CN117320683A - Oral care compositions - Google Patents
Oral care compositions Download PDFInfo
- Publication number
- CN117320683A CN117320683A CN202280035958.7A CN202280035958A CN117320683A CN 117320683 A CN117320683 A CN 117320683A CN 202280035958 A CN202280035958 A CN 202280035958A CN 117320683 A CN117320683 A CN 117320683A
- Authority
- CN
- China
- Prior art keywords
- oral care
- composition
- fluoride
- sodium
- weight
- Prior art date
- Legal status (The legal status 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 status listed.)
- Pending
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 340
- LRXTYHSAJDENHV-UHFFFAOYSA-H zinc phosphate Chemical compound [Zn+2].[Zn+2].[Zn+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O LRXTYHSAJDENHV-UHFFFAOYSA-H 0.000 claims abstract description 50
- 229910000165 zinc phosphate Inorganic materials 0.000 claims abstract description 48
- 239000004094 surface-active agent Substances 0.000 claims abstract description 47
- KRHYYFGTRYWZRS-UHFFFAOYSA-M Fluoride anion Chemical compound [F-] KRHYYFGTRYWZRS-UHFFFAOYSA-M 0.000 claims abstract description 38
- XOAAWQZATWQOTB-UHFFFAOYSA-N taurine Chemical compound NCCS(O)(=O)=O XOAAWQZATWQOTB-UHFFFAOYSA-N 0.000 claims abstract description 28
- 208000002925 dental caries Diseases 0.000 claims abstract description 17
- 229940104261 taurate Drugs 0.000 claims abstract description 17
- 208000007565 gingivitis Diseases 0.000 claims abstract description 9
- 208000008617 Tooth Demineralization Diseases 0.000 claims abstract description 5
- 206010072665 Tooth demineralisation Diseases 0.000 claims abstract description 5
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 74
- PUZPDOWCWNUUKD-UHFFFAOYSA-M sodium fluoride Chemical compound [F-].[Na+] PUZPDOWCWNUUKD-UHFFFAOYSA-M 0.000 claims description 44
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 37
- 239000000377 silicon dioxide Substances 0.000 claims description 35
- 235000019333 sodium laurylsulphate Nutrition 0.000 claims description 32
- 229940091249 fluoride supplement Drugs 0.000 claims description 26
- 229940048109 sodium methyl cocoyl taurate Drugs 0.000 claims description 26
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims description 25
- -1 amine fluorides Chemical class 0.000 claims description 24
- 210000000214 mouth Anatomy 0.000 claims description 22
- 235000013024 sodium fluoride Nutrition 0.000 claims description 22
- 239000011775 sodium fluoride Substances 0.000 claims description 22
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 18
- 239000000551 dentifrice Substances 0.000 claims description 17
- 238000000034 method Methods 0.000 claims description 16
- 239000011734 sodium Substances 0.000 claims description 16
- ANOBYBYXJXCGBS-UHFFFAOYSA-L stannous fluoride Chemical compound F[Sn]F ANOBYBYXJXCGBS-UHFFFAOYSA-L 0.000 claims description 16
- 229960002799 stannous fluoride Drugs 0.000 claims description 16
- 239000003082 abrasive agent Substances 0.000 claims description 15
- 239000003906 humectant Substances 0.000 claims description 15
- 230000002401 inhibitory effect Effects 0.000 claims description 15
- 229910052700 potassium Inorganic materials 0.000 claims description 14
- 229910052708 sodium Inorganic materials 0.000 claims description 14
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims description 12
- 239000011591 potassium Substances 0.000 claims description 12
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 claims description 11
- 239000011701 zinc Substances 0.000 claims description 11
- 241000894006 Bacteria Species 0.000 claims description 10
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims description 10
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims description 10
- HCHKCACWOHOZIP-UHFFFAOYSA-N Zinc Chemical compound [Zn] HCHKCACWOHOZIP-UHFFFAOYSA-N 0.000 claims description 10
- 239000000600 sorbitol Substances 0.000 claims description 10
- 235000010356 sorbitol Nutrition 0.000 claims description 10
- 229910052725 zinc Inorganic materials 0.000 claims description 10
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 9
- 235000011187 glycerol Nutrition 0.000 claims description 9
- 239000002888 zwitterionic surfactant Substances 0.000 claims description 9
- 238000004140 cleaning Methods 0.000 claims description 8
- 210000003298 dental enamel Anatomy 0.000 claims description 8
- 230000003628 erosive effect Effects 0.000 claims description 7
- 230000001737 promoting effect Effects 0.000 claims description 7
- 229910000318 alkali metal phosphate Inorganic materials 0.000 claims description 6
- 125000000217 alkyl group Chemical group 0.000 claims description 6
- MRUAUOIMASANKQ-UHFFFAOYSA-N cocamidopropyl betaine Chemical compound CCCCCCCCCCCC(=O)NCCC[N+](C)(C)CC([O-])=O MRUAUOIMASANKQ-UHFFFAOYSA-N 0.000 claims description 6
- 229940073507 cocamidopropyl betaine Drugs 0.000 claims description 6
- NROKBHXJSPEDAR-UHFFFAOYSA-M potassium fluoride Chemical compound [F-].[K+] NROKBHXJSPEDAR-UHFFFAOYSA-M 0.000 claims description 6
- XGRSAFKZAGGXJV-UHFFFAOYSA-N 3-azaniumyl-3-cyclohexylpropanoate Chemical compound OC(=O)CC(N)C1CCCCC1 XGRSAFKZAGGXJV-UHFFFAOYSA-N 0.000 claims description 5
- 238000005115 demineralization Methods 0.000 claims description 5
- 230000002328 demineralizing effect Effects 0.000 claims description 5
- 239000002324 mouth wash Substances 0.000 claims description 5
- 229960004711 sodium monofluorophosphate Drugs 0.000 claims description 5
- 239000011575 calcium Substances 0.000 claims description 4
- PQXKHYXIUOZZFA-UHFFFAOYSA-M lithium fluoride Chemical compound [Li+].[F-] PQXKHYXIUOZZFA-UHFFFAOYSA-M 0.000 claims description 4
- 229920006395 saturated elastomer Polymers 0.000 claims description 4
- CAVXVRQDZKMZDB-UHFFFAOYSA-M sodium;2-[dodecanoyl(methyl)amino]ethanesulfonate Chemical compound [Na+].CCCCCCCCCCCC(=O)N(C)CCS([O-])(=O)=O CAVXVRQDZKMZDB-UHFFFAOYSA-M 0.000 claims description 4
- 230000002087 whitening effect Effects 0.000 claims description 4
- ROJFMKKNPSHGIE-UHFFFAOYSA-N 2-aminoacetic acid;hydrofluoride Chemical class F.NCC(O)=O ROJFMKKNPSHGIE-UHFFFAOYSA-N 0.000 claims description 3
- DDFHBQSCUXNBSA-UHFFFAOYSA-N 5-(5-carboxythiophen-2-yl)thiophene-2-carboxylic acid Chemical compound S1C(C(=O)O)=CC=C1C1=CC=C(C(O)=O)S1 DDFHBQSCUXNBSA-UHFFFAOYSA-N 0.000 claims description 3
- 206010020751 Hypersensitivity Diseases 0.000 claims description 3
- 208000025865 Ulcer Diseases 0.000 claims description 3
- 206010052428 Wound Diseases 0.000 claims description 3
- 208000027418 Wounds and injury Diseases 0.000 claims description 3
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 claims description 3
- 230000002053 acidogenic effect Effects 0.000 claims description 3
- 208000026935 allergic disease Diseases 0.000 claims description 3
- 230000032770 biofilm formation Effects 0.000 claims description 3
- 230000015572 biosynthetic process Effects 0.000 claims description 3
- 230000036996 cardiovascular health Effects 0.000 claims description 3
- 235000015218 chewing gum Nutrition 0.000 claims description 3
- RWSWOANLVTWMDE-UHFFFAOYSA-N dodecylazanium;fluoride Chemical compound F.CCCCCCCCCCCCN RWSWOANLVTWMDE-UHFFFAOYSA-N 0.000 claims description 3
- 206010013781 dry mouth Diseases 0.000 claims description 3
- 230000035876 healing Effects 0.000 claims description 3
- 230000036541 health Effects 0.000 claims description 3
- 230000009610 hypersensitivity Effects 0.000 claims description 3
- 230000003902 lesion Effects 0.000 claims description 3
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 claims description 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 3
- 230000000813 microbial effect Effects 0.000 claims description 3
- 230000007406 plaque accumulation Effects 0.000 claims description 3
- 239000011698 potassium fluoride Substances 0.000 claims description 3
- 235000003270 potassium fluoride Nutrition 0.000 claims description 3
- 239000000843 powder Substances 0.000 claims description 3
- 235000013772 propylene glycol Nutrition 0.000 claims description 3
- 235000000346 sugar Nutrition 0.000 claims description 3
- 231100000397 ulcer Toxicity 0.000 claims description 3
- 239000000811 xylitol Substances 0.000 claims description 3
- 235000010447 xylitol Nutrition 0.000 claims description 3
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 claims description 3
- 229960002675 xylitol Drugs 0.000 claims description 3
- 241000195940 Bryophyta Species 0.000 claims description 2
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims description 2
- JGFDZZLUDWMUQH-UHFFFAOYSA-N Didecyldimethylammonium Chemical compound CCCCCCCCCC[N+](C)(C)CCCCCCCCCC JGFDZZLUDWMUQH-UHFFFAOYSA-N 0.000 claims description 2
- HAXVCJMCUKWFSB-UHFFFAOYSA-N N',N'-diethyl-N-octylethane-1,2-diamine hydrofluoride Chemical compound F.CCCCCCCCNCCN(CC)CC HAXVCJMCUKWFSB-UHFFFAOYSA-N 0.000 claims description 2
- XVRKEHYQBKGNBA-UHFFFAOYSA-N azanium;zinc;fluoride Chemical compound [NH4+].[F-].[Zn] XVRKEHYQBKGNBA-UHFFFAOYSA-N 0.000 claims description 2
- 229910052791 calcium Inorganic materials 0.000 claims description 2
- WUKWITHWXAAZEY-UHFFFAOYSA-L calcium difluoride Chemical compound [F-].[F-].[Ca+2] WUKWITHWXAAZEY-UHFFFAOYSA-L 0.000 claims description 2
- 229910001634 calcium fluoride Inorganic materials 0.000 claims description 2
- 230000001013 cariogenic effect Effects 0.000 claims description 2
- 239000006071 cream Substances 0.000 claims description 2
- 229940078672 didecyldimethylammonium Drugs 0.000 claims description 2
- FXNRKXSSLJKNGH-UHFFFAOYSA-L dipotassium;fluoro-dioxido-oxo-$l^{5}-phosphane Chemical compound [K+].[K+].[O-]P([O-])(F)=O FXNRKXSSLJKNGH-UHFFFAOYSA-L 0.000 claims description 2
- 230000009977 dual effect Effects 0.000 claims description 2
- 230000003053 immunization Effects 0.000 claims description 2
- 229940071088 methyl cocoyl taurate Drugs 0.000 claims description 2
- 235000011929 mousse Nutrition 0.000 claims description 2
- 229940071089 sarcosinate Drugs 0.000 claims description 2
- BCISDMIQYBCHAT-UHFFFAOYSA-M sodium;2-(dodecanoylamino)ethanesulfonate Chemical compound [Na+].CCCCCCCCCCCC(=O)NCCS([O-])(=O)=O BCISDMIQYBCHAT-UHFFFAOYSA-M 0.000 claims description 2
- ZUFONQSOSYEWCN-UHFFFAOYSA-M sodium;2-(methylamino)acetate Chemical compound [Na+].CNCC([O-])=O ZUFONQSOSYEWCN-UHFFFAOYSA-M 0.000 claims description 2
- UKWMFBTXDPSTCV-UHFFFAOYSA-M sodium;2-[decanoyl(methyl)amino]ethanesulfonate Chemical compound [Na+].CCCCCCCCCC(=O)N(C)CCS([O-])(=O)=O UKWMFBTXDPSTCV-UHFFFAOYSA-M 0.000 claims description 2
- PWWJJDVDTKXWOF-UHFFFAOYSA-M sodium;2-[hexadecanoyl(methyl)amino]ethanesulfonate Chemical compound [Na+].CCCCCCCCCCCCCCCC(=O)N(C)CCS([O-])(=O)=O PWWJJDVDTKXWOF-UHFFFAOYSA-M 0.000 claims description 2
- UKSFMDODPANKJI-UHFFFAOYSA-M sodium;2-[methyl(octadecanoyl)amino]ethanesulfonate Chemical compound [Na+].CCCCCCCCCCCCCCCCCC(=O)N(C)CCS([O-])(=O)=O UKSFMDODPANKJI-UHFFFAOYSA-M 0.000 claims description 2
- HJXBXTZDPSSEST-UHFFFAOYSA-M sodium;2-[methyl(tetradecanoyl)amino]ethanesulfonate Chemical compound [Na+].CCCCCCCCCCCCCC(=O)N(C)CCS([O-])(=O)=O HJXBXTZDPSSEST-UHFFFAOYSA-M 0.000 claims description 2
- IZWPGJFSBABFGL-GMFCBQQYSA-M sodium;2-[methyl-[(z)-octadec-9-enoyl]amino]ethanesulfonate Chemical compound [Na+].CCCCCCCC\C=C/CCCCCCCC(=O)N(C)CCS([O-])(=O)=O IZWPGJFSBABFGL-GMFCBQQYSA-M 0.000 claims description 2
- 239000007787 solid Substances 0.000 claims description 2
- OJECAVYUFGICLI-UHFFFAOYSA-H tin(2+);zirconium(4+);hexafluoride Chemical compound [F-].[F-].[F-].[F-].[F-].[F-].[Zr+4].[Sn+2] OJECAVYUFGICLI-UHFFFAOYSA-H 0.000 claims description 2
- GZWNUORNEQHOAW-UHFFFAOYSA-M potassium;2-aminoacetate Chemical compound [K+].NCC([O-])=O GZWNUORNEQHOAW-UHFFFAOYSA-M 0.000 claims 1
- 238000009472 formulation Methods 0.000 description 33
- 229920000642 polymer Polymers 0.000 description 21
- 150000003839 salts Chemical class 0.000 description 20
- 239000003945 anionic surfactant Substances 0.000 description 13
- 239000003795 chemical substances by application Substances 0.000 description 13
- 229910019142 PO4 Inorganic materials 0.000 description 12
- 239000004615 ingredient Substances 0.000 description 12
- 235000021317 phosphate Nutrition 0.000 description 12
- 150000003013 phosphoric acid derivatives Chemical class 0.000 description 11
- 239000000463 material Substances 0.000 description 10
- 239000000606 toothpaste Substances 0.000 description 10
- 239000000796 flavoring agent Substances 0.000 description 9
- 239000000047 product Substances 0.000 description 9
- 235000019640 taste Nutrition 0.000 description 9
- 239000002562 thickening agent Substances 0.000 description 9
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 description 8
- 239000002253 acid Substances 0.000 description 8
- 235000013355 food flavoring agent Nutrition 0.000 description 8
- 239000000178 monomer Substances 0.000 description 8
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 7
- YUJLIIRMIAGMCQ-CIUDSAMLSA-N Ser-Leu-Ser Chemical compound [H]N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(O)=O YUJLIIRMIAGMCQ-CIUDSAMLSA-N 0.000 description 7
- 230000008901 benefit Effects 0.000 description 7
- 229920001577 copolymer Polymers 0.000 description 7
- 229920001223 polyethylene glycol Polymers 0.000 description 7
- FQENQNTWSFEDLI-UHFFFAOYSA-J sodium diphosphate Chemical compound [Na+].[Na+].[Na+].[Na+].[O-]P([O-])(=O)OP([O-])([O-])=O FQENQNTWSFEDLI-UHFFFAOYSA-J 0.000 description 7
- 235000019832 sodium triphosphate Nutrition 0.000 description 7
- 235000019818 tetrasodium diphosphate Nutrition 0.000 description 7
- LDVVTQMJQSCDMK-UHFFFAOYSA-N 1,3-dihydroxypropan-2-yl formate Chemical compound OCC(CO)OC=O LDVVTQMJQSCDMK-UHFFFAOYSA-N 0.000 description 6
- 101100256231 Mus musculus Slc5a8 gene Proteins 0.000 description 6
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 6
- 229920000388 Polyphosphate Polymers 0.000 description 6
- PTFCDOFLOPIGGS-UHFFFAOYSA-N Zinc dication Chemical compound [Zn+2] PTFCDOFLOPIGGS-UHFFFAOYSA-N 0.000 description 6
- XLOMVQKBTHCTTD-UHFFFAOYSA-N Zinc monoxide Chemical compound [Zn]=O XLOMVQKBTHCTTD-UHFFFAOYSA-N 0.000 description 6
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 6
- 239000000499 gel Substances 0.000 description 6
- 239000003921 oil Substances 0.000 description 6
- 235000019198 oils Nutrition 0.000 description 6
- 239000001205 polyphosphate Substances 0.000 description 6
- 235000011176 polyphosphates Nutrition 0.000 description 6
- 229940034610 toothpaste Drugs 0.000 description 6
- 238000010521 absorption reaction Methods 0.000 description 5
- 150000007513 acids Chemical class 0.000 description 5
- 229910052783 alkali metal Inorganic materials 0.000 description 5
- 239000001768 carboxy methyl cellulose Substances 0.000 description 5
- NBIIXXVUZAFLBC-UHFFFAOYSA-M dihydrogenphosphate Chemical compound OP(O)([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-M 0.000 description 5
- 239000006260 foam Substances 0.000 description 5
- 239000002245 particle Substances 0.000 description 5
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 5
- SQUHHTBVTRBESD-UHFFFAOYSA-N Hexa-Ac-myo-Inositol Natural products CC(=O)OC1C(OC(C)=O)C(OC(C)=O)C(OC(C)=O)C(OC(C)=O)C1OC(C)=O SQUHHTBVTRBESD-UHFFFAOYSA-N 0.000 description 4
- 230000032683 aging Effects 0.000 description 4
- 229920006318 anionic polymer Polymers 0.000 description 4
- 230000000845 anti-microbial effect Effects 0.000 description 4
- 239000002585 base Substances 0.000 description 4
- 230000001680 brushing effect Effects 0.000 description 4
- RBLGLDWTCZMLRW-UHFFFAOYSA-K dicalcium;phosphate;dihydrate Chemical compound O.O.[Ca+2].[Ca+2].[O-]P([O-])([O-])=O RBLGLDWTCZMLRW-UHFFFAOYSA-K 0.000 description 4
- 235000014113 dietary fatty acids Nutrition 0.000 description 4
- 239000000194 fatty acid Substances 0.000 description 4
- 229930195729 fatty acid Natural products 0.000 description 4
- 239000004088 foaming agent Substances 0.000 description 4
- CDAISMWEOUEBRE-GPIVLXJGSA-N inositol Chemical compound O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@H](O)[C@@H]1O CDAISMWEOUEBRE-GPIVLXJGSA-N 0.000 description 4
- 229960000367 inositol Drugs 0.000 description 4
- 150000002500 ions Chemical class 0.000 description 4
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 4
- FPYJFEHAWHCUMM-UHFFFAOYSA-N maleic anhydride Chemical compound O=C1OC(=O)C=C1 FPYJFEHAWHCUMM-UHFFFAOYSA-N 0.000 description 4
- 238000004519 manufacturing process Methods 0.000 description 4
- 229940057847 polyethylene glycol 600 Drugs 0.000 description 4
- CDAISMWEOUEBRE-UHFFFAOYSA-N scyllo-inosotol Natural products OC1C(O)C(O)C(O)C(O)C1O CDAISMWEOUEBRE-UHFFFAOYSA-N 0.000 description 4
- 239000000126 substance Substances 0.000 description 4
- 229920001285 xanthan gum Polymers 0.000 description 4
- 235000010493 xanthan gum Nutrition 0.000 description 4
- 239000000230 xanthan gum Substances 0.000 description 4
- 229940082509 xanthan gum Drugs 0.000 description 4
- 150000003751 zinc Chemical class 0.000 description 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- 208000006558 Dental Calculus Diseases 0.000 description 3
- 101100256230 Homo sapiens SLC5A8 gene Proteins 0.000 description 3
- IMQLKJBTEOYOSI-GPIVLXJGSA-N Inositol-hexakisphosphate Chemical compound OP(O)(=O)O[C@H]1[C@H](OP(O)(O)=O)[C@@H](OP(O)(O)=O)[C@H](OP(O)(O)=O)[C@H](OP(O)(O)=O)[C@@H]1OP(O)(O)=O IMQLKJBTEOYOSI-GPIVLXJGSA-N 0.000 description 3
- IMQLKJBTEOYOSI-UHFFFAOYSA-N Phytic acid Natural products OP(O)(=O)OC1C(OP(O)(O)=O)C(OP(O)(O)=O)C(OP(O)(O)=O)C(OP(O)(O)=O)C1OP(O)(O)=O IMQLKJBTEOYOSI-UHFFFAOYSA-N 0.000 description 3
- OFOBLEOULBTSOW-UHFFFAOYSA-N Propanedioic acid Natural products OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 description 3
- 102100027215 Sodium-coupled monocarboxylate transporter 1 Human genes 0.000 description 3
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 3
- 239000004480 active ingredient Substances 0.000 description 3
- 239000013543 active substance Substances 0.000 description 3
- 150000001340 alkali metals Chemical group 0.000 description 3
- 229910000147 aluminium phosphate Inorganic materials 0.000 description 3
- 125000004429 atom Chemical group 0.000 description 3
- 239000007853 buffer solution Substances 0.000 description 3
- 235000010418 carrageenan Nutrition 0.000 description 3
- 229920001525 carrageenan Polymers 0.000 description 3
- 239000008139 complexing agent Substances 0.000 description 3
- 235000011180 diphosphates Nutrition 0.000 description 3
- 201000005581 enamel erosion Diseases 0.000 description 3
- 238000005187 foaming Methods 0.000 description 3
- 235000003599 food sweetener Nutrition 0.000 description 3
- 150000004676 glycans Chemical class 0.000 description 3
- 229940005740 hexametaphosphate Drugs 0.000 description 3
- 229910052500 inorganic mineral Inorganic materials 0.000 description 3
- 239000011976 maleic acid Substances 0.000 description 3
- 235000010755 mineral Nutrition 0.000 description 3
- 239000011707 mineral Substances 0.000 description 3
- 239000010452 phosphate Substances 0.000 description 3
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 3
- 239000000467 phytic acid Substances 0.000 description 3
- 229940068041 phytic acid Drugs 0.000 description 3
- 235000002949 phytic acid Nutrition 0.000 description 3
- 239000000049 pigment Substances 0.000 description 3
- 238000006116 polymerization reaction Methods 0.000 description 3
- 229920001282 polysaccharide Polymers 0.000 description 3
- 239000005017 polysaccharide Substances 0.000 description 3
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 3
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 3
- 235000019982 sodium hexametaphosphate Nutrition 0.000 description 3
- GCLGEJMYGQKIIW-UHFFFAOYSA-H sodium hexametaphosphate Chemical compound [Na]OP1(=O)OP(=O)(O[Na])OP(=O)(O[Na])OP(=O)(O[Na])OP(=O)(O[Na])OP(=O)(O[Na])O1 GCLGEJMYGQKIIW-UHFFFAOYSA-H 0.000 description 3
- 159000000000 sodium salts Chemical class 0.000 description 3
- 239000003765 sweetening agent Substances 0.000 description 3
- 239000001577 tetrasodium phosphonato phosphate Substances 0.000 description 3
- WGIWBXUNRXCYRA-UHFFFAOYSA-H trizinc;2-hydroxypropane-1,2,3-tricarboxylate Chemical compound [Zn+2].[Zn+2].[Zn+2].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O.[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O WGIWBXUNRXCYRA-UHFFFAOYSA-H 0.000 description 3
- 239000011746 zinc citrate Substances 0.000 description 3
- 235000006076 zinc citrate Nutrition 0.000 description 3
- 229940068475 zinc citrate Drugs 0.000 description 3
- 239000011787 zinc oxide Substances 0.000 description 3
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- ZPWVASYFFYYZEW-UHFFFAOYSA-L dipotassium hydrogen phosphate Chemical compound [K+].[K+].OP([O-])([O-])=O ZPWVASYFFYYZEW-UHFFFAOYSA-L 0.000 description 1
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- 208000024693 gingival disease Diseases 0.000 description 1
- 239000004220 glutamic acid Substances 0.000 description 1
- 235000013922 glutamic acid Nutrition 0.000 description 1
- 239000010651 grapefruit oil Substances 0.000 description 1
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- 239000000665 guar gum Substances 0.000 description 1
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- WGACCFVMCVLMQZ-UHFFFAOYSA-N n-[2-(diethylamino)ethyl]octanamide;hydrofluoride Chemical compound F.CCCCCCCC(=O)NCCN(CC)CC WGACCFVMCVLMQZ-UHFFFAOYSA-N 0.000 description 1
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- NFHFRUOZVGFOOS-UHFFFAOYSA-N palladium;triphenylphosphane Chemical compound [Pd].C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1.C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1.C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1.C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1 NFHFRUOZVGFOOS-UHFFFAOYSA-N 0.000 description 1
- RUVINXPYWBROJD-UHFFFAOYSA-N para-methoxyphenyl Natural products COC1=CC=C(C=CC)C=C1 RUVINXPYWBROJD-UHFFFAOYSA-N 0.000 description 1
- XYJRXVWERLGGKC-UHFFFAOYSA-D pentacalcium;hydroxide;triphosphate Chemical compound [OH-].[Ca+2].[Ca+2].[Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O XYJRXVWERLGGKC-UHFFFAOYSA-D 0.000 description 1
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- BZQFBWGGLXLEPQ-REOHCLBHSA-N phosphoserine Chemical compound OC(=O)[C@@H](N)COP(O)(O)=O BZQFBWGGLXLEPQ-REOHCLBHSA-N 0.000 description 1
- 238000005498 polishing Methods 0.000 description 1
- 229920001308 poly(aminoacid) Polymers 0.000 description 1
- 229920001390 poly(hydroxyalkylmethacrylate) Polymers 0.000 description 1
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- 229920000515 polycarbonate Polymers 0.000 description 1
- 229920000867 polyelectrolyte Polymers 0.000 description 1
- 229920000120 polyethyl acrylate Polymers 0.000 description 1
- 229940068886 polyethylene glycol 300 Drugs 0.000 description 1
- 229920000193 polymethacrylate Polymers 0.000 description 1
- 229920005862 polyol Polymers 0.000 description 1
- 150000003077 polyols Chemical class 0.000 description 1
- 229920001451 polypropylene glycol Polymers 0.000 description 1
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- 239000011118 polyvinyl acetate Substances 0.000 description 1
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- OQZCJRJRGMMSGK-UHFFFAOYSA-M potassium metaphosphate Chemical compound [K+].[O-]P(=O)=O OQZCJRJRGMMSGK-UHFFFAOYSA-M 0.000 description 1
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- 235000018102 proteins Nutrition 0.000 description 1
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- KSAVQLQVUXSOCR-UHFFFAOYSA-M sodium lauroyl sarcosinate Chemical compound [Na+].CCCCCCCCCCCC(=O)N(C)CC([O-])=O KSAVQLQVUXSOCR-UHFFFAOYSA-M 0.000 description 1
- 229940045885 sodium lauroyl sarcosinate Drugs 0.000 description 1
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- 239000004334 sorbic acid Substances 0.000 description 1
- 235000010199 sorbic acid Nutrition 0.000 description 1
- 229940075582 sorbic acid Drugs 0.000 description 1
- 150000005846 sugar alcohols Polymers 0.000 description 1
- 150000008163 sugars Chemical class 0.000 description 1
- BDHFUVZGWQCTTF-UHFFFAOYSA-M sulfonate Chemical compound [O-]S(=O)=O BDHFUVZGWQCTTF-UHFFFAOYSA-M 0.000 description 1
- 150000003871 sulfonates Chemical class 0.000 description 1
- 230000009747 swallowing Effects 0.000 description 1
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- 230000002588 toxic effect Effects 0.000 description 1
- GTZCVFVGUGFEME-UHFFFAOYSA-N trans-aconitic acid Natural products OC(=O)CC(C(O)=O)=CC(O)=O GTZCVFVGUGFEME-UHFFFAOYSA-N 0.000 description 1
- LDHQCZJRKDOVOX-UHFFFAOYSA-N trans-crotonic acid Natural products CC=CC(O)=O LDHQCZJRKDOVOX-UHFFFAOYSA-N 0.000 description 1
- 229940078499 tricalcium phosphate Drugs 0.000 description 1
- 229910000391 tricalcium phosphate Inorganic materials 0.000 description 1
- 235000019731 tricalcium phosphate Nutrition 0.000 description 1
- 229960003500 triclosan Drugs 0.000 description 1
- 235000011178 triphosphate Nutrition 0.000 description 1
- 239000001226 triphosphate Substances 0.000 description 1
- 125000002264 triphosphate group Chemical class [H]OP(=O)(O[H])OP(=O)(O[H])OP(=O)(O[H])O* 0.000 description 1
- VSJRDSLPNMGNFG-UHFFFAOYSA-H trizinc;2-hydroxypropane-1,2,3-tricarboxylate;trihydrate Chemical compound O.O.O.[Zn+2].[Zn+2].[Zn+2].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O.[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O VSJRDSLPNMGNFG-UHFFFAOYSA-H 0.000 description 1
- GPTWCNIDKQZDFF-UHFFFAOYSA-H trizinc;diphosphate;hydrate Chemical compound O.[Zn+2].[Zn+2].[Zn+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O GPTWCNIDKQZDFF-UHFFFAOYSA-H 0.000 description 1
- 150000003722 vitamin derivatives Chemical class 0.000 description 1
- 239000011592 zinc chloride Substances 0.000 description 1
- 235000005074 zinc chloride Nutrition 0.000 description 1
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- 229940085658 zinc citrate trihydrate Drugs 0.000 description 1
- 229940077935 zinc phosphate Drugs 0.000 description 1
- OMSYGYSPFZQFFP-UHFFFAOYSA-J zinc pyrophosphate Chemical compound [Zn+2].[Zn+2].[O-]P([O-])(=O)OP([O-])([O-])=O OMSYGYSPFZQFFP-UHFFFAOYSA-J 0.000 description 1
- NWONKYPBYAMBJT-UHFFFAOYSA-L zinc sulfate Chemical compound [Zn+2].[O-]S([O-])(=O)=O NWONKYPBYAMBJT-UHFFFAOYSA-L 0.000 description 1
- 229960001763 zinc sulfate Drugs 0.000 description 1
- 229910000368 zinc sulfate Inorganic materials 0.000 description 1
Landscapes
- Cosmetics (AREA)
Abstract
The present disclosure relates to oral care compositions comprising zinc phosphate, a fluoride source, and a taurate surfactant. In one aspect, the compositions of the present disclosure may be used to treat or reduce aggressive tooth demineralization, gingivitis, plaque, and caries.
Description
Cross Reference to Related Applications
The present application claims the benefit of priority from U.S. provisional patent application serial No. 63/192,876, filed 5/25/2021, and U.S. provisional patent application serial No. 63/221,703, filed 7/2021, each of which is incorporated herein by reference in its entirety.
Technical Field
The present disclosure relates to oral care compositions comprising zinc phosphate, a fluoride source, and a taurate surfactant. In one aspect, the compositions of the present disclosure may be used to treat or reduce aggressive tooth demineralization, gingivitis, plaque, and caries. In one aspect, the oral care composition comprises zinc phosphate, sodium fluoride, and at least one taurate surfactant.
Background
Dental erosion involves demineralization and damage to tooth structure due to acid erosion from non-bacterial sources. Erosion initially occurs in enamel and, if not inhibited, may progress to the underlying dentin.
Dental plaque is a viscous biofilm or group of bacteria that is commonly present between teeth, along the gum line and below the edge of the gum line. Plaque can cause caries and periodontal problems such as gingivitis and periodontitis. Caries decay or tooth demineralization is caused by acids produced by bacterial degradation of fermentable sugars.
Soluble zinc salts such as zinc citrate have been used in dentifrice compositions but have several disadvantages. Zinc ions in solution impart an unpleasant astringent taste and thus it is difficult to obtain a formulation that provides effective levels of zinc and also has acceptable organoleptic properties. In addition, free zinc ions may react with fluoride ions to form zinc fluoride, which is insoluble and thus reduces the availability of both zinc and fluoride. Finally, the zinc ions will react with anionic surfactants such as sodium lauryl sulfate, thereby interfering with foaming and cleaning.
Although zinc phosphate (Zn) 3 (PO 4 ) 2 ) May be soluble in acidic or basic solutions, such as solutions of mineral acids, acetic acid, ammonia or alkali metal hydroxides, but which are insoluble in water. See, e.g., merck Index, 13 th edition, (2001) page 1812, monograph number 10205. In part because zinc phosphate is considered in the art to be a generally inert material, it is commonly used in dental cements, such as in the cementing of inlays, crowns, bridges and appliances, which are intended to last in the mouth for many years. Zinc phosphate dental cements are generally prepared by mixing zinc oxide and magnesium oxide powders with a main component consisting of phosphoric acid A liquid mixture of water and buffer, so that a cement comprising zinc phosphate is formed in situ by reaction with phosphoric acid.
Sodium lauryl sulfate (sodium lauryl sulfate, SLS) is widely used in dentifrice formulation surfactants. SLS has benefits such as being neutral in terms of product taste and generally not affecting the stability of the active ingredient. However, recently consumers are interested in developing a variety of oral care products that do not include sodium lauryl sulfate. However, one of the drawbacks of developing formulations without SLS is that the use of new surfactant combinations in various oral care compositions (e.g., toothpastes) may result in product segregation due to changes in the balance of ingredients in the formulation. In some cases, surfactant substitution (e.g., substitution of a surfactant for SLS) may have a negative impact on taste or active ingredient stability. Furthermore, the absence of sodium lauryl sulfate may negatively affect the microbiological stability of the formulation. There are also production benefits to having SLS in a given formulation. By removing the SLS, the product may be caused to air during production and it may be more difficult to clean the equipment after the manufacturing process.
Thus, there is a need to provide improved zinc and fluoride containing products for treating or preventing enamel erosion that do not contain sodium lauryl sulfate, but nonetheless have sufficient stability, antimicrobial effectiveness, and reduce plaque and treat or control gingivitis as conventional products that contain sodium lauryl sulfate surfactants.
Disclosure of Invention
The applicant has unexpectedly found how to formulate an oral care composition having zinc phosphate, a taurate surfactant, and a fluoride ion source, wherein the composition is free or substantially free of sodium lauryl sulfate. The formulations of the present disclosure comprising a taurate surfactant as defined by formula (1) (e.g., sodium methyl cocoyl taurate) are unexpectedly physically stable and do not segregate. The formulations of the present disclosure (e.g., composition 1.0 and any of the following, etc.) may maintain acceptable fluoride and zinc stability and acceptable taste despite not comprising sodium lauryl sulfate.
Disclosed herein are oral care compositions comprising:
zinc phosphate;
a fluoride source; and
a taurine salt surfactant represented by the formula (1):
Wherein R is 1 Is a saturated or unsaturated, linear or branched alkyl chain having 6 to 18C atoms, R 2 Is H or methyl, and M + H, sodium or potassium.
Methods and uses for the composition are also described throughout. The compositions disclosed herein provide improved demineralization protection and enhanced antimicrobial activity compared to the prior art. In some embodiments, zinc phosphate is added to the dentifrice as a preformed salt. In some embodiments, the oral care composition is a toothpaste or an oral gel composition.
Further areas of applicability of the present disclosure will become apparent from the detailed description provided hereinafter. It should be understood that the detailed description and specific examples, while indicating the preferred embodiment of the disclosure, are intended for purposes of illustration only and are not intended to limit the scope of the disclosure.
Detailed Description
The following description of the preferred embodiment(s) is merely exemplary in nature and is in no way intended to limit the disclosure, its application, or uses.
As used throughout, ranges are used as shorthand for describing the individual values and each value that are within the range. Any value within the range can be selected as the terminus of the range. In addition, all references cited herein are incorporated by reference in their entirety. In the event of a conflict between a definition in the present disclosure and a definition of a cited reference, the present disclosure controls.
Unless otherwise specified, all percentages and amounts expressed herein and elsewhere in this specification are to be understood as referring to percentages by weight of the entire composition. The given amount is based on the effective weight of the material.
It has unexpectedly been found that oral care compositions comprising zinc phosphate, stannous fluoride, and taurine salt surfactants selected in specific concentrations and amounts provide effective anti-erosion and antimicrobial properties as compared to similar oral care formulations comprising anionic surfactants in place of taurine salt surfactants. Furthermore, the compositions of the present disclosure provide stable formulations comprising zinc ions and fluoride ions compared to similar formulations in the prior art comprising sodium lauryl sulfate in place of a taurate surfactant.
Composition 1.0, which may comprise a toothpaste or an oral gel, and the following, and the like, may comprise from 10% to 99% water by weight of the composition. For example, the composition may comprise at least 10%, 15%, 20%, 25%, 30%, 35% or 40% water, up to, for example, 60%, 70%, 80%, 90%, 95% or 99% water, by weight of the composition. As used herein, the amount of water refers to water added directly to the composition, as well as water added as part of the ingredients or components added as an aqueous solution. In some embodiments, the composition comprises from 10% to 60% water, or from 10% to 50% water, or from 10% to 40% water, or from 10% to 30% water, or from 15% to 30% water, or from 20% to 30% water, or about 25% water, by weight of the composition.
As used herein, the term "preformed salt" when used in reference to zinc phosphate means that the zinc phosphate is not formed in situ in the oral care composition, for example by the reaction of phosphoric acid and another zinc salt.
In one aspect, the present disclosure thus provides an oral care composition (composition 1.0), wherein the oral care composition comprises:
a. ) An orally acceptable carrier, which is a solid carrier,
b. ) Zinc phosphate (e.g., zinc phosphate)
c. ) A fluoride ion source, and
d. ) A taurine salt surfactant represented by the formula (1):
wherein R is 1 Is a saturated or unsaturated, linear or branched alkyl chain having 6 to 18C atoms, R 2 Is H or methyl, and M + Is H, sodium or potassium (e.g., sodium methyl cocoyl taurate).
For example, composition 1.0 may further comprise the following:
1.1 composition 1.0 oral care composition, wherein R 1 Is a saturated or unsaturated, straight or branched alkyl chain having 8 to 14C atoms.
1.2 1.0 or 11, wherein the taurate surfactant comprises one or more surfactants selected from the group consisting of: potassium cocoyl taurate, potassium methyl cocoyl taurate, sodium caproyl methyl taurate, sodium cocoyl taurate, sodium lauroyl taurate, sodium methyl cocoyl taurate, sodium methyl lauroyl taurate, sodium methyl myristoyl taurate, sodium methyl oleoyl taurate, sodium methyl palmitoyl taurate, sodium methyl stearoyl taurate, and combinations thereof.
1.3 any of the foregoing oral care compositions, wherein the taurine salt surfactant comprises one or more surfactants selected from the group consisting of: sodium lauroyl methyl taurate (or sodium methyl lauroyl taurate), sodium methyl cocoyl taurate, and combinations thereof.
1.4 any of the foregoing oral care compositions, wherein the taurate surfactant comprises sodium methyl cocoyl taurate (e.g., 1% to 3% sodium methyl cocoyl taurate by weight) (e.g., 1.75% to 1.95% sodium methyl cocoyl taurate by weight) (e.g., about 2% sodium methyl cocoyl taurate by weight).
1.5 any of the foregoing oral care compositions, wherein the taurine salt surfactant is present in the following amounts: from 0.4% to 3%, for example, from 0.4% to 2.5%, from 0.4% to 2%, from 0.4% to 1.5%, from 0.5% to 3%, from 0.8% to 3%, from 1% to 3%, from 1.2% to 2.7%, from 1.5% to 3%, from 2% to 3%, from 1% to 2.8%, from 1% to 2.7%, from 1% to 2.5%, from 1.5% to 2.8%, from 1.5% to 2.5%, from 1.8% to 3%, from 1.8% to 2.8%, from 1.8% to 2.7%, from 1.8% to 2.5%, for example, about 2%, by weight of the composition.
1.6 any of the foregoing oral care compositions, wherein the zinc phosphate is a preformed salt of zinc phosphate (e.g., zinc phosphate hydrate).
1.7 any of the foregoing oral care compositions, wherein the amount of zinc phosphate relative to the weight of the oral care composition is from 0.05% to 10% by weight, such as from 0.1% to 8% by weight, or from 0.5% to 5% by weight, or from 0.5% to 4% by weight, or from 1% to 3% by weight, or from 2% to 3% by weight, or from about 1% or about 2% or about 2.25% or about 2.5% by weight.
1.8 any of the foregoing oral care compositions, wherein the fluoride ion source is present in the following amounts relative to the weight of the oral care composition: 0.01% to 5% by weight, for example 0.05% to 4% by weight, or 0.1% to 3% by weight, or 0.2% to 2% by weight, or 0.3% to 1% by weight (e.g., about 0.53% by weight), or 0.3% to 0.5% by weight, or about 0.32% by weight (e.g., 0.32% by weight).
1.9 any of the foregoing oral care compositions, wherein the fluoride source is selected from the group consisting of: sodium fluoride, potassium fluoride, calcium fluoride, zinc ammonium fluoride, lithium fluoride, ammonium fluoride, stannous fluorozirconate, sodium monofluorophosphate, potassium monofluorophosphate, laurylamine hydrofluoric acid (laurylamine hydrofluoride), diethylaminoethyl octylamide hydrofluoric acid (diethylaminoethyloctoylamide hydrofluoride), didecyldimethyl ammonium fluoride, cetylpyridine fluoride Fluorinated dilaurylmeline->Stannous fluoride sarcosinate, potassium glycine fluoride, glycine hydrofluoric acid (glycine hydrofluoride), amine fluoride, and combinations thereof.
1.10 the foregoing oral care composition, wherein the fluoride ion source comprises sodium fluoride (e.g., 0.2% to 2% sodium fluoride by weight).
1.11 1.9, wherein the fluoride ion source comprises stannous fluoride.
1.12 1.9, wherein the fluoride ion source comprises sodium monofluorophosphate.
1.13 1.9, wherein the fluoride ion source comprises sodium fluoride and stannous fluoride (e.g., wherein the combination is present at 0.1% to 2% by weight relative to the total weight of the composition).
1.14 any of the foregoing oral care compositions, wherein the composition comprises water in the following amounts relative to the weight of the oral care composition: 10% or more by weight, for example 10% to 90%, or 10% to 80%, or 10% to 70%, or 10% to 60%, or 10% to 50%, or 10% to 40%, or 10% to 30%, or 15% to 30%, 15% to 40%, 20% to 35%, or 20% to 50%, 25% to 35%, or 30% to 35%, or about 25% by weight, or about 27% by weight, or about 30% by weight, or about 34% by weight of the composition.
1.15 any of the foregoing oral care compositions further comprising an organic buffer system, wherein the buffer system comprises a carboxylic acid and one or more conjugate base salts thereof, such as alkali metal salts thereof (e.g., citric acid and sodium citrate).
1.16 any of the foregoing oral care compositions, wherein the composition comprises an organic acid buffer system in the following amounts, as measured by the combined amounts of an organic acid and any conjugate base salt (e.g., citric acid and sodium citrate): 0.1% to 5.0% by weight of the composition; for example, from 0.5% to 4.0%, or from 1.0% to 3.0%, or from 1.5% to 3.0%, or from 1.0% to 2.4%, or from 1.0% to 2.0%, or from 1.0% to 1.5%, or about 1.2% by weight of the composition.
1.17 any of the foregoing oral care compositions, wherein the oral care composition further comprises an abrasive, such as a silica abrasive, a calcium abrasive, and other abrasives as disclosed herein.
1.18 any of the foregoing oral care compositions further comprising one or more humectants as described herein, e.g., selected from sorbitol, glycerin, xylitol, and propylene glycol, or a combination thereof, e.g., a combination of sorbitol and glycerin.
1.19 1.18, wherein the humectant comprises sorbitol (e.g., 20% to 55% sorbitol by weight) (e.g., 25% to 35% by weight).
1.20 1.18, wherein the humectant comprises glycerin (e.g., 1% to 10% glycerin by weight) (e.g., 7% to 10% glycerin by weight).
1.21 1.18, wherein the humectant comprises sorbitol and glycerin.
1.22 any of the foregoing oral care compositions further comprising a zwitterionic surfactant.
1.23 the foregoing oral care composition, wherein the zwitterionic surfactant comprises cocamidopropyl betaine ("CAPB") (e.g., in an amount of 0.5% to 5% by weight) (e.g., about 0.45% by weight) (e.g., about 0.6% by weight) (e.g., about 1.5% by weight) (e.g., about 2% by weight).
1.24 any of the foregoing oral care compositions further comprising an effective amount of one or more alkali metal phosphates, such as orthophosphates, pyrophosphates, tripolyphosphates, tetraphosphates, or higher polyphosphates.
1.25 1.24, wherein the alkali metal phosphate comprises tetrasodium pyrophosphate or tetrapotassium pyrophosphate, for example, in an amount of from 0.5% to 5% by weight of the composition, for example, from 1% to 4% by weight, or from about 2% to 4% by weight, or from about 1% to 2% by weight, or about 1.5% by weight, or about 2% by weight, or about 4% by weight.
1.26 1.24 or 1.25, wherein the alkali metal phosphate comprises sodium or potassium tripolyphosphate, for example in an amount of from 0.5% to 6% by weight of the composition, for example from 1% to 4% by weight, or from 2% to 3% by weight, or about 3% by weight.
1.27 any of the foregoing oral care compositions, further comprising a whitening agent.
1.28 any of the foregoing oral care compositions further comprising one or more sources of zinc ions other than the zinc phosphate, such as a zinc salt selected from the group consisting of zinc citrate, zinc oxide, zinc lactate, zinc pyrophosphate, zinc sulfate, zinc chloride, and combinations thereof.
1.29 any of the foregoing oral care compositions, wherein the oral care composition is in a form selected from the group consisting of: dentifrices (e.g., toothpastes or oral gels), powders (e.g., toothpowders), creams, mouthwashes, mousses, foams, oral sprays, oral tablets, strips, or gums (e.g., chewing gums).
1.30, wherein the pH of the composition is from 6 to 9, such as from 6.5 to 8, or from 6.5 to 7.5, or about 7.0.
1.31 any of the foregoing oral care compositions, wherein the composition is a single phase composition (e.g., not a dual phase composition).
1.32 any of the foregoing oral care compositions, wherein the composition does not comprise one or more of zinc oxide, zinc citrate, or zinc lactate.
1.33 any of the foregoing oral care compositions, wherein the zinc phosphate is the sole source of zinc ions.
1.34 any of the foregoing oral care compositions, wherein the composition is substantially free or free of phosphates having more than four phosphate groups.
1.35 any of the foregoing oral care compositions, wherein the composition is substantially free or free of phosphates having more than three phosphate groups.
1.36 any of the foregoing oral care compositions, wherein the composition is substantially free or free of hexametaphosphate (e.g., sodium hexametaphosphate).
1.37 any of the foregoing oral care compositions, wherein the composition is effective when applied to the oral cavity, for example, by rinsing, optionally in combination with brushing: (i) reducing or inhibiting the formation of dental caries, (ii) reducing, repairing or inhibiting pre-caries lesions of enamel, for example, as detected by quantitative light-induced fluorescence (QLF) or Electrical Caries Measurement (ECM), (iii) reducing or inhibiting demineralization and promoting remineralization of teeth, (iv) reducing hypersensitivity of teeth, (v) reducing or inhibiting gingivitis, (vi) promoting healing of ulcers or wounds in the mouth, (vii) reducing the level of acidogenic bacteria, (viii) increasing the relative level of arginine-decomposing bacteria, (ix) inhibiting microbial biofilm formation in the oral cavity, (x) increasing and/or maintaining plaque pH at a level of at least pH 5.5 after a sugar challenge, (xi) reducing plaque accumulation, (xii) treating, alleviating or reducing dry mouth, (xiii) cleaning teeth and oral cavity, (xiv) reducing erosion, (xv) preventing dental caries and/or whitening teeth, (xvi) immunizing teeth against cariogenic bacteria; and/or (xvii) promote general health, including cardiovascular health, for example by reducing the likelihood of systemic infection occurring via oral tissue.
1.38 any of the foregoing oral care compositions, wherein the composition further comprises a polymer selected from the group consisting of: carboxymethyl cellulose (free form or salt, such as sodium salt), gums (e.g., xanthan gum, carrageenan, or gum arabic), polyethylene glycols (e.g., polyethylene glycol 200, polyethylene glycol 400, polyethylene glycol 600, or polyethylene glycol 800, or mixtures thereof), and combinations thereof, such as mixtures of sodium carboxymethyl cellulose, xanthan gum, polyethylene glycol 600.
1.39 composition 1.38 wherein the polymer comprises sodium carboxymethyl cellulose.
1.40 composition 1.38 wherein the polymer comprises xanthan gum.
1.41 composition 1.38, wherein the polymer comprises polyethylene glycol 600.
1.42 any of the foregoing oral care compositions further comprising a silica thickener and/or silica abrasive.
1.43, wherein the oral cavity isThe care composition comprises an additional anionic surfactant that is not sodium lauryl sulfate, wherein the additional anionic surfactant is selected from the group consisting of: water-soluble salts of higher fatty acid monoglyceride monosulfates (e.g., sodium salt of monosulfated monoglyceride of hydrogenated coconut oil fatty acids), sodium coco monoglyceride sulfate, higher alkyl ether sulfates (e.g., having the formula CH) 3 (CH 2 ) m CH 2 (OCH 2 CH 2 ) n OSO 3 X, where m is 6 to 16, such as 10, n is 1 to 6, such as 2, 3 or 4, and X is Na or K, such as sodium laureth-2 sulfate (CH 3 (CH 2 ) 10 CH 2 (OCH 2 CH 2 ) 2 OSO 3 Na)), higher alkylaryl sulfonates such as sodium dodecyl benzene sulfonate (sodium laurylbenzene sulfonate), higher alkyl sulfoacetates (such as sodium laurylsulfonate (sodium laurylsulfonate)), higher fatty acid esters of 1, 2-dihydroxypropane sulfonate, sulfolaurate (N-2-ethyl laurate potassium sulfoacetamide) and sodium lauryl sarcosinate.
1.44 any of the foregoing oral care compositions, wherein the oral care composition is free of sodium lauryl sulfate.
1.45 any of the foregoing oral care compositions, wherein the composition comprises:
zinc phosphate;
sodium fluoride;
sodium methyl cocoyl taurate; and
an orally acceptable carrier.
1.46 any of the foregoing oral care compositions, wherein the composition comprises:
0.5% to 4% by weight of the total composition of zinc phosphate;
sodium fluoride;
0.5% to 3% sodium methyl cocoyl taurate (e.g., about 2% SMCT);
water in an amount of 10% to 40% by weight of the total composition; and
an orally acceptable carrier.
1.47, wherein the composition comprises:
zinc phosphate;
sodium fluoride;
0.5% to 3% sodium methyl cocoyl taurate (e.g., about 2% SMCT);
water in an amount of 10% to 40% by weight of the total composition;
an orally acceptable carrier; and is also provided with
Wherein the composition is free of sodium lauryl sulfate.
1.48 any of the foregoing oral care compositions, wherein the composition comprises:
zinc phosphate;
stannous fluoride;
sodium methyl cocoyl taurate (e.g., 0.5% to 3%) (e.g., about 2%)
SMCT);
Water in an amount of 10% to 50% by weight of the total composition;
an orally acceptable carrier.
1.49, wherein the composition comprises:
zinc phosphate;
stannous fluoride;
sodium methyl cocoyl taurate (e.g., 0.5% to 3%) (e.g., about 2% smct);
water in an amount of 10% to 50% by weight of the total composition;
an orally acceptable carrier; and is also provided with
Wherein the composition does not contain any sodium lauryl sulfate.
1.50 any of the foregoing oral care compositions, wherein the composition comprises:
zinc phosphate;
stannous fluoride;
sodium methyl cocoyl taurate (e.g., 0.5% to 3%) (e.g., about 2% smct);
Zwitterionic surfactants (e.g., cocamidopropyl betaine)
Water in an amount of 10% to 50% by weight of the total composition; and
an orally acceptable carrier.
1.51 any of the foregoing oral care compositions, wherein the composition comprises:
zinc phosphate;
stannous fluoride;
sodium methyl cocoyl taurate (e.g., 0.5% to 3%) (e.g., about 2% smct);
zwitterionic surfactants (e.g., cocamidopropyl betaine)
Water in an amount of 10% to 50% by weight of the total composition; and
an orally acceptable carrier;
wherein the composition does not contain any sodium lauryl sulfate.
1.52 any of the foregoing compositions comprising the following ingredients:
1.53 may employ any of the foregoing oral care compositions comprising zinc phosphate in an amount effective to prevent enamel erosion and/or provide any of the other benefits described herein. Examples of suitable amounts of zinc phosphate may range from 0.05% to 5% by weight, relative to the weight of the oral care composition, for example from 0.1% to 4% by weight, or from 0.5% to 3% by weight, or from 0.5% to 2% by weight, or from 0.8% to 1.5% by weight, or from 0.9% to 1.1% by weight, or about 1% by weight.
1.54, wherein the composition does not comprise any sodium lauryl sulfate.
1.55 any of the foregoing oral care compositions, wherein the composition comprises:
0.5 to 4% by weight of zinc phosphate;
0.2% to 2% by weight (e.g., about 0.45% by weight) of stannous fluoride;
0.05% to 2% by weight (e.g., about 0.78% by weight) sodium fluoride;
sodium methyl cocoyl taurate (e.g., 0.5% to 3%) (e.g., about 2% smct);
water in an amount of 10% to 50% by weight of the total composition (e.g., about 25% by weight) (e.g., about 30% by weight); and
an orally acceptable carrier.
1.56 any of the foregoing oral care compositions, wherein the composition comprises:
0.5 to 4% by weight of zinc phosphate;
0.2% to 2% by weight (e.g., about 0.45% by weight) of stannous fluoride;
0.05% to 2% by weight (e.g., about 0.78% by weight) sodium fluoride;
sodium methyl cocoyl taurate (e.g., 0.5% to 3%) (e.g., about 2% smct);
water in an amount of 10% to 50% by weight of the total composition (e.g., about 25% by weight) (e.g., about 30% by weight);
An orally acceptable carrier; and is also provided with
Wherein the composition does not contain any sodium lauryl sulfate.
1.57, wherein the composition comprises:
0.5 to 4% by weight of zinc phosphate;
0.2% to 2% by weight (e.g., about 0.45% by weight) of stannous fluoride;
0.05% to 2% by weight (e.g., about 0.78% by weight) sodium fluoride;
sodium methyl cocoyl taurate (e.g., 0.5% to 3%) (e.g., about 2% smct);
zwitterionic surfactants (e.g., cocamidopropyl betaine);
water in an amount of 10% to 50% by weight of the total composition (e.g., about 25% by weight) (e.g., about 30% by weight); and is also provided with
Wherein the composition does not contain any sodium lauryl sulfate.
1.58 any of the foregoing oral care compositions, wherein the composition is free of sodium lauryl sulfate.
1.59 any of the foregoing oral care compositions, wherein the composition comprises sodium fluoride in an amount of from 0.05% to 2% by weight of the composition (e.g., about 0.07% by weight).
1.60 any of the foregoing oral care compositions comprising hyaluronic acid.
Formulations of the present disclosure (e.g., composition 1.0 and any of the following, etc.) comprising zinc phosphate and taurine salt surfactants do not exhibit the poor taste and mouthfeel, poor fluoride delivery, and poor foaming and cleaning associated with conventional zinc-based oral care products that use more soluble zinc salts. And the formulations of the present disclosure can provide acceptable taste, mouthfeel, foaming, and fluoride delivery expected by consumers for similar oral care compositions comprising sodium lauryl sulfate as the primary surfactant.
In one aspect, in the compositions of the present disclosure (e.g., composition 1.0 and any of the following, etc.), the combination of zinc and a taurate surfactant (e.g., sodium methyl cocoyl taurate) in the oral care composition does not affect the product stability of a silica toothpaste comprising zinc phosphate, tetrasodium pyrophosphate, and sodium fluoride, wherein the effect on stability is measured relative to a similar oral care composition using sodium lauryl sulfate as the primary surfactant. In another aspect, the compositions of the present disclosure (e.g., any of composition 1.0 and the following, etc.) do not comprise sodium lauryl sulfate, but rather may be formulated as a single phase composition that does not separate.
The compositions of the present disclosure (e.g., any of composition 1.0 and the following, etc.) may optionally comprise additional ingredients suitable for use in oral care compositions. Examples of such ingredients include active agents such as fluoride sources and/or phosphate sources other than zinc phosphate. The composition may be formulated in a suitable dentifrice base, for example, comprising an abrasive (e.g., a silica abrasive), a surfactant, a foaming agent, a vitamin, a polymer, an enzyme, a humectant, a thickener, an additional antimicrobial agent, a preservative, a flavoring agent, a colorant, and/or combinations thereof. Examples of suitable dentifrice bases are known in the art. Alternatively, the composition may be formulated as a gel (e.g., for use in a dental tray), chewing gum, lozenge or menthol. Examples of suitable additional ingredients that may be used in the compositions of the present disclosure are discussed in more detail below.
As used herein, "oral care composition" refers to compositions that are palatable and safe for topical application to the oral cavity and provide benefits to the teeth and/or oral cavity, with the intended use including oral care, oral hygiene, and/or oral appearance, or with the intended method of use including application to the oral cavity. Thus, the term "oral care composition" specifically excludes compositions that are highly toxic, unpalatable, or otherwise unsuitable for application to the oral cavity. In some embodiments, the oral care composition is not intended to be swallowed, but rather remains in the oral cavity for a time sufficient to affect the intended utility. The oral care compositions as disclosed herein can be used in non-human mammals such as companion animals (e.g., dogs and cats) as well as for human use. In some embodiments, the oral care compositions as disclosed herein are for human use. Oral care compositions include, for example, dentifrices and mouthwashes. In some embodiments, the present disclosure provides mouthwash formulations.
As used herein, "orally acceptable" refers to materials that are safe and palatable at the relevant concentrations for oral care formulations, such as mouthwashes or dentifrices.
As used herein, an "orally acceptable carrier" refers to any carrier that can be used to formulate the oral care compositions disclosed herein. An orally acceptable carrier is not harmful to mammals in the amounts disclosed herein when retained in the mouth without swallowing for a time sufficient to allow effective contact with the tooth surfaces as required herein. In general, an orally acceptable carrier is not harmful even if inadvertently swallowed. Suitable orally acceptable carriers include, for example, one or more of the following: water, thickening agents, buffering agents, humectants, surfactants, abrasives, sweeteners, flavoring agents, pigments, dyes, anticaries agents, antibacterial agents, whitening agents, desensitizing agents, vitamins, preservatives, enzymes, and mixtures thereof.
Active agent: the compositions of the present disclosure (e.g., composition 1.0 and any of the following, etc.) may comprise a variety of other agents that are active for protecting and enhancing the strength and integrity of enamel and tooth structures and/or reducing bacteria and associated caries and/or gum disease or providing other desired benefits. The effective concentration of the active ingredient used herein will depend on the particular agent and delivery system used. The concentration will also depend on the exact salt or polymer selected. For example, where the active agent is provided in salt form, the counter ion will affect the weight of the salt, such that if the counter ion is heavier, more salt by weight will be required to provide the same concentration of active ion in the final product.
The compositions of the present disclosure may comprise 0.1 wt% to 1 wt% antimicrobial agent, for example about 0.3 wt%. Any suitable antimicrobial active may be employed.
Fluoride ion source: the oral care compositions of the present disclosure (e.g., oral care composition of any of composition 1.0 and the following, etc.) can comprise one or more additional fluoride ion sources, e.g., soluble fluoride salts. Various fluoride ion-generating materials may be employed as a source of soluble fluoride in the compositions of the invention. Examples of suitable fluoride ion-generating materials are found in U.S. Pat. No. 3,535,421 to Briner et al, U.S. Pat. No. 4,885,155 to Parran, jr et al, and U.S. Pat. No. 3,678,154 to Widder et al, the disclosures of each of which are incorporated herein by reference in their entirety. Representative fluoride ion sources include, but are not limited to, sodium fluoride, potassium fluoride, sodium monofluorophosphate, fluorineSodium silicate, ammonium fluorosilicate, amine fluoride, ammonium fluoride, and combinations thereof. In certain embodiments, the fluoride ion source comprises sodium fluoride, sodium monofluorophosphate, and mixtures thereof. In certain embodiments, the oral care compositions of the present disclosure can comprise stannous fluoride and any additional fluoride ion source or fluoride providing agent in an amount sufficient to provide a total of 25ppm to 25,000ppm (mass fraction), typically at least 500ppm, e.g., 500ppm to 2000ppm, e.g., 1000ppm to 1600ppm, e.g., about 1450ppm fluoride ions. The appropriate level of fluoride will depend on the particular application. Toothpastes for use by average consumers will typically have 1000ppm to about 1500ppm, with children's toothpastes being somewhat lower. The dentifrice or coating agent for professional applications may have up to 5,000ppm or even about 25,000ppm of fluoride. Additional fluoride ion sources may be added to the compositions of the present disclosure at levels of from 0.01% to 10% by weight, or from 0.03% to 5% by weight, in one embodiment from 0.1% to 1% by weight, based on the weight of the composition. As discussed above, the weight of the fluoride salt that provides the appropriate level of fluoride ions will vary based on the weight of the counter ions in the salt.
Abrasive material: the oral care compositions of the present disclosure (e.g., composition 1.0 and any of the following, etc.) can comprise an abrasive. Examples of suitable abrasives include silica abrasives such as standard cleaning force silica, gao Qingjie force silica, or any other suitable abrasive silica. Further examples of abrasives that may be used in addition to or in place of the silica abrasive include, for example, calcium phosphate abrasives, such as tricalcium phosphate (Ca 3 (PO 4 ) 2 ) Hydroxyapatite (Ca) 10 (PO 4 ) 6 (OH) 2 ) Or dicalcium phosphate dihydrate (CaHPO) 4 ·2H 2 O, also sometimes referred to herein as DiCal) or calcium pyrophosphate; a calcium carbonate abrasive; or an abrasive such as sodium metaphosphate, potassium metaphosphate, aluminum silicate, calcined alumina, bentonite or other siliceous material; or a combination thereof.
Silica abrasive polishing materials and other abrasives useful herein generally haveAverage particle sizes ranging from 0.1 microns to 30 microns, e.g., 5 microns to 15 microns. The silica abrasive may be derived from precipitated silica or silica gels, such as silica xerogels described in U.S. patent No. 3,538,230 to Pader et al and U.S. patent No. 3,862,307 to Digiulio, the disclosures of which are incorporated herein by reference in their entirety. Specific silica xerogels are described by W.R.Grace &Co.Davison Chemical Division under the trade nameAnd (5) selling. The precipitated silica material comprises a silica material known by J.M. Huber Corp. Under the trade name +.>Those sold include silica with the designations Zeodent 115 and 119. These silica abrasives are described in U.S. Pat. No. 4,340,583 to Wason, the disclosure of which is incorporated herein by reference in its entirety. In certain embodiments, abrasive materials useful in the practice of oral care compositions according to the present disclosure include silica gels and precipitated amorphous silica having an oil absorption value of less than 100cc/100g silica, for example, 45cc/100g silica to 70cc/100g silica. The oil absorption value was measured using the ASTA Rub-Out Method (Rub-Out Method) D281. In certain embodiments, the silica is a colloidal particle having an average particle size of 3 microns to 12 microns and 5 microns to 10 microns. Examples of low oil absorption silica abrasives useful in the practice of the present disclosure are described by w.r.Grace&Co., balmo, malyland. Davison Chemical Division under the trade name Sylodent +.>And (5) selling. Sylodent 650->As one example of a low oil absorption silica abrasive useful in the practice of the present disclosure, it is a silica hydrogel composed of particles of colloidal silica A gum, the particles having a water content of 29% by weight, an average diameter of 7 microns to 10 microns and an oil absorption of less than 70cc/100g silica. In some aspects, the compositions of the present disclosure comprise synthetic amorphous silica, such as Sylodent VP5 (w.r.Grace) as described in U.S. patent application 2012/0100193 (the contents of which are incorporated herein by reference)&Davison Chemical Division of co (balm, maryland, usa)).
Any suitable amount of silica abrasive may be employed. Examples of suitable amounts include 10 wt% or more dry weight silica particles, such as 15 wt% to 30 wt% or 15 wt% to 25 wt%, based on the total weight of the composition.
Foaming agent: the oral care compositions of the present disclosure (e.g., oral care composition of any of composition 1.0 and the following, etc.) can comprise an agent that increases the amount of foam generated when brushing the oral cavity. Illustrative examples of foam increasing agents include, but are not limited to, polyoxyethylene and certain polymers, including, but not limited to, alginate polymers. Polyoxyethylene can increase the amount of foam and the consistency of foam produced by the oral care compositions of the present disclosure. Polyoxyethylene is also commonly referred to as polyethylene glycol ("PEG") or polyethylene oxide. The polyoxyethylene suitable for use in the compositions of the present disclosure may have a molecular weight of 200,000 to 7,000,000. In one embodiment, the molecular weight may be 600,000 to 2,000,000, and in another embodiment 800,000 to 1,000,000.Is a trade name for high molecular weight polyoxyethylene produced by Union Carbide. The foaming agent (e.g., polyoxyethylene) may be present in an amount of 0.1% to 50%, in one embodiment 0.5% to 20%, and in another embodiment 1% to 10%, or 2% to 5% by weight of the oral care composition of the present disclosure.
Surface active agent: the oral care compositions of the present disclosure (e.g., composition 1.0 and oral care combinations of any of the following, and the like)An anionic surfactant other than sodium lauryl sulfate). In one aspect, the taurate surfactant of formulation 1 (e.g., composition 1.0 and any of the following, etc.) can be an anionic surfactant. For example, any of composition 1.0 and the following, etc. may optionally comprise any of the following surfactants:
i. water-soluble salts of higher fatty acid monoglyceride monosulfates (e.g., sodium salt of monosulfated monoglyceride of hydrogenated coconut oil fatty acids), sodium coco monoglyceride sulfate,
higher alkyl ether sulfates, e.g. of formula CH 3 (CH 2 ) m CH 2 (OCH 2 CH 2 ) n OSO 3 X, where m is 6 to 16, such as 10, n is 1 to 6, such as 2, 3 or 4, and X is Na or K, such as sodium laureth-2 sulfate (CH 3 (CH 2 ) 10 CH 2 (OCH 2 CH 2 ) 2 OSO 3 Na),
Higher alkylaryl sulfonates such as sodium dodecyl benzene sulfonate (sodium laurylbenzenesulfonate), iv higher alkylsulfonylacetate such as sodium laurylsulfoacetate (sodium laurylsulfoacetate), higher fatty acid esters of 1,2 dihydroxypropane sulfonate, sulfolaurate (N-2-ethyl potassium sulfoacetamide laurate) and sodium lauryl sarcosinate.
By "higher alkyl" is meant, for example, C 6-30 An alkyl group. In certain embodiments, anionic surfactants useful herein include the water-soluble salts of alkyl sulfates having from 10 to 18 carbon atoms in the alkyl radical and the water-soluble salts of sulfonated monoglycerides of fatty acids having from 10 to 18 carbon atoms. Sodium lauroyl sarcosinate and sodium cocomonoglyceride sulfonate are examples of this type of anionic surfactant. The anionic surfactant may be present in an effective amount (e.g., by weight of the formulation>0.01%) but not at concentrations that would stimulate oral tissue (e.g.,<10%) and the optimal concentration depends on the particular formulation and the particular surfactant. In one embodiment, the anionic surfactant is 0.3% to 4.5% by weightFor example about 1.5% is present in toothpaste. The compositions of the present disclosure may optionally comprise a mixture of surfactants, for example, comprising an anionic surfactant and other surfactants that may be anionic, cationic, zwitterionic, or nonionic. In general, suitable surfactants are those that are relatively stable throughout a wide pH range. Surfactants are more fully described, for example, in U.S. Pat. No. 3,959,458 to Agricola et al, U.S. Pat. No. 3,937,807 to Haefele, and U.S. Pat. No. 4,051,234 to Gieske et al, the disclosures of which are incorporated herein by reference in their entirety.
Surfactants or mixtures of compatible surfactants that are included in addition to the anionic surfactant may be present in the compositions of the present disclosure at 0.1% to 5.0%, in another embodiment 0.3% to 3.0%, and in another embodiment 0.5% to 2.0% by weight of the total composition. These ranges do not include the amount of anionic surfactant.
In some embodiments, the oral care compositions of the present disclosure (e.g., oral care compositions of any of composition 1.0 and the following, etc.) can comprise a zwitterionic surfactant, such as a betaine surfactant, such as cocamidopropyl betaine, e.g., in an amount of 0.1% to 4.5% by weight (e.g., about 0.45% by weight), such as 0.5% to 2% by weight (e.g., about 0.6% by weight).
Tartar control agent: in various embodiments of the present disclosure, the oral care compositions of the present disclosure (e.g., oral care composition of any of composition 1.0 and the following, etc.) can comprise an anticalculus agent. Suitable anticalculus agents include, without limitation, phosphates and polyphosphates (e.g., pyrophosphates and triphosphates), polyaminopropane sulfonic Acid (AMPS), hexametaphosphate, zinc citrate trihydrate, polypeptides, polyolefin sulfonates, polyolefin phosphates, and bisphosphonates. Thus, the compositions of the present disclosure may comprise phosphates other than zinc phosphate. In particular embodiments, these The salt is an alkali metal phosphate, for example a salt of an alkali metal hydroxide or an alkaline earth metal hydroxide, for example a sodium, potassium or calcium salt. "phosphate" as used herein encompasses orally acceptable mono-and polyphosphates, such as P 1-6 Phosphates, such as monomeric phosphates, e.g., dihydrogen phosphate, hydrogen phosphate, or ternary phosphates; and dimeric phosphates such as pyrophosphates; and polyphosphates such as tripolyphosphate, tetraphosphate, hexaphosphate, and hexametaphosphate (e.g., sodium hexametaphosphate). In particular examples, the selected phosphate salt is selected from alkali metal hydrogen phosphate and alkali metal pyrophosphate salts, for example selected from disodium hydrogen phosphate, dipotassium hydrogen phosphate, dicalcium phosphate dihydrate, calcium pyrophosphate, tetrasodium pyrophosphate, tetrapotassium pyrophosphate, sodium tripolyphosphate, and mixtures of any two or more of these. In a particular embodiment, for example, the composition may comprise tetrasodium pyrophosphate in an amount of from 0.5% to 5% by weight, for example from 1% to 3%, or from 1% to 4%, or from 2% to 4%, or from 1% to 2%, or about 4% by weight of the composition. In another embodiment, the composition may comprise a mixture of tetra sodium pyrophosphate (TSPP) and Sodium Tripolyphosphate (STPP), for example, with a proportion of TSPP of 0.5 to 5 wt%, such as 1 to 2 wt% or 1 to 4 wt%, and a proportion of STPP of 0.5 to 6 wt%, such as 1 to 4% or 2 to 3%, by weight of the composition. Such phosphate salts are provided in an amount effective to reduce erosion of enamel, aid cleaning teeth, and/or reduce build-up of tartar on teeth, for example in an amount of 0.2 to 20 wt%, such as 1 to 15 wt%, by weight of the composition.
Flavoring agent: in certain aspects, the oral care compositions of the present disclosure (e.g., oral care composition of any of composition 1.0 and the following, etc.) can comprise a flavoring agent. Flavoring agents used in the practice of the present disclosure include, but are not limited to, essential oils and various flavoring aldehydes, esters, alcohols, and the like. Examples of essential oils include spearmint, peppermint, wintergreen, sassafras, and combinations thereof flos Caryophylli, herba Salvia officinalis, eucalyptus, marjoram, cortex Cinnamomi, fructus Citri Limoniae,Lime (lime), grapefruit, and orange oil. Chemicals such as menthol, carvone, and anethole may also be used. Certain embodiments employ oils of peppermint and spearmint. The flavoring agent may be incorporated into the oral composition at a concentration of 0.1% to 5% by weight, for example 0.5% to 1.5% by weight.
Polymer: in certain aspects, the oral care compositions of the present disclosure (e.g., oral care composition of any of composition 1.0 and the following, etc.) can comprise additional polymers to adjust the viscosity of the formulation or enhance the solubility of other ingredients. Such additional polymers include polyethylene glycol, polysaccharides (e.g., cellulose derivatives such as carboxymethyl cellulose, hydroxymethyl cellulose, ethyl cellulose, microcrystalline cellulose, or polysaccharide gums such as xanthan gum, guar gum, or carrageenan). The acidic polymer (e.g., polyacrylate gel) may be provided in the form of its free acid or partially or fully neutralized water soluble alkali metal (e.g., potassium and sodium) or ammonium salts. In one embodiment, the oral care composition may comprise PVP. PVP generally refers to polymers that contain vinyl pyrrolidone (also known as N-vinyl pyrrolidone, N-vinyl-2-pyrrolidone, and N-vinyl-2-pyrrolidone) as monomer units. The monomer unit consists of one polar imide group, four nonpolar methylene groups and one nonpolar methane group.
In some embodiments, the compositions of the present disclosure (e.g., composition 1.0 and any of the following, etc.) may comprise one or more polyethylene glycols, such as polyethylene glycols having a molecular weight in the range of 200 to 800. For example, the composition may comprise one or more of polyethylene glycol 200, polyethylene glycol 300, polyethylene glycol 400, polyethylene glycol 600, or polyethylene glycol 800.
Silica thickeners may be present that form polymeric structures or gels in aqueous media. Note that these silica thickeners are physically and functionally different from the particulate silica abrasives also present in the composition, in that the silica thickener is very finely divided and provides little or no abrasive action. Other thickeners are carboxyvinyl polymers, carrageenans, hydroxyethyl cellulose and water soluble salts of cellulose ethers (e.g., sodium carboxymethyl cellulose and sodium carboxymethyl hydroxyethyl cellulose). Natural gums such as karaya, gum arabic and gum tragacanth can also be incorporated. Colloidal magnesium aluminum silicate may also be used as a component of the thickening composition to further improve the texture of the composition. In certain embodiments, the thickener is used in an amount of 0.5% to 5.0% by weight of the total composition.
In some embodiments, the oral care compositions of the present disclosure (e.g., oral care compositions of any of compositions 1.0 and following, etc.) can comprise anionic polymer, for example, in an amount of 0.05% to 5%. Examples of such agents commonly known for use in dentifrices are disclosed in U.S. Pat. nos. 5,188,821 and 5,192,531, both of which are incorporated herein by reference in their entirety; and includes synthetic anionic polymer polycarbonates such as maleic anhydride or a 1:4 to 4:1 copolymer of maleic acid with another polymerizable ethylenically unsaturated monomer, preferably methyl vinyl ether/maleic anhydride having a molecular weight (m.w.) of 30,000 to 1,000,000, for example 300,000 to 800,000. These copolymers are available, for example, as Gantrez, for example, AN 139 (M.W.500,000), AN 119 (M.W.250,000) and preferably S-97 pharmaceutical grades (M.W.700,000) available from ISP Technologies, inc., bound Brook, N.J.08805. The enhancer, when present, is present in an amount ranging from 0.05% to 3% by weight. Other useful polymers include 1:1 copolymers such as maleic anhydride with ethyl acrylate, hydroxyethyl methacrylate, N-vinyl-2-pyrrolidone, or ethylene, the latter available, for example, as Monsanto EMA number 1103, M.W.10,000, and EMA grade 61; and those of 1:1 copolymers of acrylic acid with methyl methacrylate or hydroxyethyl methacrylate, methyl acrylate or ethyl acrylate, isobutyl vinyl ether or N-vinyl-2-pyrrolidone. In general, suitable are polymeric ethylenically or ethylenically unsaturated carboxylic acids containing an activated carbon-to-carbene double bond and at least one carboxyl group, i.e. acids containing an olefinic double bond that is readily available for functioning in the polymerization because it is in the alpha-beta position relative to the carboxyl group or is present as part of the terminal methylene group in the monomer molecule. Examples of such acids are acrylic acid, methacrylic acid, ethacrylic acid, α -chloroacrylic acid, crotonic acid, β -acryloxypropionic acid, sorbic acid, α -chlorosorbic acid, cinnamic acid, β -styrylacrylic acid, muconic acid, itaconic acid, citraconic acid, mesaconic acid, glutaconic acid, aconitic acid, α -phenylacrylic acid, 2-benzylacrylic acid, 2-cyclohexylacrylic acid, angelic acid, umbellic acid, fumaric acid, maleic acid and anhydrides. Other different olefinic monomers copolymerizable with such carboxylic acid monomers include vinyl acetate, vinyl chloride, dimethyl maleate, and the like. The copolymer contains carboxylate groups sufficient for water solubility. Another class of polymerization agents includes compositions comprising homopolymers of substituted acrylamides and/or homopolymers of unsaturated sulfonic acids and salts thereof, particularly wherein the polymer is based on an unsaturated sulfonic acid selected from acrylamidoalkanesulfonic acids, such as 2-acrylamido 2-methylpropanesulfonic acid, having a molecular weight of 1,000 to 2,000,000. Another useful class of polymerization agents includes polyamino acids containing proportional anionic surface active amino acids (e.g., aspartic acid, glutamic acid, and phosphoserine), for example, as disclosed in U.S. Pat. No. 4,866,161 to Sikes et al, which is also incorporated herein by reference in its entirety.
In some embodiments, the anionic polymer is not present in the composition. In other embodiments, anionic polymers may be present, but they do not include copolymers of methyl vinyl ether and maleic acid or anhydride.
Humectant type: within certain embodiments of the present disclosure (e.g., composition 1.0 and any of the following, etc.), the composition comprises one or more humectants. Certain humectants can also impart a desired sweetness or flavor to dentifrice compositions. Suitable humectants include edible polyhydric alcohols such as glycerin, sorbitol, xylitol, propylene glycol, and other polyols, as well as mixtures of these humectants. In one embodiment of the present disclosure, the primary humectant is one of glycerin, sorbitol, or a combination thereof. The humectant may be present in an amount of greater than 15 wt%, such as 15 wt% to 55 wt%, or 20 wt% to 50 wt%,or from 20 wt% to 40 wt%, or about 20 wt%, or about 30 wt%, or about 40 wt% of the total weight of the composition.
Other optional ingredients: in addition to the above-described components, in certain aspects, the oral care compositions of the present disclosure (e.g., oral care composition of any of composition 1.0 and the following, etc.) can comprise a variety of optional oral care ingredients, some of which are described below. Optional ingredients include, but are not limited to, for example, binders, foaming agents, flavoring agents, sweeteners (e.g., sodium saccharin), additional antiplaque agents, abrasives, aesthetic materials (e.g., tiO) 2 Coated mica) or other colorants (e.g., dyes and/or pigments).
In some embodiments, the compositions of the present disclosure (e.g., any of composition 1.0 and the following, etc.) can have any pH suitable for use in products for oral care. Examples of suitable pH ranges are 6 to 9, e.g. 6.5 to 8, or 6.5 to 7.5, or about 7.0.
In some embodiments, the oral care compositions of the present disclosure (e.g., oral care composition of any of composition 1.0 and the following, etc.) are substantially free, or do not comprise any sodium hexametaphosphate. In some embodiments, the oral care compositions of the present disclosure are substantially free, or do not comprise any halogenated diphenyl ether (e.g., triclosan).
In at least one aspect, the compositions of the present disclosure (e.g., composition 1.0 and any of the following, etc.) are substantially free, or do not comprise any sodium lauryl sulfate.
By "substantially free" is meant that the composition has no more than 0.01% by weight of these compounds.
In some embodiments, the compositions of the present disclosure (e.g., composition 1.0 and any of the following, etc.) are substantially free, or free of any complexing agent for increasing the solubility of zinc phosphate. Examples of known complexing agents that may be excluded from the compositions of the present disclosure include chelating agents taught in U.S. patent application No. 2007/0025928, the disclosure of which is incorporated herein by reference in its entirety. Such chelating agents include mineral surfactants, including such mineral surfactants: which is a polymer and/or polyelectrolyte and is selected from phosphorylated polymers, wherein if the phosphorylated polymer is a polyphosphate, the average chain length of the polyphosphate is 3.5 or greater, e.g., 4 or greater; polyphosphonates; a polycarboxylic acid ester; a carboxyl-substituted polymer; a copolymer of: a phosphate or phosphonate containing monomer or polymer with an ethylenically unsaturated monomer, amino acid, protein, polypeptide, polysaccharide, poly (acrylate), poly (acrylamide), poly (methacrylate), poly (ethyl acrylate), poly (hydroxyalkyl methacrylate), poly (vinyl alcohol), poly (maleic anhydride), poly (maleate), poly (amide), poly (vinylamine), poly (ethylene glycol), poly (propylene glycol), poly (vinyl acetate), and poly (vinylbenzyl chloride); and mixtures thereof. Other known complexing agents that may be excluded from the compositions of the present disclosure include those taught in CA2634758 (the disclosure of which is incorporated herein by reference in its entirety). Examples include polyphosphorylated inositol compounds such as phytic acid, inositol pentakis (dihydrogen phosphate); an alkali metal, alkaline earth metal or ammonium salt of any of inositol tetrakis (dihydrogen phosphate), inositol tris (dihydrogen phosphate) or any of the above inositol compounds. Phytic acid is also known as inositol 1,2,3,4,5, 6-hexa (dihydrogen phosphate) or phytic acid.
In another aspect, the present disclosure provides a method of treating or preventing aggressive tooth demineralization, gingivitis, plaque, and/or caries comprising applying a composition according to the present invention (e.g., composition 1.0 and the following, etc.) to the oral cavity of a person in need thereof, such as by brushing, e.g., one or more times per day.
In another aspect, the present disclosure provides methods of using the compositions described herein (e.g., composition 1.0 and any of the following, etc.) to increase zinc levels in dental enamel and treat, reduce, or control the occurrence of dental enamel erosion. The method comprises applying any of the compositions as described herein to the teeth, for example by brushing or otherwise applying the composition to the oral cavity of a subject in need thereof. The composition may be administered periodically, for example, once or more times per day. In various embodiments, administration of the compositions of the present disclosure to a patient may provide one or more of the following benefits: (i) reducing hypersensitivity of the tooth, (ii) reducing plaque accumulation, (iii) reducing or inhibiting demineralization and promoting remineralization of the tooth, (iv) inhibiting microbial biofilm formation in the oral cavity, (v) reducing or inhibiting gingivitis, (vi) promoting healing of ulcers or wounds in the mouth, (vii) reducing the level of acidogenic bacteria, (viii) increasing the relative level of non-caries and/or non-plaque forming bacteria, (ix) reducing or inhibiting caries formation, (x) reducing, repairing or inhibiting pre-caries lesions of the enamel, e.g., as detected by quantitative light-induced fluorescence (QLF) or Electrical Caries Measurement (ECM), (xi) treating, alleviating or reducing dry mouth, (xii) cleaning the teeth and oral cavity, (xiii) reducing erosion, (xiv) whitening the teeth; (xv) Reducing dental calculus build-up, and/or (xvi) promoting general health, including cardiovascular health, for example, by reducing the likelihood of systemic infection occurring via oral tissue. The present disclosure also provides compositions for use in any of the above methods. Further embodiments provide methods wherein at least one tooth is remineralized after administration of a composition as described herein.
Also disclosed are methods of making any of the compositions of the present disclosure (e.g., composition 1.0 and any of the following, etc.). The method comprises combining zinc phosphate, sodium fluoride, and a taurate surfactant in water to form an aqueous zinc phosphate mixture. In some embodiments, zinc phosphate is added to the dentifrice composition as a preformed salt and remains substantially insoluble in the aqueous mixture. The amount of water employed in the mixture may be any of the amounts recited herein for the compositions of the present disclosure. Any standard mixing technique may be employed to combine the ingredients and form a stable composition. In one aspect, the method comprises combining zinc phosphate and sorbitol, wherein the combination of zinc phosphate and sorbitol produces a dispersion. Subsequently, a dispersion of zinc phosphate and stannous fluoride is added to the aqueous solution (aqueous mixture). Finally, sodium methyl cocoyl taurate (the final ingredient) is added to the aqueous mixture comprising zinc phosphate and stannous fluoride.
Examples
EXAMPLE 1 dentifrice formulation
Representative dentifrice formulations according to the present disclosure were prepared according to table 1 below:
TABLE 1
Composition of the components | Weight% (by weight) |
Water and its preparation method | Moderate (e.g., 15% to 40%) |
Humectant type | 15 to 55 (e.g., 30% to 40%) |
Polymer | 1% to 5% (e.g., 3.8%) |
Abrasive material | 10% to 30% (e.g., 20%) |
Thickening agent | 05% to 5% (e.g., 1.5%) |
Zinc phosphate | 005% to 5% (e.g., 1%) |
Flavoring agent, sweetener, and pigment | 05% to 5% (e.g., 1.7%) |
Alkali metal phosphates | 0.5% to 5% (e.g., 2%) |
Sodium methyl cocoyl taurate | 0.01% to 10% (e.g., 2%) |
Zwitterionic surfactants | 0.1% to 4.5% (e.g., 1.5%) |
Sodium fluoride | 0.5 to 11% (e.g., 0.32%) |
Total composition | 100% |
Example 2 stability, taste and formulation production
The stability and taste of the compositions detailed in table 2 below over a span of six weeks to six months were studied:
TABLE 2
During the aging test at 40C, formulation a was stable at 6 months. Formulation a was also stable and met acceptable microbiological criteria in the taste-related test comprising 6 weeks.
Table 3: aging stability study of formulation A
Formulation B, with 10% less water, was also stable at 3 months during the aging test at 40 ℃. In addition, formulation B was stable in recyclable pipes and aluminum laminated pipes.
Table 4: aging stability study of formulation B
Additionally, the surfactant system of formulation B comprising sodium methyl cocoyl taurate had no effect on the cleaning step. Sample studies showed that both a toothpaste containing SLS and a toothpaste containing taurine salt (formula B) could be cleaned in the same way.
Thus, formulations a and B, each containing taurine salts, were shown to be physically stable and not isolated. Formulations a and B are also acceptable from a taste perspective and provide acceptable fluoride and zinc stability.
EXAMPLE 3 dentifrice formulation
Representative dentifrice formulations according to the present disclosure were prepared according to table 5 below:
table 5:
while the present disclosure has been described with respect to specific examples including presently preferred modes of carrying out the disclosure, those skilled in the art will appreciate that there are numerous variations and permutations of the above described systems and techniques. It is to be understood that other embodiments may be utilized and structural and functional modifications may be made without departing from the scope of the present disclosure.
Claims (22)
1. An oral care composition comprising:
a. ) An orally acceptable carrier, which is a solid carrier,
b. ) A zinc phosphate salt of zinc and a zinc phosphate salt of zinc,
c. ) A fluoride ion source; and
d. ) A taurine salt surfactant represented by the formula (1):
wherein R is 1 Is a saturated or unsaturated, linear or branched alkyl chain having 6 to 18C atoms, R 2 Is H or methyl, and M + H, sodium or potassium.
2. The oral care composition of claim 1, wherein the taurate surfactant comprises one or more surfactants selected from the group consisting of: potassium cocoyl taurate, potassium methyl cocoyl taurate, sodium caproyl methyl taurate, sodium cocoyl taurate, sodium lauroyl taurate, sodium methyl cocoyl taurate, sodium methyl lauroyl taurate, sodium methyl myristoyl taurate, sodium methyl oleoyl taurate, sodium methyl palmitoyl taurate, sodium methyl stearoyl taurate, and combinations thereof.
3. The oral care composition of claim 1 or 2, wherein the taurate surfactant comprises sodium methyl cocoyl taurate.
4. The oral care composition of any preceding claim, wherein the taurine salt surfactant is present in an amount of from 0.4% to 3%.
5. The oral care composition of any preceding claim, wherein the amount of zinc phosphate is from 0.05% to 10% by weight relative to the weight of the oral care composition.
6. The oral care composition of any preceding claim, wherein the fluoride ion source is in an amount of 0.01% to 5% by weight.
7. The oral care composition of any preceding claim, wherein the fluoride source is selected from the group consisting of: sodium fluoride, potassium fluoride, calcium fluoride, zinc ammonium fluoride, lithium fluoride, ammonium fluoride, stannous fluorozirconate, sodium monofluorophosphate, potassium monofluorophosphate, laurylamine hydrofluoric acid, diethylaminoethyloctylamide hydrofluoric acid, didecyldimethyl ammonium fluoride, cetylpyridine fluorideFluorinated dilaurylmeline->Stannous sarcosinate fluoride, potassium glycinate fluoride, glycine hydrofluoric acid salts, amine fluorides, and combinations thereof.
8. The oral care composition of any preceding claim, wherein the fluoride ion source comprises sodium fluoride.
9. The oral care composition of any preceding claim, wherein the fluoride ion source comprises sodium fluoride and stannous fluoride.
10. The oral care composition of any preceding claim, wherein the composition comprises water in an amount of 10% by weight or greater relative to the weight of the oral care composition.
11. The oral care composition of any preceding claim, wherein the oral care composition further comprises an abrasive, e.g., a silica abrasive, a calcium abrasive, and other abrasives as disclosed herein.
12. The oral care composition of any preceding claim, further comprising one or more humectants selected from the group consisting of: sorbitol, glycerin, xylitol and propylene glycol, and combinations thereof.
13. The oral care composition of any preceding claim, further comprising a zwitterionic surfactant.
14. The oral care composition of claim 13, wherein the zwitterionic surfactant comprises cocamidopropyl betaine.
15. The oral care composition of any preceding claim, further comprising an effective amount of one or more alkali metal phosphates.
16. The oral care composition of any preceding claim, wherein the oral care composition is selected from the group consisting of: dentifrices, powders, creams, mouthwashes, mousses, strips or chewing gums.
17. The oral care composition of any preceding claim, wherein the composition is a single phase composition (e.g., not a dual phase composition).
18. The oral care composition of any preceding claim, wherein the composition comprises:
zinc phosphate;
sodium fluoride;
0.5% to 3% sodium methyl cocoyl taurate;
water in an amount of 10% to 40% by weight of the total composition; and
an orally acceptable carrier.
19. The oral care composition of any one of claims 1 to 17, wherein the composition comprises:
0.5 to 4% by weight of zinc phosphate;
0.2 to 2% by weight of stannous fluoride;
0.05 to 2% by weight of sodium fluoride;
sodium methyl cocoyl taurate; and
water in an amount of 10% to 50% by weight of the total composition.
20. The oral care composition of any preceding claim, wherein the oral care composition is free or substantially free of sodium lauryl sulfate.
21. A method of treating or preventing aggressive tooth demineralization, gingivitis, plaque and/or caries, the method comprising applying to the oral cavity of a person in need thereof a composition according to any of the preceding claims.
22. Use of a composition according to any one of claims 1 to 18 for: (i) reducing or inhibiting caries formation, (ii) reducing, repairing or inhibiting pre-caries lesions of enamel, (iii) reducing or inhibiting demineralization and promoting remineralization of teeth, (iv) reducing hypersensitivity of teeth, (v) reducing or inhibiting gingivitis, (vi) promoting healing of ulcers or wounds in the mouth, (vii) reducing levels of acidogenic bacteria, (viii) increasing relative levels of arginine-decomposing bacteria, (ix) inhibiting microbial biofilm formation in the oral cavity, (x) increasing and/or maintaining plaque pH at a level of at least pH 5.5 after a sugar challenge, (xi) reducing plaque accumulation, (xii) treating, alleviating or reducing dry mouth, (xiii) cleaning teeth and oral cavity, (xiv) reducing erosion, (xv) preventing dental stains and/or whitening teeth, (xvi) immunizing teeth against cariogenic bacteria; and/or (xvii) promote general health, including cardiovascular health.
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