JP2019052110A - Oral composition - Google Patents

Abstract

To provide an oral composition that maintains a refreshing feeling of a preparation thereof by improving a discomfort of aftertaste caused by a combination of cetylpyridinium chloride and tranexamic acid, and further has excellent bactericidal action.SOLUTION: An oral composition contains (A) tranexamic acid or a salt thereof; (B) a cationic bactericide; (C) a bactericide as an anionic surfactant; and (D) a fluorine-containing compound whose amount is 1001 ppm-3000 ppm in terms of fluorine concentrations.SELECTED DRAWING: None

Description

  The present invention relates to a composition for oral cavity containing tranexamic acid, a cationic fungicide, a fungicide which is an anionic surfactant, and fluorine.

  In oral compositions such as dentifrices and mouthwashes, the cationic fungicide cetylpyridinium chloride is often used to suppress plaque and prevent periodontal disease and caries. Tranexamic acid is also added as an anti-inflammatory agent having an excellent effect on gingivitis. However, there is a problem that the feeling of use deteriorates because there is an uncomfortable feeling of the aftertaste with a unique astringent feeling, and the unpleasant aftertaste after use cannot give a refreshing and refreshing feeling of use. .

  Cetylpyridinium chloride, which is widely used in oral compositions as a cationic bactericidal agent, has a unique bitter taste, and it is common to increase the amount of sweeteners such as saccharin to suppress it, and in combination with stevia sweeteners A technique for improving palatability has been proposed (for example, see Patent Document 1). Alternatively, it has been proposed to mask bitterness by using magnesium chloride in combination. (For example, refer to Patent Document 2). Moreover, the method of masking with a fragrance | flavor component is also proposed (for example, refer patent document 3). However, these methods have a problem that the refreshing feeling of the preparation is lowered due to the sweetness of the sweetener or the stimulation of the fragrance component.

  Tranexamic acid also has an excellent anti-inflammatory and hemostatic effect and is known to be effective for the prevention of periodontal diseases and has been widely used as a composition for oral cavity. In order to actually use it with a bitter taste, it is necessary to improve it. In order to suppress this, it has been proposed to use maltitol (for example, see Patent Document 4) or use a water-soluble calcium salt. (For example, refer to Patent Document 5) However, these methods limit the taste and have problems such as being unable to cope with various user preferences. Furthermore, the combination of cetylpyridinium chloride and tranexamic acid has been studied for its preventive effect on periodontal disease (see, for example, Non-Patent Document 1). There are no studies on the suppression of these bacteria.

  Further, for the purpose of providing a dentifrice composition excellent in caries prevention effect, a dentifrice composition characterized by containing a fluorine-containing compound in an amount of 1100 ppm to 3000 ppm as a fluorine concentration has been proposed. (See Patent Document 6). Furthermore, it is characterized in that 1100 ppm to 3000 ppm of a fluorine compound as a fluorine compound is compounded in a dentifrice composition containing isopropylmethylphenol, an anionic surfactant, and a nonionic surfactant filled in a container made of polyethylene as the innermost layer. A dentifrice composition has been proposed (see Patent Document 7).

  However, conventional dentifrices have not been provided with an oral composition containing a high concentration of fluorine and a combination of a cationic bactericidal agent and tranexamic acid.

JP 05-931 A JP-A-9-95457 JP 2004-18431 A JP 2003-128540 A JP 2005-104911 A Japanese Patent Laid-Open No. 2006-124787 Japanese Patent Laid-Open No. 2006-199473

Periodontal Journal 36 (2): 466-473 1994

  While the present inventors have confirmed the excellent action of a preparation comprising cetylpyridinium chloride and tranexamic acid, the present inventors have found a problem that the feeling of discomfort after use is increased. An object of the present invention is to provide an oral composition having a further excellent bactericidal action while maintaining the refreshing feeling of the preparation by improving the discomfort of the aftertaste caused by the combination of cetylpyridinium chloride and tranexamic acid. is there.

  As a result of intensive studies to solve the above-mentioned problems, the present inventors have added an antibacterial agent that is an anionic surfactant and a high concentration of fluorine to a preparation containing cetylpyridinium chloride and tranexamic acid, thereby improving the aftertaste. It was found that a composition for oral cavity having both a refreshing and refreshing feeling of use and an excellent bactericidal effect can be obtained. The present invention has been completed based on the above findings.

That is, the present invention relates to the following (1) to (8).
(1) (A) tranexamic acid or a salt thereof;
(B) a cationic fungicide;
(C) a bactericidal agent which is an anionic surfactant; and (D) a fluorine-containing compound in an amount of 1001 ppm to 3000 ppm as the fluorine concentration;
The composition for oral cavity containing this.
(2) The composition for oral cavity according to (1), wherein the cationic bactericidal agent is a quaternary ammonium salt type cationic bactericidal agent.
(3) The composition for oral cavity according to (1) or (2), wherein the cationic bactericidal agent is cetylpyridinium chloride.
(4) The composition for oral cavity according to any one of (1) to (3), wherein the content of the cationic bactericide is 0.01 to 0.5% by mass.
(5) The composition for oral cavity according to any one of (1) to (4), wherein the bactericide which is an anionic surfactant is sodium lauroyl sarcosine.
(6) The composition for oral cavity as described in any one of (1) to (5) whose content of the bactericide which is an anionic surfactant is 0.01-1.0 mass%.
(7) The composition for oral cavity as described in any one of (1) to (6) whose content of tranexamic acid or its salt is 0.001-0.5 mass%.
(8) The composition for oral cavity according to any one of (1) to (7), which is a mouthwash or a dentifrice.

  ADVANTAGE OF THE INVENTION According to this invention, the discomfort of the aftertaste of the formulation which mix | blends a cationic disinfectant and tranexamic acid can be improved dramatically, and the composition for oral cavity which has the outstanding bactericidal action can be provided. Therefore, it can be suitably used for the prevention or suppression of periodontal diseases due to the excellent usability and bactericidal power according to the present invention.

Embodiments of the present invention will be described below.
The composition for oral cavity of the present invention is
(A) tranexamic acid or a salt thereof;
(B) a cationic fungicide;
(C) a bactericidal agent that is an anionic surfactant; and (D) a fluorine-containing compound in an amount of 1001 ppm to 3000 ppm as the fluorine concentration,
It is a composition for oral cavity containing this.

  The composition for oral cavity of the present invention has improved aftertaste discomfort and has an excellent bactericidal action, but further promotes salivation, suppresses plaque adhesion, suppresses bad breath, improves the stability of the formulation, Effects such as optimization can be expected.

  Tranexamic acid or a salt thereof in the present invention is listed in, for example, the 17th revised Japanese Pharmacopoeia as tranexamic acid.

  As tranexamic acid, a free form or a salt of tranexamic acid may be used. Examples of “salts” of tranexamic acid include acid addition salts, alkali metal salts, alkaline earth metal salts, amine salts, and salts with amino acids.

Specific examples of the salt of tranexamic acid in the present invention include, for example, hydrohalides such as hydrofluoride, hydrochloride, hydrobromide, hydroiodide; nitrate, perchlorate, Inorganic acid salts such as sulfate and phosphate; lower alkane sulfonates such as methane sulfonate, trifluoromethane sulfonate and ethane sulfonate; aryl sulfones such as benzene sulfonate and p-toluene sulfonate Acid salts; organic acid salts such as acetate, malate, fumarate, succinate, citrate, ascorbate, tartrate, oxalate, maleate;
Alkali metal salts such as sodium salt and potassium salt; Alkaline earth metal salts such as calcium salt and magnesium salt; N-methylmorpholine salt, triethylamine salt, tributylamine salt, diisopropylethylamine salt, dicyclohexylamine salt, N-methylpiperidine salt Organic amine salts such as pyridine salt, 4-pyrrolidinopyridine salt, picoline salt; and
And salts with amino acids such as glycine salt, lysine salt, arginine salt, ornithine salt, glutamate and aspartate. In the present invention, tranexamic acid or a salt thereof is preferably tranexamic acid.

  The content of tranexamic acid or a salt thereof is preferably 0.001 to 0.5% by mass, more preferably 0.01 to 0.5% by mass, based on the total amount of the oral composition. Preferably it is 0.05-0.1 mass%, and is 0.05 mass% as an example.

The cationic fungicide in the present invention is preferably a quaternary ammonium salt type cationic fungicide.
Examples of the quaternary ammonium salt type cationic bactericides include cetylpyridinium chloride, benzethonium chloride, benzalkonium chloride, decalinium chloride, and the like, and these are compositions for oral use that are used alone or in combination of two or more. Can be blended. Of these, cetylpyridinium chloride is particularly preferred. Cetylpyridinium chloride is a cationic bactericidal agent contained in a quaternary ammonium compound, and is widely used in the field of oral compositions.

  The content of the cationic bactericidal agent is preferably 0.01 to 0.5% by mass, more preferably 0.01 to 0.3% by mass, and still more preferably based on the total amount of the oral composition. Is 0.01 to 0.1% by mass, particularly preferably 0.01 to 0.05% by mass, and as an example, 0.05% by mass.

  Examples of the bactericides that are anionic surfactants used in the present invention include lauroyl sarcosine sodium, and these can be used alone or in combination of two or more thereof in an oral composition. Among these, sodium lauroyl sarcosine is particularly preferable.

  The content of the bactericide that is an anionic surfactant is preferably 0.01 to 1.0% by mass, more preferably 0.05 to 1.0% by mass, based on the total amount of the oral composition. More preferably, it is 0.1-0.5 mass%, and is 0.3 mass% as an example.

  The fluorine-containing compound in the present invention is preferably a water-soluble fluorine-containing compound. A water-soluble fluorine-containing compound is a fluorine-containing compound that can be dissolved in 2 g or more in 100 g of water at 20 ° C. Examples of the fluorine-containing compound include sodium fluoride, potassium fluoride, ammonium fluoride, tin fluoride, amine fluoride, sodium monofluorophosphate, potassium monofluorophosphate, sodium silicon fluoride, calcium calcium fluoride, and the like. Preferably, sodium fluoride and sodium monofluorophosphate are used. One fluorine-containing compound may be used, or two or more fluorine-containing compounds may be used in combination.

  The fluorine-containing compound is used in an amount of 1001 ppm to 3000 ppm as the fluorine concentration. The fluorine concentration is preferably 1001 ppm to 2000 ppm, more preferably 1001 ppm to 1500 ppm. When the fluorine concentration is less than 1001 ppm, the bacterial inhibition rate may be insufficient, and when the fluorine concentration exceeds 3000 ppm, the effect of improving the uptake of fluorine may not be obtained.

  In the present invention, the content of each component in the oral composition is based on the charged amount of each component when producing the oral composition unless otherwise specified.

  In the oral cavity composition of the present invention, in addition to the above-described components, additive components that can be used in the oral cavity composition can be blended within a range that does not impair the effects of the present invention. Examples of the additive component include medicinal components, abrasives, binders, thickeners, surfactants, corrigents, preservatives, fragrances, colorants, pH adjusters, solvents, solubilizers, bases, and washings. An agent, an adsorbent, etc. are mentioned, and can be appropriately selected according to the dosage form. Although the specific example of an additional component is shown below, the component which can be mix | blended of this invention is not limited to these.

  As a medicinal component, a bactericidal agent, an anti-inflammatory agent, a blood circulation promoter, a calculus deposition inhibitor, a stain remover, a hypersensitivity inhibitor, a vitamin, a herbal extract, a plaque degrading enzyme, and the like can be blended. These medicinal ingredients are not particularly limited as long as they can be used for pharmaceuticals and the like.

  Examples of the disinfectant include isopropylmethylphenol, hinokitiol, chlorhexidine hydrochloride, alkyldiaminoethylglycine hydrochloride, triclosan and the like. These 1 type, or 2 or more types of combination can be selected suitably, and can be mix | blended as needed.

  Anti-inflammatory agents include β-glycyrrhetinic acid, glycyrrhetinic acid, glycyrrhizic acid, diammonium glycyrrhizinate, disodium glycyrrhizinate, trisodium glycyrrhizinate, dipotassium glycyrrhizinate, monoammonium glycyrrhizinate, ε-aminocaproic acid, azulene sulfonic acid Examples thereof include sodium hydrate, allantoin, allantoinchlorohydroxyaluminum, alcloxa, allantoindihydroxyaluminum, aldioxa, epidihydrocholesterin, dihydrocholesterol, lysozyme hydrochloride and the like. These 1 type, or 2 or more types of combination can be selected suitably, and can be mix | blended as needed.

  Examples of the blood circulation promoter include sodium chloride. These 1 type, or 2 or more types of combination can be selected suitably, and can be mix | blended as needed.

  As calculus deposition inhibitors, zeolite, disodium hydrogen phosphate, disodium dihydrogen pyrophosphate, sodium pyrophosphate, anhydrous sodium pyrophosphate, tetrasodium pyrophosphate (anhydrous), disodium monohydrogen phosphate, sodium hydrogen phosphate Hydrates, disodium hydrogen phosphate (crystal), trisodium phosphate, sodium polyphosphate and the like can be mentioned. These 1 type, or 2 or more types of combination can be selected suitably, and can be mix | blended as needed.

  As a stain remover, macrogoal (macrogoal 200, macrogoal 300, macrogoal 400, macrogoal 600, macrogoal 1000, macrogoal 1500, macrogoal 1540, macrogoal 4000, macrogoal 6000, macrogoal 20000, etc.) , Sodium polyphosphate, polyvinylpyrrolidone, and the like. These 1 type, or 2 or more types of combination can be selected suitably, and can be mix | blended as needed.

  Examples of the hypersensitivity inhibitor include potassium nitrate and aluminum lactate. These 1 type, or 2 or more types of combination can be selected suitably, and can be mix | blended as needed.

  As vitamins, ascorbic acid, L-ascorbic acid, sodium ascorbate, sodium L-ascorbate, pyridoxine hydrochloride, DL-α-tocopherol acetate, tocopherol acetate, dl-α-tocopherol nicotinate, tocopherol nicotinate Etc. These 1 type, or 2 or more types of combination can be selected suitably, and can be mix | blended as needed.

  Examples of the abrasive include silica-based abrasives such as silicic anhydride, silica (crystalline silica or amorphous silica), silica gel, aluminosilicate, zeolite, calcium hydrogen phosphate anhydrous, calcium hydrogen phosphate 2 water. Examples include Japanese, calcium pyrophosphate, calcium carbonate, aluminum hydroxide, alumina, magnesium carbonate, tertiary magnesium phosphate, zirconium silicate, tertiary calcium phosphate, hydroxyapatite, quaternary calcium phosphate, and synthetic resin-based abrasives. These 1 type, or 2 or more types of combination can be selected suitably, and can be mix | blended as needed.

  Examples of the binder include pullulan, gelatin, methyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, sodium carboxymethyl cellulose, carrageenan, sodium alginate, xanthan gum, sodium polyacrylate, gum arabic, guar gum, locust bean gum, polyvinyl alcohol, polyvinyl Examples thereof include organic binders such as pyrrolidone and carboxyvinyl polymer, and inorganic binders such as thickening silicic anhydride and bentonite. These 1 type, or 2 or more types of combination can be selected suitably, and can be mix | blended as needed.

  The thickener may be any commercially available raw material for pharmaceuticals, foods, and cosmetics. For example, polyhydric alcohol, more specifically sorbit, glycerin, concentrated glycerin, ethylene glycol, propylene glycol, 1,3- Examples include butylene glycol, propanediol (1,3-propanediol), polyethylene glycol, polypropylene glycol, xylit, maltite, lactit, trehalose, sodium hyaluronate, hydrolyzed collagen, and the like. These 1 type, or 2 or more types of combination can be selected suitably, and can be mix | blended as needed.

Examples of the surfactant include an anionic surfactant such as an N-acyl amino acid salt, an α-olefin sulfonate, an N-acyl sulfonate, an alkyl sulfate (for example, sodium lauryl sulfate), and a glycerin fatty acid ester. Examples thereof include sulfates.
Nonionic surfactants include, for example, polyoxyethylene alkyl ether, polyoxyethylene-polyoxypropylene block copolymer, polyoxyethylene hydrogenated castor oil, glycerin ester polyoxyethylene ether, sucrose fatty acid ester, alkylolamide, glycerin Examples include fatty acid esters.
Examples of amphoteric surfactants include alkyl betaine surfactants, amine oxide surfactants, and imidazolinium betaine surfactants. Specific examples thereof include 2-alkyl-N-carboxymethyl-N-hydroxyethyl imidazolinium betaine and coconut oil fatty acid amide alkyl betaine.

  Examples of the corrigent include, for example, sodium L-glutamate, saccharin, sodium saccharin, disodium glycyrrhizinate, trisodium glycyrrhizinate, sucrose, glucose, fructose, lactose, honey, aspartame, stevia, sucralose, xylitol, inositol, D-sorbitol , D-mannitol, arabitol, raffinose, lactulose, lactitol, erythritol, reduced palatinose, palatinose, palatinit, acesulfame K, maltose, maltosyl trehalose or maltitol, neohesperidin dihydrochalcone, perilartin, p-methoxycinnamic aldehyde, thaumatin, etc. Is mentioned. These 1 type, or 2 or more types of combinations can be selected suitably, and can be mix | blended.

  Examples of the preservative include, for example, sodium benzoate, methyl paraben, ethyl paraben, butyl paraben, isopropyl paraben, propyl paraben, isobutyl paraben, benzyl paraben and other paraoxybenzoic acid esters, phenoxyethanol, alcohols such as ethanol, sorbic acid, benzoic acid, etc. Examples include acid, dehydroacetic acid, propionic acid or salts thereof, ethylenediaminetetraacetate, benzalkonium chloride, alkyldiaminoethylglycine hydrochloride, and the like. These 1 type, or 2 or more types of combination can be selected suitably, and can be mix | blended as needed.

  Examples of the fragrance include L-menthol, peppermint, spearmint or fruit fragrance, mint oil and the like. The perfume also has the advantage of stimulating salivation. These 1 type, or 2 or more types of combinations can be selected suitably, and can be mix | blended.

  Examples of the colorant include natural pigments such as safflower red pigment, gardenia yellow pigment, gardenia blue pigment, perilla pigment, sockeye pigment, red cabbage pigment, carrot pigment, hibiscus pigment, cacao pigment, spirulina pigment, and coumarindo pigment. Red 3, No. 104, Red No. 105, Red No. 106, Yellow No. 4, Yellow No. 5, Green No. 3, Blue No. 1 and other legal dyes, riboflavin, copper chlorophyllin sodium, titanium dioxide and the like. These 1 type, or 2 or more types of combination can be selected suitably, and can be mix | blended as needed.

  Examples of the pH adjuster include acetic acid, hydrochloric acid, sulfuric acid, nitric acid, citric acid, phosphoric acid, malic acid, gluconic acid, maleic acid, succinic acid, glutamic acid, pyrophosphoric acid, tartaric acid, sodium acetate hydroxide, potassium hydroxide, Examples include acids, alkalis, and buffers such as sodium acetate, sodium carbonate, sodium citrate, sodium hydrogen citrate, phosphoric acid, sodium phosphate, sodium monohydrogen phosphate, sodium dihydrogen phosphate, potassium dihydrogen phosphate, and the like. These 1 type, or 2 or more types of combination can be selected suitably, and can be mix | blended as needed.

  Examples of the solvent include water and lower alcohols such as ethanol and propanol. These 1 type, or 2 or more types of combination can be selected suitably, and can be mix | blended as needed.

  A solubilizer may be added to promote the dissolution of the above-mentioned additives and medicinal ingredients in water. Examples of such a solubilizer include polyhydric alcohols such as propylene glycol, dipropylene glycol, butylene glycol, and polyethylene glycol. These 1 type, or 2 or more types of combinations can be selected suitably, and can be mix | blended.

  Examples of the base include sodium hydrogen carbonate. These 1 type, or 2 or more types of combinations can be selected suitably, and can be mix | blended.

  Examples of the cleaning agent include sodium polyphosphate. These 1 type, or 2 or more types of combinations can be selected suitably, and can be mix | blended.

  Examples of the adsorbent include β-cyclodextrin. These 1 type, or 2 or more types of combinations can be selected suitably, and can be mix | blended.

  In addition to the above-described components, the oral composition of the present invention can be appropriately mixed with components suitable for the use of the oral composition as long as the content of the present invention is not impaired.

The example of prescription of the composition for oral cavity of this invention is shown below.
In addition, components other than sodium fluoride, cetylpyridinium chloride, sodium lauroyl sarcosine and tranexamic acid are optional components, and the above optional components may or may not be included in the oral composition.
Sodium fluoride 0.11-0.31% by weight
Isopropylmethylphenol 0.02-0.1% by weight
Cetylpyridinium chloride 0.01-0.05% by weight
Lauroyl sarcosine sodium 0.1-0.5 wt%
Tranexamic acid 0.001-0.5 wt%
β-glycyrrhetinic acid 0.0063-0.2% by weight
Tocopherol acetate 0.05-1% by weight
Sodium chloride 0.5-20% by weight
Zeolite 0.5-20% by weight
Sodium bicarbonate 0.5-50% by weight
Macrogol 0.5-10% by weight
Concentrated glycerin 0.4-40% by weight
Polyoxyethylene hydrogenated castor oil 0.6-9% by weight
Paraben 0.02 to 2% by weight
Silica 0.1-10% by weight
Sodium lauryl sulfate 1-5% by weight
Sodium carboxymethylcellulose 0.5-5% by weight
Dipotassium glycyrrhizinate 0.01 to 0.22% by weight
Disodium hydrogen phosphate 0.01-5% by weight
1-15% by weight of propylene glycol
Sodium L-glutamate 0.01 to 0.1% by weight
Sodium citrate 0.01-1.2% by weight
Citric acid 0.02-0.3 wt%
Alkyldiaminoethylglycine hydrochloride 0.01-0.2% by weight
Xylitol 0.001-0.5% by weight
Saccharin sodium 0.001-0.01 wt%
2-Alkyl-N-carboxymethyl-N-hydroxyethylimidazolinium betaine 0.5-3 wt%
Sodium polyphosphate 0.7-2% by weight
Polyvinylpyrrolidone 0.01-1% by weight
1-10% by weight potassium nitrate
β-cyclodextrin 0.05-0.3 wt%
Perfume Appropriate amount Colorant Appropriate amount Purified water The remainder

The composition of the present invention can be formulated as an oral composition.
The present invention is used as pharmaceuticals, quasi drugs, cosmetics and the like.

  The form of this invention and the application method to an oral cavity are not specifically limited. For example, mouthwash (mouth wash), toothpaste (toothpaste, liquid toothpaste, toothpaste etc.), gum, troche, buccal tablet, gingival adhesive tape formulation, oral gel formulation, oral ointment, Oral spray, oral paste, oral paste, oral pill, oral tablet, oral powder, oral powder, oral liquid, oral suspension, oral cavity Examples thereof include emulsions for internal use, granules for oral use, capsules for oral use, and the like. A mouthwash (a mouthwash) or a toothpaste (a toothpaste, a liquid toothpaste or a toothpaste) is preferable.

  The present invention will be described more specifically with reference to the following examples, but the present invention is not limited by these examples.

[Test example]
(1) Test substance Cetylpyridinium chloride is from Merck, Tranexamic acid is from Daiichi Fine Chemical, sodium fluoride is from Nacalai Tesque, and lauryl sarcosine sodium is from Kawaken Fine Chemical. Were used respectively.

  An oral composition having the composition shown in Table 1 was prepared by a conventional method and evaluated by the following method. The results are shown in Table 1.

(2) Test method The sample contains about 4 mL of liquid oral composition, rinsed for 15 seconds, and then evaluated on a four-point basis for the discomfort of the aftertaste after mouthwash. , ◎, ○, △, ×.
The “uncomfortable feeling of aftertaste” is an uncomfortable feeling accompanied by an astringent feeling after mouthwashing, and is a feeling that the ingredients remain and give an unpleasant taste and feeling.
Four-level evaluation criteria:
4 points: There was no discomfort in the aftertaste.
3 points: There was almost no discomfort in the aftertaste.
2 points: There was a feeling of discomfort in the aftertaste.
1 point: Discomfort of aftertaste was strong.
Average point criteria:
◎: 3.5 points or more and 4.0 points or less ○: 3.0 points or more and less than 3.5 points △: 2.0 points or more and less than 2.5 points ×: Less than 2.0 points

Samples in the oral cavity are collected before and after the mouthwash using a cotton swab, and the number of bacteria is measured using a bacteria counter (product number: DU-AA01NP-H manufactured by Panasonic Healthcare). The inhibition rate of the bacteria after mouthwashing was calculated.
Criteria for inhibition rate (average value) of bacteria:
○: 30% or more Δ: 10% or more and less than 30% ×: less than 10%

(3) Test results

  From the results shown in Table 1, in the preparation (Example 1) in which lauryl sarcosine sodium as a fungicide which is an anionic surfactant and a high concentration of fluorine were added to a preparation containing cetylpyridinium chloride and tranexamic acid Thus, it was demonstrated that a feeling of discomfort in the aftertaste was improved and an oral composition having an excellent bactericidal effect was obtained. On the other hand, in Comparative Example 2 in which the fluorine concentration was lower than the range defined in the present invention, the bacterial inhibition rate was low. Moreover, in Comparative Example 1 and Comparative Example 3 in which lauroyl sarcosine sodium as a bactericide that is an anionic surfactant was not blended, the evaluation of the feeling of discomfort in the aftertaste was poor (Δ).

[Production example]
The following preparations are prepared in the usual manner described in the Japanese Pharmacopoeia General Rules for Semi-solid oral preparations and mouthwashes.
(Mouthwash)
A water-soluble component is dissolved in purified water, and a mixture prepared separately with a water-insoluble and oil-soluble component, a surface active component, and a compatible component is added thereto, and the mixture is uniformly mixed to prepare.
(Toothpaste)
A water-soluble component is dissolved in purified water, and a water-insoluble and oil-soluble component, a surface active component, and a mixture of insoluble components separately prepared, and an insoluble component are added thereto, and the mixture is uniformly mixed to prepare.

  Specific production examples are shown below. The content is expressed in% by weight.

<Production Example 1> (Mouth Wash)
Sodium fluoride 0.31
Isopropylmethylphenol 0.1
Cetylpyridinium chloride 0.05
Lauroyl sarcosine sodium 0.1
Tranexamic acid 0.5
Tocopherol acetate 0.1
Macrogol 0.5
Concentrated glycerin 0.4
Polyoxyethylene hydrogenated castor oil 9
Paraben 0.3
Dipotassium glycyrrhizinate 0.22
Disodium hydrogen phosphate 5
Propylene glycol 1
Sodium chloride 2.1
Sodium L-glutamate 0.1
Sodium citrate 1.2
Citric acid 0.02
Alkyldiaminoethylglycine hydrochloride 0.01
Xylitol 0.001
Saccharin sodium 0.001
Perfume Appropriate amount Colorant Appropriate amount Purified water The remainder

<Production Example 2> (Mouth Wash)
Sodium fluoride 0.31
Isopropylmethylphenol 0.02
Cetylpyridinium chloride 0.01
Lauroyl sarcosine sodium 0.5
Tranexamic acid 0.001
Tocopherol acetate 1
Macrogol 10
Concentrated glycerin 6
Polyoxyethylene hydrogenated castor oil 0.6
Paraben 0.02
Dipotassium glycyrrhizinate 0.01
Disodium hydrogen phosphate 0.01
Propylene glycol 15
Sodium chloride 0.02
Sodium L-glutamate 0.01
Sodium citrate 0.01
Citric acid 0.3
Alkyldiaminoethylglycine hydrochloride 0.2
Xylitol 0.5
Saccharin sodium 0.01
Peppermint oil 0.2
Perfume Appropriate amount Colorant Appropriate amount Purified water The remainder

<Production Example 3> (Dentifier)
Sodium fluoride 0.31
Isopropylmethylphenol 0.02
Cetylpyridinium chloride 0.03
Lauroyl sarcosine sodium 0.5
Tranexamic acid 0.003
β-glycyrrhetinic acid 0.04
Tocopherol acetate 0.06
Sodium chloride 5
Zeolite 0.9
Sodium bicarbonate 0.5
Macrogol 0.8
Concentrated glycerin 40
Polyoxyethylene hydrogenated castor oil 5
Paraben 2
Sodium carboxymethylcellulose 4
2-alkyl-N-carboxymethyl-N-hydroxyethylimidazolinium betaine 0.5
Sodium polyphosphate 2
Perfume Appropriate amount Colorant Appropriate amount Purified water The remainder

<Production Example 4> (Dentifrice)
Sodium fluoride 0.31
Isopropyl methylphenol 0.05
Cetylpyridinium chloride 0.01
Lauroyl sarcosine sodium 0.2
Tranexamic acid 0.05
β-glycyrrhetinic acid 0.15
Tocopherol acetate 0.5
Sodium chloride 15
Zeolite 10
Sodium bicarbonate 30
Macrogol 4
Concentrated glycerin 10
Polyoxyethylene hydrogenated castor oil 1
Paraben 0.1
Sodium carboxymethylcellulose 1
2-alkyl-N-carboxymethyl-N-hydroxyethylimidazolinium betaine 3
Sodium polyphosphate 0.7
Perfume Appropriate amount Colorant Appropriate amount Purified water The remainder

<Production Example 5> (Dentifier)
Sodium fluoride 0.31
Isopropylmethylphenol 0.06
Cetylpyridinium chloride 0.05
Lauroyl sarcosine sodium 0.1
Tranexamic acid 0.3
β-glycyrrhetinic acid 0.2
Tocopherol acetate 0.6
Sodium chloride 10
Zeolite 5
Sodium bicarbonate 10
Macrogol 6
Concentrated glycerin 25
Polyoxyethylene hydrogenated castor oil 5
Paraben 0.18
Silica 2
Sodium lauryl sulfate 1
Sodium carboxymethylcellulose 2
Perfume Appropriate amount Colorant Appropriate amount Purified water The remainder

<Production Example 6> (Dentifier)
Sodium fluoride 0.31
Isopropylmethylphenol 0.02
Cetylpyridinium chloride 0.02
Lauroyl sarcosine sodium 0.4
Tranexamic acid 0.001
β-glycyrrhetinic acid 0.15
Tocopherol acetate 1
Sodium chloride 8
Zeolite 0.9
Sodium bicarbonate 25
Macrogol 2
Concentrated glycerin 10
Polyoxyethylene hydrogenated castor oil 1
Paraben 0.2
Silica 9
Sodium lauryl sulfate 5
Sodium carboxymethylcellulose 3
Perfume Appropriate amount Colorant Appropriate amount Purified water The remainder

<Production Example 7> (Toothpaste)
Sodium fluoride 0.31
Isopropylmethylphenol 0.09
Cetylpyridinium chloride 0.04
Lauroyl sarcosine sodium 0.3
Tranexamic acid 0.4
β-glycyrrhetinic acid 0.01
Tocopherol acetate 0.08
Sodium chloride 20
Zeolite 1
Sodium bicarbonate 20
Macrogol 8
Concentrated glycerin 25
Polyoxyethylene hydrogenated castor oil 1
Paraben 0.15
Silica 1
Sodium lauryl sulfate 3
Sodium carboxymethylcellulose 1
β-cyclodextrin 0.05
Perfume Appropriate amount Colorant Appropriate amount Purified water The remainder

<Production Example 8> (Dentifier)
Sodium fluoride 0.31
Isopropylmethylphenol 0.1
Cetylpyridinium chloride 0.03
Lauroyl sarcosine sodium 0.1
Tranexamic acid 0.5
β-glycyrrhetinic acid 0.1
Tocopherol acetate 0.05
Sodium chloride 15
Zeolite 0.6
Sodium bicarbonate 45
Macrogol 4
Concentrated glycerin 15
Polyoxyethylene hydrogenated castor oil 2
Paraben 0.3
Silica 3
Sodium lauryl sulfate 2
Sodium carboxymethylcellulose 2
β-cyclodextrin 0.3
Peppermint oil 0.2
Perfume Appropriate amount Colorant Appropriate amount Purified water The remainder

<Production Example 9> (Dentifier)
Sodium fluoride 0.31
Isopropyl methylphenol 0.05
Cetylpyridinium chloride 0.01
Lauroyl sarcosine sodium 0.5
Tranexamic acid 0.03
β-glycyrrhetinic acid 0.09
Tocopherol acetate 0.9
Sodium chloride 0.5
Zeolite 5
Sodium bicarbonate 40
Macrogol 1
Concentrated glycerin 13
Polyoxyethylene hydrogenated castor oil 4
Paraben 0.05
Silica 2
Sodium lauryl sulfate 1
Sodium carboxymethylcellulose 0.5
Potassium nitrate 10
Perfume Appropriate amount Colorant Appropriate amount Purified water The remainder

<Manufacture example 10> (Dentifier)
Sodium fluoride 0.31
Isopropylmethylphenol 0.1
Cetylpyridinium chloride 0.03
Lauroyl sarcosine sodium 0.2
Tranexamic acid 0.15
β-glycyrrhetinic acid 0.07
Tocopherol acetate 0.6
Sodium chloride 7
Zeolite 0.5
Sodium bicarbonate 50
Macrogol 3
Concentrated glycerin 10
Polyoxyethylene hydrogenated castor oil 2
Paraben 0.1
Silica 10
Sodium lauryl sulfate 2.5
Sodium carboxymethylcellulose 2
Potassium nitrate 1
Perfume Appropriate amount Colorant Appropriate amount Purified water The remainder

<Production Example 11> (Toothpaste)
Sodium fluoride 0.31
Isopropylmethylphenol 0.07
Cetylpyridinium chloride 0.02
Lauroyl sarcosine sodium 0.1
Tranexamic acid 0.25
β-glycyrrhetinic acid 0.11
Tocopherol acetate 0.9
Sodium chloride 4
Zeolite 20
Sodium bicarbonate 15
Macrogol 7
Concentrated glycerin 5
Polyoxyethylene hydrogenated castor oil 5
Paraben 0.4
Silica 10
Sodium lauryl sulfate 3.2
Sodium carboxymethylcellulose 0.01
Polyvinylpyrrolidone 0.1
Perfume Appropriate amount Colorant Appropriate amount Purified water The remainder

<Production Example 12> (Dentifier)
Sodium fluoride 0.31
Isopropylmethylphenol 0.02
Cetylpyridinium chloride 0.01
Lauroyl sarcosine sodium 0.4
Tranexamic acid 0.4
β-glycyrrhetinic acid 0.19
Tocopherol acetate 0.05
Sodium chloride 18
Zeolite 2
Sodium bicarbonate 30
Macrogol 10
Concentrated glycerin 10
Polyoxyethylene hydrogenated castor oil 1
Paraben 0.2
Silica 7
Sodium lauryl sulfate 1.5
Sodium carboxymethylcellulose 0.03
Polyvinylpyrrolidone 0.4
Perfume Appropriate amount Colorant Appropriate amount Purified water The remainder

Claims (8)

(A) tranexamic acid or a salt thereof;
(B) a cationic fungicide;
(C) a bactericidal agent which is an anionic surfactant; and (D) a fluorine-containing compound in an amount of 1001 ppm to 3000 ppm as the fluorine concentration;
The composition for oral cavity containing this. The composition for oral cavity according to claim 1, wherein the cationic bactericidal agent is a quaternary ammonium salt type cationic bactericidal agent. The composition for oral cavity according to claim 1 or 2, wherein the cationic bactericidal agent is cetylpyridinium chloride. The composition for oral cavity according to any one of claims 1 to 3, wherein the content of the cationic fungicide is 0.01 to 0.5% by mass. The composition for oral cavity according to any one of claims 1 to 4, wherein the bactericide which is an anionic surfactant is sodium lauroyl sarcosine. The composition for oral cavity as described in any one of Claims 1-5 whose content of the bactericidal agent which is an anionic surfactant is 0.01-1.0 mass%. The composition for oral cavity according to any one of claims 1 to 6, wherein the content of tranexamic acid or a salt thereof is 0.001 to 0.5 mass%. The composition for oral cavity according to any one of claims 1 to 7, which is a mouthwash or a dentifrice.