Oral composition
By combining tranexamic acid or Ipshiron aminocapronic acid with water-soluble salts and tocopherol esters to form an oral composition, solving the problems of anti-inflammatory effects and appearance stability in a single use, enhancing the user experience and the long-lasting firmness of the formulation.
Patent Information
- Application Number
- JP2020206704
- Authority / Receiving Office
- JP · JP
- Patent Type
- Patents
- Current Assignee / Owner
- Filing Date
- 2020-12-14
- Publication Date
- 2025-02-04
- Estimated Expiration
- 2040-12-14
AI Technical Summary
In the prior art, the effects of anti-inflammatory drugs such as tranexamic acid and Ipshiron aminocapronic acid on gum disease need to be continuously used to manifest. The user's willingness to continue to use is insufficient, and there are problems with the appearance stability of the formulation.
The tranexamic acid or Ipshiron aminocapronic acid is combined with water-soluble salts and tocopherol or its esters to form an oral composition that provides instant gingival firmness and improves appearance stability, inhibiting discoloration of the preparation by adding tocopherol esters.
Provide anti-inflammatory effects in a single use and maintain a firm gum feel while ensuring the appearance stability and long-term effect of the preparation, improving users' willingness to use it.
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Figure 0007625843000003
Abstract
Description
[Technical field]
[0001] The present invention relates to an oral composition containing tranexamic acid or epsilon aminocaproic acid, which provides a high feeling of effectiveness in the oral cavity, particularly on the gums, even with a single use, and is effective for preventing or suppressing periodontal disease. [Background technology]
[0002] Tranexamic acid and epsilon aminocaproic acid are known anti-inflammatory agents, and have been incorporated into oral compositions as components for preventing or suppressing periodontal disease (Patent Document 1; JP 2009-149565 A).
[0003] However, the anti-inflammatory effect of tranexamic acid or epsilon aminocaproic acid against periodontal disease can be gradually felt as a tightening of the gums with continued use, but it is difficult to feel it immediately after one use, so the user's motivation to use may not be maintained. In order to maximize the effect of tranexamic acid or epsilon aminocaproic acid, it is important to maintain the user's motivation to use and encourage continued use. For this purpose, it is effective to let the user feel that tranexamic acid or epsilon aminocaproic acid is effective in the oral cavity, especially in the gums, every time it is used, thereby increasing the user's motivation. [Prior art documents] [Patent documents]
[0004] [Patent Document 1] JP 2009-149565 A [Patent Document 2] Special Publication No. 2019-532946 [Patent Document 3] JP 2017-155010 A 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 tranexamic acid or epsilon aminocaproic acid, which provides a high feeling of effectiveness in the oral cavity, particularly on the gums, even with just one use, and is effective for preventing or suppressing periodontal disease. [Means for solving the problem]
[0006] As a result of intensive research by the present inventors to achieve the above object, it was found that when a water-soluble tin salt and tocopherol or a derivative thereof are combined in an oral composition containing tranexamic acid and / or epsilon aminocaproic acid, a unique, long-lasting, and remarkable feeling of firmness is imparted to the oral cavity, particularly to the gums, with a single use, thereby providing a high feeling of effectiveness that tranexamic acid and / or epsilon aminocaproic acid is working on the gums with each use.Furthermore, it was found that discoloration of the formulation can be suppressed and improved over time, and appearance stability can be ensured. That is, in the present invention, it has been discovered that an oral composition containing (A) one or more selected from tranexamic acid and epsilon aminocaproic acid, (B) a water-soluble tin salt, and (C) one or more selected from tocopherol, its esters with organic acids, and salts thereof, not only has an actual anti-inflammatory effect, but also provides a high level of effectiveness that can be felt in the oral cavity, particularly on the gums, even with just one use, has a stable appearance, and is effective for preventing or suppressing periodontal diseases such as gingivitis, which has led to the completion of the present invention.
[0007] More specifically, in the present invention, by using the component (A) in combination with the component (B) in the oral composition, a unique and long-lasting noticeable feeling of gum tightening (a unique feeling that the feeling of gum tightening continues even after time has passed from immediately after use and is felt prominently, hereinafter sometimes abbreviated as "feeling of gum tightening") can be given, and a high feeling of effectiveness can be given to the gums. The feeling of gum tightening is a unique feeling obtained by the specific action of the component (B) on the component (A) as an effect feeling imparting agent, and is different from the feeling of astringency caused by, for example, other astringents. Furthermore, when the component (A) is used in combination with the component (B), a problem occurs in that the discoloration of the preparation caused by the component (A) significantly worsens over time. However, by further adding the component (C), which is tocopherol or a derivative thereof, the discoloration of the preparation is suppressed and improved without worsening over time as described above, and the appearance stability is maintained, and a high feeling of effectiveness can be given by the feeling of gum tightening. As shown in the comparative examples below, when the oral composition contained the component (A) but did not contain the components (B) and (C), the feeling of tightness of the gums (the feeling of tightness of the gums immediately after use and 10 minutes after use) was low (Comparative Example 1), and when the oral composition contained the components (A) and (B) but did not contain the component (C), the appearance stability (lack of discoloration over time) was poor (Comparative Example 2). In contrast, the oral composition of the present invention containing the components (A), (B) and (C) shown in the examples had excellent feeling of tightness of the gums and appearance stability (lack of discoloration over time). In addition, in Patent Document 2 (JP Patent Publication No. 2019-532946), tranexamic acid or epsilon aminocaproic acid is used in combination with a stannous ion source to impart gingival wound healing and antibacterial effects to an oral care composition, and in Patent Document 3 (JP Patent Publication No. 2017-155010), epsilon aminocaproic acid is combined with pyrrolidone carboxylic acid, vitamins, etc. to improve anti-inflammatory effects and discoloration stability, but these are not improvements in the feeling of effect. In contrast, the present invention combines components (A), (B), and (C) to impart a unique and sustained noticeable feeling of gum tightening, improving the feeling of effect due to component (A) and ensuring appearance stability.
[0008] Accordingly, the present invention provides the following oral compositions. [1] (A) one or more selected from tranexamic acid and epsilon aminocaproic acid, (B) Water-soluble tin salts and (C) one or more selected from tocopherol, its esters with organic acids, and salts thereof An oral composition comprising: [2] (B) The oral composition according to [1], wherein the water-soluble tin salt is one or more selected from tin chloride and tin fluoride. [3] The oral composition according to [1] or [2], wherein the mass ratio of (A) / (C) is 0.2 to 2. [4] The oral composition according to any one of [1] to [3], wherein the mass ratio of (B) (the amount of tin ions in component (B)) / (C) is 0.2 to 10. [5] The oral composition according to any one of [1] to [4], wherein the content of the (A) component is 0.01 to 0.2 mass%, the content of the (B) component is 0.02 to 1 mass% as tin ions, and the content of the (C) component is 0.05 to 0.5 mass%. [6] The oral composition according to any one of [1] to [5], further comprising (D) a cooling agent. [7] The oral composition according to [6], wherein the cooling agent (D) is one or more selected from N-ethyl-p-menthane-3-carboxamide, ethyl-3-(p-menthane-carboxamide) acetate, N-(4-cyanomethylphenyl)-p-menthanecarboxamide, N-(2-(pyridin-2-yl)-3-p-menthanecarboxamide), 2-isopropyl-N,2,3-trimethylbutyramide, menthone glycerol acetal, menthoxypropane-1,2-diol, menthyl lactate and menthyl succinate. [8] The oral composition according to [6] or [7], wherein the content of component (D) is 0.00001 to 0.1 mass%. [9] The oral composition according to any one of [1] to [8], which is a dentifrice, a mouthwash, or a mouth spray. Effect of the Invention
[0009] According to the present invention, it is possible to provide an oral composition that has an appearance stability and that provides a high sense of effectiveness in the oral cavity, such as anti-inflammatory effects due to component (A), even with a single use, and that gives the impression that component (A) is working on the gums. The oral composition of the present invention effectively exerts the anti-inflammatory effects due to component (A), and is effective for preventing or suppressing periodontal diseases such as gingivitis. DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS
[0010] The present invention will now be described in further detail. The oral composition of the present invention contains (A) one or more selected from tranexamic acid and epsilon aminocaproic acid, (B) a water-soluble tin salt, and (C) one or more selected from tocopherol, its esters with organic acids, and salts thereof.
[0011] Component (A) is tranexamic acid and / or epsilon aminocaproic acid, which have anti-inflammatory effects and are effective in preventing or suppressing periodontal disease. From the viewpoint of the effect of preventing or suppressing periodontal disease, the component (A) is preferably tranexamic acid, and a combination of tranexamic acid and epsilon-aminocaproic acid is more preferable.
[0012] The blending amount of component (A) is preferably 0.01 to 0.2% (mass%, hereinafter the same) of the total composition, more preferably 0.03 to 0.1%. When the blending amount is 0.01% or more, a feeling of firmness of the gums is sufficiently obtained, and when it is 0.2% or less, the effect of component (C) in improving the preparation discoloration is sufficiently exhibited, and the stability of the appearance is ensured.
[0013] (B) Water-soluble tin salt, when used in combination with component (A), provides a unique, long-lasting and noticeable feeling of gum tightening, and this feeling of gum tightening provides a sense of actual effectiveness. (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, tin phosphate, tin pyrophosphate, and tin metaphosphate. Of these, tin chloride and tin fluoride are preferred. As the tin chloride, tin(II) chloride (stannous chloride) can be used, and it may be a hydrate such as tin(II) chloride dihydrate. 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 also impart a caries prevention effect. These may be used alone or in combination of two or more.
[0014] The amount of the water-soluble tin salt (B) is preferably 0.02 to 1% of the total composition in terms of tin ions, more preferably 0.03 to 0.7%, and even more preferably 0.1 to 0.7%. If the tin ion content is 0.02% or more, a feeling of firmness of the gums is sufficiently obtained, and if it is 1% or less, the effect of component (C) in improving the discoloration of the preparation is sufficiently exhibited, and the stability of the appearance is ensured.
[0015] The component (C) is tocopherol or a derivative thereof, and the derivative may be an ester of tocopherol with an organic acid or a salt thereof. These may be used alone or in combination of two or more. The component (C) prevents the discoloration of the formulation caused by the combined use of the components (A) and (B), suppresses and improves the discoloration of the formulation over time, and ensures the stability of the appearance.
[0016] Examples of tocopherol include d-α-tocopherol, dl-α-tocopherol, β-tocopherol, γ-tocopherol, δ-tocopherol, etc. Examples of tocopherol derivatives include esters of the above tocopherol with organic acids such as acetic acid, nicotinic acid, succinic acid, linolenic acid, etc., or salts thereof. Specific examples include tocopherol acetate esters such as d-α-tocopherol acetate and dl-α-tocopherol acetate, tocopherol nicotinic acid esters such as d-α-tocopherol nicotinic acid and dl-α-tocopherol nicotinic acid, tocopherol succinic acid esters such as d-α-tocopherol succinate and dl-α-tocopherol succinate, tocopherol linolenic acid esters such as d-α-tocopherol linolenic acid and dl-α-tocopherol linolenic acid, and tocopherol calcium succinate. Among these, tocopherol acetate is preferred in terms of suppressing discoloration of the preparation. These tocopherols or derivatives thereof that can be used are those that comply with the former Cosmetic Raw Materials Standards (Shogenki) or the Quasi-drug Raw Materials Standards 2006, and commercially available products manufactured by DSM Nutrition Japan, Eisai Food & Chemical Co., Ltd., BASF Japan Ltd., etc. can be used.
[0017] The amount of component (C) in the composition is preferably 0.05-0.5%, more preferably 0.05-0.2%. When the amount is 0.05% or more, the effect of improving discoloration of the preparation is sufficiently obtained. When the amount is 0.5% or less, the feeling of tightness of the gums is sufficiently maintained. When the amount is more than 0.5%, the oily component (C) may interfere with the expression of the feeling of tightness of the gums.
[0018] In the present invention, the ratio of the blend amount of the component (A) to the blend amount of the component (C), (A) / (C), is preferably 0.2-2, more preferably 0.3-1, as a mass ratio. Furthermore, the ratio (B) / (C) of the amount of component (B) (as tin ions) to the amount of component (C) is preferably 0.2-10, and more preferably 0.3-9, as a mass ratio. When either the mass ratio of (A) / (C) or the mass ratio of (B) / (C) is within the above range, the feeling of firming of the gums is better and the effect of improving discoloration of the preparation is also better. When the mass ratio of (A) / (C) is less than 0.2 or the mass ratio of (B) / (C) is less than 0.2, the feeling of firming of the gums may not be sufficient. When the mass ratio of (A) / (C) is more than 2 or the mass ratio of (B) / (C) is more than 10, the effect of improving discoloration of the preparation may not be sufficient. It is particularly preferable in terms of realizing the effects of the present invention that the mass ratio of (A) / (C) and the mass ratio of (B) / (C) are both within the above ranges.
[0019] The oral composition of the present invention preferably further contains a cooling agent (D). The incorporation of component (D) enhances the feeling of firmness of the gums, further improving the feeling of effectiveness. Examples of the (D) component include N-ethyl-p-menthane-3-carboxamide, ethyl-3-(p-menthane-carboxamide) acetate, N-(4-cyanomethylphenyl)-p-menthanecarboxamide, N-(2-(pyridin-2-yl)-3-p-menthanecarboxamide), 2-isopropyl-N,2,3-trimethylbutyramide, menthone glycerol acetal, menthoxypropane-1,2-diol, menthyl lactate, and menthyl succinate. Among these, N-(4-cyanomethylphenyl)-p-menthanecarboxamide and N-(2-(pyridin-2-yl)-3-p-menthanecarboxamide) are preferred. These may be used alone or in combination of two or more. Specifically, the following commercially available products can be used. N-Ethyl-p-menthane-3-carboxamide; Symrise, WS-3 Ethyl 3-(p-menthane-carboxamide) acetate; Toyotama Fragrance Co., Ltd., WS-5 N-(4-cyanomethylphenyl)-p-menthanecarboxamide: EVERCOOL 180, manufactured by Givaudan Japan Co., Ltd. N-(2-(pyridin-2-yl)-3-p-menthanecarboxamide); EVERCOOL 190, manufactured by Givaudan Japan Co., Ltd. 2-Isopropyl-N,2,3-trimethylbutyramide; Givaudan Japan Co., Ltd., WS-23 Menthone glycerol acetal; Symrise, MGA Menthoxypropane-1,2-diol; Takasago International Corporation, CA10 Menthyl lactate; manufactured by Symrise Menthyl succinate (monomenthyl succinate); manufactured by Vimanfis
[0020] When component (D) is included, the amount added is preferably 0.00001 to 0.1%, more preferably 0.00003 to 0.07%, and particularly preferably 0.00005 to 0.05% of the total composition.
[0021] The oral cavity composition of the present invention can be prepared in the form of a paste, gel, liquid, etc., and used as a dentifrice such as toothpaste, gel dentifrice, liquid dentifrice, lubricant dentifrice, etc., a mouthwash, a mouth spray, etc. Among them, it is suitable as a dentifrice, a mouthwash, or a mouth spray, particularly as a dentifrice. The preparation method can be a conventional method according to the form and dosage form. In this case, other optional components may be added as necessary in addition to the above-mentioned components depending on the purpose, dosage form, etc. of the oral composition. 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 may be blended alone or in combination of two or more, and the blended amount of each optional component may be a normal amount within a range that does not impair the effects of the present invention.
[0022] Surfactants: Examples of the surfactant include anionic surfactants, nonionic surfactants, and amphoteric surfactants, and specific examples thereof are shown in the following (i) to (iii). (i) Anionic surfactants Examples of the salt include alkyl sulfates such as lauryl sulfate, acyl sarcosine salts, acyl methyl taurine salts, acyl glutamate salts, and α-olefin sulfonate salts (tetradecene sulfonate salts). As the above salts, alkali metal salts such as sodium salts and potassium salts are preferred. (ii) Nonionic surfactants Examples of the fatty acid esters include polyoxyethylene hydrogenated castor oil, polyoxyethylene alkyl ethers, polyglycerin fatty acid esters, sorbitan fatty acid esters, and fatty acid monoglycerides. (iii) Amphoteric surfactants Examples of the fatty acid amidopropyl betaine include coconut oil fatty acid amidopropyl betaine and N-fatty acid acyl-N-carboxymethyl-N-hydroxyethyl ethylenediamine salts. The amount of the surfactant to be added is preferably 0.001 to 10%, and more preferably 0.1 to 5%, of the total composition.
[0023] Abrasives: Examples of the abrasive include silica-based abrasives such as silicic anhydride, zeolite, calcium carbonate, aluminum hydroxide, and aluminum oxide. The amount of the abrasive blended is usually 2 to 50%, particularly 10 to 40%, of the entire composition.
[0024] Thickener: Examples of the thickener include organic thickeners such as xanthan gum, sodium alginate, hydroxyethyl cellulose, carrageenan, sodium carboxymethyl cellulose, polyvinylpyrrolidone, sodium polyacrylate, and carboxyvinyl polymers, and inorganic thickeners such as thickening silica. The blending amount of the thickener is usually 0.1 to 10%, particularly 0.1 to 8%, of the entire composition.
[0025] Wetting Agent: Examples of the alcohol include sugar alcohols such as sorbitol, xylitol, and erythritol, and polyhydric alcohols such as glycerin, propylene glycol, and polyethylene glycol (PEG). The amount of the wetting agent is usually 2 to 50% of the entire composition.
[0026] solvent: Examples of the alcohol include purified water and lower alcohols having 1 to 3 carbon atoms, such as ethanol. When ethanol is added, it may be present in an amount of 25% or less of the entire composition, or it may not be added at all. Sweeteners: Examples include saccharin, sodium saccharin, and sucralose.
[0027] Fragrance: Examples of such oils 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. These may 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.
[0028] Preservatives: Examples include paraoxybenzoic 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 Oxide, and Titanium Mica.
[0029] Optional Active Ingredients: Examples of such additives include fluorine-containing compounds such as sodium fluoride and sodium monofluorophosphate, enzymes such as dextranase, sodium pyrrolidone carboxylate, allantoin, glycyrrhizinate, glycyrrhetinic acid, sodium chloride, isopropylmethylphenol, copper gluconate, cetylpyridinium chloride, benzalkonium chloride, benzethonium chloride, hinokitiol, pyrophosphate, polyphosphate, metaphosphate, zeolite, aluminum lactate, potassium nitrate, calcium glycerophosphate, and Phellodendron Bark extract. EXAMPLES
[0030] The present invention will be specifically described below with reference to examples, comparative examples, and formulation examples, but the present invention is not limited to the following examples. In the following examples, % indicates % by mass unless otherwise specified.
[0031] [Examples and Comparative Examples] Dentifrice compositions having the compositions shown in Tables 1 to 4 were prepared by conventional methods and evaluated by the following methods. The results are also shown in the tables. In addition, all of the dentifrice compositions of the Examples containing (A) tranexamic acid and / or epsilon aminocaproic acid had the anti-inflammatory effect and other functional effects derived from component (A).
[0032] (1) Method for evaluating the feeling of gum tightness The sensory evaluation was carried out by 10 expert panelists. The dentifrice composition packed in a laminated tube was squeezed out 1 cm onto the toothbrush, and the subjects brushed their teeth for 3 minutes in the same way as usual. They then judged the feeling of tightness of the gums immediately after use and 10 minutes after use according to the following criteria. The feeling of tight gums is a distinctive sensation that is noticeable and lasts for a long time after use, in which the feeling of tight gums continues. Judgment criteria 5 points: I felt a very strong tightening of my gums immediately after use and even after 10 minutes had passed. 4 points: I felt a strong tightening of my gums immediately after use and even after 10 minutes had passed. 3 points: Gums feel slightly tighter immediately after use and even after 10 minutes. 2 points: I don't feel much tightening of my gums immediately after use or after 10 minutes. 1 point: No feeling of tightness in the gums immediately after use or after 10 minutes The average of the results of the 10 judges was calculated and rated according to the following criteria. Those that secured the ratings of ◯, ◎, and ☆ were judged to be dentifrice compositions that gave a feeling of firmness to the gums and were excellent in terms of the effect felt on the gums. Evaluation criteria ☆: Average score 4.5 points or more ◎: Average score 4.0 or more and less than 4.5 points ○: Average score 3.0 points or more and less than 4.0 points △: Average score 2.0 to less than 3.0 ×: Average score 1.0 or more and less than 2.0 points
[0033] (2) Evaluation method for appearance stability The appearance of the dentifrice compositions immediately after production and after storage for 3 months in a 50°C environment was visually inspected, and the appearance stability (absence of discoloration over time) was evaluated according to the following criteria. The dentifrice compositions immediately after production were white in color. Evaluation criteria ◎: No discoloration observed ○: Very slight discoloration is observed, but not to a level that causes problems. △: Discoloration is observed ×: Significant discoloration is observed
[0034] Details of the raw materials used are shown below. (A) Tranexamic acid; manufactured by Kyowa Pharma Chemical Co., Ltd. (A) Epsilon-aminocaproic acid; manufactured by Daiichi Sankyo Co., Ltd. (B) Tin chloride: Fujifilm Wako Pure Chemical Industries, Ltd., tin(II) chloride dihydrate (B) Tin fluoride; Fujifilm Wako Pure Chemical Industries, Ltd., Tin(II) fluoride (C) tocopherol acetate; DSM Nutrition Japan, dl-α-tocopherol acetate (D) N-(4-cyanomethylphenyl)-p-menthanecarboxamide; Givaudan Japan Co., Ltd., Evercool 180 (D) N-(2-(pyridin-2-yl)-3-p-menthanecarboxamide); Givaudan Japan Co., Ltd., Evercool 190 The detailed composition of fragrance A is described below.
[0035] [Table 1] Note: (B) / (C) is the mass ratio of (the amount of component (B) blended as tin ion) / (the amount of component (C) blended) (hereinafter the same).
[0036] [Table 2]
[0037] [Table 3]
[0038] [Table 4]
[0039] Composition of fragrance A: Peppermint oil 50 Peppermint refined oil (20% pre-distillate cut) 5 Peppermint refined oil (15% front and rear part cut) 5 Spearmint oil 1 Spearmint refined oil (20% pre-distillate cut) 1 Japanese peppermint oil 1 Japanese peppermint refined oil (30% front distillate cut) 1 Menthol 10 Carbone 1 1,8-Cineole 1 Anethole 5 Cinnamic aldehyde 1 Eugenol 1 Methyl Salicylate 1 Flavor 1 (Table 5) 1 Flavor 2 (Table 6) 1 Flavor 3 (Table 7) 1 Flavor 4 (Table 8) 1 Flavor 5 (Table 9) 1 Flavor 6 (Table 10) 1 Flavor 7 (Table 11) 1 Solvent (Table 12) Remaining Total 100%
[0040] [Table 5]
[0041] [Table 6]
[0042] [Table 7]
[0043] [Table 8]
[0044] [Table 9]
[0045] [Table 10]
[0046] [Table 11]
[0047] [Table 12]
[0048] An example of a prescription is shown below.
[0049] [Prescription Example 1] Dentifrice (A) Tranexamic acid 0.05 (B) Tin fluoride (stannous fluoride) 0.4 (C) Tocopherol acetate 0.1 Sodium monofluorophosphate 0.38 Isopropyl methylphenol 0.05 Aluminum Lactate 2 Potassium nitrate 5 Sodium citrate 0.5 Sodium hexametaphosphate 1 Abrasive Silica 18 Sodium lauryl sulfate 0.6 Sodium methyl lauroyl taurate 0.6 Polyoxyethylene (20) hydrogenated castor oil 1 Sodium lauroyl glutamate 0.1 70% sorbitol solution 10 85% glycerin solution 30 Propylene glycol 3 Xanthan gum 0.3 Sodium carboxymethylcellulose 1.0 Polyethylene glycol 4000 0.5 Copper gluconate 0.1 Viscosifying Silica 1 Titanium dioxide 0.4 Sodium saccharin 0.08 Sodium hydroxide (adjust pH to 5.8) Fragrance A 1.3 Purified water Balance Total 100%
[0050] [Prescription Example 2] Dentifrice (A) Epsilon-aminocaproic acid 0.05 (B) Tin fluoride (stannous fluoride) 0.4 (C) Tocopherol acetate 0.1 Sodium fluoride 0.11 Isopropyl methylphenol 0.05 Aluminum Lactate 2 Potassium nitrate 5 Sodium citrate 0.5 Sodium hexametaphosphate 1 Abrasive Silica 15 Sodium lauryl sulfate 0.6 Sodium tetradecene sulfonate 0.5 Sodium Lauroyl Sarcosinate 0.2 Coconut oil fatty acid amidopropyl betaine solution (30%) 0.9 85% glycerin solution 28 Propylene glycol 3 Carrageenan 0.3 Xanthan gum 0.3 Sodium carboxymethylcellulose 0.7 Sodium pyrrolidone carboxylate 3.0 Cationic cellulose 0.05 Viscosifying Silica 2 Titanium dioxide 0.3 Sodium saccharin 0.1 Sodium hydroxide (adjust pH to 6.5) Fragrance A 1.3 Purified water Balance Total 100%
[0051] [Prescription Example 3] Mouthwash (A) Tranexamic acid 0.05 (B) Tin fluoride (stannous fluoride) 0.1 (C) Tocopherol acetate 0.05 Isopropyl methylphenol 0.05 70% sorbitol solution 5 85% glycerin solution 1 Xylitol 1 Sodium Lauroyl Sarcosinate 0.1 Propylene glycol alginate 0.1 Polyoxyethylene (60) hydrogenated castor oil 0.3 Polyoxyethylene (15) Cetyl Ether 0.1 Propylene glycol 3 Ethanol 10 Citric acid 0.05 Sodium citrate 0.3 Sodium hydroxide (adjust pH to 6.0) Fragrance A 0.1 Purified water Balance Total 100%
[0052] [Formulation Example 4] Mouth spray (A) Tranexamic acid 0.05 (B) Tin fluoride (stannous fluoride) 0.1 (C) Tocopherol acetate 0.05 Isopropyl methylphenol 0.05 Sodium hexametaphosphate 0.01 85% glycerin solution 30 70% sorbitol solution 4 Polyethylene glycol 400 2 Xylitol 1 Cetylpyridinium chloride 0.05 Ethanol 25 Polyoxyethylene (60) hydrogenated castor oil 2 Copper gluconate 0.01 Citric acid 0.05 Sodium citrate 0.3 Sodium hydroxide (adjust pH to 6.0) Fragrance A 0.5 Purified water Balance Total 100%
Claims
1. (A) one or more selected from tranexamic acid and epsilon aminocaproic acid, (B) Water-soluble tin salt and (C) one or more selected from tocopherol, its esters with organic acids, and salts thereof An oral composition comprising:
2. 2. The oral composition according to claim 1, wherein the water-soluble tin salt (B) is at least one selected from the group consisting of tin chloride and tin fluoride.
3. 3. The oral composition according to claim 1, wherein the mass ratio of (A) / (C) is 0.2 to 2.
4. 4. The oral composition according to claim 1, wherein the mass ratio of (B) (the amount of tin ions in component (B)) / (C) is 0.2 to 10.
5. The content of the (A) component is 0.01 to 0.2 mass %, 5. The oral composition according to claim 1, wherein the content of component (B) is 0.02 to 1 mass % in terms of tin ions, and the content of component (C) is 0.05 to 0.5 mass %.
6. The oral composition according to any one of claims 1 to 5, further comprising (D) a cooling agent.
7. The oral composition according to claim 6, wherein the cooling agent (D) is one or more selected from the group consisting of N-ethyl-p-menthane-3-carboxamide, ethyl-3-(p-menthane-carboxamide) acetate, N-(4-cyanomethylphenyl)-p-menthanecarboxamide, N-(2-(pyridin-2-yl)-3-p-menthanecarboxamide), 2-isopropyl-N,2,3-trimethylbutyramide, menthone glycerol acetal, menthoxypropane-1,2-diol, menthyl lactate and menthyl succinate.
8. The oral composition according to claim 6 or 7, wherein the content of component (D) is 0.00001 to 0.1 mass %.
9. The oral composition according to any one of claims 1 to 8, which is a dentifrice, a mouthwash or a mouth spray.
Citation Information
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