WO2014054257A1 - Composition de dentifrice - Google Patents

Composition de dentifrice Download PDF

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Publication number
WO2014054257A1
WO2014054257A1 PCT/JP2013/005778 JP2013005778W WO2014054257A1 WO 2014054257 A1 WO2014054257 A1 WO 2014054257A1 JP 2013005778 W JP2013005778 W JP 2013005778W WO 2014054257 A1 WO2014054257 A1 WO 2014054257A1
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WIPO (PCT)
Prior art keywords
remineralization
composition
hydroxyapatite
ultramarine
dentifrice
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PCT/JP2013/005778
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English (en)
Japanese (ja)
Inventor
佐久間　周治
恵二郎 藤田
理絵 高松
真理子 小吹
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株式会社サンギ
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Publication of WO2014054257A1 publication Critical patent/WO2014054257A1/fr

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/24—Phosphorous; Compounds thereof
    • 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 dentifrice composition having an effect of promoting recalcification of teeth.
  • Caries start from the formation of dental plaque by caries bacteria such as Streptococcus mutans adhering to the tooth surface, and organic acids produced by the metabolism of food by dental caries in dental plaque
  • the enamel is decalcified and an initial caries state is obtained.
  • Saliva has the function of remineralizing the demineralized part by the action of calcium and phosphorus in the saliva and returning the teeth to the original state. If the decalcified teeth can be sufficiently regenerated by remineralization, the occurrence of caries can be suppressed.
  • a dentifrice containing one kind of fluoride and calcium phosphate and hydroxyapatite having a crystal structure similar to the inorganic components of teeth is manufactured and sold.
  • oral compositions such as dentifrices that can sufficiently realize the promotion of remineralization because remineralization of the demineralized part is not sufficient only by using saliva or a dentifrice containing fluoride or hydroxyapatite. Development is required.
  • Dentifrice composition for oral cavity (Patent Document 2) that can retain hydroxyapatite fine powder on the tooth surface for a long time by blending hydroxyapatite fine powder with water-soluble cellulose solution, Oral bacteria (Patent Document 3) that can significantly promote remineralization by using a sugar alcohol such as xylitol and dicalcium phosphate in combination, and oral bacteria containing low crystalline hydroxyapatite Oral composition (Patent Document 4) that can prevent oral diseases and discomfort by adsorbing and sterilizing -Oral composition (patent document 5), micellar calcium phosphate-phosphopeptide which can prevent tooth decay and periodontal disease by tooth whitening, remineralization promotion, which contains calcium compounds such as hydroxya
  • Patent Document 7 Can promote remineralization and suppress caries (Patent Document 7), and pH 5 to 5 in which tricalcium phosphate is blended as calcium salt powder having the ability to convert into hydroxyapatite by contact with water in the oral cavity.
  • No. 8 dentifrice composition (Patent Document 8) and the like have been proposed.
  • ultramarine is composed of aluminum and sodium silicates, sulfide ions and sulfate ions, and is naturally present as the main component of lapis lazuli, and is known as an inorganic pigment.
  • Speaking of ultramarine meant blue ultramarine, but now there are green and purple (varieties called ultramarine violet or ultramarine red) and red (ultramarine pink) .
  • This ultramarine is used in paints, printing inks, paper, rubber, plastic coloring, wallpaper and tanning dyeing, detergents, cosmetics, liquid crystal display color filters, and the like.
  • ultramarine blue is used as a substance that modifies the color of teeth in a composition for delivering an oral care substance to the oral cavity (Patent Document 9). Furthermore, as a poorly water-soluble component in an oral composition for use in an applicator-integrated container that can stably disperse a poorly water-soluble powder component in the composition by using xanthan gum as a thickener, ultramarine, hydroxy, Apatite is exemplified (Patent Document 10). Here, unlike the present invention, the compositions in Patent Documents 9 and 10 are not used for dentifrice.
  • sodium silicate is also used as a component of oral compositions, and has been proposed as a component that stabilizes the properties of aluminum lactate, for example, for preventing hypersensitivity and for tightening gingival tissues. (Patent Document 11).
  • An object of the present invention is to provide a dentifrice composition having a high remineralization effect of demineralized tooth enamel.
  • the inventors of the present invention formulated a ultramarine composition usually used as a colorant in calcium phosphate selected from hydroxyapatite and tricalcium phosphate, and this was used as a dentifrice. Surprisingly, it was found that the remineralization of teeth was remarkably promoted, and the present invention was completed. Moreover, it discovered that these effects were further accelerated
  • the present invention relates to a dentifrice composition containing (1) ultramarine composition and calcium phosphate selected from hydroxyapatite and tricalcium phosphate, and (2) ultramarine composition comprising Na ( 6-10) it or dentifrice composition according to the above (1), characterized in a composition represented by Al 6 Si 6 O 24 S ( 2 ⁇ 4), formulation (3) ultramarine composition
  • the dentifrice composition according to the above (1) or (2), wherein the amount is 0.0001 to 0.5% by weight, and (4) the amount of hydroxyapatite is 0.001 to The dentifrice composition according to any one of the above (1) to (3), which is 30% by weight, and (5) the above (1), wherein the blending amount of tricalcium phosphate is 0.001 to 30% by weight Toothpaste composition according to any of (3), (6) and Silica The dentifrice composition according to any one of (1) to (5) above, wherein (7) sodium silicate is blended in an amount of 0.01 to 20.0% by weight, wherein sodium is blended It is related
  • the dentifrice composition of the present invention is composed of ultramarine composition, calcium phosphate selected from hydroxyapatite and tricalcium phosphate as an active ingredient, and is excellent in remineralization of decalcified tooth enamel. .
  • FIG. 4 is a diagram in which the photographs shown in FIG. 1 and FIG. 3 are drawn using dark ink and descriptions of the state of each part are added.
  • the dentifrice composition of the present invention is not particularly limited as long as it contains an ultramarine composition and a calcium phosphate selected from hydroxyapatite and tricalcium phosphate.
  • a toothpaste, A powder dentifrice, a liquid dentifrice, etc. can be illustrated. Hydroxyapatite and tricalcium phosphate may be used alone or in combination.
  • the dentifrice composition of the present invention significantly promotes the remineralization of teeth because the ultramarine composition usually used as a colorant is blended with calcium phosphate selected from hydroxyapatite and tricalcium phosphate. be able to.
  • Hydroxyapatite used in the present invention is a kind of calcium phosphate, and is obtained from fish bones of pork, pork bones, cow bones, etc. of edible fish such as salmon as natural hard tissues in addition to those synthesized by ordinary methods. There may be.
  • hydroxyapatite is stoichiometrically represented by a composition composed of Ca 10 (PO 4 ) 6 (OH) 2 , but is non-stoichiometric with a Ca / P molar ratio of not 1.67. Even in this case, it exhibits the properties of hydroxyapatite and can have an apatite structure.
  • synthetic hydroxyapatite having a Ca / P molar ratio of about 1.4 to 1.8 is also included in the hydroxyapatite in the present invention.
  • the hydroxyapatite used in the present invention may be crystalline, low crystalline, or amorphous, but it is low crystalline or amorphous hydroxyapatite from the viewpoint of caries prevention effect.
  • low crystalline hydroxyapatite and amorphous hydroxyapatite are referred to as “amorphous hydroxyapatite”.
  • “Low crystallinity” means that the X-ray diffraction peak is broader than that of highly crystalline powder, and “amorphous” means that the X-ray diffraction pattern has a wide halo. The diffraction pattern showing the characteristics of the crystal cannot be obtained.
  • Such amorphous hydroxyapatite can be obtained, for example, by freeze-drying apatite synthesized by a wet synthesis method, drying at a temperature of 100 ° C. or lower, or baking at about 300 ° C. or lower.
  • the amount of hydroxyapatite blended in the present invention is preferably 0.001 to 30% by weight, preferably 0.01 to 20% by weight of the entire dentifrice composition, from the viewpoint of the remineralization promoting effect and the feeling of use. More preferred is 0.1 to 20% by weight.
  • Tricalcium phosphate used in the present invention is also referred to as tricalcium phosphate, and is a composition represented by the chemical formula 3Ca 3 (PO 4 ) 2 .Ca (OH) 2 , including pharmaceuticals and cosmetics, foods, It is widely used in general goods and petrochemical industries.
  • the tricalcium phosphate used in the present invention may be anything such as a pharmaceutical additive standard, a quasi-drug raw material standard, and a combination component standard for each cosmetic variety.
  • the blending amount of tricalcium phosphate in the present invention is preferably 0.001 to 30% by weight, and 0.01 to 20% by weight of the entire dentifrice composition, from the viewpoint of the remineralization promoting effect and the feeling of use. %, More preferably 0.1 to 20% by weight.
  • the ultramarine composition used in the present invention is, for example, an inorganic pigment represented by the chemical formula Na ( 6-10 ) Al 6 Si 6 O 24 S (2-4) .
  • the ultramarine composition used in the present invention can be used from blue to near pink. Specifically, blue CB-80: manufactured by Daiichi Kasei Kogyo Co., Ltd., Daiichi Pink DP-3: Daiichi Kasei Kogyo ( Examples thereof include powder pigments manufactured by UNIPURE PINK LC589, manufactured by Daito Kasei Kogyo Co., Ltd.
  • the ultramarine composition of the present invention may be of any type for cosmetics, quasi-drug raw material standards, and the like.
  • the blending amount of the ultramarine composition in the present invention is preferably 0.0001 to 0.5% by weight of the entire dentifrice composition from the viewpoint of the remineralization promoting effect and the feeling of use, and is preferably 0.001 to 0. More preferably, it is 1% by weight.
  • the dentifrice composition of the present invention preferably further contains sodium silicate. By containing sodium silicate, remineralization of teeth can be further promoted.
  • Examples of the sodium silicate used in the present invention include Na 4 SiO 4 , Na 2 Si 2 O 5 , Na 2 Si 4 O 9 and the like, in addition to the sodium salt of metasilicic acid Na 2 SiO 3 . More specifically, for example, a quasi-drug raw material standard can be used.
  • the blending amount of sodium silicate in the present invention is preferably 0.01 to 20% by weight, and more preferably 0.1 to 10% by weight, from the viewpoint of remineralization promoting effect and feeling of use.
  • the dentifrice composition of the present invention contains additives, humectants, foaming agents, fragrances, sweeteners, preservatives and various active ingredients that are usually used in dentifrice compositions in addition to the aforementioned components. Can do. Specific examples of these components are shown below. In addition to the components shown below, appropriate components according to the purpose, the type of the composition, and the like can be further blended.
  • dibasic calcium phosphate, calcium carbonate, calcium pyrophosphate, abrasive precipitated silica, abrasive gel silica and other silica calcium silicate, aluminum silicate, aluminum oxide, aluminum hydroxide, alumina, zeolite, titanium oxide, silica
  • examples thereof include zirconium acid, insoluble sodium metaphosphate, tribasic magnesium phosphate, magnesium carbonate, calcium sulfate, magnesium sulfate, polymethyl methacrylate, bentonite, and a synthetic resin.
  • wetting agent examples include polyhydric alcohols such as glycerin, propylene glycol, polyethylene glycol, sorbitol, xylitol, ethylene glycol, 1,3-butylene glycol, and isopropylene glycol.
  • polyhydric alcohols such as glycerin, propylene glycol, polyethylene glycol, sorbitol, xylitol, ethylene glycol, 1,3-butylene glycol, and isopropylene glycol.
  • foaming agent examples include sodium lauryl sulfate, sodium N-lauroyl sarcosine, a nonionic surfactant, and the like.
  • thickeners examples include hydroxyethylcellulose, sodium carboxymethylcellulose, carrageenan, carboxyvinyl polymer, xanthan gum, gelatin, pullulan, sodium alginate, sodium polyacrylate, polyvinyl alcohol, locust bean gum, guar gum, hydroxypropyl methylcellulose, etc. Can do.
  • Binders include methylcellulose, propylene glycol alginate, pullulan, tragacanth gum, xanthan gum, pectin, fercelan, chitosan, polyethylene oxide, polyvinylpyrrolidone, polyacrylic acid, polymethacrylic acid, peptone, casein, collagen, albumin, gum arabic, karaya gum Eudragit, ethyl cellulose, cellulose acetate, sodium polyacrylate, polyvinyl alcohol, polyvinyl acetal / dimethylaminoacetate, cellulose acetate / dibutylhydroxypropyl ether, and the like.
  • polyoxyethylene hydrogenated castor oil sorbitan monostearate, glycerin fatty acid ester, propylene glycol fatty acid ester, alkyl glyceryl ether, polyoxyethylene sorbitol fatty acid ester, polysorbate, polyoxyethylene, lauromacrogol, sodium alkyl sulfate
  • examples include alkyl phosphate esters, sodium alkylbenzene sulfonates, sodium N-acyl sarcosine, N-acyl glutamates, sucrose fatty acid esters, alkyl glycosides, alkyl dimethyl amine oxides, alkyl betaines and the like.
  • Oils and fats include liquid paraffin, paraffin, cetyl alcohol, higher alcohols such as stearyl alcohol, fatty acid esters such as isopropyl myristate, lanolin, whale wax, carnauba wax, fatty acids, octyldodecyl myristate, diisopropyl adipate, hexadecyl isostearate And ester compounds such as decyl oleate, squalane, squalene, medium chain fatty acid triglycerides, silicon and the like.
  • alcohols such as stearyl alcohol, fatty acid esters such as isopropyl myristate, lanolin, whale wax, carnauba wax, fatty acids, octyldodecyl myristate, diisopropyl adipate, hexadecyl isostearate
  • ester compounds such as decyl oleate, squalane,
  • Alcohols include lower alcohols such as ethanol, propyl alcohol, isopropyl alcohol, butanol, isobutanol, ethylene glycol, diethylene glycol, propylene glycol, dipropylene glycol, 1,3-butylene glycol, glycerin, 1,5-pentadiol, sorbit Examples thereof include polyhydric alcohols such as polyethylene glycol.
  • Surfactants include nonionic surfactants such as sorbitan fatty acid ester, glycerin fatty acid ester, decaglycerin fatty acid ester, polyglycerin fatty acid ester, propylene glycol / pentaerythritol fatty acid ester, polyoxyethylene sorbitan fatty acid ester, polyoxyethylene.
  • nonionic surfactants such as sorbitan fatty acid ester, glycerin fatty acid ester, decaglycerin fatty acid ester, polyglycerin fatty acid ester, propylene glycol / pentaerythritol fatty acid ester, polyoxyethylene sorbitan fatty acid ester, polyoxyethylene.
  • pH adjusters examples include citric acid and its salts, phosphoric acid and its salts, malic acid and its salts, gluconic acid and its salts, maleic acid and its salts, aspartic acid and its salts, gluconic acid and its salts, succinic acid And salts thereof, glucuronic acid and salts thereof, fumaric acid and salts thereof, glutamic acid and salts thereof, adipic acid and salts thereof, inorganic acids such as hydrochloric acid, hydrofluoric acid, sodium hydroxide, potassium hydroxide, etc. Examples include alkali metals, amines such as triethanolamine, diethanolamine, and diisopropanolamine.
  • preservative examples include paraoxybenzoic acid ester, alkyldiaminoethylglycine hydrochloride, methylparaben, ethylparaben, sodium benzoate and the like.
  • the stabilizer examples include sodium sulfite, sodium hydrogen sulfite, dibutylhydroxytoluene, butylhydroxyanisole, edetic acid or salts thereof.
  • Perfumes include essential oils such as menthol, peppermint, spearmint, eucalyptus oil, orange oil, lemon oil, winder green oil, clove oil, peppermint oil, thyme oil, carvone, linalool, eugenol, anethole, herb mint, etc. Can be illustrated.
  • stabilizers include vitamin C, vitamin E and derivatives thereof, sodium sulfite, sodium pyrosulfite, sodium hydrogen sulfite, butylhydroxytoluene, butylhydroxyanisole and the like.
  • sweetening agents include saccharin sodium, aspartame, stevioside, neohesperidyl dihydrochalcone, glycyrrhizin, asparatylphenylalanine methyl ester, acesulfame potassium, perilartine, p-methoxycinnamic aldehyde, xylitol and the like.
  • Other medicinal ingredients include allantoin, tocopherol acetate, isopropylphenol, triclosan, chlorhexidine, chlorophyll, flavonoids, tranexamic acid, hinokitiol, cetylpyridinium chloride, sodium fluoride, stannous fluoride, sodium monofluorophosphate, dextranase
  • examples include mutanase, protease, aminocaproic acid, glycyrrhizic acid, glycyrrhetinic acid, azulene, allantoin, lysozyme chloride, psyllium extract, polyphosphoric acid, sodium chloride and the like.
  • the compounding quantity of these arbitrary components is used suitably in the range accept
  • the ultramarine composition, hydroxyapatite, tricalcium phosphate, sodium silicate, and other components may be added in any process of the production process.
  • a toothpaste (Examples 1 to 48) and a liquid dentifrice (Examples 49 to 88) containing a combination of ultramarine composition and hydroxyapatite or tricalcium phosphate and sodium silicate were further prepared. Acceleration test was conducted.
  • the obtained hydroxyapatite powder had a maximum particle size of about 40 ⁇ m, a minimum particle size of about 0.05 ⁇ m, and an average particle size of about 5 ⁇ m.
  • This hydroxyapatite powder was used.
  • Tricalcium phosphate As the tricalcium phosphate, ⁇ -TCP-100 (Taihei Chemical Industry Co., Ltd.) was used.
  • ultramarine composition hydroxyapatite, tricalcium phosphate, dicalcium phosphate, hydroxyapatite and sodium silicate, tricalcium phosphate and sodium silicate, ultramarine composition and sodium silicate, ultramarine
  • a remineralization acceleration test was conducted by preparing a toothpaste and a liquid dentifrice containing the composition and dicalcium phosphate and the group composition blue, sodium silicate and dicalcium phosphate.
  • an artificial initial caries test sample prepared in advance was used for the preparation of the artificial initial caries test sample.
  • bovine anterior teeth and crown labial enamel were used for the preparation of the artificial initial caries test sample.
  • the enamel surface was polished with # 1000, # 2400, and # 4000 polishing paper.
  • a 3.5 ⁇ 3.0 mm window was prepared by using Nail Enamel (Maybelin Co., Ltd.) as a test target site on the polished enamel surface, and 0.1 M lactate buffer (pH 4.5, 3.0 mM CaCl 2 , 1. 8 mM KH 2 PO 4 , 0.5% CMC) was immersed for 4 days at 37 ° C. to prepare an artificial initial caries.
  • test solution was prepared by mixing toothpaste and liquid dentifrice with artificial saliva to form a suspension solution.
  • the artificial initial caries test specimen prepared above was immersed in each test solution for 12 days, and then the specimen was about 500 ⁇ m thick so that it was parallel to the tooth axis with a microcutter. After cutting, this slice was ground using a grindstone and a natural grindstone to form parallel thin slices of about 100 ⁇ m thickness under water injection.
  • CMR contact microradiogram
  • Control surface in the figure is a part for comparing the degree of remineralization effect of the dentifrice compositions of Examples and Comparative Examples, and maintained the state of artificial initial caries. Is. Half of the artificial initial caries (3.5 ⁇ 3.0 mm window) region.
  • the “treated surface” in the figure is a portion on which the test solutions (test substances) of Examples and Comparative Examples are applied.
  • Tables 33 and 34 show the results of confirming the effect of promoting remineralization of the dentifrice composition by the computer image analysis method.
  • Example 1 (remineralization rate: 19.9%) and Comparative Example 1 and Comparative Example 12 (total remineralization rate: 14.5%)
  • Example 2 (remineralization rate: 20.0%)
  • Comparative Example 2 and Comparative Example 7 (total remineralization rate: 9.4%)
  • Example 5 (remineralization rate: 34.3%)
  • Comparative Example 3 and Comparative Example 9 (total remineralization rate: 11.5%)
  • Example 10 (remineralization rate: 24.8%)
  • Comparative Example 4 and Comparative Example 11 (total remineralization rate: 13.2%)
  • Example 11 (remineralization rate: 20.7%)
  • Comparative Example 5 and Comparative Example 8 (total remineralization rate: 9.8%)
  • Example 12 (remineralization rate: 23.6%) and Comparative Example 6 and Comparative Example 12 (
  • the dentifrice composition of the present invention is very excellent in remineralization of teeth and has high industrial utility.

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Abstract

La présente invention vise à fournir d'une composition de dentifrice ayant un effet marqué de reminéralisation de l'émail dentaire décalcifié. La présente invention concerne une composition de dentifrice caractérisée en ce qu'elle comprend une composition de bleu d'outremer et un composant phosphate de calcium sélectionné parmi l'hydroxyapatite et le triphosphate de calcium.
PCT/JP2013/005778 2012-10-04 2013-09-27 Composition de dentifrice WO2014054257A1 (fr)

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JP2012222414A JP2014073989A (ja) 2012-10-04 2012-10-04 歯磨用組成物
JP2012-222414 2012-10-04

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2960007C (fr) 2015-01-16 2019-01-08 Kabushiki Kaisha Sangi Composition de dentifrice renfermant une cire et un phosphate de calcium
RU2018117868A (ru) * 2015-11-18 2019-12-18 Кабусики Кайся Санги Композиция для использования в полости рта

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH07223930A (ja) * 1994-02-10 1995-08-22 Sumitomo Osaka Cement Co Ltd 歯磨組成物
JPH09241138A (ja) * 1996-03-04 1997-09-16 Nippon Zetotsuku Kk 歯磨剤組成物
JP2002325557A (ja) * 2001-02-28 2002-11-12 Ezaki Glico Co Ltd 抗う蝕機能を有する組成物
JP2011051927A (ja) * 2009-09-01 2011-03-17 Sunstar Inc 口腔用組成物

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH07223930A (ja) * 1994-02-10 1995-08-22 Sumitomo Osaka Cement Co Ltd 歯磨組成物
JPH09241138A (ja) * 1996-03-04 1997-09-16 Nippon Zetotsuku Kk 歯磨剤組成物
JP2002325557A (ja) * 2001-02-28 2002-11-12 Ezaki Glico Co Ltd 抗う蝕機能を有する組成物
JP2011051927A (ja) * 2009-09-01 2011-03-17 Sunstar Inc 口腔用組成物

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
TAKEO MITSUI ET AL.: "Shin Keshohingaku", 2001, NANZANDO,, article TAKEO MITSUI ET AL., pages: 100 - 105 *

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