WO2021193398A1 - 口腔用組成物 - Google Patents

口腔用組成物 Download PDF

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Publication number
WO2021193398A1
WO2021193398A1 PCT/JP2021/011299 JP2021011299W WO2021193398A1 WO 2021193398 A1 WO2021193398 A1 WO 2021193398A1 JP 2021011299 W JP2021011299 W JP 2021011299W WO 2021193398 A1 WO2021193398 A1 WO 2021193398A1
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WIPO (PCT)
Prior art keywords
oral
present
oral composition
oral cavity
mass
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Ceased
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PCT/JP2021/011299
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English (en)
French (fr)
Japanese (ja)
Inventor
真佐夫 原
俊輔 櫻井
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NOF Corp
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NOF Corp
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Application filed by NOF Corp filed Critical NOF Corp
Priority to EP21774424.2A priority Critical patent/EP4129413A4/en
Priority to JP2022510065A priority patent/JPWO2021193398A1/ja
Priority to CN202180024659.9A priority patent/CN115361936B/zh
Priority to US17/907,381 priority patent/US20230124809A1/en
Publication of WO2021193398A1 publication Critical patent/WO2021193398A1/ja
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/72Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/73Polysaccharides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/72Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/81Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions involving only carbon-to-carbon unsaturated bonds
    • A61K8/817Compositions of homopolymers or copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and at least one being terminated by a single or double bond to nitrogen or by a heterocyclic ring containing nitrogen; Compositions or derivatives of such polymers, e.g. vinylimidazol, vinylcaprolactame, allylamines (Polyquaternium 6)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34Alcohols
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/4906Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom
    • A61K8/4926Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom having six membered rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/60Sugars; Derivatives thereof
    • A61K8/602Glycosides, e.g. rutin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/64Proteins; Peptides; Derivatives or degradation products thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/67Vitamins
    • A61K8/678Tocopherol, i.e. vitamin E
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q11/00Preparations 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 capable of preventing the formation and maturation of a biofilm in the oral cavity and having an excellent usability.
  • the oral environment refers to the condition of the entire oral cavity including not only the space in the mouth but also the teeth, gums, nasal cavity, palate, oral mucosa, etc.
  • the oral environment deteriorates, bad breath, caries, teeth It causes the occurrence of periodontal disease and leads to a decrease in quality of life.
  • organic substances such as liquids, ions in the air and food waste are adsorbed on the tooth surface to form an adsorption layer called a conditioning film, and bacteria adhere to it to form plaque (a collection of bacteria).
  • a dental plaque is formed.
  • the attached bacteria secrete extracellular polysaccharides to form colonies, which are aggregates of bacteria, which mature over time to form biofilms, which are aggregates of multiple bacteria.
  • Dental plaque is relatively easy to remove by mouth cleaning such as toothpaste, but it is difficult to remove biofilm by ordinary mouth cleaning such as toothpaste.
  • the pathogenic bacteria of caries and periodontal diseases that live in the biofilm adhere to the heart valve membrane and multiply, causing bacterial endocarditis, and especially in the elderly, in the bloodstream. It can also cause circulatory disorders such as invasion, coronary artery disease, heart disease and myocardial infarction.
  • bactericides anti-inflammatory agents, vitamins, etc. are used to maintain a good oral environment and prevent the formation and maturation of biofilms in the oral cavity.
  • the feeling of use is reduced.
  • a refreshing agent such as l-menthol is used in order to impart a refreshing feeling and enhance the feeling of use, but the composition containing a cationic bactericide has a bitter taste.
  • chlorobutanol or anethole in addition to the cationic bactericide and l-menthol (Patent Document 1).
  • an object of the present invention is to provide an oral composition which can prevent the formation and maturation of a biofilm in the oral cavity, improve the taste and the residual feeling in the oral cavity, and have an excellent usability. be.
  • the present invention relates to the following.
  • An oral composition containing 0.001% by mass to 10% by mass of proteoglycan, a refreshing agent, and one or more selected from the group consisting of bactericides, anti-inflammatory agents and vitamins.
  • a method for preventing the formation and maturation of a biofilm in the oral cavity which comprises using an oral composition containing one or more of more selected.
  • the proteoglycan is a plant-derived proteoglycan.
  • the present invention it is possible to provide an oral composition which can satisfactorily prevent the formation and maturation of a biofilm in the oral cavity, improve the taste and the residual feeling in the oral cavity, and have an excellent usability.
  • the oral composition of the present invention can maintain a good oral environment and is useful for prevention of dental caries and periodontal disease.
  • the above method of the present invention is useful for maintaining a good oral environment of the subject and preventing caries and periodontal disease.
  • the present invention can provide a method for improving the taste of the oral composition and the residual feeling in the oral cavity.
  • the above method of the present invention is useful in providing an oral composition having an excellent effect of preventing dental caries and periodontal disease and having an excellent usability.
  • the present invention provides an oral composition.
  • the oral composition of the present invention contains one or more selected from the group consisting of proteoglycans, refreshing agents, and bactericides, anti-inflammatory agents and vitamins.
  • the proteoglycan contained in the oral composition of the present invention is a complex of sugar and protein having a special structure, and animal and vegetable proteoglycans are present.
  • Animal proteoglycan is a glycoprotein in which multiple glycosaminoglycans such as chondroitin sulfate and keratan sulfate are covalently bonded to one core protein, and as a component of extracellular matrix, organs, brain, skin, and cartilage. It is widely distributed in the body.
  • Plant-derived proteoglycan is a combination of arabinogalactan and core protein in a certain manner, and is officially called arabinogalactan-protein (AGP), which is used as an extracellular matrix on the cell wall and sap of plants. exist.
  • AGP arabinogalactan-protein
  • either animal proteoglycan or plant proteoglycan can be used as the proteoglycan, but it is preferable to use plant proteoglycan in consideration of the production cost and the tendency that plant raw materials are preferred in recent years. ..
  • gum arabic As the plant-derived proteoglycan, those made from gum arabic (Acacia senegal Wildenow) belonging to the genus Acacia of the subfamily Mimosoideae of the family Leguminosae, or gum arabic obtained from a plant closely related to the same genus are preferably used.
  • gum arabic is a dried secretion liquid exuding from a wound on the bark of the plant. Since a substance having physiological activity equal to or higher than that of animal proteoglycan can be obtained, the object of the present invention is to obtain gum arabic (Acacia senegal Willdenow) or gum arabic obtained from its seyal species, Acacia senedale.
  • Those used as a raw material are more preferably used, and those made from gum arabic obtained from gum arabic (Acacia senegal Wildenow) are more preferably used.
  • the plant-derived proteoglycan preferably used as a proteoglycan is obtained as a purified product obtained by removing mainly arabinogalactan and glycoprotein from gum arabic obtained from a plant such as gum arabic described above.
  • plant proteoglycans have a weight average molecular weight of 900,000 to 3,500,000 as measured by size exclusion chromatography with a multi-angle light scattering detector and a differential index detector connected online. Some are preferably used, and those having a value of 1,000,000 to 3,000,000 are more preferably used.
  • an aldehyde quantification kit such as Amplite TM aldehyde quantification kit (specific color) (Colorimetric Aldehyde Quantation Kit) (product number: 10015) (manufactured by AAT Bioquest).
  • Amplite TM aldehyde quantification kit specific color
  • Coldorimetric Aldehyde Quantation Kit product number: 10015
  • the vegetable proteoglycan may be used in any of liquid forms such as aqueous solutions, suspensions and dispersions, and solid forms such as powders and granules.
  • one type of the above-mentioned proteoglycan can be used alone, or two or more types can be used in combination.
  • Animal proteoglycans may be produced and used by extracting and purifying from animal tissues such as salmon nasal cartilage, shark fin cartilage and squid head cartilage, but commercially available products provided by each company may also be used. can.
  • animal proteoglycans may be used in any of liquid forms such as aqueous solutions, suspensions and dispersions, and solid forms such as powders and granules.
  • the vegetable proteoglycan is preferably purified by subjecting an aqueous Arabic rubber solution adjusted to 0.5% by mass to 40% by mass with a porous type I strong basic anion exchange resin and a strong acid cation exchange resin.
  • a product commercially available as an aqueous solution having an active ingredient content of about 1% by mass can also be generally used.
  • Examples of commercially available products containing vegetable proteoglycans include "phytoproteoglycans (registered trademark)" manufactured by NOF CORPORATION.
  • the content of proteoglycan in the oral composition of the present invention is 0.001% by mass to 10% by mass, preferably 0.005% by mass to 5% by mass from the viewpoint of improving the residual feeling in the oral cavity. be. If the content of proteoglycan is less than 0.001% by mass, it is not possible to impart a sufficient effect of improving the residual feeling in the oral cavity, while even if the content of proteoglycan exceeds 10% by mass, it is commensurate with the content. It may not be effective.
  • the refreshing agent contained in the oral composition of the present invention can be used without particular limitation as long as it is an acceptable refreshing agent for oral use. , Keihi oil, geraniol, methyl salicylate, spirantol, spearmint oil, timol, mint water, mint oil, peppermint oil, bergamot oil, d-borneol, l-menthol, ryuno and the like.
  • the above-mentioned refreshing agent may be used alone or in combination of two or more.
  • l-menthol, peppermint oil, spearmint oil, peppermint oil and the like are preferably used as the refreshing agent, and l-menthol and the like are more preferable. It is preferably used.
  • the content of the refreshing agent in the oral composition of the present invention is preferably 0.0001% by mass to 5% by mass, and more preferably 0.001% by mass to 1% by mass.
  • the content of the refreshing agent is within the above range, a good refreshing feeling can be imparted to the oral composition, and the bitterness caused by the bactericidal agent or the like can be reduced.
  • the oral composition of the present invention contains at least one selected from the group consisting of bactericides, anti-inflammatory agents and vitamins as an active ingredient for preventing the formation and maturation of biofilms in the oral cavity.
  • the bactericidal agent contained in the oral composition of the present invention can be used without particular limitation as long as it is an acceptable bactericidal agent for oral use.
  • Cationic surfactants such as decalinium, benzalkonium chloride, benzethonium chloride, hexadecyltrimethylammonium chloride; amphoteric surfactants such as alkyldiaminoethylglycine hydrochloride; chlorhexidine salts such as chlorhexidine hydrochloride and chlorhexidine gluconate; iodine such as povidone iodine Agents; phenol derivatives such as isopropylmethylphenol; aromatic ether derivatives such as triclosan and the like are exemplified.
  • the above-mentioned fungicide may be used alone or in combination of two or more.
  • chlorhexidine gluconate, cetylpyridinium chloride and its hydrate from the viewpoints of biofilm formation in the oral cavity, preventive effect on maturation, hypoallergenicity to the oral cavity, etc.
  • Chlorhexidine gluconate, cetylpyridinium chloride and hydrates thereof and the like are preferably used, and isopropylmethylphenol and the like are preferably used.
  • the anti-inflammatory agent contained in the oral composition of the present invention can be used without particular limitation as long as it is an anti-inflammatory agent acceptable for oral use, and for example, guaiazulene (1,4-dimethyl-).
  • Azulene derivatives such as 7-isopropylazulene), sodium azulene sulfonate; allantin, sodium allantimpyrrolidone carboxylate, allantinglycyrrhetinic acid, allantin pantothenyl alcohol and the like; alloin and its derivatives; dipotassium glycyrrhizinate, monoglycyrrhizinate Glycyrrhizic acid and its salts such as ammonium, glycyrrhetinic acid and its derivatives such as ⁇ -glycyrrhetinic acid and stearyl glycyrrhetinate; tropolone derivatives such as hinokithiol; synthetic plasmin inhibitors
  • the anti-inflammatory agent may be used alone or in combination of two or more.
  • allantoin, glycyrrhizic acid and its salts, hinokitiol, ⁇ -aminocaproic acid, tranexamic acid and the like are preferably used, and allantoin and dipotassium glycyrrhizinate are used.
  • Hinokitiol and the like are more preferably used.
  • the vitamin contained in the oral composition of the present invention can be used without particular limitation as long as it is an acceptable vitamin for oral use.
  • Vitamin B 2 such as dinucleotide (FAD) and riboflavin butyrate and its derivatives
  • Vitamin B 6 such as pyridoxin hydrochloride and pyridoxin dipalmitate, salts and derivatives thereof
  • Pantothenic acid such as pantothenic acid and D-pantothenyl alcohol and its derivatives thereof.
  • ascorbic acid such as sodium L-ascorbic acid, magnesium L-ascorbic acid ester, salts and derivatives thereof
  • vitamin E such as dl- ⁇ -tocopherol, dl- ⁇ -tocopherol acetate, dl- ⁇ -tocopherol nicotinate And its derivatives and the like
  • the above vitamins can be used alone or in combination of two or more. From the viewpoint of preventing the formation and maturation of biofilm in the oral cavity, dl- ⁇ -tocopherol acetate, pantothenic acid, sodium L-ascorbate and the like are preferably used as vitamins, and dl- ⁇ -tocopherol acetate and pantothenic acid. Etc. are more preferably used.
  • the content of one or more selected from the group consisting of bactericides, anti-inflammatory agents and vitamins in the oral composition of the present invention is the total amount thereof, preferably 0.001% by mass to 5% by mass. More preferably, it is 0.01% by mass to 2% by mass.
  • biofilms are formed and matured in the oral cavity without showing strong irritation to the oral cavity. On the other hand, a good preventive effect can be achieved.
  • the oral composition of the present invention contains a copolymer containing a structural unit based on 2- (meth) acryloyloxyethyl phosphorylcholine (MPC) (hereinafter, may be referred to as "MPC copolymer").
  • MPC copolymer a copolymer containing a structural unit based on 2- (meth) acryloyloxyethyl phosphorylcholine (MPC copolymer”
  • MPC copolymer 2- (meth) acryloyloxyethyl phosphorylcholine
  • Examples of the MPC copolymer that can be contained in the oral composition of the present invention include a copolymer containing a constitutional unit based on acrylamide and a constitutional unit based on a hydrophobic monomer, and are based on the hydrophobic monomer.
  • Examples of the structural unit include a structural unit based on a (meth) acrylic acid alkyl ester, a (meth) acrylamide derivative, and the like.
  • the structural unit based on MPC is represented by the following formula (1).
  • (meth) acryloyl means "acryloyl or methacryloyl”.
  • R 1 represents a hydrogen atom or a methyl group.
  • the structural unit based on the (meth) acrylic acid alkyl ester is represented by the following formula (2).
  • (meth) acrylic acid means "acrylic acid or methacrylic acid”.
  • R 2 represents a hydrogen atom or a methyl group
  • R 3 represents an alkyl group having 1 to 24 carbon atoms.
  • the alkyl group represented by R 3 is a linear or branched alkyl group having 1 to 24 carbon atoms, methyl, ethyl, propyl, butyl, pentyl, hexyl, octyl, 2-ethylhexyl, decyl , Dodecyl, tetradecyl, hexadecyl, octadecyl, docosyl and the like are exemplified.
  • the structural units based on the (meth) acrylic acid alkyl ester represented by the formula (2) include methyl (meth) acrylate, ethyl (meth) acrylate, propyl (meth) acrylate, and (meth) acrylic acid. Based on butyl, 2-ethylhexyl (meth) acrylate, dodecyl (meth) acrylate (lauryl), tridecyl (meth) acrylate, octadecyl (stearyl) (meth) acrylate, docosyl (meth) acrylate, etc. A constituent unit can be mentioned.
  • the structural unit based on the (meth) acrylamide derivative is represented by the following formula (3).
  • (meth) acrylamide means "acrylamide or methacrylamide”.
  • R 4 represents a hydrogen atom or a methyl group
  • R 5 and R 6 each independently represent a methyl group or an ethyl group
  • m represents an integer of 1 to 3.
  • a copolymer containing a structural unit based on N, N-dimethylaminoethyl acrylamide or N, N-dimethylaminopropyl acrylamide is preferable as the structural unit based on the (meth) acrylamide derivative.
  • the MPC copolymer a copolymer containing one or more structural units based on MPC and the above-mentioned hydrophobic monomer can be used.
  • An object of the present invention is to use a structural unit based on a (meth) acrylic acid alkyl ester, a structural unit based on 2-hydroxy-3- (meth) acryloyloxypropyltrimethylammonium chloride, as a structural unit based on a hydrophobic monomer.
  • a copolymer containing one or more selected from the group consisting of structural units based on (meth) acrylamide derivatives is preferably used.
  • the ratio of the content of the constitutional unit based on MPC and the constitutional unit based on the hydrophobic monomer in the MPC copolymer ([Structural unit based on MPC]: [Constituent unit based on hydrophobic monomer]] ) (N 1 : n 2 ) is 9: 1 to 2: 1 in molar ratio, preferably 8: 1 to 7: 3, and more preferably 6: 1 to 3: 1.
  • the weight average molecular weight of the MPC copolymer contained in the oral composition of the present invention is 10,000 to 5,000,000, preferably 20,000 to 1,000,000. If the weight average molecular weight of the MPC copolymer is less than 10,000, the residual feeling in the oral cavity may not be improved, while if the weight average molecular weight of the MPC copolymer is larger than 5,000,000, MPC may not be improved. The viscosity of the copolymer may increase sharply, making it difficult to prepare an oral composition.
  • the weight average molecular weight of the MPC copolymer is measured by gel permeation chromatography (GPC) and is indicated by the molecular weight in terms of pullulan.
  • the polymerization form of the MPC copolymer is not particularly limited, and it may be a random copolymer or a block copolymer, but a random copolymer is preferable.
  • the MPC copolymer may be a copolymer containing other structural units in addition to the structural unit based on MPC and the structural unit based on the hydrophobic monomer.
  • the other structural units can be appropriately selected from those that can usually be the structural units of the copolymer, as long as they do not affect the effects of the present invention.
  • Other building blocks include, for example, alkenyl esters of (meth) acrylic acids such as allyl (meth) acrylic acid; cyclic alkyl esters of (meth) acrylic acids such as cyclohexyl (meth) acrylic acid; tetrahydro (meth) acrylic acid.
  • Vinyl ether-based monomer A structural unit based on a vinyl ester-based monomer such as vinyl acetate and vinyl propionate can be mentioned. These other constituent units may contain one or more, and their content in the MPC copolymer is relative to the total amount of the MPC-based constituent units and the hydrophobic monomer-based constituent units. It is 40 mol% or less, preferably 20 mol% or less.
  • the MPC copolymer can be produced by a production method known per se.
  • It can be produced by polymerization in an atmosphere of an inert gas such as nitrogen by a known method such as solution polymerization.
  • the content ratio of each monomer at that time may be a ratio corresponding to the content ratio of each structural unit in the MPC copolymer.
  • the MPC copolymer can be produced and used by the above-mentioned polymerization method, but a commercially available product as a solution or dispersion of water or polyhydric alcohol can also be used.
  • one type of the above-mentioned MPC copolymer may be selected and used alone, or two or more types may be selected and used in combination.
  • the form of the MPC copolymer used in the oral composition of the present invention may be any of solids such as powders and granules, and liquids such as solutions, suspensions and dispersions.
  • the content of the MPC copolymer in the oral composition of the present invention can be appropriately selected in the range of 0.001% by mass to 10% by mass, and from the viewpoint of the effect of improving the residual feeling in the oral cavity, 0. It is preferable to select in the range of 005% by mass to 5% by mass. If the content of the MPC copolymer is less than 0.001% by mass, the residual feeling in the oral cavity may not be improved, while if the content of the MPC copolymer exceeds 10% by mass, the present The residual feeling in the oral cavity after using the oral composition of the present invention may be increased.
  • the oral composition of the present invention includes agents other than the above-mentioned bactericidal agents, anti-inflammatory agents and vitamins, which are generally used for oral compositions and generally used for oral compositions.
  • Additives other than the refreshing agent, which are the additives used can be added, if necessary, within a range that does not impair the characteristics of the present invention.
  • Agents other than the above-mentioned bactericidal agents, anti-inflammatory agents and vitamins, which are generally used in oral compositions include hemostatic agents, astringent agents, cell activators, blood circulation promoters, and dental plaque enhancers. Examples thereof include tartar deposition inhibitor, hypersensitivity improver, plaque remover, pigmentation inhibitor, halitosis remover, adsorbent and the like.
  • Additives generally used in oral compositions, other than refreshing agents include buffers, wetting agents, surfactants, preservatives, binders, abrasives, and thickeners. , Solvents, organic acids, inorganic salts, antioxidants, stabilizers, metal ion sequestering agents, fragrances, sweeteners, flavoring agents, colorants and the like.
  • the agents generally used for oral compositions other than bactericides, anti-inflammatory agents and vitamins, and the additives generally used for oral compositions other than refreshing agents are: The amount normally contained in each oral composition can be used.
  • a solvent is generally used.
  • the solvent is not particularly limited, and examples thereof include purified water and ethanol.
  • ethanol is particularly preferably used as a solvent in a content of 5% by mass to 20% by mass.
  • the oral composition of the present invention may be added to one or more selected from the group consisting of proteoglycans, refreshing agents, and bactericides, anti-inflammatory agents and vitamins, or further to MPC copolymers, if necessary, as described above.
  • the oral composition of the present invention can be provided as a powder toothpaste, a toothpaste, a liquid toothpaste, a mouthwash, a mouthwash, an oral refreshing agent, a dental gel, a dental cream, an oral spray and the like.
  • toothpaste, liquid toothpaste, mouthwash, mouthwash and the like are preferable.
  • the method of using the oral composition of the present invention is not particularly limited, but for example, in the case of a liquid oral composition, 1 mL to 25 mL is usually 1 to 10 times, preferably 1 to 8 times a day. , More preferably 1 to 6 times, still more preferably 1 to 4 times, even more preferably 1 to 3 times (particularly preferably morning, noon, evening), and wash by gargle in the mouth for 30 seconds or more each time. Mouth (gargle) can be exemplified.
  • the subject to which the oral composition of the present invention is used is not particularly limited, but is preferably a mammal including a human.
  • the oral composition of the present invention can satisfactorily prevent the formation and maturation of a biofilm in the oral cavity, and the taste of the oral composition and the residue in the oral cavity when the oral composition is used. The feeling is improved and the usability is excellent. Therefore, the oral composition of the present invention maintains a good oral environment and is useful for prevention of dental caries and periodontal disease.
  • the present invention also relates to a method for preventing the formation and maturation of a biofilm in the oral cavity in a subject who needs to prevent the formation and maturation of the biofilm in the oral cavity (hereinafter, "prevention of the present invention” in the present specification. (Sometimes called “method") is provided.
  • the prevention method of the present invention is for subjects who need to prevent the formation and maturation of biofilms in the oral cavity, by adding 0.001% by mass to 10% by mass of proteoglycan, a refreshing agent, and a bactericidal agent, an anti-inflammatory agent and the like. It comprises using an oral composition containing at least one selected from the group consisting of vitamins.
  • the "subject who needs to prevent the formation and maturation of biofilm” is not particularly limited as long as it is a human or a non-human animal whose oral environment deteriorates or is likely to deteriorate. However, it preferably refers to humans whose oral environment deteriorates or is likely to deteriorate, and non-human mammals such as monkeys, dogs, cats, cows, horses, sheep, goats, rats, mice, and rabbits.
  • an oral composition containing "0.001% by mass to 10% by mass of proteoglycan, a refreshing agent, and one or more selected from the group consisting of bactericides, anti-inflammatory agents and vitamins". Is as described above in the oral composition of the present invention.
  • the oral composition to be used by the subject can further contain 0.001% by mass to 10% by mass of the MPC copolymer, and if necessary, other than the above-mentioned bactericidal agent, anti-inflammatory agent and vitamin. It is also possible to contain an additive other than a refreshing agent, which is a drug generally used for an oral composition or an additive generally used for an oral composition.
  • a refreshing agent which is a drug generally used for an oral composition or an additive generally used for an oral composition.
  • the MPC copolymer, the above-mentioned agents and additives are also as described above in the oral composition of the present invention. Further, in the prevention method of the present invention, the method of causing the subject to use the oral composition is also the same as described above in the oral composition of the present invention.
  • the formation and maturation of a biofilm in the oral cavity of the subject can be satisfactorily prevented, and the oral environment of the subject can be kept good. Periodontal disease can be prevented satisfactorily.
  • the present invention further provides a method for improving the taste of an oral composition and the residual feeling in the oral cavity (hereinafter, may be referred to as "improvement method of the present invention” in the present specification).
  • improvement method of the present invention one or more selected from the group consisting of 0.001% by mass to 10% by mass of proteoglycan, a refreshing agent, and a bactericide, an anti-inflammatory agent and a vitamin are added to the oral composition. Including doing.
  • one or more selected from the group consisting of proteoglycans, refreshing agents, and bactericides, anti-inflammatory agents, and vitamins added to the oral composition, the oral composition of the present invention.
  • the MPC copolymer is as described above in the oral composition of the present invention.
  • a drug other than the above-mentioned bactericidal agent, anti-inflammatory agent and vitamin which is generally used for oral compositions, or generally for oral use.
  • Additives used in the composition other than the refreshing agent can be further added to the oral composition.
  • the above-mentioned agents and additives are also as described above in the oral composition of the present invention.
  • the form, production method, etc. of the oral composition are also as described above in the oral composition of the present invention.
  • the taste of the oral composition and the residual feeling when the oral composition is used can be improved, and the feeling of use of the oral composition can be improved.
  • Examples 1 to 6, Comparative Examples 1 to 6 Oral Compositions Each oral composition of Examples 1 to 6 and Comparative Examples 1 to 6 was prepared by the method shown below according to the formulation shown in Table 1. .. That is, a cooling agent (l-menthol) is added to ethanol and gently heated to dissolve it, and about 80 g of purified water is added to add a bactericide (cetylpyridinium chloride hydrate), an anti-inflammatory agent (dipotassium glycyrrhizinate) or Vitamin (dl- ⁇ -tocopherol acetate), vegetable proteoglycan, or further MPC copolymer was added, mixed and stirred to make it uniform. Next, the total amount of purified water was set to 100 g, and the oral compositions of Examples 1 to 6 and Comparative Examples 1 to 6 were prepared.
  • a cooling agent l-menthol
  • purified water is added to add a bactericide (cetylpyridinium chloride hydrate), an anti-inflammatory agent (dipot
  • the oral composition of the present invention containing at least one selected from the group consisting of plant proteoglycans, refreshing agents, and bactericides, anti-inflammatory agents and vitamins, biofilm formation in the oral cavity It was confirmed that maturation can be prevented, the unpleasant taste caused by the bactericidal agent and the like is reduced, and the residual feeling in the oral cavity caused by the refreshing agent is also improved.
  • the formation and maturation of the biofilm in the oral cavity can be satisfactorily prevented, the unpleasant taste is reduced, and the residual feeling in the oral cavity after use is also improved. It is possible to provide an oral composition having an excellent usability.
  • the oral composition of the present invention maintains a good oral environment and is useful for prevention of dental caries and periodontal disease. Further, according to the present invention, it is possible to provide a method for satisfactorily preventing the formation and maturation of a biofilm in the oral cavity in a subject who needs to prevent the formation and maturation of the biofilm in the oral cavity.
  • the prevention method of the present invention is useful for maintaining a good oral environment of the subject and preventing caries and periodontal disease. Furthermore, the present invention can provide a method for improving the taste of the oral composition and the residual feeling in the oral cavity.
  • the above-mentioned improvement method of the present invention is useful in providing an oral composition having an excellent usability.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Oral & Maxillofacial Surgery (AREA)
  • Cosmetics (AREA)
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EP21774424.2A EP4129413A4 (en) 2020-03-27 2021-03-19 Composition for oral cavity
JP2022510065A JPWO2021193398A1 (https=) 2020-03-27 2021-03-19
CN202180024659.9A CN115361936B (zh) 2020-03-27 2021-03-19 口腔用组合物
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JPWO2021193398A1 (https=) 2021-09-30
US20230124809A1 (en) 2023-04-20

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