Oral composition

The oral composition with sodium fluoride, calcium salts, and enzymes addresses enzyme stability and taste issues in dentifrice, providing stable and pleasant plaque removal.

JP2026001570APending Publication Date: 2026-01-07LION CORP
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Patent Information

Application Number
JP2024099017
Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
Filing Date
2024-06-19
Publication Date
2026-01-07

AI Technical Summary

Technical Problem

Existing dentifrice compositions containing enzymes for plaque decomposition suffer from insufficient enzyme stability during storage and harsh taste issues.

Method used

An oral composition comprising sodium fluoride, calcium salts, condensed phosphoric acid or its alkali metal salts, and specific enzymes, formulated to maintain enzyme stability and reduce harshness.

Benefits of technology

The composition achieves excellent enzyme stability and reduces the harsh taste of enzymes during storage and use, ensuring effective plaque decomposition.

✦ Generated by Eureka AI based on patent content.

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Abstract

To provide a composition for oral cavity containing an enzyme, excellent in stability of the enzyme, and capable of improving harsh taste.SOLUTION: The composition for the oral cavity comprises (A) sodium fluoride, (B) one or more kinds selected from the group consisting of calcium chloride, calcium gluconate, calcium lactate and calcium pantothenate, (C) one or more kinds selected from the group consisting of condensed phosphoric acids and their alkali metal salts and (D) an enzyme.SELECTED DRAWING: None
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Description

[Technical Field]

[0001] The present invention relates to an oral composition. [Background technology]

[0002] Removal of dental plaque is effective in preventing dental caries, and dentifrice compositions containing enzymes that contribute to the decomposition of dental plaque are known. For example, Patent Document 1 proposes a dentifrice composition containing a specific synthetic amorphous aluminum having abrasive properties and glucanase. [Prior art documents] [Patent documents]

[0003] [Patent Document 1] Japanese Patent Application Laid-Open No. 2010-275272 Summary of the Invention [Problem to be solved by the invention]

[0004] According to the findings of the present inventors, the dentifrice composition described in Patent Document 1 does not necessarily have sufficient enzyme stability (resistance to inactivation during storage). Furthermore, when used after storage, the dentifrice composition may have a harsh taste characteristic of enzymes. An object of the present invention is to provide an oral composition that contains an enzyme, has excellent enzyme stability, and can reduce harshness. [Means for solving the problem]

[0005] The present invention has the following aspects. [1] An oral composition comprising: (A) sodium fluoride; (B) one or more members selected from the group consisting of calcium chloride, 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) an enzyme. [2] The oral composition according to [1], wherein the component (C) comprises one or more selected from the group consisting of pyrophosphate, tripolyphosphate, alkali metal pyrophosphate, and alkali metal tripolyphosphate. [3] The oral composition according to [2], wherein the component (C) comprises one or more selected from the group consisting of potassium pyrophosphate, sodium pyrophosphate, potassium tripolyphosphate, and sodium tripolyphosphate. [4] The oral composition according to any one of [1] to [3], wherein the enzyme activity of the component (D) per 1 g of the oral composition is 2 to 200 units / g. [5] The oral composition according to any one of [1] to [4], wherein the enzyme activity per 1 g of the component (D) is 4,000 to 2,500,000 units / g. [6] The content (unit: mass%) of the component (B) relative to the total mass of the oral composition is B wt% The enzyme activity (unit: unit / g) of the component (D) per 1 g of the oral composition is expressed as D unit When B wt% / D unit The oral composition according to any one of [1] to [5], wherein the ratio represented by the formula (I) is 0.0005 to 0.3. [7] The oral composition according to any one of [1] to [6], wherein the component (D) comprises one or more selected from the group consisting of dextranase, mutanase, actinidin, papain, and bromelain. [8] The oral composition according to any one of [1] to [7], wherein the component (D) contains dextranase. [9] The oral composition according to any one of [1] to [8], which is a dentifrice. [Effects of the Invention]

[0006] According to the present invention, an oral composition containing an enzyme, which has excellent enzyme stability and can improve a harsh taste, 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, 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 this embodiment contains component (A), component (B), component (C), and component (D).

[0009] <Component (A)> Component (A) is sodium fluoride (NaF). Component (A) contributes to improving the stability of the enzyme and reducing the harsh taste. 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 chloride, calcium gluconate, calcium lactate, and calcium pantothenate. Component (B) may be a combination of two or more types. In this specification, "water-soluble" means that the solubility in water at 20°C is 1 g / 100 g or more. Component (B) contributes to improving the stability of the enzyme and reducing the harsh taste. As component (B), calcium chloride, calcium gluconate, and calcium lactate are preferred, with calcium chloride and calcium lactate being more preferred. 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) contributes to improving the stability of the enzyme and reducing the harsh taste.

[0012] 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 and tetrametaphosphoric acid. The degree of polymerization of the condensed phosphoric acid is, for example, 2 to 6. Examples of the alkali metal salt of condensed phosphoric acid include sodium salt and potassium salt. 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, tripolyphosphoric acid, alkali metal pyrophosphates, and alkali metal tripolyphosphates. 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] The component (C) preferably includes a component (C2) which is one or more selected from the group consisting of potassium pyrophosphate, sodium pyrophosphate, potassium tripolyphosphate, and sodium tripolyphosphate. The proportion of the (C2) 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%.

[0015] <(D) component> Component (D) is an enzyme. Any enzyme known in oral compositions can be used. Component (D) may be a combination of two or more enzymes. The component (D) preferably includes a component (D1) which is one or more selected from the group consisting of dextranase, mutanase, actinidin, papain, and bromelain. Dextranase, mutanase, actinidin, papain and bromelain each contribute to the decomposition of dental plaque. 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] The enzyme activity per 1 g of component (D) (unit: unit / g) is preferably 4,000 to 2,500,000 units / g. The enzyme activity per 1 g of dextranase is preferably 10,000 to 14,000 units / g, more preferably 13,000±1,000 units / g. The enzyme activity of mutanase is preferably 4,000 to 70,000 units / g, more preferably 6,000±2,000 units / g. The enzymatic activity of actinidin is preferably 9,000 to 210,000 units / g, more preferably 180,000±30,000 units / g. The enzymatic activity of papain is preferably 200,000 to 2,500,000 units / g, and more preferably 800,000±100,000 units / g. The enzyme activity of bromelain is preferably 300,000 to 500,000 units / g, more preferably 400,000±50,000 units / g.

[0017] As component (D), dextranase is preferred, particularly in terms of enzyme stability. The proportion of the dextranase component (D2) relative to the total mass of the component (D) may 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, or may be 100% by mass.

[0018] <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 cavity composition. When the content of component (A) is equal to or greater than the above-mentioned lower limit, the effect of improving enzyme stability is more excellent. When the content of component (A) is equal to or less than the above-mentioned upper limit, the effect of improving enzyme stability and the effect of reducing harshness are more excellent.

[0019] 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 improving enzyme stability and the effect of reducing harshness are more excellent. When the content of component (B) is equal to or less than the upper limit, the effect of improving enzyme stability is more excellent.

[0020] 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 cavity composition. When the content of component (C) is equal to or greater than the above-mentioned lower limit, the enzyme stabilization effect is more excellent. When the content of component (C) is equal to or less than the above-mentioned upper limit, the harshness-reducing effect is more excellent.

[0021] The content of component (D) is preferably an amount that results in an enzyme activity of component (D) of 2 to 200 units / g, more preferably 10 to 50 units / g, per 1 g of the oral composition. When two or more enzymes are contained as component (D), it is preferable that the enzymatic activity of each enzyme per gram of the oral composition is within the above range. Here, one unit of dextranase is the amount of dextranase that produces free reducing sugars equivalent to 1 μmol of glucose within one minute at 40° C. and pH 5 using dextran as a substrate during the initial reaction. One unit of mutanase is the amount of mutanase that produces free reducing sugars equivalent to 1 μmol of glucose within one minute of the initial reaction at 40°C and pH 5 using mutan as a substrate. One unit of actinidin, papain, or bromelain can be measured according to the Japanese Food Additives Standards. Specifically, it is the amount of each enzyme that produces an amino acid equivalent to 1 μg of tyrosine per minute using casein as a substrate.

[0022] <Ratio> The content of component (B) relative to the total mass of the oral composition (unit: mass%) is represented by B wt% The enzyme activity (unit: unit / g) per 1 g of the oral composition of component (D) is unit When B wt% / D unitThe ratio represented by the formula (1) is preferably 0.0005 to 0.3, and more preferably 0.001 to 0.25. B wt% / D unit When B is equal to or greater than the lower limit, the effect of improving the stability of the enzyme and the effect of reducing harshness are more excellent. wt% / D unit When the content is equal to or less than the upper limit, the effect of improving the stability of the enzyme is more excellent.

[0023] The content of component (A) relative to the total mass of the oral composition (unit: mass%) is represented by A wt% The enzyme activity (unit: unit / g) per 1 g of the oral composition of component (D) is unit When A wt% / D unit The ratio represented by the formula (1) is preferably 0.001 to 0.3, and more preferably 0.002 to 0.16. A wt% / D unit When the value is equal to or greater than the lower limit, the effect of improving the stability of the enzyme and the effect of reducing the harshness are more excellent. wt% / D unit When the content is equal to or less than the upper limit, the effect of improving the stability of the enzyme is more excellent.

[0024] The content of component (C) (unit: mass%) relative to the total mass of the oral composition is represented by C wt% The enzyme activity (unit: unit / g) per 1 g of the oral composition of component (D) is unit When C wt% / D unit The ratio represented by the formula (1) is preferably 0.0001 to 0.1, and more preferably 0.0005 to 0.065. C wt% / D unit When the value is equal to or greater than the lower limit, the effect of improving the harshness is more excellent. wt% / D unit When the content is equal to or less than the upper limit, the effect of improving the stability of the enzyme is more excellent.

[0025] <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 water content relative to the total mass of the oral composition is preferably 10 to 55% by mass, more preferably 15 to 50% by mass, and even more preferably 20 to 45% by mass. When the water content is equal to or greater than the lower limit, the effect of reducing harshness is more excellent. When the water content is equal to or less than the upper limit, the effect of improving enzyme stability is more excellent.

[0026] <Other ingredients> The oral composition may further contain other components in addition to the components (A), (B), (C), (D) 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 the other components include abrasives, binders, thickeners, surfactants, colorants, sweeteners, preservatives, flavorings, active ingredients, and pH adjusters.

[0027] 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.

[0028] 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.

[0029] 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.

[0030] As the surfactant, any surfactant known in oral compositions can be used, including, for example, a nonionic surfactant, an anionic surfactant, an amphoteric surfactant, etc. Examples of amphoteric surfactants include coconut oil fatty acid amidopropyl betaine, lauryl dimethylaminoacetic acid betaine, and N-coconut oil fatty acid acyl-N-carboxymethyl-N-hydroxyethylethylenediamine. Examples of anionic surfactants include alkyl sulfates, N-acyltaurates, N-acylamino acid salts, α-olefin sulfonates, sodium dodecylbenzenesulfonate, and sodium lauryl sulfoacetate. Preferred alkyl sulfates are sodium lauryl sulfate and sodium myristyl sulfate. The content of the surfactant is, for example, preferably 0 to 8.0% by mass, more preferably 0 to 5.0% by mass, relative to the total mass of the oral cavity composition.

[0031] 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.

[0032] 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.

[0033] 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)), 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, 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 blended in effective amounts within a range that does not interfere with the effects of the present invention.

[0034] Examples of pH adjusters include citric acid, tartaric acid, malic acid, and salts thereof such as potassium salts and sodium salts, and sodium hydroxide.

[0035] <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.

[0036] 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.

[0037] The oral composition described above contains the enzyme (D) as well as components (A), (B), and (C), and therefore has excellent enzyme stability and is less likely to be inactivated during storage of the oral composition. In addition, the harsh taste characteristic of enzymes is improved when the oral composition is used after storage. [Example]

[0038] 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 "%" refers to "% by mass" unless otherwise specified.

[0039] <Raw materials used> [Component (A)] Sodium fluoride: manufactured by Stella Chemifa Co., Ltd. Also referred to as "NaF" hereinafter.

[0040] [(B) Component] Calcium chloride: manufactured by Tomita Pharmaceutical Co., Ltd. Hereinafter also referred to as "Ca chloride." 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: manufactured by BASF. Hereinafter also referred to as "Ca pantothenate." [(B') component] Calcium glycerophosphate: manufactured by Iwaki Pharmaceutical Co., Ltd. Hereinafter also referred to as "calcium glycerophosphate."

[0041] [(C) component] Tetrapotassium pyrophosphate: manufactured by Taihei Chemical Industry Co., Ltd. Hereinafter also referred to as "K pyrophosphate." Sodium pyrophosphate: Taihei Chemical Industry Co., Ltd., product name "Sodium pyrophosphate (anhydrous)". Hereinafter, also referred to as "Na pyrophosphate". Potassium tripolyphosphate: manufactured by Taihei Chemical Industry Co., Ltd. Hereinafter also referred to as "potassium tripolyphosphate." Sodium tripolyphosphate: manufactured by Taihei Chemical Industry Co., Ltd. Hereinafter also referred to as "sodium tripolyphosphate."

[0042] [(D) component] Dextranase: Daiichi Sankyo Propharma Co., Ltd., enzyme activity 13,000 units / g. Mutanase: Manufactured by Amano Enzyme Co., Ltd., product name "Mutanase", enzyme activity 6,000 units / g. Actinidin: manufactured by BHN Corporation, product name "Zactinase (registered trademark)", enzyme activity 180,000 units / g. Papain: Manufactured by Mitsubishi Chemical Foods Corporation, product name "Purified Papain", enzyme activity 800,000 units / g. Bromelain: Manufactured by Godo Shusei Co., Ltd., product name "Bromelain", enzyme activity 400,000 units / g.

[0043] [Abrasive] Silica anhydrous (abrasive silica). [Fragrance] Fragrance composition A as described in Table 7 below. [water] Purified water. [Common component (arbitrary component)] Liquid sorbitol (70% concentration, thickener) 40%, propylene glycol (thickener) 3%, coconut oil fatty acid amidopropyl betaine (amphoteric surfactant) 0.5%, sodium lauryl sulfate (anionic surfactant) 1%, sodium polyacrylate (binder) 0.5%, and xanthan gum (binder) 0.5%. Total 45.7%.

[0044] <Examples 1 to 44, Comparative Examples 1 to 4> Oral compositions having the compositions shown in Tables 1 to 6 were prepared by a conventional method. Examples 1 to 37 and Comparative Examples 1 to 4 are examples of toothpastes, and Examples 38 to 44 are examples of gel toothpastes. 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 obtained oral compositions were evaluated as follows, and the results are shown in the table.

[0045] <Evaluation method> [Enzyme residual rate (enzyme stability)] 50 g of each oral composition (toothpaste) was filled into a tube (laminated tube with a diameter of 26 mm (manufactured by Dai Nippon Printing Co., Ltd.)) and stored at 45° C. for 3 weeks. The layer structure of the laminated tube used was, from the outermost layer, LDPE55 / PET12 / LDPE20 / white LDPE60 / EMAA20 / AL10 / EMAA30 / LDPE20 / LLDPE30. The abbreviations and names for the layer structure are: LDPE: low-density polyethylene, white LDPE: white low-density polyethylene, LLDPE: linear low-density polyethylene, AL: aluminum, EAA: ethylene-acrylic acid copolymer resin, PET: polyethylene terephthalate, EMAA: ethylene-methacrylic acid copolymer resin, and the numbers following the abbreviations indicate the thickness (μm) of each layer. After storage at 45°C, the oral compositions were returned to room temperature and subjected to the following tests. 0.6 g of the oral composition was suspended in 15 mL of 0.1 M phosphate buffer, and the centrifuged supernatant was used as the test solution. 1 mL of this test solution was added to 2 mL of 1% substrate solution, and the mixture was incubated in a 35°C incubator for exactly 10 minutes. The amount of reducing sugars produced was measured by the Somogyi-Nelson method. One unit of dextranase enzyme activity was defined as the amount of dextranase that produced free reducing sugars equivalent to 1 μmol of glucose per minute. One unit of mutanase enzyme activity was defined as the amount of mutanase that produced free reducing sugars equivalent to 1 μmol of glucose per minute. One unit of actinidin, papain, and bromelain enzyme activity was defined as the amount of each enzyme that produced the amino acid equivalent to 1 μg of tyrosine per minute. The enzyme activity of the initial product before storage and the enzyme activity of the preserved product after storage were measured, and the residual rate (unit: %) was calculated using the following formula. The residual rate measurement was repeated three times, and the enzyme stability was evaluated based on the average value using the following evaluation criteria. Enzyme residual rate (%) = (enzyme activity of stored product) / (enzyme activity of initial product) x 100 (Evaluation criteria) ◎: Enzyme residual rate of 95% or more. 〇: Enzyme remaining rate is 85% or more but less than 95%. △: Enzyme remaining rate is 80% or more but less than 85%. ×: Enzyme remaining rate less than 80%.

[0046] [No bitter taste when used in long-term storage (bitter taste improvement)] 50 g of each oral composition (toothpaste) was filled into the tube (a laminated tube with a diameter of 26 mm, manufactured by Dai Nippon Printing Co., Ltd.) and stored at 40° C. for one month. The oral compositions were then returned to room temperature and subjected to the following tests. Four expert flavor evaluation panelists evaluated the usability of the oral compositions using the following method. 1 g of the oral composition was placed on a toothbrush (Clinica Advantage Toothbrush, 4-row compact regular type, manufactured by Lion Corporation) and brushed teeth for 3 minutes. The absence of a harsh taste during use was judged according to the rating scale shown below and evaluated according to the following evaluation criteria. Those rated as ◯ or better were judged to be oral compositions with a reduced harsh taste, a good taste, and a refreshing, non-irritating feel when used. (Grading criteria) 4 points: No bitter taste. 3 points: Almost no bitter taste was detected. 2 points: It tasted bitter. 1 point: I felt a strong bitter taste. (Evaluation criteria) ◎: Out of 4 people, 0 people scored 2 points or less, and 3 to 4 people scored 4 points. ○: Out of 4 people, 0 people scored 2 points or less, and 0 to 2 people scored 4 points. △: 1 to 3 out of 4 people scored 2 points or less. ×: 4 out of 4 people scored 2 points or less.

[0047] [Table 1]

[0048] [Table 2]

[0049] [Table 3]

[0050] [Table 4]

[0051] [Table 5]

[0052] [Table 6]

[0053] As shown by the above results, the oral compositions of Examples 1 to 44 were excellent in enzyme stability and harshness-reducing effect. On the other hand, Comparative Example 1, which did not contain component (A), Comparative Example 2, which did not contain component (B), and Comparative Example 3, which did not contain component (C), were inferior in enzyme stability and harshness-improving effect. Comparative Example 4, in which calcium glycerophosphate (B') was used instead of component (B), was inferior in the effect of improving the harsh taste.

[0054] Next, a prescription example is shown. Oral compositions having the following compositions were prepared by conventional methods and evaluated in the same manner as above. All formulations were found to be excellent in enzyme stability and bitterness-improving effect.

[0055] <Prescription Example 1: Toothpaste> Sodium fluoride 0.32% Calcium lactate hydrate 0.5% Potassium pyrophosphate 0.1% Dextranase 20 units Silica anhydride 10% Sorbitol solution (70%) 40% Propylene glycol 3% Coconut oil amidopropyl betaine 1.0% Sodium lauryl sulfate 1.0% Xanthan gum 0.5% Sodium polyacrylate 0.5% Sodium tetradecene sulfonate 0.3% Sodium saccharin 0.2% Fragrance composition A 1% Purified water remainder

[0056] <Prescription Example 2: Toothpaste> Sodium fluoride 0.32% Calcium lactate hydrate 0.5% Sodium pyrophosphate 0.1% Dextranase 20 units Silica anhydride 10% Sorbitol solution (70%) 40% Propylene glycol 3% Coconut oil amidopropyl betaine 1.0% Sodium lauryl sulfate 1.0% Xanthan gum 0.5% Sodium polyacrylate 0.5% Sodium tetradecene sulfonate 0.3% Sodium saccharin 0.2% Fragrance composition A 1% Purified water remainder

[0057] <Formulation Example 3: Toothpaste> Sodium fluoride 0.32% Calcium lactate hydrate 0.5% Sodium tripolyphosphate 0.1% Dextranase 20 units Silica anhydride 10% Sorbitol solution (70%) 40% Propylene glycol 3% Coconut oil amidopropyl betaine 1.0% Sodium lauryl sulfate 1.0% Xanthan gum 0.5% Sodium polyacrylate 0.5% Sodium tetradecene sulfonate 0.3% Sodium saccharin 0.2% Fragrance composition A 1% Purified water remainder

[0058] <Formulation Example 4: Toothpaste> Sodium fluoride 0.32% Calcium chloride 0.5% Sodium pyrophosphate 0.1% Dextranase 20 units Silica anhydride 10% Sorbitol solution (70%) 40% Propylene glycol 3% Coconut oil amidopropyl betaine 1.0% Sodium lauryl sulfate 1.0% Xanthan gum 0.5% Sodium polyacrylate 0.5% Sodium saccharin 0.2% Fragrance composition A 1% Purified water remainder

[0059] <Formulation Example 5: Toothpaste> Sodium fluoride 0.32% Calcium gluconate 0.5% Sodium pyrophosphate 0.1% Dextranase 20 units Silica anhydride 10% Sorbitol solution (70%) 40% Propylene glycol 3% Coconut oil amidopropyl betaine 1.0% Sodium lauryl sulfate 1.0% Xanthan gum 0.5% Sodium polyacrylate 0.5% Sodium saccharin 0.2% Fragrance composition A 1% Purified water remainder

[0060] <Formulation Example 6: Toothpaste> Sodium fluoride 0.32% Calcium pantothenate 0.5% Sodium pyrophosphate 0.1% Dextranase 20 units Silica anhydride 10% Sorbitol solution (70%) 40% Propylene glycol 3% Coconut oil amidopropyl betaine 1.0% Sodium lauryl sulfate 1.0% Xanthan gum 0.5% Sodium polyacrylate 0.5% Sodium saccharin 0.2% Fragrance composition A 1% Purified water remainder

[0061] <Formulation Example 7 Toothpaste> Sodium fluoride 0.32% Calcium chloride 0.5% Sodium tripolyphosphate 0.1% Dextranase 20 units Silica anhydride 10% Sorbitol solution (70%) 40% Propylene glycol 3% Coconut oil amidopropyl betaine 1.0% Sodium lauryl sulfate 1.0% Xanthan gum 0.5% Sodium polyacrylate 0.5% Sodium saccharin 0.2% Fragrance composition A 1% Purified water remainder

[0062] <Formulation Example 8 Toothpaste> Sodium fluoride 0.32% Calcium gluconate 0.5% Sodium tripolyphosphate 0.1% Dextranase 20 units Silica anhydride 10% Sorbitol solution (70%) 40% Propylene glycol 3% Coconut oil amidopropyl betaine 1.0% Sodium lauryl sulfate 1.0% Xanthan gum 0.5% Sodium polyacrylate 0.5% Sodium saccharin 0.2% Fragrance composition A 1% Purified water remainder

[0063] <Formulation Example 9: Toothpaste> Sodium fluoride 0.32% Calcium pantothenate 0.5% Sodium tripolyphosphate 0.1% Dextranase 20 units Silica anhydride 10% Sorbitol solution (70%) 40% Propylene glycol 3% Coconut oil amidopropyl betaine 1.0% Sodium lauryl sulfate 1.0% Xanthan gum 0.5% Sodium polyacrylate 0.5% Sodium saccharin 0.2% Fragrance composition A 1% Purified water remainder

[0064] <Formulation example 10: Gel toothpaste> Sodium fluoride 0.32% Calcium chloride 0.2% Potassium pyrophosphate 0.1% Dextranase 20 units Sorbitol solution (70%) 40% Propylene glycol 3% Coconut oil amidopropyl betaine 1.0% Sodium lauryl sulfate 1.0% Xanthan gum 0.5% Sodium polyacrylate 0.5% Sodium saccharin 0.2% Fragrance composition A 1% Purified water remainder

[0065] <Formulation Example 11: Gel toothpaste> Sodium fluoride 0.32% Calcium gluconate 0.2% Potassium pyrophosphate 0.1% Dextranase 20 units Sorbitol solution (70%) 40% Propylene glycol 3% Coconut oil amidopropyl betaine 1.0% Sodium lauryl sulfate 1.0% Xanthan gum 0.5% Sodium polyacrylate 0.5% Sodium saccharin 0.2% Fragrance composition A 1% Purified water remainder

[0066] <Formulation example 12: Gel toothpaste> Sodium fluoride 0.32% Calcium pantothenate 0.2% Potassium pyrophosphate 0.1% Dextranase 20 units Sorbitol solution (70%) 40% Propylene glycol 3% Coconut oil amidopropyl betaine 1.0% Sodium lauryl sulfate 1.0% Xanthan gum 0.5% Sodium polyacrylate 0.5% Sodium saccharin 0.2% Fragrance composition A 1% Purified water remainder

[0067] <Formulation Example 13: Gel toothpaste> Sodium fluoride 0.32% Calcium chloride 0.2% Sodium pyrophosphate 0.1% Dextranase 20 units Sorbitol solution (70%) 40% Propylene glycol 3% Coconut oil amidopropyl betaine 1.0% Sodium lauryl sulfate 1.0% Xanthan gum 0.5% Sodium polyacrylate 0.5% Sodium saccharin 0.2% Fragrance composition A 1% Purified water remainder

[0068] <Formulation example 14: Gel toothpaste> Sodium fluoride 0.32% Calcium gluconate 0.2% Sodium pyrophosphate 0.1% Dextranase 20 units Sorbitol solution (70%) 40% Propylene glycol 3% Coconut oil amidopropyl betaine 1.0% Sodium lauryl sulfate 1.0% Xanthan gum 0.5% Sodium polyacrylate 0.5% Sodium saccharin 0.2% Fragrance composition A 1% Purified water remainder

[0069] <Formulation example 15: Gel toothpaste> Sodium fluoride 0.32% Calcium pantothenate 0.2% Sodium pyrophosphate 0.1% Dextranase 20 units Sorbitol solution (70%) 40% Propylene glycol 3% Coconut oil amidopropyl betaine 1.0% Sodium lauryl sulfate 1.0% Xanthan gum 0.5% Sodium polyacrylate 0.5% Sodium saccharin 0.2% Fragrance composition A 1% Purified water remainder

[0070] <Prescription Example 16: Mouthwash> Sodium fluoride 0.1% Calcium lactate hydrate 0.1% Potassium pyrophosphate 0.1% Dextranase 20 units Glycerin 2% Propylene glycol 3% Sodium lauroyl sarcosinate 0.1% Fragrance composition A 0.3% Purified water remainder

[0071] <Prescription Example 17: Mouthwash> Sodium fluoride 0.1% Calcium chloride 0.1% Potassium pyrophosphate 0.1% Dextranase 20 units Glycerin 2% Propylene glycol 3% Sodium lauroyl sarcosinate 0.1% Fragrance composition A 0.3% Purified water remainder

[0072] Furthermore, toothpastes, gel toothpastes, and mouthwashes were prepared with the same compositions as in Examples 1 to 44 and Formulation Examples 1 to 17 above, except that flavor compositions B to Q shown in Tables 7 and 8 below were used instead of flavor composition A. All of these had good enzyme stability and were also effective in improving astringency. The compositions of flavors 1 to 7 and solvents described in Tables 7 and 8 are shown in Tables 9 to 16. 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.

[0073] [Table 7]

[0074] Table 8

[0075] Table 9

[0076] Table 10

[0077] Table 11

[0078] Table 12

[0079] Table 13

[0080] Table 14

[0081] Table 15

[0082] Table 16

Claims

1. (A) sodium fluoride, (B) one or more selected from the group consisting of calcium chloride, 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) an enzyme; An oral composition comprising:

2. 2. The oral composition according to claim 1, wherein the component (C) comprises at least one selected from the group consisting of pyrophosphate, tripolyphosphate, alkali metal pyrophosphate, and alkali metal tripolyphosphate.

3. The oral composition according to claim 2, wherein the component (C) comprises one or more selected from the group consisting of potassium pyrophosphate, sodium pyrophosphate, potassium tripolyphosphate, and sodium tripolyphosphate.

4. 2. The oral composition according to claim 1, wherein the enzyme activity of component (D) per 1 g of the oral composition is 2 to 200 units / g.

5. 2. The oral composition according to claim 1, wherein the enzyme activity per gram of component (D) is 4,000 to 2,500,000 units / g.

6. The content (unit: mass%) of the component (B) relative to the total mass of the oral composition is represented by B wt% The enzyme activity (unit: unit / g) of the component (D) per 1 g of the oral composition is expressed as D unit When this is done, B wt% / D unit The oral composition according to claim 1, wherein the ratio is 0.0005 to 0.

3.

7. 2. The oral composition according to claim 1, wherein the component (D) comprises at least one selected from the group consisting of dextranase, mutanase, actinidin, papain, and bromelain.

8. The oral composition according to claim 1 , wherein the component (D) comprises dextranase.

9. The oral composition according to any one of claims 1 to 8, which is a dentifrice.

Citation Information

Patent Citations

  • Dentifrice composition

    JP2010275272A