WO2023074725A1 - Liquid composition for oral cavity - Google Patents

Liquid composition for oral cavity Download PDF

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Publication number
WO2023074725A1
WO2023074725A1 PCT/JP2022/039865 JP2022039865W WO2023074725A1 WO 2023074725 A1 WO2023074725 A1 WO 2023074725A1 JP 2022039865 W JP2022039865 W JP 2022039865W WO 2023074725 A1 WO2023074725 A1 WO 2023074725A1
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Prior art keywords
mass
composition
chloride
menthol
liquid composition
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PCT/JP2022/039865
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French (fr)
Japanese (ja)
Inventor
ヒョンソオク イム
知寛 高橋
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サンスター株式会社
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Priority claimed from JP2021176455A external-priority patent/JP2023065996A/en
Priority claimed from JP2021176454A external-priority patent/JP2023065995A/en
Application filed by サンスター株式会社 filed Critical サンスター株式会社
Publication of WO2023074725A1 publication Critical patent/WO2023074725A1/en

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34—Alcohols
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/37—Esters of carboxylic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/60—Sugars; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses

Definitions

  • the present disclosure relates to improving the usability of liquid oral compositions.
  • Oral compositions intended to prevent oral troubles such as periodontal disease contain bactericidal agents, medicinal ingredients, and other ingredients that exert useful effects. Decreased sensitivity often occurs. Oral compositions of common quasi-drugs, unlike pharmaceuticals, do not improve symptoms with a few uses, and continuous use is required for the purpose of preventing oral troubles. Therefore, in order to maintain motivation for continued use, there is a demand for an oral composition that provides a good feeling during and after use.
  • cetylpyridinium chloride has been widely used in oral compositions because of its high bactericidal activity against periodontal disease-causing bacteria. Recent studies have shown that it is important to suppress the formation of plaque, which causes periodontal disease, in order to prevent periodontal disease. It has been found that laurylpyridinium chloride is effective for sterilization (Patent Document 1).
  • Patent Document 2 describes a method for improving the bitterness and the like of a cationic fungicide by blending a flavor component such as l-menthol or anethole in an oral composition at a predetermined concentration.
  • Laurylpyridinium chloride has a stronger bitterness than cetylpyridinium chloride, and when used in combination, the feeling of use of the liquid oral composition is further reduced than when cetylpyridinium chloride is blended alone.
  • Sweeteners may be used to suppress the bitterness of oral compositions. However, the addition of sweeteners often impairs the feeling of use, such as making the composition feel too sweet.
  • the present inventors conducted a study.
  • the inventors of the present invention have conducted intensive research in view of the above problems, and found that a liquid oral composition containing cetylpyridinium chloride and laurylpyridinium chloride is blended with appropriate amounts of methyl parahydroxybenzoate, sodium saccharin, and menthol. By doing so, the inventors have found the possibility of preparing an oral composition that provides a high feeling of use while suppressing the bitterness derived from cetylpyridinium chloride and laurylpyridinium chloride. In addition, as a result of further investigation, it was found that (i) a specific amount of menthol is added, or (ii) a stevia-based sweetener is further added to suppress the bitterness and to be used as a sweetener. It has been found that an oral composition in which a decrease in sensation is also suppressed can be prepared.
  • Section 1 (A) 0.01 to 0.1% by mass of cetylpyridinium chloride; (B) 0.01 to 0.1% by mass of laurylpyridinium chloride; (C) 0.05 to 0.2% by mass of methyl paraoxybenzoate, (D) 0.002 to 0.02% by mass of sodium saccharin, and (E) 0.01% by mass or more of menthol, and (i) a menthol content of 0.01 to 0.05% by mass, or (ii) further containing (F) a stevia-based sweetener of 0.002 to 0.02% by mass, A liquid oral composition. Section 2.
  • a liquid oral composition comprising: Section 4.
  • the content of (A) cetylpyridinium chloride is 0.03 to 0.07% by weight, (B) the content of laurylpyridinium chloride is 0.03 to 0.07% by mass; (C) the content of methyl paraoxybenzoate is 0.1 to 0.15% by mass;
  • Item 3 The liquid composition for oral cavity according to Item 2, wherein the content of (D) sodium saccharin is 0.005 to 0.01% by mass, and the content of (E) menthol is 0.02 to 0.04% by mass. thing. Item 5.
  • the content of (A) cetylpyridinium chloride is 0.03 to 0.07% by weight
  • (B) the content of laurylpyridinium chloride is 0.03 to 0.07% by mass
  • (C) the content of methyl paraoxybenzoate is 0.1 to 0.15% by mass
  • the content of (D) sodium saccharin is 0.005 to 0.01% by mass
  • Item 4 The liquid composition for oral cavity according to Item 3, wherein the content of (E) menthol is 0.04% by mass or more, and the content of (F) stevia sweetener is 0.004 to 0.01% by mass. thing.
  • liquid oral composition containing cetylpyridinium chloride and laurylpyridinium chloride, which have a bitter taste, while suppressing the bitterness derived from these bactericidal components and having a high feeling of use.
  • the present disclosure preferably includes, but is not limited to, liquid oral compositions, particularly liquid oral compositions containing cetylpyridinium chloride, laurylpyridinium chloride, methyl paraoxybenzoate, sodium saccharin, and menthol. Rather, the present disclosure encompasses everything disclosed herein and recognized by a person skilled in the art.
  • the said liquid composition for oral cavity may be called the composition of this indication.
  • the amount of cetylpyridinium chloride used in the composition of the present disclosure is not particularly limited as long as the effect is exhibited, but for example, it is about 0.01 to 0.1% by mass based on the entire composition. be done.
  • the upper limit or lower limit of the range may be, for example, 0.02, 0.03, 0.04, 0.05, 0.06, 0.07, 0.08, 0.09% by mass. .
  • the range may be about 0.03 to 0.07% by mass.
  • the amount of laurylpyridinium chloride used in the composition of the present disclosure is not particularly limited as long as the effect is exhibited, but for example, about 0.01 to 0.1% by mass relative to the entire composition. be done.
  • the upper limit or lower limit of the range may be, for example, 0.02, 0.03, 0.04, 0.05, 0.06, 0.07, 0.08, 0.09% by mass. .
  • the range may be about 0.03 to 0.07% by mass.
  • the amount of methyl p-hydroxybenzoate used in the composition of the present disclosure is not particularly limited as long as the effect is exhibited, but for example, about 0.05 to 0.2% by mass based on the entire composition. mentioned.
  • the upper limit or lower limit of the range is, for example, 0.06, 0.07, 0.08, 0.09, 0.1, 0.11, 0.12, 0.13, 0.14, 0.06, 0.07, 0.08, 0.09, 0.1, 0.11, 0.12, 0.13, 0.14. 15, 0.16, 0.17, 0.18, 0.19% by mass.
  • the range may be about 0.1 to 0.15% by mass.
  • methyl paraoxybenzoate is also called methylparaben, etc.
  • the amount of saccharin sodium used in the composition of the present disclosure is not particularly limited as long as it is effective, but for example, it is about 0.002 to 0.02% by mass based on the entire composition.
  • the upper limit or lower limit of the range is, for example, 0.003, 0.004, 0.005, 0.006, 0.007, 0.008, 0.009, 0.01, 0.011, 0.011. 012, 0.013, 0.014, 0.015, 0.016, 0.017, 0.018, 0.019% by mass.
  • the range may be about 0.005 to 0.01% by mass.
  • menthol used in the composition of the present disclosure is not particularly limited as long as it is menthol, and any isomer or mixture thereof can be used, but l-menthol is preferred. Menthol may be chemically synthesized or refined from plant essential oils or the like.
  • the amount of menthol used in the composition of the present disclosure is not particularly limited as long as it is effective, but for example, it is 0.01% by mass or more based on the entire composition, and 0.01 to 0.01% by mass. About 0.1% by mass is more preferable, and about 0.01 to 0.05% by mass is more preferable.
  • the upper or lower limit of the range (0.01 to 0.1% by mass) is, 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, 0.09, or 0.095% by weight.
  • the range may be about 0.02 to 0.08% by mass, or about 0.02 to 0.04% by mass.
  • the bitterness is particularly preferably suppressed by (i) setting the amount of menthol to a specific amount, or (ii) further adding a stevia-based sweetener.
  • stevia-based sweeteners include, for example, stevia extract, stevioside, rebaudioside, and the like, and these may be used alone or in combination of two or more. can be compounded.
  • the stevia extract is preferably purified after being water-extracted from stevia leaves.
  • commercially available products can also be used.
  • the stevia extract preferably has a steviol glycoside purity of 80% or more, more preferably 90% or more.
  • the amount of the stevia-based sweetener used in the composition of the present disclosure is not particularly limited as long as it is effective, but for example, it is about 0.002 to 0.02% by weight based on the entire composition. mentioned.
  • the upper limit or lower limit of the range is, for example, 0.003, 0.004, 0.005, 0.006, 0.007, 0.008, 0.009, 0.01, 0.011, 0.011. 012, 0.013, 0.014, 0.015, 0.016, 0.017, 0.018, 0.019% by mass.
  • the range may be about 0.004 to 0.01% by mass.
  • compositions of the present disclosure include, for example, (A) 0.01 to 0.1% by mass of cetylpyridinium chloride, (B) 0.01 to 0.1% by mass of laurylpyridinium chloride, (C ) 0.05 to 0.2% by mass of methyl paraoxybenzoate, (D) 0.002 to 0.02% by mass of sodium saccharin, and (E) 0.01% by mass or more of menthol, and (i) a menthol content of 0.01 to 0.05% by mass, or (ii) further containing (F) a stevia-based sweetener of 0.002 to 0.02% by mass Oral compositions are included.
  • the content of each of these components (A) to (F) can be appropriately set, for example, within the ranges described above.
  • composition of the present disclosure can be produced by conventional methods.
  • Forms of the compositions of the present disclosure also include liquid dentifrices, mouthwashes, gels, and the like.
  • the composition of the present disclosure can be used as a quasi-drug, cosmetic, or pharmaceutical.
  • composition of the present disclosure may further contain known optional components that can generally be contained in liquid oral compositions, singly or in combination of two or more, as long as the effects are not impaired.
  • solvents examples include solvents, surfactants, bactericides, wetting agents, sweeteners, preservatives, colorants, pH adjusters, stabilizers, corrigents, astringents, and perfumes. , and other medicinal ingredients.
  • the solvent is not particularly limited, and solvents used in known liquid oral compositions can be used. For example, water, ethanol, or the like can be used.
  • the amount of such a solvent to be blended is not particularly limited, but the balance may be used as the solvent in the preparation of the composition. 9% by mass or less, 99.5% by mass or less, 99, 98, 97, or 96% by mass or less can be exemplified.
  • anionic surfactants include alkyl sulfates, polyoxyethylene alkyl ether sulfates, alkyl sulfosuccinates, polyoxyethylene alkyl ether sulfosuccinates, N-acylamino acid salts, N- acyl taurine salts, alkyl ether carboxylates, alkyl phosphates, polyoxyethylene alkyl ether phosphates, fatty acid monoglyceride sulfates, alkyl sulfoacetates and the like.
  • 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, Examples include fatty acid polyoxyethylene sorbitan.
  • amphoteric surfactants include betaine alkyldimethylaminoacetate, betaine alkylamidopropyldimethylaminoacetate, N-acyl-N-carboxymethyl-N-hydroxyethylethylenediamine, N-alkylaminoethylglycine and the like. These surfactants can be blended singly or in combination of two or more. The blending amount thereof is usually 0.1 to 5% by mass based on the total amount of the composition.
  • Bactericides other than cetylpyridinium chloride and laurylpyridinium chloride e.g., cationic bactericides such as benzalkonium chloride, benzethonium chloride, chlorhexidine hydrochloride, dl- ⁇ -tocopherol acetate, tocopherol succinate, or nicotinic acid
  • cationic bactericides such as benzalkonium chloride, benzethonium chloride, chlorhexidine hydrochloride, dl- ⁇ -tocopherol acetate, tocopherol succinate, or nicotinic acid
  • vitamin E compounds such as tocopherol
  • amphoteric fungicides such as dodecyldiaminoethylglycine
  • nonionic fungicides such as triclosan and isopropylmethylphenol. These fungicides can be blended singly or in combination of two or more.
  • Wetting agents include, for example, sorbitol, ethylene glycol, propylene glycol, 1,3-butylene glycol, polypropylene glycol, xylit, maltite, lactit, palatinit, polyethylene glycol and the like. These wetting agents can be blended singly or in combination of two or more.
  • Sweeteners other than sodium saccharin and stevia-based sweeteners such as acesulfame potassium, neohesperidyl dihydrochalcone, glycyrrhizin, perillartine, thaumatin, aspartylphenylalanine methyl ester, ⁇ -methoxycinnamic aldehyde, sucralose, etc. mentioned. These sweeteners can be blended singly or in combination of two or more.
  • antiseptics examples include sodium benzoate, phenoxyethanol, alkyldiaminoethylglycine hydrochloride and the like. These preservatives can be blended singly or in combination of two or more.
  • pH adjusters examples include citric acid, phosphoric acid, malic acid, pyrophosphate, lactic acid, tartaric acid, glycerophosphoric acid, acetic acid, nitric acid, or chemically possible salts thereof, sodium hydroxide, and the like. These pH adjusters can be blended singly or in combination of two or more.
  • Stabilizers include, for example, sodium edetate, sodium thiosulfate, sodium sulfite, sodium chloride, calcium lactate, lanolin, triacetin, castor oil, magnesium sulfate and the like. These stabilizers can be blended singly or in combination of two or more.
  • flavoring agents examples include tea extract, dry distillation of tea, propolis extract, sodium glutamate and the like.
  • astringents examples include sodium bicarbonate and aluminum lactate.
  • fragrances include carvone, anethole, methyl salicylate, limonene, ocimene, n-decyl alcohol, citronellol, ⁇ -terpineol, methyl acetate, citronellyl acetate, methyl eugenol, cineol, linalool, ethyl linalool, thymol, spearmint oil, Flavors such as peppermint oil, lemon oil, orange oil, sage oil, rosemary oil, cinnamon oil, perilla oil, wintergreen oil, and eucalyptus oil can be used alone or in combination of two or more.
  • Other medicinal agents include fluorine compounds such as sodium fluoride, sodium monofluorophosphate, and stannous fluoride; ⁇ -aminocaproic acid, aluminum chlorohydroxyallantoin, allantoin, dihydrocholesterol, glycyrrhizic acids, glycyrrhetinic acid, bisabolol, glycerophosphate, chlorophyll, copper gluconate, sodium chloride, water-soluble inorganic phosphoric acid compound; pyridoxine acetate, ascorbic acid or its salt Vitamins such as aloe, ginkgo biloba, agaricus, oolong tea, chamomile, quince, gymnema, kumazasa, sweet tea, tochu tea, houttuynia cordata, adlay, megusurinoki, mugwort, green tea, rooibos, lemon balm, rosemary, clubmin, rakanka, perilla
  • the term “comprising” includes “consisting essentially of” and “consisting of.”
  • the present disclosure encompasses any and all combinations of the constituent elements described herein.
  • the various characteristics (property, structure, function, etc.) described for each of the embodiments of the disclosure described above may be combined in any way to identify subject matter encompassed by the disclosure. That is, the present disclosure encompasses all subject matter consisting of any and all possible combinations of the features described herein.
  • Test samples liquid compositions of Examples, Comparative Examples, and Reference Examples were prepared by a conventional method at the blending amounts shown in Tables 1A, 2A, and 3A. Separately, test samples (liquid compositions of Examples, Comparative Examples, and Reference Examples) were prepared by a conventional method at the blending amounts shown in Tables 1B, 2B, and 3B. .
  • Reference Examples 1a and 1b have the same composition
  • Reference Examples 2a and 2b have the same composition
  • Comparative Examples 1a and 1b have the same composition
  • Comparative Examples 9a and 5b. have the same composition.
  • Five monitors each held 10 ml of the test subject in their mouth and used it for 20 seconds, and the following 5 levels were used for sweetness during use, bitterness during use, bitterness immediately after use, and bitterness 1 minute after use. was evaluated according to the evaluation criteria of
  • the average value of the evaluation values of 5 people is 3.5 points or more, ⁇ , 3.0 points or more and less than 3.5 points, 2.0 points or more and 3.0 points.
  • a score of less than ⁇ was given, and a score of less than 2.0 was given as ⁇ .
  • the results are shown in Tables 2A, 2B, 3A, and 3B.
  • the overall evaluation was calculated from the average value of the evaluation values of sweetness and bitterness, and the evaluation with x for either sweetness or bitterness was rated as x.
  • Formulation examples of the composition of the present disclosure are shown in Tables 4A and 4B.
  • the compounding quantity of each prescription shows the mass % unless otherwise specified.

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Abstract

The present invention provides a liquid composition for oral cavity with good feeling of use, the liquid composition containing lauryl pyridinium chloride and cetylpyridinium chloride without deteriorating the feeling of use due to the sweetness derived from a sweetener, while suppressing the bitterness due to those chloride components. More specifically, the present invention provides the following liquid composition for oral cavity. A liquid composition for oral cavity which contains 0.01% by mass to 0.1% by mass of (A) cetylpyridinium chloride, 0.01% by mass to 0.1% by mass of (B) lauryl pyridinium chloride, 0.05% by mass to 0.2% by mass of (C) methyl parahydroxybenzoate, 0.002% by mass to 0.02% by mass of (D) saccharin sodium, and 0.01% by mass or more of (E) menthol, while satisfying one of the following requirements (i) and (ii). (i) The content of menthol is 0.01% by mass to 0.05% by mass. (ii) This liquid composition for oral cavity additionally contains 0.002% by mass to 0.02% by mass of (F) a stevia-based sweetener.

Description

液体口腔用組成物Liquid oral composition
　本開示は、液体口腔用組成物の使用感改善に関する。 The present disclosure relates to improving the usability of liquid oral compositions.
　歯周病などの口腔トラブルの予防を目的とする口腔用組成物には、殺菌剤や薬用成分、およびその他の有用な効果を発揮する成分が配合されるが、各成分特有の苦味などによる使用感の低下がしばしば生じる。一般的な医薬部外品の口腔用組成物は医薬品とは異なり、数回の使用で症状を改善するものではなく、口腔トラブルの予防目的においては継続使用が必要である。よって、継続使用のモチベーションを維持するために、使用中及び使用後の使用感の良い口腔用組成物が所望されている。 Oral compositions intended to prevent oral troubles such as periodontal disease contain bactericidal agents, medicinal ingredients, and other ingredients that exert useful effects. Decreased sensitivity often occurs. Oral compositions of common quasi-drugs, unlike pharmaceuticals, do not improve symptoms with a few uses, and continuous use is required for the purpose of preventing oral troubles. Therefore, in order to maintain motivation for continued use, there is a demand for an oral composition that provides a good feeling during and after use.
殺菌剤である第四級アンモニウム塩のうち、塩化セチルピリジニウムは歯周病の原因菌に対する殺菌力が高く口腔用組成物に汎用されてきた。近年の研究により、歯周病の予防には、歯周病の原因となるプラークの形成を抑制することが重要であり、様々な細菌との共凝集を行うことによりプラーク形成に寄与するフゾバクテリウムの殺菌には塩化ラウリルピリジニウムが有効であることが明らかとなった（特許文献１）。 Among quaternary ammonium salts that are antibacterial agents, cetylpyridinium chloride has been widely used in oral compositions because of its high bactericidal activity against periodontal disease-causing bacteria. Recent studies have shown that it is important to suppress the formation of plaque, which causes periodontal disease, in order to prevent periodontal disease. It has been found that laurylpyridinium chloride is effective for sterilization (Patent Document 1).
これまでに、塩化セチルピリジニウムを含有する口腔用組成物の使用中および使用後の苦味等を低減し、使用感を良好にするために、各種添加剤を加える方法が知られている。特許文献２には、口腔用組成物中に香味成分であるｌ－メントールやアネトールを所定濃度配合して、カチオン性殺菌剤が有する苦味等を改善する方法が記載されている。 Methods of adding various additives to reduce bitterness and the like during and after use of oral compositions containing cetylpyridinium chloride and to improve the feeling of use have been known. Patent Document 2 describes a method for improving the bitterness and the like of a cationic fungicide by blending a flavor component such as l-menthol or anethole in an oral composition at a predetermined concentration.
特許第６９６８９６４号公報Japanese Patent No. 6968964 特開２０１２－０７７０３２号公報JP 2012-077032 A
　塩化ラウリルピリジニウムは、塩化セチルピリジニウムに比して苦味が強く、これらを併用すると塩化セチルピリジニウムを単独で配合した場合よりさらに液体口腔用組成物の使用感を低下させる。口腔用組成物の苦み抑制のため、甘味剤を用いることが考えられるが、甘味剤を配合することにより、今度は甘味が強く感じられすぎるなど、甘味剤により使用感が損なわれる場合も多い。塩化ラウリルピリジニウム及び塩化セチルピリジニウムを含有し、且つこれらの成分に起因する苦味を抑制しながらも、甘味料由来の甘味により使用感も損なわれない、使用感の高い液体口腔用組成物を提供することを目的に、本発明者らは検討を行った。 Laurylpyridinium chloride has a stronger bitterness than cetylpyridinium chloride, and when used in combination, the feeling of use of the liquid oral composition is further reduced than when cetylpyridinium chloride is blended alone. Sweeteners may be used to suppress the bitterness of oral compositions. However, the addition of sweeteners often impairs the feeling of use, such as making the composition feel too sweet. To provide a liquid composition for the oral cavity containing laurylpyridinium chloride and cetylpyridinium chloride, suppressing the bitterness caused by these components, and giving a high feeling of use without spoiling the feeling of use due to sweetness derived from a sweetener. For this purpose, the present inventors conducted a study.
　本発明者らは上記課題に鑑みて鋭意研究を進めた結果、塩化セチルピリジニウムと、塩化ラウリルピリジニウムとを含有する液体口腔用組成物に、パラオキシ安息香酸メチル、サッカリンナトリウム、およびメントールを適切な量配合することで、塩化セチルピリジニウム及び塩化ラウリルピリジニウムに由来する苦味を抑制しながらも、高い使用感が得られる口腔用組成物を調製できる可能性を見出した。
　また、さらに検討を進めたところ、（ｉ）メントールの配合量を特定の量とするか、あるいは（ｉｉ）さらにステビア系甘味料を配合することにより、特に好ましく苦みが抑制され且つ甘味剤による使用感低下も抑制された口腔用組成物が調製できることを見いだした。 The inventors of the present invention have conducted intensive research in view of the above problems, and found that a liquid oral composition containing cetylpyridinium chloride and laurylpyridinium chloride is blended with appropriate amounts of methyl parahydroxybenzoate, sodium saccharin, and menthol. By doing so, the inventors have found the possibility of preparing an oral composition that provides a high feeling of use while suppressing the bitterness derived from cetylpyridinium chloride and laurylpyridinium chloride.
In addition, as a result of further investigation, it was found that (i) a specific amount of menthol is added, or (ii) a stevia-based sweetener is further added to suppress the bitterness and to be used as a sweetener. It has been found that an oral composition in which a decrease in sensation is also suppressed can be prepared.
本開示は、例えば以下に記載の発明を包含する。
項１．
（Ａ）塩化セチルピリジニウムを０．０１～０．１質量％、
（Ｂ）塩化ラウリルピリジニウムを０．０１～０．１質量％、
（Ｃ）パラオキシ安息香酸メチルを０．０５～０．２質量％、
（Ｄ）サッカリンナトリウムを０．００２～０．０２質量％、及び
（Ｅ）メントールを０．０１質量％以上、
含有し、且つ
（ｉ）メントール含有量が０．０１～０．０５質量％であるか、又は
（ｉｉ）さらに（Ｆ）ステビア系甘味料を０．００２～０．０２質量％含有する、
液体口腔用組成物。
項２．
（Ａ）塩化セチルピリジニウムを０．０１～０．１質量％、
（Ｂ）塩化ラウリルピリジニウムを０．０１～０．１質量％、
（Ｃ）パラオキシ安息香酸メチルを０．０５～０．２質量％、
（Ｄ）サッカリンナトリウムを０．００２～０．０２質量％、及び
（Ｅ）メントールを０．０１～０．０５質量％、
含有する、
液体口腔用組成物。
項３．
（Ａ）塩化セチルピリジニウムを０．０１～０．１質量％、
（Ｂ）塩化ラウリルピリジニウムを０．０１～０．１質量％、
（Ｃ）パラオキシ安息香酸メチルを０．０５～０．２質量％、
（Ｄ）サッカリンナトリウムを０．００２～０．０２質量％、
（Ｅ）メントールを０．０１質量％以上、および
（Ｆ）ステビア系甘味料を０．００２～０．０２質量％、
含有する
液体口腔用組成物。
項４．
前記（Ａ）塩化セチルピリジニウムの含有量が０．０３～０．０７量％、
前記（Ｂ）塩化ラウリルピリジニウムの含有量が０．０３～０．０７質量％、
前記（Ｃ）パラオキシ安息香酸メチルの含有量が０．１～０．１５質量％、
前記（Ｄ）サッカリンナトリウムの含有量が０．００５～０．０１質量％、および
前記（Ｅ）メントールの含有量が０．０２～０．０４質量％である、項２に記載の液体口腔用組成物。
項５．
前記（Ａ）塩化セチルピリジニウムの含有量が０．０３～０．０７量％、
前記（Ｂ）塩化ラウリルピリジニウムの含有量が０．０３～０．０７質量％、
前記（Ｃ）パラオキシ安息香酸メチルの含有量が０．１～０．１５質量％、
前記（Ｄ）サッカリンナトリウムの含有量が０．００５～０．０１質量％、
前記（Ｅ）メントールの含有量が０．０４質量％以上、および
前記（Ｆ）ステビア系甘味料の含有量が０．００４～０．０１質量％である、項３に記載の液体口腔用組成物。 The present disclosure 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% by mass of laurylpyridinium chloride;
(C) 0.05 to 0.2% by mass of methyl paraoxybenzoate,
(D) 0.002 to 0.02% by mass of sodium saccharin, and (E) 0.01% by mass or more of menthol,
and (i) a menthol content of 0.01 to 0.05% by mass, or (ii) further containing (F) a stevia-based sweetener of 0.002 to 0.02% by mass,
A liquid oral composition.
Section 2.
(A) 0.01 to 0.1% by mass of cetylpyridinium chloride;
(B) 0.01 to 0.1% by mass of laurylpyridinium chloride;
(C) 0.05 to 0.2% by mass of methyl paraoxybenzoate,
(D) 0.002 to 0.02% by weight of sodium saccharin, and (E) 0.01 to 0.05% by weight of menthol,
contains,
A liquid oral composition.
Item 3.
(A) 0.01 to 0.1% by mass of cetylpyridinium chloride;
(B) 0.01 to 0.1% by mass of laurylpyridinium chloride;
(C) 0.05 to 0.2% by mass of methyl paraoxybenzoate,
(D) 0.002 to 0.02% by mass of sodium saccharin;
(E) 0.01% by mass or more of menthol, and (F) 0.002 to 0.02% by mass of a stevia-based sweetener,
A liquid oral composition comprising:
Section 4.
The content of (A) cetylpyridinium chloride is 0.03 to 0.07% by weight,
(B) the content of laurylpyridinium chloride is 0.03 to 0.07% by mass;
(C) the content of methyl paraoxybenzoate is 0.1 to 0.15% by mass;
Item 3. The liquid composition for oral cavity according to Item 2, wherein the content of (D) sodium saccharin is 0.005 to 0.01% by mass, and the content of (E) menthol is 0.02 to 0.04% by mass. thing.
Item 5.
The content of (A) cetylpyridinium chloride is 0.03 to 0.07% by weight,
(B) the content of laurylpyridinium chloride is 0.03 to 0.07% by mass;
(C) the content of methyl paraoxybenzoate is 0.1 to 0.15% by mass;
The content of (D) sodium saccharin is 0.005 to 0.01% by mass,
Item 4. The liquid composition for oral cavity according to Item 3, wherein the content of (E) menthol is 0.04% by mass or more, and the content of (F) stevia sweetener is 0.004 to 0.01% by mass. thing.
　苦味を有する塩化セチルピリジニウムと塩化ラウリルピリジニウムとを含有していながらも、これら殺菌成分に由来する苦味が抑制され、高い使用感を有する液体口腔用組成物が提供される。 Provided is a liquid oral composition containing cetylpyridinium chloride and laurylpyridinium chloride, which have a bitter taste, while suppressing the bitterness derived from these bactericidal components and having a high feeling of use.
　以下、本開示に包含される各実施形態について、さらに詳細に説明する。なお、本開示は液体口腔用組成物、特に、塩化セチルピリジニウム、塩化ラウリルピリジニウム、パラオキシ安息香酸メチル、サッカリンナトリウム、およびメントールを含む液体口腔用組成物等を好ましく包含するが、これらに限定されるわけではなく、本開示は本明細書に開示され当業者が認識できる全てを包含する。なお、当該液体口腔用組成物を本開示の組成物ということがある。 Each embodiment included in the present disclosure will be described in further detail below. The present disclosure preferably includes, but is not limited to, liquid oral compositions, particularly liquid oral compositions containing cetylpyridinium chloride, laurylpyridinium chloride, methyl paraoxybenzoate, sodium saccharin, and menthol. Rather, the present disclosure encompasses everything disclosed herein and recognized by a person skilled in the art. In addition, the said liquid composition for oral cavity may be called the composition of this indication.
　本開示の組成物に用いられる塩化セチルピリジニウムの配合量は、効果が奏される範囲であれば特に制限はされないが、例えば組成物全体に対して０．０１～０．１質量％程度が挙げられる。なお、当該範囲の上限または下限は、例えば、０．０２、０．０３、０．０４、０．０５、０．０６、０．０７、０．０８、０．０９質量％であってもよい。例えば当該範囲は、０．０３～０．０７質量％程度であってもよい。 The amount of cetylpyridinium chloride used in the composition of the present disclosure is not particularly limited as long as the effect is exhibited, but for example, it is about 0.01 to 0.1% by mass based on the entire composition. be done. The upper limit or lower limit of the range may be, for example, 0.02, 0.03, 0.04, 0.05, 0.06, 0.07, 0.08, 0.09% by mass. . For example, the range may be about 0.03 to 0.07% by mass.
　本開示の組成物に用いられる塩化ラウリルピリジニウムの配合量は、効果が奏される範囲であれば特に制限はされないが、例えば組成物全体に対して０．０１～０．１質量％程度が挙げられる。なお、当該範囲の上限または下限は、例えば、０．０２、０．０３、０．０４、０．０５、０．０６、０．０７、０．０８、０．０９質量％であってもよい。例えば当該範囲は、０．０３～０．０７質量％程度であってもよい。 The amount of laurylpyridinium chloride used in the composition of the present disclosure is not particularly limited as long as the effect is exhibited, but for example, about 0.01 to 0.1% by mass relative to the entire composition. be done. The upper limit or lower limit of the range may be, for example, 0.02, 0.03, 0.04, 0.05, 0.06, 0.07, 0.08, 0.09% by mass. . For example, the range may be about 0.03 to 0.07% by mass.
　本開示の組成物で用いられるパラオキシ安息香酸メチルの配合量は、効果が奏される範囲であれば特に制限はされないが、例えば組成物全体に対して０．０５～０．２質量％程度が挙げられる。なお、当該範囲の上限または下限は、例えば、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質量％であってもよい。例えば当該範囲は、０．１～０．１５質量％程度であってもよい。なお、パラオキシ安息香酸メチルは、メチルパラベン等とも呼ばれる The amount of methyl p-hydroxybenzoate used in the composition of the present disclosure is not particularly limited as long as the effect is exhibited, but for example, about 0.05 to 0.2% by mass based on the entire composition. mentioned. The upper limit or lower limit of the range is, for example, 0.06, 0.07, 0.08, 0.09, 0.1, 0.11, 0.12, 0.13, 0.14, 0.06, 0.07, 0.08, 0.09, 0.1, 0.11, 0.12, 0.13, 0.14. 15, 0.16, 0.17, 0.18, 0.19% by mass. For example, the range may be about 0.1 to 0.15% by mass. In addition, methyl paraoxybenzoate is also called methylparaben, etc.
　本開示の組成物で用いられるサッカリンナトリウムの配合量は、効果が奏される範囲であれば特に制限はされないが、例えば組成物全体に対して０．００２～０．０２質量％程度が挙げられる。なお、当該範囲の上限または下限は、例えば、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、０．０１９質量％であってもよい。例えば当該範囲は、０．００５～０．０１質量％程度であってもよい。 The amount of saccharin sodium used in the composition of the present disclosure is not particularly limited as long as it is effective, but for example, it is about 0.002 to 0.02% by mass based on the entire composition. The upper limit or lower limit of the range is, for example, 0.003, 0.004, 0.005, 0.006, 0.007, 0.008, 0.009, 0.01, 0.011, 0.011. 012, 0.013, 0.014, 0.015, 0.016, 0.017, 0.018, 0.019% by mass. For example, the range may be about 0.005 to 0.01% by mass.
　本開示の組成物に用いられるメントールは、メントールであれば特に限定されることはなく、あらゆる異性体もしくはその混合物を用いることができるが、ｌ－メントールが好ましい。メントールは化学的に合成されたものでも、植物の精油等から精製したものでもよい。 The menthol used in the composition of the present disclosure is not particularly limited as long as it is menthol, and any isomer or mixture thereof can be used, but l-menthol is preferred. Menthol may be chemically synthesized or refined from plant essential oils or the like.
　本開示の組成物で用いられるメントールの配合量は、効果が奏される範囲であれば特に制限はされないが、例えば組成物全体に対して０．０１質量％以上が挙げられ、０．０１～０．１質量％程度がより好ましく挙げられ、０．０１～０．０５質量％程度がさらに好ましく挙げられる。なお、当該範囲（０．０１～０．１質量％）の上限または下限は、例えば、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、０．０９、又は０．０９５質量％であってもよい。例えば当該範囲は、０．０２～０．０８質量％程度であってもよいし、あるいは０．０２～０．０４質量％程度であってもよい。
　なお、上記の通り、本開示の組成物においては、（ｉ）メントールの配合量を特定の量とするか、あるいは（ｉｉ）さらにステビア系甘味料を配合することにより、特に好ましく苦みが抑制され且つ甘味剤による使用感低下も抑制された液体口腔用組成物となり得る。 The amount of menthol used in the composition of the present disclosure is not particularly limited as long as it is effective, but for example, it is 0.01% by mass or more based on the entire composition, and 0.01 to 0.01% by mass. About 0.1% by mass is more preferable, and about 0.01 to 0.05% by mass is more preferable. The upper or lower limit of the range (0.01 to 0.1% by mass) is, 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, 0.09, or 0.095% by weight. For example, the range may be about 0.02 to 0.08% by mass, or about 0.02 to 0.04% by mass.
As described above, in the composition of the present disclosure, the bitterness is particularly preferably suppressed by (i) setting the amount of menthol to a specific amount, or (ii) further adding a stevia-based sweetener. In addition, it is possible to obtain a liquid composition for oral cavity in which deterioration of the feeling of use due to a sweetener is suppressed.
　本開示の組成物にステビア系甘味料を用いる場合、ステビア系甘味料は、例えばステビア抽出物、ステビオサイド、レバウディオサイド等が挙げられ、これらの１種を単独で又で２種以上組み合わせて配合することができる。ステビア抽出物は、ステビアの原葉から水抽出した後、精製されたものが好ましく、例えば市販のものを用いることもできる。当該ステビア抽出物は、ステビオール配糖体の純度が８０％以上であるものが好ましく、９０％以上であるものがより好ましい。 When a stevia-based sweetener is used in the composition of the present disclosure, stevia-based sweeteners include, for example, stevia extract, stevioside, rebaudioside, and the like, and these may be used alone or in combination of two or more. can be compounded. The stevia extract is preferably purified after being water-extracted from stevia leaves. For example, commercially available products can also be used. The stevia extract preferably has a steviol glycoside purity of 80% or more, more preferably 90% or more.
　　本開示の組成物で用いられるステビア系甘味料の配合量は、効果が奏される範囲であれば特に制限はされないが、例えば組成物全体に対して０．００２～０．０２量％程度が挙げられる。なお、当該範囲の上限または下限は、例えば、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、０．０１９質量％であってもよい。例えば当該範囲は、０．００４～０．０１質量％程度であってもよい。
　特に好ましい本開示の組成物の態様としては、例えば、（Ａ）塩化セチルピリジニウムを０．０１～０．１質量％、（Ｂ）塩化ラウリルピリジニウムを０．０１～０．１質量％、（Ｃ）パラオキシ安息香酸メチルを０．０５～０．２質量％、（Ｄ）サッカリンナトリウムを０．００２～０．０２質量％、及び（Ｅ）メントールを０．０１質量％以上、
含有し、且つ（ｉ）メントール含有量が０．０１～０．０５質量％であるか、又は（ｉｉ）さらに（Ｆ）ステビア系甘味料を０．００２～０．０２質量％含有する、液体口腔用組成物が挙げられる。これら（Ａ）～（Ｆ）の各成分の含有量は、例えば上述した範囲で適宜設定することができる。 The amount of the stevia-based sweetener used in the composition of the present disclosure is not particularly limited as long as it is effective, but for example, it is about 0.002 to 0.02% by weight based on the entire composition. mentioned. The upper limit or lower limit of the range is, for example, 0.003, 0.004, 0.005, 0.006, 0.007, 0.008, 0.009, 0.01, 0.011, 0.011. 012, 0.013, 0.014, 0.015, 0.016, 0.017, 0.018, 0.019% by mass. For example, the range may be about 0.004 to 0.01% by mass.
Particularly preferred embodiments of the composition of the present disclosure include, for example, (A) 0.01 to 0.1% by mass of cetylpyridinium chloride, (B) 0.01 to 0.1% by mass of laurylpyridinium chloride, (C ) 0.05 to 0.2% by mass of methyl paraoxybenzoate, (D) 0.002 to 0.02% by mass of sodium saccharin, and (E) 0.01% by mass or more of menthol,
and (i) a menthol content of 0.01 to 0.05% by mass, or (ii) further containing (F) a stevia-based sweetener of 0.002 to 0.02% by mass Oral compositions are included. The content of each of these components (A) to (F) can be appropriately set, for example, within the ranges described above.
　本開示の組成物は常法により製造することができる。また、本開示の組成物の形態としては、液体歯磨剤、洗口剤、ジェル剤等が挙げられる。また、本開示の組成物は、医薬部外品、化粧品、または医薬品として用いることができる。 The composition of the present disclosure can be produced by conventional methods. Forms of the compositions of the present disclosure also include liquid dentifrices, mouthwashes, gels, and the like. In addition, the composition of the present disclosure can be used as a quasi-drug, cosmetic, or pharmaceutical.
　本開示の組成物には、効果を損なわない範囲で、一般に液体口腔用組成物に配合し得る公知の任意成分を、単独で又は２種以上組み合わせて、さらに配合してもよい。 The composition of the present disclosure may further contain known optional components that can generally be contained in liquid oral compositions, singly or in combination of two or more, as long as the effects are not impaired.
　このような公知の任意成分としては、例えば、溶媒の他、界面活性剤、殺菌剤、湿潤剤、甘味剤、防腐剤、着色剤、ｐＨ調整剤、安定化剤、矯味剤、収斂剤、香料、他の薬効成分等が挙げられる。
　溶媒としては、特に制限されず、公知の液体口腔用組成物に用いられる溶媒を用いることができる。例えば、水、エタノール等を用いることができる。液体口腔用組成物においては、このような溶媒の配合量は特に限定はされないものの、組成物調製において残部を全て溶媒とすることもあり得、例えば９９．９１８質量％以下が例示でき、９９．９質量％以下、９９．５質量％以下、９９、９８、９７、若しくは９６質量％以下等も例示できる。 Examples of such known optional ingredients include solvents, surfactants, bactericides, wetting agents, sweeteners, preservatives, colorants, pH adjusters, stabilizers, corrigents, astringents, and perfumes. , and other medicinal ingredients.
The solvent is not particularly limited, and solvents used in known liquid oral compositions can be used. For example, water, ethanol, or the like can be used. In the liquid oral composition, the amount of such a solvent to be blended is not particularly limited, but the balance may be used as the solvent in the preparation of the composition. 9% by mass or less, 99.5% by mass or less, 99, 98, 97, or 96% by mass or less can be exemplified.
　界面活性剤として、例えば、アニオン界面活性剤、ノニオン界面活性剤、または両性イオン界面活性剤を配合することができる。具体的には、アニオン界面活性剤としては、例えば、アルキル硫酸エステル塩、ポリオキシエチレンアルキルエーテル硫酸エステル塩、アルキルスルホコハク酸塩、ポリオキシエチレンアルキルエーテルスルホコハク酸塩、Ｎ－アシルアミノ酸塩、Ｎ－アシルタウリン塩、アルキルエーテルカルボン酸塩、アルキルリン酸塩、ポリオキシエチレンアルキルエーテルリン酸塩、脂肪酸モノグリセライド硫酸塩、アルキルスルホ酢酸塩等が挙げられる。ノニオン界面活性剤としては、例えば、脂肪酸エステル、脂肪酸アルカノールアミド類、ソルビタン脂肪酸エステル、脂肪酸モノグリセライド、ポリグリセリン脂肪酸エステル、ポリオキシエチレンアルキルフェニルエーテル、アルキルグリコシド、セバシン酸ジエチル、ポリオキシエチレン硬化ヒマシ油、脂肪酸ポリオキシエチレンソルビタン等が挙げられる。両性イオン界面活性剤としては、例えば、アルキルジメチルアミノ酢酸ベタイン、アルキルアミドプロピルジメチルアミノ酢酸ベタイン、Ｎ－アシル－Ｎ－カルボキシメチル－Ｎ－ヒドロキシエチルエチレンジアミン、Ｎ－アルキルアミノエチルグリシン等が挙げられる。これらの界面活性剤は、単独または２種以上を組み合わせて配合することができる。その配合量は、通常、組成物全量に対して０．１～５質量％である。 As a surfactant, for example, an anionic surfactant, a nonionic surfactant, or a zwitterionic surfactant can be blended. Specifically, examples of anionic surfactants include alkyl sulfates, polyoxyethylene alkyl ether sulfates, alkyl sulfosuccinates, polyoxyethylene alkyl ether sulfosuccinates, N-acylamino acid salts, N- acyl taurine salts, alkyl ether carboxylates, alkyl phosphates, polyoxyethylene alkyl ether phosphates, fatty acid monoglyceride sulfates, alkyl sulfoacetates and the like. 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, Examples include fatty acid polyoxyethylene sorbitan. Examples of amphoteric surfactants include betaine alkyldimethylaminoacetate, betaine alkylamidopropyldimethylaminoacetate, N-acyl-N-carboxymethyl-N-hydroxyethylethylenediamine, N-alkylaminoethylglycine and the like. These surfactants can be blended singly or in combination of two or more. The blending amount thereof is usually 0.1 to 5% by mass based on the total amount of the composition.
　殺菌剤としては、塩化セチルピリジニウム及び塩化ラウリルピリジニウム以外の殺菌剤、例えば、塩化ベンザルコニウム、塩化ベンゼトニウム、塩酸クロルヘキシジン等のカチオン性殺菌剤、酢酸ｄｌ－α－トコフェロール、コハク酸トコフェロール、またはニコチン酸トコフェロール等のビタミンＥ類、ドデシルジアミノエチルグリシン等の両性殺菌剤、トリクロサン、イソプロピルメチルフェノール等の非イオン性殺菌剤などが挙げられる。これらの殺菌剤は、単独または２種以上を組み合わせて配合することができる。 Bactericides other than cetylpyridinium chloride and laurylpyridinium chloride, e.g., cationic bactericides such as benzalkonium chloride, benzethonium chloride, chlorhexidine hydrochloride, dl-α-tocopherol acetate, tocopherol succinate, or nicotinic acid Examples include vitamin E compounds such as tocopherol, amphoteric fungicides such as dodecyldiaminoethylglycine, and nonionic fungicides such as triclosan and isopropylmethylphenol. These fungicides can be blended singly or in combination of two or more.
湿潤剤として、例えば、ソルビット、エチレングリコール、プロピレングリコール、１，３―ブチレングリコール、ポリプロピレングリコール、キシリット、マルチット、ラクチット、パラチニット、ポリエチレングリコール等が挙げられる。これらの湿潤剤は、単独または２種以上を組み合わせて配合することができる。 Wetting agents include, for example, sorbitol, ethylene glycol, propylene glycol, 1,3-butylene glycol, polypropylene glycol, xylit, maltite, lactit, palatinit, polyethylene glycol and the like. These wetting agents can be blended singly or in combination of two or more.
　甘味剤として、サッカリンナトリウム及びステビア系甘味料以外の甘味剤、例えば、アセスルファームカリウム、ネオヘスペリジルジヒドロカルコン、グリチルリチン、ペリラルチン、タウマチン、アスパルチルフェニルアラニンメチルエステル、ρ－メトキシシンナミックアルデヒド、スクラロース等が挙げられる。これらの甘味剤は、単独または２種以上を組み合わせて配合することができる。 Sweeteners other than sodium saccharin and stevia-based sweeteners, such as acesulfame potassium, neohesperidyl dihydrochalcone, glycyrrhizin, perillartine, thaumatin, aspartylphenylalanine methyl ester, ρ-methoxycinnamic aldehyde, sucralose, etc. mentioned. These sweeteners can be blended singly or in combination of two or more.
防腐剤として、例えば、安息香酸ナトリウム、フェノキシエタノール、塩酸アルキルジアミノエチルグリシン等が挙げられる。これらの防腐剤は、単独または２種以上を組み合わせて配合することができる。 Examples of antiseptics include sodium benzoate, phenoxyethanol, alkyldiaminoethylglycine hydrochloride and the like. These preservatives can be blended singly or in combination of two or more.
ｐＨ調整剤としては、例えば、クエン酸、リン酸、リンゴ酸、ピロリン酸、乳酸、酒石酸、グリセロリン酸、酢酸、硝酸、またはこれらの化学的に可能な塩や水酸化ナトリウム等が挙げられる。これらのｐＨ調製剤は、単独または２種以上を組み合わせて配合することができる。 Examples of pH adjusters include citric acid, phosphoric acid, malic acid, pyrophosphate, lactic acid, tartaric acid, glycerophosphoric acid, acetic acid, nitric acid, or chemically possible salts thereof, sodium hydroxide, and the like. These pH adjusters can be blended singly or in combination of two or more.
安定化剤としては、例えば、エデト酸ナトリウム、チオ硫酸ナトリウム、亜硫酸ナトリウム、塩化ナトリウム、乳酸カルシウム、ラノリン、トリアセチン、ヒマシ油、硫酸マグネシウム等が挙げられる。これらの安定化剤は、単独または２種以上を組み合わせて配合することができる。 Stabilizers include, for example, sodium edetate, sodium thiosulfate, sodium sulfite, sodium chloride, calcium lactate, lanolin, triacetin, castor oil, magnesium sulfate and the like. These stabilizers can be blended singly or in combination of two or more.
矯味剤としては、例えば、チャエキス、チャ乾留液、プロポリスエキス、グルタミン酸ナトリウム等が挙げられる。 Examples of flavoring agents include tea extract, dry distillation of tea, propolis extract, sodium glutamate and the like.
　収れん剤としては、例えば、重曹、乳酸アルミニウム等が挙げられる。 Examples of astringents include sodium bicarbonate and aluminum lactate.
　香料としては、例えば、カルボン、アネトール、サリチル酸メチル、リモネン、オシメン、ｎ－デシルアルコール、シトロネロール、α－テルピネオール、メチルアセテート、シトロネリルアセテート、メチルオイゲノール、シネオール、リナロール、エチルリナロール、チモール、スペアミント油、ペパーミント油、レモン油、オレンジ油、セージ油、ローズマリー油、桂皮油、シソ油、冬緑油、ユーカリ油、などの香料を単独または２種以上を組み合わせて使用することができる。 Examples of fragrances include carvone, anethole, methyl salicylate, limonene, ocimene, n-decyl alcohol, citronellol, α-terpineol, methyl acetate, citronellyl acetate, methyl eugenol, cineol, linalool, ethyl linalool, thymol, spearmint oil, Flavors such as peppermint oil, lemon oil, orange oil, sage oil, rosemary oil, cinnamon oil, perilla oil, wintergreen oil, and eucalyptus oil can be used alone or in combination of two or more.
他の薬効剤としては、フッ化ナトリウム、モノフルオロリン酸ナトリウム、フッ化第一錫等のフッ素化合物；デキストラナーゼ、ムタナーゼ、アミラーゼ、プロテアーゼ、溶菌酵素（リテックエンザイム）等の酵素；トラネキサム酸、ε－アミノカプロン酸、アルミニウムクロルヒドロキシアラントイン、アラントイン、ジヒドロコレステロール、グリチルリチン酸類、グリチルレチン酸、ビサボロール、グリセロリン酸、クロロフィル、グルコン酸銅、塩化ナトリウム、水溶性無機リン酸化合物；酢酸ピリドキシン、アスコルビン酸またはその塩等のビタミン類；アロエ、イチョウ葉、アガリクス、ウーロン茶、カミツレ、カリン、ギムネマ、クマザサ、甜茶、杜仲茶、ドクダミ、ハトムギ、メグスリノキ、ヨモギ、緑茶、ルイボス、レモンバーム、ローズマリー、クラブミン、ラカンカ、シソ、クランベリー、ノコギリソウ、エルダー、リコリス、ハッカ、ユーカリ、ガラナ、カンゾウ、ボダイジュ、ホップ、カカオ、クワ葉、タイム、オウゴン等の植物抽出物が挙げられる。
　なお、本明細書において「含む」とは、「本質的にからなる」と、「からなる」をも包含する（The term "comprising" includes "consisting essentially of” and "consisting of."）。また、本開示は、本明細書に説明した構成要件の任意の組み合わせを全て包含する。
　また、上述した本開示の各実施形態について説明した各種特性（性質、構造、機能等）は、本開示に包含される主題を特定するにあたり、どのように組み合わせられてもよい。すなわち、本開示には、本明細書に記載される組み合わせ可能な各特性のあらゆる組み合わせからなる主題が全て包含される。 Other medicinal agents include fluorine compounds such as sodium fluoride, sodium monofluorophosphate, and stannous fluoride; ε-aminocaproic acid, aluminum chlorohydroxyallantoin, allantoin, dihydrocholesterol, glycyrrhizic acids, glycyrrhetinic acid, bisabolol, glycerophosphate, chlorophyll, copper gluconate, sodium chloride, water-soluble inorganic phosphoric acid compound; pyridoxine acetate, ascorbic acid or its salt Vitamins such as aloe, ginkgo biloba, agaricus, oolong tea, chamomile, quince, gymnema, kumazasa, sweet tea, tochu tea, houttuynia cordata, adlay, megusurinoki, mugwort, green tea, rooibos, lemon balm, rosemary, clubmin, rakanka, perilla , cranberry, yarrow, elder, licorice, mint, eucalyptus, guarana, licorice, bodaiju, hops, cacao, mulberry leaves, thyme, Scutellaria root and other plant extracts.
In this specification, the term "comprising" includes "consisting essentially of" and "consisting of." Also, the present disclosure encompasses any and all combinations of the constituent elements described herein.
Also, the various characteristics (property, structure, function, etc.) described for each of the embodiments of the disclosure described above may be combined in any way to identify subject matter encompassed by the disclosure. That is, the present disclosure encompasses all subject matter consisting of any and all possible combinations of the features described herein.
　以下、例を示して本開示の実施形態をより具体的に説明するが、本開示の実施形態は下記の例に限定されるものではない。 Hereinafter, the embodiments of the present disclosure will be described more specifically with examples, but the embodiments of the present disclosure are not limited to the following examples.
［液体口腔用組成物の使用感評価］
　表１Ａ、表２Ａ、及び表３Ａに示す配合量にて、被検体（各実施例、各比較例、及び各参考例の液体組成物）を常法にて調製した。また、これとは別に、表１Ｂ、表２Ｂ、及び表３Ｂに示す配合量にて、被検体（各実施例、各比較例、及び各参考例の液体組成物）を常法にて調製した。なお、参考例１ａと参考例１ｂは同じ組成であり、参考例２ａと参考例２ｂは同じ組成であり、比較例１ａと比較例１ｂは同じ組成であり、また、比較例９ａと比較例５ｂは同じ組成である。
　５人のモニターに、前記被検体をそれぞれ１０ｍｌ口に含み、２０秒間使用してもらい、使用中の甘味、使用中の苦味、使用直後の苦味、および使用１分後の苦味について次の５段階の評価基準により評価した。 [Usability evaluation of liquid oral composition]
Test samples (liquid compositions of Examples, Comparative Examples, and Reference Examples) were prepared by a conventional method at the blending amounts shown in Tables 1A, 2A, and 3A. Separately, test samples (liquid compositions of Examples, Comparative Examples, and Reference Examples) were prepared by a conventional method at the blending amounts shown in Tables 1B, 2B, and 3B. . Incidentally, Reference Examples 1a and 1b have the same composition, Reference Examples 2a and 2b have the same composition, Comparative Examples 1a and 1b have the same composition, and Comparative Examples 9a and 5b. have the same composition.
Five monitors each held 10 ml of the test subject in their mouth and used it for 20 seconds, and the following 5 levels were used for sweetness during use, bitterness during use, bitterness immediately after use, and bitterness 1 minute after use. was evaluated according to the evaluation criteria of
［甘味の評価基準］
５点：甘味が全く気にならない、４点：甘味がほとんど気にならない、３点：甘味がやや気になる、２点：甘味が気になる、１点：甘味がとても気になる
［苦味の評価基準］
５点：苦味を感じない、４点：苦味をほとんど感じない、３点：苦味を感じる、２点：強い苦味を感じる、１点：とても強い苦味を感じる [Evaluation criteria for sweetness]
5 points: not bothered by sweetness at all, 4 points: hardly bothered by sweetness, 3 points: slightly worried about sweetness, 2 points: worried about sweetness, 1 point: very worried about sweetness [bitter taste] evaluation criteria]
5 points: no bitterness, 4 points: almost no bitterness, 3 points: bitterness, 2 points: strong bitterness, 1 point: very strong bitterness
　甘味、苦味の各項目、および総合評価について、５人の評価値の平均値が３．５点以上を◎、３．０点以上３．５点未満を○、２．０点以上３．０点未満を△、２．０点未満を×とした。その結果を表２Ａ、表２Ｂ、表３Ａ、及び表３Ｂにあわせて示した。なお、総合評価は甘味と苦味の評価値の平均値により算出し、甘味および苦味のいずれか１つでも評価に×が付いたものは×とした。 For each item of sweetness, bitterness, and overall evaluation, the average value of the evaluation values of 5 people is 3.5 points or more, ⊚, 3.0 points or more and less than 3.5 points, 2.0 points or more and 3.0 points. A score of less than Δ was given, and a score of less than 2.0 was given as ×. The results are shown in Tables 2A, 2B, 3A, and 3B. The overall evaluation was calculated from the average value of the evaluation values of sweetness and bitterness, and the evaluation with x for either sweetness or bitterness was rated as x.
Figure JPOXMLDOC01-appb-T000001
Figure JPOXMLDOC01-appb-T000001
Figure JPOXMLDOC01-appb-T000002
Figure JPOXMLDOC01-appb-T000002
Figure JPOXMLDOC01-appb-T000003
Figure JPOXMLDOC01-appb-T000003
Figure JPOXMLDOC01-appb-T000004
Figure JPOXMLDOC01-appb-T000004
Figure JPOXMLDOC01-appb-T000005
Figure JPOXMLDOC01-appb-T000005
Figure JPOXMLDOC01-appb-T000006
Figure JPOXMLDOC01-appb-T000006
　表２Ａ、表２Ｂ、表３Ａ、及び表３Ｂに示した各例のうち、実施例はいずれも、甘味、苦味の各項目のいずれについても、良好な結果を示した。 Of the examples shown in Table 2A, Table 2B, Table 3A, and Table 3B, all of the examples showed good results for each item of sweetness and bitterness.
　本開示の組成物の処方例を表４Ａ及び表４Ｂに示す。なお各処方の配合量は特に記載のない限り質量％を示す。 Formulation examples of the composition of the present disclosure are shown in Tables 4A and 4B. In addition, the compounding quantity of each prescription shows the mass % unless otherwise specified.
Figure JPOXMLDOC01-appb-T000007
Figure JPOXMLDOC01-appb-T000007
Figure JPOXMLDOC01-appb-T000008
Figure JPOXMLDOC01-appb-T000008

Claims (3)

  1. （Ａ）塩化セチルピリジニウムを０．０１～０．１質量％、
    （Ｂ）塩化ラウリルピリジニウムを０．０１～０．１質量％、
    （Ｃ）パラオキシ安息香酸メチルを０．０５～０．２質量％、
    （Ｄ）サッカリンナトリウムを０．００２～０．０２質量％、及び
    （Ｅ）メントールを０．０１質量％以上、
    含有し、且つ
    （ｉ）メントール含有量が０．０１～０．０５質量％であるか、又は
    （ｉｉ）さらに（Ｆ）ステビア系甘味料を０．００２～０．０２質量％含有する、
    液体口腔用組成物。     (A) 0.01 to 0.1% by mass of cetylpyridinium chloride;
    (B) 0.01 to 0.1% by mass of laurylpyridinium chloride;
    (C) 0.05 to 0.2% by mass of methyl paraoxybenzoate,
    (D) 0.002 to 0.02% by mass of sodium saccharin, and (E) 0.01% by mass or more of menthol,
    and (i) a menthol content of 0.01 to 0.05% by mass, or (ii) further containing (F) a stevia-based sweetener of 0.002 to 0.02% by mass,
    A liquid oral composition.
  2. （Ａ）塩化セチルピリジニウムを０．０１～０．１質量％、
    （Ｂ）塩化ラウリルピリジニウムを０．０１～０．１質量％、
    （Ｃ）パラオキシ安息香酸メチルを０．０５～０．２質量％、
    （Ｄ）サッカリンナトリウムを０．００２～０．０２質量％、及び
    （Ｅ）メントールを０．０１～０．０５質量％、
    含有する、
    液体口腔用組成物。     (A) 0.01 to 0.1% by mass of cetylpyridinium chloride;
    (B) 0.01 to 0.1% by mass of laurylpyridinium chloride;
    (C) 0.05 to 0.2% by mass of methyl paraoxybenzoate,
    (D) 0.002 to 0.02% by weight of sodium saccharin, and (E) 0.01 to 0.05% by weight of menthol,
    contains,
    A liquid oral composition.
  3. （Ａ）塩化セチルピリジニウムを０．０１～０．１質量％、
    （Ｂ）塩化ラウリルピリジニウムを０．０１～０．１質量％、
    （Ｃ）パラオキシ安息香酸メチルを０．０５～０．２質量％、
    （Ｄ）サッカリンナトリウムを０．００２～０．０２質量％、
    （Ｅ）メントールを０．０１質量％以上、および
    （Ｆ）ステビア系甘味料を０．００２～０．０２質量％、
    含有する
    液体口腔用組成物。     (A) 0.01 to 0.1% by mass of cetylpyridinium chloride;
    (B) 0.01 to 0.1% by mass of laurylpyridinium chloride;
    (C) 0.05 to 0.2% by mass of methyl paraoxybenzoate,
    (D) 0.002 to 0.02% by mass of sodium saccharin;
    (E) 0.01% by mass or more of menthol, and (F) 0.002 to 0.02% by mass of a stevia-based sweetener,
    A liquid oral composition comprising:
PCT/JP2022/039865 2021-10-28 2022-10-26 Liquid composition for oral cavity WO2023074725A1 (en)

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JP2021-176454 2021-10-28
JP2021176454A JP2023065995A (en) 2021-10-28 2021-10-28 Liquid composition for oral cavity
JP2021-176455 2021-10-28

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Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2000256155A (en) * 1999-03-09 2000-09-19 Sunstar Inc Oral composition
JP2003095904A (en) * 2001-09-26 2003-04-03 Asahi Kasei Corp Method for producing composition for oral cavity containing cellulose
JP2004339180A (en) * 2003-05-19 2004-12-02 Asahi Kasei Chemicals Corp Composition for oral cavity
JP2006199661A (en) * 2005-01-24 2006-08-03 Sunstar Inc Coaggregation inhibitor
JP2006312592A (en) * 2005-05-06 2006-11-16 Sunstar Inc Composition for oral cavity
JP2006347986A (en) * 2005-06-17 2006-12-28 Sunstar Inc Composition for oral cavity
JP2011140454A (en) * 2010-01-06 2011-07-21 Sunstar Inc Composition for oral cavity
JP2017125072A (en) * 2017-04-25 2017-07-20 サンスター株式会社 Transparent liquid composition for oral cavity

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2000256155A (en) * 1999-03-09 2000-09-19 Sunstar Inc Oral composition
JP2003095904A (en) * 2001-09-26 2003-04-03 Asahi Kasei Corp Method for producing composition for oral cavity containing cellulose
JP2004339180A (en) * 2003-05-19 2004-12-02 Asahi Kasei Chemicals Corp Composition for oral cavity
JP2006199661A (en) * 2005-01-24 2006-08-03 Sunstar Inc Coaggregation inhibitor
JP2006312592A (en) * 2005-05-06 2006-11-16 Sunstar Inc Composition for oral cavity
JP2006347986A (en) * 2005-06-17 2006-12-28 Sunstar Inc Composition for oral cavity
JP2011140454A (en) * 2010-01-06 2011-07-21 Sunstar Inc Composition for oral cavity
JP2017125072A (en) * 2017-04-25 2017-07-20 サンスター株式会社 Transparent liquid composition for oral cavity

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