JP7625843B2 - Oral Composition - Google Patents

Description

The present invention relates to an oral composition containing tranexamic acid or epsilon aminocaproic acid that provides a high feeling of effectiveness in the oral cavity, particularly on the gums, even with a single use, and is effective in preventing or inhibiting periodontal disease.

Tranexamic acid and epsilon aminocaproic acid are known anti-inflammatory agents that have been incorporated into oral compositions as ingredients for preventing or suppressing periodontal disease (Patent Document 1; JP 2009-149565 A).

However, although the anti-inflammatory effects of tranexamic acid and epsilon aminocaproic acid against periodontal disease can be gradually felt with continued use as a feeling of tightening of the gums, it is difficult to feel the effects immediately after one use, and so users may not be able to maintain their motivation to use the product. In order to maximize the effects of tranexamic acid and epsilon aminocaproic acid, it is important to maintain the user's motivation to use the product and encourage continued use. To achieve this, it is effective to increase the user's motivation by letting them feel that tranexamic acid and epsilon aminocaproic acid are working in the oral cavity, especially on the gums, with each use.

JP 2009-149565 A Special table 2019-532946 publication JP 2017-155010 A

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 that provides a high feeling of effectiveness in the oral cavity, particularly on the gums, even with a single use, and is effective in preventing or suppressing periodontal disease.

As a result of intensive research conducted 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 level of feeling that tranexamic acid and/or epsilon aminocaproic acid is working on the gums with each use. In addition, 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 was 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 feeling of effectiveness 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, leading to the creation of the present invention.

More specifically, in the present invention, by using the component (A) in combination with the component (B) in the oral composition, a unique, long-lasting, and remarkable 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 imparted, and a high feeling of effectiveness can be imparted 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 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 imparted by the feeling of gum tightening.
As shown in the comparative examples described later, 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 containing the components (A), (B) and (C) of the present invention shown in the examples was excellent in the feeling of tightness of the gums and the 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, sustained, and remarkable feeling of gum tightening, improving the feeling of effect due to component (A) and ensuring appearance stability.

Accordingly, the present invention provides the following oral compositions.
[1]
(A) one or more selected from tranexamic acid and epsilon aminocaproic acid,
An oral composition comprising (B) a water-soluble tin salt and (C) at least one member selected from the group consisting of tocopherol, its esters with organic acids, and salts thereof.
[2]
The oral composition according to claim 1, wherein the water-soluble tin salt (B) 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 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 [1] to [8], which is a dentifrice, a mouthwash or a mouth spray.

According to the present invention, it is possible to provide an oral composition that has an appearance stability and that provides the anti-inflammatory and other effects of component (A) in the oral cavity even with a single use, as well as a high sense of effectiveness that component (A) is working on the gums. The oral composition of the present invention effectively exerts the anti-inflammatory and other effects of component (A), and is effective for preventing or suppressing periodontal diseases such as gingivitis.

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.

Component (A) is tranexamic acid and/or epsilon aminocaproic acid, which have an anti-inflammatory effect 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 even more preferable.

The amount of component (A) is preferably 0.01 to 0.2% (mass %, hereinafter the same) of the entire composition, and more preferably 0.03 to 0.1%. If the amount is 0.01% or more, a feeling of firmness of the gums is sufficiently obtained, and if it is 0.2% or less, the effect of component (C) in improving the discoloration of the formulation is sufficiently exerted, and the stability of the appearance is ensured.

(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.

The amount of water-soluble tin salt (B) is preferably 0.02-1% of the total composition in terms of tin ions, more preferably 0.03-0.7%, and even more preferably 0.1-0.7%. If the tin ion content is 0.02% or more, a sufficient feeling of firmness of the gums is obtained, and if it is 1% or less, the effect of component (C) in improving the discoloration of the formulation is fully exerted, and the stability of the appearance is ensured.

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. Component (C) prevents the discoloration of the formulation caused by the combined use of components (A) and (B), suppresses and improves discoloration of the formulation over time, and ensures the stability of appearance.

Examples of tocopherol include d-α-tocopherol, dl-α-tocopherol, β-tocopherol, γ-tocopherol, and δ-tocopherol. Examples of tocopherol derivatives include esters of the above-mentioned tocopherols with organic acids such as acetic acid, nicotinic acid, succinic acid, and linolenic acid, or salts thereof. Specific examples include tocopherol acetate esters such as d-α-tocopherol acetate and dl-α-tocopherol acetate, tocopherol nicotinate esters such as d-α-tocopherol nicotinate and dl-α-tocopherol nicotinate, tocopherol succinate esters such as d-α-tocopherol succinate and dl-α-tocopherol succinate, tocopherol linolenate esters such as d-α-tocopherol linolenate and dl-α-tocopherol linolenate, 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.

The amount of component (C) in the composition is preferably 0.05-0.5%, more preferably 0.05-0.2%, of the total composition. If the amount is 0.05% or more, the discoloration of the formulation can be sufficiently improved. If the amount is 0.5% or less, the feeling of tightness of the gums is sufficiently maintained. If the amount is more than 0.5%, the oily component (C) may interfere with the expression of a feeling of tightness of the gums.

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 to 2, more preferably 0.3 to 1, in terms of mass ratio.
Furthermore, the ratio (B)/(C) of the amount of component (B) (as tin ions) to the amount of component (C) is preferably from 0.2 to 10, and more preferably from 0.3 to 9, in terms of 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 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 when the mass ratio of (B)/(C) is less than 0.2, the feeling of firming the gums may not be sufficient.In addition, when the mass ratio of (A)/(C) is more than 2, or when 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 exerting 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.

The oral composition of the present invention preferably further contains a cooling agent (D). By including the component (D), the feeling of firmness of the gums is further enhanced, and the effect of the composition is further improved.
Examples of component (D) 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. Of 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 Ltd.
N-(2-(pyridin-2-yl)-3-p-menthanecarboxamide); EVERCOOL 190, manufactured by Givaudan Japan Ltd.
2-Isopropyl-N,2,3-trimethylbutyramide; WS-23, manufactured by Givaudan Japan Ltd.
Menthone glycerol acetal; MGA, manufactured by Symrise
Menthoxypropane-1,2-diol; manufactured by Takasago International Corporation, CA10
Menthyl lactate: manufactured by Symrise Menthyl succinate (monomenthyl succinate): manufactured by Vimanfis

When component (D) is included, the amount is preferably 0.00001 to 0.1% of the total composition, more preferably 0.00003 to 0.07%, and particularly preferably 0.00005 to 0.05%.

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 blend amount of each optional component may be a normal amount within a range that does not impair the effects of the present invention.

Surfactants:
Examples of the surfactant include anionic surfactants, nonionic surfactants, and amphoteric surfactants, and specific examples thereof are shown in (i) to (iii) below.
(i) Anionic Surfactants Examples of anionic surfactants 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 nonionic surfactants include polyoxyethylene hydrogenated castor oil, polyoxyethylene alkyl ether, polyglycerin fatty acid ester, sorbitan fatty acid ester, and fatty acid monoglyceride.
(iii) Amphoteric Surfactants Examples of amphoteric surfactants 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 the surfactant to be blended is preferably 0.001 to 10%, and more preferably 0.1 to 5%, of the total composition.

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 from 2 to 50%, particularly from 10 to 40%, of the entire composition.

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 amount of the thickener blended is usually from 0.1 to 10%, particularly from 0.1 to 8%, of the entire composition.

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 total composition.

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 25% or less of the total composition, or it may not be added at all.
Sweeteners:
Examples include saccharin, sodium saccharin, and sucralose.

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 oils may be used alone or in combination of two or more.
The amount of the fragrance blended is usually 0.01 to 2% of the total composition.

Preservatives:
Examples include paraoxybenzoic acid esters and sodium benzoate.
Colorants:
Examples 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.

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.

The present invention will be specifically explained below with examples, comparative examples, and formulation examples, but the present invention is not limited to the following examples. In the following examples, % indicates mass % unless otherwise specified.

[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).

(1) Evaluation method for gum tightness: A sensory evaluation was carried out by 10 expert panelists. The dentifrice composition filled in a laminated tube was pressed out 1 cm onto a toothbrush, and the toothbrush was brushed for 3 minutes in the same manner as usual. The gum tightness immediately after use and 10 minutes after use were evaluated 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.
Evaluation criteria: 5 points: Very strong feeling of gum tightening immediately after use and after 10 minutes 4 points: Strong feeling of gum tightening immediately after use and after 10 minutes 3 points: Slight feeling of gum tightening immediately after use and after 10 minutes 2 points: Not much feeling of gum tightening immediately after use and after 10 minutes 1 point: No feeling of gum tightening immediately after use and after 10 minutes The average of the evaluation results of 10 people was calculated and evaluated according to the following evaluation criteria. Those that secured the evaluations of ◯, ◎, and ☆ were judged to be dentifrice compositions that gave a feeling of gum tightening and were excellent in terms of the effect felt on the gums.
Evaluation criteria: ☆: Average score of 4.5 points or more ◎: Average score of 4.0 points or more and less than 4.5 points ○: Average score of 3.0 points or more and less than 4.0 points △: Average score of 2.0 points or more and less than 3.0 points ×: Average score of 1.0 points or more and less than 2.0 points

(2) Evaluation method for appearance stability The appearance of the dentifrice compositions immediately after production and after storage for 3 months in an environment of 50° C. was visually confirmed, and the appearance stability (absence of discoloration over time) was evaluated according to the following evaluation criteria. The dentifrice compositions immediately after production were white in color.
Evaluation criteria: ◎: No discoloration is observed. ○: Very slight discoloration is observed, but not at a problem level. △: Discoloration is observed. ×: Significant discoloration is observed.

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; manufactured by Fujifilm Wako Pure Chemical Industries, Ltd., tin(II) chloride dihydrate (B) Tin fluoride; manufactured by 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 composition of fragrance A will be described in detail below.

注；（Ｂ）／（Ｃ）は、（（Ｂ）成分のスズイオンとしての配合量）／（（Ｃ）成分の配合量）の質量比である（以下同様）。

Note: (B)/(C) is the mass ratio of (the amount of component (B) blended as tin ions)/(the amount of component (C) blended) (the same applies below).

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% of the front part 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) Remainder
Total 100%

An example prescription is shown below.

[Formulation 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 oxide 0.4
Sodium saccharin 0.08
Sodium hydroxide (adjust pH to 5.8)
Fragrance A 1.3
Purified water Balance
Total 100%

[Formulation 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 sarcosine 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 oxide 0.3
Sodium saccharin 0.1
Sodium hydroxide (adjust pH to 6.5)
Fragrance A 1.3
Purified water Balance
Total 100%

[Formulation 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 sarcosine 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%

[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 (9)

(A) one or more selected from tranexamic acid and epsilon aminocaproic acid,
An oral composition comprising (B) a water-soluble tin salt and (C) at least one member selected from the group consisting of tocopherol, its esters with organic acids, and salts thereof. The oral composition according to claim 1, wherein (B) the water-soluble tin salt is at least one selected from tin chloride and tin fluoride. The oral composition according to claim 1 or 2, wherein the mass ratio of (A)/(C) is 0.2 to 2. The oral composition according to any one of claims 1 to 3, wherein the mass ratio of (B) (the amount of tin ions in component (B))/(C) is 0.2 to 10. 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 %. The oral composition according to any one of claims 1 to 5, further comprising (D) a cooling agent. The oral composition according to claim 6, wherein (D) the cooling agent 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. The oral composition according to claim 6 or 7, wherein the content of component (D) is 0.00001 to 0.1% by mass. The oral composition according to any one of claims 1 to 8, which is a dentifrice, a mouthwash or a mouth spray.