WO2022145166A1

WO2022145166A1 - Composition for oral use

Info

Publication number: WO2022145166A1
Application number: PCT/JP2021/043963
Authority: WO
Inventors: 駿太石井; 将登平泉; 竜小久保
Original assignee: ライオン株式会社
Priority date: 2020-12-28
Filing date: 2021-11-30
Publication date: 2022-07-07
Also published as: CN116634986A; JPWO2022145166A1

Abstract

In view of problems in the prior art, the purpose of the present invention is to provide a composition for oral use that limits stimulation in the mouth while achieving both a sensation of preventing bad breath and the feeling that teeth are smooth and clean. The present invention provides a composition for for oral use such as a dentifrice, a mouthwash, a spray, a liniment, an adhesive patch, or an orally-dissolving drug, the composition containing: (A) a chelating agent such as a condensed phosphate, an organic acid, a salt of a condensed phosphate or organic acid, or a polyacrylate; and (B) N-(2-hydroxy-2-phenylethyl)-2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide.

Description

Oral composition

The present invention relates to an oral composition.

The feeling of cleaning the dentifrice, that is, the smooth and smooth texture of the tooth surface (smoothness) is reminiscent of bright white teeth, and it is a feeling that greatly contributes to the satisfaction of tooth brushing behavior as well as the feeling of preventing bad breath. The smooth feeling of the tooth is obtained in a state where the surface of the tooth is cleaned, and this includes, for example, a means such as chemical removal with a chelating agent. The actual feeling of the effect is usually recognized as the smoothness of the tooth surface when the toothpaste user traces the surface of the tooth with the tongue after brushing, that is, a smooth feel (smooth feel).

On the other hand, as a means for imparting a feeling of preventing bad breath to the oral composition, a cooling sensation agent may be added.

For example, in Patent Document 1, a dentin composition containing N- (4-cyanomethylphenyl) -2-isopropyl-5-methylcyclohexanecarboxamide and sodium polyacrylate and / or sodium alginate is described as persistent. It is described that it can provide a high oral cleanliness and a good feeling of use. According to Patent Document 2, a dentifrice composition containing a chelating agent and N- (4-cyanomethylphenyl) -2-isopropyl-5-methylcyclohexanecarboxamide gives a high oral cleaning sensation and an excellent halitosis prevention sensation. Is described. Patent Document 3 describes that an oral care composition containing a polyphosphorylated compound and a cooling sensation agent such as menthol has a whitening and stain-preventing effect.

International Publication No. 2018/221620 International Publication No. 2018/221617 Special Table 2009-531425 Gazette

However, in the combination of the conventional chelating agent and the cooling sensation agent in the compositions described in Patent Documents 1 to 3, the stains on the teeth can be cleanly removed from the irritation of the tongue by the cooling sensation agent. It may not be possible to fully realize the "smoothness of the tooth surface". In particular, if the amount of the cooling sensation agent is increased in order to improve the sustainability required for the feeling of prevention of bad breath, the influence on the sensation of the tongue becomes large, and the smooth feeling of the teeth becomes more difficult to feel.

In view of the above-mentioned problems of the prior art, an object of the present invention is to provide an oral composition capable of exhibiting both a feeling of preventing bad breath and a feeling of slipperiness while suppressing irritation in the oral cavity.

That is, the present invention provides the following [1] to [11].
[1] (A) Chelating agent and
(B) An oral composition containing N- (2-hydroxy-2-phenylethyl) -2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide.
[2] The oral composition according to [1], wherein the component (A) contains at least one selected from the group consisting of condensed phosphoric acid, organic acids, salts thereof, and polyacrylic acid salts.
[3] The oral composition according to [1], wherein the component (A) contains at least one of the following:
Condensed phosphoric acid and its salt, which is one or more selected from the group consisting of pyrophosphoric acid, polyphosphoric acid, hexametaphosphoric acid and salts thereof;
One or more organic acids selected from the group consisting of malic acid, tartaric acid, citric acid, succinic acid, lactic acid, phytic acid, and salts thereof; and salts thereof;
Polyacrylic acid salt which is sodium polyacrylate.
[4] The oral composition according to any one of [1] to [3], wherein the content of the component (A) is 0.1 to 3% by mass.
[5] The oral composition according to any one of [1] to [4], wherein the content of the component (B) is 0.00001 to 0.1% by mass.
[6] The oral composition according to any one of [1] to [5], further containing (C) an abrasive.
[7] The oral composition according to [6], wherein the content of the component (C) is 2 to 30% by mass.
[8] The oral composition according to [6] or [7], wherein the component (C) is at least one selected from the group consisting of silicic anhydride and aluminum oxide.
[9] The oral composition according to any one of [1] to [8], further containing (D) a lactone having 6 to 12 carbon atoms.
[10] The oral composition according to [9], wherein the content of the component (D) is 0.000001 to 0.2% by mass.
[11] The oral composition according to any one of [1] to [10], which is a dentifrice, a mouthwash, a spray, a coating agent, a patch, or an oral dissolving agent.

According to the present invention, there is provided an oral composition capable of exhibiting both a feeling of preventing bad breath and a feeling of smoothness while suppressing irritation in the oral cavity.

Hereinafter, the present invention will be described in detail.
The oral composition of the present invention contains the following components (A) and (B), and preferably further contains the component (C).

[(A) component]
The component (A) is a chelating agent. By containing the component (A), stains are removed by chemical action, and the tooth surface becomes smooth and smooth. Examples of the chelating agent include condensed phosphoric acid and its salt, organic acid and its salt, and polyacrylic acid salt. That is, the component (A) preferably contains one or more selected from the group consisting of condensed phosphoric acid, organic acids, salts thereof, and polyacrylic acid salts.

Condensed phosphoric acid and salts thereof include linear polyphosphoric acids such as pyrophosphoric acid, tripolyphosphoric acid, tetrapolyphosphoric acid, and polyphosphoric acid having a higher degree of polymerization and salts thereof; trimetaphosphate, tetramethaphosphate, hexametaphosphate. Such as cyclic polyphosphoric acid and salts thereof. Examples of the salt include alkali metal salts such as sodium salt and potassium salt. As the condensed phosphoric acid and a salt thereof, pyrophosphate, polyphosphate and hexametaphosphate are preferable, and sodium pyrophosphate, sodium polyphosphate and sodium hexametaphosphate are more preferable.

Examples of the organic acid and its salt include oxalic acid, malonic acid, maleic acid, fumaric acid, lactic acid, malic acid, tartrate acid, citric acid, pyruvate acid, oxaloacetic acid, aspartic acid, succinic acid, glucuronic acid, adipic acid, and the like. Examples thereof include 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 polyacrylic acid salt, a linear polyacrylic acid salt can be used, and it is preferable to use a polyacrylic acid salt having a weight average molecular weight (Mw) of 1,000 or more and 20,000 or less. Here, the weight average molecular weight can be measured using a gel permeation chromatograph / multi-angle laser light scattering detector (GPC-MALLS) under the following conditions.
Mobile phase: 0.3M NaClO ₄
NaN ₃ aqueous solution column: TSKgelα-M 2 pre-columns: TSK guardgroup α
Standard substance: Polyethylene glycol

Examples of the polyacrylic acid salt include alkali metal salts such as sodium salt and potassium salt. The polyacrylic acid salt is preferably sodium polyacrylate.
The component (A) may be one kind or a combination of two or more kinds.
The component (A) preferably contains at least one of the following:
Condensed phosphoric acid and its salt, which is one or more selected from the group consisting of pyrophosphoric acid, polyphosphoric acid, hexametaphosphoric acid, and salts thereof;
One or more organic acids selected from the group consisting of malic acid, tartaric acid, citric acid, succinic acid, lactic acid, phytic acid, and salts thereof; and salts thereof;
Polyacrylic acid salt which is sodium polyacrylate.

The content of the component (A) is usually 0.05% by mass or more, preferably 0.1% by mass or more, based on the entire oral composition (100% by mass). Thereby, a better stain removing effect can be obtained. The upper limit is usually 3.5% by mass or less, preferably 3% by mass or less, and more preferably 2.5% by mass or less. As a result, it is possible to suppress a decrease in usability due to 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, and more preferably 0.1 to 2.5% by mass.

[(B) component]
The component (B) is N- (2-hydroxy-2-phenylethyl) -2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide. By containing the component (B), the effect of preventing bad breath and its sustainability can be exhibited. Since the component (B) is less likely to cause tongue irritation, the above effect can be obtained without impairing the smooth feeling.

The content of the component (B) is usually 0.000005% by mass or more, preferably 0.00001% by mass or more, more preferably 0.00005% by mass or more, based on the entire oral composition (100% by mass). Is. As a result, a good feeling of prevention of bad breath can be obtained. The upper limit is usually 0.5% by mass or less, preferably 0.1% by mass or less, and more preferably 0.005% by mass or less. As a result, it is possible to prevent the stimulus from becoming too strong and the slippery feeling from being lowered. Therefore, the content of the component (A) is usually 0.000005 to 0.5% by mass, preferably 0.00001 to 0.1% by mass, and more preferably 0.00005 to 0.005% by mass. be.

[(C) component]
The component (C) is an abrasive. By containing the component (C), a stain removing effect due to a physical action can be obtained.
The abrasive may be either an inorganic abrasive or an organic abrasive. The preferred RDA value (Radioactive Dentin Abrasion Values) of the abrasive is not particularly limited. The RDA value is usually 50 or more, 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, aluminosilicate, zirconosilicate, zeolite, precipitated silica, and titanium-binding silica; hydrogen phosphate. Calcium Anhydrous, Calcium Hydrogen Phosphate Dihydrate, 1st Calcium Phosphate, 3rd Calcium Phosphate, Calcium Pyrophosphate, Insoluble Calcium Metaphosphate, 3rd Calcium Phosphate, 4th Calcium Phosphate, 8th Calcium Phosphate and other Calcium Phosphate; Calcium Carbonate (Light, Heavy) Quality), calcium salts such as calcium hydroxide and calcium sulfate; sodium hydrogen carbonate; aluminum-based abrasives such as aluminum hydroxide, aluminum oxide and alumina; magnesium salts of magnesium carbonate and tertiary magnesium phosphate; hydroxyapatite and fluoroapatite , Apatites such as calcium-deficient apatite; bentonite; titanium dioxide. Examples of the organic abrasive include synthetic resin-based abrasives and polymethylmethacrylate. Among them, an inorganic abrasive is preferable, a silica-based abrasive and an aluminum-based abrasive are more preferable, and one or more selected from the group consisting of silicic acid anhydride and aluminum oxide is more preferable.

The abrasive silica is preferably abrasive particles having an average particle size of 1 to 40 μm, and the BET specific surface area of the abrasive silica is preferably 80 to 250 square meters per gram. Here, the average particle size of the abrasive silica is a volume-based median diameter (D50) measured by a laser diffraction / scattering method. Commercially available products can be used as the silica-based polishing agent, for example, ZEODENT (registered trademark) 124, ZEODENT (registered trademark) 113 manufactured by Evonic, Tixosil (registered trademark) 73, Tixosil (registered trademark) 63 manufactured by Solvay. , Polishable silica, zirconosilicate, aluminosilicate, etc. manufactured by Taki Chemical Co., Ltd. can be mentioned.

The abrasive may be a granulated product. Examples of such granulated products include particles obtained by granulating water-insoluble powder (for example, silica gel) into granules. When granulating into granules, a conventionally known arbitrary suitable binder may be used.
The component (C) may be used alone or in combination of two or more. In the case of a combination of two or more kinds, the combination of the above-mentioned abrasive particles and the granulated product may be included.

When the oral composition contains the component (C), the content thereof is usually 1% by mass or more, preferably 2% by mass or more, based on the entire oral composition (100% by mass). This makes it possible to enhance the cleaning power against stains such as 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. Thereby, the occurrence of oral mucosal irritation can be suppressed. 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]
The component (D) is a lactone having 6 to 12 carbon atoms (hereinafter, the number of carbon atoms is shown as a number attached to "C" representing a carbon atom). That is, it is preferable that the oral composition further contains the lactone which is the component (D). In the lactone having 6 to 12 carbon atoms as the component (D), the number of carbon atoms constituting the ring structure is not particularly limited.

By containing the component (D), the oral composition can be given a sweetness during and after use, and the bitterness derived from the component (A) can be suppressed, thereby improving the feeling of use.

Specific examples of the component (D) include C6: γ-hexalactone, C7: γ-heptalactone, C8: γ-octalactone, C9: γ-nonalactone, C10: γ-decalactone, and C11: γ. -Undecalactone, C12: γ-dodecalactone, C6: δ-hexalactone, C7: δ-heptalactone, C8: δ-octalactone, C9: δ-nonalactone, C10: δ-decalactone, C11: δ-un Decalactone, C12: δ-dodecalactone. As the component (D), it is preferable to use a lactone having 6 to 11 carbon atoms, and specifically, a lactone containing a 5-membered ring (γ-lactone) and a lactone containing a 6-membered ring (δ-lactone) are used. It is preferable to use a lactone containing a 5-membered ring (γ-lactone). As the component (D), one or more of these can be used. That is, it is preferable that the oral composition further contains at least one selected from the group consisting of lactones having 6 to 12 carbon atoms as the component (D).

When the oral composition contains the component (D), the content thereof is usually 0.0000001% by mass or more, preferably 0.000005% by mass or more, based on the total amount of the oral composition (100% by mass). It is preferably 0.00001% by mass or more. As a result, good sweetness can be imparted and bitterness can be suppressed. The upper limit is usually 0.2% by mass or less, preferably 0.1% by mass or less, and more preferably 0.05% by mass or less. As a result, it is possible to prevent the sweetness from becoming too strong and the oral composition from being used poorly. Therefore, the content of the component (D) is usually 0.000001 to 0.2% by mass, preferably 0.000005 to 0.1% by mass, and more preferably 0.00001 to 0.05% by mass. be.

[Arbitrary ingredient]
The oral composition may contain any component other than the components (A) to (D) already described, as long as the effect of the present invention is not impaired.

Examples of the optional component include a surfactant, a sweetener, a fragrance, a medicinal component, an oily component, a preservative, a wetting agent, a binder, a pH adjuster, a colorant (dye), and a solvent. Hereinafter, a specific description will be given.

-Surfactant-
Examples of the surfactant other than the component (C) include an anionic surfactant, a nonionic surfactant, and an amphoteric surfactant.

Examples of the anionic surfactant include alkyl sulfates, acyl amino acid salts, acyl taurine salts, α-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 18. It is 14. The salt can be selected from pharmacologically acceptable salts. Pharmacologically acceptable salts include, for example, base addition salts and amino acid salts. Specific examples thereof include inorganic base 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 and diisopropylammonium salt; arginine salt and the like. Basic amino acid salts of. 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.

Examples of the alkyl sulfate include lauryl sulfate (sodium lauryl sulfate) and myristyl sulfate. Examples of the acyl amino acid salt include acyl sarcosine salts such as lauroyl sarcosin salt and myristoyl sarcosin salt; acyl glutamates such as lauroyl glutamate, myristoyl glutamate and palmitoyl glutamate; N-lauroyl-N-methylglycine salt and cocoyl glycine. Acylglycine salts such as salts; N-lauroyl-β-alanine salt, N-myristyl-β-alanine salt, N-cocoyl-β-alanine salt, N-lauroyl-N-methyl-β-alanine salt, N-myristoyl Acylalanine salts such as -N-methyl-β-alanine salt, N-methyl-N-acylalanine salt; acylasparaginate such as lauroyl asparagate can be mentioned. Examples of the acyl taurine salt include lauroylmethyl taurine salt, N-methyl-N-acyl taurine salt, and N-cocoyl methyl taurine salt. Examples of the α-olefin sulfonate include α-olefin sulfonates having 12 to 18 carbon atoms such as tetradecene sulfonate. Other examples of anionic surfactants include hydrogenated coconut fatty acid monoglyceride sodium monosulfate, sodium lauryl sulfoacetate.

The anionic surfactant preferably contains a sulfonic acid group in terms of foaming and good foam quality, and more preferably an alkyl sulfate or an α-olefin sulfonate.

Examples of the nonionic surfactant 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. Ethylene fatty acid esters, polyoxyethylene alkenyl ethers, glycerin fatty acid esters, sucrose fatty acid esters (eg, Martose fatty acid esters), sugar alcohol fatty acid esters (eg, multitoll fatty acid esters, lactitol fatty acid esters), fatty acid diethanolamides (eg, lauryl). Acid mono or diethanolamide), polyoxyethylene polyoxypropylene copolymer, polyoxyethylene polyoxypropylene fatty acid ester, and the like. 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 5 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. As the nonionic surfactant, polyoxyethylene hydrogenated castor oil, polyoxyethylene sorbitan fatty acid ester, and polyoxyethylene alkyl ether are preferable.

Examples of the amphoteric surfactant include betaine-type amphoteric surfactants such as alkyldimethylaminoacetic acid betaine (eg, lauryldimethylaminoacetic acid betaine) and fatty acid amide propyldimethylaminoacetic acid betaine (eg, cocamidopropyl betaine); N-. Fatty acid acyl-N-carboxymethyl-N-hydroxyethylethylenediamine salt (eg, N-palm oil fatty acid acyl-N-carboxymethyl-N-hydroxyethyl imidazolinium betaine), coconut oil fatty acid imidazolinium betaine, 2-alkyl Examples include imidazoline-type amphoteric surfactants such as -N-carboxymethyl-N-hydroxyethyl imidazolinium betaine; alkyl betaines such as lauryldimethylaminoacetic acid betaine. Examples of the cationic surfactant include an alkylammonium salt and an alkylbenzylammonium salt.

The content of the surfactant is preferably 5% by mass or less, preferably 0.1 to 5% by mass, and more preferably 0.5 to 3% by mass with respect to the entire oral composition (100% by mass). , More preferably 1 to 3% by mass.

-Wetting agent-
When the oral composition contains a wetting agent, the feeling of use can be further improved.

As the wetting agent, sugar alcohols and polyhydric alcohols other than sugar alcohols are preferable. Examples of the sugar alcohol include sugar alcohols such as sorbitol, erythritol, martitol, lactitol, xylitol, and reduced starch saccharified; glycerin; polyhydric alcohols such as ethylene glycol, propylene glycol, dipropylene glycol, butylene glycol, and polyethylene glycol. Can be mentioned. Examples of the polyethylene glycol include polyethylene glycol having an average molecular weight of 150 to 6000, and polyethylene glycol having an average molecular weight of 190 to 630 is preferable. Specific examples thereof include PEG200, PEG300, PEG400 and PEG600. 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 wetting agent is usually 40% by mass or less, preferably 1 to 30% by mass, based on the entire oral composition (100% by mass).

-Medicated ingredients-
Examples of medicinal ingredients include bactericidal or antibacterial agents such as cetylpyridinium chloride, benzalkonium chloride, benzethonium chloride, isopropylmethylphenol, zinc gluconate, zinc citrate, triclosan, timol, hinokithiol, and lysoteam chloride; Enzymes such as mutanase, amylase, protease, lytecenzyme; fluorides such as sodium fluoride, sodium monofluorophosphate, tin fluoride; ε-aminocaproic acid, allantin, tranexamic acid, glycyrrhizinate (eg, glycyrrhetin dipotassium salt) ), Glycyrrhetinic acid, glycyrrhetinic acid derivative (eg, stearyl glycyrrhetinate), anti-inflammatory agents such as allantinchlorhydroxyaluminum, azulene, dihydrocholesterol; metal salts such as zinc salt, copper salt, tin salt; condensed phosphate, ethane Toothstone preventive agent such as hydroxydiphosphonate; Blood flow promoter such as vitamin E (for example, tocopherol acetate); Sensitivity inhibitor such as potassium nitrate, aluminum lactate, strontium chloride; Coating agent such as hydroxyethylcellulosedimethyldiallylammonium chloride Astringents such as vitamin C (eg, ascorbic acid or a salt thereof), lysoteam chloride; water-soluble copper compounds such as copper chlorophyll and copper gluconate; , Chouji, Hamamelis and other plant extracts; caropeptide, polyvinylpyrrolidone and the like. The medicinal ingredient may be used alone or in combination of two or more. The content of the above medicinal component can be appropriately set as an effective amount according to a conventional method.

-Fragrance-
When the oral composition contains a fragrance other than the arbitrary component (D), the feeling of use can be further improved. Examples of fragrances other than any D component include peppermint oil, sparemint oil, Japanese peppermint oil, anis oil, cassia oil, eucalyptus oil, winter green oil, mastic oil, neroli oil (orange flower oil), and lemongrass oil. , Jasmine oil, rose oil, iris oil, clove oil, thyme oil, sage oil, cardamon oil, rosemary oil, laurel oil, camomill oil, caraway oil, basil oil, majorum oil, lemon oil, orange oil, lime oil , Yuzu oil, Natsumeg oil, Lavender oil, Paracres oil, Vanilla oil, Katsura skin oil, Pimento oil, Katsura leaf oil, Perilla oil, Winter green oil and other natural essential oils; Cineol, methylsalicylate, eugenol, timol, linalol, limonen, menton, mentylacetate, citral, decanal, camphor, borneol, pinen, spirantol, n-decyl alcohol, citronellol, α-terpineol, citronellyl acetate, cineol, ethyllinalol, Fragrance components contained in the above natural essential oils such as crocodile; ethyl acetate, ethyl butyrate, isoamyl acetate, hexanal, hexenal, methyl anthranilate, ethyl methyl phenylglycidate, benzaldehyde, vanillin, ethyl vanillin, flaneol, N-ethyl -P-mentan-3-carboxamide, mentyllactate, ethyleneglycol-l-mentylcarbonate and other fragrance ingredients; and various mint-based, fruit-based, herbal-based, etc. blended flavors made by combining several fragrance ingredients and natural essential oils. Can be mentioned. As the fragrance, the above-exemplified fragrance may be used alone or in combination of two or more as long as the effect of the present invention is not impaired.

-Sweetener-
When the oral composition contains a sweetening agent, the feeling of use can be further improved. Examples of the sweetener include saccharin, saccharin sodium, aspartame, stebioside, stevia extract, paramethoxycinnamic aldehyde, neohesperidin dihydrochalcone, perillartine, glycyrrhizin, thaumatin, aspartylphenylalanine methyl ester and the like. As the sweetener, the above-exemplified sweetener may be used alone or in combination of two or more.

-Oil component-
Examples of the oily component 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, palm oil; Examples include fatty acid esters.

-Preservative-
When the oral composition contains an antiseptic, the antiseptic power of the preparation can be ensured. Examples of 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.

-Blotting agent-
When the oral composition contains an arbitrary binder, the viscosity can be optimized, and the shape retention and usability can be further improved. As the binder, any suitable organic binder conventionally known, for example, a polysaccharide, a cellulosic binder (for example, carboxymethyl cellulose (CMC), hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropylmethyl cellulose, methyl cellulose, cation) Celluloseized cellulose, etc.), other polysaccharide thickeners (eg, xanthan gum, gua gum, gellan gum, tragant gum, karaya gum, arabiya gum, locust bean gum, carrageenan, sodium alginate), synthetic water-soluble polymers (eg, sodium polyacrylate, etc.) Cardovinyl polymer, polyvinylpyrrolidone, polyvinyl alcohol, propylene glycol alginate) can be mentioned. Further, inorganic binders such as thickening silica and aluminum silicate can also be mentioned. The content of any organic binder is preferably 0 to 3% by mass, more preferably 0.1 to 2% by mass, based on the entire oral composition (100% by mass). The content of the inorganic binder is preferably 0 to 10% by mass, more preferably 1 to 8% by mass.

-PH regulator-
When the oral composition contains a pH adjuster, the pH stability of the pharmaceutical product can be ensured. Examples of the optional pH adjuster include hydroxides such as sodium hydroxide and potassium hydroxide, phosphoric acid or a salt thereof, sodium hydrogen phosphate, sodium dihydrogen phosphate and the like.

The content of the pH adjuster can usually be such that the pH of the oral composition after addition is 5 to 9, preferably 6 to 8.5.

In the present specification, the pH value usually means a value at 25 ° C. and 3 minutes after the start of measurement. The pH value can be measured using, for example, a pH meter (model number Hm-30S) manufactured by Toa Denpa Kogyo Co., Ltd.

-Colorant-
Examples of the colorant include natural pigments such as Benibana red pigment, Kuchinashi yellow element, Kuchinashi blue pigment, perilla pigment, red koji pigment, red cabbage pigment, carrot pigment, hibiscus pigment, cacao pigment, spirulina blue pigment, and tamarind pigment. Legal dyes 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, Riboflavin, Copper Chlorophine Sodium , Titanium dioxide and the like. When the oral composition contains a colorant, the content thereof is preferably 0.00001 to 3% by mass with respect to the entire oral composition.

-solvent-
Examples of the solvent include water (purified water) and ethanol. As the solvent, one type may be used alone or two or more types may be used in combination.

-Other optional ingredients-
Examples of optional components other than the above include polyisobutylene, polybutadiene, urethane, silicon, and natural rubber. The content of these other optional components can be appropriately set as long as the effect of the present invention is not impaired.

[Dosage form and use of oral composition]
The oral composition of the present invention can be an oral preparation such as a dentifrice, a mouthwash, a spray, a coating agent, a patch, or an oral dissolving agent.
The dosage form of the oral composition can be appropriately selected depending on the usage form, and is not particularly limited. The dosage form is, for example, in the form of a paste or liquid, and if it is a dentifrice, it can be prepared as a dentifrice, a liquid dentifrice, a liquid dentifrice, or a dentifrice.

[Manufacturing method of oral composition]
The method for producing the oral composition is not particularly limited. Oral compositions can be prepared by their respective conventional methods, depending on the dosage form. For example, when it is used as a dentifrice, 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 toothpaste obtained by such a method 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. Examples of the container include a container such as a laminated tube made of plastic such as polyethylene, polypropylene, polyethylene terephthalate, and nylon.

Hereinafter, the present invention will be specifically described with reference to Examples and Comparative Examples, but the present invention is not limited to the following Examples. In addition,% in each example is a mass percentage.

Examples 1 to 21, Comparative Examples 1 to 12
Oral compositions (dentifrices) having the compositions shown in Tables 1 to 5 were prepared by a conventional method and placed in a normal oral preparation container (dentifrice: laminated tube). These were used as samples and evaluated by the method shown below. The results are also shown in Tables 1-5.

<Ingredients used>
-(A) component-
A1: Sodium pyrophosphate (trade name: sodium pyrophosphate, manufacturer: Taihei Kagaku Sangyo Co., Ltd.)
A2: Sodium polyphosphate (trade name: sodium polyphosphate, manufacturer: Taihei Kagaku Sangyo Co., Ltd.)
A3: Sodium hexametaphosphate (trade name: sodium hexametaphosphate, manufacturer: Taihei Kagaku Sangyo Co., Ltd.)
A4: Malic acid (trade name: malic acid, manufacturer: Fuso Chemical Industry Co., Ltd.)
A5: Phytic acid (trade name: phytic acid, manufacturer: Fuso Chemical Industry Co., Ltd.)
A6: Sodium polyacrylate (trade name: AC-10NPD, manufacturer: Toagosei Co., Ltd.)

-(B) component and its alternative component-
N- (2-Hydroxy-2-phenylethyl) -2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide (trade name: Coolact® 370, manufacturer: Takasago International Corporation)
N-Ethyl-p-Menthane-3-carboxamide (trade name: WS-3, manufactured by Simrise Japan)
N- (2- (2-pyridinyl) ethyl) -2-isopropyl-5-methylcyclohexanecarboxamide: (Evercool® 190, manufactured by Givaudan)

-(C) component-
C1: Polishable silica: (Tixosil® 73, manufactured by Solvay)
C2: Aluminum oxide (trade name: aluminum oxide, manufacturer: Nippon Light Metal Co., Ltd.)

-(D) component-
D1: γ-Hexalactone: (Manufacturer: Inoue Fragrance Co., Ltd.)
D2: γ-Undecalactone: (Manufacturer: Inoue Fragrance Co., Ltd.)

-Ingredients other than (A) to (D) components-
Sodium fluoride: (manufactured by Stella Chemipha Co., Ltd.)
Sodium lauryl sulfate: (manufactured by BASF)
Sorbitol liquid (70%): (manufactured by Mitsubishi Corporation Life Science Co., Ltd.)
Propylene glycol: (manufactured by ADEKA)
Viscous silica: Carplex (registered trademark) # 67 (manufactured by DSL Japan Co., Ltd.)
Saccharin sodium: (manufactured by Aisan Chemical Industry Co., Ltd.)
For ingredients other than the above, raw materials conforming to the quasi-drug raw material standard 2006 were used.

<Evaluation method>
It was evaluated by 4 subjects.
A 1 g of sample dentifrice was placed on a toothbrush (Clinica Advantage toothbrush, 4-row compact, usually manufactured by Lion Corporation), and after brushing the teeth for 3 minutes, the oral cavity was rinsed once with 10 mL of water. The irritation in the oral cavity after use, the smooth feeling of teeth after use (easiness to feel smooth), the feeling of preventing bad breath, the lack of bitterness, and the good feeling of use are judged by the following score criteria, respectively, for 4 people. The average score was calculated and evaluated according to the following evaluation criteria. Here, the actual feeling of preventing bad breath means that a refreshing feeling is felt even after 60 minutes have passed after use, and the good feeling of use means that there is no sarcasm due to bitterness or too strong sweetness.

<Stimulation in the oral cavity>
Score criteria 5: I don't feel at all 4: I don't feel much 3: I feel a little 2: I feel 1: Very feel Evaluation criteria Excellent: 4 points or more Good: 3 points or more and less than 4 points Impossible: Less than 3 points

<Smoothness of teeth>
Score criteria 5: Very feel 4: Feel 3: Slightly feel 2: Not very feel 1: Not feel at all Evaluation criteria Excellent: 4 points or more Good: 3 points or more and less than 4 points Impossible: Less than 3 points

<Halitosis prevention feeling>
Score criteria 5: Very feel 4: Feel 3: Slightly feel 2: Not very feel 1: Not feel at all Evaluation criteria Excellent: 4 points or more Good: 3 points or more and less than 4 points Impossible: Less than 3 points

<No bitterness>
Rating criteria 5: No bitterness at all 4: Almost no bitterness 3: Slight bitterness but acceptable 2: Feeling bitterness 1: Very bitterness Evaluation criteria Excellent: 4 points or higher Good: 3 Points or more and less than 4 points Impossible: Less than 3 points

<Good usability>
Rating criteria 5: Very felt 4: Slightly felt 3: Feeled 2: Not very felt 1: Not felt at all Evaluation criteria Excellent: 4 points or more Good: 3 points or more and less than 4 points Impossible: Less than 3 points

The composition of the fragrance is as follows.
Peppermint oil 50% by mass
Peppermint refined oil (20% cut in front flow) 5% by mass
Peppermint refined oil (15% cut in front and back flow) 5% by mass
Spearmint oil 1% by mass
Spearmint refined oil (20% cut in front flow) 1% by mass
Japanese mint oil 1% by mass
Japanese mint refined oil (30% cut in front flow) 1% by mass
Menthol 10% by mass
Carvone 1% by mass
Anethole 5% by mass
Solvent balance 100% by mass in total

In Comparative Examples 1 to 6 containing the component (A) but not containing the component (B), the evaluation of the halitosis prevention feeling was low, and in Comparative Example 7 containing the component (B) but not containing the component (A), the evaluation was low. The evaluation of the smoothness of the teeth was low. Further, in Comparative Examples 8 and 9 containing another cooling sensation agent instead of the component (B), the evaluation of the bad breath prevention feeling and the smooth feeling of the teeth was low. On the other hand, in Examples 1 to 13 containing the components (A) and (B), all of the evaluations of the oral irritation, the smooth feeling of the teeth, and the actual feeling of preventing bad breath were well-balanced and good. Among them, in Examples 7, 8 and 13 further containing the component (C), the evaluation of the smoothness of the teeth was more excellent. These results indicate that the oral composition of the present invention can exert both a feeling of preventing bad breath and a feeling of slipperiness while suppressing irritation in the oral cavity. Further, in Comparative Example 10 which contains the component (A) and the component (B) but does not contain the component (D), the bitterness is strong, and the component (B) and the component (D) are contained but the component (A) is not contained. In Comparative Example 11, although there is no bitterness, the evaluation of the smoothness of the teeth is low, and in Comparative Example 12, which contains the components (A) and (C) but does not contain the component (B), the evaluation of the actual feeling of preventing bad breath is low. The bitterness was also strongly evaluated. On the other hand, in Examples 14 to 21 containing the component (A), the component (B) and the component (D), the evaluation of no bitterness is excellent by further containing the component (D), and the usability is good. The evaluation was also good.

Claims

(A) Chelating agent and
(B) An oral composition containing N- (2-hydroxy-2-phenylethyl) -2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide.
The oral composition according to claim 1, wherein the component (A) contains at least one selected from the group consisting of condensed phosphoric acid, organic acids, salts thereof, and polyacrylic acid salts.
The oral composition according to claim 1, wherein the component (A) comprises at least one of the following:
Condensed phosphoric acid and its salt, which is one or more selected from the group consisting of pyrophosphoric acid, polyphosphoric acid, hexametaphosphoric acid, and salts thereof;
One or more organic acids selected from the group consisting of malic acid, tartaric acid, citric acid, succinic acid, lactic acid, phytic acid, and salts thereof; and salts thereof;
Polyacrylic acid salt which is sodium polyacrylate.
(A) The oral composition according to any one of claims 1 to 3, wherein the content of the component is 0.1 to 3% by mass.
(B) The oral composition according to any one of claims 1 to 4, wherein the content of the component (B) is 0.00001 to 0.1% by mass.
(C) The oral composition according to any one of claims 1 to 5, further containing an abrasive.
The oral composition according to claim 6, wherein the content of the component (C) is 2 to 30% by mass.
The oral composition according to claim 6 or 7, wherein the component (C) is at least one selected from the group consisting of silicic anhydride and aluminum oxide.
(D) The oral composition according to any one of claims 1 to 8, further containing a lactone having 6 to 12 carbon atoms.
The oral composition according to claim 9, wherein the content of the component (D) is 0.000001 to 0.2% by mass.
The oral composition according to any one of claims 1 to 10, which is a dentifrice, a mouthwash, a spray, a coating agent, a patch, or an oral dissolving agent.