Liquid oral components
By incorporating methyl parahydroxybenzoate, sodium saccharin, and menthol into liquid oral compositions with cetylpyridinium chloride and laurylpyridinium chloride, the bitterness is suppressed, enhancing the usability and user experience.
Patent Information
- Application Number
- JP2021176454
- Authority / Receiving Office
- JP · JP
- Patent Type
- Patents
- Current Assignee / Owner
- Filing Date
- 2021-10-28
- Publication Date
- 2025-12-02
- Estimated Expiration
- 2041-10-28
AI Technical Summary
Liquid oral compositions containing cetylpyridinium chloride and laurylpyridinium chloride suffer from increased bitterness, deteriorating the user experience, despite their effectiveness in preventing oral problems like periodontal disease.
Blending specific amounts of methyl parahydroxybenzoate, sodium saccharin, and menthol with cetylpyridinium chloride and laurylpyridinium chloride in the composition to suppress bitterness while maintaining usability.
The composition effectively masks the bitterness of the bactericides, providing a high usability and pleasant user experience.
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Abstract
Description
[Technical Field]
[0001] The present invention relates to improving the usability of a liquid oral composition. [Background technology]
[0002] Oral compositions intended to prevent oral problems such as periodontal disease contain bactericides, medicinal ingredients, and other ingredients that exert useful effects. However, the bitterness inherent in each ingredient often reduces the user experience. Unlike pharmaceuticals, typical quasi-drug oral compositions do not improve symptoms with a few uses; continuous use is required to prevent oral problems. Therefore, to maintain motivation for continued use, oral compositions that provide a pleasant user experience during and after use are desired.
[0003] Among quaternary ammonium salts that are antiseptics, cetylpyridinium chloride has a high bactericidal activity against bacteria that cause periodontal disease and has been widely used in oral compositions. Recent research has revealed that in order to prevent periodontal disease, it is important to suppress the formation of plaque that causes periodontal disease, and that laurylpyridinium chloride is effective in killing Fusobacterium, which contributes to plaque formation by coaggregating with various bacteria (Patent Document 1).
[0004] To date, methods of adding various additives to oral compositions containing cetylpyridinium chloride to reduce bitterness during and after use and improve usability have been known. Patent Document 2 describes a method of improving the bitterness of cationic antiseptics by blending flavoring ingredients such as l-menthol and anethole at predetermined concentrations in the oral composition. [Prior art documents] [Patent documents]
[0005] [Patent Document 1] Patent application No. 2020-166440 [Patent Document 2] Japanese Patent Application Laid-Open No. 2012-77032 Summary of the Invention [Problem to be solved by the invention]
[0006] Laurylpyridinium chloride has a stronger bitter taste than cetylpyridinium chloride, and when used in combination with these, the feeling of use of the liquid oral composition is further deteriorated compared to when cetylpyridinium chloride is blended alone.To provide a liquid oral composition that has a high feeling of use, suppressing this bitter taste while not impairing the feeling of use due to the sweetness derived from the sweetener. [Means for solving the problem]
[0007] The inventors have conducted extensive research in light of the above problems, and have surprisingly found that by blending appropriate amounts of methyl parahydroxybenzoate, sodium saccharin, and menthol into a liquid oral composition containing cetylpyridinium chloride and laurylpyridinium chloride, it is possible to obtain a high usability while suppressing the bitterness derived from the disinfectant.
[0008] The present invention includes, for example, the inventions described below. Section 1. (A) 0.01 to 0.1% by mass of cetylpyridinium chloride, (B) 0.01 to 0.1 mass% of laurylpyridinium chloride, (C) 0.05 to 0.2 mass% of methyl parahydroxybenzoate, (D) 0.002 to 0.02% by mass of sodium saccharin, and (E) A liquid oral composition containing 0.01 to 0.05% by mass of menthol. Section 2. The content of the (A) cetylpyridinium chloride is 0.03 to 0.07% by mass, the content of the (B) laurylpyridinium chloride is 0.03 to 0.07% by mass, the content of the (C) methyl parahydroxybenzoate is 0.1 to 0.15 mass %, The content of the (D) saccharin sodium is 0.005 to 0.01% by mass, and Item 2. The liquid oral composition according to item 1, wherein the content of (E) menthol is 0.02 to 0.04% by mass. [Effects of the Invention]
[0009] A liquid oral composition is provided which contains bitter cetylpyridinium chloride and laurylpyridinium chloride, but suppresses the bitterness derived from the bactericide, and has a high usability. DETAILED DESCRIPTION OF THE INVENTION
[0010] Each embodiment of the present invention will be described in more detail below. The present invention preferably includes a liquid oral composition, particularly a liquid oral composition containing cetylpyridinium chloride, laurylpyridinium chloride, methyl parahydroxybenzoate, saccharin sodium, and menthol, but is not limited thereto, and the present invention includes all of the compositions disclosed herein and recognizable by those skilled in the art.
[0011] The amount of cetylpyridinium chloride used in the present invention is not particularly limited as long as it is within a range that achieves the desired effect, but may be, for example, about 0.01 to 0.1% by mass based on 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 it is within a range that achieves the desired effect, but may be, for example, 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, 0.02, 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 it is within a range that achieves the desired effect, but may be, for example, 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 saccharin sodium used in the present invention is not particularly limited as long as it is within a range that achieves the desired effect, but may be, for example, 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 the present invention is not particularly limited as long as it is menthol, and any isomer or mixture thereof can be used, but 1-menthol is preferred. 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 it is within a range that achieves the desired effect, but may be, for example, about 0.01 to 0.05% by mass of the entire 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, or 0.045% by mass. For example, this range is about 0.02 to 0.04% by mass.
[0017] The liquid oral composition of the present invention can be produced by a conventional method. The liquid oral composition of the present invention can be in the form of a liquid toothpaste, a mouthwash, a gel, etc. The liquid oral composition of the present invention can be used as a quasi-drug, a cosmetic, or a pharmaceutical.
[0018] The liquid oral composition of the present invention may further contain known optional components that can generally be incorporated into liquid oral compositions, either alone or in combination of two or more, within the scope that does not impair the effects of the present invention.
[0019] Such known optional ingredients include, for example, surfactants, disinfectants, humectants, sweeteners, preservatives, colorants, pH adjusters, stabilizers, flavoring agents, astringents, fragrances, other medicinal ingredients, and the like.
[0020] The surfactant may be, for example, an anionic surfactant, a nonionic surfactant, or an amphoteric surfactant. Specific examples of anionic surfactants include alkyl sulfates, polyoxyethylene alkyl ether sulfates, alkyl sulfosuccinates, polyoxyethylene alkyl ether sulfosuccinates, N-acylamino acid salts, N-acyltaurine salts, alkyl ether carboxylates, alkyl phosphates, polyoxyethylene alkyl ether phosphates, fatty acid monoglyceride sulfates, and alkyl sulfoacetates. Nonionic surfactants include, for example, 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 zwitterionic surfactants include alkyldimethylaminoacetic acid betaine, alkylamidopropyldimethylaminoacetic acid betaine, N-acyl-N-carboxymethyl-N-hydroxyethylethylenediamine, and N-alkylaminoethylglycine. These surfactants can be used alone or in combination of two or more. The amount of surfactant used is usually 0.1 to 5% by mass based on the total amount of the composition.
[0021] Examples of disinfectants include cationic disinfectants such as benzalkonium chloride, benzethonium chloride, and chlorhexidine hydrochloride, vitamin E compounds such as dl-α-tocopherol acetate, tocopherol succinate, and tocopherol nicotinate, amphoteric disinfectants such as dodecyldiaminoethylglycine, and nonionic disinfectants such as triclosan and isopropylmethylphenol. These disinfectants can be used alone or in combination of two or more.
[0022] Examples of humectants include sorbitol, ethylene glycol, propylene glycol, 1,3-butylene glycol, polypropylene glycol, xylitol, maltitol, lactitol, palatinit, polyethylene glycol, etc. These humectants can be blended alone or in combination of two or more.
[0023] Examples of sweeteners include acesulfame potassium, stevioside, neohesperidyl dihydrochalcone, glycyrrhizin, perillartine, thaumatin, aspartylphenylalanine methyl ester, p-methoxycinnamic aldehyde, sucralose, etc. These sweeteners can be blended alone or in combination of two or more.
[0024] Examples of preservatives include sodium benzoate, phenoxyethanol, alkyldiaminoethylglycine hydrochloride, etc. These preservatives can be used alone or in combination of two or more.
[0025] Examples of pH adjusters 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 pH adjusters can be blended alone or in combination of two or more.
[0026] Examples of stabilizers include sodium edetate, sodium thiosulfate, sodium sulfite, sodium chloride, calcium lactate, lanolin, triacetin, castor oil, magnesium sulfate, etc. These stabilizers can be blended alone or in combination of two or more.
[0027] Examples of flavoring agents include tea extract, dry distillate of tea, propolis extract, and sodium glutamate.
[0028] Examples of astringents include sodium bicarbonate and aluminum lactate.
[0029] Examples of fragrances that can be used include 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, and eucalyptus oil, and these can be used alone or in combination of two or more.
[0030] Other medicinal agents include fluorine compounds such as sodium fluoride, sodium monofluorophosphate, and stannous fluoride; enzymes such as dextranase, mutanase, amylase, protease, and lytic enzyme (Retec 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 and ascorbic acid or its salts; and plant extracts such as aloe, ginkgo leaf, agaricus, oolong tea, chamomile, quince, gymnema, kumazasa, sweet tea, du zhong tea, houttuynia cordata, Job's tears, megusuri tree, mugwort, green tea, rooibos, lemon balm, rosemary, crab mint, Luo Han Guo, perilla, cranberry, yarrow, elder, licorice, peppermint, eucalyptus, guarana, licorice, linden, hops, cacao, mulberry leaf, thyme, and Scutellaria root. [Example]
[0031] The present invention will be described in detail below based on examples, but the present invention is not limited to these examples.
[0032] [Evaluation of the usability of liquid oral compositions] Test samples of Reference Examples 1 and 2, Examples 1 to 15, and Comparative Examples 1 to 10 were prepared by standard methods using the blending amounts shown in Tables 1, 2, and 3. Five monitors were asked to hold 10 ml of each test sample in their mouths and use it for 20 seconds, and the sweetness during use, bitterness during use, bitterness immediately after use, and bitterness 1 minute after use were evaluated according to the following five-point scale.
[0033] [Sweetness evaluation criteria] 5 points: The sweetness is not noticeable at all, 4 points: The sweetness is barely noticeable, 3 points: The sweetness is somewhat noticeable, 2 points: The sweetness is noticeable, 1 point: The sweetness is very noticeable [Bitterness evaluation criteria] 5 points: no bitterness, 4 points: almost no bitterness, 3 points: bitterness, 2 points: strong bitterness, 1 point: very strong bitterness
[0034] For each of the sweetness and bitterness items and the overall evaluation, an average of the five evaluation scores of 3.5 points or more was given a 1, 3.0 points or more but less than 3.5 points was given a 1, 2.0 points or more but less than 3.0 points was given a 1, and less than 2.0 points was given an X. The results are shown in Tables 2 and 3. The overall evaluation was calculated from the average of the evaluation scores for sweetness and bitterness, and if either sweetness or bitterness was given an X, it was given an X.
[0035] [Table 1]
[0036] [Table 2]
[0037] [Table 3]
[0038] Examples 1 to 15 in Tables 2 and 3 showed good results in both sweetness and bitterness.
[0039] Formulation examples of the liquid oral composition of the present invention are shown in Table 4. The blending amounts of each formulation are shown in mass % unless otherwise specified.
[0040] [Table 4]
Claims
[Claim 1] (A) 0.01 to 0.1% by mass of cetylpyridinium chloride, (B) 0.01 to 0.1 mass% of laurylpyridinium chloride, (C) 0.05 to 0.2 mass% of methyl parahydroxybenzoate, (D) 0.002 to 0.02% by weight of sodium saccharin, and (E) A liquid oral composition containing 0.01 to 0.05% by weight of menthol.
Citation Information
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