Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
  • A61K8/04—Dispersions; Emulsions
  • A61K8/046—Aerosols; Foams
• • 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
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
  • A61K8/34—Alcohols
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
  • A61K8/34—Alcohols
  • A61K8/342—Alcohols having more than seven atoms in an unbroken chain
• • 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
  • A61K8/4993—Derivatives containing from 2 to 10 oxyalkylene groups
• • 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
  • A61K8/8141—Compositions 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 only one carboxyl radical, or of salts, anhydrides, esters, amides, imides or nitriles thereof; Compositions of derivatives of such polymers
  • A61K8/8152—Homopolymers or copolymers of esters, e.g. (meth)acrylic acid esters; Compositions of derivatives of such polymers
• • 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
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
  • A61K2800/80—Process related aspects concerning the preparation of the cosmetic composition or the storage or application thereof
  • A61K2800/92—Oral administration

Definitions

• the present invention relates to an oral aerosol agent.
• oral aerosol agents which are applied by filling an aerosol container with an oral composition together with a propellant such as carbon dioxide (carbon dioxide gas) and ejecting it at the time of use, utilize the effect of promoting blood flow brought about by carbon dioxide. It is possible that it is under development.
• a propellant such as carbon dioxide (carbon dioxide gas)
• Patent Document 1 discloses a stock solution containing medicinal ingredients such as tocopherol acetate and glycyrrhetinic acid, and a foamy gingival recession prevention and improvement agent containing a carbon dioxide-containing propellant. is applied to the gingiva to prevent or improve gingival recession.
• Patent Document 2 discloses an oral aerosol containing a liquid dihydric alcohol, a medicinal ingredient, a nonionic surfactant and water in a predetermined amount and mass ratio, which contains a liquid dihydric alcohol and a propellant containing carbon dioxide.
• a drug is disclosed, and an attempt is made to enjoy the effects of medicinal ingredients while maintaining the health of the gums by the blood flow promoting effect of carbon dioxide.
• Patent Document 1 JP-A-2017-95382
• Patent Document 2 JP-A-2018-104320
• the present invention provides an oral aerosol comprising a liquid concentrate (X) and a propellant (Y), wherein the liquid concentrate (X) comprises the following components (a), (b) and (c): (a) Monohydric alcohol with 12 to 22 carbon atoms 0.6% by mass or more and 10% by mass or less (b) Surfactant (c) Contains water and contains component (b) in stock solution (X) Provided is an oral aerosol preparation having a mass ratio ((b)/(a)) of 0.08 or more and 10 or less and an ethanol content of 8 mass% or less. It is something to do.
• the present invention relates to an oral aerosol agent capable of exhibiting high foam performance and excellently protecting the gums.
• an oral aerosol containing a stock solution and a carbon dioxide-containing propellant contains a specific amount of a specific monohydric alcohol and a nonionic surfactant and water.
• the oral aerosol agent of the present invention it is possible to inject dense foam and exhibit high foam retention.
• the foam spreads widely in the oral cavity and adheres well to the gums. It is possible to obtain a coat feeling of
• FIG. 1 is a photograph taken with a digital camera of foam sprayed with the agent of Example 1.
• FIG. 4 is a photograph taken with a digital camera of bubbles sprayed with the agent of Comparative Example 1.
• FIG. 1 is a photograph taken with a digital camera of foam sprayed with the agent of Example 1.
• FIG. 4 is a photograph taken with a digital camera of bubbles sprayed with the agent of Comparative Example 1.
• the oral aerosol agent of the present invention is an agent that is applied to the oral cavity by filling an aerosol container with the undiluted solution (X) and the propellant (Y), and injecting the container at the time of use.
• the propellant (Y) contains carbon dioxide, part of it dissolves in the concentrate (X) and is also present inside the bubbles formed by the concentrate (X) after being ejected from the aerosol container. Therefore, it is possible to efficiently deliver carbon dioxide to the oral cavity while exhibiting excellent foam performance until after it is applied to the oral cavity and rinsed.
• the foam formed by spraying from the oral aerosol agent of the present invention provides a “soft and fine foam feeling” and “widely spreading in the oral cavity” after spraying and after rinsing.
• excellent foam performance The properties of "good adhesion to the gums while maintaining good adhesion” and "bringing a feeling that the gums are protected by a smooth film” are also generally referred to as "excellent foam performance”.
• the stock solution (X) contained in the oral aerosol preparation of the present invention contains 0.6% to 10% by mass of a monohydric alcohol having 12 to 22 carbon atoms as the component (a).
• component (a) By containing component (a), it is possible to form an ⁇ -gel having a lamellar structure together with component (b) in the presence of component (c), which will be described later.
• a foam can be formed that exhibits excellent foam performance.
• Component (a) is preferably one or more selected from cetanol, stearyl alcohol, lauryl alcohol, myristyl alcohol, and behenyl alcohol, more preferably one or two selected from cetanol and stearyl alcohol. , it further preferably contains both cetanol and stearyl alcohol as component (a).
• Component (a) preferably contains at least stearyl alcohol from the viewpoint of ensuring the expression of excellent foaming performance and from the viewpoint of enhancing coating feeling on the gums.
• the content of stearyl alcohol in the stock solution (X) is preferably 0.6% by mass or more, more preferably 0.65% by mass or more, and still more preferably 0.7% by mass or more. is 10% by mass or less, more preferably 7% by mass or less, still more preferably 4% by mass or less, and even more preferably 1.5% by mass or less.
• the content of component (a) is 0.6% by mass or more, preferably 0.8% by mass or more, in the stock solution (X) from the viewpoint of ensuring the expression of excellent foam performance. preferably 1.5% by mass or more, more preferably 1.8% by mass or more, and 10% by mass or less, preferably 8% by mass or less, more preferably 5% by mass or less, More preferably, it is 3% by mass or less.
• the content of component (a) is 0.6% by mass or more and 10% by mass or less, preferably 0.8 to 8% by mass, more preferably 1.5% by mass, in the stock solution (X). 5% by mass, more preferably 1.8 to 3% by mass.
• the stock solution (X) contained in the oral aerosol of the present invention contains a surfactant as component (b).
• component (b) By including component (b), together with component (a), it is possible to ensure the expression of excellent foaming performance from after spraying to after rinsing.
• the component (b) surfactant used in the present invention is preferably one or more selected from nonionic surfactants, anionic surfactants, and amphoteric surfactants.
• Ester-type nonionic surfactants are preferred as nonionic surfactants, and specific examples include sorbitan fatty acid esters, polyoxyethylene sorbitan fatty acid esters, polyoxyethylene fatty acid esters, higher fatty acid glycerol esters, and polyoxyethylene glyceryl mono-fatty acid esters. , and one or more selected from sucrose fatty acid esters. Among them, one or more selected from sorbitan fatty acid esters and polyoxyethylene sorbitan fatty acid esters are preferable from the viewpoint of imparting superior emulsion stability to the stock solution (X). It is more preferable to use ethylene sorbitan fatty acid ester together.
• those derived from fatty acids having 10 or more carbon atoms are preferable, those derived from fatty acids having 12 or more carbon atoms are more preferable, those derived from fatty acids having 20 or less carbon atoms are preferable, and those derived from fatty acids having 18 or less carbon atoms are preferable. is more preferred.
• sorbitan monocaprate sorbitan monoundecylate, sorbitan monolaurate, sorbitan monotridecylate, sorbitan monomyristate, sorbitan monopalmitate, sorbitan monooleate, sorbitan trioleate, sorbitan tetraoleate, sesqui
• sorbitan monostearate one or more selected from sorbitan monooleate, sorbitan sesquioleate, and sorbitan monostearate are preferred, and sorbitan monostearate is more preferred.
• polyoxyethylene sorbitan fatty acid ester those derived from fatty acids having 6 or more carbon atoms are preferable, those derived from fatty acids having 12 or more carbon atoms are more preferable, those derived from fatty acids having 22 or less carbon atoms are preferable, and those derived from fatty acids having 20 or less carbon atoms are preferable. are more preferred.
• the average number of added moles of ethoxy groups in the polyoxyethylene sorbitan fatty acid ester is preferably 5 to 40 mol, more preferably 10 to 25 mol, still more preferably 15 to 25 mol.
• polyoxyethylene sorbitan monolaurate polyoxyethylene sorbitan monomyristate, polyoxyethylene sorbitan monopalmitate, polyoxyethylene sorbitan monostearate, and polyoxyethylene sorbitan monooleate.
• 1 type, or 2 or more types are mentioned.
• one or more selected from polyoxyethylene sorbitan monopalmitate, polyoxyethylene sorbitan monostearate, and polyoxyethylene sorbitan monooleate are preferable, and polyoxyethylene sorbitan monostearate is more preferable.
• anionic surfactant those having a saturated or unsaturated hydrocarbon group having 8 to 18 carbon atoms and having a linear or branched chain as a lipophilic group are preferable. More preferably, the hydrocarbon group has 12 to 16 carbon atoms.
• Preferred hydrophilic groups are carboxylic acid, sulfonic acid, phosphoric acid, and salts thereof.
• ether phosphates fatty acid monoglyceride sulfates, alkylsulfoacetates, olefinsulfonates, and the like
• the salt is preferably an alkali metal salt or an alkaline earth metal salt, such as sodium salt, potassium salt, magnesium salt, etc. Among them, sodium salt is preferred.
• amphoteric surfactants include, for example, betaine acetates such as betaine lauryldimethylaminoacetate; imidazolinium betaines such as 2-alkyl-N-carboxymethyl-N-hydroxyethyl-N-imidazolium betaine; Alkylsulfobetaines such as laurylsulfobetaine and laurylhydroxysulfobetaine; coconut fatty acid amidoalkylbetaines such as coconut fatty acid amidopropyl betaine; long-chain alkyl imidazoline betaine salts such as sodium N-alkyl-1-hydroxyethylimidazoline betaine; 1 type or 2 types or more are mentioned.
• betaine acetates such as betaine lauryldimethylaminoacetate
• imidazolinium betaines such as 2-alkyl-N-carboxymethyl-N-hydroxyethyl-N-imidazolium betaine
• a nonionic surfactant is preferable as the component (b) from the viewpoint of ensuring the expression of excellent foam performance from after injection to after rinsing.
• the content of component (b) is preferably 0.03% by mass or more, more preferably 0.08% by mass or more, in the stock solution (X) from the viewpoint of ensuring the expression of excellent foam performance. , More preferably 0.15% by mass or more, still more preferably 0.3% by mass or more, still more preferably 0.5% by mass or more, preferably 15% by mass or less, more preferably is 5% by mass or less, more preferably 3% by mass or less, and even more preferably 1.8% by mass or less.
• the content of component (b) is preferably 0.03% by mass or more and 15% by mass or less, more preferably 0.08 to 5% by mass, and still more preferably 0% by mass in the stock solution (X). 0.15 to 5% by mass, more preferably 0.3 to 3% by mass, and even more preferably 0.5 to 1.8% by mass.
• component (b) is a nonionic surfactant
• its content in the stock solution (X) is preferably 0.03% by mass or more, more preferably 0.08% by mass or more, and still more preferably is 0.15% by mass or more, more preferably 0.3% by mass or more, still more preferably 0.5% by mass or more, preferably 15% by mass or less, more preferably 5% by mass % or less, more preferably 3 mass % or less, and even more preferably 1.8 mass % or less.
• component (b) is an anionic surfactant
• its content in the stock solution (X) is preferably 0.4% by mass or less, more preferably 0.1% by mass or less, and even more preferably is 0.01% by mass or less.
• component (b) is an amphoteric surfactant
• its content in the stock solution (X) is preferably 0.03% by mass or more, more preferably 0.15% by mass or more, and still more preferably is 0.3% by mass or more, preferably 15% by mass or less, more preferably 3% by mass or less, and still more preferably 1% by mass or less.
• the mass ratio ((b)/(a)) between the content of component (b) and the content of component (a) in stock solution (X) is 0 from the viewpoint of ensuring the stability of stock solution (X). 0.08 or more, preferably 0.1 or more, more preferably 0.14 or more, still more preferably 0.23 or more, still more preferably 0.3 or more, and 10 or less It is preferably 7 or less, more preferably 3 or less, still more preferably 2 or less, even more preferably 1.5 or less, and even more preferably 0.8 or less.
• the mass ratio ((b)/(a)) between the content of component (b) and the content of component (a) in stock solution (X) is 0.08 or more and 10 or less, preferably 0.1 to 7, more preferably 0.14 to 3, still more preferably 0.14 to 2, even more preferably 0.23 to 1.5, still more preferably 0. 3 to 0.8.
• the stock solution (X) contained in the oral aerosol preparation of the present invention contains water as component (c).
• the water of component (c) in the present invention means not only the purified water and the like blended in the concentrate (X) but also the water contained in each component blended, which means all the water contained in the concentrate (X). do.
• each component is well dispersed or dissolved while securing a suitable viscosity and good shape retention as the stock solution (X), and excellent foam performance is expressed. can be secured.
• the content of component (c) in stock solution (X) is preferably 50% by mass or more, more preferably 60% by mass or more, still more preferably 71% by mass or more, and even more preferably 74% by mass. % or more, preferably 98% by mass or less, more preferably 95% by mass or less, even more preferably 85% by mass or less, and even more preferably 80% by mass or less.
• the content of component (c) is preferably 50% by mass or more and 98% by mass or less, more preferably 60 to 95% by mass, and still more preferably 71 to 85% by mass in the stock solution (X). and more preferably 74 to 80% by mass.
• the stock solution (X) contained in the oral aerosol preparation of the present invention has an ethanol content of 8% by mass or less. In this way, by limiting the content of ethanol in the stock solution (X), it is possible to effectively prevent the occurrence of foam defoaming and foam breaking in the foam after spraying, and the development of unnecessary irritation. can be suppressed.
• the content of ethanol in the stock solution (X) is 8% by mass or less, preferably 6% by mass or less, more preferably 4% by mass or less, and still more preferably 2% by mass or less, Even more preferably, it is 0.4% by mass or less, or the stock solution (X) preferably does not contain ethanol.
• the stock solution (X) contained in the oral aerosol preparation of the present invention contains a binding agent
• the storage stability of the agent can be satisfactorily secured while maintaining an appropriate viscosity, and there is no need to interfere with injection. It is possible to effectively prevent serious clogging from occurring in the container.
• Specific examples of such binders include sodium carboxymethylcellulose, hydroxyethylcellulose, xanthan gum, hydroxypropylcellulose, hydroxypropylmethylcellulose, pectin, tragacanth gum, gum arabic, guar gum, karaya gum, locust bean gum, gellan gum, and tamarind gum. , psyllium seed gum, polyvinyl alcohol, sodium chondroitin sulfate, and methoxyethylene maleic anhydride copolymer.
• the content of the caking agent is preferably 1% by mass or less, more preferably 0.1% by mass, in the stock solution (X) from the viewpoint of effectively preventing unnecessary clogging while maintaining an appropriate viscosity. It is 8% by mass or less, more preferably 0.6% by mass or less, and even more preferably 0.05% by mass or less.
• the stock solution (X) may not contain a binder.
• the stock solution (X) contained in the oral aerosol preparation of the present invention is one or more polyols (d) selected from glycerin, propylene glycol, ethylene glycol, sorbitol, xylitol, erythritol, reduced palatinose, and mannitol. may contain.
• the component (d) is preferably one or more selected from glycerin, sorbitol, xylitol, erythritol, reduced palatinose, and mannitol, and one selected from glycerin, sorbitol, xylitol, and erythritol.
• a species or two or more species are more preferable.
• the content of component (d) in the stock solution (X) is preferably 30% by mass or less, more preferably 25% by mass or less, still more preferably 18% by mass or less, and even more preferably 8% by mass. % by mass or less, or the stock solution (X) may not contain the component (d).
• the stock solution (X) contained in the oral aerosol preparation of the present invention should contain, in addition to the above components, pH adjusters, preservatives, medicinal ingredients, fragrances, pigments, etc., within a range that does not inhibit the effects of the present invention. can be done.
• the viscosity of the stock solution (X) at 25° C. is preferably 500 mPa ⁇ s or more from the viewpoint of exhibiting excellent foam performance without being influenced by temperature changes and from the viewpoint of good jetting of the stock solution (X) from an aerosol container. , more preferably 700 mPa s or more, still more preferably 1000 mPa s or more, still more preferably 1300 mPa s or more, still more preferably 1800 mPa s or more, preferably 8000 mPa s or less, more preferably 6000 mPa ⁇ s or less, still more preferably 5000 mPa ⁇ s or less, and even more preferably 4000 mPa ⁇ s or less.
• the viscosity of the stock solution (X) can be measured with a BM type viscometer (manufactured by Toki Sangyo Co., Ltd.).
• the propellant (Y) contained in the oral aerosol of the present invention preferably contains carbon dioxide.
• Carbon dioxide can contribute to the development of high foam retention while facilitating dense foam jetting.
• the carbon dioxide content in the propellant (Y) is preferably 51% by mass or more, more preferably 80% by mass or more, and still more preferably 90% by mass, from the viewpoint of ensuring the expression of excellent foam performance.
• the content of carbon dioxide refers to the state before part of the carbon dioxide is dissolved in the stock solution (X), although part of it can be dissolved in the stock solution (X) during storage, that is, the stock solution ( It means the content in propellant (Y) before mixing X) and propellant (Y) or before filling them into an aerosol container.
• the propellant (Y) contains one or more selected from nitrogen; liquefied petroleum gases such as isobutane, normal butane, and mixtures thereof; and liquefied gases such as dimethyl ether and isopentane. It can also be used as a mixed gas with carbon dioxide.
• the mass ratio ((X):(Y)) of the stock solution (X) and the propellant (Y) is preferably 95: 5 to 99:1, more preferably 97:3 to 98.5:1.5.
• the mass of the content of carbon dioxide in the propellant (Y) and the content of the component (a) in the stock solution (X) is preferably 0.02 or more, more preferably 0.18 or more, still more preferably 0.2 or more, and even more preferably 0.25 or more. , more preferably 0.35 or more, preferably 5 or less, more preferably 3 or less, still more preferably 2.5 or less, and even more preferably 1.5 or less.
• the mass of the content of carbon dioxide in the propellant (Y) and the content of the component (b) in the stock solution (X) is preferably 0.02 or more, more preferably 0.25 or more, still more preferably 0.5 or more, and even more preferably 0.8 or more. , preferably 25 or less, more preferably 20 or less, even more preferably 12 or less, and even more preferably 6 or less.
• the oral aerosol agent of the present invention is obtained by compressing the propellant (Y) and filling it in an aerosol container, and from the viewpoint that it is possible to form bubbles having excellent performance by injecting from the container at the time of use,
• Such an aerosol container is preferably provided with a foam outlet.
• the production of the oral aerosol preparation of the present invention after the stock solution (X) is prepared, it is filled in an aerosol container together with the propellant (Y), and then sealed under pressure if necessary.
• the pressure inside the aerosol container is preferably 0.5 to 0.9 MPa, more preferably 0.7 to 0.8 MPa at 25° C. from the viewpoint of ensuring excellent foam performance.
• the oral aerosol preparation of the present invention is preferably sprayed from a container at the time of use, placed on a toothbrush or fingertip, and then applied to a desired site.
• the applied amount of the oral aerosol of the present invention per use is preferably 0.4-1.5 g, more preferably 0.5-1.0 g.
• the present invention further discloses the following oral aerosol agents.
• Component (a) is preferably cetanol and one or more selected from stearyl alcohol, lauryl alcohol, myristyl alcohol, and behenyl alcohol, more preferably one or more selected from cetanol and stearyl alcohol.
• the content of component (a) in the stock solution (X) is preferably 0.8% by mass or more, more preferably 1.5% by mass or more, and still more preferably 1.8% by mass.
• Component (b) is preferably one or more selected from nonionic surfactants, anionic surfactants, and amphoteric surfactants, more preferably nonionic surfactants, still more preferably is an ester-type nonionic surfactant, more preferably one or more selected from sorbitan fatty acid esters and polyoxyethylene sorbitan fatty acid esters, and even more preferably sorbitan fatty acid esters and polyoxyethylene sorbitan
• the oral aerosol agent according to any one of [1] to [3] above containing both fatty acid esters.
• the content of component (b) in the stock solution (X) is preferably 0.03% by mass or more, more preferably 0.08% by mass or more, and still more preferably 0.15% by mass. or more, more preferably 0.3% by mass or more, still more preferably 0.5% by mass or more, preferably 15% by mass or less, more preferably 5% by mass or less, and further
• the mass ratio ((b)/(a)) between the content of component (b) and the content of component (a) in stock solution (X) is preferably 0.1 or more, more preferably is 0.14 or more, more preferably 0.23 or more, still more preferably 0.3 or more, preferably 7 or less, more preferably 3 or less, still more preferably 2 or less.
• the content of component (c) in the stock solution (X) is preferably 50% by mass or more, more preferably 60% by mass or more, still more preferably 71% by mass or more, and still more It is preferably 74% by mass or more, preferably 98% by mass or less, more preferably 95% by mass or less, still more preferably 85% by mass or less, and even more preferably 80% by mass or less [ 1] to [6]
• the oral aerosol preparation according to any one of [1].
• the content of ethanol in the stock solution (X) is preferably 6% by mass or less, more preferably 4% by mass or less, still more preferably 2% by mass or less, and even more preferably 0
• the content of the caking agent in the stock solution (X) is preferably 1% by mass or less, more preferably 0.8% by mass or less, and still more preferably 0.6% by mass or less. , and more preferably 0.05% by mass or less.
• Stock solution (X) may contain one or more polyols (d) selected from glycerin, propylene glycol, ethylene glycol, sorbitol, xylitol, erythritol, reduced palatinose, and mannitol,
• the component (d) is preferably one or more selected from glycerin, sorbitol, xylitol, erythritol, reduced palatinose, and mannitol, and one or two selected from glycerin, sorbitol, xylitol, and erythritol.
• the content of component (d) in the stock solution (X) is preferably 30% by mass or less, more preferably 25% by mass or less, still more preferably 18% by mass or less, and still more
• the oral aerosol agent according to [10] above, which preferably contains 8% by mass or less, or the stock solution (X) may not contain component (d).
• the propellant (Y) preferably contains carbon dioxide, and the carbon dioxide content in the propellant (Y) is preferably 51% by mass or more, more preferably 80% by mass or more. , more preferably 90% by mass or more, still more preferably 95% by mass or more, preferably 100% by mass or less, and more preferably 100% by mass [1] to [11] Any one of Or 1 oral aerosol agent.
• the mass ratio ((X):(Y)) between the stock solution (X) and the propellant (Y) is preferably 95:5 to 99:1, more preferably 97:3 to 98.5. :
• the mass ratio (carbon dioxide/(a)) between the content of carbon dioxide in the propellant (Y) and the content of component (a) in the stock solution (X) is preferably 0.02 or more. , more preferably 0.18 or more, still more preferably 0.2 or more, still more preferably 0.25 or more, still more preferably 0.35 or more, preferably 5 or less , more preferably 3 or less, still more preferably 2.5 or less, still more preferably 1.5 or less, the oral aerosol agent of [12] or [13].
• the mass ratio (carbon dioxide/(b)) between the content of carbon dioxide in the propellant (Y) and the content of component (b) in the stock solution (X) is preferably 0.02 or more.
• Examples 1 to 33, Comparative Examples 1 to 7 Each stock solution (X) was prepared according to the prescriptions in Tables 1 to 6, and after filling an aerosol container (manufactured by Takeuchi Press Co., Ltd.) with this, the propellant (Y) was enclosed in the ratio shown in Tables 1 to 6, Each agent was manufactured by setting the pressure in the container at 25° C. to 0.9 MPa. Using the obtained agent, each measurement and evaluation were performed according to the following methods. The results are shown in Tables 1-6.
• Example 1 Foam retention: over 300 seconds Gums coated feeling: 3
• Example 16 Foam retention: over 300 seconds, feeling of gum coating: 2
• Example 6 ⁇ Evaluation of oral irritation>> Using each agent obtained in Example 1, Example 6, and Comparative Example 6, about 0.5 g of foam was sprayed from each container onto a toothbrush, brushed for 3 minutes, rinsed, and then stimulated in the oral cavity. The presence or absence of was evaluated. As a result, although Examples 1 and 6 did not feel irritation, Comparative Example 6 felt irritation.

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• 2023
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