WO2022138487A1 - Composition à prendre par voie orale - Google Patents

Composition à prendre par voie orale Download PDF

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Publication number
WO2022138487A1
WO2022138487A1 PCT/JP2021/046729 JP2021046729W WO2022138487A1 WO 2022138487 A1 WO2022138487 A1 WO 2022138487A1 JP 2021046729 W JP2021046729 W JP 2021046729W WO 2022138487 A1 WO2022138487 A1 WO 2022138487A1
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Prior art keywords
component
mass
oral composition
extract
examples
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PCT/JP2021/046729
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English (en)
Japanese (ja)
Inventor
苗穂 鈴木
麻衣 小幡
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ライオン株式会社
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Priority to CN202180087130.1A priority Critical patent/CN116710065A/zh
Priority to JP2022571402A priority patent/JPWO2022138487A1/ja
Publication of WO2022138487A1 publication Critical patent/WO2022138487A1/fr

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/25—Silicon; Compounds thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • 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
    • A61K8/46—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing sulfur
    • 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
    • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783—Angiosperms [Magnoliophyta]
    • A61K8/9789—Magnoliopsida [dicotyledons]
    • 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
    • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783—Angiosperms [Magnoliophyta]
    • A61K8/9794—Liliopsida [monocotyledons]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses

Definitions

  • the present invention relates to an oral composition.
  • Patent Document 1 describes a non-aqueous oral care composition containing a specific organic polyol such as glycerol, a particulate abrasive such as silicic acid anhydride, a surfactant, and xanthan gum.
  • Patent Document 2 describes a non-aqueous toothpaste composition containing a carboxyvinyl polymer, an anhydrous wetting agent such as glycerin, and an abrasive such as polyethylene glycol, silica, and calcium carbonate, and may further contain a surfactant.
  • the plant extract may be added to the oral composition for the purpose of imparting various physiological activities (for example, Patent Document 3).
  • An object of the present invention is to provide a non-aqueous oral composition in which an unpleasant taste is suppressed.
  • the present invention provides the following [1] to [8].
  • the component (B) contains at least one selected from shell ginger extract, sardine extract, toki extract, calendula officinalis extract, chamomile extract, and mukuroji extract.
  • an unpleasant taste can be suppressed in a non-aqueous oral composition.
  • the oral composition contains (A) component: a component having an unpleasant taste, preferably a component having a bitter taste.
  • the component (A) is usually a component other than a non-aqueous organic solvent, and is preferably an inorganic powder or a surfactant having an unpleasant taste.
  • -Inorganic powder- Inorganic powder is a component generally contained in oral compositions such as toothpaste and dentifrice as a tooth cleaning agent and a thickener.
  • the inorganic powder having an unpleasant taste include silica-based materials and calcium-based materials.
  • the silica-based material include silica (precipitating silica, titanium-binding silica, silica gel, aluminosilicate, and zirconosilicate).
  • Examples of calcium-based materials include calcium carbonate (light and heavy); calcium dibasic phosphate, dihydrate salt or anhydrate, calcium primary phosphate, calcium tertiary phosphate, calcium pyrophosphate, insoluble calcium metaphosphate, calcium tertiary phosphate, fourth.
  • Calcium phosphate-based materials such as calcium phosphate and eighth calcium phosphate; calcium hydroxide; powders of inorganic substances such as calcium sulfate can be mentioned.
  • silica is preferred. It is preferable to use silica having an RDA (Radioactive Dentin Abrasion) in the range of 50 to 250. RDA can be measured according to Hefferren's method (Hefferren (1976) Journal of Dental Research, July-August, 563-573).
  • the size of the inorganic powder can be appropriately selected depending on the type of the inorganic material constituting each powder, but usually, the average particle size (volume-based D50, measured value by laser diffraction / scattering method) is 0.1 to 40 ⁇ m, preferably 0.1 to 40 ⁇ m.
  • a particle size distribution measuring device for example, Microtrack particle size distribution measuring device (Made 117995-10, Type SRA) manufactured by Nikkiso Co., Ltd.) and adjust the turbidity (dV value) of the sample to 0.5. It can be measured, and the average particle size shown in the subsequent examples is the measured value by this method.
  • a particle size distribution measuring device for example, Microtrack particle size distribution measuring device (Made 117995-10, Type SRA) manufactured by Nikkiso Co., Ltd.
  • dV value turbidity
  • the content is preferably 8% by mass or more, more preferably 10% by mass or more.
  • the upper limit is preferably 40% by mass or less, more preferably 30% by mass or less. Thereby, the viscosity of the composition does not become too high and good physical properties can be obtained. Therefore, the content of the inorganic powder is preferably 8 to 40% by mass, more preferably 10 to 30% by mass.
  • surfactant having an unpleasant taste examples include amphoteric surfactants and anionic surfactants.
  • amphoteric surfactant examples include alkyldimethylaminoacetic acid betaine (eg, lauryldimethylaminoacetic acid betaine) and fatty acid amide propyl betaine (eg, cocamidopropyl betaine, fatty acid amide propyldimethylaminoacetic acid betaine, lauric acid amide propyl betaine). Etc.
  • alkyldimethylaminoacetic acid betaine eg, lauryldimethylaminoacetic acid betaine
  • fatty acid amide propyl betaine eg, cocamidopropyl betaine, fatty acid amide propyldimethylaminoacetic acid betaine, lauric acid amide propyl betaine
  • Betaine-type amphoteric surfactant N-fatty acid acyl-N-carboxymethyl-N-hydroxyethylethylenediamine salt (eg, N-palm oil fatty acid acyl-N-carboxymethyl-N-hydroxyethylimidazolinium betaine); Examples thereof include imidazoline-type amphoteric surfactants such as coconut oil fatty acid imidazolinium betaine and 2-alkyl-N-carboxymethyl-N-hydroxyethyl imidazolinium betaine.
  • the number of carbon atoms of the alkyl group and the acyl group is preferably 8 to 18.
  • betaine-type amphoteric tenside agents are preferable, fatty acid amide propyl betaine is more preferable, and cocamidopropyl betaine and lauric acid amide propyl betaine are more preferable.
  • anionic surfactant examples include alkyl sulfates, acyl amino acid salts, acyl taurine salts, ⁇ -olefin sulfonates, hydrogenated coconut fatty acid monoglyceride monosulfates, and lauryl sulfoacetates.
  • the alkyl group and the acyl group may be either a straight chain or a branched chain, and may be saturated or unsaturated, and the number of carbon atoms thereof is usually 10 to 20, preferably 12 to 18, and more preferably 12 to 14.
  • the salt can be selected from pharmacologically acceptable salts.
  • Examples of the pharmacologically acceptable salt include inorganic base salts such as sodium salt, potassium salt, calcium salt, magnesium salt and ammonium salt; triethylammonium salt, triethanolammonium salt, pyridinium salt, diisopropylammonium salt and the like.
  • Organic base salts examples include amino acid salts such as arginine salt, lysine salt and histidine salt. Of these, inorganic base salts are preferred, alkali metal salts (eg, sodium salts, potassium salts) or ammonium salts are more preferred, and sodium salts are even more preferred.
  • alkyl sulfate examples include lauryl sulfate and myristoyl sulfate.
  • acyl amino acid salt include acyl sarcosine salts such as lauroyl sarcosin salt and myristyl sarcosin salt; lauroyl glutamate; acyl glutamate such as myristoyl glutamate, palmitoyl glutamate and palmitoyl glutamate; N-lauroyl-N-methylglycine.
  • Acylglycine salts such as salts and cocoylglycine salts; N-lauroyl- ⁇ -alanine salt, N-myristyl- ⁇ -alanine salt, N-cocoyl- ⁇ -alanine salt, N-lauroyl-N-methyl- ⁇ -alanine salt. , N-myristoyl-N-methyl- ⁇ -alanine salt, acylalanine salt such as N-methyl-N-acylalanine salt; acylasparaginate such as lauroyl aspartate.
  • the acyl taurine salt include lauroylmethyl taurine salt, N-methyl-N-acyl taurine salt, and N-cocoyl methyl taurine salt.
  • ⁇ -olefin sulfonate examples include ⁇ -olefin sulfonates having 12 to 18 carbon atoms such as tetradecene sulfonate.
  • anionic surfactants include hydrogenated coconut fatty acid monoglyceride sodium monosulfate, sodium lauryl sulfoacetate.
  • anionic surfactant ⁇ -olefin sulfonic acid is preferable, and tetradecene sulfonic acid salt is more preferable.
  • the content of each of the anionic surfactant and the amphoteric surfactant is preferably 0.1% by mass or more, preferably 0.3% by mass or more, based on the composition. More preferred. Thereby, sufficient foaming performance can be obtained.
  • the upper limit is preferably 3% by mass or less, more preferably 2.5% by mass or less. Thereby, the bitterness can be sufficiently suppressed in the composition. Therefore, the content of the surfactant is preferably 0.1 to 3% by mass, more preferably 0.3 to 2.5% by mass.
  • the content of each component is an amount based on the amount of each component charged at the time of producing an oral composition.
  • the component (A) may be one component having an unpleasant taste alone or a combination of two or more components.
  • the component (A) preferably contains an inorganic powder and a surfactant, and more preferably contains an inorganic powder, an amphoteric surfactant, and an anionic surfactant.
  • the oral composition contains (B) component: a plant extract.
  • component (B) a plant extract.
  • the plant extract may be an extract obtained by extracting from at least a part of the raw material plant.
  • plant raw materials include shell ginger, peony, Toki, calendula officinalis, chamomile, and Sapindaceae.
  • the extraction site include leaves, stems, roots, flowers, pericarp, and combinations thereof, which may be appropriately selected depending on the plant species and / or the extraction method.
  • the extraction solvent examples include water, a polar solvent, a non-polar solvent, and a mixed solvent thereof.
  • the polar solvent include ethyl ether, ethylene chloride, dioxane, acetone, alcohol (for example, lower monohydric alcohol having 1 to 5 carbon atoms such as ethanol, methanol, propyl alcohol and isopropyl alcohol) and glycol (for example, propylene glycol). , Butylene glycol), ethyl acetate, glycerin and the like.
  • non-polar solvent examples include n-hexane, petroleum ether, ligroine, cyclohexane, carbon tetrachloride, chloroform, dichloromethane, 1,2-dichloroethane, toluene and benzene.
  • a hydrophilic solvent is preferable, water, a lower monohydric alcohol having 1 to 5 carbon atoms, glycol, and a mixed solvent of 2 or more selected from these are preferable, and water, ethanol, propylene glycol, butylene glycol, and Two or more mixed solvents selected from these are more preferable, and water is even more preferable.
  • the mixed solvent is preferably a mixed solvent of water and a lower monohydric alcohol or glycol, and more preferably a mixed solvent having a mixing ratio of water and a lower monohydric alcohol or glycol of 10:90 to 90:10 (mass ratio).
  • a sample is taken from the extraction site of a plant, the sample is crushed as necessary, and then the extraction process is performed using an extraction solvent.
  • the extraction residue obtained after the extraction is used as a raw material and the solvent is used.
  • a method of extraction processing can be mentioned.
  • post-treatment such as concentration, dilution, pulverization (for example, pulverization by a shaping treatment using dextrin), pulverization and the like may be performed, if necessary.
  • the dosage form of the extract include liquid, powder, and solid, but the dosage form is not particularly limited.
  • a plant extract obtained from the above plants can be used, and a single component contained in each plant or a combination thereof may be purified, or a commercially available product may be used.
  • Preferred examples are as follows.
  • Shell ginger extract For example, from the leaves of shell ginger (Alpinia speciosa), water, a lower monohydric alcohol having 1 to 5 carbon atoms (for example, ethanol), glycol (for example, 1,3-butylene glycol), or from these. Extracts extracted using two or more mixed solvents of choice; shell ginger extract is usually flavonoids, sugars, 7,8-dihydro-5,6-dehydrocawine ( ⁇ -pylons), cineole, pinen, And contains borneol, methyl silicate.
  • a lower monohydric alcohol having 1 to 5 carbon atoms for example, ethanol
  • glycol for example, 1,3-butylene glycol
  • Extracts extracted using two or more mixed solvents of choice shell ginger extract is usually flavonoids, sugars, 7,8-dihydro-5,6-dehydrocawine ( ⁇ -pylons), cineole, pinen, And contains borneol, methyl silicate.
  • Peony extract For example, from the roots of peony (Paeonia lactiflora), water, lower monohydric alcohols having 1 to 5 carbon atoms (eg, ethanol), glycols (eg, 1,3-butylene glycol), or selected from these. Extracts extracted using two or more mixed solvents; Peony extract usually contains monoterpene glycosyl (such as Peoniflorin) and tannins.
  • Toki extract From the roots of Angelica acutiloba, for example, water, lower monohydric alcohols with 1 to 5 carbon atoms (eg, ethanol), glycols (eg, 1,3-butylene glycol), or from these. Extracts extracted using two or more mixed solvents of choice; Angelica acutiloba extracts usually include essential oils, fatty acids, coumarin derivatives, phthalids, polyacetylene compounds.
  • Calendula officinalis extract From, for example, Calendula officinalis flowers, water, lower monohydric alcohols with 1-5 carbon atoms (eg, ethanol), glycols (eg, 1,3-butylene glycol), or from these. Extracts extracted using two or more mixed solvents of choice; calendula officinalis extract usually contains tannin, triterpenoid saponin (calendroside A).
  • Chamomile extract For example, from chamomile (chamomile, chamomile recutita (matricaria)) flowers, water, lower monovalent alcohols with 1 to 5 carbon atoms (eg, ethanol), glycols (eg, 1,3-butylene glycol), Or an extract extracted using two or more mixed solvents selected from these; chamomile extract usually contains tannin, flavonoid, coumarin derivative (hernialin, umbelliferon), essential oil component (azulene).
  • chamomile extract usually contains tannin, flavonoid, coumarin derivative (hernialin, umbelliferon), essential oil component (azulene).
  • Sapindaceae extract selected from, for example, water, lower monohydric alcohols with 1-5 carbon atoms (eg, ethanol), glycols (eg, 1,3-butylene glycol) from the skin of Sapindus sapindaceae. Extract extracted using two or more mixed solvents; Sapindaceae extract usually contains a saponin glycoside.
  • the component (B) may be used alone or in combination of two or more kinds of plant extracts.
  • the content (extract pure content) of the component (B) is usually 0.00001% by mass or more, preferably 0.00003% by mass or more, and more preferably 0.00005% by mass or more with respect to the total amount of the composition. .. Thereby, the bitterness improving effect can be fully exhibited.
  • the upper limit is usually 0.3% by mass or less, preferably 0.1% by mass or less, and more preferably 0.05% by mass or less.
  • the content of the component (B) is usually 0.00001 to 0.1% by mass or 0.00001 to 0.3% by mass, preferably 0.00003 to 0.1% by mass, and more preferably 0.00005. It is about 0.05% by mass.
  • the oral composition preferably contains (C): a polyhydric alcohol having a melting point of 25 ° C. or lower as a liquid medium.
  • the heat of hydration of the solvent can give a warm feeling to the oral composition.
  • Polyhydric alcohols having a melting point of 25 ° C. or lower include, for example, glycerin (melting point: 17.8 ° C.), polyethylene glycol (for example, polyethylene glycol having an average molecular weight of 190 to 650), propylene glycol (melting point: -59 ° C.), and dipropylene glycol. (Melting point: ⁇ 39 ° C.), butylene glycol (melting point: ⁇ 77 ° C.), polypropylene glycol and the like can be mentioned.
  • glycerin, polyethylene glycol and butylene glycol are preferable, and a combination containing at least glycerin and polyethylene glycol is more preferable from the viewpoint of improving the feeling of warmth in the oral cavity.
  • glycerin, polyethylene glycol and butylene glycol are preferable, and a combination containing at least glycerin and polyethylene glycol is more preferable from the viewpoint of improving the feeling of warmth in the oral cavity.
  • the average molecular weight of polyethylene glycol is usually 650 or less, preferably 630 or less, and more preferably 600 or less.
  • the lower limit is usually 150 or more, preferably 250 or more. Therefore, it is usually 150 to 650, preferably 150 to 630, and more preferably 250 to 600.
  • Examples of polyethylene glycol include polyethylene glycol 200 (average molecular weight 190 to 210, melting point: -50 ° C), polyethylene glycol 400 (average molecular weight 380 to 420, melting point: 5 ° C), and polyethylene glycol 600 (average molecular weight 570 to 630, melting point). : 22 ° C.) can be used.
  • the average molecular weight of polyethylene glycol is the average molecular weight described in the Quasi-drug Raw Material Standard 2006.
  • the content of the component (C) is usually 20% by mass or more, preferably 40% by mass or more, based on the total amount of the composition.
  • the upper limit is usually 85% by mass or less, preferably 80% by mass or less.
  • the content of the component (C) is usually 20 to 85% by mass, preferably 40 to 80% by mass.
  • the content thereof is usually 20% by mass or more, preferably 40% by mass or more, and more preferably 50% by mass or more with respect to the total amount of the component (C).
  • the upper limit is usually 90% by mass or less, preferably 80% by mass or less, but is not particularly limited. Therefore, the content of glycerin is usually 20 to 100% by mass, preferably 40 to 90% by mass, and more preferably 50 to 80% by mass.
  • the component (C) contains polyethylene glycol (for example, polyethylene glycol having an average molecular weight of 190 to 630), the content thereof is usually 10% by mass or more, preferably 15% by mass or more, based on the total amount of the component (C). Is. As a result, a good feeling of warmth can be exhibited. The upper limit is usually 30% by mass or less. This can result in a good flavor without bitterness. Therefore, the content of polyethylene glycol is usually 10% by mass or more, preferably 15 to 30% by mass.
  • the oral composition is a non-aqueous composition that is substantially free of water.
  • heat of hydration can be generated by contacting water with each component of the composition (mainly the component (C)) in the oral cavity during use, and a feeling of warmth can be exhibited in the oral cavity.
  • the water content is usually 2% by mass or less, preferably 1% by mass or less, and more preferably 0.5% by mass or less.
  • the water content is the ratio (%) of the total water content contained in the raw material before compounding (for example, the component (B)) to the total raw material, or the difference between the weight after drying of the oral composition and the weight before drying. Can be calculated as a ratio (%) to the weight before drying.
  • the water content in the latter example is a value calculated by the former method.
  • the oral composition may contain components other than the components (A) to (C) as long as the effects of the present invention are not impaired.
  • Other ingredients include, for example, surfactants, sweeteners, fragrances, abrasives, wetting agents, binders, organic abrasives, pH regulators, preservatives, medicinal ingredients, oily ingredients, colorants (pigments) and the like. Ingredients that can be incorporated into the oral composition of, but are not limited to these.
  • surfactant other than the component (A) examples include a nonionic surfactant and a cationic surfactant.
  • Examples of the cationic surfactant include an alkylammonium salt and an alkylbenzylammonium salt.
  • nonionic surfactant examples include polyoxyethylene alkyl ether, polyoxyethylene hydrogenated castor oil, sorbitan fatty acid ester, polyoxyethylene sorbitan fatty acid ester (eg, polyoxyethylene sorbitan monostearate), alkyrrole amide, and polyoxy.
  • the number of carbon atoms in the alkyl chain of the polyoxyethylene alkyl ether is usually 14 to 18, and the average number of moles of ethylene oxide added is usually 15 to 30 mol.
  • the average number of moles of ethylene oxide added to the polyoxyethylene hydrogenated castor oil is usually 20 to 100 mol, preferably 20 to 60 mol.
  • the number of carbon atoms of the fatty acid of the sorbitan fatty acid ester is usually 12 to 18.
  • the number of carbon atoms of the fatty acid of the polyoxyethylene sorbitan fatty acid ester is usually 16 to 18, and the average number of moles of ethylene oxide added is usually 10 to 40 mol.
  • the number of carbon atoms in the alkyl chain of the alkylolamide is usually 12 to 14.
  • the nonionic surfactant polyoxyethylene hydrogenated castor oil, polyoxyethylene sorbitan fatty acid ester, and polyoxyethylene alkyl ether are preferable.
  • anionic and cationic surfactants When anionic and cationic surfactants are contained, the respective contents are usually 0.01 to 10% by mass, preferably 0.1 to 5% by mass, and more preferably 0.2 to 3% by mass based on the total composition. Is.
  • the feeling of use can be further improved.
  • the sweetener include xylitol, erythritol, maltitol, saccharin, saccharin sodium, aspartame, stebioside, stevia extract, paramethoxycinnamic aldehyde, neohesperidin dihydrochalcone, perillartine, glycyrrhizin, thaumatin, aspartame phenylalanine methyl ester and the like. Be done.
  • the sweetener may be used alone or in combination of two or more.
  • fragrances include peppermint oil, sparemint oil, eucalyptol oil, winter green oil, clove oil, thyme oil, sage oil, cardamon oil, rosemary oil, majorum oil, lemon oil, orange oil, nutmeg oil, lavender oil, etc.
  • Natural essential oils such as parlacles oil, laurel oil, piment oil, laurel oil, perilla oil; menthol, carboxylic, synamic aldehyde, anetol, 1,8-cineole, methylsalicylate, eugenol, timole, linalol, limonene, menthol, menthyl acetate.
  • Citraal camphor, borneol, pinen, spirantol, n-decyl alcohol, citronellol, ⁇ -terpineol, citronellyl acetate, cineole, ethyllinalol, varnish and other fragrance components contained in the above natural essential oils; ethyl acetate, ethyl butyrate.
  • fragrance Isoamylacetate, hexanal, hexenal, methylanthranilate, ethylmethylphenylglycidate, benzaldehyde, vanillin, ethyl vanillin, franeol, N-ethyl-p-menthan-3-carboxamide, mentyllactate, ethyleneglycol-l-mentylcarbonate And the like; as well as various blended flavors such as mint-based, fruit-based, herbal-based, etc., which are a combination of some fragrance components and / or some natural essential oils.
  • the fragrance may be used alone or in combination of two or more.
  • medicinal ingredients include bactericidal or antibacterial agents such as cetylpyridinium chloride, benzalkonium chloride, benzethonium chloride, isopropylmethylphenol, zinc gluconate, zinc citrate, triclosan, timole, hinokithiol, and lysoteam chloride; Enzymes such as mutanase, amylase, protease, lytecenzyme; fluorides such as sodium fluoride, sodium monofluorophosphate, tin fluoride; ⁇ -aminocaproic acid, allantin, tranexamic acid, glycyrrhizinate (eg, glycyrrhetin dipotassium salt) ), Anti-inflammatory agents such as glycyrrhetinic acid, stearyl glycyrrhetinate, allantinchlorhydroxyaluminum, azulene, dihydrocholesterol
  • Prophylactic agents blood flow promoters such as vitamin E (eg, tocopherol acetate); hypersensitivity inhibitors such as potassium nitrate, aluminum lactate, strontium chloride; coating agents such as hydroxyethyl cellulose dimethyldiallyl ammonium chloride; vitamin C (eg, ascorbic acid) Or its salt), astringents such as lysozyme chloride and sodium chloride; water-soluble copper compounds such as copper chlorophyll and copper gluconate; tooth stone preventive agents such as zeolite, amino acids such as alanine, glycine and proline; caropeptide and polyvinylpyrrolidone.
  • the medicinal ingredient may be used alone or in combination of two or more. As for the content of the other active ingredients, the effective amount can be appropriately set.
  • oily component examples include hydrocarbons such as squalane, liquid paraffin, vaseline, and microcrystalin wax; and having 8 carbon atoms such as higher alcohols (eg, lauryl alcohol, cetyl alcohol, cetostearyl alcohol, oleyl alcohol, and isostearyl alcohol). ⁇ 22 alcohols); higher fatty acids (eg, fatty acids with 8 to 22 carbon atoms such as lauric acid, myristic acid, oleic acid, isostearic acid), vegetable oils such as olive oil, castor oil, coconut oil; Examples include fatty acid esters.
  • abrasive other than component (A)
  • examples of the abrasive include an inorganic abrasive other than the component (A) and an organic abrasive.
  • examples of the inorganic abrasive include aluminum-based materials such as aluminum oxide, aluminum hydroxide, and alumina; silicic acid-based materials such as anhydrous silicic acid, zeolite, and zirconium silicate; magnesium-based materials such as magnesium carbonate and tertiary magnesium phosphate.
  • Apatite-based materials such as hydroxyapatite, fluoroapatite, and calcium-deficient apatite
  • titanium-based materials such as titanium dioxide, mica titanium, and titanium oxide
  • crystalline zirconium silicates such as bentonite.
  • the organic abrasive include polymethylmethacrylate and synthetic resin-based abrasives.
  • the content of the abrasive is preferably 0 to 10% by mass. Further, the total amount of the component (A) and the component (A) is preferably 50% by mass or less, more preferably 8 to 50% by mass, based on the whole composition.
  • the antiseptic power of the pharmaceutical product can be ensured.
  • the preservative include paraoxybenzoic acid esters (for example, methyl paraoxybenzoate, ethyl paraoxybenzoate, butyl paraoxybenzoate), sodium benzoate and the like.
  • the preservative may be used alone or in combination of two or more.
  • the feeling of use can be further improved.
  • polyhydric alcohols other than the component (C) are preferable, and examples thereof include sugar alcohols such as sorbitol, erythritol, maltitol, lactitol, and xylitol; glycols such as propylene glycol and ethylene glycol; and reduced starch saccharified products. ..
  • the content of the wetting agent is usually 0 to 20% by mass, preferably 1 to 10% by mass.
  • -Blotting agent- Optional binders include known organic binders such as cellulosic binders (eg, carboxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, methyl cellulose, cationized cellulose, etc.), carrageenan, xanthan gum. , Carboxyvinyl polymer, guagam, tragant gum, carrageenan, arabia gum, locust bean gum, sodium alginate, montmorillonite, sodium polyacrylate, polyvinylpyrrolidone, polyvinyl alcohol, propylene glycol alginate and the like.
  • the content of any binder is preferably 0 to 1.0% by mass, more preferably 0.1 to 0.8% by mass.
  • the pH stability of the pharmaceutical product can be ensured.
  • the pH adjuster include organic acids such as phthalic acid, citric acid, succinic acid, acetic acid, fumaric acid, malic acid and lactic acid or salts thereof, and inorganic acids such as phosphoric acid (orthoric acid) or salts thereof.
  • organic acids such as phthalic acid, citric acid, succinic acid, acetic acid, fumaric acid, malic acid and lactic acid or salts thereof
  • inorganic acids such as phosphoric acid (orthoric acid) or salts thereof.
  • potassium salt, sodium salt and ammonium salt hydroxides such as sodium hydroxide and potassium hydroxide can be mentioned.
  • the inorganic acid salt include disodium hydrogen phosphate and sodium dihydrogen phosphate.
  • the content of the pH adjuster is usually such that the pH of the composition after addition is 5 to 9, preferably 6 to 8.5.
  • the pH value is usually a value at 25 ° C. and 3 minutes after the
  • optional ingredients examples include waxes such as carnauba wax, rosin, rice wax, microcrystalline wax, honey wax, and paraffin wax; higher alcohols such as cetanol and stearyl alcohol; polyisobutylene, polybutadiene, urethane, and silicon. , Natural rubber can be mentioned. The content of these components can be appropriately set as long as the effect of the present invention is not impaired.
  • the oral composition of the present invention can be in any suitable dosage form by any suitable method according to a conventional method.
  • Dosage forms include, for example, liquids (solutions, emulsions, suspensions, syrups, etc.), semi-solids (gels, creams, pastes, etc.), solids (tablets, particulate agents, capsules, film agents, kneaded products, melts, etc.). Solids, waxy solids, elastic solids, soft capsules, etc.).
  • the dosage form of the oral composition is preferably liquid or semi-solid.
  • the oral composition of the present invention can be widely used in oral applications.
  • Applications in solid dosage forms include, for example, troches, gummies, gums, powders or tablets of dentifrices.
  • Examples of applications in the semi-solid dosage form include dentifrices and gel-like dentifrices.
  • Examples of applications in the form of liquids include mouthwashes, liquid dentifrices, and mouthwashes (sprays and the like).
  • the oral composition of the present invention is preferably a dentifrice (dentifrice, gel-like dentifrice). It was
  • the method for producing the oral composition is not particularly limited, and can be prepared by each usual method depending on the dosage form.
  • a method of preparing a component that dissolves in a solvent, mixing other insoluble components, and defoaming (for example, reducing the pressure) as necessary can be mentioned.
  • the obtained toothpaste can be contained in a container and made into a product.
  • the shape and material of the container are not particularly limited, and a container used for a normal dentifrice composition can be used, and examples thereof include plastic containers such as polyethylene, polypropylene, polyethylene terephthalate, and nylon.
  • Examples 1-14 and Comparative Example 1 (dentifrice) Using the above-mentioned components, a dentifrice composition having a compounding composition (part by mass) shown in Tables 2 to 3 was prepared according to the following preparation method.
  • the obtained dentifrice composition was evaluated by the following procedure. The evaluation results are shown in Tables 2 and 3.
  • ⁇ Evaluation method Evaluation of unpleasant taste (bitterness) in the mouth while brushing teeth
  • a toothbrush Cosmetic Advantage toothbrush, 4-row compact, usually manufactured by Lion
  • the average score of 10 taste-sensitive testers was calculated and shown in the table as +++, ++, +,-according to the following evaluation criteria.
  • Taste-sensitive testers were selected from those who had "discontinued or changed brand due to the taste of dentifrice in the past" in the questionnaire.
  • the actual feeling was evaluated on a five-point scale according to the scoring criteria shown below.
  • the average score of 10 taste-sensitive testers was calculated and shown in the table as +++, ++, +,-according to the following evaluation criteria.
  • the "feeling of warmth” means the feeling that the oral mucosa becomes warm.
  • Taste-sensitive testers were selected from those who had "discontinued or changed brand due to the taste of dentifrice in the past" in the questionnaire.

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  • Health & Medical Sciences (AREA)
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  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Botany (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Inorganic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Oral & Maxillofacial Surgery (AREA)
  • Cosmetics (AREA)

Abstract

La présente invention aborde le problème de l'administration d'une composition non aqueuse à prendre par voie orale dans laquelle les goûts déplaisants sont supprimés. La présente invention concerne une composition à prendre par voie orale qui a une teneur en eau de 2 % en masse au plus et qui contient (A) un composant ayant un goût déplaisant et (B) un extrait végétal. Le composant (B) contient de préférence au moins une substance choisie parmi des extraits d'écorce de gingembre, des extraits de pivoine, des extraits de racine d'angélique, des extraits de Calendula officinalis, des extraits de camomille et des extraits de Sapindus mukorossi. Le composant (A) contient de préférence au moins une substance choisie parmi les poudres inorganiques et les tensioactifs. En outre, la composition à prendre par voie orale contient de préférence (C) un polyalcool ayant un point de fusion de 25 °C au plus.
PCT/JP2021/046729 2020-12-23 2021-12-17 Composition à prendre par voie orale WO2022138487A1 (fr)

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Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006347898A (ja) * 2005-06-13 2006-12-28 Ogawa & Co Ltd 血流促進剤並びに該血流促進剤を含有する外用剤、化粧料、浴用剤及び洗剤
JP2011522871A (ja) * 2008-06-17 2011-08-04 ザ プロクター アンド ギャンブル カンパニー 全般的な歯の健康及び外観を改善するための組成物及び方法
JP2018150362A (ja) * 2018-05-31 2018-09-27 小林製薬株式会社 収斂用組成物
JP2019064941A (ja) * 2017-09-29 2019-04-25 丸善製薬株式会社 正常ヒト歯肉線維芽細胞におけるｉ型コラーゲン産生促進剤及び口腔用剤
JP2019196329A (ja) * 2018-05-10 2019-11-14 一丸ファルコス株式会社 歯周病予防口腔用組成物
WO2019216568A1 (fr) * 2018-05-09 2019-11-14 주식회사 하이센스바이오 Composition de dentifrice pour soulager l'hypersensibilité de la dentine
JP2020100589A (ja) * 2018-12-21 2020-07-02 ライオン株式会社 口腔用組成物

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006347898A (ja) * 2005-06-13 2006-12-28 Ogawa & Co Ltd 血流促進剤並びに該血流促進剤を含有する外用剤、化粧料、浴用剤及び洗剤
JP2011522871A (ja) * 2008-06-17 2011-08-04 ザ プロクター アンド ギャンブル カンパニー 全般的な歯の健康及び外観を改善するための組成物及び方法
JP2019064941A (ja) * 2017-09-29 2019-04-25 丸善製薬株式会社 正常ヒト歯肉線維芽細胞におけるｉ型コラーゲン産生促進剤及び口腔用剤
WO2019216568A1 (fr) * 2018-05-09 2019-11-14 주식회사 하이센스바이오 Composition de dentifrice pour soulager l'hypersensibilité de la dentine
JP2019196329A (ja) * 2018-05-10 2019-11-14 一丸ファルコス株式会社 歯周病予防口腔用組成物
JP2018150362A (ja) * 2018-05-31 2018-09-27 小林製薬株式会社 収斂用組成物
JP2020100589A (ja) * 2018-12-21 2020-07-02 ライオン株式会社 口腔用組成物

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JPWO2022138487A1 (fr) 2022-06-30

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