WO2022145161A1 - Composition pour cavité buccale - Google Patents

Composition pour cavité buccale Download PDF

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Publication number
WO2022145161A1
WO2022145161A1 PCT/JP2021/043850 JP2021043850W WO2022145161A1 WO 2022145161 A1 WO2022145161 A1 WO 2022145161A1 JP 2021043850 W JP2021043850 W JP 2021043850W WO 2022145161 A1 WO2022145161 A1 WO 2022145161A1
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Prior art keywords
oral composition
mass
component
composition according
content
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PCT/JP2021/043850
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English (en)
Japanese (ja)
Inventor
将登 平泉
駿太 石井
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ライオン株式会社
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Priority to CN202180087598.0A priority Critical patent/CN116806140A/zh
Publication of WO2022145161A1 publication Critical patent/WO2022145161A1/fr

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • A61K31/05—Phenols
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4425—Pyridinium derivatives, e.g. pralidoxime, pyridostigmine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • 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
    • A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/41—Amines
    • 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
    • A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/42—Amides
    • 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
    • A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/44—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
    • 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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/08—Solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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 invention relates to an oral composition.
  • the bactericidal agent contained in the oral composition such as dentifrice is an important component that reduces the number of pathogenic bacteria in the oral cavity and is effective in suppressing bad breath, preventing dental caries, preventing periodontal disease, and the like.
  • the disinfectant has the bitterness peculiar to the disinfectant. Due to this bitterness, even if a refreshing agent such as menthol is blended, a refreshing sensation is not felt at the start of use of the oral composition, and the bitterness persists for a certain period of time after the start of use. The usability was significantly impaired. Therefore, various measures have been taken so far to mask the bitterness derived from the disinfectant.
  • Patent Document 1 relates to an oral composition containing a bactericidal agent (isopropylmethylphenol), polyvinylpyrrolidone, a fragrance component (at least one selected from 3-octanol, 3-octyl acetate and 3-octanone) and a surfactant.
  • a bactericidal agent isopropylmethylphenol
  • polyvinylpyrrolidone polyvinylpyrrolidone
  • a fragrance component at least one selected from 3-octanol, 3-octyl acetate and 3-octanone
  • a surfactant at least one selected from 3-octanol, 3-octyl acetate and 3-octanone
  • Patent Document 2 describes a dentifrice composition containing an ingredient effective for preventing periodontal disease (dextranase, tranexamic acid and isopropylmethylphenol), an alkyl sulfate and a fragrance ingredient (menthol, anethole and eugenol and / or thyme oil). Regarding. Patent Document 2 discloses that the complex sarcasm after toothpaste is masked by containing a perfume component in a specific ratio.
  • Patent Document 3 describes a bactericidal agent (cationic bactericidal agent), a moisturizing / antibacterial agent (alkanediol), and a cooling sensation agent (3-1-methoxypropane-1,2-diol and / or N-substituted-p-menthane-. 3-Carboxamide). Patent Document 3 discloses that the combined use of a moisturizing / antibacterial agent and a cooling sensation agent masks the off-taste derived from a bactericidal agent immediately after the oral composition is applied into the oral cavity.
  • Patent Document 4 relates to an oral composition containing a bactericide and a fragrance (Japanese mentha oil and N- (2- (2-pyridinyl) ethyl) -2-isopropyl-5-methylcyclohexanecarboxamide).
  • a bactericide Japanese mentha oil and N- (2- (2-pyridinyl) ethyl) -2-isopropyl-5-methylcyclohexanecarboxamide.
  • the bitterness derived from the bactericide is masked after mouthwash by using mentha oil and N- (2- (2-pyridinyl) ethyl) -2-isopropyl-5-methylcyclohexanecarboxamide in combination. Is disclosed.
  • Patent Document 1-4 does not disclose the oral composition from the viewpoint of sustaining the refreshing sensation and the effect of suppressing bitterness at the start of use.
  • the present invention has been made in view of the above circumstances, and has a refreshing sensation at the start of use, and is a bactericide after a certain period of time has elapsed from the start of use to the time after use (for example, in the case of a dentifrice, from the start of dentifrice to after dentifrice). It is an object of the present invention to provide an oral composition capable of suppressing and sustaining the derived bitterness.
  • the present invention provides the following [1] to [12].
  • [1] (A) disinfectant, (B) ethyl-3- (p-menthane-3-carboxamide) acetate and N- (2-hydroxy-2-phenylethyl) -2-isopropyl-5,5-dimethyl
  • An oral composition containing at least one selected from the group consisting of cyclohexane-1-carboxamide.
  • the component (A) is one or more bactericidal agents selected from the group consisting of a cationic bactericidal agent, a nonionic bactericidal agent and an anionic bactericidal agent.
  • the component (A) is one or more bactericides selected from the group consisting of quaternary ammonium salts, biguanide bactericides, phenol bactericides, cineole and acylsarcosin salts, [1] or [2]. ]
  • the oral composition according to. [4] The oral composition according to any one of [1] to [3], wherein the content of the component (A) is 0.001 to 0.5% by mass with respect to 100% by mass of the oral composition. thing.
  • [5] The oral composition according to any one of [1] to [4], wherein the content of the component (B) is 0.00001 to 0.1% by mass with respect to 100% by mass of the oral composition. thing.
  • a nonionic surfactant selected from the group consisting of polyoxyethylene hydrogenated castor oil, polyoxyethylene alkyl ether, polyglycerin fatty acid ester, and polyoxyethylene polyoxypropylene copolymer as the component (C).
  • the oral composition according to [6] which is an agent.
  • an oral composition that has a refreshing sensation at the start of use and can suppress and sustain the bitterness derived from the bactericidal agent for a certain period of time after the start of use.
  • the oral composition of the present invention contains the following components (A) and (B), and preferably further contains one or both of the components (C) and (D).
  • the content of each component is based on the amount of each component charged at the time of manufacturing a composition.
  • the component (A) is a bactericidal agent. By containing the component (A), a bactericidal effect can be exhibited.
  • the component (A) examples include a cationic bactericidal agent, a nonionic bactericidal agent and an anionic bactericidal agent.
  • the component (A) is preferably one or more fungicides selected from the group consisting of cationic fungicides, nonionic fungicides and anionic fungicides.
  • a quaternary ammonium salt or a biguanide disinfectant is preferable, and for example, a quaternary ammonium salt such as an alkylpyridinium salt, a benzyl long chain alkyl short chain dialkylammonium salt, or a long chain alkyl short chain trialkylammonium salt is preferable.
  • the component (A) includes, for example, benzethonium chloride, benzalkonium chloride, depotassium chloride, cetylpyridinium chloride, stearyldimethylbenzylammonium chloride, lauryltrimethylammonium chloride, myristyltrimethylammonium chloride, cetyltrimethylammonium chloride, and the like.
  • examples thereof include stearyltrimethylammonium chloride, chlorhexidine, chlorhexidine hydrochloride, chlorhexidine gluconate, and chlorhexidine acetate.
  • the nonionic bactericide is preferably a phenolic bactericide, cineole, and examples thereof include isopropylmethylphenol, hinokithiol, triclosan, thymol, thyme oil, cy1,8-cineole, and eucalyptol oil.
  • isopropylmethylphenol and hinokitiol are preferable as the nonionic bactericidal agent.
  • an acylsarcosine salt having an acyl group for example, an acyl group having 10 to 18 carbon atoms
  • an alkali metal salt such as a sodium salt
  • sodium lauroylsarcosine is particularly preferable.
  • the component (A) is preferably one or more bactericides selected from the group consisting of quaternary ammonium salts, biguanide bactericides, phenol bactericides, cineole and acylsarcosin salts. These may be used alone or in combination of two or more.
  • the lower limit of the content of the component (A) is the entire oral composition (100% by mass) from the viewpoint of exerting a bactericidal effect without strongly expressing the bitterness derived from the bactericidal agent (hereinafter, simply referred to as bitterness). On the other hand, it is preferably 0.001% by mass or more, and more preferably 0.005% by mass or more. Thereby, a good bactericidal effect can be obtained.
  • the upper limit is preferably 0.5% by mass or less. Thereby, the expression of bitterness can be suppressed. Therefore, the content of the component (A) is preferably 0.001 to 0.5% by mass, and more preferably 0.005 to 0.5% by mass.
  • the content of the cationic bactericide is 0.001 to 0.5% by mass with respect to the entire oral composition (100% by mass). It is preferably 0.005 to 0.2% by mass, more preferably 0.005 to 0.2% by mass.
  • the content of the nonionic bactericidal agent is preferably 0.005 to 0.2% by mass with respect to the entire oral composition (100% by mass).
  • the content of the anionic bactericidal agent is preferably 0.05 to 0.5% by mass with respect to the entire oral composition (100% by mass).
  • the component (B) consists of ethyl-3- (p-menthane-3-carboxamide) acetate and N- (2-hydroxy-2-phenylethyl) -2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide.
  • One or more species selected from the group are selected from the group.
  • the component (B) may be used alone or in combination of two, but may contain N- (2-hydroxy-2-phenylethyl) -2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide. preferable. As a result, the effect of suppressing and sustaining bitterness can be further improved from the start of use to the lapse of a certain period of time after use.
  • the lower limit of the content of the component (B) is preferably 0.00001% by mass or more, more preferably 0.00005% by mass or more, based on the entire oral composition (100% by mass). As a result, it is possible to exert the effect of suppressing and sustaining the bitterness from the start of use to the lapse of a certain period of time after use.
  • the upper limit of the content of the component (B) is preferably 0.1% by mass or less, more preferably 0.01% by mass or less, and particularly preferably 0.005, based on the entire oral composition (100% by mass). It is less than mass%. This makes it possible to suppress the expression of irritation in the oral cavity and the decrease in the flavor expression of fragrances (fragrances other than cooling sensation agents). That is, the content of the component (B) is preferably 0.00001 to 0.1% by mass, more preferably 0.00005 to 0.005% by mass, based on the entire oral composition (100% by mass). Is.
  • the component (C) is a nonionic surfactant.
  • the component (C) it is possible to suppress a decrease in the refreshing sensation at the start of use, and to impart a sustained effect of suppressing bitterness over a certain period of time after the start of use.
  • component (C) examples include polyoxyethylene alkyl ether, polyoxyethylene hydrogenated castor oil, sorbitan fatty acid ester, polyoxyethylene sorbitan fatty acid ester (eg, polyoxyethylene sorbitan monostearate), alkyrrole amide, and polyoxy.
  • Ethylene fatty acid esters polyoxyethylene alkenyl ethers, polyglycerin fatty acid esters, sucrose fatty acid esters (eg, maltose fatty acid esters), sugar alcohol fatty acid esters (eg, multitoll fatty acid esters, lactitol fatty acid esters), fatty acid diethanolamides (eg,) Lauric acid mono or diethanolamide), polyoxyethylene polyoxypropylene copolymer, polyoxyethylene polyoxypropylene fatty acid ester, and the like.
  • the number of carbon atoms in the alkyl chain of the polyoxyethylene alkyl ether is usually 14 to 18, and the average number of moles of ethylene oxide added is usually 5 to 30 mol.
  • the average number of moles of ethylene oxide added to the polyoxyethylene hydrogenated castor oil is usually 20 to 100 mol, preferably 20 to 60 mol.
  • the number of carbon atoms of the fatty acid of the sorbitan fatty acid ester is usually 12 to 18.
  • the number of carbon atoms of the fatty acid of the polyoxyethylene sorbitan fatty acid ester is usually 16 to 18, and the average number of moles of ethylene oxide added is usually 10 to 40 mol.
  • the number of carbon atoms in the alkyl chain of the alkylolamide is usually 12 to 14.
  • nonionic surfactant one or more nonionic surfactants selected from the group consisting of polyoxyethylene hydrogenated castor oil, polyoxyethylene alkyl ether, polyglycerin fatty acid ester and polyoxyethylene polyoxypropylene copolymer. Is preferable. These may be used alone or in combination of two or more.
  • the lower limit of the content of the component (C) is preferably 0.1% by mass or more, more preferably 0.3% by mass or more, based on the entire oral composition (100% by mass). Thereby, the effect of suppressing bitterness can be satisfactorily exhibited.
  • the upper limit is preferably 2% by mass or less, more preferably 1% by mass or less, and particularly preferably 0.8% by mass or less, based on the entire oral composition (100% by mass).
  • the content of the component (C) is preferably 0.1 to 2% by mass, more preferably 0.3 to 1% by mass, still more preferably, with respect to the entire oral composition (100% by mass). It is 0.3 to 0.8% by mass.
  • the component (D) is a refreshing agent.
  • a refreshing feeling can be imparted and the feeling of use during use can be improved.
  • the refreshing agent as the component (D) include menthol and carvone. Both menthol and carvone can be blended as a compound. Essential oils containing either or both of menthol and carvone can also be used. Examples of the essential oil include peppermint oil, Japanese peppermint oil, and spearmint oil.
  • the component (D) may be used alone or in combination of two or more. Of these, menthol and one or both of the essential oils containing menthol are preferably contained because a refreshing feeling can be imparted.
  • the content of the component (D) is the content of either one or both of menthol and carboxylic (when essential oil is used, the amount including menthol and carboxylic in the essential oil) as the whole oral composition (100).
  • (% by mass) it is preferably 0.001% by mass or more, and more preferably 0.01% by mass or more.
  • the upper limit is usually 1.5% by mass or less, preferably 1.2% by mass or less, and more preferably 0.8% by mass or less. Therefore, it is preferably 0.001 to 1.5% by mass, more preferably 0.001 to 1.2% by mass, and further preferably 0.01 to 0.8% by mass.
  • the oral composition of the present embodiment may contain an arbitrary component in addition to the components (A) to (D) already described, as long as the effect of the present invention is not impaired.
  • Optional components include, for example, abrasives, medicinal components, surfactants other than component (C), wetting agents, binders, sweeteners, preservatives, pH regulators, solvents, oily components, colorants (pigments).
  • component (C) examples include fragrances other than the component.
  • the abrasive may be either an inorganic abrasive or an organic abrasive.
  • the inorganic abrasive include abrasive silica such as precipitate silica, aluminosilicate, zirconosilicate, crystalline zirconium silicate, and titanium-binding silica; calcium dibasic phosphate / dihydrate or anhydrous, calcium primary phosphate.
  • Calcium phosphate-based compounds such as tertiary calcium phosphate and calcium pyrophosphate
  • calcium carbonate-based abrasives such as calcium carbonate
  • calcium-based abrasives other than carbonic acid / phosphoric acid such as calcium hydroxide and calcium sulfate
  • aluminum oxide, aluminum hydroxide, Aluminum-based materials such as alumina
  • Silica-based materials such as silicic acid anhydride, zeolite, and zirconium silicate
  • Magnesium-based materials such as magnesium carbonate and tertiary magnesium phosphate
  • Apatite-based materials such as hydroxyapatite, fluoroapatite, and calcium-deficient apatite.
  • Titanium-based materials such as titanium dioxide, mica titanium, and titanium oxide; minerals such as bentonite can be mentioned.
  • organic abrasive include polymethylmethacrylate and synthetic resin-based abrasives. Of these, silica-based abrasives are preferable.
  • the content of the abrasive is usually 70% by mass or less, preferably 50% by mass or less, and more preferably 8 to 50% by mass with respect to the entire oral composition (100% by mass).
  • medicinal ingredients include enzymes such as dextranase, mutanase, amylases, proteases, and lytec enzymes; fluorides such as sodium fluoride, sodium monofluorophosphate, and tin fluoride; ⁇ -aminocaproic acid, allantin, and tranexamic acid.
  • enzymes such as dextranase, mutanase, amylases, proteases, and lytec enzymes
  • fluorides such as sodium fluoride, sodium monofluorophosphate, and tin fluoride
  • ⁇ -aminocaproic acid allantin, and tranexamic acid.
  • Anti-inflammatory agents such as glycyrrhetinate (eg, glycyrrhetin dipotassium salt), glycyrrhetinic acid, glycyrrhetinic acid derivative (eg, stearyl glycyrrhetinate), allantinchlorhydroxyaluminum, azulene, dihydrocholesterol; zinc salt, copper salt, tin salt Metal salts such as; Toothstone preventive agents such as condensed phosphate and ethanehydroxydiphosphonate; Blood flow enhancers such as vitamin E (for example, tocopherol acetate); Hypersensitivity inhibitors such as potassium nitrate, aluminum lactate, strontium chloride, etc.
  • glycyrrhetinate eglycyrrhetin dipotassium salt
  • glycyrrhetinic acid eglycyrrhetinic acid derivative (eg, stearyl
  • Coating agents such as hydroxyethyl cellulose dimethyldiallyl ammonium chloride; astringents such as vitamin C (eg, ascorbic acid or salts thereof), lysozyme chloride, sodium chloride, etc .; water-soluble copper compounds such as copper chlorophyll, copper gluconate; tooth stone preventive agents Amino acids such as alanine, glycine and proline; plant extracts such as thyme, ginger, chow and hamamelis; caropeptides; polyvinylpyrrolidone and the like. These may be used alone or in combination of two or more.
  • the content of the medicinal component can be appropriately set as an effective amount according to a conventional method.
  • the arbitrary surfactant is a surfactant other than the component (C), and is an anionic surfactant and an amphoteric surfactant.
  • anionic surfactant examples include alkyl sulfates, acyl amino acid salts, acyl taurine salts, ⁇ -olefin sulfonates, hydrogenated coconut fatty acid monoglyceride monosulfates, and lauryl sulfoacetates.
  • the alkyl group and the acyl group may be either a straight chain or a branched chain, and may be saturated or unsaturated, and the number of carbon atoms thereof is usually 10 to 20, preferably 12 to 18, and more preferably 12 to 18. It is 14.
  • the salt can be selected from pharmacologically acceptable salts.
  • Pharmacologically acceptable salts include, for example, base addition salts and amino acid salts.
  • inorganic base salts such as sodium salt, potassium salt, calcium salt, magnesium salt and ammonium salt
  • organic base salts such as triethylammonium salt, triethanolammonium salt, pyridinium salt and diisopropylammonium salt
  • arginine salt and the like Basic amino acid salts of.
  • inorganic base salts are preferred, alkali metal salts (eg, sodium salts, potassium salts) or ammonium salts are more preferred, and sodium salts are even more preferred.
  • alkyl sulfate examples include lauryl sulfate (sodium lauryl sulfate) and myristyl sulfate.
  • acyl amino acid salt examples include acyl glutamates such as lauroyl glutamate, myristoyl glutamate and palmitoyl glutamate; acylglycine salts such as N-lauroyl-N-methylglycine salt and cocoyl glycine salt; N-lauroyl- ⁇ -.
  • acyl taurine salt examples include lauroylmethyl taurine salt, N-methyl-N-acyl taurine salt, and N-cocoyl methyl taurine salt.
  • ⁇ -olefin sulfonate examples include ⁇ -olefin sulfonate having 12 to 18 carbon atoms such as tetradecene sulfonate.
  • anionic surfactants include, for example, hydrogenated coconut fatty acid monoglyceride sodium monosulfate, sodium lauryl sulfoacetate.
  • the anionic surfactant preferably contains a sulfonic acid group from the viewpoint of foaming and good foam quality, and lauryl sulfate and tradecene sulfonate are more preferable.
  • the content of the anionic surfactant is preferably 0.1 to 2.5% by mass, more preferably 0.6 to 2.5% by mass, still more preferably 1 to 2.5% by mass of the entire oral composition. %.
  • amphoteric surfactant examples include betaine-type amphoteric surfactants such as alkyldimethylaminoacetic acid betaine (eg, lauryldimethylaminoacetic acid betaine) and fatty acid amide propyldimethylaminoacetic acid betaine (eg, cocamidopropyl betaine); N-.
  • alkyldimethylaminoacetic acid betaine eg, lauryldimethylaminoacetic acid betaine
  • fatty acid amide propyldimethylaminoacetic acid betaine eg, cocamidopropyl betaine
  • Fatty acid acyl-N-carboxymethyl-N-hydroxyethylethylenediamine salt eg, N-palm oil fatty acid acyl-N-carboxymethyl-N-hydroxyethyl imidazolinium betaine), coconut oil fatty acid imidazolinium betaine, 2-alkyl
  • imidazoline-type amphoteric surfactants such as -N-carboxymethyl-N-hydroxyethyl imidazolinium betaine
  • alkyl betaines such as lauryldimethylaminoacetic acid betaine.
  • the cationic surfactant include an alkylammonium salt and an alkylbenzylammonium salt.
  • the content of the amphoteric tenside is preferably 0.1 to 2% by mass, more preferably 0.2 to 1.5% by mass, still more preferably 0.3 to 1% by mass based on the total oral composition. ..
  • the content of the surfactant is preferably 3% by mass or less, more preferably 2% by mass or less, and 0.1 to 3% by mass, based on the entire oral composition (100% by mass). It is preferably mass%, particularly 0.3 to 2 mass%.
  • the wetting agent examples include sugar alcohols and polyhydric alcohols other than sugar alcohols.
  • sugar alcohol examples include sorbitol (sorbitol), erythritol, maltitol, lactitol, xylitol and the like.
  • polyhydric alcohols other than sugar alcohols include glycerin; glycols such as ethylene glycol, propylene glycol, dipropylene glycol, butylene glycol, and polyethylene glycol (PEG); and reduced starch saccharified products.
  • polyethylene glycol for example, polyethylene glycol having an average molecular weight of 150 to 6000 is preferable, and polyethylene glycol having an average molecular weight of 190 to 630 (PEG200, PEG300, PEG400, PEG600) is preferable.
  • the average molecular weight is the average molecular weight described in the Quasi-drug Raw Material Standard 2006.
  • the content of the wetting agent is usually 40% by mass or less, preferably 1 to 30% by mass, based on the entire oral composition (100% by mass).
  • the viscosity of the oral composition can be optimized, and the shape retention and usability can be further improved.
  • any suitable organic binder conventionally known for example, a polysaccharide, a cellulosic binder (for example, carboxymethyl cellulose (CMC), hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropylmethyl cellulose, methyl cellulose, cation) Celluloseized cellulose, etc.), other polysaccharide thickeners (eg, xanthan gum, gua gum, gellan gum, tragant gum, karaya gum, arabiya gum, locust bean gum, carrageenan, sodium alginate), synthetic water-soluble polymers (eg, sodium polyacrylate, etc.) Cardovinyl polymer, polyvinylpyrrolidone, polyvinyl alcohol, propylene glycol alginate) can be mentioned. Further, an inorganic binder such as thickening silica and aluminum silicate can be contained.
  • CMC carboxymethyl cellulose
  • hydroxyethyl cellulose hydroxypropyl cellulose,
  • the content of the organic binder is preferably 0 to 3% by mass, more preferably 0.1 to 2% by mass, based on the entire oral composition (100% by mass).
  • the content of the inorganic binder is preferably 0 to 10% by mass, more preferably 1 to 8% by mass.
  • the feeling of use can be further improved.
  • the sweetener include xylitol, erythritol, maltitol, saccharin, saccharin sodium, aspartame, stebioside, stevia extract, paramethoxycinnamic aldehyde, neohesperidin dihydrochalcone, perillartine, glycyrrhizin, thaumatin, aspartame phenylalanine methyl ester. ..
  • the above-exemplified sweetener may be used alone or in combination of two or more.
  • the antiseptic power of the preparation can be ensured.
  • preservative examples include paraoxybenzoic acid ester (for example, methyl paraoxybenzoate, ethyl paraoxybenzoate, butyl paraoxybenzoate), and sodium benzoate.
  • the preservative may be used alone or in combination of two or more.
  • the pH stability of the pharmaceutical product can be ensured.
  • Examples of the pH adjuster include organic acids such as phthalic acid, citric acid, succinic acid, acetic acid, fumaric acid, malic acid and lactic acid, or salts thereof (sodium citrate) and inorganic acids such as phosphoric acid (orthoric acid). Acids or hydroxides thereof such as salts thereof (eg, potassium salt, sodium salt and ammonium salt), sodium hydroxide, potassium hydroxide and the like can be mentioned.
  • Examples of the inorganic acid salt include disodium hydrogen phosphate and sodium dihydrogen phosphate.
  • the content of the pH adjuster can usually be such that the pH of the oral composition after addition is 5 to 9, preferably 6 to 8.5.
  • the pH value usually means a value at 25 ° C. and 3 minutes after the start of measurement.
  • the pH value can be measured using, for example, a pH meter (model number Hm-30S) manufactured by Toa Denpa Kogyo Co., Ltd.
  • the solvent examples include water (purified water), ethanol and the like, and water is preferable.
  • water purified water
  • ethanol ethanol
  • water is preferable.
  • the solvent one type may be used alone or two or more types may be used in combination.
  • oily component examples include hydrocarbons such as squalane, liquid paraffin, vaseline, and microcrystalin wax; and having 8 carbon atoms such as higher alcohols (eg, lauryl alcohol, cetyl alcohol, cetostearyl alcohol, oleyl alcohol, and isostearyl alcohol). ⁇ 22 alcohols); higher fatty acids (eg, fatty acids with 8 to 22 carbon atoms such as lauric acid, myristic acid, oleic acid, isostearic acid), vegetable oils such as olive oil, castor oil, palm oil; Examples include fatty acid esters.
  • the colorant examples include natural pigments such as Benibana red pigment, Kuchinashi yellow element, Kuchinashi blue pigment, perilla pigment, red koji pigment, red cabbage pigment, carrot pigment, hibiscus pigment, cacao pigment, spirulina blue pigment, and tamarind pigment.
  • Legal dyes such as Red No. 2, Red No. 3, Red No. 104, Red No. 105, Red No. 106, Red No. 227, Yellow No. 4, Yellow No. 5, Green No. 3, Blue No. 1, Riboflavin, Copper Chlorophine Sodium , Titanium dioxide and the like.
  • the content thereof is preferably 0.00001 to 3% by mass with respect to the entire oral composition.
  • fragrances other than the component (D) include anis oil, cassia oil, winter green oil, mastic oil, neroli oil (orange flower oil), lemongrass oil, jasmine oil, rose oil, iris oil, clove oil, and sage.
  • Oil cardamon oil, rosemary oil, laurel oil, camomill oil, basil oil, majorum oil, lemon oil, orange oil, lime oil, yuzu oil, nutmeg oil, lavender oil, paracress oil, vanilla oil, katsura oil, piment oil , Katsura leaf oil, perilla oil, winter green oil and other natural essential oils; cinnamic aldehyde, anetol, methylsalicylate, eugenol, linalol, limonen, menthon, mentholacetate, citral, decanal, camphor, borneol, pinen, spirantol, n-decyl Fragrance components contained in the above natural essential oils such as alcohol, citronellol, ⁇ -terpineol, citronellyl acetate, ethyllinalol, varinline; ethyl acetate, ethyl butyrate, isoamyl acetate, hex
  • Fragrance components such as glycidate, benzaldehyde, vanillin, ethyl vaniline, flaneol; and various blended flavors such as mint-based, fruit-based, and herb-based, which are a combination of several fragrance components and natural essential oils.
  • the above-exemplified fragrance may be used alone or in combination of two or more.
  • optional ingredients examples include polyisobutylene, polybutadiene, urethane, silicon, and natural rubber.
  • the content of these other optional components can be appropriately set as long as the effect of the present invention is not impaired.
  • the oral composition of the present invention can be an oral preparation such as a dentifrice, a mouthwash, a spray, a coating agent, a patch, or an oral dissolving agent.
  • the dosage form of the oral composition can be appropriately selected depending on the usage form, and is not particularly limited.
  • the dosage form for example, it can be prepared in the form of a paste, a liquid or the like, and if it is a dentifrice, it can be prepared as a dentifrice, a gel-like dentifrice, a liquid dentifrice, a liquid dentifrice, or a dentifrice.
  • the method for producing the oral composition is not particularly limited, and can be prepared by each usual method depending on the dosage form.
  • a method of preparing a component that dissolves in a solvent, mixing other insoluble components, and defoaming (for example, decompression) as necessary can be mentioned.
  • the obtained toothpaste can be contained in a container and made into a product.
  • the shape and material of the container are not particularly limited, and a container used for a normal dentifrice composition (dentifrice) can be used.
  • a plastic laminated tube such as polyethylene, polypropylene, polyethylene terephthalate, or nylon can be used. Containers and the like can be mentioned.
  • -Arbitrary component- Abrasive silica (Tixosil® 73, manufactured by Solvay) Sodium fluoride: (manufactured by Stella Chemipha Co., Ltd.) Sodium lauryl sulfate: (manufactured by BASF Japan Ltd.) Sorbitol liquid (70%): (manufactured by Mitsubishi Corporation Life Science Co., Ltd.) Propylene glycol: (manufactured by ADEKA CORPORATION) Viscous silica: Carplex (registered trademark) # 67 (manufactured by DSL Japan Co., Ltd.) Saccharin sodium: (manufactured by Aisan Chemical Industry Co., Ltd.) Water (purified water) For ingredients other than the above, raw materials conforming to the quasi-drug raw material standard 2006 were used.
  • Examples 1 to 30, Comparative Examples 1 to 4 The above components were contained by a conventional method to prepare a dentifrice composition (dentifrice) having the compositions shown in Tables 1 to 4 below, and contained in a laminated tube.
  • Comparative Examples 1 to 3 containing no component (B) the refreshing feeling was not felt so much at the start of brushing the teeth, the bitterness was felt very strongly, and the bitterness was felt even while brushing the teeth, so that the feeling of use was good. Not preferred. The duration of no bitterness after brushing the teeth was less than 5 minutes, and satisfactory results were not obtained. Further, the same result was obtained in the case of Comparative Example 4 in which N-ethyl-p-menthane-3-carboxamide was used instead of the component (B). On the other hand, in each of Examples 1 to 30 containing the component (A) and the component (B), satisfactory results with an average score of 3.0 or more were obtained in all the evaluation items.
  • the oral composition according to the present invention imparts a refreshing sensation at the start of use, suppresses the bitterness derived from the bactericidal agent over a certain period of time after the start of use, and further suppresses the bitterness. It shows that it can be sustained.

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Abstract

L'invention a pour objet de fournir une composition pour cavité buccale qui présente une sensation fraîche au début de sa mise en œuvre, qui inhibe l'amertume dérivée d'un agent antimicrobien du début de sa mise en œuvre jusqu'après écoulement d'une durée prédéfinie après mise en œuvre, et qui en outre permet de prolonger cet effet inhibiteur. Plus précisément, l'invention concerne une composition pour cavité buccale qui comprend : (A) l'agent antimicrobien ; et (B) au moins un élément choisi dans un groupe constitué d'un éthyl－３－（ｐ－menthane－３－carboxamide）acétate, et d'un Ｎ－（２－hydroxy－２－phényléthyl）－２－isopropyl－５，５－diméthylcyclohéxane－１－carboxamide.
PCT/JP2021/043850 2020-12-28 2021-11-30 Composition pour cavité buccale WO2022145161A1 (fr)

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Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016006647A1 (fr) * 2014-07-11 2016-01-14 ライオン株式会社 Composition pour son utilisation dans la cavité buccale
JP2017100965A (ja) * 2015-11-30 2017-06-08 ライオン株式会社 口腔用組成物
WO2018131575A1 (fr) * 2017-01-10 2018-07-19 高砂香料工業株式会社 Dérivé de méthylmenthol et composition conférant une sensation de fraîcheur en contenant
JP2020083831A (ja) * 2018-11-28 2020-06-04 ライオン株式会社 歯磨剤組成物
JP2020169150A (ja) * 2019-04-04 2020-10-15 ライオン株式会社 口腔用組成物

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016006647A1 (fr) * 2014-07-11 2016-01-14 ライオン株式会社 Composition pour son utilisation dans la cavité buccale
JP2017100965A (ja) * 2015-11-30 2017-06-08 ライオン株式会社 口腔用組成物
WO2018131575A1 (fr) * 2017-01-10 2018-07-19 高砂香料工業株式会社 Dérivé de méthylmenthol et composition conférant une sensation de fraîcheur en contenant
JP2020083831A (ja) * 2018-11-28 2020-06-04 ライオン株式会社 歯磨剤組成物
JP2020169150A (ja) * 2019-04-04 2020-10-15 ライオン株式会社 口腔用組成物

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