WO2016133063A1 - Composition orale liquide - Google Patents

Composition orale liquide Download PDF

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Publication number
WO2016133063A1
WO2016133063A1 PCT/JP2016/054370 JP2016054370W WO2016133063A1 WO 2016133063 A1 WO2016133063 A1 WO 2016133063A1 JP 2016054370 W JP2016054370 W JP 2016054370W WO 2016133063 A1 WO2016133063 A1 WO 2016133063A1
Authority
WO
WIPO (PCT)
Prior art keywords
liquid oral
oral composition
potassium nitrate
mass
composition
Prior art date
Application number
PCT/JP2016/054370
Other languages
English (en)
Japanese (ja)
Inventor
友美子 平嶋
赤羽　康宏
Original Assignee
ライオン株式会社
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by ライオン株式会社 filed Critical ライオン株式会社
Priority to CN201680010823.XA priority Critical patent/CN107249546B/zh
Priority to MYPI2017702777A priority patent/MY183114A/en
Priority to KR1020177021898A priority patent/KR102491340B1/ko
Publication of WO2016133063A1 publication Critical patent/WO2016133063A1/fr

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/44—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/84—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions otherwise than those involving only carbon-carbon unsaturated bonds
    • A61K8/86—Polyethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses

Definitions

  • the present invention relates to a liquid oral composition containing no potassium nitrate and containing no ethanol, which is excellent in hypersensitivity suppression effect and bactericidal effect in the oral cavity.
  • Patent Documents 1 and 2 As a preventive measure against dentin hypersensitivity, known potassium nitrate is blended into the oral composition as an active ingredient (Patent Documents 1 and 2). This potassium nitrate has a problem that an insoluble precipitate is formed in the presence of sodium lauryl sulfate which is generally blended in an oral composition.
  • Patent Document 3 there are many oral compositions containing potassium nitrate and sodium lauryl sulfate. By adding a monohydric alcohol and an amphoteric surfactant, precipitation of potassium lauryl sulfate is prevented and low temperature precipitation is suppressed.
  • non-alcohol type liquid preparations with less mucosal irritation and low irritation are more suitable for suppressing hypersensitivity particularly in liquid oral compositions.
  • cetylpyridinium chloride a cationic fungicide
  • cetylpyridinium chloride has an excellent bactericidal effect on airborne bacteria in the oral cavity and is effective in preventing or suppressing oral diseases such as caries, but is easily affected by a surfactant.
  • Patent Document 4 a specific compound is added to an oral composition containing a biguanide-based cationic fungicide and a nonionic surfactant to prevent deactivation of the cationic fungicide by the nonionic surfactant. Then, a stabilized blending technique has been proposed.
  • non-alcohol type liquid oral preparation containing potassium nitrate can suppress hypersensitivity and at the same time exert high bactericidal power against oral floating bacteria, it is more effective for prevention or suppression of oral diseases.
  • the current situation is that it is difficult with conventional techniques, and the development of liquid oral preparations having such excellent characteristics has been desired.
  • the present invention has been made in view of the above circumstances, and an object of the present invention is to provide an ethanol-free liquid oral composition containing potassium nitrate, which is excellent in the hypersensitivity suppressing effect and the bactericidal effect of airborne bacteria in the oral cavity.
  • the present inventors have found that (A) potassium nitrate and (B) cetylpyridinium chloride are combined with an ethanol-free liquid oral composition, and (C) nonionic By blending a surfactant and (D) an amphoteric surfactant, (E) the water content is 55% by mass or more and less than 92% by mass, and the pH of the composition is 6.8 or more and less than 8.0 by ( A), non-alcohol-type liquid oral composition is obtained, in which precipitation of insoluble precipitates generated by the combined use of components (B) is suppressed, and the perceptual hypersensitivity suppressing effect and the bactericidal effect of airborne bacteria in the oral cavity are excellent.
  • the present inventors have found that it can be suitably used for caries suppression and have made the present invention.
  • potassium nitrate-containing cetyl chloride and potassium nitrate and cetyl chloride were expected to be added to the liquid oral composition containing potassium nitrate by adding cetylpyridinium chloride, a cationic fungicide, to prevent hypersensitivity and bactericidal bacteria.
  • cetylpyridinium chloride a cationic fungicide
  • the liquid oral composition of the present invention containing no ethanol shows almost no insoluble precipitate even after 4 weeks have passed since the preparation of the liquid oral composition. Appearance is stable over time, high sensitivity to hypersensitivity and bactericidal effect on airborne bacteria in the oral cavity, and bitterness after use is suppressed, resulting in a good feeling of good use.
  • Patent Document 3 suppresses precipitation of potassium lauryl sulfate caused by the combined use of potassium nitrate and sodium lauryl sulfate in the oral composition
  • Patent Document 4 describes a cationic bactericide using a nonionic surfactant. No mention is made of using a cationic bactericide in combination with potassium nitrate.
  • Patent Documents 5 and 6 describe liquid oral compositions containing potassium nitrate and cetylpyridinium chloride, but these are ethanol-containing compositions. From Patent Documents 3 to 6, the suppression of precipitation of insoluble precipitates caused by the combined use of potassium nitrate and cetylpyridinium chloride in a liquid oral composition containing no ethanol cannot be predicted.
  • the present invention provides the following liquid oral composition and a method for suppressing the precipitation of insoluble precipitates in the composition.
  • the nonionic surfactant is polyoxyethylene hydrogenated castor oil having an average addition mole number of ethylene oxide of 40 to 100 mol
  • the amphoteric surfactant is coconut oil fatty acid amidopropyl betaine [ 1] or [2] liquid oral composition.
  • [5] The liquid oral composition according to any one of [1] to [4], wherein 0.01 to 10% by mass of component (A) and 0.001 to 0.1% by mass of component (B) are blended.
  • [6] The liquid oral composition according to any one of [1] to [5], which is a mouthwash.
  • [7] The liquid oral composition according to any one of [1] to [6], which is used for suppressing hypersensitivity and caries.
  • [8] (A) A non-ethanol-containing liquid oral composition containing potassium nitrate and (B) cetylpyridinium chloride, (C) a nonionic surfactant and (D) an amphoteric surfactant, and (E) water content 55% by mass or more and less than 92% by mass, and the pH of the composition is 6.8 or more and less than 8.0, wherein (A) potassium nitrate and (B) cetylpyridinium chloride in the liquid oral composition A method for suppressing the precipitation of insoluble precipitates produced by the combined use.
  • liquid oral composition containing no potassium nitrate and containing no ethanol, which is excellent in the effect of suppressing hypersensitivity and the bactericidal effect of floating bacteria in the oral cavity.
  • composition for liquid oral cavity of the present invention contains (A) potassium nitrate, (B) cetylpyridinium chloride, (C) nonionic surfactant, (D) amphoteric surfactant, (E) water, and contains no ethanol It is.
  • (A) Potassium nitrate is blended as an active ingredient for preventing or treating dentin hypersensitivity, and is a hypersensitivity inhibitor.
  • the blending amount of the component (A) potassium nitrate is preferably 0.01 to 10% (mass%, hereinafter the same) of the whole composition, more preferably 0.1 to 7%. As the blending amount increases, the perceptual hypersensitivity suppression effect increases, but 10% or less is more suitable for sufficient precipitation suppression and bitterness suppression.
  • Cetylpyridinium chloride is a cationic bactericidal agent and a bactericidal agent against floating bacteria in the oral cavity.
  • a commercially available cetylpyridinium chloride can be used.
  • the amount of component (B) cetylpyridinium chloride is preferably 0.001 to 0.1%, more preferably 0.005 to 0.1%, still more preferably 0.01 to 0.05% of the total composition. %. The more the compound is added, the higher the bactericidal effect, but 0.1% or less is more suitable for sufficient precipitation suppression and bitterness suppression.
  • Examples of (C) nonionic surfactants include polyoxyethylene hydrogenated castor oil, polyoxyethylene alkyl ether, and polyglycerin fatty acid ester, and one or more of these may be used.
  • (E.O.) polyoxyethylene hydrogenated castor oil having an average added mole number of 40 to 100 moles, particularly 60 to 100 moles, and an alkyl group having 16 to 18 carbon atoms.
  • O. Preferred are polyoxyethylene alkyl ethers having an average addition mole number of 10 to 40 moles, particularly 20 to 40 moles, and decaglycerin monofatty acid esters polyglycerin fatty acid esters having a fatty acid number of 12 to 18, particularly 12 to 14, among others.
  • E. O. Polyoxyethylene hydrogenated castor oil having an average added mole number of 40 to 100 moles is preferred.
  • the blending amount of the nonionic surfactant as the component (C) is preferably 0.1 to 2% of the total composition, more preferably 0.1 to 1%, still more preferably 0.2 to 0.5%. is there.
  • 0.1% or more is blended, a sufficient precipitation suppressing effect, a hypersensitivity suppressing effect and a floating bacteria sterilizing effect are exhibited, and the bitterness can be sufficiently suppressed.
  • 2% or less is more suitable for preventing the perceptual hypersensitivity suppressing effect and the floating bacteria bactericidal effect from decreasing.
  • Amphoteric surfactants include alkylamidobetaines such as coconut oil fatty acid amidopropylbetaine or salts thereof, betaine acetates such as lauryldimethylaminoacetic acid betaine, N-fatty acid acyl-N-carboxymethyl-N-hydroxyethyl Examples include imidazoline type such as ethylenediamine salt, amino acid type such as N-fatty acid acyl-L-alginate salt, and the like, and one or more of these may be used, and alkylamide betaine or a salt thereof is particularly preferable. Among these, coconut oil fatty acid amidopropyl betaine is preferable.
  • TEGO Betaine CK OK (30% aqueous solution) manufactured by Degussa Co., Ltd.
  • Amphitol 55AB (30% aqueous solution) manufactured by Kao Corporation
  • the blending amount of the amphoteric surfactant as component (D) is preferably 0.1 to 2% of the total composition, more preferably 0.1 to 1%, and still more preferably 0.2 to 0.5%. .
  • a sufficient precipitation suppressing effect, a hypersensitivity suppressing effect and a floating bacteria sterilizing effect are exhibited, and the bitterness can be sufficiently suppressed.
  • 2% or less is more suitable for preventing the perceptual hypersensitivity suppressing effect and the floating bacteria bactericidal effect from decreasing.
  • the water content that is, the water content in the composition is 55% or more and less than 92% of the whole composition, preferably 60% or more and 91% or less. Preferably they are 60% or more and 70% or less.
  • the amount of water is within the above range, insoluble precipitates can be prevented from being precipitated, and excellent perceptual hypersensitivity suppressing effects and bitterness suppressing effects can be imparted. If it is less than 55%, the precipitation cannot be suppressed, and the perceptual hypersensitivity suppressing effect and the floating bacteria sterilizing effect are inferior. When it is 92% or more, the precipitation suppressing effect is inferior, the perceptual hypersensitivity suppressing effect and the floating bacteria sterilizing effect are also inferior, and the bitterness cannot be suppressed.
  • the liquid oral composition has a pH of 6.8 or more and less than 8.0, preferably pH 6.8 to 7.8, more preferably pH 6.8 to 7.5.
  • the precipitation suppression effect, the hypersensitivity suppression effect and the bitterness suppression effect are excellent.
  • the pH is less than 6.8 or pH 8.0 or more, the precipitation cannot be suppressed, and the perceptual hypersensitivity suppressing effect and the floating bacteria sterilizing effect are inferior.
  • the pH was measured immediately after preparation using a pH meter (model number Hm-30S) manufactured by Toa Denpa Kogyo Co., Ltd., and the value after 3 minutes at 25 ° C. (the same applies hereinafter).
  • a known pH adjusting agent may be added to adjust the pH of the composition within the above range.
  • examples thereof include alkali metal hydrogen phosphates such as sodium dihydrogen phosphate and alkali metal hydroxides such as sodium hydroxide.
  • the liquid oral cavity composition of the present invention contains no ethanol.
  • “ethanol-free formulation” is one in which ethanol is not blended, but in liquid oral compositions, there are cases where a small amount of ethanol derived from the raw material is contained in the fragrance blended in the composition. In consideration of these reasons, ethanol is not included in addition to ethanol contained in a trace amount in a fragrance.
  • the amount of ethanol in the composition is preferably 100 ppm or less, more preferably 50 ppm or less, still more preferably 10 ppm or less, and may be 0 ppm with respect to the entire composition.
  • such an ethanol-free composition suppresses the precipitation of insoluble precipitates, and exhibits an excellent perceptual hypersensitivity suppressing effect and a floating bacteria sterilizing effect.
  • the liquid oral cavity composition of the present invention is particularly suitable as a mouthwash.
  • other well-known components can be mix
  • a wetting agent, a solvent, and if necessary, a sweetening agent, a coloring agent, a preservative, a fragrance, an active ingredient, and the like are blended.
  • polishing agent are not normally mix
  • surfactant surfactants other than (C) nonionic surfactant and (D) amphoteric surfactant may not be added, but in the case of adding 0.5% or less (0 to 0.5%), particularly 0.05 to 0.2% is desirable.
  • wetting agent examples include sugar alcohols such as sorbitol, and polyhydric alcohols such as glycerin and polyethylene glycol.
  • sugar alcohols such as sorbitol
  • polyhydric alcohols such as glycerin and polyethylene glycol.
  • the blending amount of these wetting agents is usually 1 to 40%, particularly 2 to 40%.
  • purified water is generally used, and the water content in the composition can be added within the above range. Further, a lower monohydric alcohol having 1 to 3 carbon atoms such as ethanol, propylene glycol or the like may be blended.
  • sweetening agents xylitol, maltitol, saccharin, saccharin sodium, stevioside, aspartame, and the like can be blended.
  • a colorant a highly safe water-soluble pigment such as Blue No. 1, Green No. 3, Yellow No. 4, Red No. 105, or the like can be added.
  • the preservative include paraoxybenzoic acid ester, benzoic acid or a salt thereof.
  • Natural flavors such as peppermint oil, spearmint oil, eucalyptus oil, wintergreen oil, clove oil, thyme oil, sage oil, cardamom oil, rosemary oil, marjoram oil, lemon oil, nutmeg oil, lavender oil, paracres oil, etc.
  • Active ingredients include potassium nitrate, cetylpyridinium chloride, bactericides such as isopropylmethylphenol, anti-inflammatory agents such as tranexamic acid and epsilon-aminocaproic acid, enzymes such as dextranase, sodium fluoride, monofluorophosphoric acid Examples include fluorides such as sodium, allantoin, vitamins such as vitamin C, copper compounds, and plant extracts. In addition amount of these active ingredients can be made into the range which does not prevent the effect of this invention.
  • Liquid oral compositions having the compositions shown in Tables 1 and 2 were prepared by a conventional method.
  • mouthwash thus obtained was evaluated by the following methods and criteria, the results shown in Tables 1 and 2 were obtained.
  • the bacterial solution used was Streptococcus as an oral resident bacteria prepared by dissolving 30 g of Trypticase Soy Broth (Difco) in 1 L of purified water as a culture solution. Prepared by adding physiological saline so that the permeability at 550 nm of a solution cultured for 1 day under anaerobic conditions (5 vol% carbon dioxide gas, 95 vol% nitrogen) using mutans ATCC 10449 strain is 20 did. Add 0.3 mL of the bacterial solution to 2.7 mL of the sample (liquid oral composition), stir, react at 37 ° C. for 1 minute, stir again, and then add five test tubes containing 2.7 mL of the culture solution in advance.
  • the compounding quantity of alkylamide betaine is also a pure part conversion value also including the inside of a table
  • the raw materials used are the same as described above.
  • This mouthwash was all excellent in appearance stability (precipitation suppression effect), hypersensitivity suppression effect, airborne bacteria sterilization effect, and feeling of use (no bitterness).
  • mouthwash A
  • B Cetylpyridinium chloride 0.05
  • C Polyoxyethylene
  • D Alkylamidobetaine 0.3
  • Glycerin 3.0 Propylene glycol 8.0 Saccharin sodium 0.1 Sodium dihydrogen phosphate 0.5 Sodium hydroxide 0.16 Fragrance 0.2
  • E Purified water 82.19 Total 100.0% pH 6.8

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Chemical & Material Sciences (AREA)
  • Inorganic Chemistry (AREA)
  • Oral & Maxillofacial Surgery (AREA)
  • Cosmetics (AREA)

Abstract

L'invention concerne une composition orale liquide qui est préparée par ajout, à une composition liquide orale dépourvue d'éthanol et comprenant du nitrate de potassium (A) et du chlorure de cétyl pyridinium (B), d'un surfactant non ionique (C) et d'un tensioactif amphotère (D), la teneur de l'eau (E) étant régulée à 55 % en masse ou plus et à moins de 92 % en masse et le pH de la composition étant ajusté à 6,8 ou plus et moins de 8,0. La composition liquide orale, présente d'excellents effets de suppression de l'hypersensibilité et de prévention des caries dentaires, la sédimentation d'un précipité insoluble, ledit précipité étant formé par l'utilisation combinée des composants (A) et (B) dans la composition orale liquide susmentionnée, étant supprimée.
PCT/JP2016/054370 2015-02-17 2016-02-16 Composition orale liquide WO2016133063A1 (fr)

Priority Applications (3)

Application Number Priority Date Filing Date Title
CN201680010823.XA CN107249546B (zh) 2015-02-17 2016-02-16 液体口腔用组合物
MYPI2017702777A MY183114A (en) 2015-02-17 2016-02-16 Oral liquid composition
KR1020177021898A KR102491340B1 (ko) 2015-02-17 2016-02-16 액체 구강용 조성물

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2015-028458 2015-02-17
JP2015028458A JP6547324B2 (ja) 2015-02-17 2015-02-17 液体口腔用組成物

Publications (1)

Publication Number Publication Date
WO2016133063A1 true WO2016133063A1 (fr) 2016-08-25

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PCT/JP2016/054370 WO2016133063A1 (fr) 2015-02-17 2016-02-16 Composition orale liquide

Country Status (5)

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JP (1) JP6547324B2 (fr)
KR (1) KR102491340B1 (fr)
CN (1) CN107249546B (fr)
MY (1) MY183114A (fr)
WO (1) WO2016133063A1 (fr)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6688072B2 (ja) * 2015-12-28 2020-04-28 花王株式会社 液体口腔用組成物
CN110974724B (zh) * 2019-12-30 2023-04-18 重庆登康口腔护理用品股份有限公司 一种含透明质酸的组合物及其制备方法和应用
WO2022255124A1 (fr) * 2021-06-03 2022-12-08 ライオン株式会社 Composition liquide à usage oral

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JPH04173728A (ja) * 1990-11-02 1992-06-22 Sunstar Inc 口腔用液体製剤
WO2009020010A1 (fr) * 2007-08-09 2009-02-12 Lion Corporation Composition orale liquide et procédé pour améliorer l'activité bactéricide d'un agent bactéricide cationique
JP2012121833A (ja) * 2010-12-08 2012-06-28 Lion Corp 口腔用組成物及び口腔疾患原因菌の歯面定着抑制剤
JP2013067568A (ja) * 2011-09-21 2013-04-18 Lion Corp 歯磨剤組成物
JP2014185126A (ja) * 2013-03-25 2014-10-02 Sunstar Inc 口腔用透明液状組成物

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US3863006A (en) 1973-01-29 1975-01-28 Milton Hodosh Method for desensitizing teeth
JPH0629177B2 (ja) 1984-06-01 1994-04-20 ライオン株式会社 口腔用組成物
JPH07101842A (ja) 1993-08-12 1995-04-18 Lion Corp 口腔用組成物
JP3978609B2 (ja) 2003-08-25 2007-09-19 ライオン株式会社 口腔用組成物及び口腔用組成物中におけるラウリル硫酸カリウムの析出防止方法
JP2007084471A (ja) 2005-09-21 2007-04-05 Sunstar Inc 口腔用組成物および口腔用製品の選択方法
JP2013035792A (ja) 2011-08-09 2013-02-21 Kao Corp 口腔用組成物

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Publication number Priority date Publication date Assignee Title
JPH04173728A (ja) * 1990-11-02 1992-06-22 Sunstar Inc 口腔用液体製剤
WO2009020010A1 (fr) * 2007-08-09 2009-02-12 Lion Corporation Composition orale liquide et procédé pour améliorer l'activité bactéricide d'un agent bactéricide cationique
JP2012121833A (ja) * 2010-12-08 2012-06-28 Lion Corp 口腔用組成物及び口腔疾患原因菌の歯面定着抑制剤
JP2013067568A (ja) * 2011-09-21 2013-04-18 Lion Corp 歯磨剤組成物
JP2014185126A (ja) * 2013-03-25 2014-10-02 Sunstar Inc 口腔用透明液状組成物

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KAZUYUKI YAHAGI: "Current aspects and prospective problems in research and development for medicated dentifrice, mouthwash, and oral freshner", FRAGRANCE JOURNAL, 15 January 2000 (2000-01-15), pages 89 - 95, XP002996583, ISSN: 0288-9803 *

Also Published As

Publication number Publication date
JP2016150912A (ja) 2016-08-22
MY183114A (en) 2021-02-15
JP6547324B2 (ja) 2019-07-24
CN107249546B (zh) 2020-07-10
KR20170117406A (ko) 2017-10-23
CN107249546A (zh) 2017-10-13
KR102491340B1 (ko) 2023-01-26

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