Oral care composition

Abstract

An oral care composition comprising: a) one or more organic polyols having 3 or more hydroxyl groups in the molecule, said organic polyols making up 20-90% by weight of the total composition; b) calcium silicate; c) sodium phosphate salt; d) monocalcium phosphate; e) xanthan gum; and f) carrageenan.

Description

Technical Field

[0001] The present invention relates to oral care compositions, such as toothpaste, powder, gel, mouthwash, etc. The present invention particularly relates to oral care compositions, in particular to toothpastes that can effectively reduce the effects of gastric acid erosion on tooth enamel. Background Art

[0002] Acid reflux can lead to chemical erosion of tooth enamel, so teeth may appear yellow due to increased dentin visibility and sensitivity issues may occur due to increased exposure of dentinal tubules.

[0003] WO20131616 relates to a method for preventing dental erosion by a combination of a basic amino acid and one or more zinc sources.

[0004] However, there remains a need to provide improved methods of using oral care compositions to protect tooth enamel from the inherent aggressive effects of gastric acid. Summary of the invention

[0005] The present invention relates to an oral care composition comprising:

[0006] a) one or more organic polyols having 3 or more hydroxyl groups in the molecule, said organic polyols accounting for 20-90 wt% of the total composition;

[0007] b) calcium silicate;

[0008] c) potassium phosphate;

[0009] d) monocalcium phosphate;

[0010] e) xanthan gum; and

[0011] f) Carrageenan.

[0012] In a second aspect, the present invention relates to the use of the oral care composition as described above in a method for reducing the erosion of tooth enamel by gastric acid. DETAILED DESCRIPTION OF THE INVENTION

[0014] Except in the examples, or where otherwise explicitly indicated, all numerical values ​​in this specification indicating amounts of materials or conditions of reactions, physical properties of materials and / or uses may optionally be understood as modified by "about".

[0015] Unless otherwise indicated, all amounts are by weight of the composition.

[0016] It should be noted that in specifying any numerical range, any upper value can be associated with any particular lower value.

[0017] If a feature is disclosed with respect to a particular aspect of the invention (eg, a composition of the invention), such disclosure should be considered applicable, mutatis mutandis, to any other aspect of the invention (eg, a method of the invention).

[0018] Any natural or naturally derived ingredients mentioned in this application are of European origin.

[0019] The compositions of the present invention are preferably used to clean the surfaces of the oral cavity and are known as oral care compositions.

[0020] Thus, preferred product forms of the compositions of the present invention are those suitable for brushing and / or rinsing oral surfaces.

[0021] The composition of the present invention is most preferably in the form of a dentifrice. The term "dentifrice" refers to an oral composition for cleaning oral surfaces. Such compositions are not intended to be deliberately swallowed for systemic administration of a therapeutic agent, but are applied to the oral cavity, used to treat the oral cavity, and then rinsed out. Typically such compositions are used with a cleaning implement such as a toothbrush, and are typically applied to the bristles of the toothbrush and then scrubbed to the accessible oral surfaces.

[0022] Preferably, the dentifrice / toothpaste is in an extrudable semi-solid form, such as a paste, a paste or a gel (or a mixture thereof). Toothpaste is particularly preferred.

[0023] The composition according to the invention comprises monocalcium phosphate. Preferably, the monocalcium phosphate is present in an amount of 0.1-10 wt %, more preferably 1-6 wt % of the total composition.

[0024] The composition of the present invention comprises one or more organic polyols having 3 or more hydroxyl groups in the molecule, said organic polyols accounting for 20-90% by weight of the total composition. Preferably, the organic polyol is glycerol.

[0025] The composition of the present invention comprises an agent for remineralization of teeth.In the context of the present invention, the term "remineralization" refers to the in situ generation of hydroxyapatite on teeth.

[0026] The composition according to the invention comprises a suitable agent for tooth remineralisation which is a mixture of calcium silicate and sodium phosphate salts which, when delivered to the teeth, will generate hydroxyapatite in situ on the teeth.

[0027] The amount of remineralizing calcium source (eg calcium silicate) in the composition of the present invention is generally 1-30%, preferably 5-20% by total weight of the remineralizing calcium source, based on the total weight of the oral care composition.

[0028] Illustrative examples of types of phosphates that can be used in the context of the present application (hereinafter referred to as "remineralized phosphate sources") include, for example, sodium dihydrogen phosphate, disodium hydrogen phosphate, sodium pyrophosphate, tetrasodium pyrophosphate, sodium tripolyphosphate, sodium hexametaphosphate, potassium dihydrogen phosphate, trisodium phosphate, tripotassium phosphate, and mixtures thereof. Preferably, the remineralized phosphate source is a mixture of trisodium phosphate and sodium dihydrogen phosphate.

[0029] The amount of remineralizing phosphate source (eg, trisodium phosphate and sodium dihydrogen phosphate) in the composition of the present invention is 2-15%, preferably 4-10%, by total weight of the remineralizing phosphate source, based on the total weight of the oral care composition.

[0030] The composition according to the invention further comprises xanthan gum and carrageenan. Particularly preferably, the carrageenan is iota or kappa carrageenan, and a mixture of the two is particularly preferred.

[0031] Preferably, the xanthan gum is present in an amount of 0.1-0.9% by weight of the total composition.

[0032] It is also preferred if the content of carrageenan is 0.1-0.9 wt% of the total composition.Preferably the weight ratio of xanthan gum to carrageenan is from 1:2 to 2:1.

[0033] Preferably, the composition comprises 0.2-5% by weight of the total composition of one or more surfactants such as anionic, nonionic, cationic and zwitterionic or amphoteric surfactants.Preferred surfactants are taurates, especially sodium methyl cocoyl taurate.

[0034] The composition (eg, dentifrice / toothpaste) according to the present invention may generally contain, in addition to the above ingredients, other ingredients to enhance performance and / or consumer acceptability.

[0035] The composition according to the present invention, especially toothpaste, preferably includes a particulate abrasive, such as silica, alumina, calcium carbonate, dicalcium phosphate, calcium pyrophosphate, hydroxyapatite, trimetaphosphate, insoluble hexametaphosphate and the like, including agglomerated particulate abrasive, usually in an amount of 3-60% by weight of the oral care composition.

[0036] Preferably, the composition, especially the toothpaste, comprises an abrasive based on silica. The preferred abrasive silica used in the present invention is a silica with a low refractive index. It can be used as the only abrasive silica, or together with a small amount of other abrasive silicas such as those according to European patent EP236070. The low refractive index silica used as an abrasive in the present invention preferably has an apparent refractive index (RI) in the range of 1.41-1.47, preferably in the range of 1.435-1.445, preferably a weight average particle size of 5-15 mm, a BET (nitrogen) surface area of ​​10-100 m 2 / g, and the oil absorption is about 70-150cm 3 / 100g, but abrasive silicas with a low apparent refractive index can also be used. Typical examples of suitable abrasive silicas with a low apparent refractive index (e.g., a refractive index between 1.435 and 1.445) are Tixosil 63 and 73 from Rhone Poulenc; Sident 10 from Degussa; Zeodent 113 from Zeofinn, Zeodent 124 from Evonik, Sorbosil AC 77 from PQ Corporation (refractive index of about 1.440). The amount of these silicas in the composition is generally 5-60% by weight, usually 5-20% by weight.

[0037] The composition, especially if it is a toothpaste, preferably includes an inorganic or natural or synthetic thickener or gelling agent, depending on the material selected, in a proportion of about 0.10-15% by weight. These proportions of thickener in the dentifrice composition of the present invention form an extrudable shape-retaining product that can be squeezed from a tube onto a toothbrush and does not fall between the bristles of the toothbrush, but rather substantially retains its shape on the bristles. Suitable thickeners or gelling agents suitable for use in the practice of the present invention include inorganic thickening silica, such as amorphous silica available from Evonik under the trademark Zeodent 165, Irish moss, iota-carrageenan, tragacanth gum and polyvinylpyrrolidone.

[0038] The composition according to the invention preferably comprises a polymeric deposition aid. Preferably, the composition comprises an anhydride polymer, particularly preferably a copolymer of maleic anhydride and methyl vinyl ether, wherein the anhydride portion may be in a partially or fully hydrolyzed or alcoholyzed form. Preferred copolymers include Gantrez(R) polymers, such as:

[0039] Gantrez S-95: molecular weight 216,000; free acid;

[0040] Gantrez S-96: molecular weight 700,000; free acid;

[0041] Gantrez S-97: molecular weight 1,500,000; free acid; and

[0042] Gantrez MS-955: molecular weight 1,060,000; calcium / sodium salt.

[0043] Particularly preferred copolymers of maleic acid and methyl vinyl ether have a molecular weight of 1,000,000 or greater, and a particularly preferred material is Gantrez S-97.

[0044] The composition according to the invention may comprise a tooth whitening agent. The whitening agent preferably comprises a green pigment and / or a blue pigment. In the context of the present invention, a pigment is generally understood to be a shade / substance that is insoluble in the relevant medium at the relevant temperature. This is in contrast to a soluble dye. In the context of the present invention, the "relevant medium" refers to the liquid medium at the temperature of the oral cavity during brushing, i.e. when the composition is used at a temperature of up to 37°C, i.e. human saliva. As a reasonable approximation, the relevant medium can be considered to be water, and the relevant temperature is 25°C.

[0045] Preferably, 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. The preferred pigment is a blue pigment, namely Phthalocyanine Blue Pigment, CI No. 74160, Covarine Blue.

[0046] A preferred green pigment is phthalocyanine green, preferably phthalocyanine green CI-74260.

[0047] Preferably, the total content of pigments in the composition is 0.01 wt% to 3 wt%, more preferably 0.02 wt% to 2 wt%.

[0048] If the composition is a toothpaste, it may be a two-phase paste, with the whitening pigment being present in one phase.

[0049] The composition according to the invention may contain a water-soluble or slightly water-soluble metal salt source. Preferred are zinc ions, such as zinc chloride, zinc acetate, zinc gluconate, zinc sulfate, zinc fluoride, zinc citrate, zinc lactate, zinc oxide, zinc monoglycerolate, zinc tartrate, zinc pyrophosphate and zinc maleate; also preferred are stannous ions, such as stannous fluoride and stannous chloride.

[0050] The composition according to the invention may comprise an oral care enzyme system, such as a hydroperoxide generating enzyme system (e.g. the oxidoreductase glucose oxidase), amyloglucosidase, glucanase and / or water-insoluble glucanase, (optionally in the presence of a compound providing zinc ions and / or an 8-hydroxyquinoline derivative), lactoperoxidase, lactoferrin, lysozyme and mixtures thereof.

[0051] The compositions of the present invention may include a fluoride source such as sodium fluoride, stannous fluoride, sodium monofluorophosphate, ammonium zinc fluoride, ammonium stannous fluoride, calcium fluoride, ammonium cobalt fluoride, and mixtures thereof.

[0052] Mixtures of any of the above may also be used.

[0053] The composition according to the present invention may include other ingredients commonly used in the art, such as:

[0054] Antimicrobial agents such as chlorhexidine, sanguinarine extract, metronidazole, quaternary ammonium compounds such as cetylpyridinium hydrochloride; cetylpyridinium chloride clay complex; biguanides such as chlorhexidine digluconate, hexetidine, orcinidine, alexidin; and halogenated bisphenol compounds such as 2,2'-methylenebis-(4-chloro-6-bromophenol);

[0055] Anti-inflammatory agents, such as ibuprofen, flurbiprofen, aspirin, indomethacin, etc.;

[0056] anticaries agents such as sodium and stannous fluoride, fluoroamine, sodium monofluorophosphate, sodium tripolyphosphate, and casein;

[0057] plaque buffers, such as urea, calcium lactate, calcium glycerophosphate, and strontium polyacrylate;

[0058] Vitamins, such as vitamin A, vitamin C, and vitamin E;

[0059] Plant extracts;

[0060] Plant-derived antioxidants such as flavonoids, catechins, polyphenols, tannin compounds, and mixtures thereof;

[0061] Desensitizing agents, such as potassium citrate, potassium chloride, potassium tartrate, potassium bicarbonate, potassium oxalate, potassium nitrate, and strontium salts;

[0062] Antitartar agents, such as alkali metal pyrophosphates, hypophosphite-containing polymers, organic phosphonates, and phosphocitrates;

[0063] Biomolecules, such as bacteriocins, antibodies, enzymes, etc.;

[0064] spices, such as peppermint and spearmint oils;

[0065] Protein substances, such as collagen;

[0066] preservative;

[0067] Opaquer;

[0068] Hyaluronic acid;

[0069] Amino acids, such as arginine;

[0070] Colorants;

[0071] pH adjusters;

[0072] Sweeteners;

[0073] Pharmaceutically acceptable carriers, such as starch, sucrose, water or water / alcohol system;

[0074] Wetting agents, such as glycerin, sorbitol, propylene glycol, xylitol, lactitol, etc.;

[0075] Binders and thickeners, such as sodium carboxymethylcellulose, hydroxyethylcellulose Xanthan gum, gum arabic, etc., as well as synthetic polymers such as polyacrylates, and carboxyvinyl polymers such as

[0076] Polymeric compounds that may enhance the delivery of active ingredients such as antimicrobial agents may also be included;

[0077] Buffering agents and salts for buffering the pH and ionic strength of the oral care composition; and

[0078] Other optional ingredients may also be included, for example bleaching agents such as peroxides, for example potassium peroxydiphosphate, effervescent systems such as sodium bicarbonate / citric acid systems, color change systems, and the like.

[0079] The following non-limiting examples illustrate the embodiments of the present invention. The embodiments of the present invention are represented by numbers and the comparative examples are represented by letters. DETAILED DESCRIPTION

[0080] Example

[0081] Table 1

[0082]

[0083] method

[0084] Baseline surface microhardness (SMH) was measured on polished human enamel blocks (3×3 mm) of three sets of pre-made templates with n=12 (using HV 0.1 kgf / 10s, 5 indentations per sample). Two treatment groups, Example 1 and Example A, were each assigned n=12 templates.

[0085] In each cycle, the enamel specimens were exposed to the following treatment cycles: (1) treatment with a 1:2 slurry of toothpaste and deionized water for 2 minutes; (2) rinsing with deionized water; (3) exposure to artificial saliva (pH 7.0, 1.5 mM calcium chloride, 0.9 mM potassium dihydrogen phosphate, 20 mM HEPES, 130 mM potassium chloride) for 2 hours; (4) exposure to gastric acid solution (pH 2.3, 10 mM hydrochloric acid) for 30 seconds; (5) rinsing with deionized water.

[0086] Enamel SMH was re-measured after 2 and 4 treatment cycles. The mean enamel SMH was calculated for each sample, and the % change in enamel SMH was calculated using the following formula:

[0087]

[0088] The overall mean % change in SMH was calculated for each treatment group and time point.

[0089]

[0090] Statistical analysis (ANOVA, Tukey-Kramer) was performed using JMP 14.0.1.

[0091] The smaller the % change in SMH, the better the product protects tooth enamel against erosive challenges.

[0092] After 2 and 4 cycles, Example 1 provided significantly greater protection than Example A against gastric acid challenge.

Claims

1. An oral care composition comprising: a) one or more organic polyols having 3 or more hydroxyl groups in the molecule, said organic polyols accounting for 20-90 wt % of the total composition; b) calcium silicate; c) sodium phosphate; d) monocalcium phosphate; e) xanthan gum; f) Carrageenan.

2. The oral care composition according to claim 1, wherein the content of xanthan gum is 0.1-0.9 wt% of the total composition.

3. An oral care composition according to claim 1 or 2, wherein the content of carrageenan is 0.1-0.9 wt% of the total composition.

4. An oral care composition according to any one of the preceding claims, wherein the sodium phosphate salt is present in an amount of 1-20 wt%, preferably 2-15 wt%, of the total composition.

5. An oral care composition according to any one of the preceding claims, wherein the calcium silicate is present in an amount of 1-30 wt%, preferably 5-20 wt%, of the total composition.

6. An oral care composition according to any one of the preceding claims, wherein the monocalcium phosphate is present in an amount of 0.1-10 wt%, preferably 1-6 wt%, of the total composition.

7. An oral care composition according to any one of the preceding claims, wherein the weight ratio of xanthan gum to carrageenan is from 1 :2 to 2:

1.

8. An oral care composition according to any preceding claim, wherein the composition comprises 0.2-5% by weight of the total composition of one or more surfactants.

9. The oral care composition of claim 9, wherein the surfactant is methyl cocoyl taurate.

10. An oral care composition according to any preceding claim comprising from 3 to 75% by weight of the total composition of one or more particulate abrasive cleaning agents.

11. An oral care composition according to any one of the preceding claims, wherein the carrageenan is a mixture of iota carrageenan and kappa carrageenan.

12. An oral care composition according to any preceding claim, wherein the organic polyol comprises glycerol.

13. An oral care composition according to any preceding claim which is a toothpaste.

14. An oral care composition according to any preceding claim for use as a medicament for reducing erosion of tooth enamel by gastric acid.

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