CN116634986A - Oral composition - Google Patents

Oral composition Download PDF

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Publication number
CN116634986A
CN116634986A CN202180087622.0A CN202180087622A CN116634986A CN 116634986 A CN116634986 A CN 116634986A CN 202180087622 A CN202180087622 A CN 202180087622A CN 116634986 A CN116634986 A CN 116634986A
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CN
China
Prior art keywords
acid
oral composition
mass
component
salts
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CN202180087622.0A
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Chinese (zh)
Inventor
石井骏太
平泉将登
小久保龙
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Lion Corp
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Lion Corp
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Publication of CN116634986A publication Critical patent/CN116634986A/en
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/02Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12Carboxylic acids; Salts or anhydrides thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/24Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/24Phosphorous; Compounds thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/25Silicon; Compounds thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/26Aluminium; Compounds thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/36Carboxylic acids; Salts or anhydrides thereof
    • A61K8/362Polycarboxylic acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/36Carboxylic acids; Salts or anhydrides thereof
    • A61K8/365Hydroxycarboxylic acids; Ketocarboxylic acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/40Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/42Amides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/55Phosphorus compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/72Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/81Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions involving only carbon-to-carbon unsaturated bonds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/06Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/08Solutions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
    • A61K9/12Aerosols; Foams
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/70Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q11/00Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses

Abstract

The present invention has been made in view of the above-described problems of the prior art, and an object of the present invention is to provide an oral composition which can suppress irritation in the oral cavity and can exhibit both a bad breath preventing sensation and a smooth sensation. Disclosed is an oral composition comprising (A) a condensed phosphate, an organic acid, a salt thereof, a chelating agent such as a polyacrylate, and (B) N- (2-hydroxy-2-phenylethyl) -2-isopropyl-5, 5-dimethylcyclohexane-1-carboxamide, such as a dentifrice, a mouthwash, a spray, a coating agent, an adhesive agent, or an oral cavity dissolving agent.

Description

Oral composition
Technical Field
The present invention relates to an oral composition.
Background
The clean feel of a dentifrice, i.e., a smooth, slippery feel (smoothness) of the tooth surface, is a feel that is reminiscent of a shiny, white tooth and that greatly aids in the prevention of malodour and satisfaction of brushing action. The smooth feeling of the teeth is obtained in a state where the tooth surface is cleaned, and examples thereof include a method of chemical removal by a chelating agent. Moreover, the effect sensation is generally recognized as the smoothness of the tooth surface, i.e., smooth touch (feeling of smoothness) when the user of the toothpaste licks the tooth surface with the tongue after cleaning the teeth.
On the other hand, as a method for imparting a bad breath preventive effect to an oral composition, there is mentioned compounding of a cold feeling agent.
For example, patent document 1 describes that a dentifrice composition containing N- (4-cyanomethylphenyl) -2-isopropyl-5-methylcyclohexane carboxamide and sodium polyacrylate and/or sodium alginate can provide a sustained and high intraoral clean feeling and a good use feeling. Patent document 2 describes that a dentifrice composition containing a chelating agent and N- (4-cyanomethylphenyl) -2-isopropyl-5-methylcyclohexane carboxamide provides high intraoral cleaning sensation and excellent bad breath prevention sensation. Patent document 3 describes that an oral care composition containing a polyphosphorylated compound and a cold feeling agent such as menthol has whitening and anti-seepage effects.
[ Prior Art literature ]
[ patent literature ]
Patent document 1: international publication No. 2018/221620
Patent document 2: international publication No. 2018/221617
Patent document 3: japanese patent application laid-open No. 2009-531425
Disclosure of Invention
[ problem to be solved by the invention ]
However, in the conventional combination of the chelating agent and the cooling agent in the compositions described in patent documents 1 to 3, there are cases where "smooth feeling on the tooth surface" is not sufficiently and practically felt, regardless of whether or not the tooth stain can be cleanly removed, due to the stimulation of the tongue by the cooling agent. In particular, if the cryoprotectant is added to improve the persistence of the halitosis preventing sensory requirements, the influence on the sensation of the tongue becomes large, and it is difficult to further feel the smooth sensation of the teeth.
The present invention has been made in view of the above-described problems of the prior art, and an object of the present invention is to provide an oral composition which can suppress irritation in the oral cavity and can exhibit both of a bad breath preventing sensation and a smooth sensation.
[ means for solving the problems ]
That is, the present invention provides the following [ 1] to [ 8 ].
[ 1] an oral composition comprising:
(A) Chelating agents
(B) N- (2-hydroxy-2-phenylethyl) -2-isopropyl-5, 5-dimethylcyclohexane-1-carboxamide.
The composition for oral cavity according to [ 2], wherein the component (A) comprises 1 or more selected from the group consisting of condensed phosphoric acid, organic acid, salts thereof, and polyacrylate.
The composition for oral cavity according to [ 1], wherein the component (A) comprises at least any one of the following:
condensed phosphoric acid and salts thereof, wherein the condensed phosphoric acid is 1 or more selected from the group consisting of pyrophosphoric acid, polyphosphoric acid, hexametaphosphoric acid and salts thereof;
an organic acid and a salt thereof, wherein the organic acid is 1 or more selected from the group consisting of malic acid, tartaric acid, citric acid, succinic acid, lactic acid, phytic acid, and salts thereof; and
polyacrylate, which is sodium polyacrylate.
The composition for oral cavity according to any one of [ 1] to [ 3], wherein the content of the component (A) is 0.1 to 3% by mass.
The composition for oral cavity according to any one of [ 1] to [ 4], wherein the content of the component (B) is 0.00001% by mass to 0.1% by mass.
The composition for oral cavity according to any one of [ 1] to [ 5], wherein the composition for oral cavity further comprises (C) an abrasive.
The composition for oral cavity according to [ 7 ], wherein the content of the component (C) is 2 to 30% by mass.
The oral composition according to [ 6 ] or [ 7 ], wherein the component (C) is 1 or more selected from the group consisting of anhydrous silicic acid (Japanese text: water compound) and alumina.
The composition for oral cavity according to any one of [ 1] to [ 8 ], wherein the composition for oral cavity further comprises (D) a lactone having 6 to 12 carbon atoms.
The composition for oral cavity according to [ 9 ], wherein the content of the component (D) is 0.000001 to 0.2% by mass.
The composition for oral cavity according to any one of [ 1] to [ 10 ], wherein the composition for oral cavity is a dentifrice, a mouthwash, a spray, a coating agent, an adhesive agent or an intraoral dissolution agent.
[ Effect of the invention ]
According to the present invention, there is provided an oral composition capable of suppressing irritation in the oral cavity and exhibiting both of a bad breath preventive feeling and a smooth feeling.
Detailed Description
The present invention will be described in detail below.
The oral composition of the present invention contains the following components (a) and (B), and preferably further contains component (C).
[ (A) component ]
(A) The component is chelating agent. By containing the component (A), the stain can be removed by chemical action, and the tooth surface becomes slippery and smooth. Examples of the chelating agent include condensed phosphoric acid and its salts, organic acids and its salts, and polyacrylates. That is, the component (a) preferably contains 1 or more selected from condensed phosphoric acid, organic acid and salts thereof, and polyacrylate.
Examples of the condensed phosphoric acid and salts thereof include linear polyphosphoric acid such as pyrophosphoric acid, tripolyphosphoric acid, tetraphosphoric acid, and polyphosphoric acid having a higher polymerization degree, and salts thereof; cyclic polyphosphoric acids such as trimetaphosphate, tetrametaphosphoric acid and hexametaphosphoric acid, and salts thereof. Examples of the salt include alkali metal salts such as sodium salts and potassium salts. As the condensed phosphoric acid and its salt, pyrophosphate, polyphosphate and hexametaphosphate are preferable, and sodium pyrophosphate, sodium polyphosphate and sodium hexametaphosphate are more preferable.
Examples of the organic acid and salts thereof include oxalic acid, malonic acid, maleic acid, fumaric acid, lactic acid, malic acid, tartaric acid, citric acid, pyruvic acid, oxaloacetic acid, aspartic acid, succinic acid, glucuronic acid, adipic acid, phytic acid, phthalic acid, acetic acid, and salts thereof (for example, alkali metal salts such as sodium salt and potassium salt). Among them, malic acid, tartaric acid, citric acid, succinic acid, lactic acid, and phytic acid, and salts thereof are preferable, and malic acid, phytic acid, or salts thereof are more preferable.
As the polyacrylate, a linear polyacrylate can be used, and a polyacrylate having a weight average molecular weight (Mw) of 1000 to 20000 is preferably used. The weight average molecular weight can be measured by gel permeation chromatography/multi-angle laser light scattering detector (GPC-MALLS) under the following conditions.
Mobile phase: 0.3M NaClO 4
NaN 3 Column of aqueous solution of TSKgel alpha-M2 roots
Presetting a column: TSK guard column alpha
Standard substance: polyethylene glycol
Examples of the polyacrylate include alkali metal salts such as sodium salts and potassium salts. The polyacrylate is preferably sodium polyacrylate.
(A) The number of the components may be 1 or 2 or more.
(A) The composition preferably comprises at least any one of the following:
condensed phosphoric acid and salts thereof, wherein the condensed phosphoric acid is 1 or more selected from pyrophosphoric acid, polyphosphoric acid, hexametaphosphoric acid, and salts thereof;
an organic acid and a salt thereof, wherein the organic acid is 1 or more selected from malic acid, tartaric acid, citric acid, succinic acid, lactic acid, phytic acid and salts thereof; and
polyacrylate, which is sodium polyacrylate.
The content of the component (a) is usually 0.05 mass% or more, preferably 0.1 mass% or more, based on the entire oral composition (100 mass%). Thus, a more excellent stain removal effect can be obtained. The upper limit is usually 3.5 mass% or less, preferably 3 mass% or less, and more preferably 2.5 mass% or less. This can suppress the reduction in feeling of use caused by excessive stimulation to the oral cavity. Therefore, the content of the component (A) is usually 0.05 to 3.5% by mass, preferably 0.1 to 3% by mass, more preferably 0.1 to 2.5% by mass.
[ (B) component ]
(B) The component is N- (2-hydroxy-2-phenylethyl) -2-isopropyl-5, 5-dimethylcyclohexane-1-carboxamide. By containing the component (B), the effect of preventing the actual bad breath and the persistence thereof can be exhibited. (B) The ingredients are less likely to cause tongue irritation, and therefore the above-described effects can be obtained without impairing the smooth feeling.
The content of the component (B) is usually 0.000005 mass% or more, preferably 0.00001 mass% or more, and more preferably 0.00005 mass% or more, based on the entire oral composition (100 mass%). Thus, a good bad breath preventive feeling can be obtained. The upper limit is usually 0.5 mass% or less, preferably 0.1 mass% or less, and more preferably 0.005 mass% or less. This can suppress the stimulus from becoming too strong and reduce the smooth feeling. Therefore, the content of the component (A) is usually 0.000005 to 0.5 mass%, preferably 0.00001 to 0.1 mass%, more preferably 0.00005 to 0.005 mass%.
[ (C) component ]
(C) The components are grinding agents. By containing the component (C), a stain removing effect by physical action can be obtained.
The polishing agent may be any of an inorganic polishing agent and an organic polishing agent. The preferred RDA value (Radioactive Dentine AbrasionValues) of the abrasive is not particularly limited. The RDA value is usually 50 or more, and particularly preferably 50 to 200. Examples of the inorganic polishing agent include silica-based polishing agents such as anhydrous silicic acid, crystalline silica, amorphous silica, silica gel, aluminum silicate, zirconium silicate, zeolite, precipitated silica, and titanium-bonded silica; calcium phosphates such as non-hydrate of calcium hydrogen phosphate, calcium hydrogen phosphate 2 hydrate, calcium dihydrogen phosphate, tricalcium phosphate, calcium pyrophosphate, insoluble calcium metaphosphate, tricalcium phosphate, tetracalcium phosphate, octacalcium phosphate and the like; calcium salts such as calcium carbonate (light and heavy), calcium hydroxide, and calcium sulfate; sodium bicarbonate; aluminum abrasives such as aluminum hydroxide, aluminum oxide, and aluminum oxide (aluminum); magnesium salts such as magnesium carbonate and magnesium phosphate; apatite such as hydroxyapatite, fluorapatite and calcium-deficient apatite; bentonite; titanium dioxide. Examples of the organic polishing agent include synthetic resin polishing agents and polymethyl methacrylate. Among these, inorganic abrasives are preferable, silica-based abrasives and aluminum-based abrasives are more preferable, and 1 or more kinds selected from anhydrous silicic acid and aluminum oxide are more preferable.
The average particle diameter of the abrasive silica is preferably 1 μm to 40 μm, and the BET specific surface area of the abrasive silica is preferably 80 square meters to 250 square meters per 1 g. The average particle diameter of the abrasive silica herein is a volume-based median particle diameter (D50) measured by a laser diffraction/scattering method. Examples of the silica-based polishing agent that can be used include commercially available products such as ZEODENT (registered trademark) 124 manufactured by Evonic corporation, ZEODENT (registered trademark) 113, tixosil (registered trademark) 73 manufactured by Solvay corporation, tixosil (registered trademark) 63, and abrasive silica, zirconium silicate, and aluminum silicate manufactured by mukory corporation.
The abrasive may also be a prill. Examples of such granules include granules obtained by granulating water-insoluble powder (for example, silica gel) into granules. In granulating, any conventionally known suitable binder may be used.
(C) The number of the components may be 1 alone or 2 or more. In the case of a combination of 2 or more kinds, the above-mentioned abrasive grains and the granulated substance may be contained in combination.
When the oral composition contains the component (C), the content thereof is usually 1% by mass or more, preferably 2% by mass or more, relative to the entire oral composition (100% by mass). This can improve the cleaning force against dirt such as color stains. The upper limit is usually 35% by mass or less, preferably 30% by mass or less, and more preferably 20% by mass or less. This can suppress the generation of irritation of the oral mucosa. Therefore, the content of the component (C) is usually 1 to 35% by mass, preferably 2 to 30% by mass, and more preferably 2 to 20% by mass.
[ (D) component ]
(D) The component (C) is a lactone having 6 to 12 carbon atoms (hereinafter, the number of carbon atoms is represented by a number indicating "C" representing a carbon atom). That is, the oral composition preferably further contains a lactone which is the component (D). In the lactone having 6 to 12 carbon atoms in the component (D), the number of carbon atoms constituting the ring structure is not particularly limited.
By containing the component (D), the composition can impart sweetness to the composition after use and during use, and can suppress bitterness derived from the component (a), thereby improving the feeling of use.
Specific examples of the component (D) include C6: gamma-caprolactone, C7: gamma-heptanolactone, C8: gamma-octalactone, C9: gamma-nonolactone, C10: gamma-decalactone, C11: gamma-undecalactone, C12: gamma-dodecalactone, C6: delta-caprolactone, C7: delta-heptanolactone, C8: delta-octalactone, C9: delta-nonolactone, C10: delta-decalactone, C11: delta-undecalactone, C12: delta-dodecalactone. As the component (D), a lactone having 6 to 11 carbon atoms is preferably used, specifically, a lactone (γ -lactone) having a 5-membered ring and a lactone (δ -lactone) having a 6-membered ring are preferably used, and a lactone (γ -lactone) having a 5-membered ring is more preferably used. As the component (D), 1 or 2 or more of them can be used. That is, the oral composition preferably further contains 1 or more kinds selected from lactones having 6 to 12 carbon atoms as component (D).
When the oral composition contains the component (D), the content thereof is usually 0.000001 mass% or more, preferably 0.000005 mass% or more, and more preferably 0.00001 mass% or more, based on the entire oral composition (100 mass%). This can impart a favorable sweet taste and suppress bitterness. The upper limit is usually 0.2 mass% or less, preferably 0.1 mass% or less, and more preferably 0.05 mass% or less. This can suppress the deterioration of the feeling of use of the oral composition due to the excessive increase of the sweetness. Therefore, the content of the component (D) is usually 0.000001 to 0.2 mass%, preferably 0.000005 to 0.1 mass%, more preferably 0.00001 to 0.05 mass%.
[ optional ingredients ]
The oral composition may contain any component other than the components (a) to (D) described above within a range that does not impair the effects of the present invention.
Examples of the optional ingredients include surfactants, sweeteners, flavors, pharmaceutical ingredients, oily ingredients, preservatives, humectants, binders, pH adjusters, colorants (pigments), and solvents. Hereinafter, the description will be made specifically.
Surfactant-containing compositions
Examples of the surfactant other than the component (C) include anionic surfactants, nonionic surfactants, and amphoteric surfactants.
Examples of the anionic surfactant include alkyl sulfate, acyl amino acid salt, acyl taurate, alpha-olefin sulfonate, hydrogenated coconut fatty acid monoglyceride monosulfate, and laurylsulfonate acetate. The alkyl group and the acyl group may be either a straight chain or a branched chain, and may be either saturated or unsaturated, and the number of carbon atoms thereof is usually 10 to 20, preferably 12 to 18, more preferably 12 to 14. The salt can be selected from pharmacologically acceptable salts. Examples of pharmacologically acceptable salts include base addition salts and amino acid salts. Specific examples thereof include inorganic alkali salts such as sodium salt, potassium salt, calcium salt, magnesium salt, and ammonium salt; organic base salts such as triethylammonium salt, triethanolammonium salt, pyridinium salt, diisopropylammonium salt, and the like; basic amino acid salts such as arginine salts. Among them, inorganic alkali salts are preferable, alkali metal salts (e.g., sodium salt, potassium salt) or ammonium salt are more preferable, and sodium salt is further preferable.
Examples of the alkyl sulfate include lauryl sulfate (sodium lauryl sulfate) and myristyl sulfate. Examples of the acyl amino acid salt include acyl sarcosinates such as lauroyl sarcosinate and myristoyl sarcosinate; acyl glutamate such as lauroyl glutamate, myristoyl glutamate, palmitoyl glutamate, and the like; acyl glycinates such as N-lauroyl-N-methylglycinate and cocoyl glycinate; acyl alanine salts such as N-lauroyl- β -alanine salt, N-myristoyl- β -alanine salt, N-cocoyl- β -alanine salt, N-lauroyl-N-methyl- β -alanine salt, N-myristoyl-N-methyl- β -alanine salt, and N-methyl-N-acyl alanine salt; acyl aspartate such as lauroyl aspartate. Examples of the acyl taurates include lauroyl methyl taurate, N-methyl-N-acyl taurate, and N-cocoyl methyl taurate. Examples of the α -olefin sulfonate include α -olefin sulfonates having 12 to 18 carbon atoms such as tetradecene sulfonate. As other examples of the anionic surfactant, sodium hydrogenated coco fatty acid monoglyceride monosulfate, sodium laurylsulfate, etc. may be mentioned.
The anionic surfactant preferably contains a sulfonic acid group, and more preferably an alkyl sulfate or an α -olefin sulfonate, from the viewpoint of good foaming and foaming properties.
Examples of the nonionic surfactant include polyoxyethylene alkyl ether, polyoxyethylene hydrogenated castor oil, sorbitan fatty acid ester, polyoxyethylene sorbitan fatty acid ester (e.g., polyoxyethylene sorbitan monostearate), alkanolamide, polyoxyethylene fatty acid ester, polyoxyethylene alkenyl ether, glycerin fatty acid ester, sucrose fatty acid ester (e.g., maltitol fatty acid ester), sugar alcohol fatty acid ester (e.g., maltitol fatty acid ester, lactitol fatty acid ester), fatty acid diethanolamide (e.g., lauric acid mono-or diethanolamide), polyoxyethylene polyoxypropylene copolymer, and polyoxyethylene polyoxypropylene fatty acid ester. The number of carbon atoms of the alkyl chain of the polyoxyethylene alkyl ether is usually 14 to 18, and the average molar number of addition of ethylene oxide is usually 5 to 30. The average number of moles of ethylene oxide added to the polyoxyethylene hydrogenated castor oil is usually 20 to 100 moles, preferably 20 to 60 moles. The fatty acid of the sorbitan fatty acid ester has usually 12 to 18 carbon atoms. The fatty acid of the polyoxyethylene sorbitan fatty acid ester has usually 16 to 18 carbon atoms, and the average molar number of ethylene oxide addition is usually 10 to 40 moles. The number of carbon atoms in the alkyl chain of the alkanolamide is usually 12 to 14. As the nonionic surfactant, polyoxyethylene hydrogenated castor oil, polyoxyethylene sorbitan fatty acid esters, and polyoxyethylene alkyl ethers are preferable.
Examples of the amphoteric surfactant include betaine type amphoteric surfactants such as alkyl dimethylaminoacetic acid betaine (e.g., lauryl dimethylaminoacetic acid betaine) and fatty acid amidopropyl dimethylaminoacetic acid betaine (e.g., cocamidopropyl betaine); imidazoline-type amphoteric surfactants such as N-fatty acid acyl-N-carboxymethyl-N-hydroxyethyl ethylenediamine salt (e.g., N-coco fatty acid acyl-N-carboxymethyl-N-hydroxyethyl imidazoline betaine), coco fatty acid imidazoline betaine, and 2-alkyl-N-carboxymethyl-N-hydroxyethyl imidazoline betaine; alkyl betaines such as lauryl dimethyl glycine betaine. Examples of the cationic surfactant include alkylammonium salts and alkylbenzylammonium salts.
The content of the surfactant is preferably 5% by mass or less, more preferably 0.1% by mass to 5% by mass, still more preferably 0.5% by mass to 3% by mass, and still more preferably 1% by mass to 3% by mass, relative to the entire oral composition (100% by mass).
Wetting agent-
By adding a humectant to the oral composition, the feeling of use can be further improved.
As the wetting agent, sugar alcohols and polyols other than sugar alcohols are preferable. Examples of sugar alcohols include sugar alcohols such as sorbitol, erythritol, maltitol, lactitol, xylitol, and reduced starch saccharides; glycerol; polyhydric alcohols such as ethylene glycol, propylene glycol, dipropylene glycol, butylene glycol, and polyethylene glycol. Examples of the polyethylene glycol include polyethylene glycols having an average molecular weight of 150 to 6000, and preferably polyethylene glycols having an average molecular weight of 190 to 630. Specifically, PEG200, PEG300, PEG400, and PEG600 may be mentioned. The average molecular weight of polyethylene glycol is the average molecular weight described in standard 2006 of quasi drug material. The content of the humectant is usually 40% by mass or less, preferably 1% by mass to 30% by mass, relative to the entire oral composition (100% by mass).
Pharmaceutical compositions
Examples of the pharmaceutical ingredient include bactericidal or antibacterial agents such as cetylpyridinium chloride, benzalkonium chloride, benzethonium chloride, isopropyl methylphenol, zinc gluconate, zinc citrate, triclosan, thymol, hinokitiol (Hinokitiol), and lysozyme chloride; glucanase, mutanase, amylase, protease, and a LeTech enzyme (japanese text: bar); fluoride such as sodium fluoride, sodium monofluorophosphate, and tin fluoride; anti-inflammatory agents such as epsilon-aminocaproic acid, allantoin, tranexamic acid, glycyrrhetate (e.g., dipotassium glycyrrhizinate), glycyrrhetinic acid, glycyrrhetinate (e.g., stearyl glycyrrhetinate), allantoin chlorohydroxy aluminum, azulene, and dihydrocholesterol; metal salts such as zinc, copper salts, and tin salts; dental calculus preventive agents such as condensed phosphates and ethane hydroxy diphosphonates; blood flow promoters such as vitamin E (e.g., tocopheryl acetate); a hyperesthesia inhibitor such as potassium nitrate, aluminum lactate, strontium chloride, etc.; coating agents such as hydroxyethylcellulose dimethyl diallyl ammonium chloride; astringents such as vitamin C (e.g., ascorbic acid or a salt thereof), lysozyme chloride, and the like; water-soluble copper compounds such as copper chlorophyll and copper gluconate; amino acids such as calculus preventive agent, alanine, glycine, proline, etc.; extracts of thyme, scutellaria baicalensis, clove, witch hazel, and the like; fur seal peptide (Caropeptide), polyvinylpyrrolidone. The pharmaceutical ingredients may be used alone or in combination of 1 or more than 2. The content of the above-mentioned medicinal ingredient can be appropriately set in an effective amount according to a conventional method.
Fragrance-mixing
By adding a flavor other than the optional component (D) to the oral composition, the feeling of use can be further improved. Examples of the perfume other than the optional component D include natural essential oils such as peppermint oil, spearmint oil, japanese peppermint oil, anise oil, cinnamon oil, eucalyptus oil, wintergreen oil, frankincense oil (mactic oil), orange flower oil (orange flower oil), lemon grass oil, jasmine oil, rose oil, iris oil, clove oil, thyme oil, sage oil, cardamon oil, rosemary oil, bay oil, chamomile oil, caraway oil, basil oil, marjoram oil, lemon oil, orange oil, lime oil, grapefruit oil, nutmeg oil, lavender oil, spica oil, vanilla (vanella) oil, cinnamon oil, pimento oil, bay leaf oil, perilla oil, wintergreen oil, and the like; perfume components contained in the above natural essential oils such as menthol, carvone (carvone), cinnamaldehyde, anethole, 1, 8-cineole, methyl salicylate, eugenol, thymol, linalool, limonene, menthone, menthyl acetate, citral, decanal, camphor, borneol (born), pinene, spilanthol, n-decanol, citronellol, α -terpineol, citronellyl acetate, eucalyptol, ethyl linalool, and vanillin; perfume components such as ethyl acetate, ethyl butyrate, isoamyl acetate, hexanal, hexenal, methyl anthranilate (methyl anthranilate), ethyl methylphenyl glycidate (ethyl methylphenylglycidate), benzaldehyde, vanillin, ethyl vanillin, furanol, N-ethyl-p-menthane-3-carboxamide, menthyl lactate, ethylene glycol-l-menthyl carbonate, and the like; and various blended essences such as peppermint system, fruit system, and herb (hereb) system, which are obtained by combining several perfume components and natural essential oils. As the perfume, 1 kind of the above-exemplified perfumes may be used alone or 2 or more kinds may be used in combination within a range not impairing the effects of the present invention.
Sweetener-
By adding a sweetener to the oral composition, the feeling of use can be further improved. Examples of the sweetener include saccharin, sodium saccharin, aspartame, stevioside, stevia extract, p-methoxycinnamaldehyde, neohesperidin dihydrochalcone, perillartine, glycyrrhizic acid, sweet taste protein (Thaumatin), aspartyl phenylalanine methyl ester (aspartyl-phenylalanine methyl ester), and the like. As the sweetener, 1 kind of the above-exemplified sweetener may be used alone, or 2 or more kinds may be used in combination.
Oily component-
Examples of the oily component include hydrocarbons such as squalane, liquid paraffin, vaseline, and microcrystalline wax; higher alcohols (for example, alcohols having 8 to 22 carbon atoms such as lauryl alcohol, cetyl alcohol, cetostearyl alcohol (Cetostearyl alcohol), oleyl alcohol, isostearyl alcohol, etc.); higher fatty acids (for example, fatty acids having 8 to 22 carbon atoms such as lauric acid, myristic acid, oleic acid, and isostearic acid), vegetable oils such as olive oil, castor oil, and coconut oil; fatty acid esters such as isopropyl myristate.
Preservative-
By incorporating a preservative into the oral composition, the preservative power of the preparation can be ensured. Examples of the preservative include parahydroxybenzoate (e.g., methyl parahydroxybenzoate, ethyl parahydroxybenzoate, butyl parahydroxybenzoate), sodium benzoate, and the like. The preservative may be used alone or in combination of 1 or more than 2.
Adhesive agent
By adding an optional binder to the oral composition, the viscosity can be optimized, and the shape retention and the feel in use can be further improved. Examples of the binder include conventionally known any suitable organic binders, such as polysaccharides, cellulose-based binders (e.g., carboxymethyl cellulose (CMC), hydroxyethyl cellulose, hydroxypropyl methylcellulose, and cationized cellulose), other polysaccharide-based tackifiers (e.g., xanthan gum, guar gum, gellan gum, tragacanth gum, karaya gum, gum arabic, locust bean gum, carrageenan, and sodium alginate), and synthetic water-soluble polymers (e.g., sodium polyacrylate, carboxyvinyl polymer, polyvinylpyrrolidone, polyvinyl alcohol, and propylene glycol alginate). Further, inorganic binders such as thickening silica and aluminum silicate may be mentioned. The content of any organic binder is preferably 0 to 3% by mass, more preferably 0.1 to 2% by mass, relative to the entire oral composition (100% by mass). The content of the inorganic binder is preferably 0 to 10 mass%, more preferably 1 to 8 mass%.
pH regulator-
By including a pH adjuster in the oral composition, the pH stability of the preparation can be ensured. Examples of the optional pH adjuster include hydroxides such as sodium hydroxide and potassium hydroxide, phosphoric acid or its salt, sodium hydrogen phosphate, and sodium dihydrogen phosphate.
The content of the pH adjustor is usually an amount capable of adjusting the pH of the oral composition after addition to 5 to 9, preferably 6 to 8.5.
In the present specification, the pH generally means a value after 3 minutes at 25 ℃ from the start of measurement. The pH value can be measured, for example, using a pH meter (model Hm-30S) manufactured by Toyama electric wave industries Co.
Coloring agent-
Examples of the coloring agent include natural pigments such as red flower pigment, gardenia yellow pigment, gardenia blue pigment, perilla pigment, monascus pigment, red cabbage pigment, carrot pigment, hibiscus (Hibiscus) pigment, cocoa pigment, spirulina blue pigment, tamarind pigment, etc., legal pigments such as red No. 2, red No. 3, red No. 104, red No. 105, red No. 106, red No. 227, yellow No. 4, yellow No. 5, green No. 3, blue No. 1, etc., riboflavin, sodium copper chlorophyll, titanium dioxide, etc. When the oral composition contains a colorant, the content thereof is preferably 0.00001 to 3% by mass relative to the entire oral composition.
Solvent-
Examples of the solvent include water (purified water) and ethanol. The solvent may be used alone or in combination of 1 or more than 2.
Other optional ingredients-
Examples of any component other than the above include polyisobutylene, polybutadiene, urethane, silicon, and natural rubber. The content of these other optional components can be appropriately set within a range that does not hinder the effects of the present invention.
[ dosage form and use of oral composition ]
The oral composition of the present invention can be formulated into oral preparations such as dentifrices, mouthwashes, sprays, coating agents, patches, and oral dissolves.
The dosage form of the oral composition is not particularly limited, and may be appropriately selected according to the mode of use. For example, the formulation may be in the form of paste, liquid, or the like, and if the formulation is a dentifrice, the formulation may be in the form of paste, liquid, or wet dentifrice.
[ method for producing oral composition ]
The method for producing the oral composition is not particularly limited. The oral composition can be produced by various usual methods depending on the dosage form. For example, when the toothpaste is used, there is a method in which after preparing a component dissolved in a solvent, other insoluble components are mixed, and if necessary, deaeration (for example, depressurization or the like) is performed. The toothpaste obtained by this method can be stored in a container to prepare a product. The shape and material of the container are not particularly limited, and a container used in a usual dentifrice composition can be used. Examples of the container include a container such as a plastic laminate tube made of polyethylene, polypropylene, polyethylene terephthalate, nylon, or the like.
Examples
Hereinafter, the present invention will be specifically described with reference to examples and comparative examples, but the present invention is not limited to the examples. In each example, the% is mass percentage.
Examples 1 to 21 and comparative examples 1 to 12
Oral compositions (toothpastes) having compositions shown in tables 1 to 5 were prepared by a conventional method, and contained in a usual oral preparation container (toothpaste: laminate tube). Using these as samples, evaluation was performed by the method shown below. The results are shown in tables 1 to 3.
< raw materials used >
Component (A)
A1: sodium pyrophosphate (trade name: sodium pyrophosphate, manufacturer: taiping chemical industry Co., ltd.)
A2: sodium polyphosphate (trade name: sodium polyphosphate, manufacturer: taiping chemical industry Co., ltd.)
A3: sodium hexametaphosphate (trade name: sodium hexametaphosphate, manufacturer: taiping chemical industry Co., ltd.)
A4: malic acid (trade name: malic acid, manufacturer: hibiscus chemical Co., ltd.)
A5: phytic acid (trade name: phytic acid, manufacturer: hibiscus chemical industry Co., ltd.)
A6: sodium polyacrylate (trade name: AC-10NPD, manufacturer: toyama Synthesis Co., ltd.)
Component (B) and its substitute
N- (2-hydroxy-2-phenylethyl) -2-isopropyl-5, 5-dimethylcyclohexane-1-carboxamide (trade name: coolact (registered trademark) 370, manufacturer: high sand fragrance industry Co., ltd.)
N-ethyl-p-menthane-3-carboxamide (trade name: WS-3, manufactured by Symprise) Japan Co., ltd
N- (2- (2-pyridyl) ethyl) -2-isopropyl-5-methylcyclohexane carboxamide: (Evercool (registered trademark) 190, manufactured by Givaudan) corporation, qi Hua Du
Component (C)
C1: abrasive silica: (Tixosil (registered trademark) 73, manufactured by Solvay Co., ltd.)
C2: alumina (trade name: alumina, manufacturer: japanese light metals Co., ltd.)
Component (D)
D1: gamma-caprolactone: (manufacturer: fragrance on well (Co., ltd))
D2: gamma-undecalactone: (manufacturer: fragrance on well (Co., ltd))
Components other than components (A) - (D)
Sodium fluoride: (company of Stella Chemifa)
Sodium lauryl sulfate: (manufactured by BASF corporation)
Sorbitol solution (70%): (Mitsubishi business life science Co., ltd.)
Propylene glycol: (manufactured by ADEKA Co., ltd.)
Thickening silica: carplex (registered trademark) #67 (DSL Japanese Co., ltd.)
Sodium saccharin: (manufactured by Aisan chemical industry Co., ltd.)
As for the components other than the above, materials conforming to the standard 2006 of quasi-drug materials are used.
< evaluation method >)
Evaluation was performed by 4 subjects.
A1 g sample of the toothpaste was placed on a toothbrush (Clinica Advantage toothbrush, 4 rows of compact conventional, manufactured by lion king Co., ltd.) and after brushing for 3 minutes, the mouth was rinsed once with 10mL of water. The oral cavity after use was stimulated, the teeth after use were smooth (smooth feeling was easy), the breath malodor was prevented, no bitterness was observed, and the use feeling was good, and the average score of 4 subjects was determined based on the following evaluation criteria, and the evaluation was performed according to the following evaluation criteria. Here, the "bad breath preventing sensation" means that the feeling of smoothness is felt even after 60 minutes after use, and the "good feeling of use" means that the bad smell generated by bitter taste and excessive sweetness is not generated.
< stimulation in oral cavity >)
Scoring benchmark
5: no sense at all
4: less feel of
3: slightly feel to
2: feel is perceived as
1: very feel is very good
Evaluation criterion
Preferably: more than 4 minutes
Good: 3 minutes or more and less than 4 minutes
Disqualification: less than 3 minutes
< smooth feel of teeth >)
Scoring benchmark
5: very feel is very good
4: feel is perceived as
3: slightly feel to
2: less feel of
1: no sense at all
Evaluation criterion
Preferably: 4 minutes above: 3 or more and less than 4 is disqualified: less than 3 minutes
< bad breath prevention feeling >)
Scoring benchmark
5: very feel is very good
4: feel is perceived as
3: slightly feel to
2: less feel of
1: no sense at all
Evaluation criterion
Preferably: 4 minutes above: 3 or more and less than 4 is disqualified: less than 3 minutes
< no bitter taste >)
Scoring benchmark
5: no bitter taste is felt at all
4: almost no bitter taste was perceived
3: slightly bitter, but within the allowable range 2: perceived bitter taste
1: very much perceived bitter taste
Evaluation criterion
Preferably: 4 minutes above: 3 or more and less than 4 is disqualified: less than 3 minutes
< good feeling of use >)
Scoring benchmark
5: very feel is very good
4: slightly feel to
3: feel is perceived as
2: less perceived 1: no evaluation criterion was perceived at all: 4 minutes above: 3 or more and less than 4 is disqualified: less than 3 minutes
TABLE 1
TABLE 2
/>
TABLE 3
TABLE 4
TABLE 5
The composition of the perfume is shown below.
In comparative examples 1 to 6 containing the component (a) but not containing the component (B), the evaluation of the bad breath preventive effect was low, and in comparative example 7 containing the component (B) but not containing the component (a), the evaluation of the tooth smoothness was low. In comparative examples 8 and 9, which contained other cold feeling agents instead of the component (B), the evaluation of the bad breath preventive effect and the smooth feeling of the teeth was low. On the other hand, in examples 1 to 13 containing the components (a) and (B), the balance was very good among all the evaluations of the oral cavity irritation, the smooth feeling of teeth, and the bad breath prevention effect. Among these, in examples 7, 8 and 13 further containing the component (C), the evaluation of the smooth feeling of teeth was more excellent. These results indicate that the oral composition of the present invention can exert both a sensation of preventing halitosis and a smooth feeling while suppressing the stimulation in the oral cavity. Further, in comparative example 10 containing component (a) and component (B) but not containing component (D), the bitterness was strong, in comparative example 11 containing component (B) and component (D) but not containing component (a), the evaluation of the smooth feeling of teeth was low although there was no bitterness, and in comparative example 12 containing component (a) and component (C) but not containing component (B), the evaluation of the bad breath preventive feeling was low, and the bitterness was also strongly evaluated. In contrast, in examples 14 to 21 containing the component (a), the component (B) and the component (D), further containing the component (D) gave excellent evaluation of no bitterness and good evaluation of the feel in use.

Claims (11)

1. An oral composition comprising:
(A) Chelating agents
(B) N- (2-hydroxy-2-phenylethyl) -2-isopropyl-5, 5-dimethylcyclohexane-1-carboxamide.
2. The oral composition of claim 1, wherein,
(A) The component (A) contains 1 or more selected from the group consisting of condensed phosphoric acid, organic acid, salts thereof, and polyacrylate.
3. The oral composition of claim 1, wherein,
(A) The composition comprises at least any one of the following components:
condensed phosphoric acid and salts thereof, wherein the condensed phosphoric acid is 1 or more selected from the group consisting of pyrophosphoric acid, polyphosphoric acid, hexametaphosphoric acid and salts thereof;
an organic acid and a salt thereof, wherein the organic acid is 1 or more selected from the group consisting of malic acid, tartaric acid, citric acid, succinic acid, lactic acid, phytic acid, and salts thereof; and
and polyacrylate, wherein the polyacrylate is sodium polyacrylate.
4. The oral composition according to any one of claim 1 to 3, wherein,
(A) The content of the components is 0.1 to 3 mass%.
5. The oral composition according to any one of claims 1 to 4, wherein,
(B) The content of the components is 0.00001 to 0.1 mass percent.
6. The oral composition according to any one of claims 1 to 5, wherein,
the oral composition further comprises (C) an abrasive.
7. The oral composition of claim 6, wherein,
(C) The content of the components is 2 to 30 mass%.
8. The oral composition according to claim 6 or 7, wherein,
(C) The component (A) is 1 or more selected from the group consisting of anhydrous silicic acid and aluminum oxide.
9. The oral composition according to any one of claims 1 to 8, wherein,
the oral composition further comprises (D) a lactone having 6 to 12 carbon atoms.
10. The oral composition of claim 9, wherein,
(D) The content of the components is 0.000001 to 0.2 mass percent.
11. The oral composition according to any one of claims 1 to 10, wherein,
the oral composition is dentifrice, collutory, spray, coating agent, patch or oral cavity dissolvent.
CN202180087622.0A 2020-12-28 2021-11-30 Oral composition Pending CN116634986A (en)

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