JP6480458B2 - 口腔用組成物 - Google Patents
口腔用組成物 Download PDFInfo
- Publication number
- JP6480458B2 JP6480458B2 JP2016542014A JP2016542014A JP6480458B2 JP 6480458 B2 JP6480458 B2 JP 6480458B2 JP 2016542014 A JP2016542014 A JP 2016542014A JP 2016542014 A JP2016542014 A JP 2016542014A JP 6480458 B2 JP6480458 B2 JP 6480458B2
- Authority
- JP
- Japan
- Prior art keywords
- oral composition
- agent
- oral
- fluoride
- composition
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 239000000203 mixture Substances 0.000 title claims description 214
- 229920001577 copolymer Polymers 0.000 claims description 47
- 239000003795 chemical substances by application Substances 0.000 claims description 41
- 230000001680 brushing effect Effects 0.000 claims description 40
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 38
- -1 ethylene glycol esters alcohols Chemical class 0.000 claims description 35
- 210000000214 mouth Anatomy 0.000 claims description 28
- 239000013543 active substance Substances 0.000 claims description 27
- KRHYYFGTRYWZRS-UHFFFAOYSA-M Fluoride anion Chemical compound [F-] KRHYYFGTRYWZRS-UHFFFAOYSA-M 0.000 claims description 24
- 239000011248 coating agent Substances 0.000 claims description 24
- 238000000576 coating method Methods 0.000 claims description 24
- 230000007935 neutral effect Effects 0.000 claims description 22
- 239000007853 buffer solution Substances 0.000 claims description 21
- 239000006184 cosolvent Substances 0.000 claims description 18
- 239000000178 monomer Substances 0.000 claims description 18
- 239000000872 buffer Substances 0.000 claims description 16
- 239000002904 solvent Substances 0.000 claims description 16
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 15
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims description 14
- 239000000159 acid neutralizing agent Substances 0.000 claims description 14
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 12
- PUZPDOWCWNUUKD-UHFFFAOYSA-M sodium fluoride Chemical group [F-].[Na+] PUZPDOWCWNUUKD-UHFFFAOYSA-M 0.000 claims description 12
- 229910000389 calcium phosphate Inorganic materials 0.000 claims description 11
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical group CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims description 10
- 239000008363 phosphate buffer Substances 0.000 claims description 10
- NIXOWILDQLNWCW-UHFFFAOYSA-M Acrylate Chemical compound [O-]C(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-M 0.000 claims description 9
- 208000006558 Dental Calculus Diseases 0.000 claims description 9
- CERQOIWHTDAKMF-UHFFFAOYSA-M Methacrylate Chemical compound CC(=C)C([O-])=O CERQOIWHTDAKMF-UHFFFAOYSA-M 0.000 claims description 9
- 230000002882 anti-plaque Effects 0.000 claims description 8
- ZCCIPPOKBCJFDN-UHFFFAOYSA-N calcium nitrate Chemical compound [Ca+2].[O-][N+]([O-])=O.[O-][N+]([O-])=O ZCCIPPOKBCJFDN-UHFFFAOYSA-N 0.000 claims description 8
- 210000003296 saliva Anatomy 0.000 claims description 8
- BHHYHSUAOQUXJK-UHFFFAOYSA-L zinc fluoride Chemical compound F[Zn]F BHHYHSUAOQUXJK-UHFFFAOYSA-L 0.000 claims description 8
- 125000005233 alkylalcohol group Chemical group 0.000 claims description 7
- 229940090898 Desensitizer Drugs 0.000 claims description 6
- 229910019142 PO4 Inorganic materials 0.000 claims description 6
- 239000007864 aqueous solution Substances 0.000 claims description 6
- 239000001506 calcium phosphate Substances 0.000 claims description 6
- 229960001714 calcium phosphate Drugs 0.000 claims description 6
- 235000011010 calcium phosphates Nutrition 0.000 claims description 6
- 235000011187 glycerol Nutrition 0.000 claims description 6
- 239000011775 sodium fluoride Substances 0.000 claims description 6
- 235000013024 sodium fluoride Nutrition 0.000 claims description 6
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 claims description 6
- BVKZGUZCCUSVTD-UHFFFAOYSA-M Bicarbonate Chemical compound OC([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-M 0.000 claims description 5
- 239000000730 antalgic agent Substances 0.000 claims description 5
- 239000003242 anti bacterial agent Substances 0.000 claims description 5
- YYRMJZQKEFZXMX-UHFFFAOYSA-L calcium bis(dihydrogenphosphate) Chemical compound [Ca+2].OP(O)([O-])=O.OP(O)([O-])=O YYRMJZQKEFZXMX-UHFFFAOYSA-L 0.000 claims description 5
- 229940062672 calcium dihydrogen phosphate Drugs 0.000 claims description 5
- 239000003086 colorant Substances 0.000 claims description 5
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- 238000000034 method Methods 0.000 claims description 5
- 235000019691 monocalcium phosphate Nutrition 0.000 claims description 5
- 229920001223 polyethylene glycol Polymers 0.000 claims description 5
- UXVMQQNJUSDDNG-UHFFFAOYSA-L Calcium chloride Chemical compound [Cl-].[Cl-].[Ca+2] UXVMQQNJUSDDNG-UHFFFAOYSA-L 0.000 claims description 4
- BVKZGUZCCUSVTD-UHFFFAOYSA-L Carbonate Chemical compound [O-]C([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-L 0.000 claims description 4
- YCKRFDGAMUMZLT-UHFFFAOYSA-N Fluorine atom Chemical compound [F] YCKRFDGAMUMZLT-UHFFFAOYSA-N 0.000 claims description 4
- 239000002202 Polyethylene glycol Substances 0.000 claims description 4
- 230000003610 anti-gingivitis Effects 0.000 claims description 4
- 239000001110 calcium chloride Substances 0.000 claims description 4
- 229910001628 calcium chloride Inorganic materials 0.000 claims description 4
- WUKWITHWXAAZEY-UHFFFAOYSA-L calcium difluoride Chemical compound [F-].[F-].[Ca+2] WUKWITHWXAAZEY-UHFFFAOYSA-L 0.000 claims description 4
- 229910001634 calcium fluoride Inorganic materials 0.000 claims description 4
- FUFJGUQYACFECW-UHFFFAOYSA-L calcium hydrogenphosphate Chemical compound [Ca+2].OP([O-])([O-])=O FUFJGUQYACFECW-UHFFFAOYSA-L 0.000 claims description 4
- 150000007942 carboxylates Chemical class 0.000 claims description 4
- 229940124447 delivery agent Drugs 0.000 claims description 4
- 235000019700 dicalcium phosphate Nutrition 0.000 claims description 4
- 239000011737 fluorine Substances 0.000 claims description 4
- 229910052731 fluorine Inorganic materials 0.000 claims description 4
- 235000013355 food flavoring agent Nutrition 0.000 claims description 4
- 239000003193 general anesthetic agent Substances 0.000 claims description 4
- 230000000395 remineralizing effect Effects 0.000 claims description 4
- FVRNDBHWWSPNOM-UHFFFAOYSA-L strontium fluoride Chemical compound [F-].[F-].[Sr+2] FVRNDBHWWSPNOM-UHFFFAOYSA-L 0.000 claims description 4
- 229910001637 strontium fluoride Inorganic materials 0.000 claims description 4
- 238000013268 sustained release Methods 0.000 claims description 4
- 239000012730 sustained-release form Substances 0.000 claims description 4
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 claims description 3
- NBIIXXVUZAFLBC-UHFFFAOYSA-L Phosphate ion(2-) Chemical compound OP([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-L 0.000 claims description 3
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims description 3
- 239000012190 activator Substances 0.000 claims description 3
- 239000004075 cariostatic agent Substances 0.000 claims description 3
- NBIIXXVUZAFLBC-UHFFFAOYSA-M dihydrogenphosphate Chemical compound OP(O)([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-M 0.000 claims description 3
- 150000002222 fluorine compounds Chemical group 0.000 claims description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-M hydroxide Chemical compound [OH-] XLYOFNOQVPJJNP-UHFFFAOYSA-M 0.000 claims description 3
- 239000010452 phosphate Substances 0.000 claims description 3
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims description 3
- 210000005239 tubule Anatomy 0.000 claims description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 claims description 2
- 239000007884 disintegrant Substances 0.000 claims description 2
- 159000000007 calcium salts Chemical group 0.000 claims 1
- 125000005587 carbonate group Chemical group 0.000 claims 1
- 239000012528 membrane Substances 0.000 description 31
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 18
- 239000002253 acid Substances 0.000 description 15
- 239000008199 coating composition Substances 0.000 description 12
- 239000000463 material Substances 0.000 description 12
- LYCAIKOWRPUZTN-UHFFFAOYSA-N ethylene glycol Natural products OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 11
- 150000003839 salts Chemical group 0.000 description 10
- MHAJPDPJQMAIIY-UHFFFAOYSA-N Hydrogen peroxide Chemical compound OO MHAJPDPJQMAIIY-UHFFFAOYSA-N 0.000 description 9
- 210000001519 tissue Anatomy 0.000 description 9
- 239000000243 solution Substances 0.000 description 7
- 238000012360 testing method Methods 0.000 description 7
- 238000005299 abrasion Methods 0.000 description 6
- 210000003298 dental enamel Anatomy 0.000 description 6
- 238000007711 solidification Methods 0.000 description 6
- 230000008023 solidification Effects 0.000 description 6
- JKNCOURZONDCGV-UHFFFAOYSA-N 2-(dimethylamino)ethyl 2-methylprop-2-enoate Chemical compound CN(C)CCOC(=O)C(C)=C JKNCOURZONDCGV-UHFFFAOYSA-N 0.000 description 5
- 239000000120 Artificial Saliva Substances 0.000 description 5
- 206010006326 Breath odour Diseases 0.000 description 5
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 5
- 125000000217 alkyl group Chemical group 0.000 description 5
- 150000002978 peroxides Chemical class 0.000 description 5
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- 239000004033 plastic Substances 0.000 description 5
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- 230000002087 whitening effect Effects 0.000 description 5
- ATRRKUHOCOJYRX-UHFFFAOYSA-N Ammonium bicarbonate Chemical compound [NH4+].OC([O-])=O ATRRKUHOCOJYRX-UHFFFAOYSA-N 0.000 description 4
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 4
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- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 description 4
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 4
- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical group [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 description 4
- 239000003513 alkali Substances 0.000 description 4
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- 150000001450 anions Chemical class 0.000 description 4
- 230000000052 comparative effect Effects 0.000 description 4
- 230000003628 erosive effect Effects 0.000 description 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 description 4
- WQYVRQLZKVEZGA-UHFFFAOYSA-N hypochlorite Chemical compound Cl[O-] WQYVRQLZKVEZGA-UHFFFAOYSA-N 0.000 description 4
- CGIGDMFJXJATDK-UHFFFAOYSA-N indomethacin Chemical compound CC1=C(CC(O)=O)C2=CC(OC)=CC=C2N1C(=O)C1=CC=C(Cl)C=C1 CGIGDMFJXJATDK-UHFFFAOYSA-N 0.000 description 4
- 229910052749 magnesium Inorganic materials 0.000 description 4
- 239000011777 magnesium Substances 0.000 description 4
- 230000003239 periodontal effect Effects 0.000 description 4
- 235000007686 potassium Nutrition 0.000 description 4
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- 239000011591 potassium Substances 0.000 description 4
- 229960003975 potassium Drugs 0.000 description 4
- BWHMMNNQKKPAPP-UHFFFAOYSA-L potassium carbonate Chemical compound [K+].[K+].[O-]C([O-])=O BWHMMNNQKKPAPP-UHFFFAOYSA-L 0.000 description 4
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- 239000000126 substance Substances 0.000 description 4
- LWIHDJKSTIGBAC-UHFFFAOYSA-K tripotassium phosphate Chemical compound [K+].[K+].[K+].[O-]P([O-])([O-])=O LWIHDJKSTIGBAC-UHFFFAOYSA-K 0.000 description 4
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 3
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- NEDGUIRITORSKL-UHFFFAOYSA-N butyl 2-methylprop-2-enoate;2-(dimethylamino)ethyl 2-methylprop-2-enoate;methyl 2-methylprop-2-enoate Chemical compound COC(=O)C(C)=C.CCCCOC(=O)C(C)=C.CN(C)CCOC(=O)C(C)=C NEDGUIRITORSKL-UHFFFAOYSA-N 0.000 description 3
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- MBMBGCFOFBJSGT-KUBAVDMBSA-N all-cis-docosa-4,7,10,13,16,19-hexaenoic acid Chemical compound CC\C=C/C\C=C/C\C=C/C\C=C/C\C=C/C\C=C/CCC(O)=O MBMBGCFOFBJSGT-KUBAVDMBSA-N 0.000 description 2
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- 235000019157 thiamine Nutrition 0.000 description 1
- 229960003495 thiamine Drugs 0.000 description 1
- 239000011721 thiamine Substances 0.000 description 1
- KYMBYSLLVAOCFI-UHFFFAOYSA-N thiamine Chemical compound CC1=C(CCO)SCN1CC1=CN=C(C)N=C1N KYMBYSLLVAOCFI-UHFFFAOYSA-N 0.000 description 1
- 229960002898 threonine Drugs 0.000 description 1
- 229960000790 thymol Drugs 0.000 description 1
- 239000011135 tin Substances 0.000 description 1
- 239000004408 titanium dioxide Substances 0.000 description 1
- 229960001017 tolmetin Drugs 0.000 description 1
- UPSPUYADGBWSHF-UHFFFAOYSA-N tolmetin Chemical compound C1=CC(C)=CC=C1C(=O)C1=CC=C(CC(O)=O)N1C UPSPUYADGBWSHF-UHFFFAOYSA-N 0.000 description 1
- 230000036347 tooth sensitivity Effects 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- YWYZEGXAUVWDED-UHFFFAOYSA-N triammonium citrate Chemical compound [NH4+].[NH4+].[NH4+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O YWYZEGXAUVWDED-UHFFFAOYSA-N 0.000 description 1
- 229940001496 tribasic sodium phosphate Drugs 0.000 description 1
- 235000013337 tricalcium citrate Nutrition 0.000 description 1
- 229960003500 triclosan Drugs 0.000 description 1
- UNXRWKVEANCORM-UHFFFAOYSA-I triphosphate(5-) Chemical compound [O-]P([O-])(=O)OP([O-])(=O)OP([O-])([O-])=O UNXRWKVEANCORM-UHFFFAOYSA-I 0.000 description 1
- 150000004788 tropolones Chemical class 0.000 description 1
- 239000004034 viscosity adjusting agent Substances 0.000 description 1
- 235000019155 vitamin A Nutrition 0.000 description 1
- 239000011719 vitamin A Substances 0.000 description 1
- 235000019154 vitamin C Nutrition 0.000 description 1
- 239000011718 vitamin C Substances 0.000 description 1
- 235000019166 vitamin D Nutrition 0.000 description 1
- 239000011710 vitamin D Substances 0.000 description 1
- 235000019165 vitamin E Nutrition 0.000 description 1
- 229940046009 vitamin E Drugs 0.000 description 1
- 239000011709 vitamin E Substances 0.000 description 1
- 229940045997 vitamin a Drugs 0.000 description 1
- 229940011671 vitamin b6 Drugs 0.000 description 1
- 239000001717 vitis vinifera seed extract Substances 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
- 150000003751 zinc Chemical class 0.000 description 1
- 239000011670 zinc gluconate Substances 0.000 description 1
- 235000011478 zinc gluconate Nutrition 0.000 description 1
- 229960000306 zinc gluconate Drugs 0.000 description 1
- 229940071566 zinc glycinate Drugs 0.000 description 1
- NWONKYPBYAMBJT-UHFFFAOYSA-L zinc sulfate Chemical compound [Zn+2].[O-]S([O-])(=O)=O NWONKYPBYAMBJT-UHFFFAOYSA-L 0.000 description 1
- 229960001763 zinc sulfate Drugs 0.000 description 1
- 229910000368 zinc sulfate Inorganic materials 0.000 description 1
- UOXSXMSTSYWNMH-UHFFFAOYSA-L zinc;2-aminoacetate Chemical compound [Zn+2].NCC([O-])=O.NCC([O-])=O UOXSXMSTSYWNMH-UHFFFAOYSA-L 0.000 description 1
- QPQOIFMSSWHRJQ-UHFFFAOYSA-L zinc;dichlorite Chemical compound [Zn+2].[O-]Cl=O.[O-]Cl=O QPQOIFMSSWHRJQ-UHFFFAOYSA-L 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/34—Alcohols
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
- A61K8/81—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions involving only carbon-to-carbon unsaturated bonds
- A61K8/8141—Compositions of homopolymers or copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and at least one being terminated by only one carboxyl radical, or of salts, anhydrides, esters, amides, imides or nitriles thereof; Compositions of derivatives of such polymers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
- A61K8/81—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions involving only carbon-to-carbon unsaturated bonds
- A61K8/8141—Compositions of homopolymers or copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and at least one being terminated by only one carboxyl radical, or of salts, anhydrides, esters, amides, imides or nitriles thereof; Compositions of derivatives of such polymers
- A61K8/8152—Homopolymers or copolymers of esters, e.g. (meth)acrylic acid esters; Compositions of derivatives of such polymers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
- A61K2800/42—Colour properties
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
- A61K2800/52—Stabilizers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
- A61K2800/54—Polymers characterized by specific structures/properties
- A61K2800/542—Polymers characterized by specific structures/properties characterized by the charge
- A61K2800/5426—Polymers characterized by specific structures/properties characterized by the charge cationic
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/80—Process related aspects concerning the preparation of the cosmetic composition or the storage or application thereof
- A61K2800/92—Oral administration
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Birds (AREA)
- Epidemiology (AREA)
- Oral & Maxillofacial Surgery (AREA)
- Emergency Medicine (AREA)
- Cosmetics (AREA)
- Medicinal Preparation (AREA)
Description
(I)、
式中、R1及びR2は、水素原子、アルキル基、C(O)R3及びSO2R4から独立して選択され、R3及びR4は、アルキル基、アリール基及びアラルキル基から独立して選択され、nは、2〜5の整数である。いくつかの実施形態では、薬剤として許容される塩は、非置換又は置換トロポロンを含まない。いくつかの実施形態では、R1及びR2は水素原子を含み、又は、水素原子及びアルキル基から独立して選択される。特定の実施態様において、R1又はR2はそれぞれ独立して、約1〜約10の炭素原子のアルキル基を含む。他の実施態様において、R1は水素原子を含み、及びR2はC(O)R3又はSO2R4を含む。通常、R3は、約1〜約26の炭素原子、より一般的には約6〜約16の炭素原子を有するアルキル基を含む。有用な抗歯垢剤を更に示したリストは、米国特許出願及び公開第US2013/0052146号に詳述されており、それは参照により本明細書に組み込まれる。
実施形態1は、
水を含む溶媒、並びに、低級アルキルアルコール及びアセトンから選択される共溶媒と、
塩基性アクリレートモノマー単位、塩基性メタクリレートモノマー単位又はこれらの組み合わせを含む塩基性コポリマーと、
0.5重量%以上の酸緩衝又は中和剤と、
任意に活性剤と、を含む口腔用組成物であって、
前記口腔用組成物が、約6〜約15重量%の水、約30〜約80重量%の共溶媒、及び約25〜約55重量%の塩基性コポリマーを含み、
前記塩基性コポリマーが前記口腔用組成物に溶解しており、
前記口腔用組成物が、水溶液と接触したとき、表面に膜を形成することができ、
各成分の重量%が前記組成物の総重量を基準としている。
ポリマー溶液が、キャップ付き250mlジャーに指定された量の溶媒を最初に量ることにより、調製された。ポリマー材料の指定された量が、次いでジャーに加えられた。ジャーは密閉されて、それからポリマーが溶媒に完全に溶解するまで、2〜3日間のWheaton Culture Rollerに置かれた(〜30rpm)。3000rpmに設定されたスピードミキサ(FlacTek,Inc.(Landrum、SC)から入手可能なSpeedMixer DAC 150.1 FVZ)に2回2分サイクルを使用して、NaF、他の塩、粘度調整剤、香味料などの追加成分がポリマー溶液に、加えられた。各コーティング組成物で使用する材料及び量(グラム)は、下記の実施例並びに表に示される。
人工唾液は、次の手順で調製された。胃ムチン3.52g、NaCl 0.610g、CaCl2.2H2O 0.341g、KH2PO4 1.183g及びKCL 1.179gが、計量されて2000mlフラスコに入れられた。脱イオン(DI)水1600mlが電磁攪拌棒を用いてゆっくりと添加されて、すべての固形分が溶解されるまで、溶液に混合された。pHは、50% NaOH溶液を使用して、7.0に調製された。
コーティング評価−感触、固化、粘着力及び耐摩耗性試験
本発明の組成物及び比較組成物が、綿棒又は小さなブラシを使用して、ガラス(又は言及があればプラスチック)スライド(VWR(Radnor PA)から入手可能)又はウシの歯上にコーティングされた。コーティング基材はそれから、室温(〜25℃)で30秒間、水道水の容器に浸漬された。コーティングが定性的に評価されて、膜が形成された(「固化」)が測定された。更に、固化した膜は、基材へのこれらの粘着力で評価された。固化した膜を指圧で押しのけることができないとき、粘着力は「良好」とみなされ、固化した膜を指圧で押しのけることができるとき、「なし」とみなされる。固化したコーティングを歯ブラシでブラッシングして、コーティングを除去するのに必要なブラシストローク数を数えることによって、耐摩耗性が評価された。
コーティング組成物約40〜50mgが、1インチ×1インチ(2.54cm×2.54cm)のプラスチックスライド(VRW(Radnor、PA)から入手可能なRinzylプラスチックマイクロスライド)上に均一に塗られた。コーティングされたスライドは、プラスチック試験管の脱イオン水25mlに1時間浸漬された。1時間後に、スライドは取り出されて、すすがれて、別の試験管の水の第2の25mlアリコートに浸漬された。3時間(全体で4時間)後、前記工程が繰り返されて、スライドは水の第3の25mlのアリコートに浸漬された。2時間(全体で6時間)後、前記工程が再び繰り返されて、スライドは水の第4の25mlのアリコートに置かれて、スライドが取り出される前まで更に18時間(全体で24時間)そのままの状態だった。脱イオン水の25mlの各アリコートが、フッ化物濃度について評価された。上記の調製からの試料溶液10mlは、10mlのTISAB IIと混合されて、フッ化物濃度測定用の溶液を作製した。TISAB IIで緩衝された標準濃度のフッ化物を使用して標準化されたフッ化物複合電極を備えているCole Parmerフッ化物イオンメータを使用して、フッ化物濃度が測定された。5つの複製試料が実施されて、平均値を得た。フッ化物濃度はppmで測定され、及びフッ化物放出は、以下の方程式を使用するμgF/cm2コーティングとして報告された。
ウシの歯が、ポリ(メチル)メタクリレート(PMMA)樹脂の瓶に入れられ、それから320グリットの研磨紙で研磨されて、エナメル表面を露出させた。露出したエナメルは紙タオルで拭かれて、過剰な水を取り除かれ、それから材料約10mgでコーティングして、エナメルに薄層を形成する。次いで種々の時間で37℃人工唾液に保存される。歯ブラシ機(Foth Production Solution、LLC(Greenbay WI)から入手可能)が、エナメル上のコーティング耐久性試験に使用された。歯ブラシヘッドは、Henry Schein製の商標名Accleanジェントルケアの歯ブラシから切り取られて、歯ブラシ機の固定具に差し込まれた。瓶に入れたウシの歯が挿入されて、ブラシ媒体が充填されたプラスチックポートに取り付けられた。歯ブラシヘッドが、前記コーティング表面で静止していた。機械が、エナメルのコーティングに対して前後に移動する歯ブラシヘッドを制御できる。ブラッシングのストロークは、前記表面を前後にブラッシングすることで1回と定義される。水:練り歯磨き(CREST虫歯予防練り歯磨き)1:1混合物5mlが、ブラシ媒体として用いられた。一定のブラッシングのストローク後、前記コーティング表面が確認されて、摩耗の量が評価された。
コーティング溶液のpHは、pH紙を使用して測定された。
下表1で概説される材料及び量(グラム)を使用して、口腔用(コーティング)組成物が、上述のとおり調製されて、コーティングされた。コーティング膜は、上述のとおり固化、粘着力及びフッ化物放出について評価された。
下表2で概説される材料及び量(グラム)を使用して、コーティング組成物が、上述のとおり調製されて、コーティングされた。コーティング膜は、上述のとおり固化、粘着力及びフッ化物放出について評価された。
下表3で概説される材料及び量(グラム)を使用して、コーティング組成物が、上述のとおり調製されて、コーティングされた。コーティング組成物のpHは上述のとおり測定されて、及びコーティング膜は固化及び粘着力について評価された。
下表4で概説される材料及び量(グラム)を使用して、コーティング組成物が、上述のとおり調製されて、コーティングされた。コーティング膜は、上述のとおり固化、粘着力及びフッ化物放出について評価された。
実施例6及び実施例7のコーティング組成物のウシの歯上の耐摩耗性は、上述のとおり測定された。コーティングされた歯の3つの複製試料が、3時間又は24時間37℃度の人工唾液に浸漬されて、それからブラッシングされた。ブラッシングの特定のストローク後、除去されたコーティングの量が、下表5で報告される。
[1]
水を含む溶媒、並びに低級アルキルアルコール及びアセトンから選択される共溶媒と、
塩基性アクリレートモノマー単位、塩基性メタクリレートモノマー単位又はこれらの組み合わせを含む塩基性コポリマーと、
0.5重量%以上の酸緩衝又は中和剤と、
任意に活性剤と、を含む口腔用組成物であって、
前記口腔用組成物が、約6〜約15重量%の水、約30〜約80重量%の共溶媒、及び約25〜約55重量%の塩基性コポリマーを含み、
前記塩基性コポリマーが前記口腔用組成物に溶解しており、
前記口腔用組成物が、水溶液と接触したとき、表面に膜を形成することができ、
各成分の重量%が前記組成物の総重量を基準としている、口腔用組成物。
[2]
前記口腔用組成物が、中性アクリレートモノマー単位、中性メタクリレートモノマー単位、又はこれらの組み合わせを含む中性コポリマーを更に含む、項目1に記載の口腔用組成物。
[3]
前記口腔用組成物が約0〜約40重量%の前記中性コポリマーを含む、項目1又は2に記載の口腔用組成物。
[4]
前記中性コポリマーがEudragit RS100及びEudragit RL100から選択される、項目1〜3のいずれか一項に記載の口腔用組成物。
[5]
前記塩基性コポリマーが、Eudragit E100及びイオン架橋のためのジメチルアミノエチルメタクリレートを含有する他のコポリマーから選択される、項目1〜4のいずれか一項に記載の口腔用組成物。
[6]
前記塩基性コポリマーの分子量が約10,000〜約100,000である、項目1〜5のいずれか一項に記載の口腔用組成物。
[7]
前記口腔用組成物が水と接触した後約30秒未満で、前記口腔用組成物が前記膜を形成することができる、項目1〜6のいずれか一項に記載の口腔用組成物。
[8]
前記口腔用組成物の稠度が約45〜約110である、項目1〜7のいずれか一項に記載の口腔用組成物。
[9]
前記共溶媒がエタノールである、項目1〜8のいずれか一項に記載の口腔用組成物。
[10]
前記溶媒が、イソプロパノール、プロピレングリコール、グリセリン、低分子量のポリエチレングリコール、エチレングリコール系エステルアルコール及びこれらの組み合わせから選択される少なくとも1つの追加の成分を更に含む、項目1〜9のいずれか一項に記載の口腔用組成物。
[11]
前記口腔用組成物が約8〜約12重量%の前記水を含む、項目1〜10のいずれか一項に記載の口腔用組成物。
[12]
前記口腔用組成物が約35〜60重量%の前記共溶媒を含む、項目1〜11のいずれか一項に記載の口腔用組成物。
[13]
前記酸緩衝又は中和剤が、炭酸塩、重炭酸塩、塩化物、水酸化物、二塩基クエン酸塩、リン酸塩、硫酸塩、及びこれらの組み合わせから選択される、項目1〜12のいずれか一項に記載の口腔用組成物。
[14]
前記酸緩衝又は中和剤が、リン酸塩系緩衝剤、リン酸水素塩系緩衝剤、リン酸二水素塩系緩衝剤、カルボン酸塩系緩衝剤、炭酸塩系緩衝剤、炭酸水素塩緩衝剤、及びこれらの組み合わせから選択される、項目1〜13のいずれか一項に記載の口腔用組成物。
[15]
前記活性剤が、増白剤、抗う蝕剤、フッ素送達剤、抗歯肉炎剤、歯石制御剤、抗歯垢剤、歯周活性物質、口臭清涼剤、臭気制御剤、歯の減感剤、唾液刺激剤、香味料、バイオフィルム崩壊剤、抗菌剤、麻酔剤、鎮痛剤、着色除去剤、着色剤、再石灰化剤、歯石軟化剤、及びこれらの組み合わせから選択される、項目1〜14のいずれか一項に記載の口腔用組成物。
[16]
前記活性剤がフッ化物組成物である、項目1〜15のいずれか一項に記載の口腔用組成物。
[17]
前記活性剤が少なくとも24時間にわたる徐放性のフッ化物放出を提供する、項目1〜16のいずれか一項に記載の口腔用組成物。
[18]
前記活性剤が少なくとも2つの異なるフッ化物塩を含む、項目1〜17のいずれか一項に記載の口腔用組成物。
[19]
前記活性剤が、フッ化ナトリウム、フッ化ストロンチウム、フッ化カルシウム、フッ化亜鉛、塩化カルシウム、硝酸カルシウム、リン酸カルシウム、リン酸水素カルシウム、リン酸二水素カルシウム、及びこれらの組み合わせから選択される、項目1〜18のいずれか一項に記載の口腔用組成物。
[20]
前記膜が、少なくとも5ストローク前記表面をブラッシングした後、前記表面の少なくとも90%に残留する、項目1〜19のいずれか一項に記載の口腔用組成物。
[21]
前記膜が、少なくとも10ストローク前記表面をブラッシングした後、前記表面の少なくとも90%に残留する、項目1〜20のいずれか一項に記載の口腔用組成物。
[22]
前記膜が、少なくとも20ストローク前記表面をブラッシングした後、前記表面の少なくとも90%に残留する、項目1〜21のいずれか一項に記載の口腔用組成物。
[23]
前記膜が、少なくとも30ストローク前記表面をブラッシングした後、前記表面の少なくとも90%に残留する、項目1〜22のいずれか一項に記載の口腔用組成物。
[24]
前記膜が、少なくとも60ストローク前記表面をブラッシングした後、前記表面の少なくとも90%に残留する、項目1〜23のいずれか一項に記載の口腔用組成物。
[25]
前記膜が、少なくとも90ストローク前記表面をブラッシングした後、前記表面の少なくとも90%に残留する、項目1〜24のいずれか一項に記載の口腔用組成物。
[26]
前記膜が、少なくとも120ストローク前記表面をブラッシングした後、前記表面の少なくとも90%に残留する、項目1〜25のいずれか一項に記載の口腔用組成物。
[27]
前記膜が、5〜120ストローク前記表面をブラッシングした後、前記表面の少なくとも90%に残留する、項目1〜26のいずれか一項に記載の口腔用組成物。
[28]
前記膜が、10〜90ストローク前記表面をブラッシングした後、前記表面の少なくとも90%に残留する、項目1〜27のいずれか一項に記載の口腔用組成物。
[29]
前記膜が、20〜60ストローク前記表面をブラッシングした後、前記表面の少なくとも90%に残留する、項目1〜28のいずれか一項に記載の口腔用組成物。
[30]
前記膜が、5〜120ストローク前記表面をブラッシングした後、前記表面の少なくとも90%に残留する、項目1〜29のいずれか一項に記載の口腔用組成物。
Claims (14)
- 水を含む溶媒、並びに低級アルキルアルコール及びアセトンから選択される共溶媒と、
塩基性アクリレートモノマー単位、塩基性メタクリレートモノマー単位又はこれらの組み合わせを含む塩基性コポリマーと、
0.5重量%以上の酸緩衝又は中和剤と、を含む口腔用組成物であって、
前記口腔用組成物が、6〜15重量%の水、30〜80重量%の共溶媒、及び25〜55重量%の塩基性コポリマーを含み、
前記塩基性コポリマーが前記口腔用組成物に溶解しており、
前記口腔用組成物が、水溶液と接触したとき、表面に膜を形成することができ、
各成分の重量%が前記口腔用組成物の総重量を基準としている、口腔用組成物。 - 前記口腔用組成物が、中性アクリレートモノマー単位、中性メタクリレートモノマー単位、又はこれらの組み合わせを含む中性コポリマーを更に含む、請求項1に記載の口腔用組成物。
- 前記口腔用組成物が0〜40重量%の前記中性コポリマーを含む、請求項2に記載の口腔用組成物。
- 前記口腔用組成物が水と接触した後30秒未満で、前記口腔用組成物が前記膜を形成することができる、請求項1〜3のいずれか一項に記載の口腔用組成物。
- 前記溶媒が、イソプロパノール、プロピレングリコール、グリセリン、低分子量のポリエチレングリコール、エチレングリコール系エステルアルコール及びこれらの組み合わせから選択される少なくとも1つの追加の成分を更に含む、請求項1〜4のいずれか一項に記載の口腔用組成物。
- 前記口腔用組成物が8〜12重量%の前記水を含み、前記口腔用組成物が35〜60重量%の前記共溶媒を含む、請求項1〜5のいずれか一項に記載の口腔用組成物。
- 前記酸緩衝又は中和剤が、炭酸塩、重炭酸塩、塩化物、水酸化物、二塩基クエン酸塩、リン酸塩、硫酸塩、及びこれらの組み合わせから選択され、前記酸緩衝又は中和剤が、リン酸塩系緩衝剤、リン酸水素塩系緩衝剤、リン酸二水素塩系緩衝剤、カルボン酸塩系緩衝剤、炭酸塩系緩衝剤、炭酸水素塩緩衝剤、及びこれらの組み合わせから選択される、請求項1〜6のいずれか一項に記載の口腔用組成物。
- 前記口腔用組成物が活性剤をさらに含み、前記活性剤が、増白剤、抗う蝕剤、フッ素送達剤、抗歯肉炎剤、歯石制御剤、抗歯垢剤、口臭清涼剤、臭気制御剤、歯の減感剤、唾液刺激剤、香味料、バイオフィルム崩壊剤、抗菌剤、麻酔剤、鎮痛剤、着色除去剤、着色剤、再石灰化剤、歯石軟化剤、及びこれらの組み合わせから選択される、請求項1〜7のいずれか一項に記載の口腔用組成物。
- 前記活性剤がフッ化物組成物である、請求項8に記載の口腔用組成物。
- 前記活性剤が少なくとも24時間にわたる徐放性のフッ化物放出を提供する、請求項9に記載の口腔用組成物。
- 前記活性剤が、フッ化ナトリウム、フッ化ストロンチウム、フッ化カルシウム、フッ化亜鉛、塩化カルシウム、硝酸カルシウム、リン酸カルシウム、リン酸水素カルシウム、リン酸二水素カルシウム、及びこれらの組み合わせから選択される、請求項8〜10のいずれか一項に記載の口腔用組成物。
- 前記膜が、少なくとも5ストローク前記表面をブラッシングした後、前記表面の少なくとも90%に残留する、請求項1〜11のいずれか一項に記載の口腔用組成物。
- 前記酸緩衝又は中和剤がカルシウム塩である、請求項1〜12のいずれか一項に記載の口腔用組成物。
- 請求項1〜13のいずれか一項に記載の口腔用組成物を使用して開いた象牙質細管上にコーティングを形成することを含む、開いた象牙質細管をふさぐ方法。
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US61/876,441 | 2013-09-11 | ||
PCT/US2014/054074 WO2015038400A1 (en) | 2013-09-11 | 2014-09-04 | Oral compositions |
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2014
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CN105530998A (zh) | 2016-04-27 |
RU2646501C2 (ru) | 2018-03-05 |
US20200022896A1 (en) | 2020-01-23 |
US10772821B2 (en) | 2020-09-15 |
US20160220472A1 (en) | 2016-08-04 |
WO2015038400A1 (en) | 2015-03-19 |
JP2016530309A (ja) | 2016-09-29 |
RU2016110110A (ru) | 2017-10-16 |
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