WO2017198399A1 - Composition de soin bucco-dentaire comprenant du silicate tricalcique - Google Patents

Composition de soin bucco-dentaire comprenant du silicate tricalcique Download PDF

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Publication number
WO2017198399A1
WO2017198399A1 PCT/EP2017/058967 EP2017058967W WO2017198399A1 WO 2017198399 A1 WO2017198399 A1 WO 2017198399A1 EP 2017058967 W EP2017058967 W EP 2017058967W WO 2017198399 A1 WO2017198399 A1 WO 2017198399A1
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WO
WIPO (PCT)
Prior art keywords
calcium
phosphate
oral care
care composition
source
Prior art date
Application number
PCT/EP2017/058967
Other languages
English (en)
Inventor
Xiaoke Li
Weining LIU
Jinfang Wang
Huaiyong XING
Original Assignee
Unilever N.V.
Unilever Plc
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 N.V., Unilever Plc, Conopco, Inc., D/B/A Unilever filed Critical Unilever N.V.
Priority to CN201780030939.4A priority Critical patent/CN109152707A/zh
Priority to BR112018072432A priority patent/BR112018072432A2/pt
Priority to EP17716282.3A priority patent/EP3458016A1/fr
Publication of WO2017198399A1 publication Critical patent/WO2017198399A1/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
    • A61K8/25—Silicon; Compounds 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
    • A61K8/19—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
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/20—Halogens; Compounds 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
    • A61K8/19—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 oral care compositions such as tooth pastes, powders, gums, mouthwashes and the like.
  • the present invention relates to an oral care composition comprising tricalcium silicate and a soluble calcium source that results in reducing sensitivity and/or remineralization of teeth.
  • the invention also relates to the use of such compositions for treating tooth hypersensitivity and/or remineralizing of teeth of an individual.
  • Tooth hypersensitivity is a temporary induced pain sensation that affects up to 20% of the adult population.
  • Hypersensitive teeth may be sensitive to temperature, pressure or chemical action.
  • the dentin of the tooth generally contains channels, called tubules, which provide for an osmotic flow between the inner pulp region of the tooth and the outer root surfaces.
  • Tooth hypersensitivity may be related to the general increase in exposed root surfaces of teeth as a result of periodontal disease, toothbrush abrasion, or cyclic loading fatigue of the thin enamel near the dentin-enamel junction. When root surfaces are exposed, dentinal tubules are also exposed.
  • tooth hypersensitivity is the hydrodynamic theory, based on the belief that open exposed dentinal tubules allow fluid flow through the tubules. This flow excites the nerve endings in the dental pulp.
  • Clinical replica of sensitive teeth viewed in a SEM (scanning electron microscopy) reveal varying numbers of open or partially occluded dentinal tubules.
  • tooth hypersensitivity There are different approaches to treat tooth hypersensitivity.
  • One approach is to reduce the excitability of the nerve in a sensitive tooth by using "nerve-depolarising agents" comprising strontium ions, potassium salts such as potassium nitrate, potassium bicarbonate, potassium chloride and the like. These nerve-depolarising agents function by interfering with neural transduction of the pain stimulus to make the nerve less sensitive.
  • tubule blocking agents that fully or partially occlude tubules such as polystyrene beads, apatite, polyacrylic acid, mineral hectorite clay and the like. These tubule blocking agents function by physically blocking the exposed ends of the dentinal tubules, thereby reducing dentinal fluid movement and reducing the irritation associated with the shear stress described by the hydrodynamic theory.
  • an oral care composition comprising tricalcium silicate, a soluble calcium source and a phosphate source provides excellent tubule blocking efficacy to reduce tooth sensitivity. Additionally, it has been further found that such oral care composition also shows excellent tooth remineralization efficacy.
  • WO 2008/068149 A discloses an oral care product comprising a first composition comprising an insoluble calcium salt that is not a calcium phosphate salt, a second independent composition comprising a source of phosphate ions, and a means for delivering each of the compositions to the surface of the teeth.
  • the preferred insoluble calcium salt is calcium silicate.
  • the additional information above does not describe an oral care composition comprising tricalcium silicate, a soluble calcium source and a phosphate source.
  • the oral care composition can treat tooth hypersensitivity and/or enhance tooth remineralization efficacy.
  • Tooth Paste for the purposes of the present invention means a paste, powder, liquid, gum or other preparation for cleaning the teeth or other surfaces in the oral cavity. Tooth Paste
  • Tooth paste for the purpose of the present invention means a paste or gel dentifrice for use with a toothbrush. Especially preferred are tooth pastes suitable for cleaning teeth by brushing for about two minutes.
  • Particle size for the purpose of the present invention means D50 particle size.
  • the D50 particle size of a particulate material is the particle size diameter at which 50 wt% of the particles are larger in diameter and 50 wt% are smaller in diameter.
  • particle sizes and distribution are measured using Malvern
  • Deposition aid for the purpose of the present invention means a material which aids deposition of actives such as tricalcium silicate and/or other benefit agents from the continuous phase of the composition onto the tooth surfaces during use of the
  • Benefit agents as used herein means an active typically delivered to human teeth and/or the oral cavity including the gums to enhance or improve a characteristic of those dental tissues.
  • pH is quoted at atmospheric pressure and a temperature of 25°C.
  • the pH may be measured by manually mixing 5 g oral care composition with 20 mL water for 30 s, then immediately testing the pH with indicator or a pH meter.
  • solubility means the solubility of a source (e.g., like calcium salts) in water at 25°C and atmospheric pressure.
  • Soluble means a source that dissolves in water to give a solution with a concentration of at least 0.1 moles per litre.
  • Insoluble means a source that dissolves in water to give a solution with a concentration of less than 0.001 moles per litre.
  • Separatingly soluble therefore, is defined to mean a source that dissolves in water to give a solution with a concentration of greater than 0.001 moles per litre and less than 0.1 moles per litre. Substantially Free
  • substantially free of for the purpose of the present invention means less than 1.5%, and preferably less than 1.0%, and more preferably less than 0.75% and more preferably still less than 0.5%, and even more preferably less than 0.1 % and most preferably from 0.0 to 0.01 % by weight, based on total weight of the oral care composition, including all ranges subsumed therein.
  • Double-Phase for the purpose of the present invention means a composition having two independent phases which are physically separate.
  • Anhydrous composition for the purpose of the present invention means the water content of the composition is less than 1 .5%, preferably from 0.0 to 0.75% by total weight of the oral care composition.
  • “Remineralization” for the purpose of the present invention means in situ (i.e. in the oral cavity) generation of calcium phosphate on teeth (including layers on teeth from 10 nm to 20 microns, and preferably from 75 nm to 10 microns, and most preferably, from 150 nm to 5 microns thick including all ranges subsumed therein) to reduce the likelihood of tooth sensitivity, tooth decay, regenerate enamel; and/or improve the appearance of teeth by whitening through the generation of such new calcium phosphate.
  • the present invention is directed to an oral care composition
  • an oral care composition comprising: a) tricalcium silicate
  • tricalcium silicate and the soluble calcium source is present in a weight ratio from 1 :3 to 20:1 .
  • the present invention is directed to a packaged oral care product comprising the oral care composition of the first aspect of this invention.
  • the present invention is directed to a method of reducing sensitivity and/or remineralization of teeth of an individual comprising the step of applying the oral care composition of any embodiment of the first aspect to at least one surface of the teeth of the individual.
  • an oral care composition comprising tricalcium silicate, a soluble calcium source and a phosphate source can efficiently seal exposed dentinal tubules, providing excellent tubule blocking efficacy to reduce tooth sensitivity.
  • Such oral care composition also shows excellent tooth remineralization efficacy.
  • Tricalcium silicate (CasSiOs), sometimes formulated as 3CaO-Si02, is a major constituent of Portland cement. Tricalcium silicate is very reactive due to its higher calcium content and the presence of an oxide ion in the lattice. It can react with water to produce calcium silicate hydrate (CSH) and calcium hydroxide. It reacts with water according to the reaction:
  • the tricalcium silicate suitable for use in the present invention is obtained from Kunshan Huaqiao New Materials Co., Ltd.
  • the tricalcium silicate may be crystalline or mesoporous.
  • the tricalcium silicate is preferably particulate as this allows for maximum surface area for contact with dental tissue.
  • the composition comprises particles comprising the tricalcium silicate.
  • Preferably from 10 to 100%, and especially, from 25 to 100%, and most especially, from 70% to 100% by weight of the particles comprising tricalcium silicate used in this invention have a particle size from 100 nm to less than 50 microns, preferably from 500 nm to 30 microns, more preferably from 700 nm to 20 microns, most preferably from 1 micron to 15 microns.
  • the particles comprising the tricalcium silicate may comprise other components, such as metal cations, anions (such as phosphate) and the like.
  • the particles comprise calcium oxide, silica in an amount of at least 70% by weight of the particles, more preferably at least 80%, more preferably still at least 90% and even more preferably at least 95%.
  • the particles consist of (or at least consist essentially of) calcium oxide, silica.
  • the oral care composition of the present invention comprises from 1 to 80% by weight of the tricalcium silicate, more preferably from 3 to 50%, most preferably from 5 to 30%, based on the total weight of the oral care composition and including all ranges subsumed therein.
  • the soluble calcium source suitable for use in this invention is limited only to the extent that the same may be used in the mouth.
  • Illustrative yet non-limiting examples of the types of soluble calcium source that may be used in this invention include, for example, calcium chloride, calcium nitrate, calcium acetate, calcium lactate, calcium gluconate, calcium formate, calcium malate, calcium propionate, calcium butyrate, calcium bicarbonate, calcium glycerophosphate, calcium ascorbate, mixtures thereof or the like.
  • the calcium source is calcium chloride, calcium nitrate or mixtures thereof.
  • the oral care composition of the present invention comprises from 0.1 to 20% by weight of the soluble calcium source, more preferably from 1 to 15%, most preferably from 2 to 10%, based on the total weight of the oral care composition and including all ranges subsumed therein.
  • the oral care composition preferably comprises the tricalcium silicate and the soluble calcium source in a weight ratio from 1 :5 to 20:1 , more preferably from 1 :3 to 20:1 , more preferably still from 1 :3 to 10:1 , most preferably from 1 :1.5 to 5:1 .
  • the phosphate source that may be used in this invention is limited only to the extent that the same may be used in a composition suitable for use in the mouth.
  • Illustrative examples of the types of phosphate source suitable for use in this invention include trisodium phosphate, monosodium dihydrogen phosphate, disodium hydrogen phosphate, ammonium phosphate, diammonium hydrogen phosphate, ammonium dihydrogen phosphate, tripotassium phosphate, monopotassium dihydrogen phosphate, dipotassium hydrogen phosphate, mixtures thereof or the like.
  • the phosphate source is preferably one which is water soluble.
  • the phosphate source When used, the phosphate source typically makes up from 0.5 to 40%, and more preferably from 1 to 30%, and most preferably, from 2 to 20% by weight of the oral care composition, based on total weight of the oral care composition and including all ranges subsumed therein.
  • the phosphate source used is trisodium phosphate and monosodium dihydrogen phosphate at a trisodium phosphate to monosodium dihydrogen phosphate weight ratio of 1 :4 to 4:1 , preferably 1 :3 to 3:1 , and most preferably, from 1 :2 to 2:1 , including all ratios subsumed therein.
  • the phosphate source used is or at least comprises monosodium dihydrogen phosphate.
  • the oral care composition of the present invention is found to be effective in blocking dentinal tubules to reduce tooth sensitivity and inducing new hydroxyapatite layer formation on enamel surface.
  • the present inventors believe that the presence of soluble calcium source increases the calcium ion concentration in the oral composition, which enhances the reaction between the calcium salts and phosphate source in the mouth to form calcium phosphate.
  • the calcium phosphate precipitation can help the deposition of tricalcium silicate particles on surfaces of dentine and/or enamel.
  • the tricalcium silicate may further release calcium ions sustainably to react with phosphate source in the saliva and/or Si-OH groups of tricalcium silicate may have an affinity for Ca ions in teeth, which further enhances the tubule blocking efficacy and/or tooth remineralization efficacy.
  • the oral care composition of the present invention may further comprise a deposition aid.
  • the deposition aid suitable for use in this invention is limited only to the extent that the same may be used in the mouth.
  • the deposition aid provides plenty of calcium ions in the mouth and is inexpensive and abundant.
  • the deposition aid is calcium salts in addition to the soluble calcium source which is included in the composition.
  • Illustrative yet non-limiting examples of the types of deposition aid that may be used in this invention include, for example, calcium sulfate hemihydrate, calcium dihydrogen phosphate, calcium aluminate, calcium monohydrogen phosphate or mixtures thereof or the like.
  • the deposition aid is calcium dihydrogen phosphate, calcium sulfate hemihydrates or mixtures thereof.
  • the materials used as deposition aids in this invention is biocompatible, and undergoes rapid reaction with water and complete resorption onto the tooth surface, therefore it can be used to aid the deposition of oral care actives such as tricalcium silicate and/or other benefit agents onto the tooth surface.
  • the oral care composition of the present invention comprises from 0.1 to 20% by weight of the deposition aid, more preferably from 0.2 to 15%, more preferably still from 0.5 to 10%, most preferably from 1 to 5%, based on the total weight of the oral care composition and including all ranges subsumed therein.
  • the oral care composition preferably comprises the tricalcium silicate and the deposition aid in a weight ratio from 20:1 to 1 :5, more preferably from 15:1 to 1 :3, most preferably from 10:1 to 1 :1 .
  • the composition of the present invention is an oral care composition and typically comprises physiologically acceptable carrier.
  • the carrier preferably comprises at least surfactant, thickener, humectant or a combination thereof.
  • the oral care composition comprises a surfactant.
  • the composition comprises at least 0.01 % surfactant by weight of the composition, more preferably at least 0.1 % and most preferably from 0.5 to 7%.
  • Suitable surfactants include anionic surfactants, such as the sodium, magnesium, ammonium or ethanolamine salts of Cs to Ci8 alkyl sulphates (for example sodium lauryl sulphate), Cs to Cis alkyl sulphosuccinates (for example dioctyl sodium sulphosuccinate), Cs to Cis alkyl sulphoacetates (such as sodium lauryl sulphoacetate), Cs to Cis alkyl sarcosinates (such as sodium lauryl sarcosinate), Cs to Cis alkyl phosphates (which can optionally comprise up to 10 ethylene oxide and/or propylene oxide units) and sulphated monoglycerides.
  • anionic surfactants such as the sodium, magnesium, ammonium or ethanolamine salts of Cs to Ci8 alkyl sulphates (for example sodium lauryl sulphate), Cs to Cis alkyl sulphosuccinates (
  • surfactants include nonionic surfactants, such as optionally polyethoxylated fatty acid sorbitan esters, ethoxylated fatty acids, esters of polyethylene glycol, ethoxylates of fatty acid monoglycerides and diglycerides, and ethylene oxide/propylene oxide block polymers.
  • suitable surfactants include amphoteric surfactants, such as betaines or sulphobetaines. Mixtures of any of the above described materials may also be used. More preferably the surfactant comprises or is anionic surfactant.
  • the preferred anionic surfactants are sodium lauryl sulphate and/or sodium dodecylbenzene sulfonate. Most preferably the surfactant is sodium lauryl sulphate.
  • Thickener may also be used in this invention and is limited only to the extent that the same may be added to a composition suitable for use in the mouth.
  • Illustrative examples of the types of thickeners that may be used in this invention include, sodium
  • SCMC carboxymethyl cellulose
  • silica based thickeners including silica aerogels, magnesium aluminum silicate (e.g., Veegum), Carbomers (cross-linked acrylates) and mixtures thereof.
  • xanthan gum and/or sodium carboxymethyl cellulose and/or a Carbomer is/are preferred.
  • a Carbomer those having a weight-average molecular weight of at least 700,000 are desired, and preferably, those having a molecular weight of at least 1 ,200,000, and most preferably, those having a molecular weight of at least about 2,500,000 are desired. Mixtures of Carbomers may also be used herein.
  • the Carbomer is Synthalen PNC, Synthalen KP or a mixture thereof. It has been described as a high molecular weight and cross-linked polyacrylic acid and identified via CAS number 9063-87-0. These types of materials are available commercially from suppliers like Sigma.
  • the sodium carboxymethyl cellulose (SCMC) used is SCMC 9H. It has been described as a sodium salt of a cellulose derivative with carboxymethyl groups bound to hydroxy groups of glucopyranose backbone monomers and identified via CAS number 9004-32-4. The same is available from suppliers like Alfa Chem.
  • the thickener is xanthan gum.
  • Thickener typically makes up from 0.01 to about 10%, more preferably from 0.1 to 9%, and most preferably, from 1 .5 to 8% by weight of the oral care composition, based on total weight of the composition and including all ranges subsumed therein.
  • the oral care composition of this invention is a toothpaste or gel, the same typically has a viscosity from about 30,000 to 180,000 centipoise, and preferably, from 60,000 to 170,000 centipoise, and most preferably, from 65,000 to 165,000 centipoise.
  • Suitable humectants are preferably used in the oral care composition of the present invention and they include, for example, glycerin, sorbitol, propylene glycol, dipropylene glycol, diglycerol, triacetin, mineral oil, polyethylene glycol (preferably, PEG-400), alkane diols like butane diol and hexanediol, ethanol, pentylene glycol, or a mixture thereof. Glycerin, polyethylene glycol, sorbitol or mixtures thereof are the preferred humectants.
  • the humectant may be present in the range of from 10 to 90% by weight of the oral care composition.
  • the carrier humectant makes up from 25 to 80%, and most preferably, from 45 to 70% by weight of the composition, based on total weight of the composition and including all ranges subsumed therein.
  • the oral care composition of the present invention may contain a variety of other ingredients which are common in the art to enhance physical properties and performance.
  • ingredients include antimicrobial agents, anti-inflammatory agents, anti-caries agents, plaque buffers, fluoride sources, vitamins, plant extracts, desensitizing agents, anti-calculus agents, biomolecules, flavors, proteinaceous materials, preservatives, opacifying agents, coloring agents, pH-adjusting agents, sweetening agents, particulate abrasive materials, polymeric compounds, buffers and salts to buffer the pH and ionic strength of the compositions, and mixtures thereof.
  • Such ingredients typically and collectively make-up less than 20% by weight of the composition, and preferably, from 0.0 to 15% by weight, and most preferably, from 0.01 to 12% by weight of the composition, including all ranges subsumed therein.
  • the oral care composition of this invention can be used in a method of reducing sensitivity and/or remineralizing of teeth of an individual comprising applying the composition to at least one surface of the teeth of an individual.
  • composition of this invention may additionally or alternatively be for use as a medicament and/or used in the manufacture of a medicament for providing an oral care benefit as described herein, such as for reducing sensitivity of the teeth of an individual.
  • the use is non-therapeutic.
  • the oral care composition is substantially free of water to prevent the premature reaction between the calcium salts and the phosphate source.
  • the oral care composition is a monophase anhydrous composition.
  • the oral care composition is a dual-phase composition comprising a calcium phase and a phosphate phase, wherein the tricalcium silicate and the soluble calcium source are present in the calcium phase and the phosphate source is present in the phosphate phase.
  • the two phases are physically separate from one another by being in independent phases.
  • the delivery of the two independent phases to the teeth may be simultaneous or sequential. In a preferred embodiment, the phases are delivered simultaneously.
  • the dual-phase composition is delivered by a dual-tube having a first compartment for calcium phase and a second compartment for phosphate phase, which allows for co-extrusion of the two phases.
  • such a dual-tube has one of the compartments surrounding the other.
  • one phase is present as a sheath, surrounding the other phase in the core.
  • the core is the calcium phase and the sheath is the phosphate phase.
  • such a dual-tube has the two compartments side by side within the same tube.
  • the two phases are extruded from the tube as one, such extrusion being termed "contact extrusion".
  • a pump head may be used in such a dual-tube for squeezing the two phases from the tube as one.
  • the dual-phase oral care composition may be a gel composition that comprises two independent gel phases, the first is the calcium phase and the second is the phosphate phase.
  • the means of delivery may involve a cotton rod, or a tray, onto which the calcium phase and the phosphate phase are applied, prior to the tray being placed in contact with the teeth.
  • the composition will be packaged.
  • tooth paste or gel form the composition may be packaged in a conventional plastic laminate, metal tube or a single compartment dispenser. The same may be applied to dental surfaces by any physical means, such as a toothbrush, fingertip or by an applicator directly to the sensitive area.
  • the composition can be effective even when used in an individual's daily oral hygiene routine.
  • the composition may be brushed onto the teeth.
  • the composition may, for example, be contacted with the teeth for a time period of one second to 20 hours. More preferably from 1 s to 10 hours, more preferably still from 10 s to 1 hour and most preferably from 30 s to 5 minutes.
  • the composition may be used daily, for example for use by an individual once, twice or three times per day.
  • the oral care composition is a dual-phase composition
  • the two phases of the composition are mixed during application.
  • the mixed phases are typically left on the teeth for from 3 minutes to 10 hours, more preferably from 3 minutes to 8 hours.
  • the application may be carried out daily.
  • This example demonstrates the improved blockage of dentinal tubules by using soluble calcium source in combination with tricalcium silicate. All ingredients are expressed by weight percent of the total formulation, and as level of active ingredient.
  • test samples was mixed with water at a ratio of 1 g to 2 mL water to make a slurry.
  • Sample 1 comprising only tricalcium silicate was used as control.
  • Human dentine disks were eroded by 37% phosphoric acid for 1 min, then they were treated with different slurries via brushing following the same protocol.
  • SOF simulated oral fluid
  • the dentine disks were brushed with the slurry by machine using the same procedure as in the first step. The brushing was repeated three times for one day, then the dentine disks were kept in SOF overnight (>12 hours) in a shaking water bath at 37°C to mimic oral environment. The dentine samples were brushed for 3 times.
  • a square (with a size of 4mm x 4mm) is selected and one image is captured under 50x magnification. Within this square, five spots (each with a size of 150 ⁇ x 150 ⁇ , one in the middle, and one in every corner) are selected and observed under 1000x magnification.
  • the blockage of tubules are accessed following the standards described in Table 3. The measurement is carried out for the two dentine disks of each test group.
  • CaSiC calcium silicate
  • Example 2 The same protocol was used to evaluate the blockage efficacy of dentinal tubules as described in Example 1 .
  • the dentine samples were brushed for 3 and 7 times.
  • Sample 6 comprising a combination of tricalcium silicate and calcium chloride showed significantly better tubule blockage efficacy compared to Sample 8 comprising a combination of calcium silicate and calcium chloride. Both of Samples 6 and 8 showed superior tubule blockage efficacy to Samples 5 and 7 comprising no calcium chloride.
  • This example demonstrates the improved blockage of dentinal tubules by using soluble calcium source in combination with calcium silicate in full formulations. All ingredients are expressed by weight percent of the total formulation, and as level of active ingredient.
  • Example 2 The same protocol was used to evaluate the blockage efficacy of dentinal tubules as described in Example 1 .
  • the dentine samples were brushed for 3 and 7 times.
  • test sample was mixed with water at a ratio of 1 g to 2 mL water to make a toothpaste slurry.
  • the bovine enamel blocks were treated with different slurries via brushing following the same protocol.
  • the enamel blocks were brushed with the slurry under a tooth brushing machine equipped with toothbrushes.
  • the load of the tooth brushing was 170 g +1-5 g and the automatic brushing operated at a speed of 150 rpm.
  • the enamel blocks were soaked in toothpaste slurry for 1 min.
  • the enamel blocks were rinsed with distilled water and placed in SOF under the condition of a shaking water bath at 37°C and 60.0 rpm.
  • the enamel blocks were brushed with the slurry by machine using the same procedure as in the first step.
  • the brushing was repeated three times for one day, then the enamel blocks were kept in SOF overnight(>12 hours) in a shaking water bath at 37°C to mimic oral environment.
  • the enamel blocks were brushed for 7 times.
  • Samples 14 comprising a combination of 5% of calcium chloride and 10% tricalcium silicate showed significantly better tubule blockage efficacy compared to Sample 15 comprising a combination of 10% of calcium chloride and 5% tricalcium silicate. Both of Samples 14 and 15 showed significantly better tubule blockage efficacy compared to Samples 13 and 17 comprising only tricalcium silicate or calcium chloride respectively.
  • Sample 14 After 3 brushings, Sample 14 also showed comparable tubule blockage efficacy compared to Samples 18 and 19 comprising a higher amount of tricalcium silicate. SEM images clearly showed that all the dentinal tubules were extensively blocked.

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Abstract

L'invention concerne une composition de soin bucco-dentaire comprenant du silicate tricalcique, une source de calcium soluble, une source de phosphate et un support physiologiquement acceptable, le silicate tricalcique et la source de calcium soluble étant présents dans un rapport en poids de 1:3 à 20:1.
PCT/EP2017/058967 2016-05-19 2017-04-13 Composition de soin bucco-dentaire comprenant du silicate tricalcique WO2017198399A1 (fr)

Priority Applications (3)

Application Number Priority Date Filing Date Title
CN201780030939.4A CN109152707A (zh) 2016-05-19 2017-04-13 包含硅酸三钙的口腔护理组合物
BR112018072432A BR112018072432A2 (pt) 2016-05-19 2017-04-13 composição para os cuidados orais e método para a redução da sensibilidade e/ou remineralização dos dentes
EP17716282.3A EP3458016A1 (fr) 2016-05-19 2017-04-13 Composition de soin bucco-dentaire comprenant du silicate tricalcique

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
CN2016082594 2016-05-19
CNPCT/CN2016/082594 2016-05-19
EP16176567 2016-06-28
EPEP16176567.2 2016-06-28

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115666729A (zh) * 2020-05-21 2023-01-31 联合利华知识产权控股有限公司 口腔护理组合物

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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