycol. Examples of polyethylene glycols include those with an average molecular weight of 150 to 6000, preferably those with an average molecular weight of 190 to 630. Specifically, PEG200, PEG300, PEG400, and PEG600 are examples. When the total amount of the oral composition is set to 100% by mass, the content of the humectant is typically 40% by mass or less, preferably 1% to 30% by mass. The average molecular weight is the average molecular weight described in the Pharmaceutical Raw Material Standard 2021. When the oral composition may contain a humectant, and the total amount of the oral composition is set to 100% by mass, its content is typically 1% to 70% by mass, preferably 1% to 50% by mass, more preferably 1% to 40% by mass, even more preferably 3% to 40% by mass, and even more preferably 3% to 30% by mass.
[0049] -Abrasive- In the case of oral compositions of this embodiment, particularly dental cleaning compositions (liquid dental cleaning agents, gel dental cleaning agents, toothpaste), abrasives can preferably be used.
[0050] As abrasives, either inorganic or organic abrasives can be used. Examples of inorganic abrasives include: calcium phosphate compounds such as dicalcium phosphate dihydrate or anhydrous dicalcium phosphate, calcium dihydrogen phosphate, calcium phosphate, and calcium pyrophosphate; abrasive silica such as precipitated silica, aluminum silicate, zirconium silicate, and titanium-bonded silica; calcium carbonate abrasives such as calcium carbonate; and calcium hydroxide, aluminum hydroxide, magnesium phosphate, magnesium carbonate, calcium sulfate, bentonite, and hydroxyapatite. Examples of organic abrasives include synthetic resin-based abrasives and polymethyl methacrylate.
[0051] In the oral composition of this embodiment, one or more of the abrasives exemplified above can be incorporated as the abrasive. Among the abrasives, inorganic abrasives are preferred, and abrasive silica or calcium carbonate abrasives with silicates such as precipitated silica, aluminum silicate, zirconium silicate, and titanium-bonded silica as the main components are more preferred. Abrasive silica such as precipitated silica is particularly preferred.
[0052] The abrasive silica preferably has a fine particle size of 1 μm to 40 μm, and the BET specific surface area of the abrasive silica is preferably 20 m² / g. 2 ~250m 2 Here, the average particle size of the abrasive silica is the median particle size (D50) on a volume basis, determined by laser diffraction-scattering.
[0053] When the total amount of the oral composition is set to 100% by mass, the amount of abrasive is preferably 7% by mass or more, more preferably 10% by mass or more. This provides adequate cleaning power and a pleasant user experience. The upper limit is preferably 50% by mass or less, more preferably 30% by mass or less. This also provides good cleaning power to the oral composition and a pleasant user experience. Therefore, the content of abrasive is preferably 7% to 50% by mass, more preferably 10% to 50% by mass, and even more preferably 10% to 30% by mass.
[0054] -Adhesive- The oral composition of this embodiment can contain any suitable binder known in the prior art in any suitable amount. By including any binder in the oral composition, the viscosity can be optimized, and the shape retention and user experience can be further improved.
[0055] As any binder that can be included in an oral composition, any suitable organic binder known in the past can be cited, such as polysaccharides, cellulose-based binders (e.g., carboxymethyl cellulose (CMC), hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, methyl cellulose, cationic cellulose, and their sodium salts and other pharmacologically acceptable salts), other polysaccharide thickeners (e.g., xanthan gum, guar gum, gellan gum, tragacanth gum, ebony gum, gum arabic, locust bean gum, carrageenan gum, sodium alginate), and synthetic water-soluble polymers (e.g., sodium polyacrylate, carboxyvinyl polymers, polyvinylpyrrolidone, polyvinyl alcohol, propylene glycol alginate). In addition, inorganic binders such as thickening silica and aluminum silicate can also be incorporated.
[0056] When the total amount of the oral composition is set to 100% by mass, the content of any organic binder is preferably more than 0% by mass, more preferably 0.1% by mass or more, preferably 4% by mass or less, more preferably 3% by mass or less, preferably more than 0% by mass and less than 4% by mass, more preferably 0.1% by mass to 3% by mass. When the total amount of the oral composition is set to 100% by mass, the content of any inorganic binder is preferably more than 0% by mass, more preferably 1% by mass or more, preferably 10% by mass or less, more preferably 8% by mass or less, preferably more than 0% by mass and less than 10% by mass, more preferably 1% by mass to 8% by mass.
[0057] pH adjuster- The oral composition of this embodiment can contain any suitable pH adjuster known in the prior art in any suitable amount. By including a pH adjuster in the oral composition, the pH stability of the oral composition can be ensured.
[0058] Examples of pH adjusters include organic acids such as phthalic acid, citric acid, succinic acid, acetic acid, fumaric acid, malic acid, and lactic acid, or their salts (e.g., sodium citrate); inorganic acids such as phosphoric acid (e.g., orthophosphoric acid), or their salts (e.g., potassium, sodium, and ammonium salts); and hydroxides such as sodium hydroxide and potassium hydroxide. Examples of inorganic acid salts include disodium hydrogen phosphate and sodium dihydrogen phosphate.
[0059] The amount of pH adjuster can usually be set to make the pH of the oral composition after addition 5.0 to 9.0, and preferably to make the pH of the oral composition after addition 6.0 to 8.5.
[0060] In this instruction manual, pH value generally refers to the value after 25°C and 3 minutes from the start of the measurement. pH value can be measured, for example, using a pH meter (model Hm-30S) manufactured by Toa Denpa Kogyo Co., Ltd.
[0061] -Coloring agents- The oral composition of this embodiment may contain any suitable colorant known in the prior art in any suitable amount.
[0062] Examples of colorants that may be included in oral compositions include: natural pigments such as safflower red pigment, gardenia yellow pigment, gardenia blue pigment, perilla pigment, red yeast rice pigment, cabbage red pigment, carotene pigment, hibiscus pigment, cocoa pigment, spirulina blue pigment, and tamarind pigment; legally permitted pigments such as Red No. 2, Red No. 3, Red No. 104, Red No. 105, Red No. 106, Red No. 227, Yellow No. 4, Yellow No. 5, Green No. 3, and Blue No. 1; riboflavin; sodium copper chlorophyllin; and titanium dioxide. When an oral composition contains a colorant, and the total amount of the oral composition is set to 100% by mass, its content is preferably 0.00001% to 3% by mass.
[0063] -Any other ingredients- The oral composition of this embodiment may contain any other ingredients besides those described above in any suitable amount.
[0064] In this embodiment, examples of other arbitrary components that may be included in the oral composition include: inorganic compounds such as mica titanium, titanium dioxide, zinc oxide, magnesium oxide, and zirconium oxide; natural polymers such as agar, gelatin, starch, and glucomannan; synthetic polymers or copolymers such as polyvinyl acetate, acrylic resin, polyurethane, polyester, polyvinyl chloride, nylon powder, and polyethylene powder; waxes such as carnauba wax, rosin, rice bran wax, microcrystalline wax, beeswax, and paraffin wax; higher alcohols such as cetyl alcohol and stearyl alcohol; and polyisobutylene, polybutadiene, urethane, silicone, and natural rubber. The content of these other arbitrary components can be appropriately set within a range that does not impair the effects of the present invention.
[0065] [Dosage Forms and Uses of Oral Compositions] The oral composition of this embodiment can be formulated into any suitable dosage form known in the conventional method. Examples of dosage forms include liquids (solutions, emulsions, suspensions, syrups, etc.), semi-solids (gels, creams, pastes, etc.), and solids (tablets, granules, capsules, films, mixtures, molten solids, waxy solids, elastic solids, soft capsules, etc.). The dosage form of the oral composition is preferably liquid or semi-solid.
[0066] The oral composition of this embodiment can be widely used in oral applications. Examples of its use as a solid dosage form include troche, gummies, chewing gum, and dental floss. Examples of its use as a semi-solid dosage form include toothpaste and gel-based dental floss. Examples of its use as a liquid dosage form include mouthwash, liquid dental floss, and oral cooling agents (sprays, etc.).
[0067] The oral composition according to this embodiment has excellent user experience due to its good foaming properties (foaming, i.e., foaming), and therefore, specifically, it is preferably formulated as a dental cleaning agent (liquid dental cleaning agent, toothpaste, gel dental cleaning agent).
[0068] In this embodiment, the pH (25°C) of the oral composition is preferably 5.0 to 9.0. The pH can be adjusted by adding a pH adjuster, adjusting the composition, etc.
[0069] The oral composition of this embodiment can be adjusted to an appropriate viscosity depending on the dosage form. In the case of an oral composition in the form of a paste or gel, the viscosity at 25°C, as measured using a BH viscometer, is preferably 30 Pa·s to 150 Pa·s.
[0070] In addition, when the oral composition is in liquid form, the viscosity at 25°C as measured by a BH viscometer should be 30 mPa·s or less, and is particularly preferably 0.7 mPa·s to 30 mPa·s.
[0071] The oral composition according to the present invention, by incorporating a specified amount of sodium fluoride and / or sodium monofluorophosphate, ensures the stability of enzyme activity and further ensures good foaming properties during use, thereby improving the user experience.
[0072] [Method for manufacturing oral compositions] The method for manufacturing the oral composition of this embodiment is not particularly limited. The oral composition can be manufactured using any suitable method known in the past, depending on the selected dosage form. As a method for manufacturing the oral composition, specifically, in the case of making toothpaste (composition), the following manufacturing method can be cited: first, a component soluble in a solvent is prepared, then other insoluble components are mixed, and defoaming is further performed as needed, for example, by reducing pressure.
[0073] By containing the toothpaste obtained in this way in a prescribed container (laminated tube), or, in the case of a mouthwash, containing the prepared liquid in a prescribed container (bottle), an article can be made.
[0074] There are no particular limitations on the shape or material of the container capable of containing the oral composition of the present invention. Any suitable, conventionally known container generally applicable to oral compositions can be used as the container. Examples of containers made of materials such as polyethylene, polypropylene, polyethylene terephthalate, and nylon are also possible. Example
[0075] The present invention will now be specifically described with reference to embodiments and comparative examples. The present invention is not limited to these embodiments. It should be noted that the numerical values described in these embodiments (including those in the tables below) represent mass percentages unless otherwise specified.
[0076] [Ingredients used in the examples and comparative examples] First, the components used in the examples and comparative examples will be described. -Ingredient(A)- (A1) Sodium fluoride (manufactured by Stella Chemifa) (A2) Sodium monofluorophosphate (manufactured by ICL Japan) (A3) Stannous fluoride (manufactured by Fujifilm and Koichi Chemical Co., Ltd.)
[0077] -Ingredient (B)- (B1) Dextranase (Dextranase 2F: manufactured by Mitsubishi Chemical Corporation, enzyme activity 4000 U / g) (B2) Papain (purified papain: manufactured by Mitsubishi Chemical Corporation, enzyme activity 800,000 U / g)
[0078] -Ingredient (C)- (C1) Sodium lauryl sulfate (Texapon: manufactured by BASF Japan) (C2) Sodium tetradecene sulfonate (K Lipolan PJ-400 CJ: manufactured by Lion Specialty Chemicals)
[0079] Components other than components (A) to (C) (any component) Sorbitol solution (70%) (manufactured by Mitsubishi Corporation Life Sciences) Propylene glycol (manufactured by ADEKA) Abrasive silica (Zeodent 124, manufactured by Evonik) Thickening silica (Carplex (registered trademark) #67: manufactured by DSL Japan) Spice A water
[0080] The composition of flavoring A used in each embodiment and formulation example, as well as the composition of flavorings B to P used in further formulation examples, are shown in Tables 1 to 10 below.
[0081] [Table 1]
[0082] [Table 2]
[0083] The compositions of fragrances 1 to 7 and solvents used in the above fragrances A to P are shown in Tables 3 to 10 below.
[0084] [Table 3]
[0085] [Table 4]
[0086] [Table 5]
[0087] [Table 6]
[0088] [Table 7]
[0089] [Table 8]
[0090] [Table 9]
[0091] [Table 10]
[0092] Examples 1-20 and Comparative Examples 1-6 Using the above-mentioned ingredients as raw materials, and by the preparation method described below, oral compositions having the compound compositions shown in Tables 11 to 14 below are prepared.
[0093] [Preparation of oral compositions] A dental cleaning composition (toothpaste) is obtained by combining the raw materials shown in Tables 11-14 below using conventional methods. The obtained dental composition is then contained in any suitable dental preparation container known in the conventional sense (a laminated tube for the dental cleaning composition).
[0094] The obtained dental cleaning compositions (Examples 1-20 and Comparative Examples 1-6) were evaluated according to the following steps. The evaluation results are shown in Tables 11-14 below.
[0095] [evaluate] (1) Evaluation of enzyme stability 50g of each of the dental cleaning compositions involved in the examples and comparative examples were filled into laminated tubes and stored at 45°C and 75% RH for 3 weeks. Then, the dental cleaning compositions restored to room temperature were subjected to the following tests corresponding to the enzymes they were formulated with.
[0096] (i) Determination of dextranase activity First, 0.6 g of the dental cleaning agent composition is suspended in 0.1 M phosphate buffer to prepare a suspension. The suspension is then centrifuged, and the supernatant is used as the test solution. The amount of 0.1 M phosphate buffer added when preparing the suspension can be adjusted according to the amount of dextranase mixed in the dental cleaning agent composition. For example, 15 mL of 0.1 M phosphate buffer is sufficient when the amount of dextranase is 0.5%.
[0097] Add 1 mL of the obtained test solution to 2 mL of 1% dextran solution, react accurately in a constant temperature bath at 35°C for 10 minutes, and determine the amount of reducing sugar generated using the Somogyi-Nelson method.
[0098] One unit of dextranase activity is the amount of dextranase that can produce the equivalent of 1 μmol of free reducing sugar of glucose per minute.
[0099] (ii) Determination of papain enzyme activity The enzyme activity of papain was determined according to the "Enzyme Activity Assay" method described in the "Papain" section of the 10th edition of the Food Additives Standard. It should be noted that, regarding the preparation of the test solution used in the enzyme activity assay, firstly, 0.5 g of the dental cleaning agent composition is suspended in a diluent to form a suspension. The supernatant obtained by centrifuging the resulting suspension is used as the test solution. The amount of diluent added when preparing the suspension can be adjusted according to the amount of papain mixed in the dental cleaning agent composition. For example, the amount of diluent is set to 20 mL when the amount of papain is 0.3%.
[0100] The enzyme activity of the dental cleaning agent composition before and after storage treatment was measured, and the enzyme survival rate (unit: %) was calculated using the following formula. Enzyme survival rate (%) = (Enzyme activity after preservation treatment) / (Enzyme activity before preservation treatment) × 100
[0101] In this embodiment, the enzyme survival rate was measured three times. Based on the average of the three results, the enzyme stability was evaluated using the following evaluation criteria. (Evaluation Criteria) ◎(Excellent): Enzyme survival rate is over 90% ○ (Good): Enzyme survival rate is above 85% and less than 90%. △ (Applicable): Enzyme survival rate is above 80% and below 85%. × (Not allowed): Enzyme survival rate less than 80%
[0102] (2) Evaluation of foaming (foaming property) The evaluation was conducted using a sensory experiment conducted by a panel of 10 experts. Approximately 1.5 cm of the dental cleaning composition was placed on a toothbrush (Clinica Advantage toothbrush, 4-row compact standard type, manufactured by Lion Corporation), and brushing was performed using the same method as usual. The foaming of the dental cleaning composition in the oral cavity during use was evaluated using the following scoring criteria. (Scoring Criteria) 4 stars: Excellent foaming power and superior user experience. 3 stars: The foaming amount is moderate and satisfactory for use. 2 points: Low foaming output, slightly less pleasant to use. 1 point: Almost no foaming, poor user experience. When the average score obtained from the evaluation results (scores) of 10 experts is evaluated according to the following evaluation criteria, the foaming toothpaste composition that achieves a rating of ◎ (excellent) and ○ (good) is evaluated as a good toothpaste composition. (Evaluation Criteria) ◎(Excellent): Average score between 3.5 and 4.0 ○ (Good): Average score of 3.0 or above but less than 3.5 △ (Acceptable): Average score of 2.0 or higher but less than 3.0. × (Not allowed): Average score less than 2.0 points
[0103] (3) Evaluation of conformability 1g of the toothpaste composition was squeezed out in a length of about 10mm and placed on a toothbrush. The shape of the toothpaste composition was observed visually after 3 minutes. The shape retention of the toothpaste composition was evaluated according to the following evaluation criteria based on the average score of 3 repeated evaluations according to the following evaluation criteria. (Scoring Criteria) 4 points: The shape remains unchanged and it does not droop from the toothbrush. 3 points: Although the shape has changed slightly, it does not droop from the toothbrush. 2 points: The shape has changed slightly, and it droops a little from the toothbrush. 1 point: The shape has changed, hanging down from the toothbrush. (Evaluation Criteria) ◎(Excellent): Average score between 3.5 and 4.0 ○ (Good): Average score of 3.0 or above but less than 3.5 △ (Acceptable): Average score of 2.0 or higher but less than 3.0. × (Not allowed): Average score of 1.0 or higher but less than 2.0.
[0104] [Table 11]
[0105] [Table 12]
[0106] [Table 13]
[0107] [Table 14]
[0108] Examples 1 to 9 show formulations of the oral composition according to this embodiment.
[0109] [Table 15-1]
[0110] [Table 15-2]
[0111] [Table 16-1]
[0112] [Table 16-2]
[0113] As can be seen from the above, in Examples 1-20, which contain components (A), (B), and (C) and contain a specified amount of component (A), the evaluations of enzyme stability, foaming, and shape retention are all good. On the other hand, in Comparative Examples 1-6, which lack any one of components (A), (B), and (C), or do not contain a specified amount of component (A), the evaluations of one of the enzyme stability, foaming, and shape retention are extremely low. It should be noted that the same effect can be obtained by replacing flavoring A used in Examples 1-20 with flavorings B to P, which have already been described.
Claims
1. An oral composition, characterized in that, contain: Ingredient (A): One or both of sodium fluoride and sodium monofluorophosphate. Component (B): Enzymes, and Component (C): Anionic surfactant. The content of component (A), converted to fluoride ion concentration, is 3000ppm to 20000ppm.
2. The oral composition according to claim 1, wherein, Component (B) is one or both of glucanase and protease.
3. The oral composition according to claim 1 or 2, wherein, Component (B) contains one or more of the following: dextranase, mutase, kiwi protease, papain, and bromelain.
4. The oral composition according to claim 1 or 2, wherein, Component (C) is one or both of alkyl sulfate and tetradecene sulfonate.
5. The oral composition according to claim 1 or 2, wherein, Component (A) is sodium fluoride, with a sodium fluoride content of 0.6% to 4.5% by mass.
6. The oral composition according to claim 1 or 2, wherein, Component (A) is sodium monofluorophosphate, with a content of sodium monofluorophosphate ranging from 2.2% to 15.2% by mass.
7. The oral composition according to claim 1 or 2, wherein, The content of component (A), converted from fluoride ion concentration, is 4000ppm to 15000ppm.
8. The oral composition according to claim 1 or 2, wherein, The amount of component (C) is 0.1% to 3.0% by mass.
9. The oral composition according to claim 1 or 2, wherein, The ratio of fluoride ion concentration corresponding to the content of component (A) to the content of component (C) (A) / (C) is 1500 to 50000.
10. The oral composition according to claim 1 or 2, wherein, The oral composition is a dental cleaning agent.
Citation Information
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