Oral composition

By using sodium fluoride, calcium glycerophosphate, and other ingredients in oral compositions to form complexes with condensed phosphates, the problem of sour taste caused by organic acids is solved, achieving a combination of biofilm removal effect and good flavor.

CN121154438APending Publication Date: 2025-12-19LION CORP
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Patent Information

Application Number
CN202510282971.8
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Priority Date
2024-06-19
Filing Date
2025-03-11
Publication Date
2025-12-19

AI Technical Summary

Technical Problem

In existing oral care compositions, the acidity of organic acids such as malic acid, citric acid, and phytic acid contributes to unpleasant flavors and affects the user experience.

Method used

It uses sodium fluoride, calcium glycerophosphate, calcium gluconate, calcium lactate and calcium pantothenate as components, combined with condensed phosphoric acid and its alkali metal salts and organic acids and their salts, and adjusts the component ratio. Amphoteric surfactants and anionic surfactants are added to form a fluorine, calcium and phosphorus ion complex, which reduces the sour taste and maintains a good flavor.

Benefits of technology

While achieving the effect of removing biofilm, it significantly reduces acidity and improves the user experience of oral care compositions.

✦ Generated by Eureka AI based on patent content.

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Abstract

Provided is an oral composition which has a biofilm removal effect and also has a good flavor. The oral composition contains (A) sodium fluoride, (B) one or more substances selected from the group consisting of calcium glycerophosphate, calcium gluconate, calcium lactate and calcium pantothenate, (C) one or more substances selected from the group consisting of condensed phosphoric acid and alkali metal salts thereof, and (D) one or more substances selected from the group consisting of organic acids and salts thereof (excluding the component (B)).
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Description

TECHNICAL FIELD

[0001] The present application relates to an oral composition. BACKGROUND

[0002] From the viewpoint of prevention of dentistry, it is also preferable to inhibit the formation of a biofilm caused by dental plaque, tongue coating, or the like in the oral cavity.

[0003] In Patent Literature 1, as a toothpaste composition having a biofilm formation inhibiting effect, an example of an oral composition containing sodium lauryl sulfate as an anionic surfactant and K-carrageenan as a binder in a specific mass ratio, and containing a specific organic acid (malic acid, citric acid, phytic acid) as a component for improving the dispersibility of K-carrageenan and sodium lauryl sulfate is described.

[0004] [PTL 1] [PTL 2] [Patent Literature 1] Japanese Patent Application Laid-Open No. 2020-033291 SUMMARY

[0005] [PROBLEMS TO BE SOLVED BY THE INVENTION] However, the sour taste of the organic acid (malic acid, citric acid, phytic acid) sometimes brings about a flavor that users do not like.

[0006] An object of the present application is to provide an oral composition having a biofilm removing effect and also a good flavor.

[0007] [MEANS FOR SOLVING THE PROBLEMS] The present application has the following modes.

[0008] [1] An oral composition containing (A) sodium fluoride, (B) one or more selected from the group consisting of calcium glycerophosphate, calcium gluconate, calcium lactate, and calcium pantothenate, (C) one or more selected from the group consisting of condensed phosphoric acid and alkali metal salts thereof, and (D) one or more selected from the group consisting of organic acids and salts thereof (excluding the (B) component).

[0009] [2] The oral composition according to [1], wherein the (C) component contains one or more selected from the group consisting of pyrophosphoric acid and alkali metal pyrophosphates.

[0010] [3] The oral composition according to [1] or [2], wherein the molar amount (unit: mmol / g) of the (B) component per 1 g of the oral composition is set as B mmol , and the mass ratio (unit: mass%) of the (D) component with respect to the total mass of the oral composition is set as D wt% , when B mmol / D wt%The ratio represented is 0.001 to 5.0.

[0011] [4] The oral composition according to any one of [1] to [3], wherein the (D) component comprises one or more selected from the group consisting of citric acid, malic acid, tartaric acid, succinic acid, fumaric acid, edetic acid, phytic acid, and salts thereof.

[0012] [5] The oral composition according to any one of [1] to [4], wherein the oral composition further comprises (E) one or more selected from the group consisting of amphoteric surfactants and anionic surfactants.

[0013] [6] The oral composition according to any one of [1] to [5], which is a dentifrice.

[0014] [Effects of the Invention] According to the present application, an oral composition having a biofilm-removing effect and also a good flavor can be obtained. DETAILED DESCRIPTION

[0015] In the present specification, "oral composition" means a composition mainly for use in the oral cavity.

[0016] In the present specification, "water-soluble" means solubility in water at 20°C of 1 g / 100 g or more.

[0017] In the present specification, "~" indicating a numerical range means that the numerical values recited before and after it are included as lower limit values and upper limit values.

[0018] [Oral Composition] The oral composition of the present application contains a (A) component, a (B) component, a (C) component, and a (D) component.

[0019] It is preferable to further contain a (E) component.

[0020] < (A) Component > The (A) component is sodium fluoride (NaF). The (A) component reduces the sour taste caused by the (D) component, and contributes to improvement of the flavor. The (A) component can be used as a commercially available product.

[0021] < (B) Component > The (B) component is a water-soluble calcium salt selected from one or more of calcium glycerophosphate, calcium gluconate, calcium lactate, and calcium pantothenate. Two or more of the (B) components can be combined.

[0022] The (B) component reduces the sour taste caused by the (D) component, and contributes to improvement of the flavor.

[0023] The (B) component can be used as a commercially available product.

[0024] < (C) component > The (C) component is at least one selected from condensed phosphoric acid and alkali metal salts thereof. Two or more kinds of (C) components can be combined.

[0025] The (C) component reduces the sourness caused by the (D) component, and contributes to the improvement of the flavor.

[0026] As the condensed phosphoric acid or the alkali metal salt thereof, a water-soluble condensed phosphoric acid or a salt thereof can be preferably used.

[0027] As the condensed phosphoric acid, for example, linear polyphosphoric acids such as pyrophosphoric acid, tripolyphosphoric acid, tetrapolyphosphoric acid, and the like; cyclic polyphosphoric acids such as trimetaphosphoric acid, tetrametaphosphoric acid, hexametaphosphoric acid, and the like can be exemplified.

[0028] As the alkali metal salt of the condensed phosphoric acid, sodium salts, potassium salts can be exemplified.

[0029] In particular, from the viewpoint of the flavor improvement effect, pyrophosphate, tripolyphosphate, hexametaphosphate are preferable, and pyrophosphate is more preferable. In particular, potassium pyrophosphate, sodium pyrophosphate are particularly preferable.

[0030] The (C) component can be used as a commercially available product.

[0031] The (C) component preferably contains a (C1) component, and the (C1) component is selected from one or more of pyrophosphoric acid and alkali metal salts of pyrophosphoric acid. The (C1) component is particularly excellent in the flavor improvement effect.

[0032] The proportion of the (C1) component with respect to the total mass of the (C) component can be, for example, 90% by mass or more, 95% by mass or more, 96% by mass or more, 97% by mass or more, 98% by mass or more, or 99% by mass or more, and can also be 100% by mass.

[0033] < (D) component > The (D) component is one or more selected from organic acids and salts thereof (excluding the (B) component described above). Two or more kinds of (D) components can be combined. The (D) component contributes to the biological membrane removal effect.

[0034] As the organic acid, citric acid, malic acid, tartaric acid, succinic acid, fumaric acid, edetic acid, phytic acid can be exemplified, and citric acid, malic acid, edetic acid, phytic acid are preferable.

[0035] As the salt of the (D) component, alkali metal salts such as sodium salts, potassium salts are preferable.

[0036] The (D) component can be used as a commercially available product.

[0037] The (D) component preferably contains a (D1) component, and the (D1) component is selected from one or more of citric acid, malic acid, tartaric acid, succinic acid, fumaric acid, edetic acid, phytic acid, and salts thereof.

[0038] The proportion of the (D1) component with respect to the total mass of the (D) component can be, for example, 90% by mass or more, 95% by mass or more, 96% by mass or more, 97% by mass or more, 98% by mass or more, or 99% by mass or more, and can also be 100% by mass.

[0039] < (E) component > The (E) component is one or more surfactants selected from amphoteric surfactants and anionic surfactants. The (E) component can combine two or more. The (E) component can use a commercially available product. The (E) component contributes to the biofilm removal effect.

[0040] [Amphoteric surfactant] As the amphoteric surfactant, for example, amidoalkyl betaine such as cocamidopropyl betaine, lauryldimethylaminoethyl betaine, N-cocoyl-N-carboxymethyl-N-hydroxyethyl ethylenediamine can be given.

[0041] [Anionic surfactant] As the anionic surfactant, for example, alkyl sulfate, N-acyl taurate, N-acyl amino acid salt, alpha-olefin sulfonate, sodium dodecylbenzenesulfonate, sodium laurylsulfonate can be given.

[0042] As the alkyl sulfate, sodium lauryl sulfate, sodium myristyl sulfate is preferred.

[0043] The number of carbon atoms of the acyl group in the N-acyl taurate is preferably 10 to 20. As the salt, an alkali metal salt such as sodium salt, potassium salt is preferred, and the sodium salt is more preferred.

[0044] As the N-acyl taurate, for example, N-cocoyl methyl taurine sodium, N-cocoyl methyl taurine potassium, N-lauryl methyl taurine sodium, N-methyl stearoyl taurine sodium, N-myristoyl methyl taurine sodium, N-oleoyl methyl taurine sodium, N-palmitoyl methyl taurine sodium, and the like N-acyl methyl taurine salt, N-cocoyl taurine sodium, and the like can be given. Among them, the N-acyl methyl taurine salt is preferred, and the N-acyl methyl taurine sodium is more preferred.

[0045] The number of carbon atoms of the acyl group in the N-acyl amino acid salt is preferably 8 to 18, and more preferably 10 to 16. As the salt, an alkali metal salt such as sodium salt, potassium salt is preferred, and the sodium salt is more preferred.

[0046] As the N-acyl amino acid salt, for example, there can be mentioned N-acyl glutamate, N-acyl aspartate and the like N-acyl acidic amino acid salt; N-acyl sarcosinate, N-acyl methylalaninate, N-acyl glycinate, N-acyl alaninate and the like N-acyl neutral amino acid salt; N-acyl arginine ethyl ester salt and the like acyl basic amino acid salt. Among them, the N-acyl neutral amino acid salt is preferred, and the N-acyl sarcosinate is more preferred.

[0047] As the N-acyl sarcosinate, a substance having an acyl group of the above-mentioned carbon atom number is preferred, and for example, there can be mentioned N-cocoyl sarcosinate, N-lauroyl sarcosinate, N-palmitoyl sarcosinate and the like. Among them, the sodium N-lauroyl sarcosinate is preferred.

[0048] The α-olefin sulfonate preferably has a carbon atom number of 8 to 18, and more preferably 14 to 16. As the salt, an alkali metal salt such as sodium salt, potassium salt and the like is preferred, and the sodium salt is more preferred.

[0049] As the α-olefin sulfonate, the α-olefin sulfonate having a carbon atom number of 14 is preferred, and the sodium salt (common name: sodium tetradecene sulfonate) is particularly preferred.

[0050] The (E) component preferably contains the (El) component, and the (El) component is one or more selected from the group consisting of amidoalkyl betaine, lauryl sulfate, N-acyl taurate and N-acyl amino acid salt. The (El) component is more excellent in the biological membrane removing ability. In particular, the amidoalkyl betaine is preferred in terms of stimulation.

[0051] The proportion of the (El) component with respect to the total mass of the (E) component is, for example, 90 mass% or more, 95 mass% or more, 96 mass% or more, 97 mass% or more, 98 mass% or more, or 99 mass% or more, and can also be 100 mass%.

[0052] <Content of each component> The content of the (A) component with respect to the total mass of the oral composition is preferably 0.09 to 1.3 mass%, and more preferably 0.10 to 1.1 mass%. When the content of the (A) component is the above lower limit value or more, the acid taste reducing effect of the (D) component is more excellent. When the content of the (A) component is the above upper limit value or less, the flavor is more excellent.

[0053] The content of the (B) component with respect to the total mass of the oral composition is preferably 0.02 to 5.0 mass%, and more preferably 0.03 to 3.0 mass%. When the content of the (B) component is the above lower limit value or more, the acid taste reducing effect of the (D) component is more excellent. When the content of the (B) component is the above upper limit value or less, the flavor is more excellent.

[0054] The content of the (C) component with respect to the total mass of the oral composition is preferably 0.02 to 3.0 mass%, more preferably 0.03 to 1.3 mass%. When the content of the (C) component is equal to or more than the lower limit of the above range, the acid taste reduction effect of the (D) component is more excellent. When the content of the (C) component is equal to or less than the upper limit of the above range, the flavor is more excellent.

[0055] The content of the (D) component with respect to the total mass of the oral composition is preferably 0.001 to 5 mass%, more preferably 0.01 to 2 mass%. When the content of the (D) component is equal to or more than the lower limit of the above range, the biofilm removal effect is more excellent. When the content of the (D) component is equal to or less than the upper limit of the above range, the acid taste is more reduced.

[0056] In the present specification, the content of the (D) component is the content as the form of an acid (acid conversion content). That is, in the case where the (D) component forms a salt, the content is based on the molecular weight when the cation is replaced with a proton.

[0057] The content of the (E) component with respect to the total mass of the oral composition is preferably 0.001 to 10 mass%, more preferably 0.1 to 5 mass%. When the content of the (E) component is equal to or more than the lower limit of the above range, the biofilm removal effect is more excellent. When the content of the (E) component is equal to or less than the upper limit of the above range, the flavor is more excellent.

[0058] The molar ratio of the (B) component with respect to the (A) component (hereinafter also referred to as "(B) / (A)") is preferably 0.03 to 10.0, more preferably 0.08 to 2.0. When (B) / (A) is within the above range, the acid taste reduction effect of the (D) component is more excellent.

[0059] The molar ratio of the (C) component with respect to the (A) component (hereinafter also referred to as "(C) / (A)") is preferably 0.005 to 1.5, more preferably 0.01 to 1.3. When (C) / (A) is within the above range, the acid taste reduction effect of the (D) component is more excellent.

[0060] When the molar amount (unit: mmol / g) of the (B) component per 1 g of the oral composition is set as B mmol and the mass ratio (unit: mass%) of the (D) component with respect to the total mass of the oral composition is set as D wt% , the ratio represented by B mmol / D wt% is preferably 0.001 to 5.0, more preferably 0.002 to 2.3.

[0061] The (D) component captures calcium ions, which are footholds of biofilm, and contributes to the biofilm removal effect, and the (B) component, which is a source of calcium ions, contributes to the reduction of the acid taste caused by the (D) component. B mmol / D wt%When the ratio of the above is within the above range, the biofilm removal effect and the sourness reduction effect can be obtained in good balance.

[0062] <water> The oral composition typically further contains water. As the water, purified water, sterilized purified water, water for injection, and the like can be given.

[0063] The content of the water in the oral composition can be appropriately set depending on the product form and the use method of the oral composition.

[0064] For example, when the oral composition is a toothpaste, the content of the water with respect to the total mass of the oral composition is preferably 5 to 90 mass%, more preferably 10 to 60 mass%, and further preferably 20 to 50 mass%.

[0065] <other components> The oral composition can further contain other components in addition to the (A) component, the (B) component, the (C) component, the (D) component, the (E) component, and the water.

[0066] The other components can be appropriately selected from publicly known components in consideration of the form and the use method of the oral composition. As examples of the other components, abrasives, binders, thickening agents, surfactants other than the (E) component, coloring agents, sweeteners, preservatives, flavorings, active ingredients, pH adjustors can be given.

[0067] As the abrasives, for example, silica-based abrasives such as anhydrous silicic acid, precipitated silica, silica gel, aluminum silicate, zirconium silicate, and calcium hydrogen phosphate dihydrate or anhydride, calcium dihydrogen phosphate, calcium phosphate, tetracalcium phosphate, calcium carbonate, calcium hydroxide, aluminum hydroxide, insoluble sodium metaphosphate, magnesium phosphate, and magnesium carbonate can be given. The silica-based abrasives are particularly preferable.

[0068] The content of the abrasives with respect to the total mass of the oral composition is, for example, preferably 0 to 60 mass%, more preferably 0 to 30 mass%, and can also be 25 mass% or less. The content of 0 mass% of the abrasives means that the abrasives are not contained.

[0069] As the binders, for example, organic binders such as water-soluble high molecular substances selected from carboxymethyl cellulose sodium, methyl cellulose, hydroxymethyl cellulose, hydroxyethyl cellulose, and the like, xanthan gum, tragacanth gum, gum karaya, gum arabic, and the like, polyacrylic acid salts such as sodium polyacrylate, and the like, and inorganic binders such as thickening silica, thickening aluminum silicate, Veegum (magnesium aluminum silicate), Laponite (lithium magnesium silicate), and the like can be given.

[0070] The content of the binders with respect to the total mass of the oral composition is, for example, preferably 0.05 to 13.0 mass% When the binder contains an organic binder, the blending amount of the organic binder is more preferably 0.1 to 3% by mass, and further preferably 0.5 to 2.5% by mass, relative to the total mass of the oral composition.

[0071] When the binder contains an inorganic binder, the content of the inorganic binder is more preferably 0 to 10.0% by mass, and further preferably 0 to 8.0% by mass, relative to the total mass of the oral composition, from the viewpoint of adsorption of fluoride ions to the tooth surface.

[0072] As the thickening agent, for example, sugar alcohols such as sorbitol, xylitol, erythritol, and maltitol; polyhydric alcohols such as glycerol, propylene glycol, and polyethylene glycol having an average molecular weight of 160 to 400 (average molecular weight according to the quasi-pharmaceutical raw material standards 2006); and the like can be given.

[0073] The content of the thickening agent is, for example, preferably 20% by mass to 70% by mass, and more preferably 25% by mass to 65% by mass, relative to the total mass of the oral composition.

[0074] As the surfactant other than the (E) component, a surfactant known in the oral composition can be used. For example, nonionic surfactants can be given.

[0075] As the nonionic surfactant, for example, fatty acid glycerol esters such as polyglyceryl-10 laurate; polyoxyethylene sorbitan fatty acid esters such as polyoxyethylene sorbitan monostearate (average addition mole number of ethylene oxide (hereinafter referred to as "E.O.") 20); alkyl glycosides in which the number of carbon atoms of the alkyl group is 12 to 16; sorbitan fatty acid esters such as sorbitan tristearate; sucrose fatty acid esters such as sucrose laurate; and polyoxyethylene alkyl ethers such as polyoxyethylene stearyl ether (E.O. 6) can be given.

[0076] The content of the surfactant other than the (E) component is, for example, preferably 0 to 8.0% by mass, and more preferably 0 to 3.0% by mass, relative to the total mass of the oral composition.

[0077] As the coloring agent, for example, Red No. 2, Red No. 3, Red No. 225, Red No. 226, Yellow No. 4, Yellow No. 5, Yellow No. 205, Blue No. 1, Blue No. 2, Blue No. 201, Blue No. 204, Green No. 3, mica titanium, and titanium oxide can be given.

[0078] As the sweetening agent, for example, sodium saccharin, aspartame, stevioside, stevia extract, p-methoxy cinnamyl aldehyde, neohesperidin dihydrochalcone, and perillartine can be given.

[0079] As the antiseptic, for example, p-hydroxybenzoic acid esters such as methyl p-hydroxybenzoate, ethyl p-hydroxybenzoate, and butyl p-hydroxybenzoate, benzoic acid and its salts such as sodium benzoate can be given.

[0080] As the flavor, for example, natural flavors such as peppermint oil, spearmint oil, anise oil, eucalyptus oil, wintergreen oil, cinnamon oil, clove oil, thyme oil, sage oil, lemon oil, orange oil, mint oil (Japanese: Hakkaoil), cardamom oil, coriander oil, orange peel oil, white lemon oil, lavender oil, rosemary oil, bay oil, chamomile oil, caraway oil, marjoram oil, lemon grass oil, oregano oil, bergamot oil, grapefruit oil, sweetie oil, Japanese yuzu oil, iris extract, peppermint absolute, rose absolute, orange flower, and the like, and flavors obtained by processing (forefraction, afterfraction, fractionation, liquid-liquid extraction, refinement, powder flavoring, and the like) of these natural flavors, menthol, carvone, anethole, eucalyptol, methyl salicylate, cinnamyl aldehyde, eugenol, 3-l-menthoxy-l,2-propanediol, thymol, linalool, linalyl acetate, limonene, menthone, menthyl acetate, N-substituted-p-menthane-3-carboxamide, pinene, octanal, citral, menthofuran, carvacryl acetate, anisaldehyde, ethyl acetate, ethyl butyrate, allyl cyclohexylpropionate, methyl anthranilate, ethyl methyl phenyl glycidate, vanillin, undecanolide, hexanal, butanol, isoamyl alcohol, hexenal, dimethyl sulfide, methyl cyclopentenolone, furfural, trimethyl pyrazine, methyl lactate, ethyl thioacetate, and the like, blended flavoring agents such as strawberry flavor, apple flavor, banana flavor, pineapple flavor, grape flavor, mango flavor, butter flavor, milk flavor, fruit mixed flavor, tropical fruit flavor, and the like, and flavor raw materials known to be used in oral compositions can be given.

[0081] The content of the flavor is not particularly limited, and the content of the above-mentioned flavor raw materials is preferably 0.000001 to 1% by mass with respect to the total mass of the oral composition. The content of the flavoring flavor using the above-mentioned flavor raw materials is preferably 0.05 to 2% by mass with respect to the total mass of the oral composition.

[0082] As the effective ingredient, for example, the following can be mentioned: bactericides such as isopropylmethylphenol, cetylpyridinium chloride, and the like; water-soluble phosphoric acid compounds (except for the (C) component) such as potassium salt, sodium salt, and the like of orthophosphoric acid; enzymes such as dextranase, mutanase, amylase, protease, and the like; tranexamic acid, epsilon-aminocaproic acid, triclosan, lysozyme chloride, allantoin, hinokitiol, ascorbic acid, tocopherol acetate, dihydrocholesterol, alpha-bisabolol, chlorhexidine salts, azulene, copper sodium chlorophyllin, water-soluble copper compounds such as copper gluconate, aluminum lactate, strontium chloride, potassium nitrate, berberine, hydroxamic acid or a derivative thereof, glycyrrhizinic acid or a salt thereof, glycyric acid or a derivative thereof, tartar-preventing agents. The above effective ingredients can be combined in an effective amount within a range not impairing the effects of the present application.

[0083] As the pH adjuster, for example, sodium hydroxide can be mentioned.

[0084] <Form, dosage form> The oral composition can be prepared in various forms such as liquid, paste, gel, solid, and the like.

[0085] The dosage form of the oral composition is not particularly limited. The dosage form of the oral composition is typically an oral preparation which is discharged from the oral cavity after use. As the oral preparation, for example, dentifrices (liquid dentifrice, liquid dentifrice, toothpaste, paste dentifrice, powder dentifrice, and the like), mouthwashes, gargles, coating agents, mouth sprays, patches, tablets, intraoral sustained-release agents, chewing agents, intraoral dissolving agents, intraoral disintegrating agents, tongue care agents, mouth cooling agents, denture care agents, and the like can be mentioned.

[0086] Among them, the oral composition of the present embodiment is preferably a dentifrice, and particularly preferably a toothpaste.

[0087] The oral composition of the present embodiment can be prepared by a publicly known method. For example, it can be prepared by mixing the (A) component, the (B) component, the (C) component, and the (D) component, and other components as necessary, by a conventional method.

[0088] It is considered that in the oral composition, fluoride ions, calcium ions, and phosphorus ions form a complex, and the above complex contributes to the reduction of the sour taste caused by the (D) component.

[0089] The formation of the above complex can be confirmed by observing the crystallite diameter based on X-ray crystal structure analysis and the heat generation peak at around 450°C near the crystal water dissociation of phosphate based on a thermal measurement (TG-DTA measurement). That is, when the complex is formed, the crystallite diameter calculated from the diffraction peak attributed to CaF2 is less than 10 nm due to the complexation with phosphate. In addition, the generation of the peak of the crystal water indicates that the CaF2 found in the X-ray crystal structure analysis is not a crystal composed of only calcium and fluorine ions, but a complex that forms a phosphate interaction.

[0090] Specifically, the formation of the complex is confirmed by identifying that the crystallite diameter is less than 10 nm in the following method (1) and that the heat generation peak at 450°C is present in the following method (2).

[0091] (1) Crystallite diameter The sample was measured with an X-ray structure diffraction device (light source Cu: Kα, 40 kV, 20 mA, divergence slit 1 / 2 deg, scattering slit 1 / 2 deg, light receiving slit 0.15 mm, scanning speed 4.000° / min, 2θ = 2.000 ~ 80.000°), and the crystallite diameter was calculated by the following formula (Scherrer formula) to evaluate the presence or absence of complex formation.

[0092] L = Kλ / (βcosθ) L: crystallite diameter, K: coefficient 0.9, β: half width, λ: 1.54056 A, θ: diffraction angle (2) TG-DTA measurement (heat generation peak) Temperature increase rate: 5°C / min, measurement range: 25°C ~ 600°C As the method of forming the above complex, there is no particular limitation, and it is preferable to adopt either of the procedures of combining the (B) component after combining the (A) component and the (C) component and the procedure of combining the (B) component and the (C) component after combining the (A) component, for example, when preparing the oral composition. In addition, if the (A) component and the (B) component are combined at the same time, calcium fluoride is partially generated, and the efficiency of the formation of the complex can be deteriorated.

[0093] The oral composition described above contains the (A) component, the (B) component, the (C) component, and the (D) component, and thus has an excellent biofilm removal effect, and the (D) component is contained to suppress the sour taste, and the flavor is good.

[0094] Examples Hereinafter, examples will be shown to describe the present application in detail, but the present application is not limited by the following description.

[0095] In addition, in the following examples, " % " as a content unit means " mass % " unless otherwise specified.

[0096] <Use of raw materials> [Component (A)] Sodium fluoride: manufactured by Stella Chemifa Corp. Hereinafter, also referred to as "NaF".

[0097] [Component (B)] Calcium glycerophosphate: manufactured by Iwanami Pharmaceutical Co., Ltd. Hereinafter, also referred to as "glycerophosphate Ca".

[0098] Calcium lactate hydrate: manufactured by Taihei Chemical Industry Co., Ltd., trade name "Calcium Lactate". Hereinafter, also referred to as "lactate Ca".

[0099] Calcium gluconate: manufactured by Fusosan Chemical Industry Co., Ltd. Hereinafter, also referred to as "gluconate Ca".

[0100] Calcium pantothenate: manufactured by BASF. Hereinafter, also referred to as "pantothenate Ca".

[0101] [Component (C)] Tetrapotassium pyrophosphate: manufactured by Taihei Chemical Industry Co., Ltd. Hereinafter, also referred to as "pyrophosphate K".

[0102] Sodium pyrophosphate: manufactured by Taihei Chemical Industry Co., Ltd., product name "Sodium Pyrophosphate (anhydrous)". Hereinafter, also referred to as "pyrophosphate Na".

[0103] Sodium tripolyphosphate: manufactured by Taihei Chemical Industry Co., Ltd. Hereinafter, also referred to as "tripolyphosphate Na".

[0104] [Component (D)] Malic acid: manufactured by Fusosan Chemical Industry Co., Ltd.

[0105] Citric acid: manufactured by Fusosan Chemical Industry Co., Ltd.

[0106] Phytic acid: manufactured by Fusosan Chemical Industry Co., Ltd. Concentration 50 mass% aqueous solution.

[0107] Edetate disodium; manufactured by Junsei Chemical Co., Ltd. Hereinafter, also referred to as "edetate Na".

[0108] Tartaric acid: manufactured by Fusosan Chemical Industry Co., Ltd.

[0109] Succinic acid: manufactured by Fusosan Chemical Industry Co., Ltd.

[0110] Fumaric acid: manufactured by Fusosan Chemical Industry Co., Ltd.

[0111] [Component (E)] Cocamidopropyl betaine: manufactured by Evonik Japan Co., Ltd., product name "TEGO BETAIN CK OKMB". Hereinafter also referred to as "amidopropyl betaine".

[0112] Sodium lauryl sulfate: manufactured by BASF, product name "Texapon OC-P". Hereinafter also referred to as "sodium lauryl sulfate Na". Hereinafter also referred to as "sodium lauryl sulfate Na".

[0113] Sodium N-lauroyl sarcosinate: manufactured by Nikko Chemicals Co., Ltd., product name "NIKKOL Sarcosinate LN". Hereinafter also referred to as "sodium lauroyl sarcosinate".

[0114] Sodium N-lauroyl methyl taurate: manufactured by Nikko Chemicals Co., Ltd., product name "NIKKOL LMT-P". Hereinafter also referred to as "sodium lauroyl methyl taurate".

[0115] [Perfume] Perfume composition A described in Table 5 below.

[0116] [Water] Purified water [Common ingredients (optional ingredients)] Anhydrous silicic acid (abrasive silica) 10%, sorbitol solution (concentration 70%, thickening agent) 40%, propylene glycol (thickening agent) 3%, xanthan gum (binder) 0.5%, and sodium saccharin (sweetening agent) 0.2%. Total 53.7%.

[0117] [Examples 1 to 28, Comparative Examples 1 to 4] Oral compositions (toothpastes) of the compositions shown in Tables 1 to 4 were prepared by a conventional method. The components were mixed in the order of an aqueous solution of the (C) component, an aqueous solution of the (B) component, and an aqueous solution of the (A) component to prepare a premix. The amount of water was set to the amount required to become the composition shown in the table. An A phase in which water-soluble components (D component, sorbitol solution, sodium saccharin) were added and dissolved in the premix was prepared. On the other hand, a B phase in which xanthan gum was dissolved and dispersed in propylene glycol at room temperature was prepared. Next, the B phase was added to the A phase under stirring to prepare a C phase.

[0118] To the C phase, the E component, perfume, and anhydrous silicic acid were added, mixed at room temperature using a 1.5L kneader (manufactured by Ishiyama Works), degassed under reduced pressure to 4 kPa, and thus 1.0 kg of toothpaste was obtained.

[0119] In the toothpaste of each example, it was confirmed that fluoride ions, calcium ions, and phosphorus ions formed a complex by the above method.

[0120] The blank in the table indicates that the ingredient is not blended. The "balance" of purified water indicates the amount to make the total of the oral composition 100%.

[0121] The resulting oral composition (toothpaste) was evaluated as follows. The results are collectively shown in the table.

[0122] <Method of evaluation> [Effect of biofilm (BF) removal] (1) Method of producing model biofilm A hydroxyapatite (HA) plate (manufactured by Asahi Techno Glass Corporation) having a diameter of 7 mm x thickness of 3.5 mm was treated with human non-irritating saliva filtered with a 0.45 μm filter for 4 hours, and used as a carrier for producing a model biofilm. As a culture solution, a mucin basal medium (Basal Medium Mucin) culture solution (BMM, the composition of which is described later) was used. The strains used for producing the model biofilm were Actinomyces viscosus ATCC43146, Veillonella parvula ATCC17745, Fusobacterium nucleatum ATCC10953, Streptococcus oralis ATCC10557, and Streptococcus mutans ATCC25175, which were purchased from American Type Culture Collection. These five strains were inoculated into a Rotating Disk Reactor (culture tank) to which BMM had been previously added at 3000 mL, so that they were 1 x 10 7 cfu / mL (cfu: colony forming units) each, and cultured at 37°C under anaerobic conditions (5 vol% carbon dioxide gas, 95 vol% nitrogen gas) for 24 hours together with the HA carrier treated with saliva. Then, the BMM culture medium was continuously supplied at a rate of 5 vol% per hour under the same conditions for 10 days, and a model biofilm of a mixture of the five strains was formed on the surface of the HA plate.

[0123] The above BMM was obtained by mixing the following ingredients (mass in 1 liter) and adjusting the total volume to 1 L, and treating with an autoclave at 121°C for 20 minutes.

[0124] Proteose peptone (manufactured by Becton and Dickinson Company): 4 g / L Trypticase (manufactured by Becton and Dickinson Company): 2 g / L Yeast extract (manufactured by Becton and Dickinson Company): 2 g / L Mucin (manufactured by Sigma): 5 g / L Hemin chloride (manufactured by Sigma): 2.5 mg / L Vitamin K (manufactured by Wako Pure Chemical Industries, Ltd.): 0.5 mg / L KCl (manufactured by Wako Pure Chemical Industries, Ltd.): 1 g / L Cysteine (manufactured by Wako Pure Chemical Industries, Ltd.): 0.2 g / L Distilled water: balance (2) Evaluation method of model biofilm removal effect The model biofilm formed in the above (1) was moved to a 24-well multiwell plate (Sumitomo Bakelite Co., Ltd.), 2 mL of the test composition was added, and it was immersed for 3 minutes. As the test composition, the centrifugal supernatant (10000 rpm, 10 minutes) of a dilution liquid in which each of the dentifrice compositions was diluted 3 times with saliva collected from a healthy person was used. Then, it was washed 6 times with 1 mL of a phosphate buffer (PBS, manufactured by Wako Pure Chemical Industries, Ltd.), dispersed in a test tube (diameter 13 mm x 100 mm) to which 2 mL of the same phosphate buffer was added by ultrasonic treatment (200 μA, 10 seconds), and a test solution was obtained. The turbidity (OD) of the test solution was measured at a wavelength of 550 nm, and the biofilm residual amount was measured. The removal rate with respect to the control was calculated by the following formula, and based on the removal rate, the oral biofilm removal effect was determined based on the following criteria. As the control, a liquid obtained in the same manner as the test solution except that the test composition was replaced with the phosphate buffer was used.

[0125] Biofilm removal rate (%) = (turbidity of the control - turbidity of the test solution) / turbidity of the control x 100 [Criteria for determining biofilm removal effect] ◎: Biofilm removal rate is 90% or more.

[0126] O: Biofilm removal rate is 80% or more and less than 90%.

[0127] Δ: Biofilm removal rate is 70% or more and less than 80%.

[0128] X: Biofilm removal rate is less than 70%.

[0129] [Flavor (degree of non-acidic taste)] The evaluation was performed by a sensory test by 10 panelists as subjects. 1 g of the dentifrice composition was extruded from a tube container in which each of the dentifrice compositions was housed, placed on a toothbrush (manufactured by Lion Corporation, Clinica brush 4-row head, medium size), and brushing was performed for 3 minutes, and the sour taste felt during use was determined based on the following scoring criteria. The average of the scores of 10 persons was calculated, and the flavor (degree of no sour taste) was evaluated based on the following evaluation criteria.

[0130] (Score Criteria) 4 points: no sour taste was felt.

[0131] 3 points: a slight sour taste was felt.

[0132] 2 points: a sour taste was felt.

[0133] 1 point: a strong sour taste was felt.

[0134] (Evaluation Criteria) ◎: average of 3.5 points or more.

[0135] O: average of 3.0 points or more and less than 3.5 points.

[0136] X: average of less than 3.0 points.

[0137] [Table 1]

[0138] [Table 2]

[0139] [Table 3]

[0140] [Table 4]

[0141] As shown in the above results, the biofilm removal effect of the oral compositions of Examples 1 to 28 was excellent. Furthermore, although containing the (D) component, the sour taste was sufficiently reduced, and the flavor was excellent.

[0142] On the other hand, in the case of Comparative Example 1 not containing the (C) component, Comparative Example 2 not containing the (B) component, and Comparative Example 3 not containing the (A) component, the reduction of the sour taste was insufficient.

[0143] In the case of Comparative Example 4 not containing the (D) component, the biofilm removal effect was poor.

[0144] (Formulation Examples) In any of the following formulation examples, the biofilm removal effect and the flavor (degree of no sour taste) were excellent.

[0145] <Formula Example 1 Toothpaste> Sodium fluoride 0.32% Calcium glycerophosphate 0.2% Tetrapotassium pyrophosphate 0.1% Citric acid 0.5% Anhydrous silicic acid 10% Sorbitol solution (70%) 40% Propylene glycol 3% Xanthan gum 0.5% Sodium polyacrylate 0.5% Cocamidopropyl betaine 0.5% Sodium saccharin 0.2% Flavor composition A 1% Purified water q.s. <Formula Example 2 Toothpaste> Sodium fluoride 0.32% Calcium glycerophosphate 0.2% Tetrapotassium pyrophosphate 0.1% Malic acid 0.5% Anhydrous silicic acid 10% Sorbitol solution (70%) 40% Propylene glycol 3% Xanthan gum 0.5% Sodium polyacrylate 0.5% Cocamidopropyl betaine 0.5% Sodium saccharin 0.2% Flavor composition A 1% Purified water q.s. <Formula Example 3 Toothpaste> Sodium fluoride 0.32% Calcium glycerophosphate 0.2% Tetrapotassium pyrophosphate 0.1% Phytic acid 0.5% Anhydrous silicic acid 10% Sorbitol solution (70%) 40% Propylene glycol 3% Xanthan gum 0.5% Sodium polyacrylate 0.5% Cocamidopropyl betaine 0.5% Sodium saccharin 0.2% Flavor composition A 1% Purified water q.s. <Formula Example 4 Toothpaste> Sodium fluoride 0.32% Calcium glycerophosphate 0.2% Tetrapotassium pyrophosphate 0.1% Disodium edetate 0.5% 10% anhydrous silica Sorbitol solution (70%) 40% 3% propylene glycol Xanthan gum 0.5% Sodium polyacrylate 0.5% Cocamidopropyl betaine 0.5% Sodium saccharin 0.2% Fragrance Composition A 1% Purified water balance <Formulation Example 5: Liquid Dental Cleaner> Sodium fluoride 0.32% Calcium glycerol phosphate 0.2% Tetrapotassium pyrophosphate 0.1% Malic acid 0.5% Glycerin 7.5% 3% propylene glycol Sorbitol solution (70%) 5% Cocamidopropyl betaine 0.3% Fragrance composition A 0.2% Purified water balance <Formulation Example 6: Mouthwash> Sodium fluoride 0.1% Calcium glycerol phosphate 0.5% Tetrapotassium pyrophosphate 0.1% Malic acid 0.5% 3% glycerol 2% propylene glycol Sorbitol solution (70%) 3% Fragrance composition A 0.2% Purified water balance Furthermore, in the above formulation examples 1 to 6, except that flavoring compositions B to P described in Tables 5 and 6 below were used to replace flavoring composition A, tooth cleaners, liquid tooth cleaners, or mouthwashes with the same composition were prepared, all of which had good biofilm removal effect and good flavor.

[0146] The compositions of fragrance 1 to fragrance 7 and solvents recorded in Tables 5 and 6 are shown in Tables 7 to 14.

[0147] Additionally, "removed a% of the first fraction" in the table means that the initial a% of the fractionated essential oil was removed, and "removed b% of the first and last fractions" means that the initial b% and the final b% of the fractionated essential oil were removed.

[0148] [Table 5]

[0149] [table 6]

[0150] [table 7]

[0151] [table 8]

[0152] [table 9]

[0153] [table 10]

[0154] [table 11]

[0155] [table 12]

[0156] [table 13]

[0157] [table 14]

Claims

1. An oral composition comprising: (A) Sodium fluoride, (B) Selected from one or more of calcium glycerophosphate, calcium gluconate, calcium lactate, and calcium pantothenate. (C) Selected from one or more of condensed phosphoric acid and its alkali metal salts, and (D) Selected from one or more organic acids and their salts, wherein, Except for component (B) above.

2. The oral composition according to claim 1, wherein, The component (C) comprises one or more selected from pyrophosphate and alkali metal pyrophosphate.

3. The oral composition according to claim 1, wherein, When the molar amount (unit: mmol / g) of component (B) in each 1g of the oral composition is denoted as B mmol The mass ratio (in mass%) of component (D) relative to the total mass of the oral composition is denoted as D. wt% At that time, with B mmol / D wt% The ratios represented are 0.001 to 5.

0.

4. The oral composition according to claim 1, wherein, The (D) component comprises one or more selected from citric acid, malic acid, tartaric acid, succinic acid, fumaric acid, edemanic acid, phytic acid, and their salts.

5. The oral composition according to claim 1, wherein, The content of component (A) is 0.09 to 1.3% by mass, the content of component (B) is 0.02 to 5.0% by mass, the content of component (C) is 0.02 to 3.0% by mass, and the content of component (D) is 0.001 to 5% by mass relative to the total mass of the oral composition.

6. The oral composition according to claim 1, wherein, The molar ratio of component (B) to component (A) is 0.03 to 10.0, and the molar ratio of component (C) to component (A) is 0.005 to 1.

5.

7. The oral composition according to claim 1, wherein, The oral composition further comprises (E) one or more selected from amphoteric surfactants and anionic surfactants.

8. The oral composition according to claim 7, wherein, The (E) component comprises one or more selected from amide alkyl betaine, lauryl sulfate, N-acyl taurine and N-acyl amino acid salt.

9. The oral composition according to claim 7, wherein, The content of component (E) relative to the total mass of the oral composition is 0.001 to 10 by mass.

10. The oral composition according to any one of claims 1 to 9, wherein, The oral composition is a dental cleaning agent.

Citation Information

Patent Citations

  • Toothpaste composition

    JP2020033291A