Oral aerosol agent
Patent Information
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- KAO CORP
- Filing Date
- 2023-09-05
- Publication Date
- 2026-06-23
Abstract
Description
[Technical field]
[0001] The present invention relates to an aerosol for the oral cavity. [Background technology]
[0002] Conventionally, many oral compositions have been known that utilize the characteristics of various dosage forms such as pastes and liquids. Among them, various preparations have been developed in which a propellant using liquefied gas, carbon dioxide, or the like is filled in an aerosol container together with the oral composition.
[0003] For example, Patent Document 1 discloses an aerosol-type preparation in which an isopropylmethylphenol-containing dentifrice composition is filled in an aerosol container together with a propellant, enhancing the biofilm disinfecting effect. Patent Document 2 discloses a foam-type gingival recession prevention and improvement agent that contains a concentrate containing a medicinal ingredient and a propellant containing carbon dioxide, and aims to prevent or improve gingival recession. On the other hand, Patent Document 3 discloses a foamable dental composition that contains a film-forming component and may further contain a propellant containing a gas such as nitrogen or carbon dioxide, a surfactant, and a higher alcohol such as cetyl alcohol as a foam stabilizer, and attempts to form a retentive coating on the surface of the teeth.
[0004] Meanwhile, compounds that contain fluorine, such as sodium fluoride and sodium monofluorophosphate, so-called fluorine-containing compounds, are known as useful components that can adsorb fluorine to the tooth surface and promote the progress of remineralization, and are described as components that can be used in all of the above patent documents. [Prior art documents] [Patent documents]
[0005] [Patent Document 1] JP 2011-256125 A [Patent Document 2] JP 2017-95382 A [Patent Document 3] Special Publication No. 2009-522003 Summary of the Invention [Problem to be solved by the invention]
[0006] However, it has now been discovered that when preparing an aerosol preparation using a propellant together with a concentrate for application to the oral cavity, if the concentrate contains a fluorine-containing compound together with a higher alcohol such as cetyl alcohol in consideration of foaming performance, etc., the storage stability of the preparation may be impaired and retention on the brush part of a toothbrush may be reduced, requiring improvement.
[0007] Therefore, the present invention relates to an oral aerosol preparation which has excellent storage stability and exhibits good retention on the brush part of a toothbrush, even though it uses a concentrate containing a higher alcohol and a fluorine-containing compound together with a propellant. [Means for solving the problem]
[0008] The present inventors have therefore conducted various investigations and have found that, in an oral aerosol preparation comprising a concentrate and a propellant, by using a concentrate containing a specific anionic surfactant together with a specific monohydric alcohol, and a fluorine-containing compound in a specific mass ratio relative to the anionic surfactant, it is possible to obtain an oral aerosol preparation which can effectively ensure the storage stability of the entire preparation.
[0009] That is, the present invention provides an oral aerosol preparation comprising a concentrate (X) and a propellant (Y), wherein the concentrate (X) contains the following components (a), (b), and (c): (a) Monohydric alcohol having 12 to 22 carbon atoms (b) Anionic surfactants having a hydrocarbon group having 12 to 22 carbon atoms (c) Fluorine-containing compounds Contains The present invention provides an oral aerosol preparation in which the mass ratio ((b) / (c)) of the content of component (b) in the original solution (X) to the content of component (c) calculated as fluorine atoms is 0.285 or more and 2500 or less. Effect of the Invention
[0010] The oral aerosol preparation of the present invention allows the concentrate (X) to maintain a suitable viscosity after storage without excessive thickening, and ensures excellent storage stability throughout the preparation. As a result, it can maintain good sprayability from the container and can be retained well on the brush part of a toothbrush, providing a comfortable feel when used. DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS
[0011] The present invention will be described in detail below. The term "toothbrushing tool" refers to a tool having a brush part formed of at least a plurality of bristles or projections, and for performing the action of brushing teeth by operating the brush part manually or electrically. The overall shape of the toothbrushing tool may be like that of a normal toothbrush, or like that of a finger cot. The oral aerosol agent of the present invention is sprayed onto the brush part of such a toothbrushing tool and temporarily placed on the brush part, and the toothbrushing tool is then moved and inserted into the oral cavity to perform the action of brushing teeth.
[0012] In addition, "excellent storage stability" means that the concentrate (X) maintains a suitable viscosity without excessive thickening from immediately after production to after storage, and that the contained components do not separate (separate water) and no precipitates are formed. Furthermore, "good retention on the brush part" means that from the time the oral aerosol of the present invention is sprayed and placed on the brush part, to the time the toothbrush instrument is moved and inserted into the oral cavity, no dripping occurs from the brush part and the shape of the agent is maintained on the brush part just after it is ejected.
[0013] The concentrate (X) contained in the oral aerosol preparation of the present invention contains, as component (a), a monohydric alcohol having 12 to 22 carbon atoms. By containing such component (a), an α-gel can be formed together with component (b) described below, and the storage stability of the entire preparation can be effectively achieved.
[0014] Component (a) has 12 or more, preferably 14 or more, more preferably 16 or more, and 22 or less, preferably 20 or less, more preferably 18 or less. Specifically, 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, still more preferably component (a) contains at least stearyl alcohol, and even more preferably contains both cetanol and stearyl alcohol.
[0015] From the viewpoint of ensuring good retention on the toothbrush, the content of component (a) in the original solution (X) is preferably 0.6% by mass or more, more preferably 0.8% by mass or more, even more preferably 1.5% by mass or more, even more preferably 1.8% by mass or more, preferably 10% by mass or less, more preferably 8% by mass or less, even more preferably 5% by mass or less, and even more preferably 3% by mass or less. The content of component (a) in the original solution (X) is preferably 0.6% by mass or more and 10% by mass or less, more preferably 0.8 to 8% by mass, even more preferably 1.5 to 5% by mass, and even more preferably 1.8 to 3% by mass.
[0016] Furthermore, when stearyl alcohol is contained as component (a), the content of such stearyl alcohol in the concentrate (X) is preferably 0.6% by mass or more, more preferably 0.65% by mass or more, even more preferably 0.7% by mass or more, preferably 10% by mass or less, more preferably 7% by mass or less, even more preferably 4% by mass or less, and even more preferably 1.5% by mass or less.
[0017] The concentrate (X) contained in the oral aerosol preparation of the present invention contains, as component (b), an anionic surfactant having a hydrocarbon group having from 12 to 22 carbon atoms. By containing such component (b) in a specific mass ratio with a fluorine-containing compound of component (c) described below, the concentrate (X) after storage can maintain an appropriate viscosity without excessive thickening, and the storage stability of the entire preparation can be effectively achieved.
[0018] The hydrocarbon group contained in component (b) is preferably a saturated or unsaturated hydrocarbon group, and is a hydrocarbon group having a straight or branched chain as a lipophilic group. The number of carbon atoms in the hydrocarbon group is 12 or more, preferably 14 or more, more preferably 16 or more, and 22 or less, preferably 20 or less, more preferably 18 or less. In addition, it is preferable that the hydrophilic group contains a carboxylic acid, a sulfonic acid, a phosphoric acid, or a salt thereof.
[0019] Specific examples of the component (b) include alkyl sulfates such as lauryl sulfate, myristyl sulfate, palmityl sulfate, stearyl sulfate, octyl sulfate, and capryl sulfate; Polyoxyethylene alkyl ether sulfates such as laureth sulfate and triethanolamine laureth sulfate; Alkyl sulfosuccinates such as lauryl sulfosuccinate dibasic and dioctyl sulfosuccinate; acylamino acid salts such as acyl glutamate and acyl sarcosine salt; acyltaurine salts such as cocoyl fatty acid taurine salts, cocoyl methyl taurine salts, cocoyl methyl taurine salts, caproyl methyl taurine salts, lauroyl taurine salts, lauroyl methyl taurine salts, myristoyl methyl taurine salts, palmitoyl methyl taurine salts, stearoyl methyl taurine salts, and oleoyl methyl taurine salts; acyl isethionates such as cocoyl isethionate; Alkyl sulfonates such as alkyl benzene sulfonates, α-olefin sulfonates, and hydroxyalkane sulfonates; Examples of the salt include one or more selected from polyoxyethylene alkyl ether sulfosuccinates, alkyl ether carboxylates, alkyl phosphates, polyoxyethylene alkyl ether phosphates, fatty acid monoglyceride sulfates, alkyl sulfoacetates, etc. As the salt, an alkali metal salt or an alkaline earth metal salt is preferred, for example, a sodium salt, a potassium salt, a magnesium salt, etc., and among these, a sodium salt is preferred.
[0020] Among these, from the viewpoint of effectively achieving the storage stability of the entire agent while maintaining the appropriate viscosity of the original solution (X) after storage, one or more types selected from acylamino acid salts, acyltaurine salts, α-olefin sulfonates, and alkyl sulfate salts are preferred, and one or more types selected from acylamino acid salts, acyltaurine salts, and α-olefin sulfonates are more preferred.
[0021] More specifically, the acyl group of the acyl amino acid salt and the acyltaurine salt is derived from a fatty acid having a saturated or unsaturated straight or branched chain or a mixed fatty acid thereof, and is preferably derived from a straight chain fatty acid or a mixed fatty acid of straight chain fatty acids.As the acyl group, one or more selected from lauroyl group, myristoyl group, palmitoyl group, stearoyl group, and cocoyl group are preferred, one or more selected from lauroyl group, myristoyl group, and stearoyl group are more preferred, and stearoyl group is even more preferred.
[0022] The amino acid moiety constituting the acylamino acid salt may be any of glutamic acid, aspartic acid, and glycine, and may be any of D-form, L-form, or a mixture of D-form and L-form, and is preferably L-form. Specifically, the acylamino acid is preferably one or more selected from lauroyl glutamic acid, myristoyl glutamic acid, stearoyl glutamic acid, cocoyl glutamic acid, lauroyl aspartic acid, myristoyl aspartic acid, cocoyl aspartic acid, lauroyl glycine, myristoyl glycine, stearoyl glycine, and cocoyl glycine, more preferably one or two selected from lauroyl glutamic acid, myristoyl glutamic acid, and stearoyl glutamic acid, and even more preferably stearoyl glutamic acid.
[0023] The acyltaurine is preferably one or more selected from cocoyl fatty acid taurine, cocoyl methyl taurine, caproyl methyl taurine, lauroyl taurine, lauroyl methyl taurine, myristoyl methyl taurine, palmitoyl methyl taurine, stearoyl methyl taurine, and oleoyl methyl taurine, more preferably one or more selected from lauroyl methyl taurine, myristoyl methyl taurine, and stearoyl methyl taurine, and even more preferably stearoyl methyl taurine.
[0024] More specifically, the olefin group contained in the α-olefin sulfonate preferably has 14 to 16 carbon atoms, and more preferably has 14 carbon atoms.
[0025] From the viewpoint of effectively achieving the storage stability of the entire agent while maintaining the appropriate viscosity of the original solution (X), the content of component (b) in the original solution (X) is preferably 0.1% by mass or more, more preferably 0.2% by mass or more, even more preferably 0.3% by mass or more, even more preferably 0.4% by mass or more, preferably 3% by mass or less, more preferably 2.5% by mass or less, even more preferably 2% by mass or less, and even more preferably 1.5% by mass or less. The content of component (b) in the original solution (X) is preferably 0.1% by mass or more and 3% by mass or less, more preferably 0.2 to 2.5% by mass, even more preferably 0.3 to 2% by mass, and even more preferably 0.4 to 1.5% by mass.
[0026] The mass ratio ((b) / (a)) of the content of component (b) to the content of component (a) is preferably 0.05 or more, more preferably 0.1 or more, even more preferably 0.2 or more, preferably 1.25 or less, more preferably 1 or less, and even more preferably 0.75 or less, from the viewpoint of maintaining an appropriate viscosity in the original solution (X) and from the viewpoint of effectively achieving the storage stability of the entire agent. The mass ratio ((b) / (a)) of the content of component (b) to the content of component (a) is preferably 0.05 to 1.25, more preferably 0.1 to 1, and even more preferably 0.2 to 0.75.
[0027] The concentrate (X) contained in the oral aerosol of the present invention contains a fluorine-containing compound as component (c). Such a fluorine-containing compound is a compound containing a fluorine atom in its molecular structure. Such component (c) is a component that releases fluoride ions when applied to the oral cavity, and can promote remineralization by adsorbing fluorine to the tooth surface, but in an oral aerosol using a propellant, it is also a component that may cause a decrease in the storage stability of the entire agent. However, the oral aerosol of the present invention can stably release fluoride ions even after storage. Specific examples of the component (c) include one or more compounds selected from monofluorophosphate ion-supplying compounds and fluoride ion-supplying compounds.
[0028] The monofluorophosphate ion supplying compound is a compound that supplies monofluorophosphate ions as fluoride ions. Examples of such monofluorophosphate ion supplying compounds include one or more selected from sodium monofluorophosphate, potassium monofluorophosphate, magnesium monofluorophosphate, calcium monofluorophosphate, etc. Among them, sodium monofluorophosphate is preferred.
[0029] The fluoride ion supplying compound is a fluorine-containing compound other than the monofluorophosphate ion supplying compound. Such a fluoride ion supplying compound may be one or more selected from sodium fluoride, stannous fluoride, potassium fluoride, zinc fluoride, betaine fluoride, stannous alanine fluoride, sodium fluorosilicate, hexylamine fluoride, etc. Among them, sodium fluoride is preferred.
[0030] Among these, from the viewpoint of ensuring excellent storage stability while fully enjoying the effects of fluoride ions, it is preferable that component (c) is a monofluorophosphate ion donating compound.
[0031] From the viewpoint of ensuring excellent storage stability and fully enjoying the effects of fluoride ions, the content of component (c) in the original solution (X) is preferably 0.001 mass% or more, more preferably 0.005 mass% or more, even more preferably 0.01 mass% or more, preferably 0.7 mass% or less, more preferably 0.6 mass% or less, and even more preferably 0.5 mass% or less, calculated as fluorine atoms. The content of component (c) in the original solution (X) is preferably 0.001 mass% or more and 0.7 mass% or less, more preferably 0.005 to 0.6 mass%, and even more preferably 0.01 to 0.5 mass%, calculated as fluorine atoms.
[0032] The mass ratio ((b) / (c)) of the content of component (b) to the content of component (c) calculated as fluorine atoms is, from the viewpoint of maintaining an appropriate viscosity in the original solution (X) and from the viewpoint of effectively achieving the storage stability of the entire agent, 0.285 or more, preferably 0.5 or more, more preferably 0.8 or more, and 2500 or less, preferably 400 or less, and more preferably 150 or less. The mass ratio ((b) / (c)) of the content of component (b) to the content of component (c) calculated as fluorine atoms is 0.285 or more and 2500 or less, preferably 0.5 to 400, and more preferably 0.8 to 150.
[0033] From the viewpoint of ensuring excellent storage stability while fully enjoying the effects of fluoride ions, the mass ratio ((c) / (a)) of the content of component (c) calculated as fluorine atoms to the content of component (a) is preferably 0.1 or more, more preferably 0.5 or more, even more preferably 1 or more, and preferably 400 or less, more preferably 300 or less, and even more preferably 200 or less. The mass ratio ((c) / (a)) of the content of component (c) calculated as fluorine atoms to the content of component (a) is preferably 0.1 to 400, more preferably 0.5 to 300, and even more preferably 1 to 200.
[0034] The concentrate (X) contained in the oral aerosol preparation of the present invention preferably further contains a nonionic surfactant (d) from the viewpoint of further enhancing the storage stability of the entire preparation.
[0035] Specific examples of the component (d) include polyoxyethylene hydrogenated castor oil; Sucrose fatty acid esters; Sorbitan fatty acid esters such as sorbitan monocaprate, sorbitan monoundecylate, sorbitan monolaurate, sorbitan monotridecylate, sorbitan monomyristate, sorbitan monopalmitate, sorbitan monooleate, sorbitan trioleate, sorbitan tetraoleate, sorbitan sesquioleate, sorbitan monostearate, and sorbitan tristearate; Polyoxyethylene sorbitan fatty acid esters such as polyoxyethylene sorbitan monolaurate, polyoxyethylene sorbitan monomyristate, polyoxyethylene sorbitan monopalmitate, polyoxyethylene sorbitan monostearate, and polyoxyethylene sorbitan monooleate; Glycerol fatty acid esters such as monostearate glyceride; Alkyl glucosides; Polyglycerol fatty acid esters such as monostearate decaglyceride and monomyristate decaglyceride; polyoxyethylene alkyl phenyl ethers such as polyoxyethylene monoalkyl (or alkenyl) ether, polyoxyethylene polyoxypropylene copolymer, and polyoxyethylene nonyl phenyl ether; fatty acid alkanolamides such as coconut fatty acid diethanolamide; One or more selected from polyethylene glycol fatty acid esters can be mentioned.
[0036] Among these, from the viewpoint of effectively enhancing the storage stability of the entire agent, one or more selected from sorbitan fatty acid esters and polyoxyethylene sorbitan fatty acid esters are preferred, and one or more selected from sorbitan monooleate, sorbitan sesquioleate, sorbitan monostearate, polyoxyethylene sorbitan monopalmitate, polyoxyethylene sorbitan monostearate, and polyoxyethylene sorbitan monooleate are more preferred, and it is even more preferred to contain both a sorbitan fatty acid ester and a polyoxyethylene sorbitan fatty acid ester.
[0037] From the viewpoint of more effectively achieving the storage stability of the entire agent, the content of component (d) in the stock solution (X) is preferably 0.03% by mass or more, more preferably 0.08% by mass or more, even more preferably 0.15% by mass or more, even more preferably 0.3% by mass or more, preferably 20% by mass or less, more preferably 15% by mass or less, even more preferably 5% by mass or less, and even more preferably 3% by mass or less. The content of component (d) in the stock solution (X) is preferably 0.03% by mass or more and 20% by mass or less, more preferably 0.08 to 15% by mass, even more preferably 0.15 to 5% by mass, and even more preferably 0.3 to 3% by mass.
[0038] From the viewpoint of effectively achieving the storage stability of the entire agent while maintaining an appropriate viscosity in the original solution (X), the mass ratio of the content of component (d) to the content of component (a) ((d) / (a)) is preferably 0.003 or more, more preferably 0.01 or more, even more preferably 0.02 or more, and preferably 40 or less, more preferably 30 or less, and even more preferably 20 or less. The mass ratio of the content of component (d) to the content of component (a) ((d) / (a)) is preferably 0.003 to 40, more preferably 0.01 to 30, and even more preferably 0.02 to 20.
[0039] The concentrate (X) contained in the oral aerosol of the present invention may contain one or more polyols (e) selected from glycerin, ethylene glycol, butylene glycol, propylene glycol, sorbitol, xylitol, erythritol, reduced palatinose, and mannitol. Among them, the component (e) is preferably one or more selected from glycerin, butylene glycol, propylene glycol, sorbitol, xylitol, erythritol, reduced palatinose, and mannitol, and more preferably one or more selected from glycerin, sorbitol, xylitol, and erythritol.
[0040] The content of component (e) in the raw solution (X) is preferably 30 mass% or less, more preferably 25 mass% or less, even more preferably 18 mass% or less, and even more preferably 8 mass% or less, or the raw solution (X) may not contain component (e).
[0041] The concentrate (X) contained in the oral aerosol of the present invention may contain a flavoring (f). Examples of such a component (f) include menthol, pulegol, carvone, anethole, cineole, methyl salicylate, cinnamic aldehyde, eugenol, 3-1-menthoxypropane-1,2-diol, thymol, citronellyl acetate, linalool, linalyl acetate, geraniol, geranyl acetate, citronellol, limonene, menthone, menthyl acetate, N-substituted-paramenthan-3-carboxamide, pinene, octyl aldehyde, citral, pulegone, carby acetate, dihydrocarbyl acetate, anisaldehyde, benzaldehyde, camphor, lactone, ethyl acetate, ethyl butyrate, allyl cyclohexyl propionate, methyl anthranilate, ethyl methylphenyl glycidate, vanillin, undecalactone, hexanal, butyl acetate, isoamyl acetate, hexenol, dimethyl sulfide, cyclotene, furfural, trimethylpyrazine, ethyl lactate, methyl lactate, ethyl thioacetate, etc. single flavoring components; blended flavoring components such as strawberry flavor, apple flavor, banana flavor, pineapple flavor, grape flavor, mango flavor, butter flavor, milk flavor, fruit mix flavor, and tropical fruit flavor; and also peppermint oil, spearmint oil, cinnamon oil, anise oil, eucalyptus oil, wintergreen oil, cassia oil, clove oil, thyme oil, sage oil, sage clary oil, nutmeg oil, funnel oil, The fragrance ingredients may be natural fragrance ingredients such as lemon oil, orange oil, mint oil, cardamom oil, coriander oil, basil oil, mandarin oil, lime oil, lavender oil, rosemary oil, ginger oil, grapefruit oil, laurel oil, chamomile oil, caraway oil, marjoram oil, bay oil, lemongrass oil, lemon balm oil, pimento berry oil, palmarosa oil, olibanum oil, pine needle oil, petitgrain oil, neroli oil, rose oil, and jasmine oil, and may also be fragrance ingredients obtained by processing these natural fragrance ingredients. In addition, fragrance compounds described in "Perfume and Flavor Chemicals" edited by Steffen Arctander, Montclair, NJ (USA) (1969), "Synthetic Fragrances - Chemistry and Product Knowledge" edited by the Synthetic Fragrances Editorial Committee (The Chemical Daily, December 20, 2016, revised and expanded edition), and "Basic Knowledge of Fragrances and Fragrances" edited by Nakajima Mototaka, Sangyo Tosho (first edition, 1995) can also be used.
[0042] The content of component (f) in the original solution (X) is preferably 0.01% by mass or more, more preferably 0.1% by mass or more, even more preferably 0.5% by mass or more, and preferably 3% by mass or less, more preferably 2% by mass or less, even more preferably 1% by mass or less.
[0043] The concentrate (X) contained in the oral aerosol of the present invention contains water (g). The water of the component (g) in the present invention means the total water contained in the concentrate (X), including not only the purified water etc. contained in the concentrate (X) but also the water contained in each of the components contained therein. By containing the water of the component (g), it is possible to ensure the appropriate viscosity and good shape retention of the concentrate (X), while dispersing or dissolving each component well, thereby improving the storage stability of the entire preparation.
[0044] The content of component (g) in the raw solution (X) is preferably 50% by mass or more, more preferably 60% by mass or more, even more preferably 71% by mass or more, still more 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 still more preferably 80% by mass or less. The content of component (g) in the raw solution (X) is preferably 50% by mass or more and 98% by mass or less, more preferably 60 to 95% by mass, still more preferably 71 to 85% by mass, and still more preferably 74 to 80% by mass.
[0045] The concentrate (X) contained in the oral aerosol preparation of the present invention has an ethanol content of 8% by mass or less. By limiting the ethanol content in the concentrate (X) in this way, it is possible to effectively prevent the storage stability of the entire preparation from being unnecessarily impaired. The content of ethanol in the original solution (X) is 8% by mass or less, preferably 6% by mass or less, more preferably 4% by mass or less, even more preferably 2% by mass or less, and even more preferably 0.4% by mass or less, or it is preferable that the original solution (X) does not contain ethanol.
[0046] When the concentrate (X) contained in the oral aerosol of the present invention contains a binder, it is preferable to moderately limit the content of the binder. In this way, by avoiding an excessive content of the binder in the concentrate (X), the storage stability of the entire preparation can be ensured while maintaining a moderate viscosity, and the occurrence of unnecessary clogging in the container that hinders spraying can be effectively prevented, and good sprayability can also be ensured. 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, tamarind gum, psyllium seed gum, polyvinyl alcohol, sodium chondroitin sulfate, and methoxyethylene maleic anhydride copolymer.
[0047] The content of the binder in the stock solution (X) is preferably 1% by mass or less, more preferably 0.8% by mass or less, even more preferably 0.6% by mass or less, and even more preferably 0.05% by mass or less, from the viewpoint of ensuring good jetting property while maintaining the storage stability of the entire agent. Alternatively, the stock solution (X) may not contain a binder.
[0048] The concentrate (X) contained in the oral aerosol of the present invention may contain, in addition to the above-mentioned components, a pH adjuster, a preservative, a medicinal ingredient, a colorant, etc., within the range that does not impair the effects of the present invention.
[0049] The viscosity (initial viscosity) of the concentrate (X) at 25°C immediately after production is preferably 500 mPa·s or more, more preferably 700 mPa·s or more, even more preferably 1000 mPa·s or more, still more preferably 1300 mPa·s or more, and even more preferably 1800 mPa·s or more, and is preferably 8000 mPa·s or less, more preferably 6000 mPa·s or less, even more preferably 5000 mPa·s or less, and even more preferably 4000 mPa·s or less, from the viewpoints of enabling the concentrate (X) to maintain an appropriate viscosity after storage without excessive thickening, ensuring excellent storage stability in the entire formulation, and ensuring good jetting properties.
[0050] Furthermore, the viscosity of the concentrate (X) at 25°C after storage (viscosity after storage), from the viewpoints of maintaining an appropriate viscosity and exhibiting good jettability as well as good retention on the brush part of the toothbrush, is preferably 250 mPa·s or more, more preferably 500 mPa·s or more, even more preferably 750 mPa·s or more, still more preferably 1000 mPa·s or more, and even more preferably 1250 mPa·s or more, preferably 20000 mPa·s or less, more preferably 15000 mPa·s or less, even more preferably 12500 mPa·s or less, and even more preferably 10000 mPa·s or less.
[0051] Furthermore, the rate of increase (%) of viscosity of the concentrate (X) at 25°C after storage (viscosity after storage) from the initial viscosity (={(viscosity after storage-initial viscosity) / initial viscosity} x 100) is, from the viewpoint of maintaining an appropriate viscosity and exhibiting good jettability as well as good retention on the brush part of the toothbrush, preferably 400% or less, more preferably 350% or less, even more preferably 300% or less, and even more preferably 250% or less. The initial viscosity and viscosity after storage of the concentrate (X) can be measured using a BM type viscometer (manufactured by Toki Sangyo Co., Ltd.).
[0052] The propellant (Y) contained in the oral aerosol of the present invention contains one or more selected from carbon dioxide, nitrogen, liquefied petroleum gases such as isobutane, normal butane, and mixtures thereof, and liquefied gases such as dimethyl ether, isopentane, etc. Among these, it is preferable that the propellant contains at least carbon dioxide, from the viewpoint of contributing to the expression of good retention on the brush part of the toothbrush while producing a foam-like spray. In addition, one or more types selected from nitrogen; liquefied petroleum gases such as isobutane, normal butane, and mixtures thereof; and liquefied gases such as dimethyl ether and isopentane may be contained together with carbon dioxide and used as a mixed gas with carbon dioxide.
[0053] When the propellant (Y) contains carbon dioxide, the content of such carbon dioxide in the propellant (Y) is, from the viewpoint of ensuring good retention on the brush part of the toothbrush, preferably 51% by mass or more, more preferably 80% by mass or more, even more preferably 90% by mass or more, still more preferably 95% by mass or more, and preferably 100% by mass or less, more preferably 100% by mass. The carbon dioxide content means the content in the propellant (Y) before a part of the carbon dioxide is dissolved in the concentrate (X), although a part of the carbon dioxide may be dissolved in the concentrate (X) during storage, that is, before the concentrate (X) and the propellant (Y) are mixed, or before they are filled into an aerosol container.
[0054] In the oral aerosol preparation of the present invention, from the viewpoint of ensuring excellent storage stability throughout the preparation, the mass ratio of the concentrate (X) to the propellant (Y) ((X):(Y)) is preferably 95:5 to 99:1, and more preferably 97:3 to 98.5:1.5.
[0055] In the oral aerosol of the present invention, when the propellant (Y) contains carbon dioxide, from the viewpoint of ensuring excellent storage stability in the entire formulation, the mass ratio of the content of carbon dioxide in the propellant (Y) to the content of component (b) in the concentrate (X) (carbon dioxide / (b)) is preferably 20.4 or more, more preferably 25.5 or more, even more preferably 34 or more, preferably 500 or less, more preferably 333 or less, and even more preferably 250 or less.
[0056] In the oral aerosol of the present invention, when the propellant (Y) contains carbon dioxide, from the viewpoint of ensuring excellent storage stability throughout the agent, the mass ratio of the content of carbon dioxide in the propellant (Y) to the content of component (c) in the concentrate (X) (carbon dioxide / (c)) is preferably 72.85 or more, more preferably 85 or more, even more preferably 102 or more, and is preferably 100,000 or less, more preferably 20,000 or less, and even more preferably 10,000 or less.
[0057] The oral aerosol of the present invention is prepared by compressing a propellant (Y) and filling it into an aerosol container, and the concentrate (X) which is the content of the container is sprayed from a discharge port of the container, placed on a brush part of a toothbrush, and then the toothbrush is moved and inserted into the oral cavity to apply to a desired area. In producing the oral aerosol of the present invention, the concentrate (X) is prepared, and then filled into an aerosol container together with the propellant (Y), and then pressurized as necessary to seal it. The pressure inside the aerosol container is preferably 0.5 to 0.9 MPa, and more preferably 0.7 to 0.8 MPa at 25° C., from the viewpoint of ensuring excellent storage stability throughout the agent. The amount of the oral aerosol of the present invention to be applied per use is preferably 0.4 to 1.5 g, and more preferably 0.5 to 1.0 g. EXAMPLES
[0058] The present invention will now be described in detail with reference to the following examples. In the tables, the content of each component is expressed as mass % unless otherwise specified.
[0059] [Examples 1 to 19, Comparative Examples 1 to 5] Each concentrate (X) was prepared according to the formulations in Tables 1 to 3, and 90 g of this was filled into an aerosol container (manufactured by Takeuchi Press Co., Ltd.). Each propellant (Y) was then added in the ratio shown in Table 1, and each agent was produced so that the pressure inside the container at 25°C was 0.9 MPa. Using the prepared stock solution (X) or the obtained agent, various measurements and evaluations were carried out according to the following methods. The results are shown in Tables 1 to 3. In addition, for Comparative Example 2, separation (separation of water) was confirmed immediately after preparation of the stock solution (X), and therefore evaluation of the "storage stability of the stock solution (X)" was not possible.
[0060] 《Initial viscosity of undiluted solution (X) (viscosity of undiluted solution (X) at 25℃)》 Immediately after preparation, each stock solution (X) was measured using a BM type viscometer (rotor No. 3, 12 rpm, 1 minute) (manufactured by Toki Sangyo Co., Ltd.).
[0061] Viscosity of stock solution (X) after storage (Viscosity of stock solution (X) at 25°C after storage) Each of the prepared stock solutions (X) was filled into a glass container and stored in a thermostatic bath at 45°C for one month, after which the viscosity was measured using a BM type viscometer (rotor No. 3, 12 rpm or 6 rpm, 1 minute) (manufactured by Toki Sangyo Co., Ltd.).
[0062] Viscosity increase rate of stock solution (X) after storage Based on the initial viscosity of the obtained stock solution (X) and the viscosity of the stock solution (X) after storage, the increase rate (%) was calculated according to the following formula (x). Increase rate (%) (= {(viscosity after storage - initial viscosity) / initial viscosity} × 100) (x)
[0063] Storage stability of the original solution (X) Each of the prepared stock solutions (X) was filled into a glass container and stored in a thermostatic chamber at 45° C. for one month, after which the properties of the agent were visually observed and evaluated according to the following criteria. AA: No separation (water separation) and no precipitate formation A: No separation (water separation), but slight formation of precipitates was confirmed. B: Slight separation (separation) or separation (separation) confirmed after 3 days or more C: Separation (release from water) was confirmed after one day. D: Separation (separation) was confirmed immediately after preparation.
[0064] Storage stability of the agent After storing each of the obtained agents in a thermostatic chamber at 45°C for one month, spraying from the container was repeated until spraying was no longer possible. Next, the amount of the sprayed original solution (X) was calculated from the remaining amount (g) of the original solution (X) in the container, and the spray rate (%) was calculated using the following formula (y). Based on the obtained value, the sprayability of the entire amount was evaluated according to the following criteria. Injection rate (%) = {amount of injected concentrate (X) / amount of concentrate (X) filled in container} ×100(%)···(y) A: Injection rate is 95% or more B: Injection rate is 92.5% or more but less than 95% C: Injection rate is 90% or more but less than 92.5% Z: Injection rate is less than 90%
[0065] <Retention on the brush part> An O-ring with an inner diameter of 21.7 mm was placed on a sieve (No. 5.5, 3350 μm), and then 1 g of each of the obtained agents was sprayed from a container and allowed to stand inside the O-ring. After leaving it to stand, the sprayed foam agent was observed from above the sieve to see whether it passed through the sieve and dripped downward. The time (seconds) from immediately after spraying until the agent dripped below the sieve was measured and used as an index of evaluation. If the retention time is 30 seconds or more, it can be determined that the oral aerosol has good retention on the brush part. A: Retention time is 30 seconds or more B: Retention time is 1 second or more and less than 30 seconds C: Retention time is 0 seconds D: Not rated
[0066] [Table 1]
[0067] [Table 2]
[0068] [Table 3]
Claims
1. An oral aerosol containing a stock solution (X) and a propellant (Y), wherein the stock solution (X) comprises the following components (a), (b), and (c): (a) Monohydric alcohols having 12 to 22 carbon atoms (b) Anionic surfactant having a hydrocarbon group with 12 to 22 carbon atoms (c) Fluorine-containing compound It contains, An oral aerosol agent wherein the mass ratio ((b) / (c)) of the amount of component (b) in the stock solution (X) to the amount of component (c) in terms of fluorine atoms is 0.285 or more and 2500 or less.
2. The oral aerosol agent according to claim 1, wherein the amount of component (c) in the stock solution (X), calculated on a fluorine atom basis, is 0.001% by mass or more and 0.7% by mass or less.
3. The oral aerosol agent according to claim 1 or 2, wherein component (a) is cetanol and stearyl alcohol.
4. The oral aerosol agent according to claim 1 or 2, wherein the mass ratio ((c) / (a)) of the amount of component (c) in terms of fluorine atoms to the amount of component (a) is 0.0001 or more and 0.4 or less.
5. The oral aerosol agent according to claim 1 or 2, wherein the content of component (a) in the undiluted solution (X) is 0.6% by mass or more and 10% by mass or less.
6. The oral aerosol agent according to claim 1 or 2, wherein the stock solution (X) further contains a nonionic surfactant (d).