Oral composition

Abstract

To provide an oral composition containing laurylpyridinium chloride with reduced stimulation and astringency.SOLUTION: An oral composition comprises: (A) laurylpyridinium chloride; and (B) an alkali metal salt of acetic acid, wherein a content of (A) is 0.03 to 5 pts.mass based on 1 pt.mass of (B).SELECTED DRAWING: None

Description

Technical Field

[0001] The present disclosure relates to oral compositions and the like. Specifically, it relates to oral compositions and the like containing (A) laurylpyridinium chloride and (B) an alkali metal acetate.

Background Art

[0002] Among the quaternary ammonium salts that are bactericides, cetylpyridinium chloride (also referred to as "CPC") has high bactericidal activity against the causative bacteria of periodontal disease and has been widely used in oral compositions. However, CPC has bitterness and irritation, which has been a problem when formulating it into oral compositions. Therefore, conventionally, methods for improving the usability with various additives have been developed to reduce the bitterness or irritation derived from CPC (Patent Documents 1 to 6).

[0003] Patent Document 1 describes a method of blending l-menthol, chlorobutanol, etc. to improve the bitterness of cationic bactericides such as CPC.

[0004] Patent Document 2 describes a method of suppressing the bitterness of CPC and improving the usability by blending low concentrations of ethyl maltol and l-menthol in a liquid oral composition.

[0005] Patent Document 3 describes a method of improving the bitterness etc. of CPC by blending anethole, eugenol, linalool, and menthol at a predetermined concentration.

[0006] Patent Document 4 describes a method of improving the discomfort of the aftertaste caused by CPC by blending specific plant extracts such as Nigaki and hops.

[0007] Patent Document 5 describes a method of improving the bitterness and irritation of cationic bactericides such as CPC by a combination of high-sweetness sweeteners and specific fragrance components.

[0008] Patent Document 6 describes a method for improving the specific bitterness and irritation of CPC by blending limonene, polyoxyethylene hydrogenated castor oil, propylene glycol, and xylitol at predetermined concentrations.

[0009] On the other hand, recent research has shown that for the prevention of periodontal disease, it is important to suppress the formation of plaque, which is the cause of periodontal disease, and laurylpyridinium chloride (also referred to as "dodecylpyridinium chloride" or "DPC") is effective in killing Fusobacterium, which contributes to plaque formation by coaggregating with various bacteria (Patent Document 7). However, DPC has a stronger irritation compared to CPC and also has a specific astringency, so there are still problems in the usability with the conventional methods for reducing the bitterness or irritation of CPC, which has been a drawback in product development.

[0010] In recent years, methods have been developed to improve the strong bitterness that occurs when CPC and DPC are used in combination by blending methyl paraben, sodium saccharin, menthol, etc. (Patent Documents 8 and 9).

Prior Art Documents

Patent Documents

[0011]

Patent Document 1

Patent Document 2

Patent Document 3

Patent Document 4

Patent Document 5

Patent Document 6

Patent Document 7

Patent Document 8

[0012] [Non-Patent Document 1] Alternative Mechanisms of Astringency - What is the Role of Saliva?(DOI:https: / / doi.org / 10.1111 / jtxs.12022) [Summary of the Invention] [Problems to be Solved by the Invention]

[0013] An object of the present invention is to provide an oral composition containing laurylpyridinium chloride with reduced irritation and astringency. [Means for Solving the Problems]

[0014] The present inventors have found that by blending (A) laurylpyridinium chloride and (B) an alkali metal acetate in a specific ratio, the irritation and astringency of DPC are reduced, and further improvements have been made.

[0015] The present disclosure includes, for example, the subject matter described in the following items. Item 1. (A) Laurylpyridinium chloride, and (B) an alkali metal acetate, and an oral composition containing 0.03 to 5 parts by mass of (A) with respect to 1 part by mass of (B). Item 2. The oral composition according to Item 1, wherein the content of (A) in the oral composition is 0.01 to 0.5% by mass. Item 3. The oral composition according to Item 1 or 2, wherein the content of (B) in the oral composition is 0.005 to 1.0% by mass. Item 4. (B) The alkali metal acetate is sodium acetate, and the composition according to any one of items 1 to 3.

Advantages of the Invention

[0016] There is provided an oral composition containing laurylpyridinium chloride with reduced irritation and astringency.

Modes for Carrying Out the Invention

[0017] Hereinafter, each embodiment included in the present disclosure will be described in more detail. The oral composition included in the present disclosure contains (A) laurylpyridinium chloride and (B) an alkali metal acetate. In this specification, the oral composition may be referred to as "the oral composition of the present disclosure". Further, each component of (A) and (B) may be referred to as "(A) component", "(B) component", etc.

[0018] Examples of the (B) alkali metal acetate include sodium acetate, potassium acetate, etc. The alkali metal acetate can be blended alone or in combination of two or more. Among them, sodium acetate is preferred.

[0019] In the oral composition of the present disclosure, the content of (A) laurylpyridinium chloride is preferably about 0.03 to 5 parts by mass with respect to 1 part by mass of the (B) alkali metal acetate. The upper or lower limit of the range may be, for example, about 0.04, 0.05, 0.06, 0.07, 0.08, 0.09, 0.1, 0.11, 0.12, 0.13, 0.14, 0.15, 0.16, 0.17, 0.18, 0.19, 0.2, 0.25, 0.3, 0.35, 0.4, 0.45, 0.5, 0.55, 0.6, 0.65, 0.7, 0.75, 0.8, 0.85, 0.9, 0.95, 1, 1.5, 2, 2.5, 3, or 4 parts by mass. More specifically, it may be about 0.04 to 4 parts by mass.

[0020] In the oral composition of the present disclosure, it is preferable to contain (A) laurylpyridinium chloride in an amount of about 0.01 to 0.5% by mass. The upper or lower limit of the range may be, for example, about 0.02, 0.03, 0.04, 0.05, 0.06, 0.07, 0.08, 0.09, 0.1, 0.11, 0.12, 0.13, 0.14, 0.15, 0.2, 0.25, 0.3, 0.35, 0.4, or 0.45% by mass. More specifically, it may be about 0.02 to 0.45% by mass.

[0021] In the oral composition of the present disclosure, it is preferable to contain (B) alkali metal acetate in an amount of about 0.005 to 1.0% by mass. The upper or lower limit of the range may be, for example, about 0.01, 0.02, 0.03, 0.04, 0.05, 0.06, 0.07, 0.08, 0.09, 0.1, 0.11, 0.12, 0.13, 0.14, 0.15, 0.2, 0.25, 0.3, 0.35, 0.4, 0.45, 0.5, 0.6, 0.7, 0.8, or 0.9% by mass. More specifically, it may be about 0.01 to 0.9% by mass, or about 0.05 to 0.5% by mass.

[0022] The composition of the present disclosure can be, for example, a solid composition, a liquid composition, etc. Among them, a liquid composition is preferable.

[0023] In addition, the oral composition of the present disclosure can also be used, for example, as a pharmaceutical, quasi-drug, or cosmetic. The form of the oral composition of the present disclosure is not particularly limited, but can be, for example, in the form of an ointment, paste, pasta, gel, liquid, spray, mouthwash, liquid dentifrice, dentifrice paste, coating agent, etc. (dosage form).

[0024] In the oral composition of the present disclosure, in addition to (A) laurylpyridinium chloride and (B) alkali metal acetate, optional components that can be incorporated into the oral composition without impairing the effects of the present invention may be further incorporated alone or in combination of two or more. Examples of the optional components include surfactants, fragrances, sweeteners, binders, wetting agents, preservatives, coloring agents, pH adjusters, medicinal components, bases, abrasives, stabilizers, etc.

[0025] As the surfactant, for example, a nonionic surfactant, an anionic surfactant, or an amphoteric surfactant can be blended. Specifically, examples of the nonionic surfactant include sugar fatty acid esters such as sucrose fatty acid ester, maltose fatty acid ester, lactose fatty acid ester; fatty acid alkanolamides; glycerin fatty acid esters; sorbitan fatty acid esters; fatty acid monoglycerides; polyoxyethylene alkyl ethers with a polyoxyethylene addition coefficient of 8 to 10 and an alkyl group having 13 to 15 carbon atoms; polyoxyethylene alkyl phenyl ethers with a polyoxyethylene addition coefficient of 10 to 18 and an alkyl group having 9 carbon atoms; diethyl sebacate; polyoxyethylene hydrogenated castor oil; fatty acid polyoxyethylene sorbitan, alkyl glucosides having 8 to 16 carbon atoms in the alkyl group, etc. Examples of the anionic surfactant include sulfate esters such as sodium lauryl sulfate, sodium polyoxyethylene lauryl ether sulfate; sulfosuccinates such as sodium lauryl sulfosuccinate, sodium polyoxyethylene lauryl ether sulfosuccinate; acyl amino acid salts such as sodium cocoyl sarcosinate, sodium lauroyl methyl alaninate; sodium cocoyl methyl taurine, etc. Examples of the amphoteric ion surfactant include betaine type surfactants such as lauryldimethylaminoacetic acid betaine, coconut oil fatty acid amidopropyldimethylaminoacetic acid betaine; imidazoline type surfactants such as N-cocoyl-N-carboxymethyl-N-hydroxyethyl ethylenediamine sodium; amino acid type surfactants such as N-lauryl diaminoethyl glycine, etc. Also preferably exemplified are coconut oil fatty acid monoethanolamide, coconut oil fatty acid diethanolamide, coconut oil fatty acid amide betaine, coconut oil fatty acid amidopropyl betaine, and N-coconut oil fatty acid acyl L-arginine ethyl dl-pyrrolidone carboxylate, etc. These surfactants can be blended alone or in combination of two or more. The blending amount is usually about 0.1 to 5% by mass based on the total amount of the composition.

[0026] As spices, for example, menthol, carboxylic acid, anethole, eugenol, methyl salicylate, limonene, ocimene, n-decyl alcohol, citronellol, α-terpineol, methyl acetate, citronellyl acetate, methyl eugenol, cineol, linalool, ethyl linalool, thymol, spearmint oil, peppermint oil, lemon oil, orange oil, sage oil, rosemary oil, perilla oil, wintergreen oil, clove oil, eucalyptus oil, pimento oil, d-camphor, d-borneol, star anise oil, cinnamon oil, cinnamaldehyde, mint oil, vanillin, ethyl vanillin, maltol, ethyl maltol, lactones having 6 to 12 carbon atoms, caryophyllene, germacrene, viridiflorol, etc. can be used. These can be used alone or in combination of two or more. Also, these can be blended in an amount of, for example, about 0.001 to 1.5% by mass based on the total amount of the composition.

[0027] As sweeteners, for example, sodium saccharin, acesulfame potassium, stevioside; stevia sweeteners such as rebaudioside, sucralose, neohesperidin dihydrochalcone, perillartine, thaumatin, aspartyl phenylalanyl methyl ester, p-methoxycinnamic aldehyde, glycyrrhizin and other licorice sweeteners can be blended. These can be used alone or in combination of two or more. Also, these can be blended in an amount of, for example, about 0.001 to 1% by mass based on the total amount of the composition.

[0028] Examples of the binder include cellulose derivatives such as sodium carboxymethyl cellulose, carboxymethyl ethyl cellulose salt, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, etc.; microbial-produced polymers such as xanthan gum and gellan gum; natural polymers or natural rubbers such as tragacanth gum, karaya gum, gum arabic, carrageenan, dextrin, etc.; synthetic polymers such as polyvinyl alcohol and polyvinyl pyrrolidone; inorganic binders such as thickening silica and beegum; and cationic binders such as O-[2-hydroxy-3-(trimethylammonio)propyl] hydroxyethyl cellulose chloride. These can be used alone or in combination of two or more.

[0029] Examples of the wetting agent include sorbitol, glycerin, propylene glycol, xylitol, maltitol, lactitol, polyoxyethylene glycol, etc. These can be blended alone or in combination of two or more. Also, they can be blended in an amount of about 5 to 20% by mass based on the total amount of the composition.

[0030] Examples of the preservative include parabens such as methylparaben, ethylparaben, propylparaben, butylparaben, etc.; sodium benzoate, phenoxyethanol, alkyl diminoethyl glycine hydrochloride, chlorobutanol, etc. These can be blended alone or in combination of two or more.

[0031] Examples of the colorant include legal dyes such as Blue No. 1, Yellow No. 4, Red No. 202, Green No. 3, etc.; mineral dyes such as ultramarine, reinforced ultramarine, dark blue, etc.; titanium oxide, etc. These can be blended alone or in combination of two or more.

[0032] Examples of the pH adjuster include citric acid, phosphoric acid, malic acid, pyrophosphoric acid, lactic acid, tartaric acid, glycerophosphoric acid, acetic acid, nitric acid, or chemically possible salts thereof, sodium hydroxide, etc. These can be blended alone or in combination of two or more so that the pH of the composition is in the range of, for example, 4 to 9. The blending amount of the pH adjuster is exemplified by about 0.01 to 2% by weight.

[0033] As the medicinal ingredient, a bactericide other than lauryl pyridinium chloride may be blended. For example, cationic bactericides such as cetyl pyridinium chloride, benzalkonium chloride, benzethonium chloride, chlorhexidine hydrochloride, chlorhexidine gluconate, etc., amphoteric bactericides such as dodecyldiaminoethyl glycine, nonionic bactericides such as triclosan, isopropylmethylphenol, hinokitiol, etc. may be mentioned. Furthermore, medicinal ingredients other than bactericides can also be blended. For example, vitamin E compounds such as aluminum lactate, potassium nitrate, dl-α-tocopherol acetate, succinic acid tocopherol, or tocopherol nicotinate, sodium fluoride, glycyrrhizinate, etc. may be blended. The medicinal ingredients can be blended alone or in combination of two or more kinds.

[0034] As the base, for example, alcohols, silicon, apatite, white petrolatum, paraffin, liquid paraffin, microcrystalline wax, squalane, plastic base, etc. can be blended alone or in combination of two or more kinds.

[0035] As the abrasive, for example, calcium carbonate, magnesium carbonate, dibasic calcium phosphate, tribasic calcium phosphate, magnesium phosphate, silica, zeolite, sodium metaphosphate, aluminum hydroxide, magnesium hydroxide, calcium pyrophosphate, bengala, calcium sulfate, anhydrous silicic acid, etc. can be blended alone or in combination of two or more kinds.

[0036] As the stabilizer, for example, sodium edetate, sodium thiosulfate, sodium sulfite, calcium lactate, lanolin, triacetin, castor oil, magnesium sulfate, etc. can be blended alone or in combination of two or more kinds.

[0037] In addition, the oral composition of the present disclosure may contain extracts of plants such as loquat leaf, hops, almond, Japanese mugwort, gentiana, and Chinese cork tree. Furthermore, it may contain quassin, iso-alpha acids, tuyonin, gentiopicroside, berberine, etc., which are these bitter components. As the above plant extract or its bitter component, those obtained by extracting raw material plants by adopting an ordinary method using an appropriate extraction solvent such as water, ethanol, etc. can be used. Commercially available products such as extracts, oils, and extracts may be used. Alternatively, synthetic products can also be used.

[0038] The oral composition of the present disclosure can be produced by a known method or a method easily conceivable from a known method. For example, it can be prepared by appropriately mixing (A) laurylpyridinium chloride, (B) an alkali metal acetate, and other components as necessary.

[0039] In this specification, "astringency" refers to a sensation perceived by a chemical response with receptors present in the oral mucosal epithelium or by friction generated by a decrease in the lubricity of the oral mucosal epithelium (Non-Patent Document 1). Note that "astringency" is a sensation of a different nature from "bitterness" perceived by a response with bitter receptors present in taste buds.

[0040] In this specification, "comprising" includes "consisting essentially of" and "consisting of." Also, the present disclosure includes all combinations of any of the constituent elements described in this specification.

[0041] In addition, the various characteristics (properties, structures, functions, etc.) described for each of the above-described embodiments of the present disclosure may be combined in any manner in identifying the subject matter encompassed by the present disclosure. That is, the present disclosure includes all subject matters consisting of any combination of the combinable characteristics described in this specification.

Examples

[0042] The content of the present disclosure will be specifically described using the following examples. However, the present disclosure is not limited thereto in any way. In the following, unless otherwise specified, the experiments are carried out under atmospheric pressure and normal temperature conditions. Also, unless otherwise specified, "%" means "% by mass". Further, the blending amount values of each component described in each table indicate "% by mass" unless otherwise specified.

[0043] <Sensory evaluation> Liquid oral compositions were prepared by a conventional method with the blending amounts shown in Tables 1 and 2.

[0044] [Table 1]

[0045] [Table 2]

[0046] Four monitors were each asked to hold 10 mL of the prepared liquid oral composition in their mouths and use it for 20 seconds, and the irritation, astringency, irritation and astringency 1 minute after use, and acetic acid odor during use were evaluated according to a five-point evaluation criterion. <Evaluation criteria: irritation, astringency, acetic acid odor> 5: Feel very strongly 4: Feel strongly 3: Feel 2: Hardly feel 1: Don't feel at all

[0047] The evaluation values of the four people were aggregated and the average value was calculated. The results are shown together with Table 2. ◎: Average score less than 2.0 〇: Average score of 2.0 or more and less than 3.0 ×: Average score of 3.0 or more and less than 4.0 ××: Average score of 4.0 or more

[0048] As shown in Table 2, it was confirmed that by blending lauryl pyridinium chloride and sodium acetate in a specific ratio, the irritation and astringency during use and 1 minute after use were reduced.

[0049] Formulation examples are shown below.

[0050] [Table 3]

[0051] [Table 4]

[0052] [Table 5]

[0053] [Table 6]

[0054] [Table 7]

[0055] [Table 8]

[0056] [Table 9]

[0057] [Table 10]

[0058] [Table 11]

Claims

1. (A) Laurylpyridinium chloride, and (B) an alkali metal acetate, and an oral composition containing 0.03 to 5 parts by mass of (A) with respect to 1 part by mass of (B).

2. The oral composition according to claim 1, wherein the content of (A) in the oral composition is 0.01 to 0.5% by mass.

3. The oral composition according to claim 1 or 2, wherein the content of (B) in the oral composition is 0.005 to 1.0% by mass.

4. The composition according to claim 1 or 2, wherein the alkali metal acetate (B) is sodium acetate.

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