Oral components
Incorporating a water-soluble tin salt into oral compositions with water-soluble condensed phosphoric acid and pyrrolidonecarboxylic acid addresses discoloration issues, ensuring stable storage and pleasant use, while maintaining dental stain removal efficacy.
Patent Information
- Application Number
- JP2021107153
- Authority / Receiving Office
- JP · JP
- Patent Type
- Patents
- Current Assignee / Owner
- Filing Date
- 2021-06-29
- Publication Date
- 2025-12-03
- Estimated Expiration
- 2041-06-29
AI Technical Summary
Existing oral compositions containing water-soluble condensed phosphoric acid or its salts suffer from discoloration over time, which affects their storage stability and user experience.
Incorporating a water-soluble tin salt into an oral composition containing water-soluble condensed phosphoric acid or its salt and pyrrolidonecarboxylic acid or its alkali metal salt significantly suppresses discoloration, maintaining the formulation's appearance and providing a pleasant feel during use.
The combined system effectively prevents discoloration, enhances storage stability, and eliminates metallic taste, while maintaining effective dental stain removal.
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Abstract
Description
[Technical Field]
[0001] The present invention relates to an oral composition containing a water-soluble condensed phosphoric acid or a salt thereof, which is inhibited from discoloring over time and has excellent storage stability. [Background technology]
[0002] Water-soluble condensed phosphoric acid or its salt has the effect of removing stains, which are a type of discoloration on teeth, and is used in oral compositions as a tooth stain removal component. Techniques have also been proposed for improving and applying this stain removal effect (Patent Document 1; Japanese Patent No. 6673348). Oral compositions such as dentifrices containing water-soluble condensed phosphoric acid or its salts have the problem of discoloration of the preparation over time, and for example, in Patent Document 2 (Japanese Patent No. 3862006), discoloration over time is suppressed by combining a water-soluble polyphosphate with zeolite treated under specific conditions. However, depending on the formulation, discoloration of the preparation may not be suppressed, and there is still room for improvement in terms of suppressing discoloration of preparations using water-soluble condensed phosphoric acid or its salts.
[0003] Incidentally, pyrrolidone carboxylic acid or a salt thereof is effective as an ingredient for removing stains such as stains on tooth dentin (Patent Document 3; Japanese Patent No. 6474375), and Patent Document 4 (WO 2018 / 043717) proposes an oral composition that combines pyrrolidone carboxylic acid or an inorganic base salt thereof with water-soluble pyrophosphoric acid or a salt thereof, and has excellent effects in inhibiting staining of the surface and subsurface of tooth dentin; however, no study or mention is made of discoloration caused by the preparation. [Prior art documents] [Patent documents]
[0004] [Patent Document 1] Patent No. 6673348 [Patent Document 2] Patent No. 3862006 [Patent Document 3] Patent No. 6474375 [Patent Document 4] International Publication No. 2018 / 043717 [Patent Document 5] Japanese Patent Application Laid-Open No. 2008-143910 Summary of the Invention [Problem to be solved by the invention]
[0005] The present invention has been made in consideration of the above circumstances, and aims to provide an oral composition containing a water-soluble condensed phosphoric acid or a salt thereof, which has excellent storage stability, suppresses discoloration of the formulation over time, and has a good feel when used. [Means for solving the problem]
[0006]
[0009] As a result of intensive research to achieve the above-mentioned object, the present inventors have found that adding a water-soluble tin salt to an oral composition containing a water-soluble condensed phosphoric acid or its salt and pyrrolidonecarboxylic acid or its alkali metal salt significantly suppresses discoloration of the preparation over time, maintains a stable appearance of the preparation, provides excellent storage stability, suppresses metallic taste, and provides a good feel when used. That is, in the present invention, the inventors have found that by preparing an oral composition containing (A) a water-soluble condensed phosphoric acid or its salt, (B) pyrrolidonecarboxylic acid or its alkali metal salt, and (C) a water-soluble tin salt, the effects of components (A) and (B) on removing dental stains and the like are exerted, and discoloration of the preparation over time is suppressed, providing excellent storage stability and a good feel when used, which has led to the completion of the present invention.
[0007]
[0004] More specifically, when an oral composition containing component (A) is combined with component (B), particularly an alkali metal salt of pyrrolidonecarboxylic acid, to improve its effectiveness in removing dental stains, the formulation discolors significantly over time, more than when component (A) is used alone, resulting in a marked deterioration in the formulation's appearance. However, when component (C) is added, the discoloration of the formulation is significantly suppressed without worsening, as described above, and the formulation's appearance can be maintained stable even after storage. In this case, in a combined system of components (A) and (B), unexpectedly, component (C) acts as a discoloration inhibitor, which eliminates the metallic taste of component (C), ensuring a good feel in use, preventing formulation discoloration, and providing excellent storage stability. Incidentally, Patent Document 5 (JP 2008-143910 A) discloses a topical oral composition containing a tin ion-containing antibacterial agent and a polyphosphate anti-tartar agent, but does not mention discoloration of the formulation. In contrast, the present invention aims to suppress discoloration of the formulation in a combined system of components (A) and (B) by component (C), thereby improving the storage stability (appearance stability) of the oral composition.
[0008] Therefore, the present invention provides the following oral compositions. [1] (A) a water-soluble condensed phosphoric acid or a salt thereof, (B) Pyrrolidonecarboxylic acid or its alkali metal salt and (C) Water-soluble tin salts An oral composition comprising: [2] The oral composition according to [1], wherein (A) the water-soluble condensed phosphoric acid or salt thereof is one or more selected from sodium pyrophosphate, sodium tripolyphosphate, and sodium hexametaphosphate. [3] (B) The oral composition according to [1] or [2], wherein the pyrrolidone carboxylic acid or its alkali metal salt is sodium pyrrolidone carboxylic acid. [4] (C) The oral composition according to any one of [1] to [3], wherein the water-soluble tin salt is at least one selected from tin chloride and tin fluoride. [5] The oral composition according to any one of [1] to [4], wherein (C) / (B), which represents the ratio of the content of the (B) component to the content of the (C) component as tin ions, is 0.01 to 0.6 in mass ratio. [6] The content of component (A) is 0.1 to 5 mass%, and the content of component (B) is 0.5 to 10 mass%, The oral composition according to any one of [1] to [5], wherein the content of component (C) is 0.02 to 1.8% by mass in terms of tin ions. [7] The oral composition according to any one of [1] to [6], which is a dentifrice. [Effects of the Invention]
[0009] According to the present invention, an oral composition containing components (A) and (B) can be provided which exhibits excellent storage stability, suppresses discoloration of the formulation over time, and provides a pleasant feel when used. This oral composition has the effect of removing dental stains, and is therefore effective for cleaning and whitening teeth. DETAILED DESCRIPTION OF THE INVENTION
[0010] The present invention will be described in further detail below. The oral composition of the present invention contains (A) a water-soluble condensed phosphoric acid or a salt thereof, (B) pyrrolidonecarboxylic acid or an alkali metal salt thereof, and (C) a water-soluble tin salt.
[0011] (A) The water-soluble condensed phosphoric acid or its salt has the effect of removing stains from teeth. Examples of water-soluble condensed phosphoric acid or a salt thereof include linear polyphosphoric acid or a salt thereof, such as pyrophosphoric acid, tripolyphosphoric acid, or tetrapolyphosphoric acid, and cyclic polyphosphoric acid or a salt thereof, such as trimetaphosphoric acid, tetrametaphosphoric acid, or hexametaphosphoric acid. Examples of these salts include alkali metal salts, such as sodium salts and potassium salts. Specific examples of water-soluble condensed phosphoric acid or a salt thereof include sodium pyrophosphate, sodium tripolyphosphate, and sodium hexametaphosphate. These may be used alone or in combination of two or more, and commercially available products may be used.
[0012] The amount of (A) water-soluble condensed phosphoric acid or its salt is preferably 0.1 to 5% (mass %, hereinafter the same) of the total composition, more preferably 0.3 to 2%. When the amount is 0.1% or more, the effect of removing dental stains is sufficient, and when it is 5% or less, discoloration is sufficiently suppressed.
[0013] (B) Pyrrolidonecarboxylic acid or an alkali metal salt thereof has an effect of removing stains from teeth, particularly dentin. Examples of pyrrolidone carboxylic acid or an alkali metal salt thereof include pyrrolidone carboxylic acid and alkali metal salts thereof such as sodium salt, potassium salt, etc. Specifically, alkali metal salts of pyrrolidone carboxylic acid such as sodium pyrrolidone carboxylate can be used. Commercially available pyrrolidone carboxylic acid or an alkali metal salt thereof can be used. For example, sodium pyrrolidone carboxylic acid such as AJIDEW (registered trademark) N-50 manufactured by Ajinomoto Healthy Supply Co., Ltd. can be used.
[0014] The amount of (B) pyrrolidonecarboxylic acid or its alkali metal salt is preferably 0.5 to 10%, more preferably 1 to 5%, of the total composition. When the amount is 0.5% or more, the effect of removing tooth stains is sufficient, and when it is 10% or less, discoloration is sufficiently suppressed.
[0015] (C) The water-soluble tin salt acts as a discoloration inhibitor that inhibits discoloration of the formulation caused by the combined use of components (A) and (B). Examples of water-soluble tin salts include tin chloride, tin fluoride, tin acetate, tin gluconate, tin oxalate, tin sulfate, tin lactate, tin tartrate, tin citrate, tin malate, and tin phosphate, with tin chloride and tin fluoride being preferred. As the tin chloride, tin(II) chloride (stannous chloride) can be used, and a hydrate such as tin(II) chloride dihydrate can also be used. As the tin fluoride, tin(II) fluoride (stannous fluoride) or tin(IV) fluoride (stannic fluoride) can be used. In particular, tin(II) fluoride (stannous fluoride) is preferred because it can provide a caries prevention effect. These may be used alone or in combination of two or more, and commercially available products may also be used.
[0016] The amount of (C) water-soluble tin salt is preferably 0.02 to 1.8%, more preferably 0.1 to 0.9%, of the total composition in terms of tin ions. If the content as tin ions is 0.02% or more, the discoloration suppression effect is sufficiently exhibited, and if it is 1.8% or less, the metallic taste of the salt itself is sufficiently suppressed.
[0017] In the present invention, the mass ratio of (C) / (B) (the amount of tin ions in component (C) / the amount of component (B)) is preferably 0.01 to 0.6, more preferably 0.04 to 0.3. When the mass ratio of (C) / (B) is within the above range, the discoloration suppression effect is more excellent and the metallic taste is further suppressed. When the mass ratio is 0.01 or more, the discoloration suppression effect is more excellent, and when it is 0.6 or less, the metallic taste is further suppressed, resulting in an even better feel when used.
[0018] The oral composition of the present invention can be prepared in the form of a paste, gel, liquid, or the like, particularly in the form of a paste or liquid, and used as a toothpaste, gel toothpaste, liquid toothpaste, lubricant toothpaste, or other dentifrices, as well as mouthwashes, mouth sprays, etc. It is particularly suitable as a dentifrices such as toothpaste. Conventional methods can be used as a preparation method depending on the form and dosage form. In this case, other appropriate optional components in addition to the above-mentioned components can be blended as needed depending on the purpose, dosage form, etc. Examples of optional components include surfactants, abrasives, thickeners, humectants, solvents, sweeteners, flavorings, preservatives, colorants, active ingredients, etc. Specific examples of optional components are shown below. These optional components can be blended singly or in combination of two or more, and the blend amount of each optional component can be a normal amount within a range that does not impair the effects of the present invention.
[0019] Surfactants: Examples of surfactants include anionic surfactants, nonionic surfactants, and amphoteric surfactants, and specific examples thereof are shown in (i) to (iii) below. (i) Anionic surfactants Examples of the salts include alkyl sulfates such as lauryl sulfate, acyl sarcosine salts, acyl methyl taurine salts, acyl glutamates, and α-olefin sulfonates (tetradecene sulfonates), and alkali metal salts such as sodium salts and potassium salts are preferred. (ii) Nonionic surfactants Examples of the oils include polyoxyethylene hydrogenated castor oil, polyoxyethylene alkyl ether, polyglycerin fatty acid ester, sorbitan fatty acid ester, and fatty acid monoglyceride. (iii) amphoteric surfactants Examples thereof include fatty acid amidopropyl betaines such as coconut oil fatty acid amidopropyl betaine, and N-fatty acid acyl-N-carboxymethyl-N-hydroxyethyl ethylenediamine salts. The amount of surfactant to be added is preferably 0.001 to 10%, and more preferably 0.1 to 5%, of the total composition.
[0020] Abrasives: The amount of silica-based abrasive such as silicic anhydride, zeolite, calcium carbonate, aluminum hydroxide, and abrasive is usually 2 to 50%, particularly 10 to 40%, of the total composition.
[0021] Thickener: Examples of thickeners include organic thickeners such as xanthan gum, sodium alginate, hydroxyethyl cellulose, carrageenan, sodium carboxymethyl cellulose, polyvinylpyrrolidone, sodium polyacrylate, cationized cellulose, and carboxyvinyl polymer, and inorganic thickeners such as thickening silica. The amount of thickener blended is usually 0.1 to 10%, and particularly 0.1 to 8%, of the total composition.
[0022] Wetting Agent: Examples include sugar alcohols such as sorbitol, xylitol, erythritol, etc., and polyhydric alcohols such as glycerin, propylene glycol, polyethylene glycol (PEG), etc. The amount of humectant blended is usually 2 to 50% of the total composition.
[0023] solvent: Examples include purified water and lower alcohols having 1 to 3 carbon atoms, such as ethanol. When ethanol is added, it may be 25% or less of the total composition, or it may not be added at all.
[0024] Sweeteners: These include saccharin, saccharin sodium, and sucralose.
[0025] Fragrance: Examples include menthol, anethole, carvone, eugenol, limonene, n-decyl alcohol, citronellol, α-terpineol, citronellyl acetate, cineole, linalool, ethyl linalool, vanillin, thymol, spearmint oil, peppermint oil, lemon oil, orange oil, sage oil, rosemary oil, cinnamon oil, pimento oil, cinnamon leaf oil, perilla oil, wintergreen oil, clove oil, and eucalyptus oil, and these can be used alone or in combination of two or more. The blending amount of the fragrance is usually 0.01 to 2% of the entire composition.
[0026] Preservatives: Examples include parahydroxybenzoic acid esters and sodium benzoate. Colorants: These include Blue No. 1, Blue No. 2, Green No. 3, Yellow No. 4, Yellow No. 5, Red No. 106, Red No. 227, caramel, titanium dioxide, and titanium mica.
[0027] Optional active ingredients: Examples of suitable anti-inflammatory agents include fluorine-containing compounds such as sodium fluoride and sodium monofluorophosphate, enzymes such as dextranase, allantoin, glycyrrhizinate, glycyrrhetinic acid, sodium chloride, isopropylmethylphenol, copper gluconate, cetylpyridinium chloride, benzalkonium chloride, benzethonium chloride, hinokitiol, zeolite, aluminum lactate, potassium nitrate, calcium glycerophosphate, and Phellodendron Bark extract. [Example]
[0028] The present invention will be described in detail below with reference to examples and comparative examples, but the present invention is not limited to the following examples. In the following examples, % indicates % by mass unless otherwise specified.
[0029] [Examples and Comparative Examples] Oral compositions (toothpastes) having the compositions shown in Tables 1 to 3 were prepared by conventional methods and evaluated by the following methods, and the results are also shown in the tables. All of the oral compositions of the examples had the effect of removing stains from teeth.
[0030] (1) Evaluation method for storage stability (absence of discoloration) The appearance of the oral compositions was visually inspected after storage for 3 months in a 50°C environment, and the storage stability (lack of discoloration) was evaluated in comparison with a control dentifrice composition stored for 3 months in a -5°C thermostatic chamber, based on the following evaluation criteria. Evaluation criteria: ◎: No discoloration compared to the control product. ○: Slight discoloration is observed compared to the control product, but it is not a problematic level. △: Discoloration is observed compared to the control product, and there is a problem. ×: Discoloration is significantly worse than the control product, and there is a problem.
[0031] (2) Evaluation method for the lack of metallic taste The oral composition was diluted three times with distilled water, and the treatment liquid was placed in the mouth and rinsed for 30 seconds. Five judges then evaluated the absence of a metallic taste based on the following criteria. The average score of the five judges was calculated, and the absence of a metallic taste was judged based on the following criteria. Evaluation criteria: 4 points: No metallic taste at all 3 points: A slight metallic taste is felt, but it is within the acceptable range and is not a problem 2 points: Metallic taste 1 point: A very strong metallic taste Judgment criteria: ◎: Average score 3.5 points or more ○: Average score 3.0 points or more and less than 3.5 points △: Average score 2.0 points or more and less than 3.0 points ×: Average score less than 2.0 points
[0032] Details of the raw materials used are shown below. (A) Sodium hexametaphosphate; manufactured by Taiheiyo Chemical Industries Co., Ltd., sodium metaphosphate (A) Sodium polyphosphate; manufactured by Taiheiyo Chemical Industries Co., Ltd., sodium tripolyphosphate (A) Sodium pyrophosphate; manufactured by Taiheiyo Chemical Industries Co., Ltd., sodium pyrophosphate (anhydrous) (B) sodium pyrrolidone carboxylate; AJIDEW (registered trademark) N-50, manufactured by Ajinomoto Healthy Supply Co., Inc. (C) Tin chloride: Tin(II) chloride dihydrate, manufactured by Fujifilm Wako Pure Chemical Industries, Ltd. (C) Tin fluoride: tin(II) fluoride manufactured by Fujifilm Wako Pure Chemical Industries, Ltd. The composition of fragrance A is detailed below.
[0033] [Table 1] Note: (C) / (B) in the table is the mass ratio of the amount of tin ions in component (C) to the amount of component (B) (the same applies below).
[0034] [Table 2]
[0035] [Table 3]
[0036] Composition of fragrance A; Peppermint oil 50 Peppermint refined oil (20% pre-distillate) 5 Peppermint refined oil (15% front and rear cut) 5 1 spearmint oil Spearmint refined oil (20% pre-distillate) 1 Japanese peppermint oil 1 Japanese mint refined oil (30% front distillate removed) 1 Menthol 10 Carvone 1 1,8-cineole 1 Anethole 5 Cinnamic aldehyde 1 Eugenol 1 Methyl Salicylate 1 Flavor 1 (Table 4) 1 Flavor 2 (Table 5) 1 Flavor 3 (Table 6) 1 Flavor 4 (Table 7) 1 Flavor 5 (Table 8) 1 Flavor 6 (Table 9) 1 Flavor 7 (Table 10) 1 Solvent (Table 11) Remaining Total 100%
[0037] [Table 4]
[0038] [Table 5]
[0039] Table 6
[0040] Table 7
[0041] Table 8
[0042] Table 9
[0043] Table 10
[0044] Table 11
Claims
1. (A) a water-soluble condensed phosphoric acid or a salt thereof, (B) Pyrrolidonecarboxylic acid or its alkali metal salt and (C) Water-soluble tin salt Contains The content of the (A) component is 0.1 to 5 mass%, and the content of the (B) component is 0.5 to 10 mass%, An oral composition in which the content of component (C) is 0.02 to 1.8 mass % in terms of tin ions, and the mass ratio (C) / (B) of the content of component (B) to the content of component (C) in terms of tin ions is 0.01 to 0.
6.
2. 2. The oral composition according to claim 1, wherein (A) the water-soluble condensed phosphoric acid or salt thereof is at least one selected from the group consisting of sodium pyrophosphate, sodium tripolyphosphate, and sodium hexametaphosphate.
3. 3. The oral composition according to claim 1, wherein the pyrrolidone carboxylic acid or the alkali metal salt thereof (B) is sodium pyrrolidone carboxylate.
4. 4. The oral composition according to claim 1, wherein the water-soluble tin salt (C) is at least one selected from the group consisting of tin chloride and tin fluoride.
5. An oral composition according to any one of claims 1 to 4, wherein component (A) is sodium hexametaphosphate.
6. The oral composition according to any one of claims 1 to 5, which is a dentifrice.
Citation Information
Patent Citations
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