JP2017214373A - Liquid oral composition - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a liquid oral composition that can effectively remove viscous substance such as saliva-derived protein and plaque to solve an intraoral sticky feeling, and has a good feeling in use, giving no bitterness at the time of use.SOLUTION: A liquid oral composition contains (A) a cationic germicide and (B) N-coconut oil fatty acid acyl-L-arginine ethyl DL-pyrrolidone carboxylic acid salt, with the content of component (A) of 0.02 mass% or less, and the content ratio of component (A) to component (B), (A)/(B), of 0.5-10.SELECTED DRAWING: None

Description

  The present invention relates to a liquid oral composition.

  Discomfort such as stickiness and bad breath in the oral cavity is attributed to bacteria and proteins in the oral cavity. In particular, the sticky sensation is thought to be due to proteins derived from saliva. Oral bacteria grow in the mouth and become plaques. Toothpaste is used to reduce oral discomfort and keep the oral cavity healthy because dirt in the oral cavity caused by saliva-derived protein and plaque and other viscous substances can cause dental caries and periodontal disease. Oral compositions such as mouthwashes are used.

  The composition for oral cavity contains a wide variety of components to impart functions according to various applications, and cationic surfactants that are hydrophilic are widely used because they exhibit various actions in the oral cavity. Has been. N-coconut oil fatty acid acyl-L-arginine ethyl DL-pyrrolidone carboxylate, which is a kind of cationic surfactant, has effects such as antibacterial activity and cleaning. An oral anti-periodontal disease endotoxin agent containing oil fatty acid acyl-L-arginine ethyl DL-pyrrolidone carboxylate has been proposed.

  It has also been proposed to improve the effect of the active ingredient by using a hydrophilic surfactant in combination with the active ingredient. For example, Patent Document 2 discloses a water-insoluble medicinal effect such as a water-insoluble vitamin. Oral composition containing an agent, a hydrophilic surfactant, and ethanol is disclosed, and examples of the hydrophilic surfactant include N-coconut oil fatty acid acyl-L-arginine ethyl DL-pyrrolidone carboxylate. ing.

  On the other hand, since cationic bactericides have high bactericidal activity against bacteria in the oral cavity, oral compositions containing such bactericides are widely used for the purpose of suppressing plaque that is a cause of caries and periodontal disease. It is used. For example, Patent Document 3 proposes an oral composition containing a cationic fungicide, a cationic polymer, and lauroyl glutamate and / or myristoyl glutamate.

JP2011-1387A Japanese Patent Laid-Open No. 4-5221 JP 2013-203676 A

  Viscous substances such as saliva-derived proteins and plaques that remain in the oral cavity are concentrated to increase the viscosity, which increases discomfort and makes removal difficult. A cationic surfactant and a cationic bactericidal agent are expected to have an effect of aggregating and removing viscous substances that also cause stickiness in the oral cavity by blending into the oral composition. However, in order to expect these effects in a liquid oral composition, a considerable amount of a cationic surfactant or a cationic bactericidal agent will be added, but the bitterness during use will increase and adversely affect the feeling of use. There was a problem of giving.

  The purpose of the present invention is to effectively remove viscous substances such as saliva-derived proteins and plaques to eliminate the sticky feeling in the oral cavity, and has almost no bitter taste during use, and a liquid oral cavity excellent in use feeling It is to provide a composition for use.

  As a result of intensive studies, the present inventors have found that in the liquid oral composition, the above problem can be solved by combining a cationic bactericide and a cationic surfactant in a specific ratio. The present invention has been completed.

That is, the present invention is achieved by the following (1) to (2).
(1) It contains (A) a cationic fungicide and (B) N-coconut oil fatty acid acyl-L-arginine ethyl DL-pyrrolidone carboxylate, and the content of the component (A) is 0.02% by mass. The composition for liquid oral cavity, wherein the content ratio of the component (A) to the component (B) ((A) / (B)) is 0.5 to 10.
(2) The composition for liquid oral cavity according to (1), wherein the cationic fungicide (A) is at least one of benzethonium chloride and cetylpyridinium chloride.

  The composition for liquid oral cavity of the present invention contains (A) a cationic fungicide and (B) N-coconut oil fatty acid acyl-L-arginine ethyl DL-pyrrolidone carboxylate as a cationic surfactant. By using these two components in combination at a specific content ratio, they can act synergistically to aggregate and insolubilize the viscous material enriched with saliva-derived proteins and the like. Thereby, the effect of removing the viscous substance in the oral cavity can be enhanced by mouth washing or the like, and the sticky feeling in the oral cavity can be removed. Moreover, there is no bitterness at the time of use, and the usability | use_condition in an intraoral area can be improved.

Hereinafter, embodiments of the present invention will be described in more detail.
The liquid oral cavity composition of the present invention comprises (A) a cationic bactericidal agent (hereinafter sometimes referred to as component (A)) and (B) N-coconut oil fatty acid acyl-L-arginine ethyl DL-pyrrolidonecarboxylic acid. Contains an acid salt (hereinafter also referred to as component (B)).

  Examples of the cationic fungicide of the present invention include benzethonium chloride, cetylpyridinium chloride, benzalkonium chloride, chlorhexidine hydrochloride, chlorhexidine gluconate, etc., and these may be used alone or in combination of two or more. You may use it in combination. Among these, from the viewpoint that aggregation and insolubilization of the above-mentioned viscous substances are promoted, the viscous substances in the oral cavity can be removed well, and that unpleasant feelings such as bitterness are suppressed during use, benzethonium chloride, chloride Cetylpyridinium is preferably used, and benzethonium chloride is more preferable.

  As content of a cationic disinfectant, it is preferable that it is 0.02 mass% or less in a composition for liquid oral cavity, and it is more preferable that it is the range of 0.005-0.02 mass%. When the content of the cationic fungicide is 0.02% by mass or less, bitterness can be sufficiently suppressed during use. In addition, the lower limit of the content of the cationic fungicide is not particularly limited, but in order to sufficiently obtain a synergistic effect with the N-coconut oil fatty acid acyl-L-arginine ethyl DL-pyrrolidone carboxylate of component (B). It is preferable to contain 0.005 mass% or more.

  The N-coconut oil fatty acid acyl-L-arginine ethyl DL-pyrrolidone carboxylate of the present invention is obtained from L-arginine, which is a kind of amino acid, coconut oil fatty acid, ethanol, and pyrrolidone carboxylic acid (PCA). Amino acid based cationic surfactant. As N-coconut oil fatty acid acyl-L-arginine ethyl DL-pyrrolidone carboxylate, commercially available products can be used, for example, “CAE” (trade name) manufactured by Ajinomoto Healthy Supply Co., Ltd. Can be used.

  The content of N-coconut oil fatty acid acyl-L-arginine ethyl / DL-pyrrolidone carboxylate is preferably 0.01% by mass or less in the liquid oral composition, 0.002 to 0.01 More preferably, it is in the range of mass%. When the content of N-coconut oil fatty acid acyl-L-arginine ethyl · DL-pyrrolidone carboxylate is 0.01% by mass or less, bitterness can be sufficiently suppressed during use. Further, the lower limit of the content of N-coconut oil fatty acid acyl-L-arginine ethyl DL-pyrrolidone carboxylate is not particularly limited, but in order to sufficiently obtain a synergistic effect with the cationic fungicide of component (A) It is preferable to contain 0.002 mass% or more.

In the present invention, by combining (A) a cationic fungicide and (B) N-coconut oil fatty acid acyl-L-arginine ethyl / DL-pyrrolidone carboxylate at a specific content ratio, such as a protein derived from saliva Although the mechanism by which the removal effect is improved is not clear, the component (A) and the component (B) act synergistically on different parts of the higher-order structure of the protein to facilitate denaturation of the protein. It is considered that the aggregation property of the protein is improved and the removal effect of the protein and the like is improved by mouth washing or the like.
Therefore, even if both component (A) and component (B) are used at a low concentration, they can exert a synergistic effect, and by reducing the amount of each component used, the bitterness can be suppressed during use in the oral cavity. A feeling can be improved.

  In the composition for liquid oral cavity of the present invention, (A) a cationic bactericide and (B) N-coconut oil fatty acid acyl-L-arginine ethyl DL-pyrrolidone carboxylate are components (A) with respect to component (B). The content ratio ((A) / (B)) is 0.5 to 10. When (A) / (B) is within the above range, a sufficient synergistic effect between component (A) and component (B) can be obtained.

  In addition, in this invention, content of a component (A) is 0.02 mass% or less, and content ratio ((A) / (B)) of the component (A) with respect to a component (B) is 0. It is shown as a suitable aspect to contain a component (A) and a component (B) in the range of 5-10.

  The liquid oral composition of the present invention can contain various components applicable to the oral cavity as long as the effects of the present invention are not impaired. For example, a solvent, a wetting agent, a sweetener, a bactericidal agent (cationic sterilization) Bactericides other than agents), surfactants (surfactants other than N-coconut oil fatty acid acyl-L-arginine ethyl / DL-pyrrolidone carboxylate), pH adjusters, enzymes, ion sources, preservatives, perfumes, Examples include crude drugs and pigments.

  Examples of the solvent include purified water, water such as ionic water, alcohol such as ethanol, and the like.

  Examples of the wetting agent include glycerin, ethylene glycol, propylene glycol, 1,3-butylene glycol, polyethylene glycol, and polypropylene glycol.

  Examples of the sweetener include steviaside, xylitol, erythritol, maltitol, sorbitol, sodium saccharin, sucralose, reduced palatinose, aspartame and the like.

  Examples of the bactericides other than the cationic bactericides include triclosan, isopropylmethylphenol, hinokitiol, thymol, alkyldiaminoethylglycine hydrochloride and the like.

  Examples of the surfactant include nonionic surfactants, cationic surfactants, anionic surfactants, and amphoteric surfactants. Specifically, nonionic surfactants include glycerin fatty acid ester, ester surfactant, and surfactant. Sugar fatty acid ester, sorbitan fatty acid ester, polyoxyethylene fatty acid ester, polyoxyethylene sorbitan fatty acid ester, fatty acid diethanolamide, fatty acid monoglyceride, polyoxyethylene alkyl ether, polyoxyethylene hydrogenated castor oil, alkyl glucoside, polyoxyethylene polyoxypropylene Examples of the cationic surfactant include alkyltrimethylammonium chloride and dialkyldimethylammonium chloride. Examples of the anionic surfactant include sulfuric acid ester. Ter salts, α-olefin sulfonates, sulfosuccinates, N-acyl amino acid salts, acylated methyl taurate salts, and the like. Examples of amphoteric surfactants include betaine acetate type activators and imidazoline type activators. It is done.

  Examples of the pH adjuster include monosodium phosphate, disodium phosphate, sodium citrate, citric acid, glucono-δ-lactone, sodium gluconate, sodium acetate, and hydrates thereof.

  Examples of the enzyme include protease, dextranase, amylase, mutanase, lysozyme and the like.

  Examples of the ion source include fluorine ion sources such as sodium fluoride, monofluorophosphate and stannous fluoride, and phosphate ion sources such as calcium phosphate and hydroxyapatite.

  Examples of the preservative include parahydroxybenzoic acid ester, sodium benzoate, phenoxyethanol and the like.

  Examples of the fragrances include peppermint oil, spearmint oil, peppermint oil, eucalyptus oil, clove oil, thyme oil, rosemary oil and other natural essential oils, l-menthol, l-carvone, carvacrol, eugenol, anethole, 1,8 -Fragrance | flavor components, such as cineol, hinokitiol, and thymol, these mixtures, a natural fragrance | flavor, a compound fragrance | flavor, a synthetic fragrance | flavor, etc. are mentioned.

  Examples of herbal medicines include a buckwheat extract, a sugar beet extract, a carrot extract, and a fennel extract.

  Examples of the dye include Blue No. 1, Yellow No. 4, Yellow No. 5, Yellow No. 202 (1), Red No. 102, Green No. 3, Green No. 201, and the like.

  The liquid oral cavity composition of the present invention can be used in the form of mouthwash, liquid toothpaste, mouth freshener, mouthwash (gargle). These can be made into preparations by known means.

  For example, in order to obtain a mouthwash, water, ethanol or the like may be used as a solvent, and various components may be added and prepared by a conventional method. For example, the mouthwash can be prepared by sequentially mixing the components under stirring.

  In the liquid oral cavity composition of the present invention, when the pH is adjusted to 5 to 10 with a pH adjuster or the like, the usability in the oral cavity can be improved. Furthermore, it is preferable that the amount of ethanol used is in the range of 25% by mass or less, preferably 10% by mass or less, based on the total amount of the mouthwash, since irritation in the oral cavity can be suppressed. Moreover, when applying the composition for liquid oral cavity of the present invention to the oral cavity as a mouthwash, the liquid oral composition of the present invention is used by rinsing in the oral cavity for about 15 to 60 seconds, for example. It can be sufficiently spread in the oral cavity.

  EXAMPLES Hereinafter, although an Example and a comparative example demonstrate this invention further, this invention is not restrict | limited to the following example.

<Test Example 1>
(Preparation of liquid oral composition)
In purified water, benzethonium chloride (BTC) and / or N-coconut oil fatty acid acyl-L-arginine ethyl DL-pyrrolidone carboxylate (“CAE” (trade name) manufactured by Ajinomoto Healthy Supply Co., Ltd.) is shown in Table 1. Were added and stirred to prepare specimens 1 to 16. Samples 1 to 10 are comparative examples, and samples 11 to 16 are examples.

(Measurement of mucin removal rate)
The mucin removal rate as a viscous substance was measured by the following procedure.
(1) Mucin (manufactured by Koken Co., Ltd. “Marine Mucin 1%” (trade name)), water and blue No. 1 0.1% aqueous solution are mixed at a volume ratio of 5: 9: 1 to prepare a total 60 ml of mucin solution. did.
(2) 400 μL of the specimen prepared above and 400 μL of the mucin solution were placed in a 1.5 mL microtube, and mixed with a vortex mixer for 15 seconds.
(3) Thereafter, the mixture was centrifuged at 10,000 rpm for 3 minutes to precipitate aggregates.
(4) 200 μL of the supernatant was placed in a 96-well microplate, and the absorbance at a wavelength of 630 nm was measured. Moreover, the light absorbency at the time of using purified water instead of the specimen as a blank (control) was measured.
(5) The mucin removal rate was calculated by the following formula.
Mucin removal rate (%) = (1−absorbance of specimen / absorbance of control) × 100

The test was performed 3 times, and the average value was obtained. The results are shown in Table 1.
In addition, the higher the mucin removal rate (%), the more the aggregation and insolubilization of the viscous substance is promoted, and the viscous substance in the oral cavity can be removed well.

<Test Example 2>
(Preparation of liquid oral composition)
In accordance with the formulation shown in Table 2, each component was mixed with stirring to prepare specimens 17 to 23. The configurations of BTC and CAE in the sample 17 correspond to the sample 2 in Test Example 1, and the samples 18 to 23 correspond to the samples 3, 4, 7, 8, 11, and 14, respectively. Samples 17 to 21 are comparative examples, and samples 22 and 23 are examples.

(Sensory evaluation test)
Fifteen panelists (8 healthy adult males and 7 healthy adult females) determined the feeling of use (bitterness) when the sample was contained in the mouth according to the following evaluation criteria, and determined the average. The results are shown in Table 2.
〔Evaluation criteria〕
3 points: No bitterness.
2 points: I feel a little bitter.
1 point: A bitter taste is felt, but there is no problem in use.
0 point: Strong bitterness and cannot be used.

  From the results in Table 1, specimens 11 to 16 containing (A) a cationic fungicide (BTC) and (B) N-coconut oil fatty acid acyl-L-arginine ethyl DL-pyrrolidone carboxylate (CAE), Despite the low concentrations of component (A) and component (B), the mucin removal rate (%) is higher than when they are used alone, and both act synergistically. Specifically, for example, the sample 15 is an example in which the sample 5 (component (A) alone) and the sample 8 (component (B) alone) are combined, but the sample 5 has a mucin removal rate (average) of 1.6. The specimen 8 had a mucin removal rate (average) of 5.7%, while the specimen 15 had a mucin removal ratio (average) of 30.4%. Therefore, even when the component (A) and the component (B) are at low concentrations, it is clear that the combined use of both of them can sufficiently remove mucinous substances in the oral cavity by obtaining a synergistic effect of mucin removal. It was. Further, from the results of Table 2, it is clear that the specimens 22 and 23 which are examples of the present invention have a sensory evaluation result of 1.5 or more, the bitterness during use is sufficiently suppressed, and the feeling of use is excellent. It was.

Claims (2)

(A) a cationic fungicide and (B) N-coconut oil fatty acid acyl-L-arginine ethyl DL-pyrrolidone carboxylate,
Content of the said component (A) is 0.02 mass% or less, and content ratio ((A) / (B)) of the said component (A) with respect to the said component (B) is 0.5-10. A liquid oral composition characterized by being. 2. The liquid oral composition according to claim 1, wherein the cationic germicide (A) is at least one of benzethonium chloride and cetylpyridinium chloride.