Liquid oral components

Abstract

To provide a liquid composition for oral cavity having a good feeling of use which is not impaired by the sweetness of a sweetener while suppressing the bitterness of laurylpyridinium chloride and cetylpyridinium chloride.SOLUTION: A liquid composition for oral cavity contains 0.01 mass% to 0.1 mass% of (A) cetylpyridinium chloride, 0.01 mass% to 0.1 mass% of (B) laurylpyridinium chloride, 0.05 mass% to 0.2 mass% of (C) methylparaben, 0.002 mass% to 0.02 mass% of (D) saccharin sodium, 0.01 mass% or more of (E) menthol, and 0.002 mass% to 0.02 mass% of (F) a stevia sweetener.SELECTED DRAWING: None

Description

Technical Field

[0001] The present invention relates to improving the usability of liquid oral compositions.

Background Art

[0002] Oral compositions for the purpose of preventing oral troubles such as periodontal diseases are formulated with bactericides, medicinal components, and other components that exhibit useful effects. However, a decrease in usability often occurs due to bitterness specific to each component. Unlike pharmaceuticals, general quasi-drug oral compositions do not improve symptoms with a few uses and require continuous use for the purpose of preventing oral troubles. Therefore, in order to maintain the motivation for continuous use, an oral composition with good usability during and after use is desired.

[0003] Among quaternary ammonium salts that are bactericides, cetylpyridinium chloride has high bactericidal power against the causative bacteria of periodontal diseases and has been widely used in oral compositions. Recent research has revealed that in the prevention of periodontal diseases, it is important to suppress the formation of plaque that causes periodontal diseases, and laurylpyridinium chloride is effective in killing Fusobacterium that contributes to plaque formation by coaggregating with various bacteria (Patent Document 1).

[0004] Hitherto, methods of adding various additives to reduce bitterness and the like during and after use of oral compositions containing cetylpyridinium chloride and improve usability have been known. Patent Document 2 describes a method of blending l-menthol and anethole, which are flavor components, in a predetermined concentration in an oral composition to improve bitterness and the like of cationic bactericides.

Prior Art Documents

Patent Documents

[0005]

Patent Document 1

Patent Document 2

[0006] Laurylpyridinium chloride has a stronger bitter taste than cetylpyridinium chloride, and using them together further reduces the usability of the liquid oral composition compared to using cetylpyridinium chloride alone. The objective is to provide a liquid oral composition that suppresses this bitterness while maintaining a good usability due to the sweetness derived from sweeteners. [Means for solving the problem]

[0007] In view of the above problems, the inventors diligently conducted research and, surprisingly, discovered that by adding appropriate amounts of methyl parahydroxybenzoate, sodium saccharin, menthol, and a stevia-based sweetener to a liquid oral composition containing cetylpyridinium chloride and laurylpyridinium chloride, a high level of usability can be obtained while suppressing the bitterness derived from the disinfectant.

[0008] The present invention encompasses, for example, the inventions described below. Section 1. (A) Cetylpyridinium chloride in a concentration of 0.01 to 0.1% by mass. (B) 0.01 to 0.1% by mass of laurylpyridinium chloride (C) Methyl parahydroxybenzoate in an amount of 0.05 to 0.2% by mass, (D) Sodium saccharin in a concentration of 0.002 to 0.02% by mass. (E) Menthol in an amount of 0.01% by mass or more, (F) A liquid oral composition containing 0.002 to 0.02% by mass of a stevia-based sweetener. Section 2. The above (A) contains cetylpyridinium chloride in an amount of 0.03 to 0.07%, The content of (B) laurylpyridinium chloride is 0.03 to 0.07% by mass. The above (C) contains methyl parahydroxybenzoate in an amount of 0.1 to 0.15% by mass. The content of (D) saccharin sodium is 0.005 to 0.01% by mass. The above (E) menthol content is 0.04% by mass or more, The liquid oral composition according to item 1, wherein the content of the aforementioned (F) stevia-based sweetener is 0.004 to 0.01% by mass. [Effects of the Invention]

[0009] A liquid oral composition is provided that contains cetylpyridinium chloride and laurylpyridinium chloride, which have a bitter taste, but in which the bitterness derived from the disinfectant is suppressed and the composition has a high level of usability. [Modes for carrying out the invention]

[0010] The embodiments included in the present invention will be described in more detail below. The present invention preferably includes liquid oral compositions, particularly liquid oral compositions containing cetylpyridinium chloride, laurylpyridinium chloride, methylparaben, sodium saccharin, menthol, and stevia-based sweeteners, but is not limited thereto. The present invention encompasses everything disclosed herein and recognizable to those skilled in the art.

[0011] The amount of cetylpyridinium chloride used in the present invention is not particularly limited as long as the effect is achieved, but for example, it is about 0.01 to 0.1% by mass of the total composition. The upper or lower limit of this range may be, for example, 0.02, 0.03, 0.04, 0.05, 0.06, 0.07, 0.08, or 0.09% by mass. For example, this range is about 0.03 to 0.07% by mass.

[0012] The amount of laurylpyridinium chloride used in the present invention is not particularly limited as long as the effect is achieved, but for example, it is about 0.01 to 0.1% by mass of the total composition. The upper or lower limit of this range may be, for example, 0.02, 0.03, 0.04, 0.05, 0.06, 0.07, 0.08, or 0.09% by mass. For example, this range is about 0.03 to 0.07% by mass.

[0013] The amount of methyl parahydroxybenzoate used in the present invention is not particularly limited as long as the effect is achieved, but for example, it is about 0.05 to 0.2% by mass of the total composition. The upper or lower limit of this range may be, for example, 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, or 0.19% by mass. For example, this range is about 0.1 to 0.15% by mass.

[0014] The amount of sodium saccharin used in the present invention is not particularly limited as long as the effect is achieved, but for example, it can be about 0.002 to 0.02% by mass of the total composition. The upper or lower limit of this range may be, for example, 0.003, 0.004, 0.005, 0.006, 0.007, 0.008, 0.009, 0.01, 0.011, 0.012, 0.013, 0.014, 0.015, 0.016, 0.017, 0.018, or 0.019% by mass. For example, this range is about 0.005 to 0.01% by mass.

[0015] The menthol used in this invention is not particularly limited as long as it is menthol, and any isomer or mixture thereof can be used, but l-menthol is preferred. The menthol may be chemically synthesized or purified from plant essential oils, etc.

[0016] The amount of menthol used in the present invention is not particularly limited as long as the effect is achieved, but for example, it can be about 0.01 to 0.1% by mass relative to the total composition. The upper or lower limit of this range may be, for example, 0.015, 0.02, 0.025, 0.03, 0.035, 0.04, 0.045, 0.05, 0.055, 0.06, 0.065, 0.07, 0.075, 0.08, 0.085, or 0.09% by mass. For example, this range is about 0.04 to 0.08% by mass.

[0017] The stevia-based sweeteners used in the present invention include, for example, stevia extracts, stevioside, rebaudioside, etc., and one of these can be used alone or in combination of two or more. The stevia extract is not particularly limited as long as it is purified after being extracted with water from the original leaves of stevia, and commercially available products can be used. The stevia extract preferably has a purity of steviol glycoside of 80% or more, more preferably 90% or more.

[0018] The blending amount of the stevia-based sweetener used in the present invention is not particularly limited as long as the effect is achieved, and for example, about 0.002 to 0.02% by mass based on the whole composition can be mentioned. The upper or lower limit of this range may be, for example, 0.003, 0.004, 0.005, 0.006, 0.007, 0.008, 0.009, 0.01, 0.011, 0.012, 0.013, 0.014, 0.015, 0.016, 0.017, 0.018, or 0.019% by mass. For example, this range is about 0.004 to 0.01% by mass.

[0019] The liquid oral composition of the present invention can be produced by a conventional method. Further, examples of the form of the liquid oral composition of the present invention include liquid dentifrices, mouthwashes, gels, etc. Further, the liquid oral composition of the present invention can be used as quasi-drugs, cosmetics, or pharmaceuticals.

[0020] In the liquid oral composition of the present invention, known optional components that can generally be blended in liquid oral compositions may be further blended alone or in combination of two or more within a range not impairing the effects of the present invention.

[0021] Examples of such known optional components include, for example, surfactants, bactericides, wetting agents, sweeteners, preservatives, colorants, pH adjusters, stabilizers, flavoring agents, astringents, fragrances, other medicinal components, etc.

[0022] As surfactants, for example, anionic surfactants, nonionic surfactants, or amphoteric surfactants can be incorporated. Specifically, examples of anionic surfactants include alkyl sulfate salts, polyoxyethylene alkyl ether sulfate salts, alkyl sulfosuccinates, polyoxyethylene alkyl ether sulfosuccinates, N-acyl amino acid salts, N-acyl taurine salts, alkyl ether carboxylates, alkyl phosphates, polyoxyethylene alkyl ether phosphates, fatty acid monoglyceride sulfates, and alkyl sulfoacetates. Examples of nonionic surfactants include fatty acid esters, fatty acid alkanolamides, sorbitan fatty acid esters, fatty acid monoglycerides, polyglycerin fatty acid esters, polyoxyethylene alkylphenyl ethers, alkyl glycosides, diethyl sebacate, polyoxyethylene hydrogenated castor oil, and fatty acid polyoxyethylene sorbitan. Examples of amphoteric surfactants include alkyldimethylaminoacetic acid betaine, alkylamidopropyldimethylaminoacetic acid betaine, N-acyl-N-carboxymethyl-N-hydroxyethylethylenediamine, and N-alkylaminoethylglycine. These surfactants can be used individually or in combination of two or more. Their concentration is typically 0.1 to 5% by mass of the total composition.

[0023] Examples of disinfectants include cationic disinfectants such as benzalkonium chloride, benzethonium chloride, and chlorhexidine hydrochloride; vitamin E derivatives such as dl-α-tocopherol acetate, tocopherol succinate, or tocopherol nicotinate; amphoteric disinfectants such as dodecyldiaminoethylglycine; and nonionic disinfectants such as triclosan and isopropylmethylphenol. These disinfectants can be used individually or in combination of two or more.

[0024] Examples of wetting agents include sorbitol, ethylene glycol, propylene glycol, 1,3-butylene glycol, polypropylene glycol, xylitol, maltitol, lactitol, palatinite, and polyethylene glycol. These wetting agents can be used individually or in combination of two or more.

[0025] Examples of sweeteners include acesulfamethamphetamine potassium, neohesperidyl dihydrochalcone, glycyrrhizin, perillartin, thaumatin, aspartylphenylalanine methyl ester, ρ-methoxycinnamic aldehyde, and sucralose. These sweeteners can be used individually or in combination of two or more.

[0026] Examples of preservatives include sodium benzoate, phenoxyethanol, and alkyldiaminoethylglycine hydrochloride. These preservatives can be used individually or in combination of two or more.

[0027] Examples of pH adjusting agents include citric acid, phosphoric acid, malic acid, pyrophosphate, lactic acid, tartaric acid, glycerophosphate, acetic acid, nitric acid, or chemically possible salts thereof, or sodium hydroxide. These pH adjusting agents can be used individually or in combination of two or more.

[0028] Examples of stabilizers include sodium edetate, sodium thiosulfate, sodium sulfite, sodium chloride, calcium lactate, lanolin, triacetin, castor oil, and magnesium sulfate. These stabilizers can be used individually or in combination of two or more.

[0029] Examples of flavoring agents include tea extract, tea distillate, propolis extract, and monosodium glutamate.

[0030] Examples of astringents include baking soda and aluminum lactate.

[0031] As fragrances, for example, carvone, anethole, methyl salicylate, limonene, ocimene, n-decyl alcohol, citronellol, α-terpineol, methyl acetate, citronellyl acetate, methyl eugenol, cineole, linalool, ethyl linalool, thymol, spearmint oil, peppermint oil, lemon oil, orange oil, sage oil, rosemary oil, cinnamon oil, perilla oil, wintergreen oil, eucalyptus oil, etc., can be used individually or in combination of two or more.

[0032] Other medicinal agents include fluorine compounds such as sodium fluoride, sodium monofluorophosphate, and stannous fluoride; enzymes such as dextranase, mutanase, amylase, protease, and lytic enzymes (Litec enzyme); tranexamic acid, ε-aminocaproic acid, aluminum chlorohydroxyallantoin, allantoin, dihydrocholesterol, glycyrrhizic acids, glycyrrhetinic acid, bisabolol, glycerophosphate, chlorophyll, copper gluconate, sodium chloride, and water-soluble inorganic phosphate. Compounds; vitamins such as pyridoxine acetate, ascorbic acid or its salts; and plant extracts such as aloe, ginkgo leaf, agaricus, oolong tea, chamomile, quince, gymnema, bamboo grass, sweet tea, eucommia tea, houttuynia cordata, coix seed, Japanese laurel, mugwort, green tea, rooibos, lemon balm, rosemary, club mint, monk fruit, perilla, cranberry, yarrow, elderflower, licorice, mint, eucalyptus, guarana, licorice, linden, hops, cacao, mulberry leaf, thyme, and scutellaria. [Examples]

[0033] The present invention will be described in detail below based on examples, but the present invention is not limited to these examples.

[0034] [Evaluation of the user experience of liquid oral compositions] The samples for Reference Examples 1 and 2, Examples 1-17, and Comparative Examples 1-13 were prepared by conventional methods using the formulations shown in Tables 1, 2, and 3. Five monitors each took 10 ml of the sample into their mouths and used it for 20 seconds. The sweetness during use, bitterness during use, bitterness immediately after use, and bitterness 1 minute after use were evaluated using the following five-point scale.

[0035] [Criteria for evaluating sweetness] 5 points: Sweetness is not noticeable at all, 4 points: Sweetness is barely noticeable, 3 points: Sweetness is slightly noticeable, 2 points: Sweetness is noticeable, 1 point: Sweetness is very noticeable [Bitterness Evaluation Criteria] 5 points: No bitterness, 4 points: Almost no bitterness, 3 points: Bitterness present, 2 points: Strong bitterness, 1 point: Very strong bitterness

[0036] For each of the sweetness and bitterness categories, as well as the overall evaluation, a score of 3.5 or higher based on the average of the five participants' evaluations was marked as 1, a score of 3.0 or higher but less than 3.5 was marked as 1, a score of 2.0 or higher but less than 3.0 was marked as 1, and a score of less than 2.0 was marked as ×. The results are shown in Tables 2 and 3. The overall evaluation was calculated using the average of the sweetness and bitterness evaluation scores, and any product that received an × in either sweetness or bitterness was marked as ×.

[0037] [Table 1]

[0038] [Table 2]

[0039] [Table 3]

[0040] Examples 1-17 in Tables 2 and 3 showed favorable results for both sweetness and bitterness.

[0041] Table 4 shows examples of formulations for the liquid oral composition of the present invention. Unless otherwise specified, the amounts of each formulation are shown in mass %.

[0042] [Table 4]

Claims

[Claim 1] (A) Cetylpyridinium chloride in an amount of 0.01 to 0.1% by mass, (B) 0.01 to 0.1% by mass of laurylpyridinium chloride (C) Methyl parahydroxybenzoate in an amount of 0.05 to 0.2% by mass, (D) Sodium saccharin in an amount of 0.002 to 0.02% by mass, (E) Menthol in a quantity of 0.01 to 0.18% by mass, and (F) A liquid oral composition containing 0.002 to 0.02% by mass of a stevia-based sweetener.

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