TWI476007B - Oral compositions and uses thereof - Google Patents
Oral compositions and uses thereof Download PDFInfo
- Publication number
- TWI476007B TWI476007B TW098117365A TW98117365A TWI476007B TW I476007 B TWI476007 B TW I476007B TW 098117365 A TW098117365 A TW 098117365A TW 98117365 A TW98117365 A TW 98117365A TW I476007 B TWI476007 B TW I476007B
- Authority
- TW
- Taiwan
- Prior art keywords
- composition
- oral
- cerium oxide
- tooth
- rda
- Prior art date
Links
- 239000000203 mixture Substances 0.000 title claims description 254
- 229910000420 cerium oxide Inorganic materials 0.000 claims description 70
- BMMGVYCKOGBVEV-UHFFFAOYSA-N oxo(oxoceriooxy)cerium Chemical compound [Ce]=O.O=[Ce]=O BMMGVYCKOGBVEV-UHFFFAOYSA-N 0.000 claims description 65
- -1 cerium oxide compound Chemical class 0.000 claims description 40
- 239000002245 particle Substances 0.000 claims description 40
- 238000000034 method Methods 0.000 claims description 29
- 239000002002 slurry Substances 0.000 claims description 28
- 210000000214 mouth Anatomy 0.000 claims description 26
- 239000003795 chemical substances by application Substances 0.000 claims description 18
- 239000003906 humectant Substances 0.000 claims description 16
- 239000004094 surface-active agent Substances 0.000 claims description 16
- 229910000422 cerium(IV) oxide Inorganic materials 0.000 claims description 13
- 229920001577 copolymer Polymers 0.000 claims description 13
- 238000010521 absorption reaction Methods 0.000 claims description 12
- CETPSERCERDGAM-UHFFFAOYSA-N ceric oxide Chemical compound O=[Ce]=O CETPSERCERDGAM-UHFFFAOYSA-N 0.000 claims description 12
- 239000003921 oil Substances 0.000 claims description 11
- 229920000642 polymer Polymers 0.000 claims description 11
- 230000002829 reductive effect Effects 0.000 claims description 11
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 10
- 230000002285 radioactive effect Effects 0.000 claims description 10
- KRHYYFGTRYWZRS-UHFFFAOYSA-M Fluoride anion Chemical compound [F-] KRHYYFGTRYWZRS-UHFFFAOYSA-M 0.000 claims description 8
- 150000001875 compounds Chemical class 0.000 claims description 8
- PUZPDOWCWNUUKD-UHFFFAOYSA-M sodium fluoride Chemical compound [F-].[Na+] PUZPDOWCWNUUKD-UHFFFAOYSA-M 0.000 claims description 8
- 239000000606 toothpaste Substances 0.000 claims description 8
- 229940034610 toothpaste Drugs 0.000 claims description 8
- 229910001369 Brass Inorganic materials 0.000 claims description 7
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims description 7
- 208000004188 Tooth Wear Diseases 0.000 claims description 7
- 239000010951 brass Substances 0.000 claims description 7
- 235000019333 sodium laurylsulphate Nutrition 0.000 claims description 7
- 230000002087 whitening effect Effects 0.000 claims description 7
- 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 6
- 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 6
- 239000003242 anti bacterial agent Substances 0.000 claims description 6
- NROKBHXJSPEDAR-UHFFFAOYSA-M potassium fluoride Chemical compound [F-].[K+] NROKBHXJSPEDAR-UHFFFAOYSA-M 0.000 claims description 6
- 239000000600 sorbitol Substances 0.000 claims description 6
- 235000010356 sorbitol Nutrition 0.000 claims description 6
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N Phenol Chemical compound OC1=CC=CC=C1 ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 claims description 5
- USIUVYZYUHIAEV-UHFFFAOYSA-N diphenyl ether Chemical class C=1C=CC=CC=1OC1=CC=CC=C1 USIUVYZYUHIAEV-UHFFFAOYSA-N 0.000 claims description 5
- 150000004673 fluoride salts Chemical class 0.000 claims description 5
- 150000004676 glycans Chemical class 0.000 claims description 5
- 235000011187 glycerol Nutrition 0.000 claims description 5
- 229920001223 polyethylene glycol Polymers 0.000 claims description 5
- 229920001282 polysaccharide Polymers 0.000 claims description 5
- 239000005017 polysaccharide Substances 0.000 claims description 5
- 239000003755 preservative agent Substances 0.000 claims description 5
- XGRSAFKZAGGXJV-UHFFFAOYSA-N 3-azaniumyl-3-cyclohexylpropanoate Chemical compound OC(=O)CC(N)C1CCCCC1 XGRSAFKZAGGXJV-UHFFFAOYSA-N 0.000 claims description 4
- 239000002202 Polyethylene glycol Substances 0.000 claims description 4
- MRUAUOIMASANKQ-UHFFFAOYSA-O carboxymethyl-[3-(dodecanoylamino)propyl]-dimethylazanium Chemical compound CCCCCCCCCCCC(=O)NCCC[N+](C)(C)CC(O)=O MRUAUOIMASANKQ-UHFFFAOYSA-O 0.000 claims description 4
- 239000011775 sodium fluoride Substances 0.000 claims description 4
- 235000013024 sodium fluoride Nutrition 0.000 claims description 4
- 229960000414 sodium fluoride Drugs 0.000 claims description 4
- 229960004711 sodium monofluorophosphate Drugs 0.000 claims description 4
- 239000000341 volatile oil Substances 0.000 claims description 4
- ZVVSSOQAYNYNPP-UHFFFAOYSA-N olaflur Chemical compound F.F.CCCCCCCCCCCCCCCCCCN(CCO)CCCN(CCO)CCO ZVVSSOQAYNYNPP-UHFFFAOYSA-N 0.000 claims description 3
- 229960001245 olaflur Drugs 0.000 claims description 3
- 239000011698 potassium fluoride Substances 0.000 claims description 3
- 235000003270 potassium fluoride Nutrition 0.000 claims description 3
- DTOUUUZOYKYHEP-UHFFFAOYSA-N 1,3-bis(2-ethylhexyl)-5-methyl-1,3-diazinan-5-amine Chemical compound CCCCC(CC)CN1CN(CC(CC)CCCC)CC(C)(N)C1 DTOUUUZOYKYHEP-UHFFFAOYSA-N 0.000 claims description 2
- CPKVUHPKYQGHMW-UHFFFAOYSA-N 1-ethenylpyrrolidin-2-one;molecular iodine Chemical compound II.C=CN1CCCC1=O CPKVUHPKYQGHMW-UHFFFAOYSA-N 0.000 claims description 2
- UOWIFEANNONTKY-UHFFFAOYSA-N 2-hydroxy-5-octanoyl-n-[3-(trifluoromethyl)phenyl]benzamide Chemical compound CCCCCCCC(=O)C1=CC=C(O)C(C(=O)NC=2C=C(C=CC=2)C(F)(F)F)=C1 UOWIFEANNONTKY-UHFFFAOYSA-N 0.000 claims description 2
- XNCOSPRUTUOJCJ-UHFFFAOYSA-N Biguanide Chemical compound NC(N)=NC(N)=N XNCOSPRUTUOJCJ-UHFFFAOYSA-N 0.000 claims description 2
- 229940123208 Biguanide Drugs 0.000 claims description 2
- 229920000153 Povidone-iodine Polymers 0.000 claims description 2
- 239000012676 herbal extract Substances 0.000 claims description 2
- 229960004867 hexetidine Drugs 0.000 claims description 2
- 229910021645 metal ion Inorganic materials 0.000 claims description 2
- 229960001621 povidone-iodine Drugs 0.000 claims description 2
- 230000002335 preservative effect Effects 0.000 claims description 2
- 150000003856 quaternary ammonium compounds Chemical class 0.000 claims description 2
- 229940090898 Desensitizer Drugs 0.000 claims 1
- 239000004698 Polyethylene Substances 0.000 claims 1
- 235000016551 Potentilla erecta Nutrition 0.000 claims 1
- ATJFFYVFTNAWJD-UHFFFAOYSA-N Tin Chemical compound [Sn] ATJFFYVFTNAWJD-UHFFFAOYSA-N 0.000 claims 1
- 241000372442 Wachendorfia thyrsiflora Species 0.000 claims 1
- LPLMZAJYUPAYQZ-UHFFFAOYSA-N diazanium;difluoride Chemical compound [NH4+].[NH4+].[F-].[F-] LPLMZAJYUPAYQZ-UHFFFAOYSA-N 0.000 claims 1
- 238000003682 fluorination reaction Methods 0.000 claims 1
- 230000001706 oxygenating effect Effects 0.000 claims 1
- 229920000573 polyethylene Polymers 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 20
- 239000010408 film Substances 0.000 description 17
- 239000000551 dentifrice Substances 0.000 description 16
- 230000002272 anti-calculus Effects 0.000 description 13
- 239000000463 material Substances 0.000 description 12
- 239000003082 abrasive agent Substances 0.000 description 11
- 210000004268 dentin Anatomy 0.000 description 11
- 150000003839 salts Chemical class 0.000 description 11
- 102000004190 Enzymes Human genes 0.000 description 10
- 108090000790 Enzymes Proteins 0.000 description 10
- 229940088598 enzyme Drugs 0.000 description 10
- 235000019198 oils Nutrition 0.000 description 10
- 239000002253 acid Substances 0.000 description 8
- 230000001680 brushing effect Effects 0.000 description 8
- 210000003298 dental enamel Anatomy 0.000 description 8
- 235000011180 diphosphates Nutrition 0.000 description 8
- 229910052708 sodium Inorganic materials 0.000 description 8
- 239000011734 sodium Substances 0.000 description 8
- 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 description 7
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 7
- 229920000388 Polyphosphate Polymers 0.000 description 7
- 201000002170 dentin sensitivity Diseases 0.000 description 7
- XPPKVPWEQAFLFU-UHFFFAOYSA-J diphosphate(4-) Chemical compound [O-]P([O-])(=O)OP([O-])([O-])=O XPPKVPWEQAFLFU-UHFFFAOYSA-J 0.000 description 7
- 238000005498 polishing Methods 0.000 description 7
- 239000001205 polyphosphate Substances 0.000 description 7
- 235000011176 polyphosphates Nutrition 0.000 description 7
- 239000002562 thickening agent Substances 0.000 description 7
- 230000036347 tooth sensitivity Effects 0.000 description 7
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 6
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 6
- XEFQLINVKFYRCS-UHFFFAOYSA-N Triclosan Chemical compound OC1=CC(Cl)=CC=C1OC1=CC=C(Cl)C=C1Cl XEFQLINVKFYRCS-UHFFFAOYSA-N 0.000 description 6
- 239000013543 active substance Substances 0.000 description 6
- 229910052783 alkali metal Inorganic materials 0.000 description 6
- 125000000129 anionic group Chemical group 0.000 description 6
- 239000003945 anionic surfactant Substances 0.000 description 6
- 230000006378 damage Effects 0.000 description 6
- FPYJFEHAWHCUMM-UHFFFAOYSA-N maleic anhydride Chemical compound O=C1OC(=O)C=C1 FPYJFEHAWHCUMM-UHFFFAOYSA-N 0.000 description 6
- 239000011591 potassium Substances 0.000 description 6
- 229910052700 potassium Inorganic materials 0.000 description 6
- 229960003975 potassium Drugs 0.000 description 6
- MHAJPDPJQMAIIY-UHFFFAOYSA-N Hydrogen peroxide Chemical compound OO MHAJPDPJQMAIIY-UHFFFAOYSA-N 0.000 description 5
- 239000001768 carboxy methyl cellulose Substances 0.000 description 5
- 239000003093 cationic surfactant Substances 0.000 description 5
- 235000010980 cellulose Nutrition 0.000 description 5
- 239000001913 cellulose Substances 0.000 description 5
- 239000000796 flavoring agent Substances 0.000 description 5
- 239000006260 foam Substances 0.000 description 5
- 239000004615 ingredient Substances 0.000 description 5
- 238000005259 measurement Methods 0.000 description 5
- 229910052751 metal Inorganic materials 0.000 description 5
- 239000002184 metal Substances 0.000 description 5
- 239000000178 monomer Substances 0.000 description 5
- 229920005646 polycarboxylate Polymers 0.000 description 5
- 239000000843 powder Substances 0.000 description 5
- 239000004575 stone Substances 0.000 description 5
- 239000000126 substance Substances 0.000 description 5
- 229960003500 triclosan Drugs 0.000 description 5
- JWAZRIHNYRIHIV-UHFFFAOYSA-N 2-naphthol Chemical compound C1=CC=CC2=CC(O)=CC=C21 JWAZRIHNYRIHIV-UHFFFAOYSA-N 0.000 description 4
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 4
- 239000004480 active ingredient Substances 0.000 description 4
- 150000001340 alkali metals Chemical class 0.000 description 4
- 230000001580 bacterial effect Effects 0.000 description 4
- 230000008901 benefit Effects 0.000 description 4
- 230000015572 biosynthetic process Effects 0.000 description 4
- YKPUWZUDDOIDPM-SOFGYWHQSA-N capsaicin Chemical compound COC1=CC(CNC(=O)CCCC\C=C\C(C)C)=CC=C1O YKPUWZUDDOIDPM-SOFGYWHQSA-N 0.000 description 4
- 125000004432 carbon atom Chemical group C* 0.000 description 4
- 229920001525 carrageenan Polymers 0.000 description 4
- 235000010418 carrageenan Nutrition 0.000 description 4
- 239000000679 carrageenan Substances 0.000 description 4
- 229940113118 carrageenan Drugs 0.000 description 4
- 229920002678 cellulose Polymers 0.000 description 4
- 239000003086 colorant Substances 0.000 description 4
- DOIRQSBPFJWKBE-UHFFFAOYSA-N dibutyl phthalate Chemical compound CCCCOC(=O)C1=CC=CC=C1C(=O)OCCCC DOIRQSBPFJWKBE-UHFFFAOYSA-N 0.000 description 4
- 238000009826 distribution Methods 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- RRAFCDWBNXTKKO-UHFFFAOYSA-N eugenol Chemical compound COC1=CC(CC=C)=CC=C1O RRAFCDWBNXTKKO-UHFFFAOYSA-N 0.000 description 4
- 229940091249 fluoride supplement Drugs 0.000 description 4
- 230000036541 health Effects 0.000 description 4
- 150000002978 peroxides Chemical class 0.000 description 4
- UHVMMEOXYDMDKI-JKYCWFKZSA-L zinc;1-(5-cyanopyridin-2-yl)-3-[(1s,2s)-2-(6-fluoro-2-hydroxy-3-propanoylphenyl)cyclopropyl]urea;diacetate Chemical compound [Zn+2].CC([O-])=O.CC([O-])=O.CCC(=O)C1=CC=C(F)C([C@H]2[C@H](C2)NC(=O)NC=2N=CC(=CC=2)C#N)=C1O UHVMMEOXYDMDKI-JKYCWFKZSA-L 0.000 description 4
- NOOLISFMXDJSKH-UTLUCORTSA-N (+)-Neomenthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@@H]1O NOOLISFMXDJSKH-UTLUCORTSA-N 0.000 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 description 3
- 241000894006 Bacteria Species 0.000 description 3
- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 description 3
- 229920002307 Dextran Polymers 0.000 description 3
- RWSOTUBLDIXVET-UHFFFAOYSA-N Dihydrogen sulfide Chemical class S RWSOTUBLDIXVET-UHFFFAOYSA-N 0.000 description 3
- 108010031186 Glycoside Hydrolases Proteins 0.000 description 3
- 102000005744 Glycoside Hydrolases Human genes 0.000 description 3
- DAOANAATJZWTSJ-UHFFFAOYSA-N N-Decanoylmorpholine Chemical compound CCCCCCCCCC(=O)N1CCOCC1 DAOANAATJZWTSJ-UHFFFAOYSA-N 0.000 description 3
- 229910019142 PO4 Inorganic materials 0.000 description 3
- 229920001213 Polysorbate 20 Polymers 0.000 description 3
- 239000004365 Protease Substances 0.000 description 3
- 229920002125 Sokalan® Polymers 0.000 description 3
- 230000003281 allosteric effect Effects 0.000 description 3
- 229910052782 aluminium Inorganic materials 0.000 description 3
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 3
- 230000000845 anti-microbial effect Effects 0.000 description 3
- 239000002585 base Substances 0.000 description 3
- FUFJGUQYACFECW-UHFFFAOYSA-L calcium hydrogenphosphate Chemical compound [Ca+2].OP([O-])([O-])=O FUFJGUQYACFECW-UHFFFAOYSA-L 0.000 description 3
- 229940043256 calcium pyrophosphate Drugs 0.000 description 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 3
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 3
- 239000008112 carboxymethyl-cellulose Substances 0.000 description 3
- 239000000969 carrier Substances 0.000 description 3
- YMKDRGPMQRFJGP-UHFFFAOYSA-M cetylpyridinium chloride Chemical compound [Cl-].CCCCCCCCCCCCCCCC[N+]1=CC=CC=C1 YMKDRGPMQRFJGP-UHFFFAOYSA-M 0.000 description 3
- 229960001927 cetylpyridinium chloride Drugs 0.000 description 3
- 239000002738 chelating agent Substances 0.000 description 3
- 230000007423 decrease Effects 0.000 description 3
- 235000013355 food flavoring agent Nutrition 0.000 description 3
- UPBDXRPQPOWRKR-UHFFFAOYSA-N furan-2,5-dione;methoxyethene Chemical compound COC=C.O=C1OC(=O)C=C1 UPBDXRPQPOWRKR-UHFFFAOYSA-N 0.000 description 3
- 208000007565 gingivitis Diseases 0.000 description 3
- 210000003128 head Anatomy 0.000 description 3
- 150000002500 ions Chemical class 0.000 description 3
- 235000021388 linseed oil Nutrition 0.000 description 3
- 239000000944 linseed oil Substances 0.000 description 3
- 229940041616 menthol Drugs 0.000 description 3
- OSWPMRLSEDHDFF-UHFFFAOYSA-N methyl salicylate Chemical compound COC(=O)C1=CC=CC=C1O OSWPMRLSEDHDFF-UHFFFAOYSA-N 0.000 description 3
- XJRBAMWJDBPFIM-UHFFFAOYSA-N methyl vinyl ether Chemical compound COC=C XJRBAMWJDBPFIM-UHFFFAOYSA-N 0.000 description 3
- 239000002736 nonionic surfactant Substances 0.000 description 3
- JRZJOMJEPLMPRA-UHFFFAOYSA-N olefin Natural products CCCCCCCC=C JRZJOMJEPLMPRA-UHFFFAOYSA-N 0.000 description 3
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 3
- 235000021317 phosphate Nutrition 0.000 description 3
- 229920002432 poly(vinyl methyl ether) polymer Polymers 0.000 description 3
- 159000000001 potassium salts Chemical class 0.000 description 3
- 238000002360 preparation method Methods 0.000 description 3
- 230000008569 process Effects 0.000 description 3
- 239000000047 product Substances 0.000 description 3
- 210000004872 soft tissue Anatomy 0.000 description 3
- 210000005239 tubule Anatomy 0.000 description 3
- 150000003751 zinc Chemical class 0.000 description 3
- 229920002818 (Hydroxyethyl)methacrylate Polymers 0.000 description 2
- AHQNFRFBKOXXBK-ODZAUARKSA-N (z)-but-2-enedioic acid;methoxymethane Chemical compound COC.OC(=O)\C=C/C(O)=O AHQNFRFBKOXXBK-ODZAUARKSA-N 0.000 description 2
- GWEHVDNNLFDJLR-UHFFFAOYSA-N 1,3-diphenylurea Chemical compound C=1C=CC=CC=1NC(=O)NC1=CC=CC=C1 GWEHVDNNLFDJLR-UHFFFAOYSA-N 0.000 description 2
- SMZOUWXMTYCWNB-UHFFFAOYSA-N 2-(2-methoxy-5-methylphenyl)ethanamine Chemical compound COC1=CC=C(C)C=C1CCN SMZOUWXMTYCWNB-UHFFFAOYSA-N 0.000 description 2
- NIXOWILDQLNWCW-UHFFFAOYSA-N 2-Propenoic acid Natural products OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 description 2
- 240000007087 Apium graveolens Species 0.000 description 2
- 235000015849 Apium graveolens Dulce Group Nutrition 0.000 description 2
- 235000010591 Appio Nutrition 0.000 description 2
- 239000004604 Blowing Agent Substances 0.000 description 2
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 2
- NPBVQXIMTZKSBA-UHFFFAOYSA-N Chavibetol Natural products COC1=CC=C(CC=C)C=C1O NPBVQXIMTZKSBA-UHFFFAOYSA-N 0.000 description 2
- 244000060011 Cocos nucifera Species 0.000 description 2
- 235000013162 Cocos nucifera Nutrition 0.000 description 2
- 208000006558 Dental Calculus Diseases 0.000 description 2
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 2
- JIGUQPWFLRLWPJ-UHFFFAOYSA-N Ethyl acrylate Chemical compound CCOC(=O)C=C JIGUQPWFLRLWPJ-UHFFFAOYSA-N 0.000 description 2
- IAYPIBMASNFSPL-UHFFFAOYSA-N Ethylene oxide Chemical compound C1CO1 IAYPIBMASNFSPL-UHFFFAOYSA-N 0.000 description 2
- 239000005770 Eugenol Substances 0.000 description 2
- 240000006927 Foeniculum vulgare Species 0.000 description 2
- 235000004204 Foeniculum vulgare Nutrition 0.000 description 2
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- AMQJEAYHLZJPGS-UHFFFAOYSA-N N-Pentanol Chemical compound CCCCCO AMQJEAYHLZJPGS-UHFFFAOYSA-N 0.000 description 2
- 108091005804 Peptidases Proteins 0.000 description 2
- WCUXLLCKKVVCTQ-UHFFFAOYSA-M Potassium chloride Chemical compound [Cl-].[K+] WCUXLLCKKVVCTQ-UHFFFAOYSA-M 0.000 description 2
- UVMRYBDEERADNV-UHFFFAOYSA-N Pseudoeugenol Natural products COC1=CC(C(C)=C)=CC=C1O UVMRYBDEERADNV-UHFFFAOYSA-N 0.000 description 2
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 description 2
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 description 2
- 244000269722 Thea sinensis Species 0.000 description 2
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 description 2
- 238000005299 abrasion Methods 0.000 description 2
- 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 2
- 125000001931 aliphatic group Chemical group 0.000 description 2
- 150000001336 alkenes Chemical class 0.000 description 2
- 125000000217 alkyl group Chemical group 0.000 description 2
- 150000003863 ammonium salts Chemical class 0.000 description 2
- 230000000844 anti-bacterial effect Effects 0.000 description 2
- 239000004599 antimicrobial Substances 0.000 description 2
- 229950011260 betanaphthol Drugs 0.000 description 2
- 238000004061 bleaching Methods 0.000 description 2
- 239000011575 calcium Substances 0.000 description 2
- 229910052791 calcium Inorganic materials 0.000 description 2
- JUNWLZAGQLJVLR-UHFFFAOYSA-J calcium diphosphate Chemical compound [Ca+2].[Ca+2].[O-]P([O-])(=O)OP([O-])([O-])=O JUNWLZAGQLJVLR-UHFFFAOYSA-J 0.000 description 2
- 229960002504 capsaicin Drugs 0.000 description 2
- 235000017663 capsaicin Nutrition 0.000 description 2
- 150000001732 carboxylic acid derivatives Chemical class 0.000 description 2
- 125000002091 cationic group Chemical group 0.000 description 2
- 210000002421 cell wall Anatomy 0.000 description 2
- QBWCMBCROVPCKQ-UHFFFAOYSA-N chlorous acid Chemical class OCl=O QBWCMBCROVPCKQ-UHFFFAOYSA-N 0.000 description 2
- 238000009833 condensation Methods 0.000 description 2
- 230000005494 condensation Effects 0.000 description 2
- 239000000001 dental powder Substances 0.000 description 2
- 239000003975 dentin desensitizing agent Substances 0.000 description 2
- 235000019821 dicalcium diphosphate Nutrition 0.000 description 2
- RBLGLDWTCZMLRW-UHFFFAOYSA-K dicalcium phosphate dihydrate Substances O.O.[Ca+2].[Ca+2].[O-]P([O-])([O-])=O RBLGLDWTCZMLRW-UHFFFAOYSA-K 0.000 description 2
- 239000003623 enhancer Substances 0.000 description 2
- 229960002217 eugenol Drugs 0.000 description 2
- 235000019634 flavors Nutrition 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- ZSIAUFGUXNUGDI-UHFFFAOYSA-N hexan-1-ol Chemical compound CCCCCCO ZSIAUFGUXNUGDI-UHFFFAOYSA-N 0.000 description 2
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Landscapes
- Cosmetics (AREA)
Description
本發明係有關一種包括口腔可接受的載劑及二氧化矽磨料之口腔用組成物,該二氧化矽磨料包括具有5μm至20μm的平均粒徑、60cc/100g至120cc/100g的吸油量、及4至11的Einlehner硬度之沉澱非晶形二氧化矽化合物,及其使用方法。The present invention relates to an oral composition comprising an orally acceptable carrier and a cerium oxide abrasive, the cerium oxide abrasive comprising an average particle diameter of from 5 μm to 20 μm, an oil absorption of from 60 cc/100 g to 120 cc/100 g, and 4 to 11 Einlehner hardness precipitated amorphous ceria compound, and method of use thereof.
口腔用組成物中之磨料清除及身體上擦洗牙齒的外部表面。此擦洗作用移除牙齒表面上之有機生物膜(亦即薄膜),其主要地由唾液蛋白質、細菌、及細菌副產物形成。薄膜亦可被食物(例如咖啡、茶及莓果)以及被菸草煙、陽離子化合物及產色細菌沾汙及變色。該沾汙薄膜之物理移除為簡單且有效方式移除每日出現的不想要表面染色及變色作用。另外,該薄膜之物理移除亦移除薄膜表面上之齒菌斑細菌,從而最小化齒齦炎、牙周炎、及齲蛀形成之可能性。然而,口腔用組成物例如牙粉不應具有如此高磨蝕性以致可對珐瑯質或組織產生潛在損害。因而,想要研發一種口腔用組成物,其完美化口腔用組成物之潔淨及/或磨光功效,同時最小化有害磨蝕性以避免潛在損害口腔表面。較好者,該口腔用組成物具有高薄膜潔淨比率(PCR),但低程度牙齒磨損,其係測量為放射性牙齒磨損(radioactive dental abrasion,RDA)。Abrasives in the oral composition remove and physically scrub the external surface of the teeth. This scrubbing action removes the organic biofilm (i.e., film) on the surface of the tooth, which is primarily formed by salivary proteins, bacteria, and bacterial by-products. Films can also be contaminated and discolored by foods such as coffee, tea and berries as well as by tobacco smoke, cationic compounds and chromogenic bacteria. Physical removal of the soiled film is a simple and effective way to remove unwanted surface staining and discoloration that occurs daily. In addition, the physical removal of the film also removes plaque bacteria on the surface of the film, thereby minimizing the likelihood of gingivitis, periodontitis, and sputum formation. However, oral compositions such as dentifrice should not be so highly abrasive that they can cause potential damage to the enamel or tissue. Accordingly, it is desirable to develop an oral composition that saturates the cleansing and/or polishing benefits of the oral composition while minimizing harmful abrasion to avoid potentially damaging the oral surface. Preferably, the oral composition has a high film cleansing ratio (PCR), but a low degree of tooth wear, which is measured as radioactive dental abrasion (RDA).
一般可接受的慣用常規中,口腔用組成物之RDA值通常保持低於250以避免經重複使用損傷珐瑯質/齒質(dentin)。然而,為了達到更高PCR,磨料之用量及硬度必須典型地增加,其慣常已知增加RDA。例如,已觀察到當牙粉組成物之RDA值超過若干數值時(例如高於100至115),牙粉不必然展現對應增加於牙粉之潔淨成果。已挑戰調配具有PCR大於80或90但仍具有RDA低於250之口腔用組成物。In a generally accepted conventional practice, the RDA value of the oral composition is typically maintained below 250 to avoid damage to the dentin/dentin. However, in order to achieve higher PCR, the amount and hardness of the abrasive must typically increase, which is conventionally known to increase RDA. For example, it has been observed that when the RDA value of the dentifrice composition exceeds several values (e.g., above 100 to 115), the dentifrice does not necessarily exhibit a corresponding increase in the cleansing effect of the dentifrice. It has been challenged to formulate oral compositions having a PCR greater than 80 or 90 but still having an RDA of less than 250.
已令人驚訝地發現在口腔用護理組成物中使用特別二氧化矽磨料給予優秀潔淨能力(如高PCR值),且同時減少對硬牙齒表面損害(如低PDA)。有用於本發明之二氧化矽磨料維持其等完整性,同時擦掉牙齒表面上的軟性物質,例如齒菌斑及薄膜。然而,由於與硬珐瑯質或齒質表面相互作用的結果,二氧化矽磨料在剪力下(如刷淨期間)破壞或斷裂。在此方面,本發明口腔用組成物提供優秀潔淨及/或磨光功效,同時達到最小化對珐瑯質或齒質潛在損害之想要低RDA。此外,本發明組成物可提供牙齒表面之潔淨及/或磨光。潔淨及/或磨光磨料可藉由各種物理參數分類。如熟習技藝者所領會,單一磨料物種典型地同時執行至少若干潔淨及磨光。It has been surprisingly found that the use of special cerium oxide abrasives in oral care compositions imparts excellent cleansing power (e.g., high PCR values) while at the same time reducing damage to hard tooth surfaces (e.g., low PDA). The cerium oxide abrasive used in the present invention maintains its integrity while wiping off soft substances such as plaque and film on the surface of the teeth. However, the cerium oxide abrasive breaks or breaks under shear (such as during brushing) as a result of interaction with the hard enamel or dentate surface. In this regard, the oral compositions of the present invention provide excellent cleansing and/or polishing benefits while minimizing the desired low RDA for potential damage to enamel or dentin. In addition, the compositions of the present invention provide for cleansing and/or polishing of the tooth surface. Clean and/or polished abrasives can be classified by various physical parameters. As is appreciated by those skilled in the art, a single abrasive species typically performs at least some cleaning and polishing at the same time.
在一項具體實例中,本發明係有關組成物1.0,一種包括口腔可接受的載劑及二氧化矽磨料之口腔用組成物,該二氧化矽磨料包括具有5μm至20μm的平均粒徑、及4至11的Einlehner硬度之二氧化矽化合物。In one embodiment, the present invention is directed to a composition 1.0, an oral composition comprising an orally acceptable carrier and a ceria abrasive comprising an average particle size of from 5 μm to 20 μm, and 4 to 11 Einlehner hardness of cerium oxide compound.
本發明額外組成物為下列組成物:The additional composition of the present invention is the following composition:
1.1組成物1.0,其中二氧化矽磨料具有8μm至11μm,如9μm至13μm的平均粒徑。1.1 Composition 1.0 wherein the cerium oxide abrasive has an average particle size of from 8 μm to 11 μm, such as from 9 μm to 13 μm.
1.2組成物1.0或1.1,其中二氧化矽磨料具有60cc/100g至120cc/100g,如70cc/100g至110cc/100g,如80cc/100g至100cc/100g的吸油量,如亞麻籽油吸收。1.2 Composition 1.0 or 1.1 wherein the cerium oxide abrasive has an absorption of from 60 cc / 100 g to 120 cc / 100 g, such as from 70 cc / 100 g to 110 cc / 100 g, such as 80 cc / 100 g to 100 cc / 100 g, such as linseed oil absorption.
1.3任何一種前述組成物,其中二氧化矽磨料具有5至10,如6至9的Einlehner硬度。1.3 Any of the preceding compositions wherein the cerium oxide abrasive has an Einlehner hardness of from 5 to 10, such as from 6 to 9.
1.4任何一種前述組成物,其具有80至105,如85至100、或90至95的薄膜潔淨比率(PCR);1.4 any of the foregoing compositions having a film clean ratio (PCR) of from 80 to 105, such as from 85 to 100, or from 90 to 95;
1.5任何一種前述組成物,其具有小於150,如90至130、100至120、或105至115的放射性齒質磨損(radioactive dentin abrasion,RDA);1.5 any of the foregoing compositions having a radioactive dentin abrasion (RDA) of less than 150, such as from 90 to 130, from 100 to 120, or from 105 to 115;
1.6任何一種前述組成物,其具有0.5至1.5,如0.8、或1的PCR/RDA比率;1.6 any of the foregoing compositions having a PCR/RDA ratio of from 0.5 to 1.5, such as 0.8, or 1.
1.7任何一種前述組成物,其中二氧化矽磨料係1重量%至95重量%的組成物。1.7 Any of the foregoing compositions, wherein the cerium oxide abrasive is from 1% to 95% by weight of the composition.
1.8任何一種前述組成物,其中二氧化矽磨料具有d10 為2.5μm至2.9μm;1.8 any one of the preceding compositions, wherein the cerium oxide abrasive has a d 10 of from 2.5 μm to 2.9 μm;
1.9任何一種前述組成物,其中當口腔用組成物塗敷於口腔中之硬表面時(如珐瑯質或齒質),二氧化矽磨料破碎;1.9 any one of the preceding compositions, wherein the cerium oxide abrasive is broken when the oral composition is applied to a hard surface in the oral cavity (such as enamel or dentin);
1.10任何一種前述組成物,其中在口腔中使用組成物時,二氧化矽磨料破裂成具有d10 為2.3μm至2.6μm之顆粒;1.10. Any of the foregoing compositions, wherein when the composition is used in the oral cavity, the ceria abrasive is broken into particles having a d 10 of from 2.3 μm to 2.6 μm;
1.11任何一種前述組成物,其中當遭受足夠時間量之剪力時,二氧化矽磨料破裂。1.11 Any of the preceding compositions wherein the cerium oxide abrasive ruptures when subjected to a sufficient amount of shear.
1.12任何一種組成物1.9至1.11,其中口腔用組成物係於牙齒上刷淨至少30秒至5分鐘;1.12 any composition 1.9 to 1.11, wherein the oral composition is brushed on the teeth for at least 30 seconds to 5 minutes;
1.13任何一種組成物1.9至1.12,其中塗敷於口腔中之硬表面後,二氧化矽磨料之平均粒徑減少16%至20%;1.13 any composition 1.9 to 1.12, wherein after application to the hard surface of the oral cavity, the average particle size of the cerium oxide abrasive is reduced by 16% to 20%;
1.14任何一種組成物1.9至1.13,其中塗敷於口腔中之硬表面後,二氧化矽磨料之d10 減少9%至12%。1.14 Any composition 1.9 to 1.13 in which the d 10 of the cerium oxide abrasive is reduced by 9% to 12% after application to a hard surface in the oral cavity.
1.15任何一種前述組成物,包括有效量氟化物鹽,如0.01重量%至2重量%、如0.1重量%至0.2重量%的總組成物重。1.15 Any of the foregoing compositions comprising an effective amount of a fluoride salt, such as from 0.01% to 2% by weight, such as from 0.1% to 0.2% by weight of the total composition.
1.16任何一種前述組成物,包括氟化物離子源,其包括選自氟化錫(II)、氟化鈉、氟化鉀、單氟磷酸鈉、氟矽酸鈉、氟矽酸銨、氟化胺、氟化胺氟化銨(amine fluoride ammonium fluoride)、及其組合之氟化物鹽。1.16 Any of the foregoing compositions, comprising a fluoride ion source comprising a tin (II) fluoride, sodium fluoride, potassium fluoride, sodium monofluorophosphate, sodium fluoroantimonate, ammonium fluoroantimonate, ammonium fluoride , fluoride fluoride of ammonium fluoride, and combinations thereof.
1.17任何一種前述組成物,其包括500至5000、1000至1500、或1450ppm氟化物離子。1.17 Any of the foregoing compositions comprising 500 to 5000, 1000 to 1500, or 1450 ppm fluoride ions.
1.18任何一種前述組成物,其包括至少一種界面活性劑。1.18 Any of the preceding compositions comprising at least one surfactant.
1.19任何一種前述組成物,其包括至少一種選自月桂基硫酸鈉、椰油醯胺基丙基甜菜鹼、及其組合之界面活性劑。1.19 Any of the preceding compositions comprising at least one surfactant selected from the group consisting of sodium lauryl sulfate, cocoamidopropyl betaine, and combinations thereof.
1.20任何一種前述組成物,其包括陰離子界面活性劑。1.20 Any of the foregoing compositions comprising an anionic surfactant.
1.21任何一種前述組成物,其包括月桂基硫酸鈉。1.21 Any of the preceding compositions comprising sodium lauryl sulfate.
1.22任何一種前述組成物,其包括至少一種保濕劑。1.22 Any of the preceding compositions comprising at least one humectant.
1.23任何一種前述組成物,其包括至少一種選自甘油、山梨醇及其組合之保濕劑。1.23 Any of the preceding compositions comprising at least one humectant selected from the group consisting of glycerin, sorbitol, and combinations thereof.
1.24任何一種前述組成物,其包括至少一種聚合物。1.24 Any of the preceding compositions comprising at least one polymer.
1.25任何一種前述組成物,其包括至少一種選自聚乙二醇、聚乙烯基甲基醚順丁烯二酸共聚物、多醣類(如纖維素衍生物,例如羧甲基纖維素,或多醣膠,例如三仙膠或鹿角菜膠)、及其組合之聚合物。1.25 any one of the foregoing compositions comprising at least one member selected from the group consisting of polyethylene glycol, polyvinyl methyl ether maleic acid copolymer, polysaccharides (such as cellulose derivatives such as carboxymethyl cellulose, or A polysaccharide gum, such as a tricyanidin or carrageenan, and a combination thereof.
1.26任何一種前述組成物,其包括調味料、香氣及/或著色劑。1.26 Any of the preceding compositions comprising a flavoring, aroma and/or colorant.
1.27任何一種前述組成物,其包括抗菌劑。1.27 Any of the preceding compositions comprising an antimicrobial agent.
1.28任何一種前述組成物,其包括選自經鹵化的二苯基醚(三氯沙)、草本萃取物或精油(如迷迭香萃取物、瑞香草、薄荷腦、桉樹腦、柳酸甲酯)、雙胍防腐劑(如氯已定(chlorhexidine)、阿來西定(alexdine)或奧替尼啶(octenidine))、四級銨化合物(如氯化鯨蠟基吡啶)、酚類防腐劑、海克西定(hexetidine)、聚維酮碘(povidone iodine)、地莫前列素(delmopinol)、salifluor、金屬離子(如鋅鹽,例如檸檬酸鋅)、血根鹼、蜂巢蠟膠(propolis)、及氧化劑(oxygenating agent)(如過氧化氫、緩衝過氧硼酸鈉或過氧碳酸鈉)之抗菌劑。1.28 Any of the foregoing compositions comprising a halogenated diphenyl ether (triclosan), an herbal extract or an essential oil (such as rosemary extract, rucola, menthol, cineole, methyl salicylate) ), biguanide preservatives (such as chlorhexidine, alexidine or octenidine), quaternary ammonium compounds (such as cetylpyridinium chloride), phenolic preservatives, Hexetidine, povidone iodine, delmopinol, salifluor, metal ions (such as zinc salts such as zinc citrate), blood base, propolis And an oxidizing agent (such as hydrogen peroxide, buffered sodium peroxyborate or sodium percarbonate).
1.29任何一種前述組成物,其包括三氯沙。1.29 Any of the foregoing compositions comprising triclosan.
1.30任何一種前述組成物,其包括抗菌劑呈用量為0.01至5、0.01至1.0、或0.3重量%的總組成物重。1.30 Any of the foregoing compositions comprising an antibacterial agent in an amount of from 0.01 to 5, from 0.01 to 1.0, or 0.3% by weight of the total composition.
1.31任何一種前述組成物,其包括牙齒減敏劑;1.31 any of the foregoing compositions, comprising a tooth desensitizing agent;
1.32任何一種前述組成物,其包括選自鉀鹽、辣椒鹼、丁香酚、鍶鹽、鋅鹽、氯化物鹽、或其組合之牙齒減敏劑;1.32 any of the preceding compositions comprising a tooth desensitizing agent selected from the group consisting of potassium salts, capsaicin, eugenol, sulfonium salts, zinc salts, chloride salts, or combinations thereof;
1.33任何一種前述組成物,其包括牙齒美白化合物;1.33 of any of the preceding compositions, comprising a tooth whitening compound;
1.34任何一種前述組成物,其其係牙齒粉末;1.34 any of the foregoing compositions, which are dental powders;
1.35任何一種前述組成物,其包括水;1.35 any of the foregoing compositions, which comprises water;
1.36任何一種前述組成物,其係牙膏或凝膠。1.36 Any of the foregoing compositions which are toothpaste or gel.
1.37任何一種前述組成物,其中口腔用組成物之RDA係藉由下列方法計算,包括將1至5ml口腔用組成物漿液塗敷於1至10cm2 表面,使表面對32 P放射的牙齒接觸,於2至5牛頓的恆定力刷淨牙齒表面300行程(stroke),其中各行程造成表面對牙齒移動1至10cm2 ,及測量RDA值。1.37 Any of the preceding compositions, wherein the RDA of the oral composition is calculated by the following method comprising applying 1 to 5 ml of the oral composition slurry to a surface of 1 to 10 cm 2 to contact the surface with 32 P radiation. A constant force of 2 to 5 Newtons is used to brush the tooth surface 300 strokes, wherein each stroke causes the surface to move 1 to 10 cm 2 of the tooth and measure the RDA value.
1.38任何一種前述組成物,其中當組成物用於口腔時(如與硬牙齒表面接觸),組成物之RDA隨時間而減少,且口腔用組成物之RDA係藉由1.37中識別之方法計算,但書為在最初時間A利用之行程數目少於在稍後時間B使用之行程數目,如300行程大約等於2分鐘刷淨;1.38 Any of the preceding compositions, wherein when the composition is applied to the oral cavity (e.g., in contact with a hard tooth surface), the RDA of the composition decreases over time, and the RDA of the oral composition is calculated by the method identified in 1.37. However, the book is that the number of trips used at the initial time A is less than the number of trips used at a later time B, such as 300 trips equal to about 2 minutes;
1.39任何一種前述組成物,其中在口腔中使用5秒的口腔用組成物之RDA為1.3至1.6倍在口腔中使用1至5分鐘(如2、3、或4分鐘)的組成物之RDA。1.39 Any of the preceding compositions wherein the RDA of the oral composition for 5 seconds in the oral cavity is 1.3 to 1.6 times the RDA of the composition for 1 to 5 minutes (e.g., 2, 3, or 4 minutes) in the oral cavity.
1.40組成物1.39,其中表面為牙刷之潔淨頭;1.40 composition 1.39, wherein the surface is a clean head of the toothbrush;
1.41組成物1.39或1.40,其中計算RDA之方法為漿液包括50重量%至100重量%的口腔用組成物。1.41 Composition 1.39 or 1.40, wherein the method of calculating RDA is that the slurry comprises from 50% to 100% by weight of the oral composition.
1.42任何一種前述組成物,其中Einlehner硬度係每174,000迴轉以黃銅網測量。1.42 Any of the foregoing compositions wherein the Einlehner hardness is measured in brass nets per 174,000 revolutions.
1.43任何一種組成物1.0至1.41,其中Einlehner硬度係每100,000迴轉以黃銅網測量。1.43 Any of the compositions 1.0 to 1.41, wherein the Einlehner hardness is measured in brass nets per 100,000 revolutions.
1.44組成物1.42或1.43,其中Einlehner硬度為100g二氧化矽磨料於1L水中之漿液。1.44 Composition 1.42 or 1.43, wherein the Einlehner hardness is 100 g of a slurry of cerium oxide abrasive in 1 liter of water.
1.45任何一種前述組成物,其中10%二氧化矽磨料之水性漿液具有PCR為65至80,如68至76、或72。1.45 Any of the preceding compositions wherein the aqueous slurry of 10% cerium oxide abrasive has a PCR of from 65 to 80, such as from 68 to 76, or 72.
1.46任何一種前述組成物,其中10%二氧化矽磨料之水性漿液具有RDA為75至91,如79至87、或83;1.46 any of the preceding compositions, wherein the aqueous slurry of 10% cerium oxide abrasive has an RDA of 75 to 91, such as 79 to 87, or 83;
1.47任何一種前述組成物,其中10%二氧化矽磨料之水性漿液具有PCR/RDA比率為0.7至0.9,如0.8至0.9,如0.86;1.47. Any one of the preceding compositions, wherein the aqueous slurry of 10% cerium oxide abrasive has a PCR/RDA ratio of from 0.7 to 0.9, such as from 0.8 to 0.9, such as 0.86;
1.48任何一種前述組成物,其中15%二氧化矽磨料之水性漿液具有PCR為68至84,如62至80、或76。1.48 Any of the preceding compositions wherein the aqueous slurry of 15% cerium oxide abrasive has a PCR of from 68 to 84, such as from 62 to 80, or 76.
1.49任何一種前述組成物,其中15%二氧化矽磨料之水性漿液具有RDA為85至105,如90至100、或95;1.49 any one of the preceding compositions, wherein the aqueous slurry of 15% cerium oxide abrasive has an RDA of 85 to 105, such as 90 to 100, or 95;
1.50任何一種前述組成物,其中15%二氧化矽磨料之水性漿液具有PCR/RDA比率為0.7至0.9,如0.76至0.8,如0.86;1.50 any of the foregoing compositions, wherein the aqueous slurry of 15% cerium oxide abrasive has a PCR/RDA ratio of from 0.7 to 0.9, such as from 0.76 to 0.8, such as 0.86;
1.51任何一種前述組成物,其中20%二氧化矽磨料之水性漿液具有PCR為76至92,如80至88、或84。1.51 Any of the foregoing compositions wherein the aqueous slurry of 20% cerium oxide abrasive has a PCR of from 76 to 92, such as from 80 to 88, or 84.
1.52任何一種前述組成物,其中20%二氧化矽磨料之水性漿液具有RDA為85至101,如89至97、或93;Any of the foregoing compositions, wherein the aqueous slurry of 20% cerium oxide abrasive has an RDA of 85 to 101, such as 89 to 97, or 93;
1.53任何一種前述組成物,其中20%二氧化矽磨料之水性漿液具有PCR/RDA比率為0.8至1.0,如0.85至0.95,如0.9;Any of the foregoing compositions, wherein the aqueous slurry of 20% cerium oxide abrasive has a PCR/RDA ratio of from 0.8 to 1.0, such as from 0.85 to 0.95, such as 0.9;
1.54任何一種前述組成物,其中30%二氧化矽磨料之水性漿液具有PCR為78至94,如82至90、或86。1.54 Any of the preceding compositions wherein the aqueous slurry of 30% cerium oxide abrasive has a PCR of from 78 to 94, such as from 82 to 90, or 86.
1.55任何一種前述組成物,其中30%二氧化矽磨料之水性漿液具有RDA為100至124,如106至118、或112;Any of the foregoing compositions, wherein the aqueous slurry of 30% cerium oxide abrasive has an RDA of from 100 to 124, such as from 106 to 118, or 112;
1.56任何一種前述組成物,其中30%二氧化矽磨料之水性漿液具有PCR/RDA比率為0.6至0.9,如0.7至0.8,如0.77;Any of the foregoing compositions, wherein the aqueous slurry of 30% cerium oxide abrasive has a PCR/RDA ratio of from 0.6 to 0.9, such as from 0.7 to 0.8, such as 0.77;
1.57組成物1.0,其中二氧化矽磨料具有8μm至11μm,例如(但不限於)9μm至13μm、8μm至12μm、或8μm至11μm的中數粒徑。1.57 Composition 1.0 wherein the cerium oxide abrasive has a median particle size of from 8 μm to 11 μm, such as, but not limited to, from 9 μm to 13 μm, from 8 μm to 12 μm, or from 8 μm to 11 μm.
1.58任何一種組成物1.9至1.12,其中塗敷於口腔中之硬表面後,二氧化矽磨料之中數粒徑減少16%至20%。1.58 Any of the compositions 1.9 to 1.12, wherein after application to a hard surface in the oral cavity, the particle size of the cerium oxide abrasive is reduced by 16% to 20%.
使用作為本發明磨料之二氧化矽化合物可為非晶形二氧化矽、沉澱二氧化矽、或非晶形沉澱二氧化矽。在一個具體實例中,二氧化矽磨料實質上由本文所述之二氧化矽化合物組成。本文所述之二氧化矽磨料可起牙齒潔淨劑、牙齒磨光劑、及/或抗敏感劑作用。The cerium oxide compound used as the abrasive of the present invention may be amorphous cerium oxide, precipitated cerium oxide, or amorphous precipitated cerium oxide. In one embodiment, the cerium oxide abrasive consists essentially of the cerium oxide compound described herein. The cerium oxide abrasive described herein can function as a tooth cleanser, a dental polish, and/or an anti-sensitizer.
本發明額外態樣涉及令人驚訝發現為斷裂二氧化矽磨料顆粒可幫助治療牙齒敏感性,因為斷裂顆粒可堵塞小管封閉作用(tubule occlusion)。此外,亦已令人驚訝發現較小顆粒更有效從口腔中裂縫移除碎片及汙跡,特別是牙齒之相鄰齒間表面。An additional aspect of the invention relates to the surprising discovery that broken cerium oxide abrasive particles can help treat tooth sensitivity because broken particles can block tubule occlusion. In addition, it has been surprisingly found that smaller particles are more effective in removing debris and stains from cracks in the oral cavity, particularly adjacent interdental surfaces of the teeth.
本發明亦含括方法2.0,一種改良口腔健康之方法,包括將有效量的組成物1.0至1.55下任何具體實例之口腔用組成物塗敷於其有需求病患之口腔,如一種方法The invention also encompasses the method 2.0, a method for improving oral health, comprising applying an effective amount of the oral composition of any specific example of 1.0 to 1.55 to the oral cavity of a patient in need thereof, such as a method
1.減少或抑制齲齒形成,1. Reduce or inhibit the formation of caries,
2.減少、修補或抑制珐瑯質之預齲蛀損傷,如藉由量化光誘致螢光(QLF)或電導測量(ECM)偵測,2. Reduce, repair or inhibit enamel pre-crack damage, such as by quantifying light-induced fluorescence (QLF) or conductance measurement (ECM) detection,
3.減少或抑制牙齒去礦質作用及促進牙齒再礦化作用,3. Reduce or inhibit tooth demineralization and promote tooth remineralization,
4.減少牙齒之過敏性,4. Reduce the allergenicity of teeth,
5.減少或抑制齒齦炎,5. Reduce or inhibit gingivitis,
6.抑制微生物生物膜形成於口腔中,6. inhibit the formation of microbial biofilm in the oral cavity,
7.減少齒菌斑累積,及/或7. Reduce plaque accumulation, and / or
8.潔淨牙齒及口腔。8. Clean teeth and mouth.
本發明其他具體實例將顯而易見於熟習技藝者。Other embodiments of the invention will be apparent to those skilled in the art.
如本文所用,除非另外指明,本文所述之所有測量水平係根據總組成物重量。此外,本文引用之所有參考文獻以其等整體於此併入為參考。然而,萬一有任何於本揭示中定義與引用參考文獻中定義之衝突,本揭示控制。As used herein, all measurement levels described herein are based on the total composition weight, unless otherwise indicated. In addition, all of the references cited herein are incorporated herein by reference in their entirety. However, in the event of any conflict between the definitions in this disclosure and the definitions in the cited references, the present disclosure controls.
本文所用之「安全及有效量」意指在未傷害口腔之組織及結構下,治療口腔(如減少齒菌斑、齒齦炎、及/或汙跡)之足夠用量。As used herein, "safe and effective amount" means a sufficient amount to treat the oral cavity (e.g., to reduce plaque, gingivitis, and/or smear) under conditions and structures that do not harm the oral cavity.
本文所用之「口腔可接受的載劑」意指以安全及有效方式塗敷本發明組成物於口腔所使用之一或多種材料。As used herein, "orally acceptable carrier" means one or more materials used in the oral administration of the compositions of the present invention in a safe and effective manner.
如本文所用,「潔淨」通常係指移除標的表面上之污染物、灰塵、雜質、及/或外來物質。例如在口腔表面(其中表面為牙齒珐瑯質)上下文中,潔淨可移除至少若干薄膜或汙跡,例如齒菌斑生物膜、薄膜或牙石。As used herein, "clean" generally refers to the removal of contaminants, dust, impurities, and/or foreign matter from the surface of the target. For example, in the context of an oral surface where the surface is a tooth enamel, the cleansing can remove at least some of the film or stain, such as a plaque biofilm, film or calculus.
如本文所用,「磨光」通常係指使表面更平滑及/或更光澤之精加工或精練方法。磨光及潔淨亦可提供出現汙跡移除之表面明亮,例如牙齒表面之美白。As used herein, "polishing" generally refers to a finishing or scouring process that makes the surface smoother and/or more lustrous. Polishing and cleansing can also provide a bright surface with smudge removal, such as whitening of the tooth surface.
在各種具體實例中,提供具有磨料之口腔用組成物。較佳者,二氧化矽磨料為沉澱非晶形二氧化矽化合物。In various embodiments, an oral composition having an abrasive is provided. Preferably, the cerium oxide abrasive is a precipitated amorphous cerium oxide compound.
本發明二氧化矽可具有5μm至205μm的平均粒徑。顆粒之平均粒徑可藉由技藝中已知之任何方式測量。例如,平均粒徑可使用Malvern Particle Size Analyzer,Model Mastersizer S,Malvern Instruments,Inc.(Southborough,Massachusetts,USA)測量,其中氦-氖氣體雷射束投射通過含有懸浮於水溶液中的磨料之透明光析管(transparent cell)。照在顆粒之光射線散射通過與粒徑成相反比例之角度。光偵測器陣列在數個預先決定的角度測量光之數量。與測量光通量值成比例之電信號然後藉由微電腦系統處理,對照從樣品與水性分散劑的折射率定義之理論顆粒所預料之散射圖案以決定主題磨料之粒徑分布。平均粒徑考量歪斜粒徑及顆粒之尺寸分布。The cerium oxide of the present invention may have an average particle diameter of from 5 μm to 205 μm. The average particle size of the particles can be measured by any means known in the art. For example, the average particle size can be measured using a Malvern Particle Size Analyzer, Model Mastersizer S, Malvern Instruments, Inc. (Southborough, Massachusetts, USA), wherein the xenon-krypton gas laser beam is projected through a transparent light containing an abrasive suspended in an aqueous solution. Transparent cell. The light rays illuminating the particles pass through an angle that is inversely proportional to the particle size. The photodetector array measures the amount of light at several predetermined angles. The electrical signal proportional to the measured luminous flux value is then processed by a microcomputer system to determine the particle size distribution of the subject abrasive against the scattering pattern expected from the theoretical particles defined by the refractive index of the sample and the aqueous dispersion. The average particle size considers the skewed particle size and the size distribution of the particles.
如本文所用,d10 係指顆粒具有直徑為10%底限的抽樣族群(亦即10%族群等於或小於d10 值)。As used herein, d 10 refers to a population of particles having a 10% diameter limit (ie, a 10% population equal to or less than a d 10 value).
已令人驚訝地發現當口腔用組成物對硬牙齒表面(如齒質或珐瑯質)刷淨時,併入口腔用組成物之磨料顆粒破壞或斷裂。亦已令人驚訝地發現當口腔用組成物對口腔之軟表面或軟生物膜(如薄膜或齒菌斑)刷淨時,併入口腔用組成物之磨料顆粒大體上保留其等原始尺寸。It has been surprisingly found that when the oral composition is brushed against a hard tooth surface such as a dentin or enamel, the abrasive particles incorporated into the oral composition are broken or broken. It has also been surprisingly found that when the oral composition is brushed against a soft surface of the oral cavity or a soft biofilm (such as a film or plaque), the abrasive particles incorporated into the oral composition substantially retain their original dimensions.
本發明二氧化矽磨料可具有特定吸油量60cc/100g至120cc/100g亞麻籽油。在一個具體實例中,二氧化矽磨料具有70cc/100g至110cc/100g的吸油量。在一個具體實例中,二氧化矽磨料具有80cc/100g至100cc/100g的吸油量。在一個具體實例中,二氧化矽磨料具有40cc/100g至60cc/100g的吸油量。吸油量可藉由熟習技藝者已知之各種方式決定。例如,吸油量可藉由每100克亞麻籽油或酞酸二丁酯(DBP)或磨料之吸收決定。吸油量值可使用ASTM Rub-Out Method D281測量。The ceria abrasive of the present invention may have a specific oil absorption of 60 cc / 100 g to 120 cc / 100 g of linseed oil. In one embodiment, the ceria abrasive has an oil absorption of from 70 cc/100 g to 110 cc/100 g. In one embodiment, the ceria abrasive has an oil absorption of from 80 cc/100 g to 100 cc/100 g. In one embodiment, the ceria abrasive has an oil absorption of from 40 cc/100 g to 60 cc/100 g. The amount of oil absorbed can be determined by various means known to those skilled in the art. For example, the oil absorption can be determined by absorption per 100 grams of linseed oil or dibutyl phthalate (DBP) or abrasive. The oil absorption value can be measured using ASTM Rub-Out Method D281.
本發明磨料可具有4至11的特定Einlehner硬度。Einlehner硬度可藉由熟習技藝者已知之各種方式決定。例如,Einlehner At-1000 Abrader可以下列方式測量磨料顆粒之硬度:將長網製紙機(Fourdrinier)金屬網(亦即銅或黃銅)秤重並暴露於磨料懸浮液(例如,10%磨料之水性懸浮液)作用達給定數目迴轉(revolution)。硬度值表達成每迴轉數目(如100,000迴轉)長網製紙機線網之毫克重量損失。在本發明中,本發明所用二氧化矽磨料之Einlehner硬度係藉由利用黃銅網決定。將100g二氧化矽添加於1L水,使漿液旋轉達100,000或174,000迴轉。The abrasive of the present invention can have a specific Einlehner hardness of 4 to 11. The Einlehner hardness can be determined by various means known to those skilled in the art. For example, the Einlehner At-1000 Abrader can measure the hardness of abrasive particles in the following manner: Weighing and exposing the Fourdrinier metal mesh (ie copper or brass) to the abrasive suspension (eg, 10% abrasive water) The suspension) acts for a given number of revolutions. The hardness value is expressed as the weight loss per milliliter of the number of revolutions (eg, 100,000 revolutions) of the long net machine wire mesh. In the present invention, the Einlehner hardness of the cerium oxide abrasive used in the present invention is determined by using a brass mesh. 100 g of cerium oxide was added to 1 liter of water to rotate the slurry up to 100,000 or 174,000 revolutions.
本發明磨料成分可以1重量%至95重量%的水平被併入口服護理產品。磨料的存在量取決於口腔用護理組成物之特別形式。例如,當口腔用護理組成物為牙膏或凝膠時,其可含有1%至75%磨料。當口腔用護理組成物為牙粉末時,其可含有50%至95%磨料。The abrasive component of the present invention can be incorporated into an oral care product at a level of from 1% to 95% by weight. The amount of abrasive present depends on the particular form of the oral care composition. For example, when the oral care composition is a toothpaste or gel, it may contain from 1% to 75% of the abrasive. When the oral care composition is a dental powder, it may contain from 50% to 95% of the abrasive.
PCR為熟習技藝者已知的方法以測量相對於標準的移除牙齒汙跡之功效。本文所指之PCR值係藉由修飾「In Vitro Removal of Stain with Dentifrice」,G. K. Stookey等人,J. Dental Research,61,123-9(1982)中所述之方法而獲得。修飾本文所用之PCR方法係敘述於兩者為Rice之美國專利案號5,658,553及5,651,958。在此修飾中,將清澈薄膜材料首先塗敷於牛齒,然後以薄膜材料與茶、咖啡及FeCl3 之組合沾汙,而在由Stookey等人所述原始方法中,薄膜與污跡兩者係同時塗敷。本發明組成物可具有PCR為80至105。在一個具體實例中,PCR為85至100。在另一態樣中,PCR為90至95。PCR is a method known to those skilled in the art to measure the efficacy of removing tooth stains relative to the standard. The PCR values referred to herein are obtained by the method described in "In Vitro Removal of Stain with Dentifrice", GK Stookey et al., J. Dental Research, 61, 123-9 (1982). Modifications The PCR methods used herein are described in U.S. Patent Nos. 5,658,553 and 5,651,958 to Rice. In this modification, a clear film material applied to a bovine tooth first, and then a combination of a thin film material with a tea, coffee and FeCl 3 of the contamination, and in the original method by Stookey et al, both the film and the stain Apply at the same time. The composition of the invention may have a PCR of from 80 to 105. In one embodiment, the PCR is from 85 to 100. In another aspect, the PCR is from 90 to 95.
本發明組成物可具有小於150,如90至130、100至120、105至115的RDA值。RDA值可藉由熟習技藝者已知之任何數量方法決定。例如,RDA值可根據美國專利案號4,340,583、4,420,312與4,421,527、及Hefferreh,Journal of Dental Research,July-August 1976,p.563-573提出之方法決定。通常,放射的32 P齒質係以如口腔用組成物刷淨。從刷淨齒質擦走之齒質量係經由在磨料漿液中觀察到之32 P分析予以量化。齒質磨損量係參考在齒質上刷淨之標準組成物,一般為焦磷酸鈣,其設定RDA值為100。通常,較少磨料組成物具有更低RDA值。The compositions of the present invention may have an RDA value of less than 150, such as from 90 to 130, from 100 to 120, from 105 to 115. The RDA value can be determined by any number of methods known to those skilled in the art. For example, the RDA value can be determined according to the methods proposed in U.S. Patent Nos. 4,340,583, 4,420,312 and 4,421,527, and Hefferreh, Journal of Dental Research, July-August 1976, p. 563-573. Usually, the radiated 32 P dentate is brushed with a composition such as an oral cavity. The quality of the teeth removed from the brushed dentin was quantified by the 32 P analysis observed in the abrasive slurry. The amount of dentin wear is based on a standard composition that is brushed on the tooth, typically calcium pyrophosphate, which has an RDA of 100. Typically, less abrasive composition has a lower RDA value.
本發明組成物可具有0.5至1.5的PCR/RDA比率。在一具體實例中,PCR/RDA比率可為0.5、0.6、0.7、0.8、0.9、1.0、1.1、1.2、1.3、1.4或1.5。使用PCR/RDA比率以決定口腔用護理組成物(如牙粉或牙膏組成物)的潔淨及磨損特徵之相對配給量。The compositions of the invention may have a PCR/RDA ratio of 0.5 to 1.5. In one embodiment, the PCR/RDA ratio can be 0.5, 0.6, 0.7, 0.8, 0.9, 1.0, 1.1, 1.2, 1.3, 1.4, or 1.5. The PCR/RDA ratio is used to determine the relative dosing of the cleansing and wear characteristics of the oral care composition (e.g., dentifrice or toothpaste composition).
製備本發明口腔用組成物之有用二氧化矽磨料材料可從Davison Chemical Division of W. R. Grace & Co. (Baltimore,Maryland,USA)以商品名GRACE VP5獲得。在一具體實例中,二氧化矽為INEOS(現在PQ Corp.)Sorbosil AC43二氧化矽。在一具體實例中,AC43二氧化矽具有下列性質,包含(但不限於)平均粒徑為2.7至4.0微米(由MALVERN MASTERSIZER決定),篩選殘渣為+45μm,於105℃濕度損失為8.0%最大,於1000℃著火損失(ignition loss)為14.0%最大,及在水性懸浮液中pH為5.5至7.5。Useful ceria abrasive materials for preparing the oral compositions of the present invention are available from Davison Chemical Division of W. R. Grace & Co. (Baltimore, Maryland, USA) under the trade name GRACE VP5. In one embodiment, the cerium oxide is INEOS (now PQ Corp.) Sorbosil AC43 cerium oxide. In one embodiment, the AC43 cerium oxide has the following properties, including, but not limited to, an average particle size of 2.7 to 4.0 microns (determined by MALVERN MASTERSIZER), a screening residue of +45 μm, and a humidity loss of 8.0% maximum at 105 °C. The ignition loss at 1000 ° C was 14.0% maximum, and the pH in the aqueous suspension was 5.5 to 7.5.
其他磨料亦可利用於本組成物中,但考量本發明組成物可含有如先前敘述之單一二氧化矽磨料化合物,且可大體上無其他矽或二氧化矽磨料及化合物。Other abrasives may also be utilized in the present compositions, but it is contemplated that the compositions of the present invention may contain a single ceria abrasive compound as previously described, and may be substantially free of other niobium or cerium oxide abrasives and compounds.
口腔可接受的載劑為技藝中熟知,且可含有界面活性劑、保濕劑、增稠劑、發泡劑、氟化物離子源、調味料、著色劑、螯合劑、聚合物、酶、水、活性物、及其他物質。口腔用組成物可進一步包括口腔可接受的載劑。載劑之特定組成物取決於組成物之意欲用途。載劑可為液相、半固相、或固相。口腔用組成物可呈牙粉(包含牙膏、牙粉末、及預防糊狀物)、糖果(包含膠、珠及咀嚼物)、膜、塗擦凝膠(paint-on gel)、或熟習使用磨料技藝者已知之任何其他形式。選擇特定載劑成分取決於想要的產品形式。Orally acceptable carriers are well known in the art and may contain surfactants, humectants, thickeners, foaming agents, fluoride ion sources, flavorings, colorants, chelating agents, polymers, enzymes, water, Active substances, and other substances. The oral composition can further comprise an orally acceptable carrier. The particular composition of the carrier will depend on the intended use of the composition. The carrier can be in the liquid phase, semi-solid phase, or solid phase. The oral composition can be tooth powder (including toothpaste, tooth powder, and prevent paste), candy (including glue, beads, and chews), film, paint-on gel, or familiar with abrasives. Any other form known. The choice of a particular carrier component depends on the desired product form.
活性成分包含例如抗菌活性劑、抗牙石劑、抗齲蛀劑、抗炎劑、抗敏感劑、酶、營養劑等。本文有用之活性物係對投予活性物之人類或較低動物患者,以足夠具有想要治療或預防效果之安全及有效量,無過度負面影響下(例如,毒性、刺激性、或過敏反應),當用於本發明方法時以合理風險/利益比率相稱,視情況存在於本發明組成物中。活性物之特定安全及有效量將隨如欲治療的特別情況、患者的身體情況、同時發生的療法(若任何)本質、所用特定活性物、特定劑量形式、所用載劑、及想要的劑量攝生(dosage regimen)之因素而變化。有用於治療如此情況之活性成分包含Doyle等人之美國專利公開案2003/0206874中所討論者。本文有用者之活性物亦討論於Durga等人之美國專利6,290,933及Lawlor之美國專利6,685,921。The active ingredient contains, for example, an antibacterial active agent, an anticalculus agent, an anticonvulsant, an anti-inflammatory agent, an anti-sensitivity agent, an enzyme, a nutrient, and the like. The actives useful herein are for a human or lower animal patient to which the active is administered, in a safe and effective amount sufficient to have a desired therapeutic or prophylactic effect, without undue adverse effects (eg, toxicity, irritation, or allergic reaction) ), when used in the process of the invention, commensurate with a reasonable risk/benefit ratio, as the case may be, in the compositions of the invention. The particular safe and effective amount of active will vary depending on the particular condition being treated, the condition of the patient, the nature of the concurrent therapy (if any), the particular active employed, the particular dosage form, the carrier employed, and the desired dosage. Changes in the factors of dosage regimen. The active ingredients for treating such conditions include those discussed in U.S. Patent Publication No. 2003/0206874 to Doyle et al. The actives of the present invention are also discussed in U.S. Patent No. 6,290,933 to Durga et al. and U.S. Patent No. 6,685,921 to Lawlor.
氟化物鹽及氟化物離子源(如可溶解之氟化物鹽)為技藝中熟知且可併入本發明組成物中。代表性氟化物離子源包含(但不限於)氟化錫(II)、氟化鈉、氟化鉀、單氟磷酸鈉、氟矽酸鈉、氟矽酸銨、氟化胺、氟化銨、及其組合。在若干具體實例中,氟化物離子源包含氟化錫(II)、氟化鈉、氟化胺、單氟磷酸鈉、以及其混合物。在若干具體實例中,本發明口腔用護理組成物亦可含有氟化物離子或提供氟的成分之來源,以足夠供應25ppm至5,000ppm氟化物離子之用量,通常至少500ppm,如500至2000ppm,如1000至1600ppm,如1450ppm。氟化物離子源可於一個具體實例中呈水平0.01重量%至10重量%被添加於本發明組成物,或於另一具體實例中呈水平0.03重量%至5重量%,及於另一具體實例中呈水平0.1重量%至1重量%組成物;然而,欲了解提供適當水平氟化物離子之氟化物鹽重量將根據鹽中相對離子重量而明顯地變化,且熟習技藝者可很快決定該用量。Fluoride salts and fluoride ion sources (e.g., soluble fluoride salts) are well known in the art and can be incorporated into the compositions of the present invention. Representative fluoride ion sources include, but are not limited to, tin (II) fluoride, sodium fluoride, potassium fluoride, sodium monofluorophosphate, sodium fluoroantimonate, ammonium fluoroantimonate, amine fluoride, ammonium fluoride, And their combinations. In several embodiments, the fluoride ion source comprises tin (II) fluoride, sodium fluoride, amine fluoride, sodium monofluorophosphate, and mixtures thereof. In several embodiments, the oral care compositions of the present invention may also contain a source of fluoride ions or a fluorine-providing component in an amount sufficient to supply 25 ppm to 5,000 ppm of fluoride ions, typically at least 500 ppm, such as 500 to 2000 ppm, such as 1000 to 1600 ppm, such as 1450 ppm. The fluoride ion source may be added to the composition of the invention at a level of from 0.01% to 10% by weight in one embodiment, or from 0.03% to 5% by weight in another embodiment, and in another embodiment The composition is in the range of 0.1% by weight to 1% by weight in the middle; however, it is to be understood that the weight of the fluoride salt providing the appropriate level of fluoride ion will vary significantly depending on the relative ionic weight in the salt, and the skilled artisan can quickly determine the amount. .
本發明口腔用組成物可包含一或多種試劑以增加刷淨口腔時所製造之泡沫量。該發泡劑為熟習技藝者已知。增加泡沫量的試劑之說明實例包含(但不限於)聚氧乙烯及若干聚合物包含(但不限於)藻酸酯聚合物。聚氧乙烯可增加由本發明口服護理載劑成分產生之泡沫量及泡沫厚度。聚氧乙烯一般亦已知為聚乙二醇(「PEG」)或聚環氧乙烷。適合於本發明之聚氧乙烯將具有分子量200,000至7,000,000。在一個具體實例中,分子量將為600,000至2,000,000,且在另一具體實例中為800,000至1,000,000。聚氧乙烯存在量可呈1重量%至90重量%,於一個具體實例中5重量%至50重量%及於另一具體實例中10重量%至20重量%本發明口腔用護理組成物之口服護理載劑成分。口腔用護理組成物中發泡劑劑量(亦即單一劑量)為0.01至0.9重量%、0.05至0.5重量%、且於另一具體實例中0.1至0.2重量%。The oral compositions of the present invention may comprise one or more agents to increase the amount of foam produced when the mouth is brushed. Such blowing agents are known to those skilled in the art. Illustrative examples of agents that increase the amount of foam include, but are not limited to, polyoxyethylene and several polymers including, but not limited to, alginate polymers. Polyoxyethylene can increase the amount of foam and foam thickness produced by the oral care vehicle component of the present invention. Polyoxyethylene is also generally known as polyethylene glycol ("PEG") or polyethylene oxide. Polyoxyethylenes suitable for the present invention will have a molecular weight of from 200,000 to 7,000,000. In one embodiment, the molecular weight will be from 600,000 to 2,000,000, and in another embodiment from 800,000 to 1,000,000. The polyoxyethylene may be present in an amount from 1% to 90% by weight, in one embodiment from 5% to 50% by weight, and in another embodiment from 10% to 20% by weight of the oral care composition of the present invention. Care carrier ingredients. The amount of blowing agent (i.e., a single dose) in the oral care composition is from 0.01 to 0.9% by weight, from 0.05 to 0.5% by weight, and in another embodiment from 0.1 to 0.2% by weight.
本發明組成物亦可合併一或多種技藝中已知之界面活性劑。適合界面活性劑包含合理穩定遍佈寬廣pH範圍者,例如陰離子、陽離子、非離子或兩性離子界面活性劑。適合界面活性劑更完全敘述於例如Agricola等人之美國專利號3,959,458、Haefele之美國專利號3,937,807、及Gieske等人之美國專利號4,051,234,其等併入本文為參考。在若干具體實例中,本文有用之陰離子界面活性劑包含於烷基具有10至18個碳原子的硫酸烷酯之水溶性鹽及具有10至18個碳原子的脂肪酸磺化單甘油酯之水溶性鹽。月桂基硫酸鈉、月桂醯基肌胺酸鈉及椰子單甘油酯磺酸鈉為此類型陰離子界面活性劑實例。亦可利用陰離子界面活性劑之混合物。在另一具體實例中,有用於本發明之陽離子界面活性劑可概括定義為具有一個長烷基鏈含有8至18個碳原子的脂族四級銨化合物之衍生物,例如氯化月桂基三甲基銨、氯化鯨蠟基吡啶、溴化鯨蠟基三甲基銨、氯化二異丁基苯氧基乙基二甲基苄基銨、亞硝酸椰子烷基三甲基銨、氟化鯨蠟基吡啶、及其混合物。說明陽離子界面活性劑為Briner等人之美國專利3,535,421中所述四級銨氟化物,本文併入為參考。若干陽離子界面活性劑亦可作為組成物之殺菌劑。在本發明一個具體實例中,口腔用組成物大體上無陽離子界面活性劑。可用於本發明組成物之說明非離子界面活性劑可概括定義為藉由環氧烷基(本質親水)與可為本質脂族或烷基芳香族之有機疏水化合物縮合而製造之化合物。適合非離子界面活性劑實例包含(但不限於)Pluronics、烷基酚之聚環氧乙烷縮合物、從環氧乙烷與環氧丙烷及伸乙二胺的反應產物縮合而衍生之產物、脂族醇之環氧乙烷縮合物、長鏈三級胺氧化物、長鏈三級膦氧化物、長鏈二烷基亞碸、及該等材料之混合物。在若干具體實例中,有用於本發明之兩性離子合成界面活性劑可概括定義為脂族四級銨、鏻及鋶化合物(sulfonium compound)之衍生物,其中脂族基可為直鏈或分支,且其中一個脂族取代基含有8至18個碳原子及一個含有陰離子水溶性基,如羧基、磺酸鹽、硫酸鹽、磷酸鹽或膦酸鹽。適合內含於組成物中之界面活性劑說明實例包含(但不限於)烷基硫酸鈉、月桂醯基肌胺酸鈉、椰油醯胺基丙基甜菜鹼及聚山梨醇酯20、及其組合。The compositions of the present invention may also incorporate one or more surfactants known in the art. Suitable surfactants include those which are reasonably stable throughout a broad pH range, such as anionic, cationic, nonionic or zwitterionic surfactants. Suitable surfactants are more fully described in, for example, U.S. Patent No. 3,959,458 to Agricola et al., U.S. Patent No. 3,937,807 to Haefele, and U.S. Patent No. 4,051,234 to the name of U.S. Pat. In several embodiments, useful anionic surfactants herein include water soluble salts of alkyl sulfates having from 10 to 18 carbon atoms in the alkyl group and water soluble salts of fatty acid sulfonated monoglycerides having from 10 to 18 carbon atoms. salt. Sodium lauryl sulfate, sodium lauryl sarcosinate, and sodium coconut monoglyceride sulfonate are examples of this type of anionic surfactant. Mixtures of anionic surfactants can also be utilized. In another embodiment, a cationic surfactant useful in the present invention can be broadly defined as a derivative of an aliphatic quaternary ammonium compound having a long alkyl chain having from 8 to 18 carbon atoms, such as lauryl chloride. Methylammonium, cetylpyridinium chloride, cetyltrimethylammonium bromide, diisobutylphenoxyethyldimethylbenzylammonium chloride, coconut alkyltrimethylammonium nitrite, fluorine Whale-based pyridine, and mixtures thereof. The cationic surfactant is described as a quaternary ammonium fluoride as described in U.S. Patent No. 3,535,421, the disclosure of which is incorporated herein by reference. Several cationic surfactants can also be used as bactericides for the composition. In one embodiment of the invention, the oral composition is substantially free of cationic surfactants. Description of the Compositions of the Invention The nonionic surfactant can be broadly defined as a compound produced by the condensation of an alkylene oxide (essentially hydrophilic) with an organic hydrophobic compound which can be an essential aliphatic or alkyl aromatic. Examples of suitable nonionic surfactants include, but are not limited to, Pluronics, polyethylene oxide condensates of alkyl phenols, products derived from the condensation of ethylene oxide with a reaction product of propylene oxide and ethylenediamine, An ethylene oxide condensate of an aliphatic alcohol, a long chain tertiary amine oxide, a long chain tertiary phosphine oxide, a long chain dialkyl fluorene, and a mixture of such materials. In a number of specific examples, the zwitterionic synthetic surfactants useful in the present invention can be broadly defined as derivatives of aliphatic quaternary ammonium, phosphonium and sulfonium compounds, wherein the aliphatic group can be linear or branched. And one of the aliphatic substituents has 8 to 18 carbon atoms and one contains an anionic water-soluble group such as a carboxyl group, a sulfonate, a sulfate, a phosphate or a phosphonate. Examples of surfactants suitable for inclusion in the composition include, but are not limited to, sodium alkyl sulfate, sodium lauryl sarcosinate, cocoamidopropyl betaine, and polysorbate 20, and combination.
本發明組成物可包括陰離子界面活性劑,如月桂基硫酸鈉。界面活性劑或相容界面活性劑之混合物可存在於本發明組成物呈0.1重量%至5.0重量%、於另一具體實例中0.3重量%至3.0重量%及於另一具體實例中0.5重量%至2.0重量%的總組成物。The compositions of the present invention may include an anionic surfactant such as sodium lauryl sulfate. The surfactant or mixture of compatible surfactants may be present in the compositions of the invention from 0.1% to 5.0% by weight, in another embodiment from 0.3% to 3.0% by weight and in another embodiment 0.5% by weight. Up to 2.0% by weight of the total composition.
本發明組成物亦可包含一或多種熟習技藝者已知之調味劑。用於實踐本發明之調味劑包含(但不限於)精油以及各種調味醛、酯、醇、及類似材料。精油實例包含綠薄荷油、薄荷油、冬青油、黃樟油、丁香油、鼠尾草油、桉油、馬鬱蘭油、桂皮油、檸檬油、萊姆油、葡萄柚油、及橙油。亦有用者為如薄荷腦、香旱芹酮、及茴香腦之化學物。若干具體實例使用薄荷油及綠薄荷油。調味劑係以濃度0.1至5重量%及0.5至1.5重量%併入口腔用組成物。在個別口腔用護理組成物劑量中(亦即單一劑量)之調味劑劑量為0.001至0.05重量%及於另一具體實例為0.005至0.015重量%。The compositions of the present invention may also comprise one or more flavoring agents known to those skilled in the art. Flavoring agents useful in the practice of the present invention include, but are not limited to, essential oils as well as various flavoring aldehydes, esters, alcohols, and the like. Examples of essential oils include spearmint oil, peppermint oil, wintergreen oil, sassafras oil, clove oil, sage oil, eucalyptus oil, marjoram oil, cinnamon oil, lemon oil, lime oil, grapefruit oil, and orange oil. Also useful are chemicals such as menthol, fragrant celery, and fennel. Peppermint oil and spearmint oil are used in several specific examples. The flavoring agent is incorporated into the oral composition at a concentration of 0.1 to 5% by weight and 0.5 to 1.5% by weight. The flavoring dose in the individual oral care composition dose (i.e., a single dose) is from 0.001 to 0.05% by weight and in another embodiment from 0.005 to 0.015% by weight.
本發明口腔用護理組成物亦可視情況包含一或多種能夠使在細菌細胞壁中發現的鈣錯合之螯合劑。結合此鈣使細菌細胞壁變弱及擴大細菌溶胞。可有用於本發明之螯合劑的另一組群為可溶性焦磷酸鹽。用於本組成物之焦磷酸鹽可為任何鹼金屬焦磷酸鹽。在若干具體實例中,鹽包含四鹼金屬焦磷酸鹽、二鹼金屬二酸焦磷酸鹽、三鹼金屬單酸焦磷酸鹽及其混合物,其中鹼金屬為鈉或鉀。鹽係有用於其等水合及未水合形式兩者。有用於本組成物之有效量焦磷酸鹽通常足夠提供至少1.0重量%焦磷酸根離子、1.5重量%至6重量%、3.5重量%至6重量%的該離子。The oral care compositions of the present invention may also optionally comprise one or more chelating agents which are capable of aligning the calcium found in the bacterial cell wall. Combining this calcium weakens the bacterial cell wall and enlarges bacterial lysis. Another group that may be present in the chelating agents of the present invention is soluble pyrophosphate. The pyrophosphate used in the present composition may be any alkali metal pyrophosphate. In several embodiments, the salt comprises a tetra alkali metal pyrophosphate, a dialkali metal diacid pyrophosphate, a tribasic metal monoacid pyrophosphate, and mixtures thereof, wherein the alkali metal is sodium or potassium. Salts are used in both their hydrated and unhydrated forms. An effective amount of pyrophosphate for use in the present compositions is generally sufficient to provide at least 1.0% by weight pyrophosphate ion, 1.5% to 6% by weight, 3.5% to 6% by weight of the ion.
本發明口腔用組成物亦視情況包含一或多種聚合物,例如聚乙二醇、聚乙烯基甲基醚順丁烯二酸共聚物、多醣類(如纖維素衍生物,例如羧甲基纖維素,或多醣膠,例如三仙膠或鹿角菜膠)。酸性聚合物(例如聚丙烯酸酯凝膠)可呈其等自由酸或部分或全部中和的水溶性鹼金屬(如鉀及鈉)或銨鹽形式提供。若干具體實例包含1:4至4:1順丁烯二酐或酸與另一可聚合乙烯系不飽和單體之共聚物,例如具有分子量(M.W.)30,000至1,000,000之甲基乙烯基醚(甲氧基乙烯)。此等共聚物係可得例如為GAF Chemicals Corporation之Gantrez AN 139(M.W.500,000)、AN 119(M.W.250,000)及S-97醫藥等級(M.W.70,000)。其他操作聚合物包含例如順丁烯二酐與丙烯酸乙酯、甲基丙烯酸羥乙酯、N-乙烯基-2-吡咯酮(N-vinyl-2-pyrollidone)、或乙烯(後者係可得例如為Monsanto EMA No. 1103,M.W.10,000及EMA Grade 61)之1:1共聚物,及丙烯酸與甲基或羥乙基甲基丙烯酸酯、甲基或乙基丙烯酸酯、異丁基乙烯基醚或N-乙烯基-2-吡咯酮之1:1共聚物。適合者通常為含有活化碳對碳烯烴雙鍵及至少一個羧基之聚合烯烴系或乙烯系不飽和羧酸,亦即含有烯烴雙鍵之酸,該烯烴雙鍵很快於聚合起作用係因為其呈相對羧基為α-β位置或作為部分亞甲基端基存在於單體分子。該酸之說明為丙烯酸、甲基丙烯酸、乙基丙烯酸、α-氯丙烯酸、巴豆酸、β-丙烯氧基丙酸、山梨酸、α-氯山梨酸、桂皮酸、β-苯乙烯基丙烯酸、黏康酸、衣康酸、檸康酸、中康酸、戊烯二酸、烏頭酸、α-苯基丙烯酸、2-苄基丙烯酸、2-環己基丙烯酸、白芷酸、繖形酸、反丁烯二酸、順丁烯二酸及酐。與該羧酸單體可共聚合之其他不同烯烴單體包含乙烯基乙酸酯、氯乙烯、順丁烯二酸二甲酯等。共聚物含有充足水溶性用之羧酸鹽基。進一步分類的聚合劑包含含有經取代丙烯醯胺的同元聚合物及/或不飽和磺酸及其鹽的同元聚合物之組成物,特別是其中聚合物係以具有分子量1,000至2,000,000選自丙烯醯胺基烷磺酸(如2-丙烯醯胺2甲基丙烷磺酸)之不飽和磺酸為主,敘述於Zahid於1989年6月27日之美國專利案號4,842,847,併入本文為參考。The oral composition of the present invention also optionally contains one or more polymers such as polyethylene glycol, polyvinyl methyl ether maleic acid copolymer, polysaccharides (such as cellulose derivatives such as carboxymethyl groups). Cellulose, or polysaccharide gum, such as Sanxian gum or carrageenan). The acidic polymer (e.g., polyacrylate gel) can 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 salt. Several specific examples include 1:4 to 4:1 maleic anhydride or a copolymer of an acid with another polymerizable ethylenically unsaturated monomer, such as methyl vinyl ether having a molecular weight (MW) of 30,000 to 1,000,000 (A) Oxyethylene). Such copolymers are available, for example, from Gantrez AN 139 (M.W. 500,000), AN 119 (M.W. 250,000) and S-97 medical grade (M.W. 70,000) of GAF Chemicals Corporation. Other operating polymers include, for example, maleic anhydride with ethyl acrylate, hydroxyethyl methacrylate, N-vinyl-2-pyrolidone, or ethylene (the latter is available, for example). 1:1 copolymer of Monsanto EMA No. 1103, MW 10,000 and EMA Grade 61), and acrylic acid with methyl or hydroxyethyl methacrylate, methyl or ethyl acrylate, isobutyl vinyl ether or A 1:1 copolymer of N-vinyl-2-pyrrolidone. Suitable as a polymerized olefin-based or ethylenically unsaturated carboxylic acid containing an activated carbon-to-carbon olefin double bond and at least one carboxyl group, that is, an acid containing an olefinic double bond, the olefinic double bond is very fast in polymerization because of its It is present in the monomer molecule at the α-β position relative to the carboxyl group or as a partial methylene end group. The acid is described as 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, leucovoric acid, umbrella acid, anti Butylene diacid, maleic acid and anhydride. Other different olefin monomers copolymerizable with the carboxylic acid monomer include vinyl acetate, vinyl chloride, dimethyl maleate, and the like. The copolymer contains a carboxylate group which is sufficiently water-soluble. Further classified polymeric agents comprise a composition comprising a homopolymer of a substituted acrylamide and/or a homopolymer of an unsaturated sulfonic acid and a salt thereof, particularly wherein the polymer has a molecular weight of from 1,000 to 2,000,000 selected from the group consisting of An unsaturated sulfonic acid of acrylamidoalkyl alkane sulfonic acid (e.g., 2-propenylamine 2 methylpropane sulfonic acid) is described in U.S. Patent No. 4,842,847, issued toJahid et al. reference.
在製備口腔用護理組成物中,有時必須添加若干增稠材料以提供想要稠度或穩定或增進調配物之性能。在若干具體實例中,增稠劑為羧乙烯基聚合物、鹿角菜膠、羥乙基纖維素及纖維素醚之水溶性鹽(例如羧甲基纖維素鈉及羧甲基羥乙基纖維素鈉)。亦可合併天然膠,例如刺梧桐膠、阿拉伯膠、及黃蓍膠。膠狀矽酸鎂鋁或精細分割的二氧化矽可使用作為增稠組成物之成分以進一步改良組成物質地。在若干具體實例中,使用增稠劑呈用量0.5重量%至5.0重量%的總組成物。In the preparation of oral care compositions, it is sometimes necessary to add a number of thickening materials to provide the desired consistency or to stabilize or enhance the properties of the formulation. In several embodiments, the thickening agent is a carboxyvinyl polymer, carrageenan, hydroxyethyl cellulose, and a water soluble salt of a cellulose ether (eg, sodium carboxymethyl cellulose and carboxymethyl hydroxyethyl cellulose) sodium). Natural gums such as karaya gum, gum arabic, and tragacanth can also be combined. Colloidal magnesium aluminum silicate or finely divided cerium oxide can be used as a component of the thickening composition to further improve the constituent materials. In several embodiments, the thickener is used in an amount from 0.5% to 5.0% by weight of the total composition.
本發明口腔用護理組成物亦可視情況包含一或多種酶。有用的酶包含任何可得之蛋白酶、葡聚糖水解酶、內醣苷酶、澱粉酶、葡聚糖變構水解酶(mutanase)、脂酶及黏蛋白酶或其相容混合物。在若干具體實例中,酶為蛋白酶、聚葡糖酶、內醣苷酶及葡聚糖變構水解酶。在另一具體實例中,酶為木瓜酶、內醣苷酶或聚葡糖酶與葡聚糖變構水解酶之混合物。適合用於本發明之額外酶係揭示於Dring等人之美國專利案號5,000,939、美國專利案號4,992,420、美國專利案號4,355,022、美國專利案號4,154,815、美國專利案號4,058,595、美國專利案號3,991,177、及美國專利案號3,696,191,所有併入本文為參考。本發明中數種相容酶之混合物的酶構成0.002%至2.0%於一個具體實例中,或0.05%至1.5%於另一具體實例中,或0.1%至0.5%於又一具體實例中。The oral care compositions of the present invention may also optionally comprise one or more enzymes. Useful enzymes include any available protease, glucanohydrolase, endoglycosidase, amylase, dextran allosteric hydrolase (mutanase), lipase and mucinase or compatible mixtures thereof. In several embodiments, the enzyme is a protease, a polyglucosidase, a endoglycosidase, and a dextran allosteric hydrolase. In another embodiment, the enzyme is a mixture of papain, endoglycosidase or polyglucosidase and a dextran allosteric enzyme. Additional enzymes suitable for use in the present invention are disclosed in U.S. Patent No. 5,000,939 to Dring et al., U.S. Patent No. 4,992,420, U.S. Patent No. 4,355,022, U.S. Patent No. 4,154,815, U.S. Patent No. 4,058,595, U.S. Patent No. 3,991,177 And U.S. Patent No. 3,696,191, the disclosure of which is incorporated herein by reference. The enzyme of a mixture of several compatible enzymes in the present invention constitutes 0.002% to 2.0% in one specific example, or 0.05% to 1.5% in another specific example, or 0.1% to 0.5% in yet another embodiment.
水亦可存在於本發明口腔用組成物中。用於製備商業口腔用組成物之水應去離子化且無有機雜質。水一般補償組成物的差額且包含10重量%至90重量%、20重量%至60重量%或10重量%至30重量%的口腔用組成物。此水量包含加上以其他材料(例如山梨醇或本發明任何成分)導入用量而添加之自由水。Water may also be present in the oral compositions of the present invention. The water used to prepare the commercial oral composition should be deionized and free of organic impurities. The water generally compensates for the difference in composition and comprises from 10% to 90%, from 20% to 60% or from 10% to 30% by weight of the oral composition. This amount of water includes free water added in an amount introduced by other materials such as sorbitol or any of the ingredients of the present invention.
本發明組成物亦可包括保濕劑,如阻止組成物暴露於空氣時免於硬化。若干保濕劑亦可給予牙粉組成物想要甜味或風味。以純保濕劑為主之保濕劑通常於一個具體實例中包含15重量%至70重量%或於另一具體實例中包含30重量%至65重量%的牙粉組成物。適合保濕劑包含食用多元醇,例如甘油、山梨醇、木糖醇、丙二醇以及其他多元醇及此等保濕劑之混合物。甘油及山梨醇之混合物可用於若干具體實例中作為本文牙膏組成物之保濕劑成分。The compositions of the present invention may also include a humectant, such as to prevent the composition from being hardened upon exposure to air. Some humectants can also be given to the dentifrice composition for sweetness or flavor. The humectant which is mainly a pure humectant generally contains 15% by weight to 70% by weight in one specific example or 30% by weight to 65% by weight of the dentifrice composition in another specific example. Suitable humectants include edible polyols such as glycerin, sorbitol, xylitol, propylene glycol, and other polyols and mixtures of such humectants. Mixtures of glycerin and sorbitol can be used in some specific examples as a humectant component of the toothpaste composition herein.
本發明組成物亦可包含一或多種抗菌劑。抗菌劑為技藝中已知且包含苄酸、苄酸鈉、苄酸鉀、硼酸、及酚化合物例如β萘酚(betanaphthol)、氯瑞香草酚、瑞香草酚、茴香腦、桉樹腦、香旱芹酚、薄荷腦、酚、戊酚、己酚、庚酚、辛酚、己間苯二酚、氯化月桂基吡啶、氯化肉豆蔻基吡啶、氟化鯨蠟基吡啶、氯化鯨蠟基吡啶、溴化鯨蠟基吡啶、及經鹵化的二苯基醚(例如三氯沙)。本發明組成物亦可包含一或多種呈自由鹼或鹽形式之鹼性胺基酸,如精胺酸。該試劑可取決於所選之試劑以有效量如1重量%至20重量%(以組成物總重為基礎)添加。The compositions of the present invention may also comprise one or more antimicrobial agents. Antibacterial agents are known in the art and include benzylic acid, sodium benzylate, potassium benzylate, boric acid, and phenolic compounds such as beta naphthol (betanaphthol), clariparin, thymol, fennel, eucalyptus, and aroma Celery, menthol, phenol, pentanol, hexanol, heptol, octylphenol, hexylbenzenediol, lauryl pyridine chloride, myristyl chloride, cetylpyridinium chloride, cetyl chloride Pyridine, brominated cetylpyridine, and halogenated diphenyl ether (eg, triclosan). The compositions of the present invention may also comprise one or more basic amino acids in the form of a free base or salt, such as arginine. The agent may be added depending on the agent selected, in an effective amount, such as from 1% to 20% by weight, based on the total weight of the composition.
本發明組成物可合併一或多種抗敏感劑,如鉀鹽例如硝酸鉀、碳酸氫鉀、氯化鉀、檸檬酸鉀、及草酸鉀;辣椒鹼;丁香酚;鍶鹽;鋅鹽;氯化物鹽及其組合。該試劑可取決於所選之試劑以有效量如1重量%至20重量%(以組成物總重為基礎)添加。本發明組成物當塗敷於牙齒時亦可用於治療由阻塞齒質小管(dentin tubule)之過敏性。The composition of the present invention may be combined with one or more anti-sensitivity agents such as potassium salts such as potassium nitrate, potassium hydrogencarbonate, potassium chloride, potassium citrate, and potassium oxalate; capsaicin; eugenol; sulfonium salt; zinc salt; Salt and its combination. The agent may be added depending on the agent selected, in an effective amount, such as from 1% to 20% by weight, based on the total weight of the composition. The compositions of the present invention can also be used to treat allergies caused by occlusion of a dentin tubule when applied to a tooth.
本發明組成物亦可包含技藝中已知之牙齒美白或牙齒漂白組成物。適合美白及漂白組成物包含過氧化物、金屬亞氯酸鹽、過硫酸鹽。過氧化物包含氫過氧化物、過氧化氫、鹼及鹼土金屬之過氧化物、有機過氧基化合物、過氧酸、及其混合物。鹼及鹼土金屬之過氧化物包含過氧化鋰、過氧化鉀、過氧化鈉、過氧化鎂、過氧化鈣、過氧化鋇、及其混合物。其他過氧化物包含過硼酸鹽、脲過氧化物、及其混合物。適合金屬亞氯酸鹽可包含亞氯酸鈣、亞氯酸鋇、亞氯酸鎂、亞氯酸鋰、亞氯酸鈉、及亞氯酸鉀。該試劑可取決於所選之試劑以有效量如1重量%至20重量%(以組成物總重為基礎)添加。The compositions of the present invention may also comprise tooth whitening or tooth bleaching compositions known in the art. Suitable for whitening and bleaching compositions comprising peroxides, metal chlorites, persulphates. The peroxide comprises a hydroperoxide, hydrogen peroxide, a peroxide of an alkali and an alkaline earth metal, an organic peroxy compound, a peroxyacid, and mixtures thereof. The base and alkaline earth metal peroxides include lithium peroxide, potassium peroxide, sodium peroxide, magnesium peroxide, calcium peroxide, barium peroxide, and mixtures thereof. Other peroxides include perborates, urea peroxides, and mixtures thereof. Suitable metal chlorites may include calcium chlorite, barium chlorite, magnesium chlorite, lithium chlorite, sodium chlorite, and potassium chlorite. The agent may be added depending on the agent selected, in an effective amount, such as from 1% to 20% by weight, based on the total weight of the composition.
除了上述成分外,本發明具體實例可含有若干下述之多樣化視情況牙粉成分。視情況成分包含例如(但不限於)黏著劑、皂洗劑、調味劑、甜味劑、額外抗齒菌斑劑、磨料、及著色劑。此等及其他視情況成分進一步敘述於Majeti之美國專利案號5,004,597、Agricola等人之美國專利案號3,959,458、及Haefele之美國專利案號3,937,807。In addition to the above ingredients, specific examples of the present invention may contain a plurality of the following diverse dentifrice components. Optionally, ingredients include, but are not limited to, adhesives, soaps, flavors, sweeteners, additional anti-plaque agents, abrasives, and color formers. These and other optional components are further described in U.S. Patent No. 5,004,597 to Majeti, U.S. Patent No. 3,959,458 to Agricola et al., and U.S. Patent No. 3,937,807 to Haefele.
本口腔用組成物用之磨料選擇可解釋為磨料類型、細度(粒徑)、粒徑分布及磨料用量,以確保牙齒珐瑯質在正常使用組成物期間無法過度地擦掉,但充分地潔淨及/或磨光。在口腔護理上下文中,磨料之功效可根據牙粉之潔淨或磨損準則表達,即分別薄膜潔淨比率(PCR)或放射性齒質磨損(RDA)。執行PCR及RDA之方法為技藝中已知,如敘述於如美國專利案號5,939,051及6,290,933。The choice of abrasive for the oral composition can be interpreted as the type of abrasive, fineness (particle size), particle size distribution and amount of abrasive to ensure that the tooth enamel cannot be excessively rubbed during normal use of the composition, but is sufficiently clean And / or polished. In the context of oral care, the efficacy of the abrasive can be expressed in terms of the cleanliness or wear criteria of the dentifrice, ie, the film cleansing ratio (PCR) or the radioactive dentin wear (RDA), respectively. Methods of performing PCR and RDA are known in the art, as described in U.S. Patent Nos. 5,939,051 and 6,290,933.
在若干具體實例中,組成物係對人類或其他動物安全於口腔使用,且任何達到以上提出要求之口腔用或化妝可接受的磨料可被選擇於口腔用組成物。In several embodiments, the composition is safe for oral use to humans or other animals, and any oral or cosmetically acceptable abrasive that meets the above requirements can be selected for use in the oral composition.
額外磨料亦可被包含於本發明組成物中,包含鋁氧(煅氧化鋁)、矽藻土、浮石、碳酸鈣、墨魚骨(cuttlebone)、不溶磷酸鹽、複合樹脂(例如三聚氰胺樹脂、酚樹脂、及脲-甲醛樹脂)、聚碳酸酯、碳化硼、微晶蠟、微晶纖維素(包含膠狀微晶纖維素及羧甲基纖維素之組合)、及其組合及衍生物。在不溶磷酸鹽中,有用磨料為原磷酸鹽、聚偏磷酸鹽及焦磷酸鹽。說明實例為二水合原磷酸二鈣、二水合磷酸二鈣、磷酸氫鈣、焦磷酸鈣、焦磷酸β-鈣、磷酸三鈣、偏磷酸鈣、偏磷酸鉀、及偏磷酸鈉。Additional abrasives may also be included in the compositions of the present invention, including aluminum oxide (calcined alumina), diatomaceous earth, pumice, calcium carbonate, cuttlebone, insoluble phosphate, composite resins (eg, melamine resin, phenolic resin). And urea-formaldehyde resin), polycarbonate, boron carbide, microcrystalline wax, microcrystalline cellulose (including a combination of colloidal microcrystalline cellulose and carboxymethyl cellulose), and combinations and derivatives thereof. Among the insoluble phosphates, the useful abrasives are the orthophosphate, polymetaphosphate and pyrophosphate. Examples are dicalcium phosphate dihydrate, dicalcium phosphate dihydrate, calcium hydrogen phosphate, calcium pyrophosphate, beta-calcium pyrophosphate, tricalcium phosphate, calcium metaphosphate, potassium metaphosphate, and sodium metaphosphate.
在若干具體實例中,口腔用組成物係呈牙粉形式,且示範載劑大體上為半固體或固體。載劑可為水性,亦即包括5%至95%水。在其他具體實例中,載劑大體上為非水性。載劑視情況包括例如口腔用護理活性成分、表面活性劑(例如界面活性劑、乳化劑、及泡沫調節物)、黏度改質劑與增稠劑、保濕劑、稀釋劑、填料、額外pH改質劑、著色劑、防腐劑、溶劑、及其組合。欲瞭解雖然以上種類各材料之一般屬性可不同,但可有若干共同屬性且任何給定材料可供應多重目的於二或多項該種類材料內。如熟習技藝者認識,除了先前敘述之彼等材料外,口腔用組成物視情況包含其他材料,包含例如軟化劑、潤膚劑(Moisturizer)、口感劑等。口腔用組成物之適合載劑實例係討論於Boyd等人之美國專利案號6,669,929、Gebreselassie等人之美國專利案號6,379,654、及Nabi等人之美國專利案號4,894,220。In several embodiments, the oral composition is in the form of a dentifrice and the exemplary carrier is substantially semi-solid or solid. The carrier can be aqueous, that is, including from 5% to 95% water. In other embodiments, the carrier is substantially non-aqueous. Carriers include, for example, oral active ingredients, surfactants (eg, surfactants, emulsifiers, and foam regulators), viscosity modifiers and thickeners, humectants, diluents, fillers, additional pH changes. A coloring agent, a coloring agent, a preservative, a solvent, and combinations thereof. It is to be understood that although the general attributes of the various materials of the above categories may vary, there may be several attributes in common and any given material may be supplied for multiple purposes within two or more of that type of material. As will be appreciated by those skilled in the art, in addition to the materials previously described, the oral compositions, as appropriate, comprise other materials including, for example, softeners, emollients, mouth feel agents, and the like. Examples of suitable carriers for the oral compositions are discussed in U.S. Patent No. 6,669,929 to Boyd et al., U.S. Patent No. 6,379,654 to Gebreselassie et al., and U.S. Patent No. 4,894,220 to Nabi et al.
口腔用組成物視情況包括抗結石組成物,例如Gaffar等人之美國專利案號5,292,526中所述之一或多種抗結石組成物。在各種具體實例中,抗結石組成物包含一或多種聚磷酸鹽。抗結石組成物可包含至少一種以有效抗結石量存在於口腔用組成物中之完全或部分中和的鹼金屬或銨三聚磷酸鹽或六偏磷酸鹽。抗結石活性物亦可包含至少一種呈有效抗結石量之水溶性、直線、分子脫水的聚磷酸鹽。抗結石活性物亦可包含鉀及鈉鹽之混合物,其至少一種係以有效抗結石量存在作為聚磷酸鹽抗結石劑。抗結石活性劑亦可含有呈鈉及鉀鹽混合物存在之有效抗結石量之直線分子脫水的聚磷酸鹽抗結石劑。組成物中鉀與鈉之比率可高至小於3:1。聚磷酸鹽可呈各種用量存在於口腔用組成物中,例如用量為聚磷酸根離子(polyphosphate ion)與抗菌劑之重量比率範圍超過0.72:1至小於4:1,或抗菌增進劑與聚磷酸根離子之重量比率範圍1:6至2.7:1,或抗菌增進劑與聚磷酸鹽之重量比率範圍1:6至2.7:1。其他有用抗結石劑包含聚羧酸酯聚合物及聚乙烯基甲基醚/順丁烯二酐(PVM/MA)共聚物,例如GANTREZ。The oral composition, as appropriate, includes an anti-calculus composition, such as one or more of the anti-calculus compositions described in U.S. Patent No. 5,292,526 to Gaffar et al. In various embodiments, the anti-calculus composition comprises one or more polyphosphates. The anti-calculus composition may comprise at least one alkali metal or ammonium tripolyphosphate or hexametaphosphate which is wholly or partially neutralized in the oral composition in an amount effective to resist stone. The anticalculus active may also comprise at least one water soluble, linear, molecularly dehydrated polyphosphate salt in an amount effective to resist stone. The anticalculus active may also comprise a mixture of potassium and sodium salts, at least one of which is present as a polyphosphate anticalculus in an amount effective against stone. The anticalculus active agent may also contain a polyphosphate anticalculus agent which is an effective anti-stone amount in the presence of a mixture of sodium and potassium salts. The ratio of potassium to sodium in the composition can be as high as less than 3:1. The polyphosphate may be present in the oral composition in various amounts, for example, in a weight ratio ranging from polyphosphate ion to antibacterial agent in a range from more than 0.72:1 to less than 4:1, or an antibacterial enhancer and polyphosphoric acid. The weight ratio of the root ions ranges from 1:6 to 2.7:1, or the weight ratio of the antimicrobial enhancer to the polyphosphate ranges from 1:6 to 2.7:1. Other useful anticalculus agents include polycarboxylate polymers and polyvinyl methyl ether/maleic anhydride (PVM/MA) copolymers such as GANTREZ .
有用於本發明牙粉組成物之另外活性劑為抗菌劑,其可以用量0.001至3.0重量%的口腔用組成物存在。有用額外口腔用護理化合物之非限定表單包含非離子抗菌劑,包含酚及雙酚化合物,例如經鹵化的二苯基醚,包含三氯沙(2,4,4’-三氯-2’-羥-二苯基醚)、三氯卡班(triclocarban)(3,4,4-三氯均二苯脲,3,4,4-trichlorocarbanilide),以及2-苯氧基乙醇、苄酸酯、及均二苯脲(carbanilide)。經鹵化的二苯基醚(例如三氯沙)可例如以用量0.3重量%的口腔用組成物存在。An additional active agent useful in the dentifrice composition of the present invention is an antibacterial agent which may be present in an amount of from 0.001 to 3.0% by weight of the oral composition. A non-limiting form of useful oral care compound comprising a nonionic antimicrobial comprising phenol and a bisphenol compound, such as a halogenated diphenyl ether, comprising triclosan (2,4,4'-trichloro-2'- Hydroxy-diphenyl ether), triclocarban (3,4,4-trichlorodiphenylurea, 3,4,4-trichlorocarbanilide), and 2-phenoxyethanol, benzyl ester, And carbanilide. The halogenated diphenyl ether (e.g., triclosan) can be present, for example, in an amount of 0.3% by weight of the oral composition.
適合表面活性劑為合理穩定遍佈寬廣pH範圍者。此等化合物為技藝中熟知,且包含非肥皂陰離子(如月桂基硫酸鈉(SLS)、N-肉荳蔻醯基及N-棕櫚醯基肌胺酸),非離子(如聚山梨糖醇酯(Polysorbate)20(聚氧乙烯20山梨醇酐單月桂酸酯,20)及聚山梨糖醇酯80(聚氧乙烯20山梨醇酐單油酸酯,80)、Poloxamer 407、從BASF Corporation可得之商品名F127),陽離子,兩性離子(如椰油醯胺基丙基甜菜鹼及月桂醯胺基丙基甜菜鹼),及兩性有機合成清潔劑。用於口腔用組成物之適合表面活性劑實例係討論於例如Nabi等人之美國專利案號4,894,220、Glandorf等人之美國專利案號6,555,094、及Lawlor等人之美國專利案號6,706,256。在各種具體實例中,一或多種表面活性劑係以範圍0.001%至5%或0.5%至2.5%存在於本發明口腔用組成物中。Suitable for surfactants that are reasonably stable throughout a wide pH range. Such compounds are well known in the art and include non-soap anions (such as sodium lauryl sulfate (SLS), N-myristyl and N-palmitoyl sarcosine), nonionics (such as polysorbates) Polysorbate) 20 (polyoxyethylene 20 sorbitan monolaurate, 20) and polysorbate 80 (polyoxyethylene 20 sorbitan monooleate, 80), Poloxamer 407, trade name available from BASF Corporation F127), cationic, zwitterionic (such as cocoamidopropyl betaine and laurylpropyl betaine), and amphoteric organic synthetic detergents. Examples of suitable surfactants for use in oral compositions are discussed, for example, in U.S. Patent No. 4,894,220 to Nabi et al., U.S. Patent No. 6,555,094 to Glandorf et al., and U.S. Patent No. 6,706,256 to Lawlor et al. In various embodiments, one or more surfactants are present in the oral compositions of the present invention in a range of from 0.001% to 5% or from 0.5% to 2.5%.
用於口腔用組成物之視情況增稠劑包含天然及合成膠及膠體,例如鹿角菜膠(愛爾蘭紅藻)、三仙膠、羧甲基纖維素鈉、澱粉、聚乙烯基吡咯酮、羥乙基丙基纖維素、羥丁基甲基纖維素、羥丙基甲基纖維素、及羥乙基纖維素。在各種具體實例中,增稠劑係以用量0.1至10重量%或0.5至4重量%存在於牙粉組成物中。As the case for oral compositions, thickeners include natural and synthetic gums and colloids, such as carrageenan (Irish red algae), sancaria, sodium carboxymethylcellulose, starch, polyvinylpyrrolidone, hydroxy Ethyl propyl cellulose, hydroxybutyl methyl cellulose, hydroxypropyl methyl cellulose, and hydroxyethyl cellulose. In various embodiments, the thickening agent is present in the dentifrice composition in an amount of from 0.1 to 10% by weight or from 0.5 to 4% by weight.
用於製備牙粉組成物之口腔可接受的牙粉載劑媒液(carrier vehicle)視情況包括保濕劑。保濕劑可為甘油、山梨醇、及木糖醇、分子量範圍為200至1,000之丙二醇;或其他保濕劑及其混合物。保濕劑濃度典型地合計為5至70重量%的口腔用組成物。水典型存在量為至少10重量%,且通常為25至70重量%的口腔用組成物。The orally acceptable carrier vehicle for the preparation of the dentifrice composition optionally comprises a humectant. The humectant can be glycerin, sorbitol, and xylitol, propylene glycol having a molecular weight in the range of 200 to 1,000; or other humectants and mixtures thereof. The humectant concentration typically amounts to 5 to 70% by weight of the oral composition. Water is typically present in an amount of at least 10% by weight, and typically from 25 to 70% by weight of the oral composition.
合成陰離子直線聚羧酸酯為功效增進劑,其視情況用於具有若干活性成分(包含抗菌劑、抗牙石劑或其他活性劑於口腔用組成物內)的口腔用組成物。該陰離子聚羧酸酯通常係呈其等自由酸、或部分或完全中和的水溶性鹼金屬(如鉀及較好為鈉)或銨鹽形式使用。術語「合成」及「直線」排除包括羧甲基纖維素及纖維素與天然膠的其他衍生物之已知增稠劑或膠化劑,也不是由於交聯而具有減少溶解度之卡波莫(carbopol)。Synthetic anionic linear polycarboxylates are efficacy enhancers which are optionally used in oral compositions having several active ingredients, including antibacterial agents, anticalculus agents or other active agents in the oral compositions. The anionic polycarboxylate is typically used in the form of its free acid or partially or fully neutralized water soluble alkali metal (e.g., potassium and preferably sodium) or ammonium salt. The terms "synthetic" and "straight line" exclude known thickeners or gelling agents including carboxymethylcellulose and other derivatives of cellulose and natural gum, nor are carbomers having reduced solubility due to cross-linking ( Carbopol).
較好共聚物為1:4至4:1順丁烯二酐或酸與另一可聚合乙烯系不飽和單體之共聚物,較好為具有分子量(M.W.)30,000至1,000,000之甲基乙烯基醚(甲氧基乙烯)。一種有用共聚物為甲基乙烯基醚/順丁烯二酐。此等共聚物實例從ISP Corporation以商品名GANTREZ可得。當存在時,陰離子聚羧酸酯係以有效達到任何抗菌劑、抗牙石劑或其他活性劑於牙粉組成物內之想要增強功效用量使用。在各種具體實例中,口腔用組成物中所含之合成陰離子聚羧酸酯係以0.001至5%或0.1至2.0%的口腔用組成物存在。Preferably, the copolymer is a copolymer of 1:4 to 4:1 maleic anhydride or an acid with another polymerizable ethylenically unsaturated monomer, preferably a methyl vinyl group having a molecular weight (MW) of 30,000 to 1,000,000. Ether (methoxyethylene). One useful copolymer is methyl vinyl ether/maleic anhydride. Examples of such copolymers from ISP Corporation under the trade name GANTREZ Available. When present, the anionic polycarboxylate is used in an amount effective to achieve the desired efficacy of any antimicrobial, anticalculus or other active agent in the dentifrice composition. In various embodiments, the synthetic anionic polycarboxylate contained in the oral composition is present in an amount of from 0.001 to 5% or from 0.1 to 2.0% of the oral composition.
製得本發明口腔用組成物可藉由技藝中已知之任何方法組合成分以製造口腔用護理組成物。可使用之方法實例係提出於如Martin等人之美國專利案號6,403,059;Clinical Pharmacology for Dental Professionals(Mosby-Year Book,Inc.,第3版1989);Mosby's Dental Hygiene:Concepts,Cases and Competencies(Daniel,S.及Harfst,S. eds.,Elsevier Science Health Science Div. 2002);及Ernest W. Flick,Cosmetic and Toiletry Formulations,第2版。The oral compositions of the present invention can be prepared by combining the ingredients by any of the methods known in the art to produce oral care compositions. Examples of methods that can be used are set forth in U.S. Patent No. 6,403,059 to Martin et al.; Clinical Pharmacology for Dental Professionals (Mosby-Year Book, Inc., 3rd edition 1989); Mosby's Dental Hygiene: Concepts, Cases and Competencies (Daniel) , S. and Harfst, S. eds., Elsevier Science Health Science Div. 2002); and Ernest W. Flick, Cosmetic and Toiletry Formulations, 2nd edition.
本發明提供一種使用本發明口腔用組成物以潔淨及/或磨光口腔表面之方法及過程。另外,口腔用組成物視情況治療及抑制口腔症狀,例如口腔炎性症狀、牙齒菌斑、及牙結石。口腔用組成物可以技藝中已知之任何適合方式塗敷於患者;例如藉由使用適合塗敷器或傳遞裝置,例如刷子、牙條、膜、注射器、線帶、藥丸、或技藝中已知之任何其他塗敷器或傳遞裝置,將口腔用組成物導入患者口腔。組成物可用於預防方法及過程以促進及維持口腔健康、外觀、維持全身健康等。口腔用組成物可根據特別治療計畫表重複地塗敷於患者超過數日,以治療及/或抑制污跡、齒菌斑、結石或牙石形成。提出治療計畫表之操作指南可提供產品於商業包裝,如商業製備及貯存者。The present invention provides a method and process for using the oral compositions of the present invention to clean and/or polish an oral surface. In addition, the oral composition treats and inhibits oral symptoms such as stomatological symptoms, dental plaque, and calculus as appropriate. The oral composition can be applied to the patient in any suitable manner known in the art; for example, by using a suitable applicator or delivery device, such as a brush, a strip, a film, a syringe, a tape, a pill, or any of the techniques known in the art. Other applicators or delivery devices introduce the oral composition into the patient's mouth. The composition can be used in prophylactic methods and procedures to promote and maintain oral health, appearance, overall health, and the like. The oral composition can be repeatedly applied to the patient for more than a few days according to a special treatment schedule to treat and/or inhibit the formation of stains, plaque, stones or tartar. An operational guide for a treatment plan can be provided for commercial packaging, such as commercial preparation and storage.
在不打算受理論束縛下,據信用於本發明口腔用組成物之二氧化矽磨料具有最初平均粒徑。當本發明口腔用組成物被用於刷淨軟組織時,如以移除齒菌斑或薄膜,二氧化矽磨料足夠從如牙齒表面移除該軟組織。從而,口腔用組成物最初具有高PCR。然而,當二氧化矽磨料顆粒對硬牙齒表面(如齒質或珐瑯質)接觸時,其等斷裂成更小顆粒;由此導致低RDA。因此,當本發明組成物用於治療口腔時,軟組織已被剝離,且防止硬組織免於磨損。據信當組成物用於口時,由於二氧化矽磨料尺寸減小,PCR及/或RDA可隨時間減少兩者數值。Without intending to be bound by theory, it is believed that the ceria abrasive used in the oral compositions of the present invention has an initial average particle size. When the oral composition of the present invention is used to brush soft tissue, such as to remove plaque or film, the cerium oxide abrasive is sufficient to remove the soft tissue from, for example, the tooth surface. Thus, the oral composition initially has high PCR. However, when the cerium oxide abrasive particles are in contact with a hard tooth surface such as a dentin or tannin, they break into smaller particles; thereby resulting in low RDA. Therefore, when the composition of the present invention is used for treating the oral cavity, the soft tissue has been peeled off and the hard tissue is prevented from being worn. It is believed that when the composition is applied to the mouth, PCR and/or RDA can reduce both values over time due to the reduced size of the cerium oxide abrasive.
起因於與硬表面接觸之所得破碎二氧化矽顆粒亦給予額外想不到的優勢;亦即磨光牙齒表面及/或阻塞牙齒小管(dental tubule)之能力,導致更乾淨牙齒及/或減少牙齒敏感性。因此,本發明組成物導致改良的潔淨、磨光、及減少牙齒敏感性。The resulting broken ceria particles resulting from contact with a hard surface also give an unexpected advantage; that is, the ability to polish the surface of the tooth and/or block the dental tubule, resulting in cleaner teeth and/or reduced tooth sensitivity. . Thus, the compositions of the present invention result in improved cleansing, polishing, and reduced tooth sensitivity.
本發明透過下列非限定實施例予以進一步說明。The invention is further illustrated by the following non-limiting examples.
二氧化矽A及二氧化矽B之特徵係如下決定。二氧化矽A為Grace VP5。二氧化矽B為來自J.M. Huber(Havre de Grace,Maryland,USA)之ZEODENT105。The characteristics of cerium oxide A and cerium oxide B are determined as follows. Ceria A is Grace VP5. Ceria B is ZEODENT from JM Huber (Havre de Grace, Maryland, USA) 105.
用於Einhleiner試驗之條件係使用黃銅網及100g二氧化矽於1000mL之120分鐘174000迴轉。吸油量及平均粒徑係藉由熟習技藝者已知之方法測量。測量係呈現於表1。The conditions used in the Einhleiner test were performed using a brass mesh and 100 g of cerium oxide at 1000 mL for 120 minutes and 174,000 revolutions. The oil absorption and average particle size are measured by methods known to those skilled in the art. The measurement system is presented in Table 1.
使用去離子水以二氧化矽A及B製備20%w/w漿液。最初漿液之粒徑分布係以Malvern 2000粒徑分析儀用Hydro 2000S小體積自動樣品分散單元決定。將漿液於測量前在水浴中以聲波振動處理1分鐘以破裂任何大黏聚物。使用平台縱橫交刷機,將20ml漿液添加於有側牆(sidewall)70°測量之鋁槽。使軟式方頭硬毛刷(頭尺寸大約長x寬為2.8cm x 1.0cm)架置以沿著整個鋁槽基座移動。添加重量於刷頭背部(250克)以於刷淨期間製造正向力。刷淨機器以速率為每分鐘100加倍行程運轉沿著鋁表面達總計300行程。刷淨後,使漿液從槽基底移除並以聲波振動處理1分鐘。樣品裝載入Malvern 2000粒徑分析儀。然後決定二氧化矽磨料粒徑,並呈現於表2。A 20% w/w slurry was prepared using deionized water with cerium oxide A and B. The particle size distribution of the initial slurry was determined using a Hydro 2000S small volume automated sample dispersion unit on a Malvern 2000 particle size analyzer. The slurry was sonicated in a water bath for 1 minute before the measurement to break any large cohesive polymer. Using a platform crossbar brush, add 20 ml of slurry to a sidewall 70° measurement Aluminum trough. A soft square head bristle brush (head size approximately length x width 2.8 cm x 1.0 cm) was placed to move along the entire aluminum trough base. The weight was added to the back of the brush head (250 grams) to create a positive force during brushing. The brushing machine runs at a rate of 100 doublings per minute along the aluminum surface for a total of 300 strokes. After brushing, the slurry was removed from the tank substrate and sonicated for 1 minute. The sample was loaded into a Malvern 2000 particle size analyzer. The cerium oxide abrasive particle size was then determined and presented in Table 2.
表2Table 2
令人驚訝地,結果指出二氧化矽A於刷淨攝生(brushing regimen)期間顯著破壞的能力,而二氧化矽B保持相對地未改變。Surprisingly, the results indicate the ability of cerium oxide A to significantly destroy during brushing regimen, while cerium oxide B remains relatively unchanged.
各種二氧化矽A漿液之PCR及RDA值係藉由本文先前敘述之方法決定。製備10%、15%、20%及30%w/w二氧化矽漿液,以及其等PCR及RDA值係藉由本文先前敘述之方法決定。結果呈現於表3。The PCR and RDA values of various cerium oxide A slurries are determined by the methods previously described herein. The 10%, 15%, 20%, and 30% w/w cerium oxide slurries were prepared, and their PCR and RDA values were determined by the methods previously described herein. The results are presented in Table 3.
根據表4製備牙粉組成物,如牙膏。A dentifrice composition such as a toothpaste was prepared according to Table 4.
對罹患牙齒敏感性之兩組30人給予牙膏MF-A或MF-B,並指示根據其等正常刷牙習慣使用組成物作為其等唯一牙粉一個月。一個月結束後,以MF-A刷牙之75%人報告減少牙齒敏感性,以及以MF-B刷牙之10%人報告減少牙齒敏感性。一個月結束後,以MF-A刷牙之3%人報告增加牙齒敏感性,以及以MF-B刷牙之15%人報告增加牙齒敏感性。The two groups of 30 people who were sensitive to teeth were given toothpaste MF-A or MF-B, and indicated that the composition was used as its sole tooth powder for one month according to its normal brushing habit. At the end of the month, 75% of people brushed with MF-A reported reduced tooth sensitivity, and 10% of people brushed with MF-B reported reduced tooth sensitivity. At the end of the month, 3% of people brushed with MF-A reported increased tooth sensitivity, and 15% of people brushed with MF-B reported increased tooth sensitivity.
對兩組50人給予牙膏WD-A或WD-B,並指示根據其等正常刷牙習慣使用組成物作為其等唯一牙粉一個月。以WD-A刷牙之80%人報告其等觀察到美白/磨光效果,而以WD-B刷牙之5%人報告其等觀察到美白/磨光效果。Tooth cream WD-A or WD-B was administered to 50 groups of 50 people, and the composition was used as its sole tooth powder for one month according to its normal brushing habit. 80% of people who brushed their teeth with WD-A reported that they observed a whitening/buffing effect, while 5% of those who brushed their teeth with WD-B reported that they observed a whitening/buffing effect.
對兩組15位吸煙者(平均每日1.4包)給予牙膏MF-A或MF-B,並指示根據其等正常刷牙習慣使用組成物作為其等唯一牙粉。一個月結束後,以MF-A刷牙之85%人察覺其等牙齒污跡減少,以及以MF-B刷牙之12%人察覺其等牙齒污跡減少。Tooth smokers MF-A or MF-B were given to 15 groups of 15 smokers (average 1.4 packs per day) and indicated that the composition was used as their sole tooth powder according to their normal brushing habits. At the end of the month, 85% of people brushed with MF-A noticed a decrease in their stains, and 12% of those brushed with MF-B noticed a decrease in their stains.
包括20%二氧化矽A及20%二氧化矽B的兩種組成物之RDA及PCR值係藉由本文先前敘述之方法決定。除不同二氧化矽磨料外,兩種組成物實質上相同。結果呈現於表5。The RDA and PCR values of the two compositions comprising 20% cerium oxide A and 20% cerium oxide B were determined by the methods previously described herein. The two compositions are substantially identical except for the different cerium oxide abrasives. The results are presented in Table 5.
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