Oral composition
Stabilizing enzymes in oral compositions with sodium fluoride and/or sodium monofluorophosphate maintains enzyme activity and foaming properties, addressing the denaturation issue with anionic surfactants.
Patent Information
- Application Number
- JP2024144482
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2024-08-15
- Filing Date
- 2024-08-26
- Publication Date
- 2026-02-24
AI Technical Summary
Anionic surfactants in oral compositions can denature and inactivate enzymes, leading to reduced enzyme stability and foaming properties when used in combination with enzymes.
Incorporating sodium fluoride and/or sodium monofluorophosphate in specific concentrations with anionic surfactants to stabilize enzyme activity and maintain foaming properties.
Ensures enzyme stability and provides good foaming properties in oral compositions, enhancing usability.
Abstract
Description
[Technical Field]
[0001] The present invention relates to an oral composition. [Background technology]
[0002] Conventionally, various enzymes have been blended into oral compositions from the viewpoints of preventing and inhibiting the progression of dental caries, preventing bad breath, and further improving the aesthetics of teeth. For example, dextranase, an enzyme that can be blended into oral compositions, is known to have a caries-preventing effect by decomposing plaque.
[0003] On the other hand, a surfactant is usually blended into an oral composition to improve the feel and ease of use. Examples of surfactants blended into oral compositions include anionic surfactants that are blended to ensure sufficient foaming properties.
[0004] However, anionic surfactants contained in oral compositions may denature and inactivate enzymes.
[0005] Therefore, a technique for preventing the denaturation and further deactivation of the enzyme and stabilizing the activity of the enzyme is essential, particularly when an anionic surfactant and an enzyme are used in combination.
[0006] Conventionally, when an enzyme such as dextranase is incorporated into an oral composition, it is known to incorporate specific amphoteric surfactants or nonionic surfactants in order to ensure the stabilization of the activity of dextranase.
[0007] Specifically, for example, Patent Document 1 below describes the incorporation of a carboxylic acid type amphoteric surfactant, Patent Document 2 below describes the incorporation of a polyoxyethylene alkyl ether, Patent Document 3 below describes the incorporation of a glycerin fatty acid ester, and Patent Document 4 below describes the incorporation of a fatty acid diethanolamide. [Prior art documents] [Patent documents]
[0008] [Patent Document 1] Japanese Patent Application Publication No. 58-225007 [Patent Document 2] Japanese Patent Application Publication No. 176518 / 1983 [Patent Document 3] Japanese Patent Application Publication No. 03-181413 [Patent Document 4] Japanese Patent Application Publication No. 08-12543 Summary of the Invention [Problem to be solved by the invention]
[0009] However, when an anionic surfactant and an enzyme are used in combination, if a surfactant such as a nonionic surfactant as disclosed in the above patent document is blended in a larger amount, the excellent foaming properties of the anionic surfactant may be reduced.
[0010] Therefore, the object of the present invention is to provide an oral composition that can ensure stability of enzyme activity, even when an anionic surfactant and an enzyme are used in combination, and that also has excellent usability, such as foaming properties. [Means for solving the problem]
[0011] That is, the present invention provides the following [1] to [9]. [1] Component (A) one or both of sodium fluoride and sodium monofluorophosphate; Component (B) an enzyme; Component (C) anionic surfactant; It contains An oral composition, wherein the content of component (A) is an amount equivalent to a fluoride ion concentration of 3000 ppm to 20000 ppm. [2] The oral composition according to [1], wherein component (B) is one or both of a glucanase and a protease. [3] The oral composition according to [1] or [2], wherein component (B) comprises one or more selected from the group consisting of dextranase, mutanase, actinidin, papain, and bromelain. [4] The oral composition according to any one of [1] to [3], wherein component (C) is one or both of an alkyl sulfate and a tetradecene sulfonate. [5] The 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% by mass to 4.5% by mass. [6] The 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% by mass to 15.2% by mass. [7] The oral composition according to any one of [1] to [6], wherein the content of component (A) is an amount equivalent to a fluoride ion concentration of 4000 ppm to 15000 ppm. [8] The oral composition according to any one of [1] to [7], wherein the ratio (A) / (C) of the fluoride ion concentration corresponding to the content of component (A) to the content of component (C) is 1500 to 50000. [9] The oral composition according to any one of [1] to [8], which is a dentifrice. [Effects of the Invention]
[0012] According to the present invention, even when an anionic surfactant and an enzyme are used in combination in an oral composition, the stability of the enzyme activity can be ensured by adding a predetermined amount of sodium fluoride and / or sodium monofluorophosphate, and an oral composition having good foaming properties (foaming properties), or in other words, good foaming properties, and an excellent feel when used can be provided. DETAILED DESCRIPTION OF THE INVENTION
[0013] The present invention will be described in detail below. The oral composition of the present invention comprises component (A) one or both of sodium fluoride and sodium monofluorophosphate, component (B) an enzyme, and component (C) an anionic surfactant. The oral composition contains component (A) in an amount that is 3000 ppm to 20000 ppm when converted into a fluoride ion concentration.
[0014] First, the components (A), (B) and (C) contained in the oral cavity composition of this embodiment will be described.
[0015] [Component (A) Sodium fluoride and / or sodium monofluorophosphate] The "component (A)" according to an embodiment of the present invention is sodium fluoride and / or sodium monofluorophosphate.
[0016] In this embodiment, component (A) is a component that can impart stability to the activity of the enzyme to the oral composition even when an anionic surfactant and an enzyme are used in combination.
[0017] In this embodiment, from the viewpoint of ensuring the stability of the enzyme activity and improving the foaming properties (foaming properties, i.e., lathering) during use, the content of component (A) is, when converted into a fluoride ion concentration, 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, 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, when the total amount of the oral composition is taken as 100% by mass, in order to ensure the stability of enzyme activity and further improve shape retention.
[0019] Furthermore, for example, when component (A) is sodium monofluorophosphate, the content of sodium monofluorophosphate is, from the viewpoint of ensuring the stability of enzyme activity and further improving shape retention, 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, when the total amount of the oral composition is taken as 100% by mass.
[0020] [Component (B) Enzyme] Component (B) is an enzyme. In this embodiment, the activity of the enzyme is not particularly limited, provided that it contributes to beneficial effects of the oral composition, such as decomposition and removal of plaque (biofilm) on tooth surfaces, in periodontal pockets, and on the tongue, and prevention and inhibition of the progression of dental caries.
[0021] In this embodiment, the component (B) enzyme is preferably a glucanase and / or a protease, i.e., for example, a glucanase capable of decomposing glucans contained in plaque that can cause dental caries or that cause plaque formation, and / or a protease capable of decomposing proteins contained in plaque as well as tongue coating and even stains.
[0022] More specifically, in this embodiment, the component (B) enzyme is more preferably one or more selected from the group consisting of dextranase, mutanase, actinidin, papain, and bromelain.
[0023] In this embodiment, when component (B) is dextranase, the amount of component (B) is preferably 2 U / g or more, more preferably 10 U / g or more, and 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, based on the enzyme activity, from the viewpoint of effectively preventing and inhibiting the progression of dental caries by, for example, decomposing plaque and further suppressing the occurrence of astringency during use. More specifically, when dextranase with an enzyme activity of 4000 U / g is used, the amount is preferably 0.05% to 5% by mass, based on the total amount of the oral composition as 100% by mass.
[0024] In this embodiment, when component (B) is papain, the amount of component (B) is preferably 400 U / g or more, more preferably 2000 U / g or more, and preferably 40,000 U / g or less, more preferably 10,000 U / g or less, and preferably 400 U / g to 40,000 U / g, and more preferably 2000 U / g to 10,000 U / g, based on the enzyme activity, from the viewpoint of effectively decomposing tongue coating and stains and suppressing the occurrence of a bitter taste during use. More specifically, when papain with an enzyme activity of 800,000 U / g is used, the amount is preferably 0.05% to 5% by mass, based on the total amount of the oral composition as 100% by mass.
[0025] [Component (C) Anionic Surfactant] The "component (C)" according to the embodiment of the present invention is an anionic surfactant. The anionic surfactant imparts foaming properties (effervescence, i.e., foaming) to the oral composition, which is a liquid (gel) or paste-like dentifrice composition, and can improve the feeling of use when brushing teeth with a toothbrush or the like.
[0026] In this embodiment, examples of the anionic surfactant as component (C) include α-olefin sulfonates such as tetradecene sulfonates, N-acylsulfonates, alkyl sulfates, N-acyltaurine salts such as sodium lauroylmethyl taurate, N-acylamino acid salts such as sodium lauroyl sarcosine and sodium lauroyl glutamate, and sulfates of glycerin fatty acid esters.
[0027] In this embodiment, it is preferable to use, as the component (C) anionic surfactant, specifically, for example, one or both of an alkyl sulfate and a tetradecene sulfonate.
[0028] In this embodiment, the amount of the anionic surfactant (Component (C)) blended is not particularly limited, provided that it does not impair the effects of the present invention.
[0029] The amount of component (C) anionic surfactant is, from the viewpoint of ensuring the stability of enzyme activity and further ensuring good foaming properties (foaming properties, i.e., lathering) during use to improve the feel of use, 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, when the total amount of the oral composition is 100% by mass.
[0030] [Content ratio] -Ingredient (A) / Ingredient (C)- The ratio of the 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, from the viewpoints of ensuring the stability of the enzyme activity and further ensuring good foaming properties (foaming properties, i.e., lathering) during use to improve the feel when used.
[0031] [Optional ingredients] The oral composition of this embodiment may contain any optional components other than the components (A) to (C) already described, provided that the effects of the present invention are not impaired. These will be specifically described below.
[0032] When the oral composition is a dentifrice composition (liquid dentifrice, gel dentifrice, or toothpaste), examples of optional components include solvents, surfactants, sweeteners, flavorings, medicinal ingredients, oily ingredients, preservatives, humectants, abrasives, binders, pH adjusters, and colorants (pigments).When the oral composition is a mouthwash, examples of optional components include solvents, humectants, surfactants, sweeteners, preservatives, pH adjusters, and flavorings.These are described in detail below.
[0033] In this specification, the content of each component is based on the amount of each component charged when producing the oral composition.
[0034] -solvent- The oral composition of the present embodiment may further contain a solvent, preferably water (purified water) or ethanol.
[0035] -Surfactants- The oral composition of the present embodiment may further contain a surfactant. Examples of surfactants that can be used in the oral composition 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), alkylolamides, polyoxyethylene fatty acid esters, polyoxyethylene alkenyl ethers, glycerin 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 diethanolamide), polyoxyethylene polyoxypropylene copolymers, and polyoxyethylene polyoxypropylene fatty acid esters. The alkyl chain of the polyoxyethylene alkyl ether typically has 14 to 18 carbon atoms, and the average number of moles of ethylene oxide added is typically 5 to 30 moles. The average number of moles of ethylene oxide added in polyoxyethylene hydrogenated castor oil is typically 20 to 100 moles, preferably 20 to 60 moles. The fatty acid of the sorbitan fatty acid ester typically has 12 to 18 carbon atoms. The number of carbon atoms in the fatty acid of the polyoxyethylene sorbitan fatty acid ester is usually 16 to 18, and the average number of moles of ethylene oxide added is usually 10 to 40. The number of carbon atoms in the alkyl chain of the alkylolamide is usually 12 to 14. Preferred nonionic surfactants are polyoxyethylene hydrogenated castor oil, polyoxyethylene sorbitan fatty acid ester, and polyoxyethylene alkyl ether.
[0037] Examples of amphoteric surfactants include betaine-type amphoteric surfactants such as alkyl dimethylamino acetic acid betaine (e.g., lauryl dimethylamino acetic acid betaine) and fatty acid amidopropyl dimethylamino acetic acid betaine (e.g., cocamidopropyl betaine); imidazoline-type amphoteric surfactants such as N-fatty acid acyl-N-carboxymethyl-N-hydroxyethyl ethylenediamine salts (e.g., N-coconut oil fatty acid acyl-N-carboxymethyl-N-hydroxyethyl imidazolinium betaine), coconut oil fatty acid imidazolinium betaine, and 2-alkyl-N-carboxymethyl-N-hydroxyethyl imidazolinium betaine; and alkyl betaines such as lauryl dimethylamino acetic acid betaine.
[0038] The content of the optional surfactant, excluding the content of the anionic surfactant (C) already described, is typically 0.001% by mass or more, preferably 0.1% by mass or more, and more preferably 0.5% by mass or more, when the total amount of the oral composition is 100% by mass, and is typically 10% by mass or less, preferably 5% by mass or less, and more preferably 3% by mass or less, and is typically 0.001% by mass to 10% by mass, preferably 0.1% by mass to 5% by mass, and more preferably 0.5% by mass to 3% by mass.
[0039] -Sweetener- The oral composition of the present embodiment may contain any suitable conventionally known sweetener in any suitable amount. By including a sweetener in the oral composition, the feeling of use can be further improved.
[0040] Examples of sweeteners include saccharin, saccharin sodium, aspartame, stevioside, stevia extract, paramethoxycinnamic aldehyde, neohesperidin dihydrochalcone, perillartine, thaumatin, and aspartylphenylalanine methyl ester. The sweeteners may be used singly or in combination of two or more of the above-listed sweeteners.
[0041] -Fragrance- The oral composition of the present embodiment may contain any suitable conventionally known flavor in any suitable amount. By including a flavor in the oral composition, the feeling of use can be further improved.
[0042] Examples of fragrances include natural essential oils such as peppermint oil, spearmint oil, Japanese peppermint oil, anise oil, cassia oil, eucalyptus oil, wintergreen oil, mastic oil, neroli 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, marjoram oil, lemon oil, orange oil, lime oil, yuzu oil, nutmeg oil, lavender oil, paracles oil, vanilla oil, cinnamon oil, pimento oil, cinnamon leaf oil, perilla oil, and wintergreen oil; menthol, carvone, cinnamic aldehyde, anethole, 1,8-cineole, methyl salicylate, eugenol, thymol, linalool, limonene, menthone, menthyl acetate, citrate, and citric acid. These include fragrance components contained in the above-mentioned natural essential oils, such as ral, decanal, camphor, borneol, pinene, spilanthol, n-decyl alcohol, citronellol, α-terpineol, citronellyl acetate, cineole, ethyl linalool, and vanillin; fragrance components, such as ethyl acetate, ethyl butyrate, isoamyl acetate, hexanal, hexenal, methyl anthranilate, ethyl methylphenylglycidate, benzaldehyde, vanillin, ethyl vanillin, furaneol, N-ethyl-p-menthane-3-carboxamide, menthyl lactate, and ethylene glycol-l-menthyl carbonate; and various blended flavors, such as mint, fruit, and herb flavors, which are made by combining several fragrance components and natural essential oils. Examples of fragrances that can also function as cooling agents include N-ethyl-p-menthane-3-carboxamide, menthyl lactate, menthyl monosuccinate, isopulegol, menthone glycerol ketal, N-(4-cyanomethylphenyl)-p-menthanecarboxamide, 3-l-menthoxypropane-1,2-diol, 5-methyl-2-propan-2-yl-N-(2-pyridin-2-ylethyl)cyclohexane-1-carboxamide, ethyl 3-(p-menthane-3carboxamide)acetate, and 2-isopropyl-N,2,3-trimethylbutyramide. The fragrances exemplified above may be used alone or in combination of two or more.When the oral composition contains a flavoring, the content thereof is usually 0.000001% by mass to 1% by mass, and preferably 0.01% by mass to 1% by mass, when the total amount of the oral composition is taken as 100% by mass. When the oral composition contains a flavoring that can also function as a cooling agent, the content thereof is preferably 0.00001% by mass to 0.01% by mass, when the total amount of the oral composition is taken as 100% by mass.
[0043] -Medicinal ingredients- Examples of medicinal ingredients include anti-inflammatory agents such as tranexamic acid, ε-aminocaproic acid, allantoin, allantoin chlorhydroxyaluminum, azulene, glycyrrhizinic acid or a salt thereof (e.g., dipotassium glycyrrhizinate), and glycyrrhetinic acid or a salt thereof (e.g., stearyl glycyrrhetinate); cell activators such as sodium chloride and vitamins; isopropylmethylphenol, cetylpyridinium chloride, benzalkonium chloride, benzethonium chloride, hinokitiol, thymol, lysozyme chloride, chlorhexidine, triclosan, zinc gluconate, and citric acid. Examples of suitable oral compositions include bactericidal or antibacterial agents such as zinc acetate; water-soluble copper compounds such as copper chlorophyll and copper gluconate; anti-tartar agents such as zeolite, ethanehydroxydiphosphonate, and polyphosphates; vitamins such as vitamin C (e.g., ascorbic acid), vitamin E (e.g., tocopherol acetate, tocopherol nicotinate, and tocopherol), and pyridoxine; astringents such as sodium chloride, alum, and lysozyme chloride; anti-dentin hypersensitivity agents such as potassium nitrate, aluminum lactate, and strontium chloride; amino acids such as alanine, glycine, and proline; and peptides such as callopeptides. When the oral composition contains a medicinal ingredient, the amount of the ingredient can be an effective amount within a range that does not interfere with the effects of the present invention (a pharmacologically acceptable range).
[0044] -Oil-based ingredients- Examples of oily components include hydrocarbons such as squalane, (light) liquid paraffin, petrolatum, and microcrystalline wax; higher alcohols (e.g., alcohols having 8 to 22 carbon atoms such as lauryl alcohol, cetyl alcohol, cetostearyl alcohol, oleyl alcohol, and isostearyl alcohol); higher fatty acids (e.g., fatty acids having 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] -Preservatives- The oral composition of the present embodiment may contain any suitable preservative known in the art in any suitable amount. By including a preservative in the oral composition, the oral composition can ensure its preservative effect.
[0046] Examples of preservatives that may be contained in the oral cavity composition include parahydroxybenzoic acid esters (e.g., methyl parahydroxybenzoate, ethyl parahydroxybenzoate, butyl parahydroxybenzoate), sodium benzoate, etc. The preservatives may be used alone or in combination of two or more.
[0047] -Wetting agent- The oral composition of the present embodiment may contain any suitable conventionally known humectant in any suitable amount. By including any suitable humectant in the oral composition, the feeling of use can be further improved.
[0048] Preferred humectants are sugar alcohols and polyhydric alcohols other than sugar alcohols. Examples of sugar alcohols include sugar alcohols such as sorbitol, erythritol, maltitol, lactitol, xylitol, and reduced starch saccharification products; glycerin; and polyhydric alcohols such as ethylene glycol, propylene glycol, dipropylene glycol, butylene glycol, and polyethylene glycol. Examples of polyethylene glycols include polyethylene glycols with an average molecular weight of 150 to 6,000, preferably polyethylene glycols with an average molecular weight of 190 to 630. Specific examples include PEG200, PEG300, PEG400, and PEG600. The content of the humectant is typically 40% by mass or less, preferably 1 to 30% by mass, based on 100% by mass of the total amount of the oral composition. The average molecular weight is the average molecular weight specified in the Quasi-drug Raw Materials Standards 2021. When the oral composition may contain a humectant, the content thereof is typically 1% by mass to 70% by mass, preferably 1% by mass to 50% by mass, more preferably 1% by mass to 40% by mass, even more preferably 3% by mass to 40% by mass, and even more preferably 3% by mass to 30% by mass, when the total amount of the oral composition is 100% by mass.
[0049] -Abrasives- The abrasive can be suitably used when the oral composition of this embodiment is a dentifrice composition (liquid dentifrice, gel dentifrice, toothpaste).
[0050] The abrasive may be either inorganic or organic. Examples of inorganic abrasives include calcium phosphate compounds such as dibasic calcium phosphate dihydrate or anhydrate, monobasic calcium phosphate, tribasic calcium phosphate, and calcium pyrophosphate; abrasive silicas such as precipitated silica, aluminosilicate, zirconosilicate, and titanium-bonded silica; calcium carbonate abrasives such as calcium carbonate; calcium hydroxide, aluminum hydroxide, tribasic magnesium phosphate, magnesium carbonate, calcium sulfate, bentonite, and hydroxyapatite. Examples of organic abrasives include synthetic resin abrasives and polymethyl methacrylate.
[0051] The oral composition of this embodiment may contain one or more of the above-listed abrasives as the abrasive. Among these, inorganic abrasives are preferred, and abrasive silicas containing silicates such as precipitated silica, aluminosilicate, zirconosilicate, and titanium-bonded silica as the main component, and calcium carbonate abrasives are more preferred, with precipitated silica being particularly preferred.
[0052] The abrasive silica is preferably abrasive particles having an average particle size of 1 μm to 40 μm, and the BET specific surface area of the abrasive silica is preferably 20 m per 1 g. 2 ~250m 2 Here, the average particle size of the abrasive silica is the volume-based median diameter (D50) measured by a laser diffraction / scattering method.
[0053] The amount of abrasive blended is preferably 7% by mass or more, more preferably 10% by mass or more, when the total amount of the oral composition is taken as 100% by mass. This allows for appropriate cleaning properties to be imparted and a good usability can be achieved. The upper limit is preferably 50% by mass or less, more preferably 30% by mass or less. This allows for good cleaning properties to be imparted to the oral composition and a good usability can be achieved. Therefore, the content of the abrasive is preferably 7% by mass to 50% by mass, more preferably 10% by mass to 50% by mass, and even more preferably 10% by mass to 30% by mass.
[0054] -Binder- The oral composition of the present embodiment may contain any suitable conventionally known binder in any suitable amount. By including any suitable binder in the oral composition, the viscosity can be optimized, and shape retention and usability can be further improved.
[0055] Examples of optional binders that may be contained in the oral composition include any suitable conventionally known organic binders, such as polysaccharides, cellulose-based binders (e.g., carboxymethylcellulose (CMC), hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropylmethylcellulose, methylcellulose, cationized cellulose, and pharmacologically acceptable salts thereof, such as sodium salts), other polysaccharide thickeners (e.g., xanthan gum, guar gum, gellan gum, tragacanth gum, karaya gum, gum arabic, locust bean gum, carrageenan, sodium alginate), and synthetic water-soluble polymers (e.g., sodium polyacrylate, carboxyvinyl polymer, polyvinylpyrrolidone, polyvinyl alcohol, propylene glycol alginate). Furthermore, inorganic binders such as thickening silica and aluminum silicate can also be blended.
[0056] The content of the optional organic binder is preferably greater than 0% by mass, more preferably 0.1% by mass or greater, preferably 4% by mass or less, more preferably 3% by mass or less, preferably greater than 0% by mass and 4% by mass and more preferably 0.1% to 3% by mass, when the total amount of the oral composition is taken as 100% by mass. The content of the optional inorganic binder is preferably greater than 0% by mass, more preferably 1% by mass or greater, preferably 10% by mass or less, more preferably 8% by mass or less, preferably greater than 0% by mass and 10% by mass or less, more preferably 1% to 8% by mass, when the total amount of the oral composition is taken as 100% by mass.
[0057] - pH adjuster - The oral composition of the present embodiment may contain any suitable conventionally known pH adjuster 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 salts, sodium salts, 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 content of the pH adjuster can usually be an amount that will give a pH of the oral composition after addition of the pH adjuster of 5.0 to 9.0, preferably 6.0 to 8.5.
[0060] In this specification, the pH value generally refers to the value measured 3 minutes after the start of measurement at 25° C. The pH value can be measured, for example, using a pH meter (model number Hm-30S) manufactured by Toa Dempa Kogyo Co., Ltd.
[0061] -Coloring agent- The oral composition of the present embodiment may contain any suitable colorant known in the art in any suitable content.
[0062] Examples of colorants that the oral composition may contain include natural colorants such as safflower red colorant, gardenia yellow colorant, gardenia blue colorant, perilla colorant, monascus colorant, red cabbage colorant, carrot colorant, hibiscus colorant, cacao colorant, spirulina blue colorant, and tamarind colorant, as well as legally designated colorants 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, copper chlorophyll sodium, and titanium dioxide. When the oral composition contains a colorant, the content thereof is preferably 0.00001% to 3% by mass when the total amount of the oral composition is taken as 100% by mass.
[0063] -Other optional ingredients- The oral composition of the present embodiment may contain any suitable amount of optional components other than those described above.
[0064] In this embodiment, examples of other optional components that may be contained in the oral composition include inorganic compounds such as titanium mica, titanium oxide, zinc oxide, magnesium oxide, and zirconium oxide; natural polymer compounds such as agar, gelatin, starch, and glucomannan; synthetic polymer compounds or copolymers thereof such as polyvinyl acetate, acrylic resin, polyurethane, polyester, polyvinyl chloride, nylon powder, and polyethylene powder; waxes such as carnauba wax, rosin, rice wax, microcrystalline wax, beeswax, and paraffin wax; higher alcohols such as cetanol and stearyl alcohol; polyisobutylene, polybutadiene, urethane, silicone, and natural rubber. The content of these other optional components can be appropriately set within a range that does not interfere with the effects of the present invention.
[0065] [Dosage form and use of oral composition] The oral composition of this embodiment can be made into any suitable conventional dosage form by any suitable method according to conventional methods. Examples of dosage forms include liquids (liquids such as solutions, emulsions, suspensions, syrups, etc.), semi-solids (gels, creams, pastes, etc.), and solids (tablets, particulates, capsules, films, kneaded materials, molten solids, waxy solids, elastic solids, soft capsules, etc.). The dosage form of the oral composition is preferably a liquid or semi-solid.
[0066] The oral composition of the embodiment can be widely used in oral applications. Examples of applications in solid dosage forms include lozenges, gummies, chewing gum, and dentifrices. Examples of applications in semisolid dosage forms include toothpastes and gel dentifrices. Examples of applications in liquid dosage forms include mouthwashes, liquid dentifrices, and mouth fresheners (sprays, etc.).
[0067] The oral composition of this embodiment has an excellent feel when used, such as good foaming properties (foaming, i.e., foaming), and is therefore preferably formulated into a dentifrice (liquid dentifrice, toothpaste, gel dentifrice), for example.
[0068] In this embodiment, the oral composition preferably has a pH (25° C.) of 5.0 to 9.0. The pH can be adjusted by adding a pH adjuster, adjusting the component composition, and the like.
[0069] The viscosity of the oral composition of this embodiment can be adjusted appropriately depending on the dosage form, for example. When the oral composition is in paste or gel form, the viscosity at 25°C measured with a BH viscometer is preferably 30 Pa s to 150 Pa s.
[0070] In the case of an oral composition in a liquid dosage form, the viscosity at 25°C measured with a BH viscometer may be 30 mPa·s or less, and preferably 0.7 mPa·s to 30 mPa·s.
[0071] According to the oral composition of the present invention, by blending a predetermined amount of sodium fluoride and / or sodium monofluorophosphate, it is possible to ensure the stability of enzyme activity and further to ensure good foaming properties (foaming properties, i.e., foaming) during use, thereby improving the feeling of use.
[0072] [Method of manufacturing oral composition] The method for producing the oral composition of this embodiment is not particularly limited. The oral composition can be produced by any suitable method known in the art depending on the selected dosage form. Specific examples of the method for producing the oral composition include, for example, a method in which, when a toothpaste (composition) is produced, components that are soluble in a solvent are first prepared, and then other insoluble components are mixed in, and if necessary, degassing is further performed, for example, by reducing the pressure.
[0073] The toothpaste thus obtained can be placed in a designated container (laminated tube), or in the case of a mouthwash, the prepared liquid can be placed in a designated container (bottle) to make the final product.
[0074] The shape and material of the container in which the oral composition of the present invention can be stored are not particularly limited. Any suitable conventional container that is normally used for oral compositions can be used as the container. Examples of the container include plastic containers made of polyethylene, polypropylene, polyethylene terephthalate, and nylon. [Example]
[0075] The present invention will be specifically described below with reference to examples and comparative examples. The present invention is not limited to these examples. Numerical values described in these examples (including the numerical values in the following table) represent mass % unless otherwise specified.
[0076] [Components used in the Examples and Comparative Examples] First, the components used in the examples and comparative examples will be described. -Component (A)- (A1) Sodium fluoride (manufactured by Stella Chemifa Co., Ltd.) (A2) Sodium monofluorophosphate (manufactured by ICL Japan) (A3) Stannous fluoride (Fujifilm Wako Pure Chemical Industries, Ltd.)
[0077] -Component (B)- (B1) Dextranase (Dextranase 2F: Mitsubishi Chemical Corporation, enzyme activity 4000 U / g) (B2) Papain (purified papain: Mitsubishi Chemical Corporation, enzyme activity 800,000 U / g)
[0078] -Component (C)- (C1) Sodium lauryl sulfate (Texapon: manufactured by BASF Japan) (C2) Sodium tetradecene sulfonate (K-Lipolan PJ-400CJ: manufactured by Lion Specialty Chemicals)
[0079] Ingredients other than ingredients (A) to (C) (optional ingredients) Sorbitol solution (70%) (Mitsubishi Corporation Life Sciences) Propylene glycol (ADEKA) Abrasive silica (Zeodent 124, Evonik) Viscosity-increasing silica (Carplex® #67: manufactured by DSL Japan Co., Ltd.) Fragrance A water
[0080] The composition of fragrance A used in each example and formulation example, and the compositions of fragrances B to P used in the formulation examples are shown in Tables 1 to 10 below.
[0081] [Table 1]
[0082] [Table 2]
[0083] The compositions of flavors 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 to 20 and Comparative Examples 1 to 6 Using the above ingredients as raw materials, oral compositions having the formulations shown in Tables 11 to 14 below were prepared according to the preparation methods described below.
[0093] [Preparation of oral composition] The raw materials shown in Tables 11 to 14 below were blended in a conventional manner to obtain oral compositions, i.e., dentifrice compositions ((paste) dentifrices). The obtained oral compositions were then placed in any suitable conventionally known oral preparation container (a laminated tube for the dentifrice composition).
[0094] The resulting dentifrice compositions (Examples 1 to 20 and Comparative Examples 1 to 6) were evaluated according to the following procedures. The evaluation results are shown in Tables 11 to 14 below.
[0095] [evaluation] (1) Evaluation of enzyme stability 50 g of each of the dentifrice compositions according to the Examples and Comparative Examples was packed into a laminated tube and stored at 45°C and 75% RH for 3 weeks. After that, the dentifrice compositions were returned to room temperature and subjected to the following tests according to the type of enzymes incorporated.
[0096] (i) Measurement of dextranase enzyme activity First, 0.6 g of the dentifrice composition was suspended in 0.1 M phosphate buffer to prepare a suspension, and the resulting suspension was centrifuged to obtain a supernatant, which was used as the test solution. The amount of 0.1 M phosphate buffer added when preparing the suspension can be adjusted depending on the amount of dextranase in the dentifrice composition. For example, when the amount of dextranase is 0.5%, the amount of 0.1 M phosphate buffer should be 15 mL.
[0097] 1 mL of the obtained test solution was added to 2 mL of 1% dextran solution, and the mixture was reacted in a constant temperature bath at 35°C for exactly 10 minutes, and the amount of reducing sugars produced was measured using the Somogyi-Nelson method.
[0098] One unit of dextranase enzyme activity was defined as the amount of dextranase capable of producing free reducing sugars equivalent to 1 μmol of glucose per minute.
[0099] (ii) Measurement of papain enzyme activity The enzyme activity of papain was measured according to the "Enzyme activity measurement method" described in the "Papain" section of the 10th edition of the Japanese Standards for Food Additives. The test solution used to measure the enzyme activity was prepared by first suspending 0.5 g of the dentifrice composition in a diluent to form a suspension, and then centrifuging the resulting suspension to obtain a supernatant, which was used as the test solution. The amount of diluent added to prepare the suspension can be adjusted depending on the amount of papain in the dentifrice composition. For example, when the amount of papain is 0.3%, the amount of diluent was 20 mL.
[0100] The enzyme activity in the dentifrice composition before and after the preservation treatment was measured, and the enzyme residual rate (unit: %) was calculated using the following formula. Enzyme residual rate (%) = (enzyme activity after preservation) / (enzyme activity before preservation) × 100
[0101] In this example, the measurement of the enzyme residual rate was repeated three times, and the enzyme stability was evaluated based on the average value of the three results obtained, using the following evaluation criteria. (Evaluation criteria) ◎(Excellent): Enzyme residual rate 90% or more 〇 (Good): Enzyme remaining rate is 85% or more but less than 90% △ (Acceptable): Enzyme remaining rate is 80% or more but less than 85% × (Not acceptable): Enzyme remaining rate is less than 80%
[0102] (2) Evaluation of foaming (foaming ability) The evaluation was carried out by a sensory test using 10 expert panelists. An approximately 1.5 cm length of the dentifrice composition was placed on a toothbrush (Clinica Advantage Toothbrush, 4-row compact regular type, manufactured by Lion Corporation), and the subject brushed their teeth in the same manner as usual. The foaming of the dentifrice composition in the oral cavity during use was evaluated according to the following rating scale. (Grading criteria) 4 points: Sufficient foaming and excellent usability 3 points: The amount of foam is moderate and the feel is satisfactory 2 points: Low foaming and slightly inferior usability 1 point: Almost no foaming, poor usability When evaluated according to the following evaluation criteria based on the average score obtained by averaging the evaluation results (scores) of 10 people, dentifrice compositions that achieved foaming rated as ◎ (excellent) and ○ (good) were evaluated as good dentifrice compositions. (Evaluation criteria) ◎(Excellent): Average score of 3.5 points or more and 4.0 points or less ○ (Good): Average score 3.0 points or more and less than 3.5 points △ (Acceptable): Average score between 2.0 and 3.0 points × (Fail): Average score less than 2.0 points
[0103] (3) Evaluation of shape retention 1 g of the dentifrice composition was extruded onto a toothbrush to a length of approximately 10 mm, and the shape of the dentifrice composition was visually observed after 3 minutes had passed. The shape retention of the dentifrice composition was evaluated according to the following evaluation criteria, based on the average score of three repeated evaluations according to the following evaluation criteria. (Grading criteria) 4 points: No change in shape and no dripping from the toothbrush 3 points: There is a slight change in shape, but it does not drip from the toothbrush. 2 points: There is a slight change in shape and the toothbrush drips slightly. 1 point: The shape has changed and the toothbrush is dripping (Evaluation criteria) ◎(Excellent): Average score of 3.5 points or more and 4.0 points or less ○ (Good): Average score 3.0 points or more and less than 3.5 points △ (Acceptable): Average score between 2.0 and 3.0 points × (Fail): Average score is 1.0 or more and less than 2.0 points
[0104] [Table 11]
[0105] [Table 12]
[0106] [Table 13]
[0107] [Table 14]
[0108] Formulation examples 1 to 9 of the oral cavity composition of this embodiment are shown below.
[0109] [Table 15-1]
[0110] [Table 15-2]
[0111] [Table 16-1]
[0112] [Table 16-2]
[0113] As is clear from the above, Examples 1 to 20, which contain components (A), (B), and (C) and also contain a predetermined amount of component (A), were good in the evaluations of enzyme stability, foaming, and shape retention, while Comparative Examples 1 to 6, which lacked any of components (A), (B), and (C), or did not contain the predetermined amount of component (A), were extremely poor in the evaluations of any of enzyme stability, foaming, and shape retention. Note that similar effects were obtained even when fragrance A used in Examples 1 to 20 was replaced with each of fragrances B to P already described.
Claims
1. Component (A) one or both of sodium fluoride and sodium monofluorophosphate; Component (B) an enzyme; Component (C) anionic surfactant; It contains The oral composition contains component (A) in an amount that is 3,000 ppm to 20,000 ppm when converted into a fluoride ion concentration.
2. 2. The oral composition of claim 1, wherein component (B) is one or both of a glucanase and a protease.
3. 3. The oral composition according to claim 1, wherein component (B) comprises at least one member selected from the group consisting of dextranase, mutanase, actinidin, papain, and bromelain.
4. 3. The oral composition according to claim 1, wherein component (C) is one or both of an alkyl sulfate and a tetradecene sulfonate.
5. 3. The oral composition according to claim 1, wherein component (A) is sodium fluoride and the content of sodium fluoride is 0.6% by mass to 4.5% by mass.
6. 3. The oral composition according to claim 1, wherein component (A) is sodium monofluorophosphate and the content of sodium monofluorophosphate is 2.2% by mass to 15.2% by mass.
7. 3. The oral composition according to claim 1, wherein the content of component (A) is an amount equivalent to a fluoride ion concentration of 4,000 ppm to 15,000 ppm.
8. 3. The oral composition according to claim 1, wherein the ratio (A) / (C) of the fluoride ion concentration corresponding to the content of component (A) to the content of component (C) is 1,500 to 50,000.
9. The oral composition according to claim 1 or 2, which is a dentifrice.
Citation Information
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