WO2014124950A1 - Nouvelle composition - Google Patents

Nouvelle composition Download PDF

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Publication number
WO2014124950A1
WO2014124950A1 PCT/EP2014/052689 EP2014052689W WO2014124950A1 WO 2014124950 A1 WO2014124950 A1 WO 2014124950A1 EP 2014052689 W EP2014052689 W EP 2014052689W WO 2014124950 A1 WO2014124950 A1 WO 2014124950A1
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WO
WIPO (PCT)
Prior art keywords
fluoride
calcium
ppm
phosphate
composition according
Prior art date
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PCT/EP2014/052689
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English (en)
Inventor
Christabel Fowler
Robert KARLINSEY
Original Assignee
Glaxo Group Limited
Indiana Nanotech Llc
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Filing date
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Application filed by Glaxo Group Limited, Indiana Nanotech Llc filed Critical Glaxo Group Limited
Publication of WO2014124950A1 publication Critical patent/WO2014124950A1/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
    • 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
    • A61K8/21—Fluorides; Derivatives 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 an aqueous single phase oral care composition
  • a fluoride salt and a catalytic and fluoride-stable amount of a calcium phosphate compound, which is not ⁇ -tricalcium phosphate.
  • the calcium phosphate compound is present in an amount sufficient to increase the efficacy of fluoride ions in strengthening dental enamel of teeth against acidic challenges, whilst not significantly compromising the long term storage stability of the fluoride ions in the oral care composition.
  • Such compositions are of use in combating (i.e. helping to prevent, inhibit and/or treat) dental erosion and/or tooth wear.
  • Such compositions are of use in combating dental and/or root caries.
  • Such compositions are of use in combating dentine hypersensitivity.
  • Tooth mineral is composed predominantly of calcium hydroxyapatite, Cai 0 (PO 4 )6(OH) 2 , which may be partially substituted with anions such as carbonate or fluoride, and cations such as zinc or magnesium. Tooth mineral may also contain non-apatitic mineral phases such as octacalcium phosphate and calcium carbonate. Tooth loss may occur as a result of dental caries, which is a multifactorial disease where bacterial acids such as lactic acid produce sub-surface demineralisation that does not fully remineralise, resulting in progressive tissue loss and eventually cavity formation. The presence of a plaque biofilm is a prerequisite for dental caries, and acidogenic bacteria such as Streptococcus mutans may become pathogenic when levels of easily fermentable carbohydrate, such as sucrose, are elevated for extended periods of time.
  • acidogenic bacteria such as Streptococcus mutans may become pathogenic when levels of easily fermentable carbohydrate, such as sucrose, are elevated for extended periods of time.
  • Dental erosion i.e. acid erosion or acid wear
  • acid erosion is a surface phenomenon that involves demineralisation, and ultimately complete dissolution of the tooth surface by acids that are not of bacterial origin.
  • the acid will be of dietary origin, such as citric acid from fruit or carbonated drinks, phosphoric acid from cola drinks and acetic acid such as from vinaigrette.
  • Dental erosion may also be caused by repeated contact with hydrochloric acid (HCl) produced in the stomach, which may enter the oral cavity through an involuntary response such as gastroesophageal reflux, or through an induced response as may be encountered in sufferers of bulimia.
  • HCl hydrochloric acid
  • Tooth wear ie physical tooth wear
  • Attrition occurs when tooth surfaces rub against each other, a form of two -body wear.
  • An often dramatic example is that observed in subjects with bruxism, a grinding habit where the applied forces are high, and is characterised by accelerated wear, particularly on the occlusal surfaces.
  • Abrasion typically occurs as a result of three-body wear and the most common example is that associated with brushing with a toothpaste.
  • levels of wear caused by commercially available toothpastes are minimal and of little or no clinical consequence.
  • enamel has been demineralised and softened by exposure to an erosive challenge, the enamel becomes more susceptible to tooth wear.
  • Dentine is much softer than enamel and consequently is more susceptible to wear. Subjects with exposed dentine should avoid the use of highly abrasive toothpastes, such as those based on alumina. Again, softening of dentine by an erosive challenge will increase susceptibility of the tissue to wear.
  • Dentine is a vital tissue that in vivo is normally covered by enamel or cementum depending on the location i.e. crown versus root respectively. Dentine has a much higher organic content than enamel and its structure is characterised by the presence of fluid- filled tubules that run from the surface of the dentine-enamel or dentine-cementum junction to the odontoblast/pulp interface. It is widely accepted that the origins of dentine hypersensitivity relate to changes in fluid flow in exposed tubules, (the hydrodynamic theory), that result in stimulation of mechanoreceptors thought to be located close to the odontoblast/pulp interface.
  • dentine is sensitive since it is generally covered with a smear layer; an occlusive mixture comprised predominantly of mineral and proteins derived from dentine itself, but also containing organic components from saliva. Over time, the lumen of the tubule may become progressively occluded with mineralised tissue. The formation of reparative dentine in response to trauma or chemical irritation of the pulp is also well documented. Nonetheless, an erosive challenge can remove the smear layer and tubule "plugs" causing outward dentinal fluid flow, making the dentine much more susceptible to external stimuli such as hot, cold and pressure. As previously indicated, an erosive challenge can also make the dentine surface much more susceptible to wear.
  • dentine hypersensitivity worsens as the diameter of the exposed tubules increases, and since the tubule diameter increases as one proceeds in the direction of the odontoblast/pulp interface, progressive dentine wear can result in an increase in hypersensitivity, especially in cases where dentine wear is rapid. Loss of the protective enamel layer through erosion and/or acid-mediated wear will expose the underlying dentine, and are therefore primary aetiological factors in the development of dentine hypersensitivity.
  • oral care compositions which can help prevent dental erosion and tooth wear, in addition to dental caries, would be advantageous.
  • Oral care compositions comprising a source of fluoride ions have been known for many years for combating dental caries. Fluoride ions are known to inhibit plaque bacteria that can cause plaque acid. Fluoride ions are also known to enhance remineralisation and to decrease demineralisation of dental enamel, thereby strengthening dental enamel from acidic challenges. In more recent years, oral care compositions comprising a source of fluoride ions have also been marketed for combating dental erosion; for example using the technologies described in WO 2006/100071 and WO 2010/066655 (both in the name of Glaxo Group Limited).
  • WO 2006/100071 describes a dentifrice composition especially formulated to maximise both the availability of fluoride ions in the composition and their uptake by dental enamel, so to strengthen teeth from both dietary and plaque acidic challenges. It is suggested that such dentifrices suitably do not contain a calcium salt. Attempts have been made over many years to maximise the efficacy of fluoride ions, in strengthening dental enamel, by including a source of calcium and phosphate ions to supplement the natural remineralisation provided by such ions already present in saliva.
  • US-A-5993786 (in the name of ADAHF) describes, amongst other formulations, anti- carious remineralising gels, toothpastes and dentifrices comprising from about 0.5 to 10% by weight of a-tricalcium phosphate, tetracalcium phosphate or monocalcium phosphate monohydrate, suitably present in a dry mixture to be reconstituted into a gel by the addition of water which may contain other components including a source of fluoride ions, so to prevent premature reaction of the calcium and fluoride ions.
  • US-A-6159448 (Enamelon) describes oral care compositions comprising various partially water soluble calcium salts, such as calcium sulphate, together with a source of phosphate and fluoride ions.
  • Such calcium salts are separated until use from the source of phosphate and fluoride ions either by being formulated in a single phase anhydrous system or by means of a physical barrier in a two phase aqueous composition.
  • the oral care compositions preferably contain from about 0.05% to about 15.0% by weight, more preferably from about 0.10% to about 10.0% by weight of the calcium salt(s), from about 0.05%) to about 15.0% by weight, more preferably from about 0.10 to about 10.0% by weight of the phosphate salt(s) and from about 0.01% to about 5.0%, more preferably from about 0.02%> to about 2.0%> by weight of the fluoride salt(s).
  • WO 2006/133747 (in the name of Henkel) describes oral care compositions comprising low quantities (ie from 0.01 to 0.09 % by weight of the composition) of various sparingly soluble rod-shaped nanoparticulate calcium compounds such as hydroxyapatite, fluorapatite or calcium fluoride. It is suggested that such compositions can also contain other calcium compounds, which need not be nanoparticulate, such as calcium glycerophosphate, or calcium containing abrasives such as chalk, calcium pyrophosphate or dicalcium phosphate dihydrate. Such compositions can also comprise a source of fluoride ions, preferably in an amount of 0.01 to 0.2% by weight.
  • WO 2009/074589 (in the name of Glaxo Group Limited) describes oral care compositions comprising nanoparticulate calcium fluoride for combating dental erosion and/or tooth wear.
  • the nanoparticulate calcium fluoride may be present in an amount of 0.001 to 20.0% by weight of the total composition, suitably from 0.01 to 10%, for example from 0.1 to 5.0% by weight of the total composition.
  • the oral care composition may further comprise a source of soluble fluoride ions, which can be present in an amount to provide from 25 to 3500 ppm, preferably from 100 to 1500 ppm of fluoride ions.
  • US patent 4, 193,988 (in the name of Beecham Group Ltd) describes anti-cariogenic oral hygiene compositions comprising calcium glycerophosphate and from 0.08 to 7.6% by weight of sodium monofluorophosphate, the sodium monofluorophosphate and the calcium glycerophosphate being present in the composition in a weight ratio of 10: 1 to 3 : 1.
  • WO 2007/089894 (in the name of Indiana University Research & Technology Corporation) describes dentifrices comprising an alloy comprising amorphous tricalcium phosphate and at least one metal oxide, such as titanium dioxide or silicon dioxide. Such dentifrices may further comprise a fluoride ion source.
  • WO 2008/137190 US 2010/0068159, US 2010/0291164 and US2011/0020245 (in the name of Indiana Nanotech) describe dental or confectionary products comprising a functionalised calcium compound such as calcium phosphate, especially tricalcium phosphate (TCP), functionalised by mechanochemically combining the calcium compound with an organic compound such as an surfactant, eg sodium lauryl sulphate (SLS) or an acid such as fumaric acid.
  • an organic compound such as an surfactant, eg sodium lauryl sulphate (SLS) or an acid such as fumaric acid.
  • an surfactant treated minerals such as TCP/SLS are compatible with fluoride and can improve reminineralisation efficiency.
  • WO 20010/017104 (in the name of Indiana Nanotech) describes dental formulations with fluoride comprising a functionalised calcium phosphate material comprising substantially crystalline ⁇ -tricalcium phosphate, at least one metal oxide (such as silica) and at least one organic compound (such as urea).
  • WO 2010/068359 (in the name of 3M) describes oral care compositions comprising a fluoride providing agent and calcium phosphate (especially tricalcium phosphate) particles surface-treated with a sugar alcohol, (such as xylitol) or glycerophosphoric acid or a mixture thereof.
  • an uniunctionalised calcium phosphate compound is compatible with a source of fluoride ions in an aqueous single phase oral care composition, providing the uniunctionalised calcium phosphate compound is used in a low enough amount relative to the amount of fluoride ions present.
  • the present invention is therefore based upon the two-fold discovery that a fluoride salt can be combined together with an unfunctionalised calcium phosphate compound in a single phase aqueous oral care composition providing that the calcium compound is present in a catalytic and fluoride-stable amount relative to the fluoride salt, so to enhance fluoride efficacy but not to compromise long term storage stability of the fluoride in the composition.
  • the present invention provides an aqueous single phase oral care composition
  • a fluoride salt and an unfunctionalised calcium phosphate compound, which is not ⁇ -tricalcium phosphate, characterised in that the calcium phosphate compound is present in a catalytic and fluoride-stable amount relative to the fluoride salt.
  • the compound, ⁇ -tricalcium phosphate is expressly excluded from the definition of an unfunctionalised calcium phosphate compound and does not fall within the scope of the present invention. This is because an aqueous single phase oral care composition comprising a fluoride salt and unfunctionalised ⁇ -tricalcium phosphate is the subject of, and is being claimed in, a separate patent application, filed on the same day as the present patent application. Without wishing to be bound by theory, it is believed that a catalytic amount of an unfunctionalised calcium phosphate compound can act as a nucleating template or seed, thereby enhancing the efficacy of fluoride, together with calcium and phosphate ions naturally present in saliva, in remineralising dental enamel. DETAILED DESCRIPTION OF THE INVENTION
  • aqueous single phase is meant that the oral care composition comprises water as an excipient and that all ingredients of the oral care composition are combined in one phase; ie they are not kept apart in separate compartments or by means of an anhydrous carrier.
  • catalytic and fluoride-stable amount is meant an amount sufficient to enhance the efficacy of fluoride in strengthening dental enamel from acidic challenges but not sufficient to compromise the long term storage stability of fluoride ions in the oral care composition.
  • the minimum amount of a calcium phosphate compound that can be present relative to the amount of fluoride salt in an oral care composition, to enhance fluoride efficacy can be determined by adding decreasing amounts of a calcium phosphate compound to a fixed amount of a fluoride salt and determining the relative efficacy of the oral care compositions (with and without the calcium phosphate compound) in strengthening dental enamel using a variety of methods, such as surface microhardness measurements as shown in Examples 1 and 2.
  • the maximum amount of a calcium phosphate compound that can be present relative to the amount of fluoride salt in an oral care composition, without compromising fluoride stability, can be determined by adding increasing amounts of a calcium phosphate compound to a fixed amount of a fluoride salt and measuring the levels of available fluoride over time using accelerated aging conditions, as shown in Examples 3 and 4.
  • a composition is deemed to have acceptable fluoride stability if the levels of available fluoride are no less than 10% of the theoretical amount that should be present.
  • Suitable fluoride salts are those that directly provide free fluoride ions in the oral care composition, such as alkali metal fluorides (eg sodium or potassium fluoride) or stannous fluoride.
  • salts that indirectly provide free fluoride ions, such as sodium monofluorophosphate, which is hydro lyzed by salivary enzymes in the mouth, releasing free fluoride in situ.
  • Sodium monofluorophosphate has previously been used in aqueous oral care compositions comprising ingredients, such as calcium compounds, which are incompatible with free fluoride ions, especially on long term storage.
  • the present invention avoids the need to use such a salt, and instead has found an elegantly simple way of formulating a calcium phosphate compound with a salt directly providing free fluoride ions.
  • a preferred fluoride salt is sodium fluoride.
  • the fluoride salt is generally present in an amount to provide from 10 to 5000ppm, eg from 25 to 3500pm of fluoride ions, preferably from 100 to 1500ppm, for example the composition may contain 0.1 to 0.5% by weight of sodium fluoride, eg 0.205%) by weight (equating to 927ppm of fluoride ions), 0.2542%> by weight (equating to 1150ppm of fluoride ions) or 0.315% by weight (equating to 1426ppm of fluoride ions).
  • an unfunctionalised calcium phosphate compound is meant a calcium phosphate compound that is not functionalised in the manner described in the above noted Indiana Nanotech or 3M patent applications, and which is not ⁇ -tricalcium phosphate.
  • An unfunctionalised calcium phosphate compound may be selected from the group consisting of calcium glycerophosphate, dicalcium phosphate dihydrate, tetracalcium phosphate, a-tricalcium phosphate, octacalcium phosphate, hydroxyapatite or fluroapatite, or a mixture thereof.
  • the unfunctionalised calcium phosphate compound is selected from the group consisting of tetracalcium phosphate, a-tricalcium phosphate, octacalcium phosphate, hydroxyapatite or fluroapatite, or a mixture thereof.
  • Such compounds are sparingly soluble in water.
  • the unfunctionalised calcium phosphate compound is selected from the group consisting of calcium glycerophosphate or dicalcium phosphate dihydrate, or a mixture thereof.
  • Such compounds are generally more water soluble than the other calcium phosphate compounds described hereinbefore.
  • the weight ratio of fluoride ions to total calcium ions will vary depending upon the relative solubilities of the calcium compounds and the presence of other excipients used in the oral care compositions. However, as noted above, suitable amounts of the calcium phosphate compounds can readily determined by assessing the fluoride stability and relative fluoride efficacy of the oral care compositions according to the methods described in the Examples.
  • the weight ratio of fluoride ions to total calcium ions present in the oral care composition of the present invention ranges from about 2: 1 to 100: 1, suitably from 2.5: 1 to 50: 1, more suitably from 3: 1 to 40: 1, preferably from 3.5: 1 to 30: 1.
  • the weight ratio of fluoride ions to total calcium ions present in the oral care composition of the present invention ranges from about 5: 1 to 100: 1, suitably from 7.5: 1 to 50: 1, more suitably from 10: 1 to 40: 1, preferably from 12.5: 1 to 30: 1.
  • total calcium ions is meant all the calcium ions provided by the calcium compound, both dissolved and undissolved in the oral care composition.
  • the compositions of the present invention do not require, and suitably do not contain, an alkali metal phytate or an anti- nucleating agent, for example as defined in US patents 4,177,258, 4,183,915, 4,348,381 or 4,528,181, the contents of which are incorporated herein by reference.
  • compositions of the present invention may further comprise one or more active agents conventionally used in oral healthcare compositions, for example, a desensitising agent, an anti-erosion agent, an anti-plaque agent; an anti-calculus agent, a whitening agent, an oral malodour agent, anti-inflammatory agent, an anti-oxidant, anti-fungal or wound healing agent or a mixture of at least two thereof. Such agents may be included at levels to provide the desired therapeutic effect.
  • Compositions of the present invention may comprise a desensitising agent, for combating dentine hypersensitivity. Examples of desensitising agents include a tubule blocking agent or a nerve desensitising agent and mixtures thereof, for example as described in WO 02/15809.
  • Suitable desensitising agents include a strontium salt such as strontium chloride, strontium acetate or strontium nitrate or a potassium salt such as potassium citrate, potassium chloride, potassium bicarbonate, potassium gluconate and especially potassium nitrate.
  • a strontium salt such as strontium chloride, strontium acetate or strontium nitrate or a potassium salt such as potassium citrate, potassium chloride, potassium bicarbonate, potassium gluconate and especially potassium nitrate.
  • a desensitising amount of a potassium salt is generally between 2 to 8% by weight of the total composition, for example 5% by weight of potassium nitrate can be used.
  • compositions of the present invention may comprise an anti-erosion agent, for example a polymeric mineral surface active agent or a stannous, zinc or copper compound, as described in WO 04/054529 (Procter & Gamble) or a nanoparticulate zinc oxide, as described in WO 08/054045 (Glaxo Group Limited), or a mixture thereof.
  • an anti-erosion agent for example a polymeric mineral surface active agent or a stannous, zinc or copper compound, as described in WO 04/054529 (Procter & Gamble) or a nanoparticulate zinc oxide, as described in WO 08/054045 (Glaxo Group Limited), or a mixture thereof.
  • compositions of the present invention will contain appropriate formulating agents such as abrasives, surfactants, thickening agents, humectants, flavouring agents, sweetening agents, opacifying or colouring agents, preservatives and water, selected from those conventionally used in the oral care composition art for such purposes.
  • appropriate formulating agents such as abrasives, surfactants, thickening agents, humectants, flavouring agents, sweetening agents, opacifying or colouring agents, preservatives and water, selected from those conventionally used in the oral care composition art for such purposes.
  • Suitable oral care actives and orally acceptable carriers or excipients are described for example in US 2007/0053849 (Procter & Gamble) or EP 929287 (Beecham Group Ltd).
  • compositions of the present invention are typically formulated in the form of toothpastes, sprays, mouthwashes, or gels.
  • compositions of the present invention may be prepared by admixing the ingredients in the appropriate relative amounts in any order that is convenient and if necessary adjusting the pH to give a desired value, for example from 5.5 to 9.0
  • the pH is measured when the composition is slurried with water in a 1 :3 weight ratio of the composition to water.
  • the calcium phosphate compound may be incorporated into an oral care composition of the type described in WO2006/100071 or WO 2010/066655, the contents of which are incorporated herein by reference.
  • the present invention also provides a method of combating dental erosion and/or tooth wear which comprises applying an effective amount of a composition as hereinbefore defined to an individual in need thereof.
  • the present invention also provides a method of combating dental and/or root caries which comprises applying an effective amount of a composition as hereinbefore defined to an individual in need thereof.
  • the present invention also provides a method of combating dentine hypersensitivity which comprises applying an effective amount of a composition as hereinbefore defined to an individual in need thereof
  • a method of combating dentine hypersensitivity which comprises applying an effective amount of a composition as hereinbefore defined to an individual in need thereof
  • the invention is further illustrated by the following Examples.
  • the model includes two one-minute treatment periods performed an hour apart in the morning, followed by one four-hour lactic acid-polyacrylic acid challenge, and finally two more one-minute treatment periods in the afternoon, administered daily for 10 days.
  • AS artificial saliva
  • the treatments were diluted three-fold with distilled (DI) water (5 mL treatment solution: 10 mL DI water).
  • DI distilled
  • the treatments and saliva events were magnetically agitated at 300 rpm, while the acid challenge was static.
  • the specimens were rinsed with DI water prior to placement into AS.
  • Four fresh treatment slurries and fresh acid solution were used daily, with the artificial saliva solution changed once daily after the third treatment. Solution used for the acid challenge was the same as used to prepare the initial white-spot lesions.
  • Enamel fluoride uptake was determined for the remaining six specimens in units of micrograms of fluoride per unit enamel area ⁇ g F/cm 2 ).
  • the enamel specimens were immersed and continuously agitated in 0.5 ml of 1 N HC10 4 for 15 seconds.
  • 0.25 ml of this etchant was combined with 0.25 ml of 1 N NaOH and 0.5 ml of TISAB II. This solution was magnetically stirred, and a fluoride ion specific electrode was used to measure the free fluoride ion potential. These measurements were then converted to fluoride concentrations by using a fluoride electrode calibration curve constructed from known standards prepared with NaF. These data are presented in Table 3.
  • One-way analysis of variance (ANOVA) was performed to test for significant differences, followed by comparison tests at a 95% confidence level (p ⁇ 0.05).
  • Enamel fluoride uptake was determined in units of micrograms of fluoride per unit enamel area ( ⁇ F/cm 2 ). Six enamel specimens were immersed and continuously agitated in 0.5 ml of 1 N HCIO 4 for 15 seconds. To determine fluoride concentration, 0.25 ml of this etchant was combined with 0.25 ml of 1 N NaOH and 0.5 ml of TISAB II. This solution was magnetically stirred, and a fluoride ion specific electrode (Thermo Fisher, Pittsburgh, PA, USA) was used to measure the free fluoride ion potential. These measurements were converted to fiuoride concentrations by using a fluoride electrode calibration curve constructed from known standards prepared with NaF. These data are presented in Table 5.
  • One-way analysis of variance (ANOVA) was performed to test for significant differences, followed by comparison tests at a 95% confidence level (p ⁇ 0.05).
  • Table 4 Summary of surface microhardness results after cycling through an anti- erosion remin/demin model lasting 20 days.
  • Fluoride availability was measured in triplicate for fluoride plus ⁇ -TCP. Solutions/suspensions of 0.24% NaF (1100 ppm F " ) plus ⁇ -TCP were prepared and stored at elevated conditions for 32 days at 40°C. Measurements were made using a fluoride- sensitive electrode and Accument AR Dual Channel pH meter. TISAB II ionic strength adjuster was added in a 1 : 1 ratio with a sample volume (e.g. 5 ml), and standards were and measured in order to generate the calibration curve. Conversions from mV to ppm were determined based on the calibration curve and the data are presented in Table 6.
  • Fluoride availability was measured in triplicate for the fluoride plus CaP system combinations described in Table 7. Solutions/suspensions of 0.05%> NaF (225 ppm F ion) plus CaP systems were prepared and stored at elevated conditions for 30, 60 and 90 days at 40°C. Measurements were made using a fluoride-sensitive electrode and Accument AR Dual Channel pH meter. TISAB II ionic strength adjuster was added in a 1 : 1 ratio with a sample volume (e.g. 5 ml), and standards were made and measured in order to generate the calibration curve. Conversions from mV to ppm were determined based on the calibration curve and the data are presented in Tables 8, 9 and 10.
  • Beta-tricalcium phosphate ( ⁇ -TCP) Beta-tricalcium phosphate ( ⁇ -TCP)
  • DCPD diicalcium phosphate dihydrate
  • CaGLYP Calcium glycerophosphate
  • Acceptable fluoride levels should be within 10% of the theoretical at 30, 60 and 90 days .
  • the relatively high solublility formats of calcium include DCPD, calcium sulfate, calcium chloride and calcium glycerophosphate.
  • the relatively low solubility formats of calcium include a-TCP, ⁇ -TCP, and HA. Over the duration and in consideration of the calcium concentration range of this stability study, the more soluble formats appeared to impair fluoride availability relative to the less soluble systems.
  • Calcium sulfate and calcium chloride dihydrate did not provide good stability of fluoride at any of the concentrations investigated.

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Abstract

L'invention concerne des compositions de soins orales à phase aqueuse unique comprenant un sel de fluorure et un composé de phosphate de calcium non fonctionnalisé qui n'est pas un phosphate tricalcique β, caractérisées en ce que le composé de phosphate de calcium est présent à raison d'une dose catalytique stable en fluorure par rapport au sel de fluorure. Ces compositions sont utilisées pour lutter contre les caries dentaires, l'érosion dentaire et/ou l'usure des dents.
PCT/EP2014/052689 2013-02-14 2014-02-12 Nouvelle composition WO2014124950A1 (fr)

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020128680A1 (fr) * 2018-12-17 2020-06-25 Johnson & Johnson Consumer Inc. Méthode de fourniture d'un bienfait de soin buccodentaire faisant appel à un composé du calcium faiblement soluble et un fluorure

Citations (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1384375A (en) * 1971-04-29 1975-02-19 Beecham Group Ltd Oral hygiene compositions
US4098435A (en) 1976-08-16 1978-07-04 Colgate-Palmolive Company Stabilized dentrifice containing initially physically separated normally reactive components
US4177258A (en) 1978-10-13 1979-12-04 Colgate Palmolive Company Dentifrice for dental remineralization
US4183915A (en) 1978-10-13 1980-01-15 Colgate-Palmolive Company Stable solution for dental remineralization
US4193988A (en) 1971-04-29 1980-03-18 Beecham Group Limited Oral hygiene compositions
US4348381A (en) 1981-05-06 1982-09-07 Colgate-Palmolive Company Dental remineralization composition
US4528181A (en) 1984-02-01 1985-07-09 Colgate-Palmolive Company Dentifrice containing dual sources of fluoride
US5571502A (en) 1995-08-08 1996-11-05 Enamelon Research Stable single-part compositions and the use thereof for remineralization of lesions in teeth
US5603922A (en) 1995-08-08 1997-02-18 Enamelon Inc. Processes and compositions for the remineralization of teeth
US5605675A (en) 1995-06-06 1997-02-25 Enamelon Inc. Processes and compositions for remineralization and prevention of demineralization of dental enamel
JPH11106322A (ja) * 1997-08-04 1999-04-20 Kao Corp 口腔用組成物
EP0929287A1 (fr) 1996-09-12 1999-07-21 SmithKline Beecham Consumer Healthcare GmbH Composition de remineralisation
US5993786A (en) 1996-08-20 1999-11-30 American Dental Association Health Foundation Anti-carious chewing gums, candies, gels, toothpastes and dentifrices
US6159448A (en) 1996-09-27 2000-12-12 Enamelon, Inc. Products and methods for the remineralization and prevention of demineralization of teeth
WO2002015809A2 (fr) 2000-08-21 2002-02-28 Block Drug Company, Inc. Composition dentaire pour dents hypersensibles
WO2004054529A1 (fr) 2002-12-13 2004-07-01 The Procter & Gamble Company Methode de protection des dents contre l'erosion
US20060134020A1 (en) * 2004-12-21 2006-06-22 Robinson Richard S Anti-caries oral care composition with a chelating agent
WO2006100071A1 (fr) 2005-03-21 2006-09-28 Glaxo Group Limited Formule de dentifrice sans sulfate d’alkyle ni orthophosphate comprenant une source de fluorure et un abrasif dentaire à base de silice
WO2006133747A1 (fr) 2005-06-15 2006-12-21 Henkel Kommanditgesellschaft Auf Aktien Agents a effet remineralisant destines au nettoyage et a l'hygiene des dents et de la bouche
US20070053849A1 (en) 2000-06-30 2007-03-08 The Procter & Gamble Company Oral care compositions containing combinations of anti-bacterial and host-response modulating agents
WO2007050684A2 (fr) * 2005-10-27 2007-05-03 Ada Foundation Compositions de fluorure-calcium, produits dentaires et procedes d'apport de fluorure dentaire
US20070128131A1 (en) * 2003-12-26 2007-06-07 Kao Corporation Composition for oral cavity
WO2007089894A2 (fr) 2006-01-31 2007-08-09 Indiana University Research & Technology Corporation Matériaux et procédés de fabrication d'alliages de phosphate tricalcique amorphe et d'oxyde métallique de phosphate tricalcique amorphe et procédés d'utilisation correspondants
WO2008054045A1 (fr) 2006-10-31 2008-05-08 Korea Advanced Institute Of Science And Technology Appareil pour combiner et découper une bande de longueur d'ondes comportant trois ports entrée et sortie
EP1952801A1 (fr) * 2005-11-25 2008-08-06 "WDS" Company Composition de soins et de prevention pour la cavite buccale
WO2008137190A2 (fr) 2007-02-06 2008-11-13 Indiana Nanotech Division Of Therametric Technologies, Inc. Systèmes hybrides organiques/inorganiques, comprenant des systèmes hybrides de phosphate de calcium fonctionnalisé, et un procédé de production à l'état solide de tels systèmes
WO2009074589A2 (fr) 2007-12-12 2009-06-18 Glaxo Group Limited Nouvel usage pour soins buccaux
WO2010017104A1 (fr) 2008-08-06 2010-02-11 Indiana Nanotech Llc Procédé de broyage pour la manipulation ou la conservation des propriétés hybrides de phosphate de calcium
US20100068159A1 (en) 2008-09-12 2010-03-18 Karlinsey Robert L Functionalized calcium phosphate hybrid systems for confectionery and foodstuff applications
WO2010068359A1 (fr) 2008-12-11 2010-06-17 3M Innovative Properties Company Particules de phosphate de calcium traitées en surface pour soins buccaux et compositions dentaires
WO2010066655A1 (fr) 2008-12-09 2010-06-17 Glaxo Group Limited Nouvel usage
US20100291164A1 (en) 2007-01-31 2010-11-18 Karlinsey Robert L Functionalized calcium phosphate hybrid systems for the remineralization of teeth and a method for producing the same
US20110020245A1 (en) 2006-01-31 2011-01-27 Karlinsey Robert L Functionalized calcium phosphate hybrid systems for confectionery and foodstuff applications

Patent Citations (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4193988A (en) 1971-04-29 1980-03-18 Beecham Group Limited Oral hygiene compositions
GB1384375A (en) * 1971-04-29 1975-02-19 Beecham Group Ltd Oral hygiene compositions
US4098435A (en) 1976-08-16 1978-07-04 Colgate-Palmolive Company Stabilized dentrifice containing initially physically separated normally reactive components
US4177258A (en) 1978-10-13 1979-12-04 Colgate Palmolive Company Dentifrice for dental remineralization
US4183915A (en) 1978-10-13 1980-01-15 Colgate-Palmolive Company Stable solution for dental remineralization
US4348381A (en) 1981-05-06 1982-09-07 Colgate-Palmolive Company Dental remineralization composition
US4528181A (en) 1984-02-01 1985-07-09 Colgate-Palmolive Company Dentifrice containing dual sources of fluoride
US5605675A (en) 1995-06-06 1997-02-25 Enamelon Inc. Processes and compositions for remineralization and prevention of demineralization of dental enamel
US5603922A (en) 1995-08-08 1997-02-18 Enamelon Inc. Processes and compositions for the remineralization of teeth
US5571502A (en) 1995-08-08 1996-11-05 Enamelon Research Stable single-part compositions and the use thereof for remineralization of lesions in teeth
US5993786A (en) 1996-08-20 1999-11-30 American Dental Association Health Foundation Anti-carious chewing gums, candies, gels, toothpastes and dentifrices
EP0929287A1 (fr) 1996-09-12 1999-07-21 SmithKline Beecham Consumer Healthcare GmbH Composition de remineralisation
US6159448A (en) 1996-09-27 2000-12-12 Enamelon, Inc. Products and methods for the remineralization and prevention of demineralization of teeth
JPH11106322A (ja) * 1997-08-04 1999-04-20 Kao Corp 口腔用組成物
US20070053849A1 (en) 2000-06-30 2007-03-08 The Procter & Gamble Company Oral care compositions containing combinations of anti-bacterial and host-response modulating agents
WO2002015809A2 (fr) 2000-08-21 2002-02-28 Block Drug Company, Inc. Composition dentaire pour dents hypersensibles
WO2004054529A1 (fr) 2002-12-13 2004-07-01 The Procter & Gamble Company Methode de protection des dents contre l'erosion
US20070128131A1 (en) * 2003-12-26 2007-06-07 Kao Corporation Composition for oral cavity
US20060134020A1 (en) * 2004-12-21 2006-06-22 Robinson Richard S Anti-caries oral care composition with a chelating agent
WO2006100071A1 (fr) 2005-03-21 2006-09-28 Glaxo Group Limited Formule de dentifrice sans sulfate d’alkyle ni orthophosphate comprenant une source de fluorure et un abrasif dentaire à base de silice
WO2006133747A1 (fr) 2005-06-15 2006-12-21 Henkel Kommanditgesellschaft Auf Aktien Agents a effet remineralisant destines au nettoyage et a l'hygiene des dents et de la bouche
WO2007050684A2 (fr) * 2005-10-27 2007-05-03 Ada Foundation Compositions de fluorure-calcium, produits dentaires et procedes d'apport de fluorure dentaire
EP1952801A1 (fr) * 2005-11-25 2008-08-06 "WDS" Company Composition de soins et de prevention pour la cavite buccale
WO2007089894A2 (fr) 2006-01-31 2007-08-09 Indiana University Research & Technology Corporation Matériaux et procédés de fabrication d'alliages de phosphate tricalcique amorphe et d'oxyde métallique de phosphate tricalcique amorphe et procédés d'utilisation correspondants
US20110020245A1 (en) 2006-01-31 2011-01-27 Karlinsey Robert L Functionalized calcium phosphate hybrid systems for confectionery and foodstuff applications
WO2008054045A1 (fr) 2006-10-31 2008-05-08 Korea Advanced Institute Of Science And Technology Appareil pour combiner et découper une bande de longueur d'ondes comportant trois ports entrée et sortie
US20100291164A1 (en) 2007-01-31 2010-11-18 Karlinsey Robert L Functionalized calcium phosphate hybrid systems for the remineralization of teeth and a method for producing the same
WO2008137190A2 (fr) 2007-02-06 2008-11-13 Indiana Nanotech Division Of Therametric Technologies, Inc. Systèmes hybrides organiques/inorganiques, comprenant des systèmes hybrides de phosphate de calcium fonctionnalisé, et un procédé de production à l'état solide de tels systèmes
WO2009074589A2 (fr) 2007-12-12 2009-06-18 Glaxo Group Limited Nouvel usage pour soins buccaux
WO2010017104A1 (fr) 2008-08-06 2010-02-11 Indiana Nanotech Llc Procédé de broyage pour la manipulation ou la conservation des propriétés hybrides de phosphate de calcium
US20100068159A1 (en) 2008-09-12 2010-03-18 Karlinsey Robert L Functionalized calcium phosphate hybrid systems for confectionery and foodstuff applications
WO2010066655A1 (fr) 2008-12-09 2010-06-17 Glaxo Group Limited Nouvel usage
WO2010068359A1 (fr) 2008-12-11 2010-06-17 3M Innovative Properties Company Particules de phosphate de calcium traitées en surface pour soins buccaux et compositions dentaires

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020128680A1 (fr) * 2018-12-17 2020-06-25 Johnson & Johnson Consumer Inc. Méthode de fourniture d'un bienfait de soin buccodentaire faisant appel à un composé du calcium faiblement soluble et un fluorure
CN113271910A (zh) * 2018-12-17 2021-08-17 强生消费者公司 使用难溶性钙化合物和氟化物提供口腔护理有益效果的方法
US11857653B2 (en) 2018-12-17 2024-01-02 Johnson & Johnson Consumer Inc. Method of providing an oral care benefit using a poorly-soluble calcium compound and fluoride

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