WO2022145166A1 - Composition pour la cavité buccale - Google Patents

Composition pour la cavité buccale Download PDF

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Publication number
WO2022145166A1
WO2022145166A1 PCT/JP2021/043963 JP2021043963W WO2022145166A1 WO 2022145166 A1 WO2022145166 A1 WO 2022145166A1 JP 2021043963 W JP2021043963 W JP 2021043963W WO 2022145166 A1 WO2022145166 A1 WO 2022145166A1
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Prior art keywords
acid
component
oral composition
mass
salts
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PCT/JP2021/043963
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English (en)
Japanese (ja)
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駿太 石井
将登 平泉
竜 小久保
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ライオン株式会社
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Priority to CN202180087622.0A priority Critical patent/CN116634986A/zh
Priority to JP2022572945A priority patent/JPWO2022145166A1/ja
Publication of WO2022145166A1 publication Critical patent/WO2022145166A1/fr

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    • 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
    • A61K47/02—Inorganic compounds
    • 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
    • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
    • 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
    • A61K47/24—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
    • 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
    • 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
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/24—Phosphorous; Compounds 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
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/25—Silicon; Compounds 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
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/26—Aluminium; Compounds 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
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/36—Carboxylic acids; Salts or anhydrides thereof
    • A61K8/362—Polycarboxylic 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
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/36—Carboxylic acids; Salts or anhydrides thereof
    • A61K8/365—Hydroxycarboxylic acids; Ketocarboxylic 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
    • A61K8/40—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
    • A61K8/49—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
    • A61K8/55—Phosphorus 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
    • A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/81—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions involving only carbon-to-carbon unsaturated bonds
    • 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
    • A61K9/10—Dispersions; Emulsions
    • A61K9/12—Aerosols; Foams
    • 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 feeling of cleaning the dentifrice that is, the smooth and smooth texture of the tooth surface (smoothness) is pronounced of bright white teeth, and it is a feeling that greatly contributes to the satisfaction of tooth brushing behavior as well as the feeling of preventing bad breath.
  • the smooth feeling of the tooth is obtained in a state where the surface of the tooth is cleaned, and this includes, for example, a means such as chemical removal with a chelating agent.
  • the actual feeling of the effect is usually recognized as the smoothness of the tooth surface when the toothpaste user traces the surface of the tooth with the tongue after brushing, that is, a smooth feel (smooth feel).
  • a cooling sensation agent may be added.
  • Patent Document 1 a dentin composition containing N- (4-cyanomethylphenyl) -2-isopropyl-5-methylcyclohexanecarboxamide and sodium polyacrylate and / or sodium alginate is described as persistent. It is described that it can provide a high oral cleanliness and a good feeling of use.
  • Patent Document 2 a dentifrice composition containing a chelating agent and N- (4-cyanomethylphenyl) -2-isopropyl-5-methylcyclohexanecarboxamide gives a high oral cleaning sensation and an excellent halitosis prevention sensation.
  • Patent Document 3 describes that an oral care composition containing a polyphosphorylated compound and a cooling sensation agent such as menthol has a whitening and stain-preventing effect.
  • the stains on the teeth can be cleanly removed from the irritation of the tongue by the cooling sensation agent. It may not be possible to fully realize the "smoothness of the tooth surface".
  • the amount of the cooling sensation agent is increased in order to improve the sustainability required for the feeling of prevention of bad breath, the influence on the sensation of the tongue becomes large, and the smooth feeling of the teeth becomes more difficult to feel.
  • an object of the present invention is to provide an oral composition capable of exhibiting both a feeling of preventing bad breath and a feeling of slipperiness while suppressing irritation in the oral cavity.
  • the present invention provides the following [1] to [11].
  • [1] (A) Chelating agent and (B) An oral composition containing N- (2-hydroxy-2-phenylethyl) -2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide.
  • [2] The oral composition according to [1], wherein the component (A) contains at least one selected from the group consisting of condensed phosphoric acid, organic acids, salts thereof, and polyacrylic acid salts.
  • the component (A) contains at least one of the following: Condensed phosphoric acid and its salt, which is one or more selected from the group consisting of pyrophosphoric acid, polyphosphoric acid, hexametaphosphoric acid and salts thereof; One or more organic acids selected from the group consisting of malic acid, tartaric acid, citric acid, succinic acid, lactic acid, phytic acid, and salts thereof; and salts thereof; Polyacrylic acid salt which is sodium polyacrylate.
  • Condensed phosphoric acid and its salt which is one or more selected from the group consisting of pyrophosphoric acid, polyphosphoric acid, hexametaphosphoric acid and salts thereof
  • One or more organic acids selected from the group consisting of malic acid, tartaric acid, citric acid, succinic acid, lactic acid, phytic acid, and salts thereof
  • Polyacrylic acid salt which is sodium polyacrylate.
  • an oral composition capable of exhibiting both a feeling of preventing bad breath and a feeling of smoothness while suppressing irritation in the oral cavity.
  • the oral composition of the present invention contains the following components (A) and (B), and preferably further contains the component (C).
  • the component (A) is a chelating agent.
  • the chelating agent include condensed phosphoric acid and its salt, organic acid and its salt, and polyacrylic acid salt. That is, the component (A) preferably contains one or more selected from the group consisting of condensed phosphoric acid, organic acids, salts thereof, and polyacrylic acid salts.
  • Condensed phosphoric acid and salts thereof include linear polyphosphoric acids such as pyrophosphoric acid, tripolyphosphoric acid, tetrapolyphosphoric acid, and polyphosphoric acid having a higher degree of polymerization and salts thereof; trimetaphosphate, tetramethaphosphate, hexametaphosphate. Such as cyclic polyphosphoric acid and salts thereof.
  • the salt include alkali metal salts such as sodium salt and potassium salt.
  • pyrophosphate, polyphosphate and hexametaphosphate are preferable, and sodium pyrophosphate, sodium polyphosphate and sodium hexametaphosphate are more preferable.
  • Examples of the organic acid and its salt include oxalic acid, malonic acid, maleic acid, fumaric acid, lactic acid, malic acid, tartrate acid, citric acid, pyruvate acid, oxaloacetic acid, aspartic acid, succinic acid, glucuronic acid, adipic acid, and the like.
  • Examples thereof include phytic acid, phthalic acid, acetic acid, and salts thereof (for example, alkali metal salts such as sodium salt and potassium salt).
  • malic acid, tartaric acid, citric acid, succinic acid, lactic acid, and phytic acid, and salts thereof are preferable, and malic acid, phytic acid, or salts thereof are more preferable.
  • a linear polyacrylic acid salt can be used, and it is preferable to use a polyacrylic acid salt having a weight average molecular weight (Mw) of 1,000 or more and 20,000 or less.
  • Mw weight average molecular weight
  • the weight average molecular weight can be measured using a gel permeation chromatograph / multi-angle laser light scattering detector (GPC-MALLS) under the following conditions.
  • Mobile phase 0.3M NaClO 4 NaN 3
  • aqueous solution column TSKgel ⁇ -M 2 pre-columns: TSK guardgroup ⁇ Standard substance: Polyethylene glycol
  • the polyacrylic acid salt examples include alkali metal salts such as sodium salt and potassium salt.
  • the polyacrylic acid salt is preferably sodium polyacrylate.
  • the component (A) may be one kind or a combination of two or more kinds.
  • the component (A) preferably contains at least one of the following: Condensed phosphoric acid and its salt, which is one or more selected from the group consisting of pyrophosphoric acid, polyphosphoric acid, hexametaphosphoric acid, and salts thereof; One or more organic acids selected from the group consisting of malic acid, tartaric acid, citric acid, succinic acid, lactic acid, phytic acid, and salts thereof; and salts thereof; Polyacrylic acid salt which is sodium polyacrylate.
  • the content of the component (A) is usually 0.05% by mass or more, preferably 0.1% by mass or more, based on the entire oral composition (100% by mass). Thereby, a better stain removing effect can be obtained.
  • the upper limit is usually 3.5% by mass or less, preferably 3% by mass or less, and more preferably 2.5% by mass or less. As a result, it is possible to suppress a decrease in usability due to excessive stimulation to the oral cavity. Therefore, the content of the component (A) is usually 0.05 to 3.5% by mass, preferably 0.1 to 3% by mass, and more preferably 0.1 to 2.5% by mass.
  • the component (B) is N- (2-hydroxy-2-phenylethyl) -2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide.
  • the content of the component (B) is usually 0.000005% by mass or more, preferably 0.00001% by mass or more, more preferably 0.00005% by mass or more, based on the entire oral composition (100% by mass). Is. As a result, a good feeling of prevention of bad breath can be obtained.
  • the upper limit is usually 0.5% by mass or less, preferably 0.1% by mass or less, and more preferably 0.005% by mass or less. As a result, it is possible to prevent the stimulus from becoming too strong and the slippery feeling from being lowered. Therefore, the content of the component (A) is usually 0.000005 to 0.5% by mass, preferably 0.00001 to 0.1% by mass, and more preferably 0.00005 to 0.005% by mass. be.
  • the component (C) is an abrasive.
  • the abrasive may be either an inorganic abrasive or an organic abrasive.
  • the preferred RDA value (Radioactive Dentin Abrasion Values) of the abrasive is not particularly limited.
  • the RDA value is usually 50 or more, particularly preferably 50 to 200.
  • examples of the inorganic polishing agent include silica-based polishing agents such as anhydrous silicic acid, crystalline silica, amorphous silica, silica gel, aluminosilicate, zirconosilicate, zeolite, precipitated silica, and titanium-binding silica; hydrogen phosphate.
  • silica-based polishing agents such as anhydrous silicic acid, crystalline silica, amorphous silica, silica gel, aluminosilicate, zirconosilicate, zeolite, precipitated silica, and titanium-binding silica; hydrogen phosphate.
  • organic abrasive examples include synthetic resin-based abrasives and polymethylmethacrylate.
  • an inorganic abrasive is preferable, a silica-based abrasive and an aluminum-based abrasive are more preferable, and one or more selected from the group consisting of silicic acid anhydride and aluminum oxide is more preferable.
  • the abrasive silica is preferably abrasive particles having an average particle size of 1 to 40 ⁇ m, and the BET specific surface area of the abrasive silica is preferably 80 to 250 square meters per gram.
  • the average particle size of the abrasive silica is a volume-based median diameter (D50) measured by a laser diffraction / scattering method.
  • Commercially available products can be used as the silica-based polishing agent, for example, ZEODENT (registered trademark) 124, ZEODENT (registered trademark) 113 manufactured by Evonic, Tixosil (registered trademark) 73, Tixosil (registered trademark) 63 manufactured by Solvay. , Polishable silica, zirconosilicate, aluminosilicate, etc. manufactured by Taki Chemical Co., Ltd. can be mentioned.
  • the abrasive may be a granulated product.
  • granulated products include particles obtained by granulating water-insoluble powder (for example, silica gel) into granules.
  • a conventionally known arbitrary suitable binder may be used.
  • the component (C) may be used alone or in combination of two or more. In the case of a combination of two or more kinds, the combination of the above-mentioned abrasive particles and the granulated product may be included.
  • the content thereof is usually 1% by mass or more, preferably 2% by mass or more, based on the entire oral composition (100% by mass). This makes it possible to enhance the cleaning power against stains such as stains.
  • the upper limit is usually 35% by mass or less, preferably 30% by mass or less, and more preferably 20% by mass or less. Thereby, the occurrence of oral mucosal irritation can be suppressed. Therefore, the content of the component (C) is usually 1 to 35% by mass, preferably 2 to 30% by mass, and more preferably 2 to 20% by mass.
  • the component (D) is a lactone having 6 to 12 carbon atoms (hereinafter, the number of carbon atoms is shown as a number attached to "C" representing a carbon atom). That is, it is preferable that the oral composition further contains the lactone which is the component (D).
  • the number of carbon atoms constituting the ring structure is not particularly limited.
  • the oral composition By containing the component (D), the oral composition can be given a sweetness during and after use, and the bitterness derived from the component (A) can be suppressed, thereby improving the feeling of use.
  • component (D) examples include C6: ⁇ -hexalactone, C7: ⁇ -heptalactone, C8: ⁇ -octalactone, C9: ⁇ -nonalactone, C10: ⁇ -decalactone, and C11: ⁇ . -Undecalactone, C12: ⁇ -dodecalactone, C6: ⁇ -hexalactone, C7: ⁇ -heptalactone, C8: ⁇ -octalactone, C9: ⁇ -nonalactone, C10: ⁇ -decalactone, C11: ⁇ -un Decalactone, C12: ⁇ -dodecalactone.
  • the component (D) it is preferable to use a lactone having 6 to 11 carbon atoms, and specifically, a lactone containing a 5-membered ring ( ⁇ -lactone) and a lactone containing a 6-membered ring ( ⁇ -lactone) are used. It is preferable to use a lactone containing a 5-membered ring ( ⁇ -lactone). As the component (D), one or more of these can be used. That is, it is preferable that the oral composition further contains at least one selected from the group consisting of lactones having 6 to 12 carbon atoms as the component (D).
  • the content thereof is usually 0.0000001% by mass or more, preferably 0.000005% by mass or more, based on the total amount of the oral composition (100% by mass). It is preferably 0.00001% by mass or more. As a result, good sweetness can be imparted and bitterness can be suppressed.
  • the upper limit is usually 0.2% by mass or less, preferably 0.1% by mass or less, and more preferably 0.05% by mass or less. As a result, it is possible to prevent the sweetness from becoming too strong and the oral composition from being used poorly. Therefore, the content of the component (D) is usually 0.000001 to 0.2% by mass, preferably 0.000005 to 0.1% by mass, and more preferably 0.00001 to 0.05% by mass. be.
  • the oral composition may contain any component other than the components (A) to (D) already described, as long as the effect of the present invention is not impaired.
  • the optional component examples include a surfactant, a sweetener, a fragrance, a medicinal component, an oily component, a preservative, a wetting agent, a binder, a pH adjuster, a colorant (dye), and a solvent.
  • a surfactant e.g., a surfactant, a sweetener, a fragrance, a medicinal component, an oily component, a preservative, a wetting agent, a binder, a pH adjuster, a colorant (dye), and a solvent.
  • surfactant other than the component (C) examples include an anionic surfactant, a nonionic 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 sarcosine salts such as lauroyl sarcosin salt and myristoyl sarcosin salt; acyl glutamates such as lauroyl glutamate, myristoyl glutamate and palmitoyl glutamate; N-lauroyl-N-methylglycine salt and cocoyl glycine.
  • Acylglycine salts such as salts; N-lauroyl- ⁇ -alanine salt, N-myristyl- ⁇ -alanine salt, N-cocoyl- ⁇ -alanine salt, N-lauroyl-N-methyl- ⁇ -alanine salt, N-myristoyl Acylalanine salts such as -N-methyl- ⁇ -alanine salt, N-methyl-N-acylalanine salt; acylasparaginate such as lauroyl asparagate can be mentioned.
  • the acyl taurine salt include lauroylmethyl taurine salt, N-methyl-N-acyl taurine salt, and N-cocoyl methyl taurine salt.
  • ⁇ -olefin sulfonate examples include ⁇ -olefin sulfonates having 12 to 18 carbon atoms such as tetradecene sulfonate.
  • anionic surfactants include hydrogenated coconut fatty acid monoglyceride sodium monosulfate, sodium lauryl sulfoacetate.
  • the anionic surfactant preferably contains a sulfonic acid group in terms of foaming and good foam quality, and more preferably an alkyl sulfate or an ⁇ -olefin sulfonate.
  • nonionic surfactant 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.
  • 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.
  • the nonionic surfactant polyoxyethylene hydrogenated castor oil, polyoxyethylene sorbitan fatty acid ester, and polyoxyethylene alkyl ether are preferable.
  • 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 surfactant is preferably 5% by mass or less, preferably 0.1 to 5% by mass, and more preferably 0.5 to 3% by mass with respect to the entire oral composition (100% by mass). , More preferably 1 to 3% by mass.
  • sugar alcohols and polyhydric alcohols other than sugar alcohols are preferable.
  • sugar alcohol include sugar alcohols such as sorbitol, erythritol, martitol, lactitol, xylitol, and reduced starch saccharified; glycerin; polyhydric alcohols such as ethylene glycol, propylene glycol, dipropylene glycol, butylene glycol, and polyethylene glycol.
  • polyethylene glycol include polyethylene glycol having an average molecular weight of 150 to 6000, and polyethylene glycol having an average molecular weight of 190 to 630 is preferable. Specific examples thereof include PEG200, PEG300, PEG400 and PEG600.
  • the average molecular weight of polyethylene glycol 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).
  • medicinal ingredients include bactericidal or antibacterial agents such as cetylpyridinium chloride, benzalkonium chloride, benzethonium chloride, isopropylmethylphenol, zinc gluconate, zinc citrate, triclosan, timol, hinokithiol, and lysoteam chloride; Enzymes such as mutanase, amylase, protease, lytecenzyme; fluorides such as sodium fluoride, sodium monofluorophosphate, tin fluoride; ⁇ -aminocaproic acid, allantin, tranexamic acid, glycyrrhizinate (eg, glycyrrhetin dipotassium salt) ), Glycyrrhetinic acid, glycyrrhetinic acid derivative (eg, stearyl glycyrrhetinate), anti-inflammatory agents such as allantinchlorhydroxy
  • fragrances other than any D component include peppermint oil, sparemint oil, Japanese peppermint oil, anis oil, cassia oil, eucalyptus oil, winter green oil, mastic oil, neroli oil (orange flower oil), and lemongrass oil.
  • the feeling of use can be further improved.
  • the sweetener include saccharin, saccharin sodium, aspartame, stebioside, stevia extract, paramethoxycinnamic aldehyde, neohesperidin dihydrochalcone, perillartine, glycyrrhizin, thaumatin, aspartylphenylalanine methyl ester and the like.
  • the above-exemplified sweetener may be used alone or in combination of two or more.
  • 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 antiseptic power of the preparation can be ensured.
  • the preservative include paraoxybenzoic acid esters (for example, methyl paraoxybenzoate, ethyl paraoxybenzoate, butyl paraoxybenzoate), sodium benzoate and the like.
  • the preservative may be used alone or in combination of two or more.
  • 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.
  • CMC carboxymethyl cellulose
  • hydroxyethyl cellulose hydroxypropyl cellulose
  • hydroxypropylmethyl cellulose hydroxypropylmethyl cellulose
  • methyl cellulose c
  • inorganic binders such as thickening silica and aluminum silicate can also be mentioned.
  • the content of any 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 pH stability of the pharmaceutical product can be ensured.
  • the optional pH adjuster include hydroxides such as sodium hydroxide and potassium hydroxide, phosphoric acid or a salt thereof, sodium hydrogen phosphate, sodium dihydrogen phosphate and the like.
  • 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 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.
  • the solvent examples include water (purified water) and ethanol.
  • water purified water
  • ethanol ethanol
  • the solvent one type may be used alone or two or more types may be used in combination.
  • 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 is, for example, in the form of a paste or liquid, and if it is a dentifrice, it can be prepared as a dentifrice, a liquid dentifrice, a liquid dentifrice, or a dentifrice.
  • the method for producing the oral composition is not particularly limited.
  • Oral compositions can be prepared by their respective conventional methods, depending on the dosage form. For example, when it is used as a dentifrice, a method of preparing a component that dissolves in a solvent, mixing other insoluble components, and defoaming (for example, reducing the pressure) as necessary can be mentioned.
  • the toothpaste obtained by such a method 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 can be used. Examples of the container include a container such as a laminated tube made of plastic such as polyethylene, polypropylene, polyethylene terephthalate, and nylon.
  • A1 Sodium pyrophosphate (trade name: sodium pyrophosphate, manufacturer: Taihei Kagaku Sangyo Co., Ltd.)
  • A2 Sodium polyphosphate (trade name: sodium polyphosphate, manufacturer: Taihei Kagaku Sangyo Co., Ltd.)
  • A3 Sodium hexametaphosphate (trade name: sodium hexametaphosphate, manufacturer: Taihei Kagaku Sangyo Co., Ltd.)
  • A4 Malic acid (trade name: malic acid, manufacturer: Fuso Chemical Industry Co., Ltd.)
  • A5 Phytic acid (trade name: phytic acid, manufacturer: Fuso Chemical Industry Co., Ltd.)
  • A6 Sodium polyacrylate (trade name: AC-10NPD, manufacturer: Toagosei Co., Ltd.)
  • N- (2-Hydroxy-2-phenylethyl) -2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide (trade name: Coolact® 370, manufacturer: Takasago International Corporation)
  • N-Ethyl-p-Menthane-3-carboxamide (trade name: WS-3, manufactured by Simrise Japan)
  • polishable silica (Tixosil® 73, manufactured by Solvay)
  • C2 Aluminum oxide (trade name: aluminum oxide, manufacturer: Nippon Light Metal Co., Ltd.)
  • -(D) component- D1 ⁇ -Hexalactone: (Manufacturer: Inoue Fragrance Co., Ltd.)
  • D2 ⁇ -Undecalactone: (Manufacturer: Inoue Fragrance Co., Ltd.)
  • ⁇ Evaluation method> It was evaluated by 4 subjects. A 1 g of sample dentifrice was placed on a toothbrush (Clinica Advantage toothbrush, 4-row compact, usually manufactured by Lion Corporation), and after brushing the teeth for 3 minutes, the oral cavity was rinsed once with 10 mL of water. The irritation in the oral cavity after use, the smooth feeling of teeth after use (easiness to feel smooth), the feeling of preventing bad breath, the lack of bitterness, and the good feeling of use are judged by the following score criteria, respectively, for 4 people. The average score was calculated and evaluated according to the following evaluation criteria.
  • the actual feeling of preventing bad breath means that a refreshing feeling is felt even after 60 minutes have passed after use
  • the good feeling of use means that there is no sarcasm due to bitterness or too strong sweetness.
  • composition of the fragrance is as follows. Peppermint oil 50% by mass Peppermint refined oil (20% cut in front flow) 5% by mass Peppermint refined oil (15% cut in front and back flow) 5% by mass Spearmint oil 1% by mass Spearmint refined oil (20% cut in front flow) 1% by mass Japanese mint oil 1% by mass Japanese mint refined oil (30% cut in front flow) 1% by mass Menthol 10% by mass Carvone 1% by mass Anethole 5% by mass Solvent balance 100% by mass in total
  • Comparative Example 11 Although there is no bitterness, the evaluation of the smoothness of the teeth is low, and in Comparative Example 12, which contains the components (A) and (C) but does not contain the component (B), the evaluation of the actual feeling of preventing bad breath is low. The bitterness was also strongly evaluated. On the other hand, in Examples 14 to 21 containing the component (A), the component (B) and the component (D), the evaluation of no bitterness is excellent by further containing the component (D), and the usability is good. The evaluation was also good.

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Abstract

L'invention a pour objet de fournir une composition pour la cavité buccale qui inhibe l'irritation à l'intérieur de la cavité buccale, et qui permet de développer à la fois une véritable sensation de prévention de la mauvaise haleine et une sensation de poli, compte tenu des problèmes existant dans l'art antérieur. Plus précisément, l'invention fournit une composition pour la cavité buccale telle qu'un dentifrice, un bain de bouche, un agent à vaporiser, un onguent, un timbre, un agent solubilisant intra-buccal, ou similaire, qui comprend : (A) un agent chélateur tel qu'un phosphate condensé, un acide organique, un sel de phosphate condensé, un sel d'acide organique, un polyacrylate, ou similaire ; et (B) un Ｎ－（２－hydroxy－２－phényléthyl）－２－isopropyl－５，５－ diméthylcyclohexane－１－carboxamide.
PCT/JP2021/043963 2020-12-28 2021-11-30 Composition pour la cavité buccale WO2022145166A1 (fr)

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CN202180087622.0A CN116634986A (zh) 2020-12-28 2021-11-30 口腔用组合物
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Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009531414A (ja) * 2006-03-29 2009-09-03 ザ プロクター アンド ギャンブル カンパニー 消費者美的特徴及び味の改善された口腔ケア組成物
JP2013035792A (ja) * 2011-08-09 2013-02-21 Kao Corp 口腔用組成物
JP2015204849A (ja) * 2007-11-29 2015-11-19 インターコンチネンタル グレート ブランズ エルエルシー 活性物を有する多領域チューインガム
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
US20190175486A1 (en) * 2017-12-07 2019-06-13 Johnson & Johnson Consumer Inc. Oral Care Compositions
WO2019131061A1 (fr) * 2017-12-27 2019-07-04 ライオン株式会社 Composition de dentifrice

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009531414A (ja) * 2006-03-29 2009-09-03 ザ プロクター アンド ギャンブル カンパニー 消費者美的特徴及び味の改善された口腔ケア組成物
JP2015204849A (ja) * 2007-11-29 2015-11-19 インターコンチネンタル グレート ブランズ エルエルシー 活性物を有する多領域チューインガム
JP2013035792A (ja) * 2011-08-09 2013-02-21 Kao Corp 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
US20190175486A1 (en) * 2017-12-07 2019-06-13 Johnson & Johnson Consumer Inc. Oral Care Compositions
WO2019131061A1 (fr) * 2017-12-27 2019-07-04 ライオン株式会社 Composition de dentifrice

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