Oral composition
An oral composition combining sodium fluoride, calcium salts, and phosphoric acid salts with surfactants addresses the sour taste issue of organic acids, achieving effective biofilm removal and improved flavor.
Patent Information
- Application Number
- JP2024098780
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- Filing Date
- 2024-06-19
- Publication Date
- 2026-01-07
AI Technical Summary
Existing oral compositions that inhibit biofilm formation, such as those containing sodium lauryl sulfate and κ-carrageenan with organic acids, often have an undesirable sour taste due to the inclusion of malic acid, citric acid, and phytic acid.
An oral composition comprising sodium fluoride, calcium glycerophosphate, calcium gluconate, calcium lactate, calcium pantothenate, condensed phosphoric acids, and organic acids, along with surfactants, to balance biofilm removal efficacy with a pleasant flavor.
The composition achieves effective biofilm removal while reducing sourness and improving flavor, using a combination of calcium and phosphoric acid salts to neutralize the sour taste of organic acids.
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Abstract
Description
[Technical Field]
[0001] The present invention relates to an oral composition. [Background technology]
[0002] Inhibition of the formation of biofilms in the oral cavity, such as dental plaque and tongue coating, is desirable from the perspective of preventive dentistry. Patent Document 1 describes an example of an oral composition that is a toothpaste composition having a biofilm formation inhibitory effect, which contains sodium lauryl sulfate, an anionic surfactant, and κ-carrageenan, a binder, in a specific mass ratio, and further contains specific organic acids (malic acid, citric acid, phytic acid) as components that enhance the dispersibility of the κ-carrageenan and sodium lauryl sulfate. [Prior art documents] [Patent documents]
[0003] [Patent Document 1] Japanese Patent Application Publication No. 2020-033291 Summary of the Invention [Problem to be solved by the invention]
[0004] However, the sour taste of organic acids (malic acid, citric acid, phytic acid) can sometimes result in a flavor that is undesirable to users. An object of the present invention is to provide an oral composition that has a biofilm removing effect and a good flavor. [Means for solving the problem]
[0005] The present invention has the following aspects. [1] An oral composition containing (A) sodium fluoride, (B) one or more members selected from the group consisting of calcium glycerophosphate, calcium gluconate, calcium lactate, and calcium pantothenate, (C) one or more members selected from the group consisting of condensed phosphoric acids and alkali metal salts thereof, and (D) one or more members selected from the group consisting of organic acids and salts thereof (excluding the component (B)). [2] The oral composition according to [1], wherein the component (C) comprises at least one selected from the group consisting of pyrophosphoric acid and alkali metal pyrophosphates. [3] The molar amount (unit: mmol / g) of the component (B) per 1 g of the oral composition is B mmol The mass ratio (unit: mass%) of the component (D) to the total mass of the oral composition is D wt% When B mmol / D wt% The oral composition according to [1] or [2], wherein the ratio represented by the formula (I) is 0.001 to 5.0. [4] The oral composition according to any one of [1] to [3], wherein the component (D) 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. [5] The oral composition according to any one of [1] to [4], further comprising (E) one or more surfactants selected from the group consisting of amphoteric surfactants and anionic surfactants. [6] The oral composition according to any one of [1] to [5], which is a dentifrice. [Effects of the Invention]
[0006] According to the present invention, an oral composition having a biofilm removing effect and a good flavor can be obtained. DETAILED DESCRIPTION OF THE INVENTION
[0007] As used herein, "oral composition" means a composition intended primarily for use in the oral cavity. In this specification, "water-soluble" means that the solubility in water at 20°C is 1 g / 100 g or more. In this specification, the use of "to" to indicate a range of values means that the values before and after it are included as the lower and upper limits.
[0008] [Oral composition] The oral composition of the present invention contains component (A), component (B), component (C), and component (D), and preferably further contains component (E).
[0009] <Component (A)> Component (A) is sodium fluoride (NaF). Component (A) reduces the sourness caused by component (D) and contributes to improving the flavor. Component (A) can be a commercially available product.
[0010] <(B) component> Component (B) is one or more water-soluble calcium salts selected from the group consisting of calcium glycerophosphate, calcium gluconate, calcium lactate, and calcium pantothenate. Component (B) may be a combination of two or more types. Component (B) reduces the sourness caused by component (D) and contributes to improving the flavor. Component (B) can be a commercially available product.
[0011] <(C) component> Component (C) is at least one selected from the group consisting of condensed phosphoric acid and alkali metal salts thereof. Component (C) may be a combination of two or more types. Component (C) reduces the sourness caused by component (D) and contributes to improving the flavor.
[0012] As the condensed phosphoric acid or its alkali metal salt, a water-soluble condensed phosphoric acid or its salt can be preferably used. Examples of condensed phosphoric acid include linear polyphosphoric acids such as pyrophosphoric acid, tripolyphosphoric acid, and tetrapolyphosphoric acid; and cyclic polyphosphoric acids such as trimetaphosphoric acid, tetrametaphosphoric acid, and hexametaphosphoric acid. Examples of the alkali metal salt of condensed phosphoric acid include sodium salt and potassium salt. In particular, from the viewpoint of flavor improving effect, pyrophosphate, tripolyphosphate, and hexametaphosphate are preferred, and pyrophosphate is more preferred, specifically potassium pyrophosphate and sodium pyrophosphate are particularly preferred. Component (C) can be a commercially available product.
[0013] Component (C) preferably includes component (C1), which is at least one selected from the group consisting of pyrophosphoric acid and alkali metal pyrophosphates. Component (C1) is particularly effective in improving flavor. The proportion of the (C1) component relative to the total mass of the (C) component may be, 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, or may be 100 mass%.
[0014] <(D) component> Component (D) is one or more selected from the group consisting of organic acids and their salts (excluding component (B)). Two or more types of component (D) may be combined. Component (D) contributes to the biofilm removal effect. Examples of organic acids include citric acid, malic acid, tartaric acid, succinic acid, fumaric acid, edetic acid, and phytic acid, with citric acid, malic acid, edetic acid, and phytic acid being preferred. As the salt of component (D), alkali metal salts such as sodium salts and potassium salts are preferred. Component (D) can be a commercially available product.
[0015] Component (D) preferably includes component (D1), which is 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. The proportion of the (D1) component relative to the total mass of the (D) component may be, 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, or may be 100 mass%.
[0016] <(E) component> Component (E) is one or more surfactants selected from the group consisting of amphoteric surfactants and anionic surfactants. Two or more types of component (E) may be combined. Component (E) can be a commercially available product. Component (E) contributes to the biofilm removal effect.
[0017] [Amphoteric surfactants] Examples of amphoteric surfactants include amidoalkyl betaines such as coconut oil fatty acid amidopropyl betaine, lauryl dimethylaminoacetic acid betaine, and N-coconut oil fatty acid acyl-N-carboxymethyl-N-hydroxyethylethylenediamine.
[0018] [Anionic surfactants] Examples of anionic surfactants include alkyl sulfates, N-acyltaurine salts, N-acylamino acid salts, α-olefin sulfonates, sodium dodecylbenzenesulfonate, and sodium lauryl sulfoacetate. As the alkyl sulfate, sodium lauryl sulfate and sodium myristyl sulfate are preferred.
[0019] The number of carbon atoms in the acyl group in the N-acyltaurine salt is preferably 10 to 20. As the salt, alkali metal salts such as sodium salts and potassium salts are preferred, and sodium salts are more preferred. Examples of N-acyltaurate salts include N-acylmethyltaurine salts such as sodium N-cocoylmethyltaurine, potassium N-cocoylmethyltaurine, sodium N-lauroylmethyltaurine, sodium N-stearoylmethyltaurine, sodium N-myristoylmethyltaurine, sodium N-oleoylmethyltaurine, and sodium N-palmitoylmethyltaurine, as well as sodium N-cocoyltaurine, etc. Among these, N-acylmethyltaurine salts are preferred, and sodium N-acylmethyltaurine is more preferred.
[0020] The number of carbon atoms in the acyl group in the N-acylamino acid salt is preferably 8 to 18, more preferably 10 to 16. As the salt, alkali metal salts such as sodium salts and potassium salts are preferred, and sodium salts are more preferred. Examples of N-acyl amino acid salts include N-acyl acidic amino acid salts such as N-acyl glutamate and N-acylaspartate; N-acyl neutral amino acid salts such as N-acyl sarcosine salt, N-acyl methylalanine salt, N-acyl glycine salt and N-acylalanine salt; and acyl basic amino acid salts such as N-acyl arginine ethyl ester salt. Among these, N-acyl neutral amino acid salts are preferred, and N-acyl sarcosine salt is more preferred. The N-acyl sarcosine salt is preferably one having an acyl group with the above carbon number, such as N-cocoyl sarcosine salt, N-lauroyl sarcosine salt, N-palmitoyl sarcosine salt, etc. Among these, sodium N-lauroyl sarcosine is preferred.
[0021] The number of carbon atoms in the α-olefin sulfonate is preferably 8 to 18, more preferably 14 to 16. As the salt, alkali metal salts such as sodium salts and potassium salts are preferred, and sodium salts are more preferred. As the α-olefin sulfonate, an α-olefin sulfonate having 14 carbon atoms, particularly a sodium salt (general name: sodium tetradecene sulfonate) is preferred.
[0022] Component (E) preferably includes component (E1), which is one or more selected from the group consisting of amidoalkyl betaine, lauryl sulfate, N-acyltaurine salt, and N-acylamino acid salt. Component (E1) has superior biofilm removal ability. Amidoalkyl betaine is particularly preferred in terms of its mildness. The proportion of the (E1) component relative to the total mass of the (E) component may be, 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, or may be 100 mass%.
[0023] <Content of each ingredient> The content of component (A) is preferably 0.09 to 1.3% by mass, more preferably 0.10 to 1.1% by mass, based on the total mass of the oral composition. When the content of component (A) is equal to or greater than the lower limit, the effect of reducing the sourness of component (D) is more excellent. When the content of component (A) is equal to or less than the upper limit, the flavor is more excellent.
[0024] The content of component (B) is preferably 0.02 to 5.0% by mass, more preferably 0.03 to 3.0% by mass, based on the total mass of the oral composition. When the content of component (B) is equal to or greater than the lower limit, the effect of reducing the sourness of component (D) is more excellent. When the content of component (B) is equal to or less than the upper limit, the flavor is more excellent.
[0025] The content of component (C) is preferably 0.02 to 3.0% by mass, more preferably 0.03 to 1.3% by mass, based on the total mass of the oral composition. When the content of component (C) is equal to or greater than the lower limit, the effect of reducing the sourness of component (D) is more excellent. When the content of component (C) is equal to or less than the upper limit, the flavor is more excellent.
[0026] The content of component (D) is preferably 0.001 to 5% by mass, more preferably 0.01 to 2% by mass, based on the total mass of the oral composition. When the content of component (D) is equal to or greater than the above-mentioned lower limit, the biofilm removal effect is more excellent. When the content of component (D) is equal to or less than the above-mentioned upper limit, the sourness is further reduced. In this specification, the content of component (D) is the content in the form of an acid (converted to acid content). In other words, when component (D) forms a salt, the content is based on the molecular weight when cations are replaced with protons.
[0027] The content of component (E) is preferably 0.001 to 10% by mass, more preferably 0.1 to 5% by mass, based on the total mass of the oral composition. When the content of component (E) is equal to or greater than the above-mentioned lower limit, the biofilm removal effect is more excellent. When the content of component (E) is equal to or less than the above-mentioned upper limit, the flavor is more excellent.
[0028] The molar ratio of component (B) to component (A) (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 effect of reducing the sourness of component (D) is more excellent.
[0029] The molar ratio of component (C) to component (A) (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 effect of reducing the sourness of component (D) is more excellent.
[0030] The molar amount of component (B) per 1 g of oral composition (unit: mmol / g) is B mmol The mass ratio (unit: mass%) of component (D) to the total mass of the oral composition is D wt% When B mmol / D wt% The ratio represented by the formula (1) is preferably 0.001 to 5.0, and more preferably 0.002 to 2.3. Component (D) supplements calcium ions, which act as a scaffold for biofilms, contributing to the biofilm removal effect, while component (B), which serves as a calcium ion source, contributes to reducing the sourness of component (D). mmol / D wt% When the ratio is within the above range, a good balance of the biofilm removal effect and the sourness reduction effect can be obtained.
[0031] <Water> The oral composition typically further contains water, such as purified water, sterilized purified water, and water for injection. The content of water in the oral composition can be appropriately set depending on the product form and method of use of the oral composition. For example, when the oral composition is a toothpaste, the content of water relative to the total mass of the oral composition is preferably 5 to 90 mass%, more preferably 10 to 60 mass%, and even more preferably 20 to 50 mass%.
[0032] <Other ingredients> The oral composition may further contain other components in addition to the components (A), (B), (C), (D), (E) and water. The other components can be appropriately selected from known components taking into consideration the form and method of use of the oral composition, etc. Examples of other components include abrasives, binders, thickeners, surfactants other than component (E), colorants, sweeteners, preservatives, flavorings, active ingredients, and pH adjusters.
[0033] Examples of abrasives include silica-based abrasives such as silicic acid anhydride, precipitated silica, silica gel, aluminosilicate, and zirconosilicate; dibasic calcium phosphate dihydrate or anhydrate, monobasic calcium phosphate, tribasic calcium phosphate, tetrabasic calcium phosphate, calcium carbonate, calcium hydroxide, aluminum hydroxide, insoluble sodium metaphosphate, tribasic magnesium phosphate, and magnesium carbonate. Silica-based abrasives are particularly preferred. The content of the abrasive is, for example, preferably 0 to 60% by mass, more preferably 0 to 30% by mass, and may be 25% by mass or less, relative to the total mass of the oral composition. An abrasive content of 0% by mass means that no abrasive is contained.
[0034] Examples of binders include organic binders selected from water-soluble polymeric substances such as cellulose derivatives such as sodium carboxymethylcellulose, methylcellulose, hydroxymethylcellulose, and hydroxyethylcellulose; gums such as xanthan gum, tragacanth gum, karaya gum, and gum arabic; and polyacrylates such as sodium polyacrylate; and inorganic binders such as thickening silica, thickening aluminum silica, Veegum, and Laponite. The content of the binder is preferably, for example, 0.05 to 13.0% by mass relative to the total mass of the oral composition. When the binder contains an organic binder, the blending amount of the organic binder is more preferably 0.1 to 3 mass %, and even more preferably 0.5 to 2.5 mass %, relative to the total mass of the oral composition. When the binder contains an inorganic binder, the content of the inorganic binder is more preferably 0 to 10.0 mass %, and even more preferably 0 to 8.0 mass %, relative to the total mass of the oral composition, in terms of the adsorption of fluoride ions to the tooth surface.
[0035] Examples of thickening agents include sugar alcohols such as sorbitol, xylitol, erythritol, and maltitol, and polyhydric alcohols such as glycerin, propylene glycol, and polyethylene glycol having an average molecular weight of 160 to 400 (average molecular weight according to the Quasi-drug Raw Materials Standards 2006). The content of the thickener is, for example, preferably 20 to 70% by mass, more preferably 25 to 65% by mass, relative to the total mass of the oral composition.
[0036] As the surfactant other than component (E), any surfactant known in oral compositions can be used, such as a nonionic surfactant. Examples of nonionic surfactants include glycerin fatty acid esters such as decaglycerol laurate, polyoxyethylene sorbitan fatty acid esters such as polyoxyethylene sorbitan monostearate (average number of moles of ethylene oxide added (hereinafter abbreviated as "EO"): 20), alkyl glycosides having an alkyl group with 12 to 16 carbon atoms, 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 (EO6). The content of surfactants other than component (E) is, for example, preferably 0 to 8.0% by mass, more preferably 0 to 3.0% by mass, relative to the total mass of the oral cavity composition.
[0037] Examples of colorants include 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, titanium mica, and titanium oxide. Examples of sweeteners include saccharin sodium, aspartame, stevioside, stevia extract, paramethoxycinnamic aldehyde, neohesperidin dihydrochalcone, and perillartine. Examples of preservatives include parahydroxybenzoic acid esters such as methylparaben, ethylparaben, and butylparaben, and benzoic acid or a salt thereof such as sodium benzoate.
[0038] Examples of fragrances include peppermint oil, spearmint oil, anise oil, eucalyptus oil, wintergreen oil, cassia oil, clove oil, thyme oil, sage oil, lemon oil, orange oil, peppermint oil, cardamom oil, coriander oil, mandarin oil, lime oil, lavender oil, rosemary oil, laurel oil, chamomile oil, caraway oil, marjoram oil, bay oil, lemongrass oil, origanum oil, pine needle oil, neroli oil, rose oil, jasmine oil, and grapefruit oil. Natural fragrances such as citrus oil, sweetie oil, yuzu oil, iris concrete, peppermint absolute, rose absolute, orange flower, and processed fragrances (front distillation, tail distillation, liquid-liquid extraction, essence, powder fragrance, etc.) of these natural fragrances, menthol, carvone, anethole, cineole, methyl salicylate, cinnamic aldehyde, eugenol, 3-l-menthoxypropane-1,2-diol, thymol, linalool, linalyl aqua Examples of flavoring materials that can be used include single flavors such as acetate, limonene, menthone, menthyl acetate, N-substituted-paramenthan-3-carboxamide, pinene, octyl aldehyde, citral, pulegone, carbyl acetate, anisaldehyde, ethyl acetate, ethyl butyrate, allyl cyclohexane propionate, methyl anthranilate, ethyl methylphenyl glycidate, vanillin, undecalactone, hexanal, butanol, isoamyl alcohol, hexenol, dimethyl sulfide, cyclotene, furfural, trimethylpyrazine, ethyl lactate, and ethyl thioacetate, and compound flavors such as strawberry flavor, apple flavor, banana flavor, pineapple flavor, grape flavor, mango flavor, butter flavor, milk flavor, fruit mix flavor, and tropical fruit flavor. These flavoring materials can also be used in combination with other flavoring materials known for oral compositions. The content of the flavoring material is not particularly limited, but the content of the above-mentioned flavoring material is preferably 0.000001 to 1% by mass relative to the total mass of the oral composition. The content of the flavoring material used for flavoring is preferably 0.05 to 2% by mass relative to the total mass of the oral composition.
[0039] Examples of active ingredients include disinfectants such as isopropylmethylphenol and cetylpyridinium chloride, water-soluble phosphate compounds such as potassium and sodium orthophosphate (excluding component (C)), enzymes such as dextranase, mutanase, amylase, and protease, tranexamic acid, epsilon aminocaproic acid, triclosan, lysozyme chloride, aluminum chlorohydroxyallantoin, hinokitiol, ascorbic acid, tocopherol acetate, dihydrocholesterol, α-bisabolol, chlorhexidine salts, azulene, water-soluble copper compounds such as copper chlorophyllin sodium, chlorophyll, and copper gluconate, aluminum lactate, strontium chloride, potassium nitrate, berberine, hydroxamic acid or a derivative thereof, glycyrrhizic acid or a salt thereof, glycyrrhetinic acid or a derivative thereof, and anti-tartar agents. The above active ingredients can be incorporated in effective amounts within a range that does not interfere with the effects of the present invention.
[0040] An example of a pH adjuster is sodium hydroxide.
[0041] <Form, dosage form> The oral composition can be prepared in various forms, for example, liquid, paste, gel, or solid. The dosage form of the oral composition is not particularly limited. The dosage form of the oral composition is typically an oral preparation that is expelled from the oral cavity after use. Examples of oral preparations include dentifrices (liquid dentifrices, liquid dentifrices, toothpastes, lubricating dentifrices, powder dentifrices, etc.), mouthwashes, mouthwashes, liniments, mouth sprays, patches, sheets, oral sustained-release agents, chewable agents, oral dissolving agents, oral disintegrating agents, tongue care agents, mouth fresheners, denture care agents, etc. Among the above, the oral composition of the present embodiment is suitable as a dentifrice, and is particularly suitable as a toothpaste.
[0042] The oral composition of this embodiment can be prepared by a known method, for example, by mixing components (A), (B), (C), and (D), and optionally other components, by a conventional method.
[0043] In the oral composition, fluoride ions, calcium ions, and phosphorus ions form a complex, and it is believed that this complex contributes to the reduction of the sourness caused by component (D). The formation of the complex can be confirmed by observing the crystallite size by X-ray crystal structure analysis and the exothermic peak observed when water of crystallization near the phosphate group is released at around 450 °C by calorimetry (TG-DTA measurement). In other words, when the complex is formed, the crystallite size determined from the diffraction peaks attributable to CaF2 becomes less than 10 nm due to the complexation with the phosphate group. Furthermore, the appearance of a peak for water of crystallization indicates that the CaF2 observed in X-ray crystal structure analysis is not a crystal composed only of calcium and fluoride ions, but forms a complex in which the phosphate group interacts. Specifically, the formation of a complex is confirmed by the fact that the crystallite size is less than 10 nm as determined by the following method (1) and the presence of an exothermic peak at 450°C as determined by the following method (2). (1) Crystallite size The sample was measured using an X-ray structural diffractometer (light source Cu:Kα, 40 kV, 20 mA, divergence slit 1 / 2 deg, scattering slit 1 / 2 deg, receiving slit 0.15 mm, scan speed 4,000° / min, 2θ = 2,000 to 80,000°), and the crystallite diameter was calculated using the following formula (Scherrer's formula) to evaluate whether or not a complex was formed. L=Kλ / (βcosθ) L: crystallite diameter, K: coefficient 0.9, β: half-width, λ: 1.54056 Å, θ: diffraction angle (2) TG-DTA measurement (exothermic peak) Heating speed: 5℃ / min, Measurement range: 25℃~600℃
[0044] The method for forming the above-mentioned complex is not particularly limited, but when preparing the oral composition, it is preferable to adopt, for example, a process of blending component (A) and component (C) and then blending component (B), or a process of blending component (B) and component (C) and then blending component (A). Note that if component (A) and component (B) are blended simultaneously, calcium fluoride may be partially produced, which may result in a lower efficiency of complex formation.
[0045] The oral composition described above contains components (A), (B), (C), and (D), and therefore has excellent biofilm removal effects, and while it contains component (D), it has a reduced acidity and a good flavor. [Example]
[0046] The present invention will be described in detail below with reference to examples, but the present invention is not limited to the following description. In the following examples, the unit of content "%" indicates "% by mass" unless otherwise specified.
[0047] <Raw materials used> [Component (A)] Sodium fluoride: manufactured by Stella Chemifa Co., Ltd. Also referred to as "NaF" hereinafter.
[0048] [(B) Component] Calcium glycerophosphate: manufactured by Iwaki Pharmaceutical Co., Ltd. Hereinafter also referred to as "calcium glycerophosphate." Calcium lactate hydrate: trade name "Calcium lactate" manufactured by Taihei Chemical Industry Co., Ltd. Also referred to as "Ca lactate" hereinafter. Calcium gluconate: manufactured by Fuso Chemical Co., Ltd. Hereinafter also referred to as "Calcium gluconate." Calcium pantothenate: BASF. Hereinafter referred to as "Ca pantothenate."
[0049] [(C) component] Tetrapotassium pyrophosphate: manufactured by Taihei Chemical Industry Co., Ltd. Also referred to as "K pyrophosphate" hereinafter. Sodium pyrophosphate: Taihei Chemical Industry Co., Ltd., product name "Sodium pyrophosphate (anhydrous)". Hereinafter, also referred to as "Na pyrophosphate". Sodium tripolyphosphate: manufactured by Taihei Chemical Industry Co., Ltd. Hereinafter also referred to as "sodium tripolyphosphate."
[0050] [(D) component] Malic acid: manufactured by Fuso Chemical Co., Ltd. Citric acid: manufactured by Fuso Chemical Co., Ltd. Phytic acid: 50% by mass aqueous solution manufactured by Fuso Chemical Co., Ltd. Disodium edetate: manufactured by Junsei Chemical Co., Ltd. Hereinafter also referred to as "Na edetate." Tartaric acid: manufactured by Fuso Chemical Co., Ltd. Succinic acid: manufactured by Fuso Chemical Co., Ltd. Fumaric acid: manufactured by Fuso Chemical Co., Ltd.
[0051] [(E) component] Coconut oil fatty acid amidopropyl betaine: Product name "TEGO BETAIN CK OK MB" manufactured by Evonik Japan Co., Ltd. Also referred to as "amidopropyl betaine" hereinafter. Sodium lauryl sulfate: BASF, product name "Texapon OC-P". Also referred to as "sodium lauryl sulfate" below. Also referred to as "sodium lauryl sulfate" below. Sodium N-lauroyl sarcosinate: manufactured by Nikko Chemicals Co., Ltd., product name "NIKKOL Sarcosinate LN." Hereinafter, also referred to as "Na lauroyl sarcosinate." Sodium N-lauroylmethyl taurate: NIKKOL LMT-P, manufactured by Nikko Chemicals Co., Ltd. (hereinafter also referred to as "Na lauroylmethyl taurate").
[0052] [Fragrance] Fragrance composition A as described in Table 5 below. [water] Purified water. [Common component (arbitrary component)] Silica anhydride (abrasive silica) 10%, sorbitol solution (70% concentration, thickener) 40%, propylene glycol (thickener) 3%, xanthan gum (binder) 0.5%, and sodium saccharin (sweetener) 0.2%. Total 53.7%.
[0053] <Examples 1 to 28 and Comparative Examples 1 to 4> Oral compositions (toothpastes) having the compositions shown in Tables 1 to 4 were prepared by conventional methods. The components were mixed in the following order to prepare a preliminary mixture: an aqueous solution of component (C), an aqueous solution of component (B), and an aqueous solution of component (A). The amount of water was the amount necessary to achieve the composition shown in the table. Phase A was prepared by adding and dissolving water-soluble components (component D, liquid sorbitol, and sodium saccharin) in this preliminary mixture. Phase B was prepared by dissolving and dispersing xanthan gum in propylene glycol at room temperature. Phase B was then added and mixed with phase A while stirring to prepare phase C. Component E, flavoring, and silicic anhydride were added to phase C, and the mixture was mixed at room temperature using a 1.5 L kneader (manufactured by Ishiyama Kosakusho Co., Ltd.). The mixture was then degassed at a reduced pressure of 4 kPa to obtain 1.0 kg of toothpaste. In each toothpaste, it was confirmed by the above-mentioned method that fluoride ions, calcium ions, and phosphorus ions formed a complex. A blank space in the table indicates that the component is not blended. The "balance" of purified water indicates the amount that makes the total amount of the oral composition 100%. The resulting oral compositions (toothpastes) were evaluated as follows, and the results are shown in the table.
[0054] <Evaluation method> [Biofilm (BF) removal effect] (1) Method for preparing model biofilms Hydroxyapatite (HA) plates (Asahi Optical Co., Ltd.) measuring 7 mm in diameter and 3.5 mm in thickness were treated with 0.45 μm filtered unstimulated human saliva for 4 hours and used as supports for model biofilm preparation. Basal medium mucin broth (BMM, composition described below) was used as the culture medium. The bacterial strains used to prepare the model biofilms were Actinomyces viscosus ATCC 43146, Veillonella parvula ATCC 17745, Fusobacterium nucleatum ATCC 10953, Streptococcus oralis ATCC 10557, and Streptococcus mutans ATCC 25175, all purchased from the American Type Culture Collection. These five strains were each cultured in a rotating disk reactor (culture tank) containing 3,000 mL of BMM at 1 × 10 7 The bacteria were inoculated at a concentration of cfu / mL (cfu: colony forming units) and cultured with saliva-treated HA carriers at 37°C under anaerobic conditions (5 vol% carbon dioxide, 95 vol% nitrogen) for 24 hours. After that, BMM medium was continuously supplied at a replacement rate of 5 vol% / hour under the same conditions, and the culture was continued for 10 days, forming a model biofilm of a mixture of five bacterial species on the surface of the HA plate. The BMM used was prepared by mixing the following components (expressed as mass per liter), measuring up the mixture to a total volume of 1 L, and autoclaving at 121° C. for 20 minutes. Proteose peptone (Becton and Dickinson): 4g / L Tryptone (Becton and Dickinson): 2g / L Yeast extract (Becton and Dickinson): 2g / L Mucin (Sigma): 5g / L Hemin (Sigma): 2.5 mg / L Vitamin K (Wako Pure Chemical Industries, Ltd.): 0.5 mg / L KCl (manufactured by Wako Pure Chemical Industries): 1g / L Cysteine (Wako Pure Chemical Industries, Ltd.): 0.2 g / L Distilled water: Remaining
[0055] (2) Evaluation method for model biofilm removal effect The model biofilms formed in (1) above were transferred to a 24-well multi-plate (Sumitomo Bakelite Co., Ltd.), and 2 mL of the test composition was added and allowed to soak for 3 minutes. The test compositions were prepared by diluting each dentifrice composition three-fold with saliva collected from healthy volunteers, and then centrifuging the resulting supernatant (10,000 rpm, 10 minutes). The samples were then washed six times with 1 mL of phosphate buffer (PBS, Wako Pure Chemical Industries, Ltd.) and dispersed by ultrasonic treatment (200 μA, 10 seconds) in a test tube (13 mm diameter × 100 mm) containing 2 mL of the same phosphate buffer to obtain a test solution. The turbidity (OD) of the test solution at a wavelength of 550 nm was measured to determine the amount of remaining biofilm. The removal rate relative to the control was calculated using the following formula, and the oral biofilm removal effect was evaluated based on this removal rate and the following criteria. Phosphate buffer was used as the control. Biofilm removal rate (%) = (turbidity of control - turbidity of test solution) / turbidity of control × 100 [Criteria for assessing biofilm removal effectiveness] ◎: Biofilm removal rate is over 90%. ○: Biofilm removal rate is 80% or more but less than 90%. △: Biofilm removal rate is 70% or more but less than 80%. ×: Biofilm removal rate is less than 70%.
[0056] [Flavor (lack of sourness)] The evaluation was carried out by a sensory test conducted by 10 expert panelists. 1 g of each dentifrice composition was squeezed out of the tube containing the dentifrice composition and placed on a toothbrush (Lion Corporation, Clinica Toothbrush 4-row head, medium size), and brushed for 3 minutes. The sourness felt during use was judged according to the following rating scale. The average of the scores of the 10 panelists was calculated, and the flavor (absence of sourness) was evaluated according to the following rating scale. (Grading criteria) 4 points: No sourness. 3 points: Slightly sour. 2 points: Sour taste. 1 point: Strongly sour taste. (Evaluation criteria) ◎: Average score of 3.5 points or more. ○: Average score is 3.0 or more but less than 3.5 points. ×: Average score less than 3.0 points.
[0057] [Table 1]
[0058] [Table 2]
[0059] [Table 3]
[0060] [Table 4]
[0061] As shown by the above results, the oral compositions of Examples 1 to 28 had excellent biofilm removing effects. In addition, despite containing component (D), the sourness was sufficiently reduced and the flavor was excellent. On the other hand, Comparative Example 1, which did not contain the component (C), Comparative Example 2, which did not contain the component (B), and Comparative Example 3, which did not contain the component (A), showed insufficient reduction in sourness. Comparative Example 4, which did not contain component (D), had an inferior biofilm removal effect.
[0062] <Prescription example> All of the following formulation examples were excellent in biofilm removal effect and flavor (absence of sourness). <Prescription Example 1: Toothpaste> Sodium fluoride 0.32% Calcium glycerophosphate 0.2% Tetrapotassium pyrophosphate 0.1% Citric acid 0.5% Silica anhydride 10% Sorbitol solution (70%) 40% Propylene glycol 3% Xanthan gum 0.5% Sodium polyacrylate 0.5% Coconut oil fatty acid amidopropyl betaine 0.5% Sodium saccharin 0.2% Fragrance composition A 1% Purified water remainder
[0063] <Prescription Example 2: Toothpaste> Sodium fluoride 0.32% Calcium glycerophosphate 0.2% Tetrapotassium pyrophosphate 0.1% Malic acid 0.5% Silica anhydride 10% Sorbitol solution (70%) 40% Propylene glycol 3% Xanthan gum 0.5% Sodium polyacrylate 0.5% Coconut oil fatty acid amidopropyl betaine 0.5% Sodium saccharin 0.2% Fragrance composition A 1% Purified water remainder
[0064] <Formulation Example 3: Toothpaste> Sodium fluoride 0.32% Calcium glycerophosphate 0.2% Tetrapotassium pyrophosphate 0.1% Phytic acid 0.5% Silica anhydride 10% Sorbitol solution (70%) 40% Propylene glycol 3% Xanthan gum 0.5% Sodium polyacrylate 0.5% Coconut oil fatty acid amidopropyl betaine 0.5% Sodium saccharin 0.2% Fragrance composition A 1% Purified water remainder
[0065] <Formulation Example 4: Toothpaste> Sodium fluoride 0.32% Calcium glycerophosphate 0.2% Tetrapotassium pyrophosphate 0.1% Disodium edetate 0.5% Silica anhydride 10% Sorbitol solution (70%) 40% Propylene glycol 3% Xanthan gum 0.5% Sodium polyacrylate 0.5% Coconut oil fatty acid amidopropyl betaine 0.5% Sodium saccharin 0.2% Fragrance composition A 1% Purified water remainder
[0066] <Formulation Example 5: Liquid toothpaste> Sodium fluoride 0.32% Calcium glycerophosphate 0.2% Tetrapotassium pyrophosphate 0.1% Malic acid 0.5% Glycerin 7.5% Propylene glycol 3% Sorbitol solution (70%) 5% Coconut oil fatty acid amidopropyl betaine 0.3% Fragrance composition A 0.2% Purified water remainder
[0067] <Prescription Example 6: Mouthwash> Sodium fluoride 0.1% Calcium glycerophosphate 0.5% Tetrapotassium pyrophosphate 0.1% Malic acid 0.5% Glycerin 3% Propylene glycol 2% Sorbitol solution (70%) 3% Fragrance composition A 0.2% Purified water remainder
[0068] Furthermore, toothpastes, liquid toothpastes, and mouthwashes were prepared with the same compositions as those in the above prescription examples 1 to 6, except that flavor compositions B to P shown in Tables 5 and 6 below were used instead of flavor composition A. All of these had good biofilm removal effects and a good flavor. The compositions of flavors 1 to 7 and solvents described in Tables 5 and 6 are shown in Tables 7 to 14. In the table, "cut a% of the front end" means that the first a% is removed when the essential oil is distilled, and "cut b% of the front and back ends" means that the first b% and the last b% are removed when the essential oil is distilled.
[0069] [Table 5]
[0070] [Table 6]
[0071] [Table 7]
[0072] [Table 8]
[0073] Table 9
[0074] Table 10
[0075] Table 11
[0076] Table 12
[0077] Table 13
[0078] Table 14
Claims
1. (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 members 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 component (B)); An oral composition comprising:
2. 2. The oral composition according to claim 1, wherein the component (C) comprises at least one member selected from the group consisting of pyrophosphoric acid and alkali metal pyrophosphates.
3. The molar amount (unit: mmol / g) of the component (B) per 1 g of the oral composition is expressed as B mmol The mass ratio (unit: mass%) of the component (D) to the total mass of the oral composition is D wt% When this is done, B mmol / D wt% The oral composition according to claim 1, wherein the ratio represented by the formula (I) is 0.001 to 5.
0.
4. The oral composition according to claim 1, wherein the component (D) 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.
5. The oral composition according to claim 1, further comprising (E) one or more surfactants selected from the group consisting of amphoteric surfactants and anionic surfactants.
6. The oral composition according to any one of claims 1 to 5, which is a dentifrice.
Citation Information
Patent Citations
Toothpaste composition
JP2020033291A