WO2023213460A1 - Composition de soin buccodentaire - Google Patents

Composition de soin buccodentaire Download PDF

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Publication number
WO2023213460A1
WO2023213460A1 PCT/EP2023/055199 EP2023055199W WO2023213460A1 WO 2023213460 A1 WO2023213460 A1 WO 2023213460A1 EP 2023055199 W EP2023055199 W EP 2023055199W WO 2023213460 A1 WO2023213460 A1 WO 2023213460A1
Authority
WO
WIPO (PCT)
Prior art keywords
oral care
care composition
composition according
composition
carrageenan
Prior art date
Application number
PCT/EP2023/055199
Other languages
English (en)
Inventor
Stuart Anthony Barnett
Andrew Joiner
Sarah Louise GILLIGAN
Original Assignee
Unilever Ip Holdings B.V.
Unilever Global Ip Limited
Conopco, Inc., D/B/A Unilever
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 Unilever Ip Holdings B.V., Unilever Global Ip Limited, Conopco, Inc., D/B/A Unilever filed Critical Unilever Ip Holdings B.V.
Publication of WO2023213460A1 publication Critical patent/WO2023213460A1/fr

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Classifications

    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/24Phosphorous; Compounds thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/25Silicon; Compounds thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics 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
    • A61K8/34Alcohols
    • A61K8/345Alcohols containing more than one hydroxy group
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/72Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/73Polysaccharides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/59Mixtures
    • A61K2800/592Mixtures of compounds complementing their respective functions
    • A61K2800/5922At least two compounds being classified in the same subclass of A61K8/18

Definitions

  • the present invention relates to oral care compositions such as toothpastes, powders, gums, mouthwashes and the like.
  • oral care compositions particularly toothpastes that are effective in mitigating the effects of gastric acid erosion on tooth enamel.
  • Gastric acid reflux can lead to chemical erosion of dental enamel, as a result the teeth can appear yellow due to increased dentin visibility and sensitivity problems can arise due to increased exposure of the dentin tubules.
  • WO20131616 relates to a method of preventing dental erosion by combinations of a basic amino acid and one or more sources of zinc.
  • the present invention relates to an oral care composition
  • an oral care composition comprising: a) from 20 to 90wt% of the total composition of one or more organic polyols having 3 or more hydroxyl groups in the molecule b) calcium silicate c) a potassium phosphate salt d) mono calcium phosphate e) xanthan gum; and f) carrageenan
  • the invention in a second aspect relates to an oral care composition as described above for use in a method to mitigate erosion of tooth enamel by gastric acid.
  • composition of the invention is used to preferably used to clean the surfaces of the oral cavity and is known as an oral care composition.
  • compositions of the invention are those which are suitable for brushing and/or rinsing the surfaces of the oral cavity.
  • the composition of the invention is most preferably in the form of a dentifrice.
  • dentifrice denotes an oral composition which is used to clean the surfaces of the oral cavity. Such a composition is not intentionally swallowed for purposes of systemic administration of therapeutic agents, but is applied to the oral cavity, used to treat the oral cavity and then expectorated. Typically such a composition is used in conjunction with a cleaning implement such as a toothbrush, usually by applying it to the bristles of the toothbrush and then brushing the accessible surfaces of the oral cavity.
  • the dentifrice/toothpaste is in the form of an extrudable semi-solid such as a cream, paste or gel (or mixture thereof). Toothpastes are particularly preferred.
  • Compositions according to the thein invention comprise mono calcium phosphate.
  • the monocalcium phosphate is present at levels from 0.1 to 10 wt% of the total composition, more preferably 1 to 6 wt%.
  • compositions of the invention comprise from 20 to 90 wt% of the total composition of one or more organic polyols having 3 or more hydroxyl groups in the molecule.
  • organic polyol is glycerol.
  • compositions of the invention include agents for the remineralisation of teeth.
  • remineralisation in the context of the present invention means the in-situ generation of hydroxyapatite on teeth.
  • compositions according to the invention comprise a suitable agent for the remineralisation of teeth this a mixture of a calcium silicate and a sodium phosphate salt which, when delivered to the teeth results in the in situ generation of hydroxyapatite on teeth.
  • the amount of remineralising calcium source(s) (e.g. calcium silicate) in the composition of the invention typically ranges from 1 to 30%, preferably from 5 to 20% by total weight remineralising calcium source based on the total weight of the oral care composition.
  • remineralising phosphate sources include, for example, monosodium dihydrogen phosphate, disodium hydrogen phosphate, sodium pyrophosphate, tetrasodium pyrophosphate, sodium tripolyphosphate, sodium hexametaphosphate, potassium dihydrogenphosphate, trisodium phosphate, tripotassium phosphate and mixtures thereof.
  • the remineralising phosphate source is a mixture of trisodium phosphate and sodium dihydrogen phosphate.
  • the amount of remineralising phosphate source(s) (e.g. trisodium phosphate and sodium dihydrogen phosphate) in the composition of this invention typically ranges from 2 to 15%, preferably from 4 to 10% by total weight re-mineralising phosphate source based on the total weight of the oral care composition.
  • compositions according to the invention further comprise xanthan gum and carrageenan.
  • carrageenan is either iota or kappa carrageenan, a mixture of the two being particularly preferred. It is preferred if the level of xanthan gum is from 0.1 to 0.9wt% of the total composition.
  • the level of carrageenan is from is from 0.1 to 0.9wt% of the total composition.
  • the weight ratio of xanthan gum to carrageenan is from 1 :2 to 2: 1.
  • the composition comprises from 0.2 to 5wt% of the total composition of one or more surfactants, such as anionic, nonionic, cationic and zwitterionic or amphoteric surfactants.
  • a preferred surfactant is a taurate, in particular sodium methyl cocoyl taurate.
  • a composition according to the invention (such as a dentifrice/toothpaste) will generally contain further ingredients to enhance performance and/or consumer acceptability, in addition to the ingredients specified above.
  • Compositions according to the invention preferably comprise particulate abrasive materials such as silicas, aluminas, calcium carbonates, dicalciumphosphates, calcium pyrophosphates, hydroxyapatites, trimetaphosphates, insoluble hexametaphosphates and so on, including agglomerated particulate abrasive materials, usually in amounts between 3 and 60% by weight of the oral care composition.
  • particulate abrasive materials such as silicas, aluminas, calcium carbonates, dicalciumphosphates, calcium pyrophosphates, hydroxyapatites, trimetaphosphates, insoluble hexametaphosphates and so on, including agglomerated particulate abrasive materials, usually in amounts between 3 and 60% by weight of the oral care composition.
  • the composition particularly a toothpaste, comprises a silica based abrasive.
  • the preferred abrasive silicas used in the present invention is a silica with a low refractive index. It may be used as the sole abrasive silica, or in conjunction with a low level of other abrasive silicas, e.g. those according to EP 236070.
  • the low refractive index silicas, used as abrasives in the present invention are preferably silicas with an apparent refractive index (R.l.) in the range of 1.41 - 1 .47, preferably 1.435 - 1.445, preferably having a weight mean particle size of between 5 and 15 mm, a BET (nitrogen) surface area of between 10 and 100 m 2 /g and an oil absorption of about 70 - 150 cm 3 /100 g, but abrasive silicas with a lower apparent refractive index may also be used.
  • suitable low refractive index abrasive silicas e.g. having an R.l.
  • silicas of between 1.435 and 1.445 are Tixosil 63 and 73 ex Rhone Poulenc; Sident 10 ex Degussa; Zeodent 113 ex Zeofinn; Zeodent 124 ex Evonik, Sorbosil AC 77 ex PQ Corporation (having an R.l. of approximately 1 .440).
  • the amount of these silicas in the composition generally ranges from 5-60% by weight, usually 5- 20% by weight.
  • composition particularly if a toothpaste preferably comprises an inorganic or a natural or synthetic thickener or gelling agent in proportions of about 0.10 to about 15% by weight depending on the material chosen.
  • thickeners in the dentifrice compositions of the present invention form an extrudable, shape-retaining product which can be squeezed from a tube onto a toothbrush and will not fall between the bristles of the brush but rather, will substantially maintain its shape thereon.
  • Suitable thickeners or gelling agents useful in the practice of the present invention include inorganic thickening silicas such as amorphous silicas available from Evonik under the trade designation Zeodent 165, Irish moss, iota-carrageenan, gum tragacanth, and polyvinylpyrrolidone.
  • inorganic thickening silicas such as amorphous silicas available from Evonik under the trade designation Zeodent 165, Irish moss, iota-carrageenan, gum tragacanth, and polyvinylpyrrolidone.
  • compositions according to the invention preferably comprise a polymeric deposition aid.
  • the composition comprises acid anhydride polymers, particularly preferred are co-polymers of maleic anhydride with methyl vinylether, in which the anhydride moiety may be in a partially or folly hydrolysed or alcoholysed form.
  • Preferred copolymers include Gantrez(R) polymers such as: Gantrez S-95: molecular weight 216,000; free acid;
  • Gantrez S-96 molecular weight 700,000; free acid
  • Gantrez S-97 molecular weight 1 ,500,000; free acid
  • Gantrez MS-955 molecular weight 1,060,000; calcium/sodium salt.
  • Particularly preferred co-polymers of maleic acid and methyl vinylether have a molecular weight of 1 ,000,000 or greater and an especially preferred material is Gantrez S-97.
  • compositions according to the invention may comprise a tooth whitening agent.
  • the whitening agent preferably comprises a green and/or a blue pigment.
  • a pigment is generally understood to be a shade/material which is insoluble in the relevant medium, at the relevant temperature. This is in contrast to dyes which are soluble.
  • the "relevant medium” is human saliva, the liquid medium in which the composition is used, at the temperature of the oral cavity during brushing of the teeth, i.e. up to 37 Degrees C. As a reasonable approximation, the relevant medium may be considered to be water and the relevant temperature to be 25 Degrees C.
  • the blue pigment is Pigment Blue 15, more preferably Pigment Blue 15:1, 15:2, 15:3, 15:4, 15:5 or 15:6, most preferably 15:1.
  • a preferred pigment is blue pigment is Phthalocyanine Blue Pigment, Cl No. 74160, blue covarine.
  • the preferred Green pigment is Phthalocyanine Green, preferably Phthalocyanine Green CI-74260.
  • the total level of pigment in the composition is from 0.01 wt% to 3 wt%, more preferably from 0.02 to 2 wt%. If the composition is a toothpaste it may be a dual phase paste, with the whitening pigments present in one phase.
  • compositions according to the invention may comprise water-soluble or sparingly water-soluble sources of metal salts
  • zinc ions such as zinc chloride, zinc acetate, zinc gluconate, zinc sulphate, zinc fluoride, zinc citrate, zinc lactate, zinc oxide, zinc monoglycerolate, zinc tartrate, zinc pyrophosphate and zinc maleate
  • stannous ions such as stannous fluoride and stannous chloride.
  • compositions according to the invention may comprise oral care enzyme systems such as hydrogen peroxide producing enzyme systems (e.g. the oxidoreductase enzyme glucose oxidase), amyloglucosidase, dextranase and/or mutanase, (optionally in the presence of zinc ion providing compounds and/or 8- hydroxyquinoline derivatives), lactoperoxidase, lactoferrin, lysozyme and mixtures thereof.
  • hydrogen peroxide producing enzyme systems e.g. the oxidoreductase enzyme glucose oxidase
  • amyloglucosidase e.g. the oxidoreductase enzyme glucose oxidase
  • dextranase and/or mutanase e.g. the oxidoreductase enzyme glucose oxidase
  • mutanase e.g. the mutanase
  • lactoperoxidase e.g. the
  • Compositions of the invention may comprise fluoride sources such as sodium fluoride, stannous fluoride, sodium monofluorophosphate, zinc ammonium fluoride, tin ammonium fluoride, calcium fluoride, cobalt ammonium fluoride and mixtures thereof.
  • fluoride sources such as sodium fluoride, stannous fluoride, sodium monofluorophosphate, zinc ammonium fluoride, tin ammonium fluoride, calcium fluoride, cobalt ammonium fluoride and mixtures thereof.
  • composition according to the invention will comprise further ingredients which are common in the art, such as: antimicrobial agents, e.g. chlorhexidine, sanguinarine extract, metronidazole, quaternary ammonium compounds, such as cetylpyridinium chloride; bis-guanides, such as chlorhexidine digluconate, hexetidine, octenidine, alexidine; and halogenated bisphenolic compounds, such as 2,2' methylenebis-(4-chloro-6-bromophenol); anti-inflammatory agents such as ibuprofen, flurbiprofen, aspirin, indomethacin etc.; anti-caries agents such as sodium- and stannous fluoride, aminefluorides, sodium monofluorophosphate, sodium trimeta phosphate and casein; plaque buffers such as urea, calcium lactate, calcium glycerophosphate and strontium polyacrylates; vitamins such as Vitamins A, C and E; plant extracts; plant
  • Humectants such as glycerol, sorbitol, propyleneglycol, xylitol, lactitol etc.; binders and thickeners such as sodium carboxymethyl-cellulose, hydroxyethyl cellulose (Natrosol®), xanthan gum, gum arabic etc. as well as synthetic polymers such as polyacrylates and carboxyvinyl polymers such as Carbopol®; polymeric compounds which can enhance the delivery of active ingredients such as antimicrobial agents can also be included; buffers and salts to buffer the pH and ionic strength of the oral care composition; and other optional ingredients that may be included are e.g. bleaching agents such as peroxy compounds e.g. potassium peroxydiphosphate, effervescing systems such as sodium bicarbonate/citric acid systems, colour change systems, and so on.
  • bleaching agents such as peroxy compounds e.g. potassium peroxydiphosphate, effervescing systems such as sodium bicarbonate/c
  • enamel specimens were exposed to a cycle of treatments as follows: (1) toothpaste in the form of a 1:2 slurry with deionised water for 2mins; (2) rinsed with deionised water; (3) exposure to artificial saliva for2hours (pH7.0, 1.5mM calcium chloride, 0.9mM potassium dihydrogenphosphate, 20mM HEPES, 130mM potassium chloride); (4) exposure to gastric acid solution for 30s (pH2.3, 10mM hydrochloric acid); (5) rinsed with deionised water.
  • Enamel SMH was remeasured after 2 and 4 treatment cycles. The mean enamel SMH was calculated for each specimen and the % change in enamel SMH was calculated using: 100 The overall mean % change SMH was calculated for each treatment group and time point.
  • Example 1 delivers significantly greater protection against gastric acid challenges than Example A.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Birds (AREA)
  • Chemical & Material Sciences (AREA)
  • Inorganic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Emergency Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Oral & Maxillofacial Surgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Cosmetics (AREA)

Abstract

L'invention concerne une composition de soin buccodentaire comprenant : a) de 20 à 90 % en poids de la composition totale d'un ou de plusieurs polyols organiques ayant 3 groupes hydroxyles ou plus dans la molécule ; b) du silicate de calcium ; c) un sel de phosphate de sodium ; d) du phosphate de monocalcium ; e) de la gomme xanthane ; f) du carraghénane.
PCT/EP2023/055199 2022-05-03 2023-03-01 Composition de soin buccodentaire WO2023213460A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP22171331 2022-05-03
EP22171331.6 2022-05-03

Publications (1)

Publication Number Publication Date
WO2023213460A1 true WO2023213460A1 (fr) 2023-11-09

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Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020131616A1 (fr) 2018-12-20 2020-06-25 Colgate-Palmolive Company Composition de soin buccodentaire comprenant du zinc et un acide aminé pour le traitement de symptômes d'un trouble gastrique dans la cavité buccale

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020131616A1 (fr) 2018-12-20 2020-06-25 Colgate-Palmolive Company Composition de soin buccodentaire comprenant du zinc et un acide aminé pour le traitement de symptômes d'un trouble gastrique dans la cavité buccale

Non-Patent Citations (7)

* Cited by examiner, † Cited by third party
Title
CHANGYU SHAO ET AL: "Repair of tooth enamel by a biomimetic mineralization frontier ensuring epitaxial growth", SCIENCE ADVANCES, vol. 5, no. 8, 1 August 2019 (2019-08-01), pages eaaw9569 - 30, XP055646890, DOI: 10.1126/sciadv.aaw9569 *
DATABASE GNPD [online] MINTEL; February 2015 (2015-02-01), "Fluoride Toothpaste with Enamel Shield", XP002809232, Database accession no. 2995071 *
DATABASE GNPD [online] MINTEL; February 2022 (2022-02-01), "Gentle Mint Flavoured Fluoride Toothpaste", XP002809231, Database accession no. 9409368 *
DATABASE GNPD [online] MINTEL; May 2011 (2011-05-01), "Iso-Active Foaming Gel", XP002809233, Database accession no. 1537904 *
DATABASE GNPD [online] MINTEL; September 2021 (2021-09-01), "Advanced Toothpaste", XP002809230, Database accession no. 9029750 *
REUSSNER G H ET AL: "EFFECTS OF PHOSPHATES IN ACID-CONTAINING BEVERAGES ON TOOTH EROSION", JOURNAL OF DENTAL RESEARCH, INTERNATIONAL ASSOCIATION FOR DENTAL RESEARCH, US, vol. 54, no. 2, 1 March 1975 (1975-03-01), pages 365 - 370, XP000999505, ISSN: 0022-0345 *
VRANIC EDINA ET AL: "Formulation ingredients for toothpastes and mouthwashes.", BOSNIAN JOURNAL OF BASIC MEDICAL SCIENCES OCT 2004, vol. 4, no. 4, October 2004 (2004-10-01), pages 51 - 58, XP002809234, ISSN: 1512-8601 *

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