WO2020100703A1 - Liquid oral composition - Google Patents

Liquid oral composition Download PDF

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Publication number
WO2020100703A1
WO2020100703A1 PCT/JP2019/043602 JP2019043602W WO2020100703A1 WO 2020100703 A1 WO2020100703 A1 WO 2020100703A1 JP 2019043602 W JP2019043602 W JP 2019043602W WO 2020100703 A1 WO2020100703 A1 WO 2020100703A1
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Prior art keywords
mass
composition
liquid
component
acid
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PCT/JP2019/043602
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French (fr)
Japanese (ja)
Inventor
智哉 佐藤
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花王株式会社
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Publication of WO2020100703A1 publication Critical patent/WO2020100703A1/en

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/02Cosmetics or similar toiletry preparations characterised by special physical form
    • 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
    • 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
    • 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
    • A61K8/41Amines
    • 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
    • A61K8/44Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
    • 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

Definitions

  • fatty acids or salts thereof have been widely known as components that can bring about desired effects.
  • fatty acid soaps such as sodium salts and potassium salts of fatty acids are used as detergents, as in the dentifrice composition described in Patent Document 1, for example.
  • the present invention comprises the following components (A) and (B): (A) Fatty acid having a hydrocarbon group having 10 to 22 carbon atoms, which contains unsaturated fatty acid at least in part (B) From organic amine, alkali metal hydroxide, carbonate, bicarbonate, and sesquicarbonate
  • the present invention provides a liquid oral composition containing one or more selected basic compounds and having a pH at 25 ° C of 9.6 or more and 11 or less.
  • liquid composition for oral cavity of the present invention immediately after being applied to the oral cavity, it exhibits excellent cleaning ability, and it is possible not only to remove the plaque firmly attached to the tooth surface but also in the oral cavity. It is possible to effectively suppress the adhesion of plaque to the tooth surface while being gradually diluted with saliva.
  • the liquid oral composition of the present invention comprises the following components (A) and (B): (A) Fatty acid having a hydrocarbon group having 10 to 22 carbon atoms, which contains unsaturated fatty acid at least in part (B) From organic amine, alkali metal hydroxide, carbonate, bicarbonate, and sesquicarbonate It contains one or more selected basic compounds and has a pH at 25 ° C. of 9.6 or more and 11.0 or less.
  • the liquid composition for oral cavity of the present invention comprises a combination of the fatty acid of component (A) and the basic compound of component (B) in a high pH range, immediately after being applied to the oral cavity, the component ( By mainly adsorbing to the plaque and rapidly detaching it from the tooth surface, A) mainly forms a micelle-like aggregate and can effectively remove the plaque adhered to the tooth surface. Then, as the composition is gradually diluted with saliva in the oral cavity and transitions to a low pH range, component (A) and component (B) form a vesicle-like aggregate, which densely covers the tooth surface. Thus, it is possible to effectively prevent the plaque from adhering to the tooth surface again or newly.
  • the present inventor makes the component (A) and the component (B) coexist in a state where the pH of the composition is controlled in a specific high region in advance, and the pH of the composition is adjusted by dilution with saliva during use. It has been discovered that, by transitioning to a low region, it is possible to unexpectedly achieve both a plaque removal effect and a plaque adhesion suppression effect.
  • the present invention contains, as the component (A), a fatty acid having a hydrocarbon group having 10 to 22 carbon atoms, the unsaturated fatty acid being contained at least in part.
  • the number of carbon atoms of the hydrocarbon group contained in the component (A) fatty acid is 10 or more, preferably 12 or more, more preferably 14 or more, and further preferably 18 from the viewpoint of enhancing the effect of removing plaque. It is above, is 22 or less, and is preferably 20 or less.
  • Examples of such a hydrocarbon group include a saturated hydrocarbon group, an unsaturated hydrocarbon group, a linear hydrocarbon group, and a hydrocarbon group having a branched chain. Specific examples include capric acid, lauric acid, and myristic acid.
  • Pentadecylic acid palmitic acid, palmitoleic acid, stearic acid, isostearic acid, oleic acid, linoleic acid, linolenic acid, arachidonic acid and behenic acid.
  • the component (A) contains a fatty acid having an unsaturated hydrocarbon group at least in part, that is, an unsaturated fatty acid.
  • unsaturated hydrocarbon groups include one or more selected from palmitoleic acid, oleic acid, linoleic acid, linolenic acid, and the like. Among them, one or more selected from palmitoleic acid, oleic acid, and linoleic acid are preferable, and oleic acid is more preferable, from the viewpoint of well achieving both the effect of removing plaque and the effect of suppressing adhesion of plaque.
  • the content of the unsaturated fatty acid is preferably 15% by mass or more, more preferably 20% by mass or more in the component (A) from the viewpoint of achieving both the effect of removing plaque and the effect of suppressing adhesion of plaque. And more preferably 25 mass% or more, still more preferably 30 mass% or more, still more preferably 35 mass% or more, still more preferably 50 mass% or more, and even more preferably It is 55% by mass or more, more preferably 75% by mass or more, even more preferably 90% by mass or more, still more preferably 95% by mass or more.
  • the content of the component (A) exerts an excellent cleaning effect in a high pH region in the oral cavity, and from the viewpoint of effectively removing plaque adhered to the tooth surface, the liquid oral composition of the present invention In the above, it is preferably 0.05% by mass or more, more preferably 0.1% by mass or more, further preferably 0.2% by mass or more, and still more preferably 0.4% by mass or more. , And more preferably 0.5% by mass or more.
  • the content of the component (A) is such that when the composition is diluted with saliva in the oral cavity and transitions to a low pH range, it forms a vesicle-like association with the component (B) described below to form plaque.
  • the liquid oral composition of the present invention is preferably 5% by mass or less, more preferably 3% by mass or less, and further preferably 1.5% by mass or less. And more preferably 1% by mass or less.
  • the content of the component (A) in the liquid oral composition of the present invention is preferably 0.05 to 5% by mass, more preferably 0.1 to 3% by mass, and further preferably 0.2 to 1.5% by mass, more preferably 0.2 to 1% by mass, even more preferably 0.4 to 1% by mass, still more preferably 0.5 to 1% by mass. %.
  • organic amine examples include one or more basic amino acids selected from arginine, lysine, and histidine; monoethanolamine, diethanolamine, triethanolamine, morpholine, triisopropanolamine, 2- Examples thereof include one or more alkanolamine compounds selected from amino-2-methyl-1,3-propanediol and 2-amino-2-methyl-1-propanol.
  • alkali metal hydroxide examples include one or more selected from sodium hydroxide, potassium hydroxide, calcium hydroxide, and lithium hydroxide.
  • carbonate, bicarbonate, and sesquicarbonate include one or two selected from sodium carbonate, potassium carbonate, calcium carbonate, sodium bicarbonate, potassium bicarbonate, and sodium sesquicarbonate. The above is mentioned.
  • the component (B) when the composition is diluted with saliva in the oral cavity and transitions from the high pH range to the low pH range, the vesicle-like association with the component (A) is favorably and rapidly formed.
  • one or more basic compounds selected from basic amino acids and alkanolamine compounds are preferable, and arginine or 2-amino-2-methyl-1-propanol is more preferable.
  • the content of the component (B) is such that when the composition is diluted with saliva in the oral cavity and transitions to a low pH range, it forms a vesicle-like association with the component (A) to suppress the plaque adhesion. From the viewpoint of sufficiently exhibiting, in the liquid oral cavity composition of the present invention, preferably 0.01% by mass or more, more preferably 0.1% by mass or more, and further preferably 0.17% by mass or more. And more preferably 0.25 mass% or more. In addition, the content of the component (B) in the liquid oral composition of the present invention is to be exhibited in a high pH region in the oral cavity, mainly from the viewpoint of ensuring an excellent cleaning effect by the component (A).
  • the content of the component (B) in the liquid oral composition of the present invention is preferably 0.01 to 3% by mass, more preferably 0.01 to 2% by mass, and further preferably The amount is 0.1 to 1% by mass, more preferably 0.17 to 0.8% by mass, and still more preferably 0.25 to 0.8% by mass.
  • the liquid composition for oral cavity of the present invention contains water (C) from the viewpoint that each component can be well dispersed or dissolved and well diffused in the oral cavity while maintaining good shape retention. Is preferred.
  • the water of the component (C) in the present invention includes not only purified water and the like mixed in the composition for liquid oral cavity but also each of the mixed components such as 70% sorbitol liquid (aqueous solution) used in the formulation. The total moisture contained in the liquid oral composition, including the moisture contained therein.
  • the content of such water (C) in the liquid oral composition of the present invention is preferably 50% by mass or more, more preferably 70% by mass or more, further preferably 80% by mass or more, It is preferably 99% by mass or less, more preferably 97% by mass or less, and further preferably 95% by mass or less.
  • the liquid oral composition of the present invention is a vesicle-like aggregate of the component (A) and the component (B) when the composition is diluted with saliva in the oral cavity and transitions from a high pH range to a low pH range. It is preferable to limit the content of free divalent metal ions from the viewpoint of not inhibiting the formation of the plaque and the effect of suppressing the adhesion of plaque. Specific examples of the free divalent metal ion include calcium ion and magnesium ion. The content of such free divalent metal ions in the liquid oral composition of the present invention is preferably 0.5% by mass or less, more preferably 0.1% by mass or less, and further preferably 0%.
  • liquid oral composition of the present invention in addition to the above components, for example, anionic surfactants such as alkyl sulfate ester salts; polyoxyethylene hydrogenated castor oil, sucrose fatty acid ester, etc., within the range that does not impair the effects of the present invention.
  • anionic surfactants such as alkyl sulfate ester salts; polyoxyethylene hydrogenated castor oil, sucrose fatty acid ester, etc.
  • the pH of the liquid oral composition of the present invention at 25 ° C. is 9.6 or more, preferably 9.8 or more, from the viewpoint of exhibiting an excellent cleaning effect by setting the pH environment in the oral cavity in a high pH range. And more preferably 10 or more, and further preferably 10.2 or more.
  • the pH of the liquid oral composition of the present invention at 25 ° C. changes to a low pH range when the composition is diluted with saliva in the oral cavity, and exhibits an excellent effect of suppressing plaque adhesion. Therefore, it is 11 or less, preferably 10.8 or less, more preferably 10.6 or less, and further preferably 10.4 or less.
  • the pH of the liquid oral composition of the present invention at 25 ° C. is 9.6 or more and 11 or less, preferably 9.8 to 10.8, more preferably 10 to 10.6, More preferably, it is 10.2 to 10.4.
  • organic acids such as citric acid, malic acid, lactic acid, tartaric acid and succinic acid other than the above components or salts thereof.
  • two or more kinds may be used as a pH adjusting agent.
  • the liquid oral composition of the present invention retains the composition in the oral cavity and is diluted with saliva in the oral cavity to remove the plaque adhering to the tooth surface while or after removing the dental plaque. It can be used for a method of suppressing the adhesion of plaque to the skin.
  • liquid oral composition of the present invention not only for suppressing the adhesion of the oral biofilm, it can be used for the removal of the oral biofilm, effectively both effects Can be demonstrated.
  • the present invention further discloses the following liquid oral compositions.
  • the carbon number of the hydrocarbon group contained in the fatty acid of the component (A) is preferably 12 or more, more preferably 14 or more, still more preferably 18 or more, preferably 20 or less, or
  • the hydrocarbon group contained in the fatty acid of component (A) is preferably capric acid, lauric acid, myristic acid, pentadecyl acid, palmitic acid, palmitoleic acid, stearic acid, isostearic acid, oleic acid, linoleic acid, linolenic acid, arachidonic acid.
  • the liquid oral composition according to the above [1] which is one or more selected from behenic acid and the like.
  • the unsaturated hydrocarbon group of the unsaturated fatty acid contained in the component (A) is preferably one or more selected from palmitoleic acid, oleic acid, linoleic acid, and linolenic acid, and more preferably palmitoleic.
  • the content of the unsaturated fatty acid in the component (A) is preferably 15% by mass or more, preferably 20% by mass or more, more preferably 25% by mass or more, and more preferably 30 mass% or more, more preferably 35 mass% or more, further preferably 50 mass% or more, even more preferably 55 mass% or more, even more preferably 75 mass% or more,
  • the composition for liquid oral cavity according to any one of [1] to [3] above, which is more preferably 90% by mass or more, and preferably 95% by mass or more.
  • the content of the component (A) is preferably 0.05% by mass or more, more preferably 0.1% by mass or more, further preferably 0.2% by mass or more, and further preferably 0.4 mass% or more, more preferably 0.5 mass% or more, preferably 5 mass% or less, more preferably 3 mass% or less, and more preferably 1.5 mass% or less.
  • the component (B) is preferably one or more selected from basic amino acids and alkanolamine compounds, more preferably arginine or 2-amino-2-methyl-1-propanol.
  • the content of the component (B) is preferably 0.01% by mass or more, more preferably 0.1% by mass or more, further preferably 0.17% by mass or more, and further preferably 0.25% by mass or more, preferably 3% by mass or less, more preferably 2% by mass or less, further preferably 1% by mass or less, and further preferably 0.8% by mass or less.
  • the molar ratio ((B) / (A)) of the component (B) and the component (A) is preferably 0.5 to 40, more preferably 0.9 to 30, and further preferably. 0.95 to 30, more preferably 0.95 to 20, further preferably 1 to 20, further preferably 1.5 to 20, and further preferably 1.5 to 15.
  • the pH at 25 ° C. is preferably 9.8 or higher, more preferably 10 or higher, still more preferably 10.2 or higher, preferably 10.8 or lower, more preferably 10 or higher.
  • the content of the free divalent metal ion is preferably 0.5% by mass or less, more preferably 0.1% by mass or less, further preferably 0.05% by mass or less, or The composition for liquid oral cavity according to any one of the above [1] to [9], which preferably contains no free divalent metal ion.
  • Method. Use of the liquid oral composition according to any one of the above [1] to [12], for removing the oral biofilm while suppressing the adhesion of the oral biofilm.

Abstract

The present invention pertains to a liquid oral composition that is capable of exerting excellent washing performance to thereby remove dental plaque firmly adhering to the tooth surface and, at the same time, efficiently preventing the adhesion of dental plaque to the tooth surface. Namely, the present invention pertains to a liquid oral composition comprising: (A) a fatty acid having a hydrocarbon group with 10-22 carbon atoms, inclusive, which at least partly contains an unsaturated fatty acid; and (B) one or more kinds of basic compounds selected from among an organic amine, an alkali metal hydroxide, a carbonate, a bicarbonate and a sesquicarbonate, and having a pH of 9.6-11 inclusive at 25°C.

Description

液体口腔用組成物Liquid oral composition
 本発明は、液体口腔用組成物に関する。 The present invention relates to a liquid oral composition.
 従来より、種々の口腔用組成物において、脂肪酸又はその塩は、所望の作用をもたらし得る成分として広く知られる成分である。なかでも、例えば特許文献1に記載の歯磨剤組成物のように、脂肪酸のナトリウム塩やカリウム塩等の脂肪酸石鹸は、洗浄剤として用いられている。 In the various oral compositions, fatty acids or salts thereof have been widely known as components that can bring about desired effects. Among them, fatty acid soaps such as sodium salts and potassium salts of fatty acids are used as detergents, as in the dentifrice composition described in Patent Document 1, for example.
 一方、特許文献2に記載の口腔用組成物では、脂肪酸塩を歯面コート剤として配合しており、さらに特許文献3~4に記載の口腔用組成物では、脂肪酸又はその塩と脱感作剤、或いは脂肪酸と塩基性アミノ酸により、塩を形成させて象牙質細管を封鎖し、象牙質知覚過敏症の症状を軽減する効果を発揮させている。 On the other hand, in the oral composition described in Patent Document 2, a fatty acid salt is blended as a tooth surface coating agent, and in the oral compositions described in Patent Documents 3 to 4, the fatty acid or its salt and desensitization are used. The agent, or a fatty acid and a basic amino acid, forms a salt to block the dentin tubules and exert the effect of reducing the symptoms of dentin hypersensitivity.
  (特許文献1)特開2009-40756号公報
  (特許文献2)特開2000-103726号公報
  (特許文献3)特開2015-124216号公報
  (特許文献4)特開2014-62066号公報
(Patent Document 1) JP 2009-40756 A (Patent Document 2) JP 2000-103726 A (Patent Document 3) JP 2005-124216 A (Patent Document 4) JP 2014-62066 A
 本発明は、次の成分(A)及び(B):
 (A)少なくとも一部に不飽和脂肪酸を含む、炭素数10以上22以下の炭化水素基を有する脂肪酸
 (B)有機アミン、アルカリ金属水酸化物、炭酸塩、重炭酸塩、及びセスキ炭酸塩から選ばれる1種又は2種以上の塩基性化合物
を含有し、かつ25℃におけるpHが9.6以上11以下である液体口腔用組成物を提供するものである。
The present invention comprises the following components (A) and (B):
(A) Fatty acid having a hydrocarbon group having 10 to 22 carbon atoms, which contains unsaturated fatty acid at least in part (B) From organic amine, alkali metal hydroxide, carbonate, bicarbonate, and sesquicarbonate The present invention provides a liquid oral composition containing one or more selected basic compounds and having a pH at 25 ° C of 9.6 or more and 11 or less.
 ところで、脂肪酸を用いつつ、良好な口腔内環境を保持することのできる有用な口腔用組成物の実現を試みるにあたっては、高い洗浄能を発揮して歯面に堅固に付着した歯垢を除去できるだけでなく、その後においても歯面に歯垢が付着してしまうのを有効に抑制できる組成物であることが望まれる。
 しかしながら、特許文献1に記載の組成物であると、歯垢除去効果についてはある程度発揮し得るであろうものの、歯垢付着抑制効果までをも発揮させるには、さらなる改善を要する。一方、特許文献2~4に記載の組成物であっても、歯垢の除去や付着抑制については何らの検討もなされておらず、充分に改善の余地がある。
By the way, in attempting to realize a useful oral composition capable of maintaining a good oral environment while using a fatty acid, it is possible to remove plaque firmly adhered to the tooth surface by exerting high cleaning ability. Moreover, it is desired that the composition can effectively suppress the adhesion of plaque to the tooth surface even after that.
However, although the composition described in Patent Document 1 may be able to exert the plaque removal effect to some extent, further improvement is required in order to exert the plaque adhesion suppression effect. On the other hand, even the compositions described in Patent Documents 2 to 4 have not been examined in terms of removing plaque and suppressing adhesion, and there is room for improvement.
 すなわち、本発明は、優れた洗浄能を発揮して歯面に堅固に付着した歯垢を除去するとことができるとともに、歯面に歯垢が付着するのをも有効に抑制することのできる液体口腔用組成物に関する。 That is, the present invention is capable of removing the plaque firmly adhered to the tooth surface by exerting an excellent cleaning ability, and also capable of effectively suppressing the adhesion of the plaque to the tooth surface. It relates to a composition for oral cavity.
 そこで本発明者は、上記課題を解決すべく鋭意検討を行った結果、特定の脂肪酸と特定の塩基とを併用しつつ、pHを特定の値に制御することにより、優れた洗浄能を発揮して歯面に付着した歯垢を除去するとともに、歯面への歯垢の付着を抑制する効果を有効に発揮することのできる液体口腔用組成物を見出した。 Therefore, the present inventor, as a result of earnest studies to solve the above problems, while using a specific fatty acid and a specific base in combination, by controlling the pH to a specific value, exhibits an excellent cleaning ability. The present inventors have found a liquid oral composition capable of effectively removing the plaque attached to the tooth surface and effectively suppressing the attachment of the plaque to the tooth surface.
 本発明の液体口腔用組成物によれば、口腔内に適用した直後は、優れた洗浄能を発揮して、歯面に堅固に付着した歯垢を除去することができるだけでなく、口腔内において次第に唾液で希釈されながら、歯面へ歯垢が付着するのを有効に抑制することができる。 According to the liquid composition for oral cavity of the present invention, immediately after being applied to the oral cavity, it exhibits excellent cleaning ability, and it is possible not only to remove the plaque firmly attached to the tooth surface but also in the oral cavity. It is possible to effectively suppress the adhesion of plaque to the tooth surface while being gradually diluted with saliva.
発明の詳細な説明Detailed Description of the Invention
 以下、本発明について詳細に説明する。
 本発明の液体口腔用組成物は、次の成分(A)及び(B):
 (A)少なくとも一部に不飽和脂肪酸を含む、炭素数10以上22以下の炭化水素基を有する脂肪酸
 (B)有機アミン、アルカリ金属水酸化物、炭酸塩、重炭酸塩、及びセスキ炭酸塩から選ばれる1種又は2種以上の塩基性化合物
を含有し、かつ25℃におけるpHが9.6以上11.0以下である。
Hereinafter, the present invention will be described in detail.
The liquid oral composition of the present invention comprises the following components (A) and (B):
(A) Fatty acid having a hydrocarbon group having 10 to 22 carbon atoms, which contains unsaturated fatty acid at least in part (B) From organic amine, alkali metal hydroxide, carbonate, bicarbonate, and sesquicarbonate It contains one or more selected basic compounds and has a pH at 25 ° C. of 9.6 or more and 11.0 or less.
 本発明の液体口腔用組成物は、高pH領域下で、成分(A)の脂肪酸と成分(B)の塩基性化合物とを併用してなることから、口腔内に適用した直後は、成分(A)が主となって速やかに歯垢に吸着して歯面から離脱させることにより、ミセル様の会合体を形成して歯面に固着した歯垢を効果的に除去することができる。そして、口腔内で次第に組成物が唾液により希釈されて低pH領域へと変遷するにつれて、成分(A)と成分(B)によりベシクル様の会合体が形成され、これが歯面を密に被覆して、歯面に歯垢が再び又は新たに付着するのを有効に抑制することができる。
 このように、本発明者は、あらかじめ組成物のpHを特定の高領域に制御した状態で成分(A)と成分(B)を共存させ、使用時の唾液による希釈にて組成物のpHが低領域へと変遷することにより、予想外にも歯垢除去効果と歯垢付着抑制効果との両立が可能になることを見出したものである。
Since the liquid composition for oral cavity of the present invention comprises a combination of the fatty acid of component (A) and the basic compound of component (B) in a high pH range, immediately after being applied to the oral cavity, the component ( By mainly adsorbing to the plaque and rapidly detaching it from the tooth surface, A) mainly forms a micelle-like aggregate and can effectively remove the plaque adhered to the tooth surface. Then, as the composition is gradually diluted with saliva in the oral cavity and transitions to a low pH range, component (A) and component (B) form a vesicle-like aggregate, which densely covers the tooth surface. Thus, it is possible to effectively prevent the plaque from adhering to the tooth surface again or newly.
As described above, the present inventor makes the component (A) and the component (B) coexist in a state where the pH of the composition is controlled in a specific high region in advance, and the pH of the composition is adjusted by dilution with saliva during use. It has been discovered that, by transitioning to a low region, it is possible to unexpectedly achieve both a plaque removal effect and a plaque adhesion suppression effect.
 本発明は、成分(A)として、少なくとも一部に不飽和脂肪酸を含む、炭素数10以上22以下の炭化水素基を有する脂肪酸を含有する。成分(A)の脂肪酸が有する炭化水素基の炭素数は、歯垢除去効果を高める観点から、10以上であって、好ましくは12以上であり、より好ましくは14以上であり、さらに好ましくは18以上であり、22以下であって、好ましくは20以下である。かかる炭化水素基としては、飽和炭化水素基、不飽和炭化水素基、直鎖炭化水素基、分岐鎖を有する炭化水素基が挙げられ、具体的には、例えば、カプリン酸、ラウリン酸、ミリスチン酸、ペンタデシル酸、パルミチン酸、パルミトレイン酸、ステアリン酸、イソステアリン酸、オレイン酸、リノール酸、リノレン酸、アラキドン酸及びベヘン酸等から選ばれる1種又は2種以上が挙げられる。 The present invention contains, as the component (A), a fatty acid having a hydrocarbon group having 10 to 22 carbon atoms, the unsaturated fatty acid being contained at least in part. The number of carbon atoms of the hydrocarbon group contained in the component (A) fatty acid is 10 or more, preferably 12 or more, more preferably 14 or more, and further preferably 18 from the viewpoint of enhancing the effect of removing plaque. It is above, is 22 or less, and is preferably 20 or less. Examples of such a hydrocarbon group include a saturated hydrocarbon group, an unsaturated hydrocarbon group, a linear hydrocarbon group, and a hydrocarbon group having a branched chain. Specific examples include capric acid, lauric acid, and myristic acid. , Pentadecylic acid, palmitic acid, palmitoleic acid, stearic acid, isostearic acid, oleic acid, linoleic acid, linolenic acid, arachidonic acid and behenic acid.
 また成分(A)は、少なくとも一部に不飽和炭化水素基を有する脂肪酸、すなわち不飽和脂肪酸を含む。かかる不飽和炭化水素基としては、例えば、パルミトレイン酸、オレイン酸、リノール酸及びリノレン酸等から選ばれる1種又は2種以上が挙げられる。なかでも、歯垢除去効果と歯垢付着抑制効果とを良好に両立させる観点から、パルミトレイン酸、オレイン酸及びリノール酸から選ばれる1種又は2種以上が好ましく、オレイン酸がより好ましい。 Further, the component (A) contains a fatty acid having an unsaturated hydrocarbon group at least in part, that is, an unsaturated fatty acid. Examples of such unsaturated hydrocarbon groups include one or more selected from palmitoleic acid, oleic acid, linoleic acid, linolenic acid, and the like. Among them, one or more selected from palmitoleic acid, oleic acid, and linoleic acid are preferable, and oleic acid is more preferable, from the viewpoint of well achieving both the effect of removing plaque and the effect of suppressing adhesion of plaque.
 不飽和脂肪酸の含有量は、歯垢除去効果と歯垢付着抑制効果とを良好に両立させる観点から、成分(A)中に、好ましくは15質量%以上であり、より好ましくは20質量%以上であり、さらに好ましくは25質量%以上であり、またさらに好ましくは30質量%以上であり、よりさらに好ましくは35質量%以上であり、よりさらに好ましくは50質量%以上であり、よりさらに好ましくは55質量%以上であり、よりさらに好ましくは75質量%以上であり、よりさらに好ましくは90質量%以上であり、よりさらに好ましくは95質量%以上である。 The content of the unsaturated fatty acid is preferably 15% by mass or more, more preferably 20% by mass or more in the component (A) from the viewpoint of achieving both the effect of removing plaque and the effect of suppressing adhesion of plaque. And more preferably 25 mass% or more, still more preferably 30 mass% or more, still more preferably 35 mass% or more, still more preferably 50 mass% or more, and even more preferably It is 55% by mass or more, more preferably 75% by mass or more, even more preferably 90% by mass or more, still more preferably 95% by mass or more.
 成分(A)の含有量は、口腔内での高pH領域下において優れた洗浄効果を発揮し、歯面に固着した歯垢を効果的に除去する観点から、本発明の液体口腔用組成物中に、好ましくは0.05質量%以上であり、より好ましくは0.1質量%以上であり、さらに好ましくは0.2質量%以上であり、またさらに好ましくは0.4質量%以上であり、よりさらに好ましくは0.5質量%以上である。また、成分(A)の含有量は、口腔内で組成物が唾液により希釈されて低pH領域へと変遷した際、後述する成分(B)とベシクル様の会合体を形成して、歯垢付着抑制効果を充分に発揮させる観点から、本発明の液体口腔用組成物中に、好ましくは5質量%以下であり、より好ましくは3質量%以下であり、さらに好ましくは1.5質量%以下であり、またさらに好ましくは1質量%以下である。そして、成分(A)の含有量は、本発明の液体口腔用組成物中に、好ましくは0.05~5質量%であり、より好ましくは0.1~3質量%であり、さらに好ましくは0.2~1.5質量%であり、またさらに好ましくは0.2~1質量%であり、よりさらに好ましくは0.4~1質量%であり、よりさらに好ましくは0.5~1質量%である。 The content of the component (A) exerts an excellent cleaning effect in a high pH region in the oral cavity, and from the viewpoint of effectively removing plaque adhered to the tooth surface, the liquid oral composition of the present invention In the above, it is preferably 0.05% by mass or more, more preferably 0.1% by mass or more, further preferably 0.2% by mass or more, and still more preferably 0.4% by mass or more. , And more preferably 0.5% by mass or more. In addition, the content of the component (A) is such that when the composition is diluted with saliva in the oral cavity and transitions to a low pH range, it forms a vesicle-like association with the component (B) described below to form plaque. From the viewpoint of sufficiently exhibiting the adhesion suppressing effect, in the liquid oral composition of the present invention, it is preferably 5% by mass or less, more preferably 3% by mass or less, and further preferably 1.5% by mass or less. And more preferably 1% by mass or less. The content of the component (A) in the liquid oral composition of the present invention is preferably 0.05 to 5% by mass, more preferably 0.1 to 3% by mass, and further preferably 0.2 to 1.5% by mass, more preferably 0.2 to 1% by mass, even more preferably 0.4 to 1% by mass, still more preferably 0.5 to 1% by mass. %.
 本発明は、成分(B)として、有機アミン、アルカリ金属水酸化物、炭酸塩、重炭酸塩、及びセスキ炭酸塩から選ばれる1種又は2種以上の塩基性化合物を含有する。かかる成分(B)を含有することにより、口腔内への適用後に唾液により希釈されるに伴い、ミセル様の会合体を形成していた成分(A)とベシクル様の会合体を形成して、歯垢付着抑制効果を発揮させることができる。 The present invention contains, as the component (B), one or more basic compounds selected from organic amines, alkali metal hydroxides, carbonates, bicarbonates, and sesquicarbonates. By containing such component (B), as it is diluted with saliva after application in the oral cavity, it forms a vesicle-like association with component (A) that had formed a micelle-like association, The effect of suppressing plaque adhesion can be exerted.
 有機アミンとしては、具体的には、例えば、アルギニン、リジン、及びヒスチジンから選ばれる1種又は2種以上の塩基性アミノ酸;モノエタノールアミン、ジエタノールアミン、トリエタノールアミン、モルホリン、トリイソプロパノールアミン、2-アミノ-2-メチル-1,3-プロパンジオール、及び2-アミノ-2-メチル-1-プロパノールから選ばれる1種又は2種以上のアルカノールアミン化合物が挙げられる。 Specific examples of the organic amine include one or more basic amino acids selected from arginine, lysine, and histidine; monoethanolamine, diethanolamine, triethanolamine, morpholine, triisopropanolamine, 2- Examples thereof include one or more alkanolamine compounds selected from amino-2-methyl-1,3-propanediol and 2-amino-2-methyl-1-propanol.
 アルカリ金属水酸化物としては、具体的には、例えば、水酸化ナトリウム、水酸化カリウム、水酸化カルシウム、及び水酸化リチウムから選ばれる1種又は2種以上が挙げられる。 Specific examples of the alkali metal hydroxide include one or more selected from sodium hydroxide, potassium hydroxide, calcium hydroxide, and lithium hydroxide.
 炭酸塩、重炭酸塩、及びセスキ炭酸塩としては、具体的には、例えば、炭酸ナトリウム、炭酸カリウム、炭酸カルシウム、重炭酸ナトリウム、重炭酸カリウム、及びセスキ炭酸ナトリウムから選ばれる1種又は2種以上が挙げられる。 Specific examples of the carbonate, bicarbonate, and sesquicarbonate include one or two selected from sodium carbonate, potassium carbonate, calcium carbonate, sodium bicarbonate, potassium bicarbonate, and sodium sesquicarbonate. The above is mentioned.
 なかでも成分(B)としては、口腔内で組成物が唾液により希釈されて高pH領域から低pH領域へと変遷した際、成分(A)とベシクル様の会合体を良好かつ迅速に形成する観点から、塩基性アミノ酸、及びアルカノールアミン化合物から選ばれる1種又は2種以上の塩基性化合物であるのが好ましく、アルギニン、又は2-アミノ-2-メチル-1-プロパノールがより好ましい。 Among them, as the component (B), when the composition is diluted with saliva in the oral cavity and transitions from the high pH range to the low pH range, the vesicle-like association with the component (A) is favorably and rapidly formed. From the viewpoint, one or more basic compounds selected from basic amino acids and alkanolamine compounds are preferable, and arginine or 2-amino-2-methyl-1-propanol is more preferable.
 成分(B)の含有量は、口腔内で組成物が唾液により希釈されて低pH領域へと変遷した際、成分(A)とベシクル様の会合体を形成して、歯垢付着抑制効果を充分に発揮させる観点から、本発明の液体口腔用組成物中に、好ましくは0.01質量%以上であり、より好ましくは0.1質量%以上であり、さらに好ましくは0.17質量%以上であり、またさらに好ましくは0.25質量%以上である。また、成分(B)の含有量は、口腔内での高pH領域下において発揮されるべき、主として成分(A)による優れた洗浄効果を確保する観点から、本発明の液体口腔用組成物中に、好ましくは3質量%以下であり、より好ましくは2質量%以下であり、さらに好ましくは1質量%以下であり、またさらに好ましくは0.8質量%以下である。そして、成分(B)の含有量は、本発明の液体口腔用組成物中に、好ましくは0.01~3質量%であり、より好ましくは0.01~2質量%であり、さらに好ましくは0.1~1質量%であり、よりさらに好ましくは0.17~0.8質量%であり、またさらに好ましくは0.25~0.8質量%である。 The content of the component (B) is such that when the composition is diluted with saliva in the oral cavity and transitions to a low pH range, it forms a vesicle-like association with the component (A) to suppress the plaque adhesion. From the viewpoint of sufficiently exhibiting, in the liquid oral cavity composition of the present invention, preferably 0.01% by mass or more, more preferably 0.1% by mass or more, and further preferably 0.17% by mass or more. And more preferably 0.25 mass% or more. In addition, the content of the component (B) in the liquid oral composition of the present invention is to be exhibited in a high pH region in the oral cavity, mainly from the viewpoint of ensuring an excellent cleaning effect by the component (A). In addition, it is preferably 3% by mass or less, more preferably 2% by mass or less, further preferably 1% by mass or less, and further preferably 0.8% by mass or less. The content of the component (B) in the liquid oral composition of the present invention is preferably 0.01 to 3% by mass, more preferably 0.01 to 2% by mass, and further preferably The amount is 0.1 to 1% by mass, more preferably 0.17 to 0.8% by mass, and still more preferably 0.25 to 0.8% by mass.
 成分(B)と成分(A)のモル比((B)/(A))は、歯垢除去効果と歯垢付着抑制効果とを良好に両立させる観点から、好ましくは0.5~40であり、より好ましくは0.9~30であり、さらに好ましくは0.95~30であり、またさらに好ましくは0.95~20であり、よりさらに好ましくは1~20であり、よりさらに好ましくは1.5~20であり、よりさらに好ましくは1.5~15であり、よりさらに好ましくは2~10である。 The molar ratio ((B) / (A)) of the component (B) and the component (A) is preferably 0.5 to 40 from the viewpoint of achieving both a plaque removing effect and a plaque adhesion suppressing effect. Yes, more preferably 0.9 to 30, still more preferably 0.95 to 30, still more preferably 0.95 to 20, even more preferably 1 to 20, and even more preferably It is 1.5 to 20, more preferably 1.5 to 15, and even more preferably 2 to 10.
 本発明の液体口腔用組成物は、良好な保形性を保持しつつ、各成分を良好に分散又は溶解させて口腔内で良好に拡散させることができる観点から、水(C)を含有するのが好ましい。本発明における成分(C)の水とは、液体口腔用組成物に配合した精製水等だけでなく、例えば処方する際に用いる70%ソルビトール液(水溶液)のように、配合した各成分に含まれる水分をも含む、液体口腔用組成物中に含まれる全水分を意味する。かかる水(C)の含有量は、本発明の液体口腔用組成物中に、好ましくは50質量%以上であり、より好ましくは70質量%以上であり、さらに好ましくは80質量%以上であり、好ましくは99質量%以下であり、より好ましくは97質量%以下であり、さらに好ましくは95質量%以下である。 The liquid composition for oral cavity of the present invention contains water (C) from the viewpoint that each component can be well dispersed or dissolved and well diffused in the oral cavity while maintaining good shape retention. Is preferred. The water of the component (C) in the present invention includes not only purified water and the like mixed in the composition for liquid oral cavity but also each of the mixed components such as 70% sorbitol liquid (aqueous solution) used in the formulation. The total moisture contained in the liquid oral composition, including the moisture contained therein. The content of such water (C) in the liquid oral composition of the present invention is preferably 50% by mass or more, more preferably 70% by mass or more, further preferably 80% by mass or more, It is preferably 99% by mass or less, more preferably 97% by mass or less, and further preferably 95% by mass or less.
 本発明の液体口腔用組成物は、口腔内で組成物が唾液により希釈されて高pH領域から低pH領域へと変遷した際、成分(A)と成分(B)とがベシクル様の会合体を形成して歯垢付着抑制効果を発揮するのを阻害しない観点から、遊離の2価金属イオンの含有を制限するのが好ましい。かかる遊離の2価金属イオンとしては、具体的には、カルシウムイオン、マグネシウムイオンが挙げられる。かかる遊離の2価金属イオンの含有量は、本発明の液体口腔用組成物中に、好ましくは0.5質量%以下であり、より好ましくは0.1質量%以下であり、さらに好ましくは0.05質量%以下であり、或いは本発明の液体口腔用組成物は、遊離の2価金属イオンを含有しないのが好ましい。
 なお、かかる遊離の2価金属イオンの含有量は、ICP発光分析法(ICP発光分析装置:Perkin Elmer社製 Optima 5300DV)により、遊離の2価金属イオンの合計量として測定される値である。
The liquid oral composition of the present invention is a vesicle-like aggregate of the component (A) and the component (B) when the composition is diluted with saliva in the oral cavity and transitions from a high pH range to a low pH range. It is preferable to limit the content of free divalent metal ions from the viewpoint of not inhibiting the formation of the plaque and the effect of suppressing the adhesion of plaque. Specific examples of the free divalent metal ion include calcium ion and magnesium ion. The content of such free divalent metal ions in the liquid oral composition of the present invention is preferably 0.5% by mass or less, more preferably 0.1% by mass or less, and further preferably 0%. It is preferably 0.05% by mass or less, or the liquid composition for oral cavity of the present invention does not contain a free divalent metal ion.
The content of the free divalent metal ion is a value measured as the total amount of the free divalent metal ion by an ICP emission analysis method (ICP emission analysis device: Optima 5300 DV manufactured by Perkin Elmer).
 本発明の液体口腔用組成物は、本発明の効果を阻害しない範囲で、上記成分のほか、例えば、アルキル硫酸エステル塩等のアニオン界面活性剤;ポリオキシエチレン硬化ヒマシ油やショ糖脂肪酸エステル等のノニオン界面活性剤;アルギン酸ナトリウム、カルボキシメチルセルロース又はその塩、ヒドロキシエチルセルロース、カラギーナン、キサンタンガム等の粘結剤;イソプロピルメチルフェノールや塩化セチルピリジニウム等の殺菌剤;ソルビトール、キシリトール、エリスリトール等の糖アルコール;グリセリン等の湿潤剤;保存剤;フッ化物やその他の薬効剤;顔料;色素;香料等を適宜含有させることができる。 The liquid oral composition of the present invention, in addition to the above components, for example, anionic surfactants such as alkyl sulfate ester salts; polyoxyethylene hydrogenated castor oil, sucrose fatty acid ester, etc., within the range that does not impair the effects of the present invention. Nonionic surfactants; binding agents such as sodium alginate, carboxymethyl cellulose or salts thereof, hydroxyethyl cellulose, carrageenan, xanthan gum; bactericides such as isopropylmethylphenol and cetylpyridinium chloride; sugar alcohols such as sorbitol, xylitol, erythritol; glycerin A wetting agent such as; a preservative; a fluoride or other medicinal effect agent; a pigment; a dye;
 本発明の液体口腔用組成物の25℃におけるpHは、口腔内のpH環境を高pH領域下として優れた洗浄効果を発揮させる観点から、9.6以上であって、好ましくは9.8以上であり、さらに好ましくは10以上であり、またさらに好ましくは10.2以上である。また、本発明の液体口腔用組成物の25℃におけるpHは、口腔内で組成物が唾液により希釈された際、低pH領域へと変遷して、優れた歯垢付着抑制効果を発揮させる観点から、11以下であって、好ましくは10.8以下であり、さらに好ましくは10.6以下であり、またさらに好ましくは10.4以下である。そして、本発明の液体口腔用組成物の25℃におけるpHは、9.6以上11以下であって、好ましくは9.8~10.8であり、より好ましくは10~10.6であり、さらに好ましくは10.2~10.4である。 The pH of the liquid oral composition of the present invention at 25 ° C. is 9.6 or more, preferably 9.8 or more, from the viewpoint of exhibiting an excellent cleaning effect by setting the pH environment in the oral cavity in a high pH range. And more preferably 10 or more, and further preferably 10.2 or more. In addition, the pH of the liquid oral composition of the present invention at 25 ° C. changes to a low pH range when the composition is diluted with saliva in the oral cavity, and exhibits an excellent effect of suppressing plaque adhesion. Therefore, it is 11 or less, preferably 10.8 or less, more preferably 10.6 or less, and further preferably 10.4 or less. The pH of the liquid oral composition of the present invention at 25 ° C. is 9.6 or more and 11 or less, preferably 9.8 to 10.8, more preferably 10 to 10.6, More preferably, it is 10.2 to 10.4.
 なお、本発明の液体口腔用組成物のpHを上記範囲に調整する上で、上記成分以外のクエン酸、リンゴ酸、乳酸、酒石酸、コハク酸等の有機酸又はこれらの塩から選ばれる1種又は2種以上をpH調整剤として用いてもよい。 In adjusting the pH of the liquid oral composition of the present invention to the above range, one kind selected from organic acids such as citric acid, malic acid, lactic acid, tartaric acid and succinic acid other than the above components or salts thereof. Alternatively, two or more kinds may be used as a pH adjusting agent.
 本発明の液体口腔用組成物は、該組成物を口腔内に滞留させ、かつ口腔内において唾液で希釈させることにより、歯面に付着した歯垢を除去しながら又は除去した後において、歯面への歯垢の付着を抑制する方法に用いることができる。 The liquid oral composition of the present invention retains the composition in the oral cavity and is diluted with saliva in the oral cavity to remove the plaque adhering to the tooth surface while or after removing the dental plaque. It can be used for a method of suppressing the adhesion of plaque to the skin.
 このように、本発明の液体口腔用組成物であれば、口腔内バイオフィルムの付着抑制のためだけでなく、口腔内バイオフィルムの除去のためにも用いることができ、双方の効果を有効に発揮することができる。 Thus, if the liquid oral composition of the present invention, not only for suppressing the adhesion of the oral biofilm, it can be used for the removal of the oral biofilm, effectively both effects Can be demonstrated.
 上述した実施形態に関し、本発明はさらに以下の液体口腔用組成物を開示する。
 [1]次の成分(A)及び(B):
 (A)少なくとも一部に不飽和脂肪酸を含む、炭素数10以上22以下の炭化水素基を有する脂肪酸
 (B)有機アミン、アルカリ金属水酸化物、炭酸塩、重炭酸塩、及びセスキ炭酸塩から選ばれる1種又は2種以上の塩基性化合物
を含有し、かつ25℃におけるpHが9.6以上11以下である液体口腔用組成物。
 [2]成分(A)の脂肪酸が有する炭化水素基の炭素数が、好ましくは12以上であり、より好ましくは14以上であり、さらに好ましくは18以上であり、好ましくは20以下であり、或いは成分(A)の脂肪酸が有する炭化水素基が、好ましくはカプリン酸、ラウリン酸、ミリスチン酸、ペンタデシル酸、パルミチン酸、パルミトレイン酸、ステアリン酸、イソステアリン酸、オレイン酸、リノール酸、リノレン酸、アラキドン酸及びベヘン酸等から選ばれる1種又は2種以上である上記[1]の液体口腔用組成物。
 [3]成分(A)が含む不飽和脂肪酸の不飽和炭化水素基が、好ましくはパルミトレイン酸、オレイン酸、リノール酸及びリノレン酸等から選ばれる1種又は2種以上であり、より好ましくはパルミトレイン酸、オレイン酸及びリノール酸から選ばれる1種又は2種以上であり、さらに好ましくはオレイン酸である上記[1]又は[2]の液体口腔用組成物。
 [4]不飽和脂肪酸の含有量が、成分(A)中に、好ましくは15質量%以上であり、好ましくは20質量%以上であり、よりさらに好ましくは25質量%以上であり、より好ましくは30質量%以上であり、よりさらに好ましくは35質量%以上であり、さらに好ましくは50質量%以上であり、よりさらに好ましくは55質量%以上であり、よりさらに好ましくは75質量%以上であり、よりさらに好ましくは90質量%以上であり、好ましくは95質量%以上である上記[1]~[3]いずれか1の液体口腔用組成物。
 [5]成分(A)の含有量が、好ましくは0.05質量%以上であり、より好ましくは0.1質量%以上であり、さらに好ましくは0.2質量%以上であり、さらに好ましくは0.4質量%以上であり、さらに好ましくは0.5質量%以上であり、好ましくは5質量%以下であり、より好ましくは3質量%以下であり、より好ましくは1.5質量%以下であり、さらに好ましくは1質量%以下である上記[1]~[4]いずれか1の液体口腔用組成物。
With respect to the embodiments described above, the present invention further discloses the following liquid oral compositions.
[1] The following components (A) and (B):
(A) Fatty acid having a hydrocarbon group having 10 to 22 carbon atoms, which contains unsaturated fatty acid at least in part (B) From organic amine, alkali metal hydroxide, carbonate, bicarbonate, and sesquicarbonate A composition for liquid oral cavity containing one or more selected basic compounds and having a pH at 25 ° C of 9.6 or more and 11 or less.
[2] The carbon number of the hydrocarbon group contained in the fatty acid of the component (A) is preferably 12 or more, more preferably 14 or more, still more preferably 18 or more, preferably 20 or less, or The hydrocarbon group contained in the fatty acid of component (A) is preferably capric acid, lauric acid, myristic acid, pentadecyl acid, palmitic acid, palmitoleic acid, stearic acid, isostearic acid, oleic acid, linoleic acid, linolenic acid, arachidonic acid. And the liquid oral composition according to the above [1], which is one or more selected from behenic acid and the like.
[3] The unsaturated hydrocarbon group of the unsaturated fatty acid contained in the component (A) is preferably one or more selected from palmitoleic acid, oleic acid, linoleic acid, and linolenic acid, and more preferably palmitoleic. The liquid oral composition according to the above [1] or [2], which is one or more selected from acids, oleic acid and linoleic acid, and more preferably oleic acid.
[4] The content of the unsaturated fatty acid in the component (A) is preferably 15% by mass or more, preferably 20% by mass or more, more preferably 25% by mass or more, and more preferably 30 mass% or more, more preferably 35 mass% or more, further preferably 50 mass% or more, even more preferably 55 mass% or more, even more preferably 75 mass% or more, The composition for liquid oral cavity according to any one of [1] to [3] above, which is more preferably 90% by mass or more, and preferably 95% by mass or more.
[5] The content of the component (A) is preferably 0.05% by mass or more, more preferably 0.1% by mass or more, further preferably 0.2% by mass or more, and further preferably 0.4 mass% or more, more preferably 0.5 mass% or more, preferably 5 mass% or less, more preferably 3 mass% or less, and more preferably 1.5 mass% or less. The composition for liquid oral cavity according to any one of [1] to [4] above, which is 1% by mass or less.
 [6]成分(B)が、好ましくは塩基性アミノ酸、及びアルカノールアミン化合物から選ばれる1種又は2種以上であり、より好ましくはアルギニン、又は2-アミノ-2-メチル-1-プロパノールである上記[1]~[5]いずれか1の液体口腔用組成物。
 [7]成分(B)の含有量が、好ましくは0.01質量%以上であり、より好ましくは0.1質量%以上であり、さらに好ましくは0.17質量%以上であり、さらに好ましくは0.25質量%以上であり、好ましくは3質量%以下であり、より好ましくは2質量%以下であり、さらに好ましくは1質量%以下であり、またさらに好ましくは0.8質量%以下である上記[1]~[6]いずれか1の液体口腔用組成物。
 [8]成分(B)と成分(A)のモル比((B)/(A))が、好ましくは0.5~40であり、より好ましくは0.9~30であり、さらに好ましくは0.95~30であり、またさらに好ましくは0.95~20であり、さらに好ましくは1~20であり、さらに好ましくは1.5~20であり、さらに好ましくは1.5~15であり、またさらに好ましくは2~10である上記[1]~[7]いずれか1の液体口腔用組成物。
[6] The component (B) is preferably one or more selected from basic amino acids and alkanolamine compounds, more preferably arginine or 2-amino-2-methyl-1-propanol. The liquid composition for oral cavity according to any one of [1] to [5] above.
[7] The content of the component (B) is preferably 0.01% by mass or more, more preferably 0.1% by mass or more, further preferably 0.17% by mass or more, and further preferably 0.25% by mass or more, preferably 3% by mass or less, more preferably 2% by mass or less, further preferably 1% by mass or less, and further preferably 0.8% by mass or less. The liquid composition for oral cavity according to any one of [1] to [6] above.
[8] The molar ratio ((B) / (A)) of the component (B) and the component (A) is preferably 0.5 to 40, more preferably 0.9 to 30, and further preferably. 0.95 to 30, more preferably 0.95 to 20, further preferably 1 to 20, further preferably 1.5 to 20, and further preferably 1.5 to 15. The liquid oral composition according to any one of the above [1] to [7], which is more preferably 2 to 10.
 [9]25℃におけるpHが、好ましくは9.8以上であり、さらに好ましくは10以上であり、またさらに好ましくは10.2以上であり、好ましくは10.8以下であり、さらに好ましくは10.6以下であり、またさらに好ましくは10.4以下である上記[1]~[8]いずれか1の液体口腔用組成物。
 [10]遊離の2価金属イオンの含有量が、好ましくは0.5質量%以下であり、より好ましくは0.1質量%以下であり、さらに好ましくは0.05質量%以下であり、或いは好ましくは遊離の2価金属イオンを含有しない上記[1]~[9]いずれか1の液体口腔用組成物。
 [11]遊離の2価金属イオンが、カルシウムイオン又はマグネシウムイオンである上記[1]~[10]いずれか1の液体口腔用組成物。
 [12]成分(C)の含有量が、好ましくは50質量%以上であり、より好ましくは70質量%以上であり、さらに好ましくは80質量%以上であり、好ましくは99質量%以下であり、より好ましくは97質量%以下であり、さらに好ましくは95質量%以下である上記[1]~[11]いずれか1の液体口腔用組成物。
[9] The pH at 25 ° C. is preferably 9.8 or higher, more preferably 10 or higher, still more preferably 10.2 or higher, preferably 10.8 or lower, more preferably 10 or higher. The liquid oral composition according to any one of the above [1] to [8], which is 0.6 or less, and more preferably 10.4 or less.
[10] The content of the free divalent metal ion is preferably 0.5% by mass or less, more preferably 0.1% by mass or less, further preferably 0.05% by mass or less, or The composition for liquid oral cavity according to any one of the above [1] to [9], which preferably contains no free divalent metal ion.
[11] The liquid oral composition according to any one of the above [1] to [10], wherein the free divalent metal ion is a calcium ion or a magnesium ion.
[12] The content of the component (C) is preferably 50% by mass or more, more preferably 70% by mass or more, further preferably 80% by mass or more, preferably 99% by mass or less, The liquid oral composition according to any one of the above [1] to [11], which is more preferably 97% by mass or less, and further preferably 95% by mass or less.
 [13]口腔内バイオフィルムの付着抑制のためと口腔内バイオフィルムの除去のための組成物である上記[1]~[12]いずれか1の液体口腔用組成物。
 [14]上記[1]~[12]いずれか1の液体口腔用組成物を口腔内において次第に唾液により希釈させながら適用する、口腔内バイオフィルムの付着を抑制しつつ口腔内バイオフィルムを除去する方法。
 [15]口腔内バイオフィルムの付着を抑制しつつ口腔内バイオフィルムを除去するための、上記[1]~[12]いずれか1の液体口腔用組成物の使用。
[13] The liquid oral composition according to any one of the above [1] to [12], which is a composition for suppressing adhesion of oral biofilm and for removing oral biofilm.
[14] Applying the liquid oral composition according to any one of [1] to [12] while gradually diluting it in the oral cavity with saliva, and removing the oral biofilm while suppressing the adhesion of the oral biofilm. Method.
[15] Use of the liquid oral composition according to any one of the above [1] to [12], for removing the oral biofilm while suppressing the adhesion of the oral biofilm.
 以下、本発明について、実施例に基づき具体的に説明する。なお、表中に特に示さない限り、各成分の含有量は質量%を示す。 Hereinafter, the present invention will be specifically described based on Examples. Unless otherwise specified in the table, the content of each component is% by mass.
 [実施例1~15、比較例1~3]
 表1に示す処方にしたがって、液体口腔用組成物を調製した。得られた各液体口腔用組成物は遊離の2価金属イオンの含有量が0.05質量%以下であった。得られた各液体口腔用組成物を用い、下記方法にしたがって各評価を行った。
 結果を表1に示す。
[Examples 1 to 15 and Comparative Examples 1 to 3]
A liquid oral composition was prepared according to the formulation shown in Table 1. Each of the obtained liquid oral compositions had a content of free divalent metal ions of 0.05% by mass or less. Using each of the obtained liquid oral compositions, each evaluation was performed according to the following methods.
The results are shown in Table 1.
 [歯垢除去率の評価]
 1)刺激唾液の採取
 20~30代の健常男性を対象に、デントバフ ストリップ(オーラルケア社製)に含まれているガムペレットを噛ませ、その都度口の中に溜まった唾液をファルコンチューブに吐き出させて、かかるファルコンチューブに唾液を採取した。なお、唾液中の細菌には個人差があるため、1名の健常男性の唾液により、全ての実施例と比較例について評価を行った。
[Evaluation of plaque removal rate]
1) Collection of stimulated saliva Targeting healthy men in their twenties to thirties, chew the gum pellets contained in Dentbuff Strip (made by Oral Care Co., Ltd.) and spit saliva accumulated in the mouth into the falcon tube each time. Then, saliva was collected in the Falcon tube. Since there are individual differences in the bacteria in saliva, the saliva of one healthy man was used to evaluate all the examples and comparative examples.
 2)歯垢モデルの作製
 ファルコンチューブに採取した唾液を、3000rpm/25℃/10minにて遠心分離した(遠心分離機の装置名:冷却遠心分離機CF15RN、HITACHI社製)。分離された上澄み唾液を用い、スクロースを5質量%溶液となるように添加した後、撹拌機器(voltex、日本ジェネティクス社製)を用いて撹拌し、歯垢モデル試験液を調製した。
 次にHAp基板(コスモ・バイオ社製、1cm角)の片面を40μm、12μm、3μmの研磨紙を用いて鏡面研磨した後、1N HClに1分間浸漬して酸脱灰処理を施した。処理後のHAp板をイオン交換水で洗浄して乾燥し、24穴プレートに入れ、上記調製した歯垢モデル試験液を1mLずつ添加した。その後、HAp基板をCO2パックとともにプラスチックケースに格納して嫌気条件下とし、37℃で48時間培養した。
2) Preparation of dental plaque model Saliva collected in a falcon tube was centrifuged at 3000 rpm / 25 ° C / 10min (centrifuge device name: cooling centrifuge CF15RN, manufactured by HITACHI). Using the separated supernatant saliva, sucrose was added so as to be a 5 mass% solution, and then stirred using a stirring device (voltex, manufactured by Nippon Genetics Co., Ltd.) to prepare a plaque model test solution.
Next, one surface of the HAp substrate (manufactured by Cosmo Bio Co., Ltd., 1 cm square) was mirror-polished using polishing paper of 40 μm, 12 μm, and 3 μm, and then immersed in 1N HCl for 1 minute for acid deashing treatment. The HAp plate after the treatment was washed with ion-exchanged water, dried, put in a 24-well plate, and 1 mL of the prepared plaque model test solution was added thereto. Then, the HAp substrate was stored in a plastic case together with a CO 2 pack under anaerobic conditions and incubated at 37 ° C. for 48 hours.
 3)歯垢除去効果の評価
 減圧ポンプを用い、プレート中の唾液を吸い取り、イオン交換水1mLを添加して5分間振盪した。次にポンプを用いて水を吸い取り、実施例及び比較例で得られた各組成物1mLに人口唾液0.13mLを添加した溶液を別途24穴プレートに調製した。次いで、調製した溶液にモデル歯垢を形成したHAp基板を浸漬し、1分間振盪した。振盪は、振盪機(BioShake iQ(ワケンビーテック社製))を用い、室温(25℃)、500rpmの条件で行った。
 その後、各組成物を吸い取り、イオン交換水1mLを添加して5分間振盪し、これを2回繰り返した。次いで、水を吸い取り、0.1質量%クリスタルバイオレット(CV)溶液を750μL添加して15分間振盪した。
 さらにポンプでCV染色液を吸い取り、イオン交換水1mLを添加して5分間振盪し、これを2回繰り返した。次いで、水をポンプで吸い取り、エタノール500μLを添加してピペッティングした後、抽出液をイオン交換水で10倍希釈し、マイクロプレートレコーダー(TECAN社製 波長可変型吸光マイクロプレートリーダー サンライズレインボーサーモ)で吸光度OD595nmを測定した。
 また、上記得られた組成物を用いることなく、イオン交換水で洗浄したのみの吸光度OD595nm(初期値)を基準とし、下記式にしたがって歯垢除去率(%)を算出した。
 なお、得られた歯垢除去率の値が大きいほど、歯垢除去効果が高いことを意味する。
  歯垢除去率(%)=100-{上記得られた組成物を用いた際のOD595nm/イオン交換水で洗浄したのみのOD595nm}×100
3) Evaluation of plaque removal effect Using a vacuum pump, saliva in the plate was absorbed, 1 mL of ion-exchanged water was added, and the mixture was shaken for 5 minutes. Next, water was absorbed using a pump, and 0.13 mL of artificial saliva was added to 1 mL of each composition obtained in Examples and Comparative Examples to separately prepare a 24-well plate. Then, the HAp substrate on which the model plaque was formed was immersed in the prepared solution and shaken for 1 minute. Shaking was performed using a shaker (BioShake iQ (manufactured by Waken Betech Co.)) at room temperature (25 ° C.) and 500 rpm.
Then, each composition was absorbed, 1 mL of ion-exchanged water was added, and the mixture was shaken for 5 minutes, and this was repeated twice. Next, water was absorbed, 750 μL of a 0.1 mass% crystal violet (CV) solution was added, and the mixture was shaken for 15 minutes.
Further, the CV staining solution was sucked with a pump, 1 mL of ion-exchanged water was added, and the mixture was shaken for 5 minutes, and this was repeated twice. Then, suck up the water with a pump, add 500 μL of ethanol and pipette, dilute the extract 10 times with ion-exchanged water, and use a microplate recorder (TECAN wavelength tunable absorption microplate reader Sunrise Rainbow Thermo). Absorbance OD 595 nm was measured.
Further, without using the composition obtained above, the plaque removal rate (%) was calculated according to the following formula, using the absorbance OD 595 nm (initial value) just washed with ion-exchanged water as a reference.
The larger the obtained plaque removal rate value, the higher the plaque removal effect.
Plaque removal ratio (%) = 100- × 100 { OD 595nm only washed with OD 595 nm / ion-exchanged water at the time of using the resulting composition}
 [歯垢形成抑制の評価]
 1)組成物による処理
 HAp基板(コスモ・バイオ社製、1cm角)の片面を40μm、12μm、3μmの研磨紙を用いて鏡面研磨した後、1N HClに1分間浸漬して酸脱灰処理を施した。処理後のHAp板をイオン交換水で洗浄して乾燥し、24穴プレートに入れ、実施例及び比較例で得られた各組成物1mL、及び人口唾液0.13mLを添加して5分間振盪した。振盪は、振盪機(BioShake iQ(ワケンビーテック社製))を用い、室温(25℃)、500rpmの条件で行った。その後、各組成物を吸い取り、イオン交換水1mLを添加して5分間振盪した後、水を吸い取り処理基板とした。
[Evaluation of plaque formation inhibition]
1) Treatment with the composition One side of the HAp substrate (1 cm square manufactured by Cosmo Bio Co., Ltd.) was mirror-polished using 40 μm, 12 μm, 3 μm polishing paper, and then acid decalcified by immersion in 1N HCl for 1 minute. gave. The HAp plate after the treatment was washed with ion-exchanged water, dried, put in a 24-well plate, 1 mL of each composition obtained in Examples and Comparative Examples, and 0.13 mL of artificial saliva were added, and shaken for 5 minutes. . Shaking was performed using a shaker (BioShake iQ (manufactured by Waken Betech Co.)) at room temperature (25 ° C.) and 500 rpm. Thereafter, each composition was absorbed, 1 mL of ion-exchanged water was added, and the mixture was shaken for 5 minutes, and then water was absorbed to obtain a treated substrate.
 2)刺激唾液の採取
 20~30代の健常男性を対象に、デントバフ ストリップ(オーラルケア社製)に含まれているガムペレットを噛ませ、その都度口の中に溜まった唾液をファルコンチューブに吐き出させて、かかるファルコンチューブに唾液を採取した。なお、唾液中の細菌には個人差があるため、1名の健常男性の唾液により、全ての実施例と比較例について歯垢形成抑制試験を行った。
2) Collection of stimulated saliva Targeting healthy men in their 20s to 30s, chew the gum pellets contained in Dent Buff Strip (made by Oral Care Co., Ltd.) and spit saliva accumulated in the mouth into a falcon tube each time. Then, saliva was collected in the Falcon tube. Since there are individual differences in the bacteria in saliva, a plaque formation inhibition test was carried out for all Examples and Comparative Examples using saliva of one healthy male.
 3)モデル歯垢の形成
 ファルコンチューブに採取した唾液を、冷却遠心分離機(CF15RN、HITACHI社製)を用いて3000rpm/25℃/10minにて遠心分離した。分離された上澄み唾液を用い、スクロースを5質量%溶液となるように添加した後、撹拌機器(voltex、日本ジェネティクス社製)を用いて撹拌し、歯垢モデル試験液を調製した。
 次に、1)にて処理を施したHAp基板に上記調製した歯垢モデル試験液を1mLずつ添加した後、これをCO2パックとともにプラスチックケースに格納して嫌気条件下とし、37℃で48時間培養した。
3) Formation of model plaque The saliva collected in a falcon tube was centrifuged at 3000 rpm / 25 ° C / 10min using a cooling centrifuge (CF15RN, manufactured by HITACHI). Using the separated supernatant saliva, sucrose was added so as to be a 5 mass% solution, and then stirred using a stirring device (voltex, manufactured by Nippon Genetics Co., Ltd.) to prepare a plaque model test solution.
Next, 1 mL each of the above-prepared dental plaque model test solution was added to the HAp substrate treated in 1), and this was stored in a plastic case together with a CO 2 pack under anaerobic conditions at 37 ° C. for 48 hours. Incubated for hours.
 4)歯垢形成抑制効果の評価
 減圧ポンプを用い、プレート中の唾液を吸い取り、イオン交換水1mLを添加して5分間1回振盪した。次にポンプを用いて水を吸い取り、0.1質量%クリスタルバイオレット(CV)溶液を750μL添加して15分間振盪した。
 さらにポンプでCV染色液を吸い取り、イオン交換水1mLを添加して5分間振盪し、これを2回繰り返した。次いで、水をポンプで吸い取り、エタノール500μLを添加してピペッティングした後、抽出液をイオン交換水で10倍希釈し、マイクロプレートレコーダー(TECAN社製 波長可変型吸光マイクロプレートリーダー サンライズレインボーサーモ)で吸光度OD595nmを測定した。
 また、上記得られた組成物を用いることなく、イオン交換水で洗浄したのみの吸光度OD595nm(初期値)を基準とし、下記式にしたがって歯垢形成抑制率(%)を算出した。
 なお、得られた歯垢形成抑制率の値が大きいほど、歯垢形成抑制効果が高いことを意味する。
 歯垢形成抑制率(%)=100-{上記得られた組成物にて処理した基板のOD595nm/未処理基板のOD595nm}×100
4) Evaluation of Plaque Formation Inhibitory Effect Using a vacuum pump, saliva in the plate was absorbed, 1 mL of ion-exchanged water was added, and the mixture was shaken once for 5 minutes. Next, water was absorbed using a pump, 750 μL of a 0.1 mass% crystal violet (CV) solution was added, and the mixture was shaken for 15 minutes.
Further, the CV staining solution was sucked with a pump, 1 mL of ion-exchanged water was added, and the mixture was shaken for 5 minutes, and this was repeated twice. Then, suck up the water with a pump, add 500 μL of ethanol and pipette, dilute the extract 10 times with ion-exchanged water, and use a microplate recorder (TECAN wavelength tunable absorption microplate reader Sunrise Rainbow Thermo). Absorbance OD 595 nm was measured.
Further, without using the composition obtained above, the plaque formation inhibition rate (%) was calculated according to the following formula, using the absorbance OD 595 nm (initial value) just washed with ion-exchanged water as a reference.
It should be noted that the larger the obtained plaque formation inhibiting rate, the higher the plaque formation inhibiting effect.
Plaque formation inhibition rate (%) = 100- × 100 { OD 595nm of OD 595 nm / unprocessed substrate board treated in the above obtained composition}
Figure JPOXMLDOC01-appb-T000001
Figure JPOXMLDOC01-appb-T000001

Claims (9)

  1.  次の成分(A)及び(B):
     (A)少なくとも一部に不飽和脂肪酸を含む、炭素数10以上22以下の炭化水素基を有する脂肪酸
     (B)有機アミン、アルカリ金属水酸化物、炭酸塩、重炭酸塩、及びセスキ炭酸塩から選ばれる1種又は2種以上の塩基性化合物
    を含有し、かつ25℃におけるpHが9.6以上11以下である液体口腔用組成物。
    The following components (A) and (B):
    (A) Fatty acid having a hydrocarbon group having 10 to 22 carbon atoms, which contains unsaturated fatty acid at least in part (B) From organic amine, alkali metal hydroxide, carbonate, bicarbonate, and sesquicarbonate A liquid composition for oral cavity containing one or more selected basic compounds and having a pH at 25 ° C of 9.6 or more and 11 or less.
  2.  成分(A)が有する炭化水素基の炭素数が、18以上22以下である請求項1に記載の液体口腔用組成物。 The composition for liquid oral cavity according to claim 1, wherein the hydrocarbon group contained in the component (A) has 18 or more and 22 or less carbon atoms.
  3.  不飽和脂肪酸の含有量が、成分(A)中に15質量%以上である請求項1又は2に記載の液体口腔用組成物。 The liquid oral composition according to claim 1 or 2, wherein the content of the unsaturated fatty acid is 15% by mass or more in the component (A).
  4.  成分(A)に含まれる不飽和脂肪酸が、パルミトレイン酸、オレイン酸及びリノール酸から選ばれる1種又は2種以上である請求項1~3のいずれか1項に記載の液体口腔用組成物。 The liquid oral composition according to any one of claims 1 to 3, wherein the unsaturated fatty acid contained in the component (A) is one or more selected from palmitoleic acid, oleic acid and linoleic acid.
  5.  水(C)の含有量が、50質量%以上である請求項1~4のいずれか1項に記載の液体口腔用組成物。 The liquid oral composition according to any one of claims 1 to 4, wherein the content of water (C) is 50% by mass or more.
  6.  遊離の2価金属イオンの含有量が、0.5質量%以下である請求項1~5のいずれか1項に記載の液体口腔用組成物。 The liquid composition for oral cavity according to any one of claims 1 to 5, wherein the content of free divalent metal ions is 0.5% by mass or less.
  7.  成分(B)が、塩基性アミノ酸、及びアルカノールアミン化合物から選ばれる1種又は2種以上の塩基性化合物である請求項1~6のいずれか1項に記載の液体口腔用組成物。 The liquid oral composition according to any one of claims 1 to 6, wherein the component (B) is one or more basic compounds selected from basic amino acids and alkanolamine compounds.
  8.  口腔内バイオフィルムの付着抑制のためと口腔内バイオフィルムの除去のための組成物である請求項1~7のいずれか1項に記載の液体口腔用組成物。 The liquid composition for oral cavity according to any one of claims 1 to 7, which is a composition for suppressing adhesion of oral biofilm and for removing oral biofilm.
  9.  請求項1~8のいずれか1項に記載の液体口腔用組成物を口腔内に滞留させ、かつ口腔内において唾液で希釈させる、歯面に付着した歯垢を除去しながら又は除去した後における歯面への歯垢の付着を抑制する方法。 The liquid oral composition according to any one of claims 1 to 8 is retained in the oral cavity and diluted with saliva in the oral cavity, while removing plaque adhering to the tooth surface or after the removal. A method of suppressing the adhesion of plaque to the tooth surface.
PCT/JP2019/043602 2018-11-14 2019-11-07 Liquid oral composition WO2020100703A1 (en)

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Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS63188619A (en) * 1987-01-29 1988-08-04 Shiseido Co Ltd Composition for oral cavity
JPH02250816A (en) * 1989-03-23 1990-10-08 Kao Corp Composition for oral cavity application
JPH06145033A (en) * 1992-11-09 1994-05-24 Shiro Urabe Dentifrice composition containing povidone iodine
JPH09143042A (en) * 1995-11-24 1997-06-03 Lion Corp Composition for oral cavity
JP2008001657A (en) * 2006-06-23 2008-01-10 Tokyo Medical & Dental Univ Mouth washing agent, method for producing ozone water and apparatus for producing mouth washing agent
JP2018104294A (en) * 2016-12-22 2018-07-05 花王株式会社 Granules for dentifrices, and dentifrice composition containing the same

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS63188619A (en) * 1987-01-29 1988-08-04 Shiseido Co Ltd Composition for oral cavity
JPH02250816A (en) * 1989-03-23 1990-10-08 Kao Corp Composition for oral cavity application
JPH06145033A (en) * 1992-11-09 1994-05-24 Shiro Urabe Dentifrice composition containing povidone iodine
JPH09143042A (en) * 1995-11-24 1997-06-03 Lion Corp Composition for oral cavity
JP2008001657A (en) * 2006-06-23 2008-01-10 Tokyo Medical & Dental Univ Mouth washing agent, method for producing ozone water and apparatus for producing mouth washing agent
JP2018104294A (en) * 2016-12-22 2018-07-05 花王株式会社 Granules for dentifrices, and dentifrice composition containing the same

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