MXPA02005771A - Oral care ultramulsion based products. - Google Patents
Oral care ultramulsion based products.Info
- Publication number
- MXPA02005771A MXPA02005771A MXPA02005771A MX9705771A MXPA02005771A MX PA02005771 A MXPA02005771 A MX PA02005771A MX PA02005771 A MXPA02005771 A MX PA02005771A MX 9705771 A MX9705771 A MX 9705771A MX PA02005771 A MXPA02005771 A MX PA02005771A
- Authority
- MX
- Mexico
- Prior art keywords
- surfactant
- ultramulsion
- polydimethylsiloxane
- dispersion
- silicone
- Prior art date
Links
- 239000006185 dispersion Substances 0.000 claims abstract description 122
- 229920001296 polysiloxane Polymers 0.000 claims abstract description 87
- 239000004094 surface-active agent Substances 0.000 claims abstract description 76
- 238000000576 coating method Methods 0.000 claims abstract description 21
- 239000000126 substance Substances 0.000 claims abstract description 18
- 239000000839 emulsion Substances 0.000 claims abstract description 17
- 239000011248 coating agent Substances 0.000 claims abstract description 14
- 239000000606 toothpaste Substances 0.000 claims abstract description 14
- 239000004530 micro-emulsion Substances 0.000 claims abstract description 11
- 239000006184 cosolvent Substances 0.000 claims abstract description 5
- 230000003610 anti-gingivitis Effects 0.000 claims abstract 2
- -1 polydimethylsiloxane Polymers 0.000 claims description 96
- 239000000203 mixture Substances 0.000 claims description 84
- 229920000435 poly(dimethylsiloxane) Polymers 0.000 claims description 61
- 239000004205 dimethyl polysiloxane Substances 0.000 claims description 48
- 239000002245 particle Substances 0.000 claims description 44
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 37
- 210000000214 mouth Anatomy 0.000 claims description 26
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 claims description 21
- 239000007788 liquid Substances 0.000 claims description 17
- 239000004615 ingredient Substances 0.000 claims description 14
- 239000002736 nonionic surfactant Substances 0.000 claims description 14
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical class [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 claims description 12
- 238000000034 method Methods 0.000 claims description 12
- 210000003800 pharynx Anatomy 0.000 claims description 12
- 229920001983 poloxamer Polymers 0.000 claims description 11
- 210000003238 esophagus Anatomy 0.000 claims description 10
- 150000002632 lipids Chemical class 0.000 claims description 10
- 229960000502 poloxamer Drugs 0.000 claims description 9
- 210000002784 stomach Anatomy 0.000 claims description 9
- 229940069428 antacid Drugs 0.000 claims description 7
- 239000003159 antacid agent Substances 0.000 claims description 7
- 230000001458 anti-acid effect Effects 0.000 claims description 6
- 229920001400 block copolymer Polymers 0.000 claims description 6
- 210000000936 intestine Anatomy 0.000 claims description 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 6
- 239000006072 paste Substances 0.000 claims description 6
- 239000004480 active ingredient Substances 0.000 claims description 5
- 230000000694 effects Effects 0.000 claims description 5
- 235000020357 syrup Nutrition 0.000 claims description 5
- 239000006188 syrup Substances 0.000 claims description 5
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 4
- 238000010438 heat treatment Methods 0.000 claims description 4
- 238000002156 mixing Methods 0.000 claims description 4
- 239000001301 oxygen Substances 0.000 claims description 4
- 229910052760 oxygen Inorganic materials 0.000 claims description 4
- 229920002503 polyoxyethylene-polyoxypropylene Polymers 0.000 claims description 4
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims description 3
- 239000002612 dispersion medium Substances 0.000 claims description 3
- 210000001198 duodenum Anatomy 0.000 claims description 3
- 239000012530 fluid Substances 0.000 claims description 3
- 239000007787 solid Substances 0.000 claims description 3
- 239000002270 dispersing agent Substances 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 239000002609 medium Substances 0.000 claims description 2
- 239000006187 pill Substances 0.000 claims description 2
- 241000590002 Helicobacter pylori Species 0.000 claims 1
- PPKXEPBICJTCRU-UHFFFAOYSA-N [2-hydroxy-2-(3-methoxyphenyl)cyclohexyl]methyl-dimethylazanium;chloride Chemical compound Cl.COC1=CC=CC(C2(O)C(CCCC2)CN(C)C)=C1 PPKXEPBICJTCRU-UHFFFAOYSA-N 0.000 claims 1
- 229940037467 helicobacter pylori Drugs 0.000 claims 1
- 239000011261 inert gas Substances 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 239000007934 lip balm Substances 0.000 claims 1
- 229940054370 ultram Drugs 0.000 claims 1
- 238000002604 ultrasonography Methods 0.000 claims 1
- 230000003750 conditioning effect Effects 0.000 abstract description 2
- 239000000047 product Substances 0.000 description 29
- 235000013870 dimethyl polysiloxane Nutrition 0.000 description 28
- IAYPIBMASNFSPL-UHFFFAOYSA-N Ethylene oxide Chemical compound C1CO1 IAYPIBMASNFSPL-UHFFFAOYSA-N 0.000 description 21
- 125000004432 carbon atom Chemical group C* 0.000 description 19
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 15
- KWIUHFFTVRNATP-UHFFFAOYSA-N glycine betaine Chemical compound C[N+](C)(C)CC([O-])=O KWIUHFFTVRNATP-UHFFFAOYSA-N 0.000 description 15
- LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 description 14
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 12
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 12
- 125000000217 alkyl group Chemical group 0.000 description 12
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 12
- 229910052698 phosphorus Inorganic materials 0.000 description 12
- 229960003237 betaine Drugs 0.000 description 11
- 239000000796 flavoring agent Substances 0.000 description 11
- 235000019634 flavors Nutrition 0.000 description 11
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 10
- 150000001875 compounds Chemical class 0.000 description 10
- 238000009826 distribution Methods 0.000 description 10
- 235000019441 ethanol Nutrition 0.000 description 9
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 8
- GOOHAUXETOMSMM-UHFFFAOYSA-N Propylene oxide Chemical compound CC1CO1 GOOHAUXETOMSMM-UHFFFAOYSA-N 0.000 description 8
- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 description 8
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 description 8
- ILRSCQWREDREME-UHFFFAOYSA-N dodecanamide Chemical compound CCCCCCCCCCCC(N)=O ILRSCQWREDREME-UHFFFAOYSA-N 0.000 description 8
- 239000000463 material Substances 0.000 description 8
- QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 description 8
- 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 description 7
- 229940008099 dimethicone Drugs 0.000 description 7
- 235000010270 methyl p-hydroxybenzoate Nutrition 0.000 description 7
- 239000004292 methyl p-hydroxybenzoate Substances 0.000 description 7
- 229960002216 methylparaben Drugs 0.000 description 7
- 150000003254 radicals Chemical class 0.000 description 7
- 235000002639 sodium chloride Nutrition 0.000 description 7
- 239000000600 sorbitol Substances 0.000 description 7
- GVJHHUAWPYXKBD-UHFFFAOYSA-N (±)-α-Tocopherol Chemical compound OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-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
- 239000003795 chemical substances by application Substances 0.000 description 6
- 238000004140 cleaning Methods 0.000 description 6
- 235000011187 glycerol Nutrition 0.000 description 6
- 229910052757 nitrogen Inorganic materials 0.000 description 6
- 229920000642 polymer Polymers 0.000 description 6
- 229960003500 triclosan Drugs 0.000 description 6
- 229910019142 PO4 Inorganic materials 0.000 description 5
- 239000010452 phosphate Substances 0.000 description 5
- 230000000704 physical effect Effects 0.000 description 5
- 239000011780 sodium chloride Substances 0.000 description 5
- 150000003462 sulfoxides Chemical class 0.000 description 5
- 229920001285 xanthan gum Polymers 0.000 description 5
- QGZKDVFQNNGYKY-UHFFFAOYSA-O Ammonium Chemical compound [NH4+] QGZKDVFQNNGYKY-UHFFFAOYSA-O 0.000 description 4
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 4
- 239000003109 Disodium ethylene diamine tetraacetate Substances 0.000 description 4
- ZGTMUACCHSMWAC-UHFFFAOYSA-L EDTA disodium salt (anhydrous) Chemical compound [Na+].[Na+].OC(=O)CN(CC([O-])=O)CCN(CC(O)=O)CC([O-])=O ZGTMUACCHSMWAC-UHFFFAOYSA-L 0.000 description 4
- 229920002025 Pluronic® F 88 Polymers 0.000 description 4
- 229920002517 Poloxamer 338 Polymers 0.000 description 4
- 239000004372 Polyvinyl alcohol Substances 0.000 description 4
- PMZURENOXWZQFD-UHFFFAOYSA-L Sodium Sulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=O PMZURENOXWZQFD-UHFFFAOYSA-L 0.000 description 4
- KDYFGRWQOYBRFD-UHFFFAOYSA-N Succinic acid Natural products OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 description 4
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 4
- 229910000147 aluminium phosphate Inorganic materials 0.000 description 4
- 125000000129 anionic group Chemical group 0.000 description 4
- KDYFGRWQOYBRFD-NUQCWPJISA-N butanedioic acid Chemical compound O[14C](=O)CC[14C](O)=O KDYFGRWQOYBRFD-NUQCWPJISA-N 0.000 description 4
- 239000004202 carbamide Substances 0.000 description 4
- 239000003093 cationic surfactant Substances 0.000 description 4
- 239000007795 chemical reaction product Substances 0.000 description 4
- 239000003086 colorant Substances 0.000 description 4
- 235000019301 disodium ethylene diamine tetraacetate Nutrition 0.000 description 4
- WYGJAQAXAYSMNH-UHFFFAOYSA-M dodecanoyl(trimethyl)azanium;chloride Chemical compound [Cl-].CCCCCCCCCCCC(=O)[N+](C)(C)C WYGJAQAXAYSMNH-UHFFFAOYSA-M 0.000 description 4
- 125000003976 glyceryl group Chemical group [H]C([*])([H])C(O[H])([H])C(O[H])([H])[H] 0.000 description 4
- 230000002209 hydrophobic effect Effects 0.000 description 4
- 229940116335 lauramide Drugs 0.000 description 4
- 150000004668 long chain fatty acids Chemical class 0.000 description 4
- OSWPMRLSEDHDFF-UHFFFAOYSA-N methyl salicylate Chemical compound COC(=O)C1=CC=CC=C1O OSWPMRLSEDHDFF-UHFFFAOYSA-N 0.000 description 4
- NQMRYBIKMRVZLB-UHFFFAOYSA-N methylamine hydrochloride Chemical compound [Cl-].[NH3+]C NQMRYBIKMRVZLB-UHFFFAOYSA-N 0.000 description 4
- 239000003002 pH adjusting agent Substances 0.000 description 4
- 239000002304 perfume Substances 0.000 description 4
- WVDDGKGOMKODPV-ZQBYOMGUSA-N phenyl(114C)methanol Chemical compound O[14CH2]C1=CC=CC=C1 WVDDGKGOMKODPV-ZQBYOMGUSA-N 0.000 description 4
- 229920001993 poloxamer 188 Polymers 0.000 description 4
- 229920001223 polyethylene glycol Polymers 0.000 description 4
- 229920002451 polyvinyl alcohol Polymers 0.000 description 4
- 235000019422 polyvinyl alcohol Nutrition 0.000 description 4
- 239000003755 preservative agent Substances 0.000 description 4
- 235000010232 propyl p-hydroxybenzoate Nutrition 0.000 description 4
- 239000004405 propyl p-hydroxybenzoate Substances 0.000 description 4
- 229960003415 propylparaben Drugs 0.000 description 4
- 239000003352 sequestering agent Substances 0.000 description 4
- 229910000029 sodium carbonate Inorganic materials 0.000 description 4
- 229910052938 sodium sulfate Inorganic materials 0.000 description 4
- 235000011152 sodium sulphate Nutrition 0.000 description 4
- AYGJDUHQRFKLBG-UHFFFAOYSA-M sodium;1,1-dioxo-1,2-benzothiazol-3-olate;dihydrate Chemical compound O.O.[Na+].C1=CC=C2C(=O)[N-]S(=O)(=O)C2=C1 AYGJDUHQRFKLBG-UHFFFAOYSA-M 0.000 description 4
- ANOBYBYXJXCGBS-UHFFFAOYSA-L stannous fluoride Chemical compound F[Sn]F ANOBYBYXJXCGBS-UHFFFAOYSA-L 0.000 description 4
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- QAOWNCQODCNURD-UHFFFAOYSA-N sulfuric acid Substances OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 description 4
- 239000002562 thickening agent Substances 0.000 description 4
- MGSRCZKZVOBKFT-UHFFFAOYSA-N thymol Chemical compound CC(C)C1=CC=C(C)C=C1O MGSRCZKZVOBKFT-UHFFFAOYSA-N 0.000 description 4
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- 229940082509 xanthan gum Drugs 0.000 description 4
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 description 3
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- 229940090898 Desensitizer Drugs 0.000 description 3
- KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 description 3
- CPELXLSAUQHCOX-UHFFFAOYSA-N Hydrogen bromide Chemical compound Br CPELXLSAUQHCOX-UHFFFAOYSA-N 0.000 description 3
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- 125000003342 alkenyl group Chemical group 0.000 description 3
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- 239000002585 base Substances 0.000 description 3
- UHKXAKWTDCVRCO-UHFFFAOYSA-M benzoyl-dimethyl-octadecylazanium;chloride Chemical compound [Cl-].CCCCCCCCCCCCCCCCCC[N+](C)(C)C(=O)C1=CC=CC=C1 UHKXAKWTDCVRCO-UHFFFAOYSA-M 0.000 description 3
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- 238000009472 formulation Methods 0.000 description 3
- ZTHYODDOHIVTJV-UHFFFAOYSA-N gallic acid propyl ester Natural products CCCOC(=O)C1=CC(O)=C(O)C(O)=C1 ZTHYODDOHIVTJV-UHFFFAOYSA-N 0.000 description 3
- WIGCFUFOHFEKBI-UHFFFAOYSA-N gamma-tocopherol Natural products CC(C)CCCC(C)CCCC(C)CCCC1CCC2C(C)C(O)C(C)C(C)C2O1 WIGCFUFOHFEKBI-UHFFFAOYSA-N 0.000 description 3
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- 239000002888 zwitterionic surfactant Substances 0.000 description 3
- NOOLISFMXDJSKH-UTLUCORTSA-N (+)-Neomenthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@@H]1O NOOLISFMXDJSKH-UTLUCORTSA-N 0.000 description 2
- VCGRFBXVSFAGGA-UHFFFAOYSA-N (1,1-dioxo-1,4-thiazinan-4-yl)-[6-[[3-(4-fluorophenyl)-5-methyl-1,2-oxazol-4-yl]methoxy]pyridin-3-yl]methanone Chemical compound CC=1ON=C(C=2C=CC(F)=CC=2)C=1COC(N=C1)=CC=C1C(=O)N1CCS(=O)(=O)CC1 VCGRFBXVSFAGGA-UHFFFAOYSA-N 0.000 description 2
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- 239000003082 abrasive agent Substances 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
- 239000002253 acid Substances 0.000 description 2
- 150000001298 alcohols Chemical class 0.000 description 2
- 125000001931 aliphatic group Chemical group 0.000 description 2
- 125000002947 alkylene group Chemical group 0.000 description 2
- 150000001412 amines Chemical class 0.000 description 2
- BLFLLBZGZJTVJG-UHFFFAOYSA-N benzocaine Chemical compound CCOC(=O)C1=CC=C(N)C=C1 BLFLLBZGZJTVJG-UHFFFAOYSA-N 0.000 description 2
- 238000004061 bleaching Methods 0.000 description 2
- WOWHHFRSBJGXCM-UHFFFAOYSA-M cetyltrimethylammonium chloride Chemical compound [Cl-].CCCCCCCCCCCCCCCC[N+](C)(C)C WOWHHFRSBJGXCM-UHFFFAOYSA-M 0.000 description 2
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- 206010013781 dry mouth Diseases 0.000 description 2
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- SPTAJTRODSJRMF-UHFFFAOYSA-N n,n-dimethylheptadecan-1-amine;hydrochloride Chemical compound [Cl-].CCCCCCCCCCCCCCCCC[NH+](C)C SPTAJTRODSJRMF-UHFFFAOYSA-N 0.000 description 2
- CXQXSVUQTKDNFP-UHFFFAOYSA-N octamethyltrisiloxane Chemical compound C[Si](C)(C)O[Si](C)(C)O[Si](C)(C)C CXQXSVUQTKDNFP-UHFFFAOYSA-N 0.000 description 2
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Classifications
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- 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
- A61K8/347—Phenols
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
- A61K8/04—Dispersions; Emulsions
- A61K8/06—Emulsions
- A61K8/062—Oil-in-water emulsions
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- A—HUMAN NECESSITIES
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- 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
- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
- A61K8/494—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom
- A61K8/4946—Imidazoles or their condensed derivatives, e.g. benzimidazoles
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
- A61K8/84—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions otherwise than those involving only carbon-carbon unsaturated bonds
- A61K8/89—Polysiloxanes
- A61K8/891—Polysiloxanes saturated, e.g. dimethicone, phenyl trimethicone, C24-C28 methicone or stearyl dimethicone
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
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- A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
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- A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
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- 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
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Abstract
The present invention is directed to oral care ULTRAMULSION based oral care products, including, toothpastes, treated flosses and dental stimulators, interdental coating substances, oral rinses, mouth/throat conditioning internal treatment products, and anti-gingivitis products. All of these products are improved when an ULTRAMULSION dispersion containing silicone and a surfactant is used as taught herein. The ULTRAMULSION dispersions of the present invention combine certain characteristics of emulsions with certain features of microemulsions. Like conventional emulsions, they are two phase systems comprising a silicone dispersed in a continuous, surfactant phase, wherein the silicone is insoluble in the surfactant. Unlike conventional emulsions, but like microemulsions, these dispersions are stable. Unlike microemulsions, but like conventional emulsions, mechanical work is required to form ULTRAMULSION dispersions. Unlike microemulsions, but like conventional emulsions, these ULTRAMU LSION dispersions are not formed spontaneously. Like conventional emulsions, the ULTRAMULSION dispersions do not contain a cosolvent commonly found in microemulsions.
Description
Like conventional emulsions, ULTRAMULSION ™ dispersions do not contain a cosolvent commonly found in microemulsions. Of course, the ULTRAMULSION ™ dispersions of the present invention can be easily dispersed in various liquids such as water, to obtain stable dispersions. These dispersions of ULTRAMULSION ™ dispersions in water have excellent utility in various non-oral care products. For the purposes of the present invention: a. "stable" as defined below; a dispersion of the ULTRAMULSION ™ dispersion in water when subjected to centrifugation in a 100 G environment for 5 minutes, less than about 10% by weight of the ULTRAMULSION ™ dispersion is separated from the continuous water phase and / or a substantial portion (ie: 50%) of the dispersed phase separation. This last definition is particularly applicable to silicones of higher viscosity. b. "Water-free" means that the ULTRAMULSION ™ dispersion of silicone and surfactant is substantially free of water. c. "solventless" means that the ULTRAMULSION ™ dispersion of silicone and surfactant is substantially free of cosolvents such as ethanol, isopropanol and the like.
d. "oriented" means that the polar portions of the "uncoiled" polydimethylsiloxane in the ULTRA ULSION ™ dispersion are generally aligned in a plane with the hydrophilic oil that looks for alienated portions in the background as illustrated in FIG. 2. e. "monolayer" means that the monomolecular film of the ULTRAMULSION ™ dispersion of the present invention when dispersed in water is attracted to the teeth and surfaces of the mouth by secondary bonding force to form a substantive coating therein. As described above, a preferred embodiment of the present invention relates to various oral care products containing stable dispersions of certain high viscosity silicones in certain surfactants; where: a. the dispersed silicones, which are insoluble in said surfactant, are oriented by the surfactant so that when dispersed in water they are adept at forming coatings oriented on, the teeth and surfaces of the mouth with increased substantivity, and b. the particle size of the dispersed silicone is between about 0.1 and about 10 microns, with a particle size distribution between about 80 and 95% of the dispersed silicone being within this scale of particle size. In certain embodiments, between 80-95% of two dispersed silicones is less than 1-2 microns in particle size. These stable dispersions are described as dispersions of ULTRAMULSION ™, which, along with their physical properties, when contained in care products oral, provide these oral care products with distinctive conditioning, wetting, protection, etc., properties where the phase functions are continuous silicone as a reservoir for various oral care treatment substances. The present invention relates to various oral care rinses containing stable dispersions of certain high viscosity silicones in certain surfactants; where: a. the dispersed silicones, which are insoluble in said surface-active agent, are oriented by the surfactant so that when they are dispersed in water they are particularly adept in forming coatings oriented on surfaces of the mouth with increased substantivity, and b. the particle size of the dispersed silicone is between about 0.1 and about 10 microns, with a particle size distribution so that between about 80 and 95% of the dispersed silicone is within this particle size range. These stable dispersions are described as ULTRAMULSION ™ dispersions, which, together with their physical properties, when contained in mouthwash mouthwashes, provide these rinses with increased substantivity for the surfaces of the mouth where the non-continuous silicone phase functions as a reservoir for various active ingredients contained therein, including, but not limited to an essential mixture of thymol, eucalyptol, menthol and methyl salicylate. The present invention relates to unique interdictal delivery devices, other than dental floss, which are suitable for cleaning, massaging and / or treating surfaces of teeth and gums including interproximal and subgingival areas.; wherein these devices contain ULTRAMULSION ™ dispersions of high viscosity silicones dispersed in surfactants, these dispersions are released into the oral cavity of these devices during use where the dispersed silicone. to. is insubjected to the surfactant and oriented so as to form coatings in the oral cavity with increased substantivity, b. the functions as a reservoir for various soluble dispersible ingredients and / or lipid liquids to be released on oral cavity surfaces, and c. it has a particle size of between about 0.1 to about 10 microns between about 80% and about 95% of the particles within this scale. The present invention relates to various oral care products containing stable dispersions, of certain high viscosity silicones in certain surfactants to be used for the purpose of treating mucosal containing surfaces, such as in the mouth, throat and stomach and the intestine and the surface of the esophagus that contains many. to. the dispersed silicones, which are insoluble in said surfactant are oriented by the surfactant so that when dispersed in water they are particularly adept at forming coatings oriented in the mouth, throat and esophagus and surfaces of the stomach with increased substantivity, and b. the particle size of the dispersed silicone is between about 0.1 and about 10 microns, with a particle size distribution so that substantially all of the dispersed silicone is within this particle size range. These stable dispersions are described as ULTRAMULSION ™ dispersions, which, together with their physical properties, when contained in properties for the treatment of the mouth, throat, esophagus, stomach, intestine, when contained in the products, provide these products with substantive coating protection properties wherein the silicone seal discontinues said coating functions as a reservoir for several suitable liquid treatment substances suitable for releasing the surface being treated. The present invention is directed to various toothpastes containing stable dispersions of certain high viscosity silicones in certain surfactants; where: a. the dispersed silicones, which contain betrayals, 2,4,4'-triclosan-2'-hydroxy / epoxy / ether, are insoluble in said surfactant, are oriented by the surfactant so that when dispersed in water they are particularly adapted by forming non-helical coatings oriented on the surfaces of the mouth with increased substantivity, and b. the particle size of the dispersed silicone is between about 0.1 and about 10 microns, with a particle size distribution so that between about 80 and 95% of the dispersed silicone is within this particle size range. these stable dispersions are described as ULTRAMULSION ™ dispersions, which, together with their physical properties, when contained in toothpastes, provide toothpaste with increased substantivity for the surfaces of the mouth, where the silicone phase does not continue to function as a deposit for the triclosan contained in it. The present invention relates to various oral care products containing stable dispersions of certain high viscosity silicones in certain surfactants; where. to. the dispersed silicones, which are insoluble in said surfactant, are oriented by the surfactant as when dispersed in water they are particularly adept at forming coatings oriented on surfaces of the mouth with increased substantivity, and b. the particle size of the dispersed silicone is between about 0.1 and about 10 microns, with a particle size distribution so that between about 80 and 95% of the dispersed silicone is within this particle size range. These stable dispersions are described as ULTRAMULSION, which, together with their physical properties, when contained in oral care products, provide these oral care products with improved substantivity to the mouth surfaces, when the silicone phase does not continue to function as a reservoir for several ingredients contained in it. BRIEF DESCRIPTION OF THE DRAWINGS Figure 1 illustrates the "coiled" molecular configuration proposed for the polydiethylsiloxanes. Figure 2 illustrates the proposed molecular configuration of oriented polydimethylsiloxanes after processing of the ULTRAMULSION ™ dispersion; Figure 3 schematically illustrates a ULTRAMULSION ™ dispersion process of the present invention; and Figures 4 and 5 illustrate that the ULTRAMULSION ™ dispersions of the present invention produced via various high shear dispersing means having particle size distribution of 80 +% under 10 microns. DETAILED DESCRIPTION OF THE PREFERRED MODALITIES Referring to the drawings, Figure 1 illustrates the "coiled" configuration accepted for polydimethylsiloxane, where the methyl portions are oriented outward while the oxygen portions are oriented inward toward the serpentine axis. propeller. This configuration is not easily primed, joining between the oxygen portions and compatible surfaces such as tooth enamel. Figure 2 illustrates the "uncoiled oriented" configuration proposed for polydimethylsiloxanes that have been dispersed in the stable ULTRAMULSION ™ dispersions of the present invention, wherein the oxygen portions are generally oriented in a different plane than the portions of methyl groups in a plane different from that of the methyl portions. This proposed unrolled oriented configuration appears to withstand unique and unexpected stability, uniting and improving the substantivity properties of the ULTRAMULSION ™ dispersions of the present invention, as evidenced by the different coating applications of these ULTRAMULSION ™ dispersions to the teeth. . See the examples provided below. Figure 3 illustrates the ULTRAMULSION ™ dispersion process of the present invention wherein a nonionic surfactant and a polydimethylsiloxane 1, substantially free of water and cosolvent and mixed in the container 2, provided with mixing means 3, source of heat 4 and inert head space 5. The heated and mixed surfactant-polydimethylsiloxane agent 6 is then subjected to high shear dispersion at an elevated temperature in the dispersion means 7, to produce the dispersion of ULTRAMULSION ™ 8, the present invention. The high shear dispersion device (7) is normally selected from devices manufactured by Ross, IKA Works, etc. Other energy sources such as through-flow ultrasonic cells can also be used. Figure 4 is a graph describing the particle size distribution of a ULTRA ULSION ™ dispersion of the present invention containing from about 50 to 95% by weight of nonionic surfactant and from about 5 to 50% by weight of polydimethylsiloxane (2.5 million is) produced in a continuous process with a dispersion medium from IKA Works, (high shear dispersant) with an inlet temperature of 140 ° C and an outlet temperature of 210 ° C. Figure 5 is a graph describing the particle size distribution of a ULTRAMULSION ™ dispersion of the present invention containing from about 50 to 95% by weight of nonionic surfactant and from about 5 to 50% by weight of polydimethylsiloxane (2.5 million is) produced in a batch process with a dispersion measurement of Ross M / E 100 LC adapted with a 20 mesh screen, operated at a temperature of approximately 120 ° to 160 ° C. For purposes of the present invention, the term "silicone" means a clear, colorless substance, containing polydialkylsiloxane polymers with average kinematic viscosities ranging from about 100,000 centistokes (s) to about 50 million, preferably from about 1 million is to about 25 million is, more preferably from about 1.5 million is to about 10 million is, and more preferably from 2 million to about 5 million is. This definition intentionally includes the so-called "rubber" silicones that have viscosities of 30 to 50 million. Certain high viscosity polydimethylsiloxanes having viscosities of about 25 million is about 4 million is particularly preferred for the oral care products of the present invention. Other polydimethylsiloxanes suitable for the present invention include insoluble silicones of "substituted" water and mixtures of polydiorganosiloxanes and insoluble silicones of substituted water. Specifically, water soluble silicones are excluded from the ULTRAMULSION ™ dispersions of the present invention. See also tables 1 and 2 below. The viscosity of some silicones can be measured by means of a capillary glass viscometer as established in Dow Corning Corporate Test Method CTM0004, July 20, 1970. The silicone can be both a high viscosity polyalkylsiloxane and described in detail below, a polyaryl siloxane, a polyalkylaryl siloxane or a polyether siloxane compolymer. Mixtures of these silicones can also be used and are preferred in certain embodiments of the present invention. Polyalkylaryl siloxanes that can be used include, for example, polymethylfinylsiloxanes having viscosities above 1 million centistokes at 20 ° C. Some of these siloxanes are available, for example, from the General Electric Company of Dow Corning and / or Rhone-Poulenc. The polyether siloxane copolymer that can be used, for example, is a dimethylpolysiloxane modified by polypropylene oxide although ethylene oxide or mixtures of ethylene oxide and propylene oxide can also be used. References describing suitable silicone fluids include US Pat. No. .2,826,551 to Green; Patent of E.U.A. No. 3,964,500 from Dradkoff; Patent of E.U.A. No. 4,364,837 to Padner and British Patent No. 849,433 to Woolston. See also, Silicon Compounds distributed by Petrarch Systems, Inc., 1984. This reference provides a very good list of suitable silicone materials. Silicone materials that were found to be especially useful in the present compositions for providing good dry warpage are silicone gums. The silicone gums described by Petrarch et al. Including US Pat. No. 4,152,416, May 1, 1979 to Spitzer et al. And Noli, Walter, "Chemistry and Technology of Silicones," Academic Press, New York (1968). Also several General Electric Silicone Rubber Product Data Sheets describe silicone rubber. The "silicone gum" materials denote high molecular weight polydiorganosiloxanes having a viscosity up to about 50,000,000 is. Specific examples include polydimethylsiloxane; polydimethylsiloxane;
methyl vinyl siloxane copolymer; polydimethylsiloxane; diphenylmethylvinylsiloxane copolymer and mixtures thereof. As noted above, high viscosity polydimethylsiloxanes, ie those of more than 100,000 is preferred in this invention. Particularly preferred are polydimethylsiloxanes having viscosities ranging from about 2.5 million and about 50 million is. The safety of polydimethylsiloxanes for use in these different products is well documented. See Rowe et al., Journal of Industrial Hygiene, 30 (6); 332-352 (1948). Also see Calandra et al., ACS Polymer Preprints, 17: 1-4 (1976) and Kennedy et al., J. Toxicol. & Environmental Health, 1: 909-920 (1976). As noted above, the preferred polydimethylsiloxanes useful in oral care compositions! of the present invention are described as polymethylsiloxanes with the chemical composition (CH3) 3SiO [SiO (CH3) 2] «Si (CH3) 3 wherein n is an integer. These polydimethylsiloxanes have viscosities that vary up to about 50 million and are generally described as having high molecular weight. The particle size of the silicone in the dispersions of
ULTRAMULSION ™ of the present invention may vary from about 0.1 to about 10 microns. In a preferred embodiment of the present invention, the particle size of polydimethylsiloxanes in the ULTRAMULSION ™ dispersion ranges from less than 1 to about 5 microns. The particle size distribution of the polydimethylsiloxanes in the ULTRA ULSION ™ dispersions of the present invention they generally vary between about 80% and about 95% of the particles under 10 microns. See especially Figures 4 and 5. In a preferred embodiment of the present invention, between about 80% and about 95% the particles are under 5 microns. See also Table 2. An essential component of the ULTRAMULSION ™ dispersion of the present invention is a surfactant. The surfactant can be selected from any of a wide variety of synthetic anionic, amphoteric, zwitterionic and nonionic surfactants. Suitable surfactants for the purposes of the present invention should function as the continuous phase and contain the discontinuous silicone phase. The synthetic anionic surfactants can be exemplified by the alkali metal salts of the organic sulfuric reaction products having in their molecular structure an alkyl radical containing 8-22 carbon atoms and a radical of sulfuric acid ester or sulfuric acid (NOTE: the alkyl portion of higher acid radicals is included in the term "alkyl"). Preferred are sodium, ammonium, potassium or triethanolamine-alkylated sulfates, especially those obtained by sulfating the higher alcohols (C8-CiB carbon atoms), sulphates and sulfonates of coconut oil and sodium fatty acid monoglyceride, sodium salts or potassium of sulfuric acid esters of the reaction product of 1 mole of a higher fatty alcohol (g.vr., tallow or coconut oil alcohols) and from 1 to 12 moles of ethylene oxide ether sulfate with 1 to 1 0 units of ethylene oxide per molecule and in which the alkyl radicals contain from 8 to 1 2 carbon atoms, sodium alkyl glyceryl ether sulfonates; the reaction product of fatty acids having from 10 to 22 carbon atoms esterified with isothionic acid and neutralized with sodium hydroxide; water soluble salts of condensation products of fatty acids with sarcosin; and others known in the field. The zwitterionic surfactants can be exemplified by those which can be broadly described as derivatives of aliphatic quaternary compounds of ammonium, phosphonium and its lfonium, in which the aliphatic radicals can be straight or branched chain and wherein one of the substituents Aliphatic contains approximately 8 to 18 carbon atoms and one contains an anionic water solubilizing group, v. g r. , carboxy, sulfonate, sulfate, phosphate or phosphonate. A general formula for these compounds is:
(R 3) "R2-Y (+, -C H2-R4 Z (" " wherein R2 contains an alkyl, a l-aryl, or an alkyl-alkyl-radical of about 8 to 1 8 carbon atoms, from 0 to about 1 0 portions of ethylene oxide and 0 to 1 glyceryl portion; Y is selected from the group consisting of nitrogen, gold phosphorus, and sulfur atoms; R 3 is an alkyl or monohydroxyalkyl group containing 1; to about 3 carbon atoms, x is 1 when Y is a sulfur atom and 2 when it is a phosphorus nitrogen atom, R4 is an alkylene or hydroxyalkylene of 1 to about 4 carbon atoms and Z is a radical selected from group consisting of carboxylate, sulfonate, sulfate, phosphonate and phosphate groups Examples include 4-, [N, N-di (2-hydroxyethyl) -N-octadecylammonium] -butane-1-carboxylate, 5- (S-3) -hydroxypropyl-S-hexadecylsulfonium] -3-hydroxypentane-1-sulfate; 3- [P, P-diethyl-P-3,6,9-trioxatetradecocylphosphonium] -2-hydroxypropane-1-phosphate; 3- [N , Nd i prop i lN-3-dodecoxy-2-h id roxi propila moni or] -pro cloth- 1 -phosphate; 3- [N, N-dimethyl-N-hexadecylammonium] -propane-1-sulfonate; 4- [N, N-di (2-hydroxyethyl) -N- (2-hydroxydedecyl) ammonium] -butane-1-carboxylate; 3- [S-ethyl-S- (3-dodecoxy-2-hydroxypropyl) sulfonium] -propa non-1-phosphate; 3- [P, P-dimethyl-P-dimethyl-P-dodecylphosphonium] -pro ano-1-phosphonate; and 5- (N, N-di (3-hydroxypropyl) -N-hexadecylammonium] -2-hydroxypentane-1-sulfate Other zwitterionics such as betaines are also useful in the present invention Examples of betaines useful herein include Higher alkyl betaines such as cocodimethylcaboxymethyl betaine, lauryl dimethyl carboxymethyl betaine, lauryl dimethyl alpha-carboxyethylene betaine, cetyl dimethyl carboxymethyl betaine, lauryl bis- (2-hydroxyethyl) carboxyl methyl betaine, stearyl bis- (20-hydroxy-propyl) -caboxymethylbetaine , oleyl dimethyl gamma-carboxypropyl betaine, lauryl bis- (2-hydroxypropyl) alpha-carboxyethyl betaine, etc. The sulfobetaines can be represented by cocodimetiisutfopropylbetaine, stearyl dimethyl sulfopropylbetaine, lauryl dimethyl sulfoethyl betaine, lauroyl bis- (2-hydro-ethyl) sulfopropyl Betaine and the like, amido betaines and amidosulfobetaines wherein the radical RCONH (CH2) 3 binds to the nitrogen atom of betaine are also useful in this invention. they are preferred for use in some of the compositions of this invention. A particularly preferred composition utilizes an amido betaine, a quaternary compound, a silicone, a suspending agent and has a pH of about 2 to about 4. Examples of amphoteric surfactants that are used in the ULTRAMULSION ™ dispersions of the present invention are those which can be broadly described as aliphatic secondary and tertiary amine derivatives in which the aliphatic radical can be straight or branched chain and wherein one of the aliphatic substituents contains from about 8 to about 18 carbon atoms and one contains a anionic water solubilizing group, e.g., carboxyl, sulfonate, sulfate, phosphate or phosphonate. Examples of compounds that fall within this definition are sodium 3-dodecylpropionate, sodium 3-dodecylamino-propane sulfonate, N-alkyltarines such as those prepared by reacting dodecylamine with sodium isethionate according to the teachings of US Pat. .. U A. No. 2,658,072, aspartic N-higher alkyl acids such as those produced in accordance with the teachings of the US Patent No. 2,438,091, and the products sold under the trade name "iranol" and described in the U.S. Patent. No. 2,528,378. The nonionic surfactants, which are preferably used in combination with an anionic, amphoteric or zwitterionic surfactant, can be broadly defined as compounds produced by the condensation of alkylene oxide groups (hydrophilic in nature) with an organic hydrophobic compound which can be be of aliphatic or aromatic alkyl nature. Examples of preferred classes of nonionic surfactants are: 1. The condensates of polyethylene oxide of alkyl phenols., e.g., the condensation products of alkyl phenols having an alkyl group containing from about 6 to 12 carbon atoms in a straight chain or branched chain configuration, with ethylene oxide, ethylene oxide being present in amounts equal to 10 to 60 moles of ethylene oxide per mole of alkyl phenol. The alkyl substituent in said compounds can be derived, for example, from polymerized propylene, di-isobutylene, octane or nonane. 2. Those derived from the condensation of ethylene oxide with the product resulting from the reaction of propylene oxide and ethylenediamine products which can vary in composition depending on the balance between hydrophobic and hydrophilic elements that are desired. For example, the compounds that they contain from about 40% to about 80% polyoxyethylene by weight and have a molecular weight of from about 5,000 to about 15,000 which result from the reaction of the ethylene oxide groups with a hydrophobic base constituted from the ethylene diamine reaction product. and excess propylene oxide, said base having a molecular weight in the order of 2,500 to 3,000 are satisfactory. 3. The condensation product of aliphatic alcohols having 8 to 18 carbon atoms, in straight or branched chain configuration, with ethylene oxide, e.g., a condensate of ethylene oxide of coconut alcohol having 10 to 30 moles of ethylene oxide per mole of coconut alcohol, the coconut alcohol fraction having from 10 to 14 carbon atoms. 4. The long chain tertiary amine oxides corresponding to the following general formula:
RrN- 0 I R2 wherein Ri contains an alkyl, alkenyl or monohydroxyalkyl radical of from about 8 to about 18 carbon atoms from 0 to about 10 percent ethylene oxide and from 0 to 1 glyceryl portions and R2 and R3 it contains from 1 to about 3 carbon atoms and from 0 to about 1 hydroxy radical groups, e.g., methyl, ethyl, propyl, hydroxyethyl, or hydroxypropyl. The arrow in the formula is a conventional representation of a semipolar link. Examples of amine oxides suitable for use in this invention include a dimethyldoacetylamine oxide, oleyl di (2-hydroxyethyl) amine oxide, dimethyloctylamine oxide, dimethyl-decylamine oxide, dimethyltetradecylamine oxide, 3,6,9-oxide. -trioxaheptadecyldietylamine, di (2-hydroxyethyl) -tetracylamine oxide, 2-dodecoxyethyldimethylamine oxide, 3-dodedekoxy-2-hydroxypropyl (3-hydroxypropyl) amine oxide, dimethylhexadecylamine oxide.
5. long-chain tertiary phosphine oxides corresponding to the following general formula: R
I R'-N? 0 I R "
wherein R contains an alkyl, alkenyl or monohydroxyalkyl radical ranging from 8 to 18 carbon atoms in chain length from 0 to about 10 portions of ethylene oxide and from 0 to 1 glyceryl potions and R 'and R "are each alkyl or monohydroxyalkyl groups containing from 1 to 3 carbon atoms The arrow in the formula again is the conventional representation of a semi-polar bond Examples of suitable phosphine oxides are: dodecyldimethylphosphine oxide, tetradecyl-dimethyl- phosphine, tetradecyl-methylethylphosphine oxide, 3,6,9-trioxaocta-decyl dimethylphosphine oxide, cetyl dimethylphosphine oxide, 3-dodecoxy-2-hydroxypropyl-di (2-hydroxyl) -phosphine oxide, stearyldimethylphosphine oxide, oxide of cetylethylpropylphosphine, cetyldiethylphosphine oxide, dodecyldiothiphene oxide, tetradecyldiethylphosphine oxide, dodecyldipropylphosphine oxide, dodecyl (2-hydroxyethyl) phosphine oxide, decylmethyl-2-hydroxydecide ildimethyl phosphine.
6. Long chain dialkyl sulfoxides containing a short chain alkyl or hydroxyalkyl radical of from 1 to about 3 carbon atoms (usually methyl) and a long hydrophobic chain containing alkyl, alkenyl, hydroxyalkyl or ketoalkyl radicals containing about 8 carbon atoms. to about 20 carbon atoms, from 0 to about 10 portions of ethylene oxide and from 0 to 1 glyceryl portions. Examples include octadecylmethyl sulphoxide, 2-ketotidecylmethyl sulfoxide, 3,6,9-trioxo-octadyl 2-hydroxyethyl sulfoxide, dodecylmethyl sulfoxide, oleyl 3-hydroxypropyl sulfoxide, tetradecylcyl sulfoxide, 3-methoxytridecyl methyl sulfoxide, sulfoxide. of 3-hydroxytridecylmethyl, tetracylementyl sulfoxide, 3-methoxytridecylmethyl sulfoxide, 3-hydroxytridecylethyl sulfoxide, 3-hydroxy-3-hydroxy-3-dodecoxy-buyl methyl sulfoxide. Many surfactant agents without additional soap were described in McCUTCHEON'S, DETERGENTS AND EMULSIFIERS, 1979 ANNUAL, published by Allured Publishing Corporation. Particular preference is given to nonionic surfactants which are nonionic poloxamer surfactants of ethylene oxide and propylene oxide block copolymers varying from fluids of variable viscosities, to paste, pills and cast solids if molecular weights of 1,100 to 150,000. The surfactants are suitable ionic are manufactured and marketed by BASF Corporation lowered the Pluronic marks. Particularly preferred nonionic surfactants are Pluronic F-68, F-88, F-108 and Pluronic F-127. These are described in a BASF booklet entitled "Pluronic and Tetronic Block Copolymer Surfactant". These surfactants are ionic suitable for the present invention can be described by the following structure: CH2 I
OH- (CH2CH2)) X- (CH2CHO) Y- (CH2CH20) X-H where x, y and x 'are integers. Surprisingly, the nonionic surfactants of choice for the ULTRAMULSION ™ dispersions of the present invention are reported in the reference booklet to have marginal properties of detergency, emulsification and wetting. As noted above, the preferred nonionic poloxamer surfactants useful in the coating compositions of the present invention are described as polyoxyethylene-polyoxypropylene block copolymers such as Pluronic F-68, F-88, F-108 and F -127 (BASF) having molecular weights of at least about 1000 such as those described in US Pat. Nos. 4,343,785, 4,465,663, 4,511,563 and 4,476,107. Emulsions of various coating substances including polydimethylsiloxanes in various surfactants including nonionic surfactants are described and claimed in U.S. Pat. 4,91,927, 4,942,034; 4,950,479; 5,009,881; 5,032,387; 5,057,306; 5,057,307; 5,057,308; 5,057,309;
5,057,310, 5,057,310, 5,098,711, 5,165,913 and 5,284,648. However, there is no teaching or suggestion in these references that these high viscosity silicone emulsions are stable or that the "coating" substances are oriented since they are in the ULTRAMULSION ™ dispersions of the present invention. The ratio of surfactant to silicone in the ULTRAMULSION ™ dispersion coating compositions of the present invention may vary from about 400: 1 to about 1: 2. In a preferred embodiment of the invention, the ratio of surfactant to silicone is between about 25: 1 and 1: 2. The ULTRAMULSION ™ dispersions of the present invention can be prepared in the following manner: generally, if it is not a liquid, the surfactant first is heated to a temperature at which it becomes a liquid. The silicone is then dispersed in the hot surfactant with various shear dispersing means. In a preferred method, the hot surfactant is mechanically stirred together with the silicone, to form a pre-emulsion mixture in which the silicone is uniformly dispersed in the surfactant in drops of a size larger than that desired for the dispersions of ULTRAMULSION ™ but small enough to optimize the subsequent dispersions of high shear stress. This mixture is subjected to high shear dispersions with a medium such as the IKA-WORKS DISPAX reactor with at least one superfine generator, alternatively, a Ross Model .E., 100 LC adapted with a 20 mesh screen or it can be use a device for ultrasound treatment such as MEDSONIC XL2010 adapted with a 1.9 cm hinged cornet of 800-CY 8800-21CT Flow Cell. The discontinuous silicone phase of the ULTRAMULSION ™ dispersion may also contain a wide range of lipid soluble and / or lipid-dispersible lipid-active oral care ingredients ranging from antimicrobials to desensitizers / substances, to cures such as aloe for vitamins such as vitamin E, to flavoring, etc. These various ingredients in the silicone phase of the ULTRAMULSION ™ dispersion work on several oral care products although they are contained in a "reservoir" as they continue to be available as the ULTRAMULSION ™ oral surface dispersion interface, while the ULTRAMULSION ™ dispersion coating remains substantive to the surfaces of the mouth. The various toothpastes of the present invention can be made by mixing the materials and heating if necessary and emerging manufacturing practices, accepted for these different products as described in detail below. In addition, other toothpastes are included in the present invention including whitening toothpastes, toothpastes for treating hyposensitivity, toothpastes for those suffering from dry mouth, toothpastes for patients undergoing radiation therapy, etc. The oral care products containing the ULTRAMULSION ™ dispersions of the present invention will contain a variety of essential components varying from surfactants and abrasives to cleaning, bleaching, gelling, to flavoring gelling aids, etc. These will; detailed in several Examples described below. In addition to the above, other oral care products are included in the present invention, such as chewing gums, prophylactic pastes and products for people who use dentures to treat stomatitis. While also in the latter, the ULTRAMULSION ™ dispersion provides base performance as a vehicle for specific active ingredients such as yeast antifungal agents of Candida sp. Such as stannous fluoride. In addition, the oral care products of this invention may contain a variety of non-essential optional components suitable for rendering said compositions more acceptable, said conventional optional ingredients being well known to those skilled in the art, e.g., preservatives such as Benzyl alcohol, methylparaben, propyl paraben and imidiazolidil urea; cationic surfactants such as cetyl trimethylammonium chloride. lauroyl trimethyl ammonium chloride, methyl ammonium chloride, stearyldimethylbenzoyl ammonium chloride, and di (partially hydrogenated bait) -dimethylammonium chloride; thickeners and viscosity modifiers such as diethanolamide of a long-chain fatty acid (e.g., lauramide PEG 3), block polymers of ethylene oxide and propylene oxide such as Pluronic F88 offered by BASF Wyandotte, sodium chloride, sodium sulfate, polyvinyl alcohol and ethyl alcohol; pH adjusting agents such as citric acid, succinic acid, phosphoric acid, sodium hydroxide, sodium carbonate, etc., perfumes; colorants; and sequestering agents such as disodium ethylene diamine tetra acetate. Such agents are generally used individually at a level of from about 0.01% to about 10%, preferably from about 0.5% to about 5.0% by weight of the composition. The discontinuous silicone phase of the pastes based on the ULTRAMULSION ™ dispersion can also contain a wide range of lipid-soluble oral and / or lipid dispersible oral care ingredients ranging from antimicrobials to desensitizers / substances, for cures such as aloe for vitamins such as vitamin E, for flavoring, etc. These different ingredients in a silicone phase of toothpastes based on the ULTRAMULSION ™ dispersion of the present invention work similar to triclosan, that is, as taught are contained in a "reservoirs". These different lipid soluble substances in the silicone phase continue to be available in the ULTRAMULSION ™ oral surface dispersion interface while the ULTRAMULSION ™ dispersion coating remains substantive to buccal surfaces. The effects attributed to this "deposit" are described in Rolla et al., Supra. The toothpastes containing the ULTRAMULSION ™ and triclosan dispersions of the present invention will contain a variety of essential components ranging from surfactants to abrasives for cleaning, bleaching, for gelling flavoring gelling aids, etc. In addition to the toothpaste products of the invention may contain a variety of optional components are essential suitable to make said compositions more acceptable. Such conventional optional ingredients are well known to those skilled in the art, e.g., preservatives such as benzyl alcohol, methylparaben, methylparaben, propyl paraben, and midemylazidyl urea; cationic surfactants such as cetyl trimethylammonium chloride, lauroyl trimethyl ammonium chloride, tricyclo methyl ammonium chloride, stearyldimethylbenzoyl chloride; ammonium and di chloride (partially hydrogenated bait) -dimethylammonium; thickeners and viscosity modifiers such as diethanolamide of a long-chain fatty acid (e.g., lauramide PEG 3), block polymers of ethylene oxide and propylene oxide such as Pluronic F88 offered by BASF Wyandotte, sodium chloride, sodium sulfate, polyvinyl alcohol and ethyl alcohol; pH adjusting agents such as citric acid, succinic acid, phosphoric acid, sodium hydroxide, sodium carbonate, etc., perfumes; colorants; and sequestering agents such as disodium ethylenediamine tetra-acetate. Such agents are generally used individually at a level of from about 0.01% to about 10%, preferably from about 0.5% to about 5.0% by weight of the composition. When used for internal treatment products (oral or ingested), the discontinuous silicone phase of the ULTRAMULSION ™ dispersion can also contain a wide variety of lipid-soluble and / or lipid-dispersible ingredients suitable for treating various surface conditions in the lips in the mouth, or the throat, stomach and esophagus. These different ingredients in the silicone phase of the ULTRAMULSION ™ dispersion perform their intended function in various treatment products, etc. as taught they are contained in a "tank" as they continue to be available on the surfaces containing ULTRAMULSION ™ dispersion to be treated interface while the ULTRAMULSION ™ coating remains substantive to said surface. These coatings of substantive treatment are treated in different following examples.
Such conventional optional ingredients are well known to those skilled in the art, e.g., preservatives such as benzyl alcohol, methylparaben, methylparaben. propyl paraben and imidiazolidil urea; cationic surfactants such as cetyl trimethylamine chloride, lauroyl trimethyl ammonium chloride, tricethyl methyl ammonium chloride, stearyldimethylbenzoyl ammonium chloride and di (partially hydrogenated bait) -dimethylammonium chloride; thickeners and viscosity modifiers such as diethanolamide of a long-chain fatty acid (e.g., lauramide PEG 3), block polymers of ethylene oxide and propylene oxide such as Pluronic F88 offered by BASF Wyandotte, sodium chloride, sodium sulfate, polyvinyl alcohol and ethyl alcohol; pH adjusting agents such as citric acid, succinic acid, phosphoric acid, sodium hydroxide, sodium carbonate, etc., perfumes; colorants; and sequestering agents such as disodium ethylenediamine tetra-acetate. Such agents are generally used individually at a level of from about 0.01% to about 10%, preferably from about 0.5% to about 5.0% by weight of the composition. The conditions of the treatment surface of the lips and esophagus as well as several surfaces that contain many such as the mouth, throat, stomach and duodenum and intestines. These surfaces can be treated with various forms of the U LTRAMU LSION ™ dispersions of the invention ranging from gels and lotions for the lips, to liquids, to the mouth, to liquids and syrups for the throat, to liquids for the esophagus, to liquids and tablets for the stomach, duodenum and intestines.
For internal treatment (eg, mouth, throat, etc.), the discontinuous silicone phase of the ULTRAMULSION ™ dispersion may also contain a wide range of active ingredients for lipid soluble and / or dispersible oral care. in lipids varying from antimicrobials to desensitizers / substances, for cures such as aloe, to vitamins such as vitamin E, to flavoring, etc. These different ingredients in the silicone phase of the ULTRAMULSION ™ dispersion work on various interdictal delivery devices once they are released from the device as shown to be contained in a "reservoir" as they continue to be available at the surface interface oral dispersion of ULTRAMULSION ™, while ULTRAMULSION ™ dispersion coating remains substantive for mouth surfaces. Similar effects attributed to this effect of the deposit are described by Rolla et al., Supra. The interdental delivery device of the present invention containing the ULTRAMULSION ™ dispersions will contain a variety of essential components varying from surfactants for cleaning, to bleach, to flavoring, etc. These are detailed in several examples described below. The ULTRAMULSION ™ dispersions of the invention are particularly useful in compositions used by professionals for cleaning teeth. The inclusion of stannous fluoride in the discontinuous phase of the emulsion is particularly attractive as a means to treat interproximal caries. See Segueto et al., Journal of Dental Research, Vol. 10, No. 1, p. 90-96, 1961 and Peterson et al., Northwest Dentistry, 276-278, Sep / Oc. 1963. For oral care, the pH of the present compositions is preferably from 6 to 8. The ULTRAMULSION ™ dispersions of the invention are particularly useful in interdental devices whose use is under the supervision of a professional. The inclusion of stannous fluoride in the discontinuous phase of the emulsion is particularly attractive as a means to treat interproximal caries. See Segueto et al., Journal of Dental Research, Vol. 10, No. 1, p. 90-96, 1961 and Peterson et al., Northwest Dentistry, 276-278, Sep./Oct. 1963. The pH of the ULTRAMULSION ™ dispersions for use with interdental devices is preferably from about 6 to 8. The oral care mouthwashes containing the ULTRAMULSION ™ dispersions of the present invention may contain a variety of essential components that vary from other surfactants for cleaning, to other flavorings etc. In addition, these oral care rinses may also contain a variety of optional components that are essential to make such compositions more palatable. Such conventional optional ingredients are well known to those skilled in the art, e.g., preservatives such as benzyl alcohol, methylparaben, propyl paraben and iodothylaminidyl urea; cationic surfactants such as cetyl trimethylamine chloride, lauroyl trimethyl ammonium chloride, tricethyl methyl ammonium chloride, stearyldimethylbenzoyl ammonium chloride and di (partially hydrogenated bait) -dimethylammonium chloride; thickeners and viscosity modifiers such as diethanolamide of a long-chain fatty acid (e.g., lauramide PEG 3), block polymers of ethylene oxide and propylene oxide such as Pluronic F88 offered by BASF Wyandotte, sodium chloride, sodium sulfate, polyvinyl alcohol and ethyl alcohol; pH adjusting agents such as citric acid, succinic acid, phosphoric acid, sodium hydroxide, sodium carbonate, etc., perfumes; colorants; and sequestering agents such as disodium ethylenediamine tetra-acetate. Such agents are generally used individually at a level of from about 0.01% to about 10%, preferably from about 0.5% to about 5.0% by weight of the composition. The pH of the compositions present for use with oral rinse products preferably is from about 6 to 8. Water is an essential component of most of the oral care products of the present invention that contain one or more of the different dispersions of ULTRAMULSION ™ described above. Water in these products is generally present at a level of from about 20% to about 95%, preferably between about 60% and about 90%.
The following Tables provide a number of examples for oral care using the ULTRAMULSION ™ dispersions of the present invention.
TABLE 1 ULTRAMULSION DISPERSIONS FOR ORAL CARE% W / W Example No. 1 2 3 4 5 6 7 8 9 10 11
Components Viscosity of Dimethicone (cs) 100,000 0 - - - - - - - - 33 - 600,000 10 - - 33 2,500,000 - 10 - - - 33 - - 10
4,000,000 - - - 10 - - - 33 30,000,000. . . 10 50,000,000 - - - - - 10 - - - - - Poloxamer-188 - - - - - - - - - 90 - Poloxamer-238 - - - - - - - - - - 90
Poloxamer-338 90 90 90 90 90 90 -Poloxamer-407 - - - - - - 67 67 67 - TABLE 2 ULTRAMULATION COMPOSITIONS FOR ORAL CARE% P / P Example No. 12 13 14 15 16 17 18 19 20 21 Components Viscosity of dimethicone (cs) 600,000 - 11.6 - - - 10.0. . . . 2,500,000 10.0 - - 11.9 11.9. . . . 14.0 4,000,000 - - 11.9 10.0
30,000,000 11.6. . . .
50,000,000 11.6 10.0 -
TABLE 2 (Continued)% P / P Example No. 12 13 14 15 16 17 18 19 20 21 Components of soluble lipids Mixture of: Thymol 0.063 0.063 1.0 2 3 4 0.1 0.2 0.3 0.4 Menthol 0.055 0.55 1.0 2 3 4 0.1 0.2 0.3 0.4 Eucalyptol 0.091 0.91 1.0 2 3 4 0.1 0.2 0.3 0.4 Methyl Salicylate 0.055 0.55 1.0 2 3 4 0.1 0.2 0.3 0.4 03 OI Surfactant Poloxamer-388 86.76 85.76 84.4 80.1 76.4 74.0 88.0 89.2 88.8 84.4
TABLE 3 Distribution of Particle Size (%)
Example Product Composition < 1μ < 2μ < 3μ < 4μ < 5μ < 10 μ No. 22 67/33 Poloxamer 44 50 4 1 1 0 338 / 100,000 is. Dimeticone 23 90/10 Poloxamer 24 4 5 1 2 0 338 / 600,000 is. Dimeticonz 24 90/10 Poloxamer 2 3 63 24 8 0? 407 / 2,500,000 is. Dimethicone s >
25 90/10 Poloxamer 1.5 6 0.51 43.5 14 0 407 / 4,000,000 en. Dimethicone
TABLE 4 ORAL CARE% W / W Example No. 27 28 29 30 31 32 33 34 35
Component Viscosity of Dimethicone (cs) 600,000 11.6 10.0 2,500,000 11.9 11.9 14.0
4,000,000 11.6 30,000,000 11.6 50,000,000 11.6 10.0 Soluble Lipid Compound Mixture Thiol-24% Menthol-16% 0.0 Eucalyptol-36% Methyl Salicylate -24% Fluoride 1.75 Triclosan 1.16 1.16 1.16 1.16 2.0
Chlorhexidine Metronidazole 1.3 Benzocaine 1.0 Poloxamer Surfactant 338 80.0 97.24 87.24 86.8 87.25 89.0 87.24 87.24 80.0 84.0 TABLE 5 COMPOSITIONS OF ULTRAMULSION DENTAL PASTE% P / P Example # 36 37 38 39 40 41 42 43 44 45 46 47 Component
Dihydrate of 49.0 49.0 49.0 49.0 49.0 49.0 49.0 49.0 49.0 49.0 49.0 49.0 Dicalcium phosphate Sorbitol 18.0 18.0 18.0 18.0 18.0 18.0 18.0 18.0 18.0 18.0 18.0 18.0
-70% Ac. Water 16.67 16.67 16.67 16.67 16.67 16.67 16.67 16.67 16.67 16.67 16.67 16.67
Glycerin 10.0 10.0 10.0 10.0 10.0 10.0 10.0 10.0 10.0 10.0 10.0 10.0 8 Sodium Carboxymethyl Cellulose 1.0 1.0 1.0 1.0 1.0 1.0 1.0. 1.0 1.0 1.0 1.0 1.0 Flavor 1.0 1.0 1.0 1.0 1.0 1.0 1.0 1.0 1.0 1.0 1.0 1.0 Lauroyl Sodium Sulphate 0.8 0.8 0.8 0.8 0.8 0.8 0.8 0.8 0.8 0.8 0.8 0.8 Titanium Dioxide 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 Monofluoro Sodium phosphate 0.76 0.76 0.76 0.76 0.76 0.76 0.76 0.76 0.76 0.76 0.76 0.76
Sodium saccharin 0.27 0.27 0.27 0.27 0.27 0.27 0.27 0.27 0.27 0.27 0.27 0.27
TABLE 5 (continued) COMPOSITIONS OF ULTRAMULSION DENTAL PASTE% P / P Example # 48 49 50 51 52 53 55 ULTRAMULSION ™ Component Example 1 2.0 Example 3 2.0 Example 6 2.0 Example 4 2.0 Example 7. . . - 2.0 Example 12 - - - - - 2.0 Example 14. . . . . . Example 15 . . . . . Example 18 Example 21
TABLE 6 COMPOSITIONS ULTRAMULSION DENTAL DEHYLL% P / P EXAMPLE # 60 61 62 63 64 65 66 Component Dicalcium Phosphate Dihydrate 14.0 14.0 1144..00 1 144..00 1 144..00 1 144..00 14.0 Carrageenan 14.0 14.0 1144..00 1144..00 1144..00 1144..00 14.0 Sacarine Insoluole 22..22 22..22 22..22 2 2..22 2 2..22 2 2..22 2.2 Taste 88 ..99 88..99 88..99 88..99 88..99 88..99 8.9 EDTA 00..22 00..22 00..22 00..22 00..22 00..22 0.2 -t- Propyl Gallate 00..11 00..11 00..11 00..11 00..11 00..11 0.1 OR ULTRAMULSION ™ Example 4 6600..66 Example 5 - 6600..66 Example 6 - - 60.6 ULTRAMULSION ™ Example 2. . . 60.6 Example 3. . . 60.6 Example 1 60.0 Example 10 60.6 Each composition was loaded in a dental floss of Nylon 800 Denier between 40-60
TABLE 7 ROCIO COMPOSITIONS FOR ULTRAMULSION BREATH% W / W Example # 67 68 69 70 Component Water 82.75 82.75 82.75 82.75 Sorbitol -70% Aq. 8.5 8.5 8.5 8.5 Glycerin 3.0 3.0 3.0 3.0 Xanthan Gum 0.4 0.4 0.4 0.4 Sodium Saccharin 0.4 0.4 0.4 0.4 Sodium Benzoate 0.3 0.3 0.3 0.3 EDTA 0.05 0.05 0.05 0.05 Flavor 0.6 0.6 0.6 0.6 U LTRAMU LS ION ™ Example 3 4.0 - - - Example 4 - 4.0 - - Example 5 - - 4.0 - Example 9 - - - 4.0
TABLE 8 SPRAY COMPOSITIONS FOR DRY MOUTH
ULTRAMULSION% P / P Example # 71 72 73 Component Water 93.86 93.86 93.86 Xanthan gum 0.7 0.7 0.7 Sorbitol -70% Ac. 3.5 3.5 3.5 Potassium Chloride 0.1 0.1 0.1 Sodium Chloride 0.06 0.06 0.06 Calcium Chloride 0.02 0.02 0.02 Potassium phosphate dihydrate 0.04 0.04 0.04 Flavor 0.06 0.06 0.06 Propyl gallate 0.01 0.01 0.01 ULTRAMULSION ™ Example 2 1.5 Example 4 - 1.5 - Example 6 - 1.5 - TABLE 9 GEL COMPOSITIONS FOR ULTRAMULSION DENTURES% P / P Example # 74 75 Component Water 45.7 45.7 Sorbitol -70% Ac 34.3 34.3 Glycerin 5.0 5.0 Potassium Sorbate 0.151 0.151 Sodium Saccharin 0.075 0.075 Citrus 0.1 0.1 Methyl Paraben 0.15 0.15 Propylene Glycol 10.0 10.0 Carboxymethyl Sodium Cellulose 2.52 2.52 ULTRAMULSION ™ Example 4 2.0 Example 6 - 2.0
TABLE 10 ULTRAMULSION COMPOSITIONS FOR ORAL CARE% P / P Example # 76 77 78 79 80 81 82 83 84 85 86
Component Viscosity of Dimethicone (cs) 100,000 10 33 600,000 10 33 2,500,000 10 33 10
4,000,000 10 33 30,000,000 10 50,000,000 10 Triclosan 8 10 Poloxamer- 188 59 Poloxamer-238 80 Poloxamer-338 89 88 87 86 85 84 Poloxamer-407 65 63 61
TABLE 11 ULTRAMULATION COMPOSITIONS FOR ORAL CARE% P / P Example # 87 88 89 90 91 92 93 94 95 96 Component Dimethicone Viscosity (cs) 600,000 11.6 10.0 2,500,000 10.0 11.9 11.9 14.0 4,000,000 11.6 30,000,000 10 11.6 50,000,000 11.6 10.0 4 * . n Lipido Soluble Triclosan 10 1.16 1.16 1.3 1.0 1.75 1.16 1.16 2.0 Surfactant Poloxamer-338 80.0 75.64 88.84 86.8 87.15 88.25 87.24 88.84 83.4 84.0
TABLE 12 Example # 97 98 99 100 101
DIMETICONA 2,500,000 c. 10 10 10 10 4,000,000 is. - - - - 10
SOLUBLE LIPIDS / DISPERSIBLE Dextrometrophenyl Hydrobromide 1.0 Dextrometrophenyl Hydrobromide - 2.0 Dextrometrophenyl Hydrobromide - - 1.0 Fragrance # 17.92.3415 (IFF) - - - 1.5 1.0
SOFTENER AGENT
POLOXAMER-338 89.0 88.0 89.0 88.5 89.0
TABLE 13 ULTRAMULATION COMPOSITIONS FOR MOUTH AND LIPS% W / W A. Example: 102 103 Mineral Oil -USP 220 250 Oil Jelly- 50 50 USP Ozokerite Box 13.0 5.0 Paraffin Box 12.0 17.0 ULTRAMULSION ™ Example # 3 3.0 Example # 8 - 3.0 TABLE 14 B. Gel for treatment 102 103 for healing ulcers D I. Water 56.1 46.6 Sorbitol -70% 32.0 32.0 Propylene glycol Glycerin-USP 6.0 6.0 Potassium sorbate 0.14 0.14 Sodium saccharine 0.06 0.06 Sodium CMC 2.50 2.50 Flavor 0 20 0.20 Camphor 0 50 0.50 ULTRAMULSION Example # 10 2.50 Example # 7 2.0
TABLE 15 EXAMPLES 106-108 Compositions for Phlegm Cough or Throat Pain% p / p EXAMPLE 106 (Cough with phlegm): Glucose 26.5 Corn Syrup 40.0 Sugar 30.0 Flavor 0.5 ULTRAMULSION: Example # 8 3.0 Example 107 (Cough Syrup) : Corn Syrup 15.0 Flavor 0.3 Water D I. 83.7 ULTRAMULSION: Example # 15 1.0 Example 108 (Throat Pain Sprayer): Water D I. 74.55 Sorbitol-70% Ac. 20.0 Glycerin 3.0 Gum 0.05 Xanthan Flavor 0.40 ULTRAMULSION: Example # 13 2.00
Table 16 - EXAMPLES 109-110 Example 109 (Rinsing Without Alcohol for Starter Mouth) Water D.l 83.02 Sorbitol -70% ac. 10.0 Glycerin - USP 3.0 Saccharin 0.06 Sodium Butyrate 0.44 EDTA 0.05 Xanthan Gum 0.03 ULTRAMULSION: Example # 12 3.0 emplo 110 (Double Dispensing Rinse Concentrate) Phase A Glycerin-Anhydride 84.553 SiO-Zeodent 113 15.0 Stannous Fluoride 0 447 Phase B Water Dl 70.0 Flavor 4.6 Color Blue # 1 0.001 ULTRAMULSION Example # 14 25,399
TABLE 17 pio 111 (Tablets Antacids) Tablet A. Mineral Oil 10 0 Flavor 6.0 2.0 Sodium Polyphosphate Corn Starch 0.6 Sucrose 41.9 Talc 0.6 Carbonate of 39.0 Calcium B. ULTRAMULSION: Example # 13 5.0 Phase A - Only 95.0
Procedure for Forming the Compound of Example 111 Phase A is dry mix in a paddle mixer, e.g., Hobart, to form a so-called wet / dry granulation. Phase A is then heated to 65-70 ° C while mixing and the U LTRA U LSION ™ dispersion is added to the granulation. The ULTRAMULSION ™ dispersion melts and "plaque forms" on the surface of each granulation particle. The resulting granulated material is cooled to room temperature and formed into tablets using 1.3 grams and 18,000 kg. Table 18 Example 112 (Liquid Antacid): Phase A 96.0 Calcium Carbonate ULTRAMULSION: Example # 7 4.0 Phase B Phase A 4.0 Water D. 85.4 Sucrose 6.0 Flavor 1.5 Xanthan Gum 0 1 Glycerin 3.0
Compound Formation Procedure for Example 112:
Phase A was prepared by heating calcium carbonate in a 65-70% air stream, the ULTRAMULSION ™ dispersion is introduced at 65-70 ° C and melts in the hot air stream and "plaque form" of each particle individual of CaCO3. The material is cooled and prepared in a liquid antacid by Phase B. Example 113 (Tablet for Ulcer Treatment) Aluminum Hydroxide Mineral Oil Sodium Phosphate Talc ULTRAMULSION: Example # 12
TABLE 19 FORMULATIONS FOR INTERDENTAL DEVICE (% P / P)
Example # 114 115 116 117 118 Components: Sorbitol -70% Ac. 7.5 7.5 8.0 9.0 7.0 Sodium Saccharin 0.4 0.4 0.4 0.4 0.4 Flavor 5.0 5.0 5.4 5.1 4.8 Water D.l. 75.1 75.1 71.2 74.5 78.8 ULTRAMULSION Example 1 Example 3 12 Example 12 15 Example 14 - - - 11 - Example 2 9
Procedure to impregnate Interdental Stimulators. 1. Material to be impregnated (eg wood sticks) with the dispersion (or formulation) of ULTRAMULSION ™ is placed in the suitable container capable of maintaining a vacuum, such as a desiccator, covered stainless steel reactor or similar device.
2. The liquid formulation is poured into the upper part of the material and completely covered by the liquid. A perforated disc with reinforcement is placed in the material so that it does not float. 3. The container is then sealed and vacuum applied for varying periods ranging from 1 min to several hours with the preferred time being between 5-10 min. 4. The vacuum is maintained so that the liquid does not boil, but enough vacuum to remove trapped air from the device. TABLE 19 CONTINUOUS Example of laboratory preparation using Interdental Wood Stimulators (EIO) Collectively, 87.0 grams of interdental wood stimulators (EID) is equal to approximately 260 individual stimulators. This batch of EID was impregnated with the ULTRAMULSIO ™ dispersion formulation of Example 22 under vacuum, at 30 mm of mercury for a period of 10 minutes. The resulting impregnated IDS batch was removed from the remaining solution and dried at 40 ° C in a normal oven for 1.5 hours. The EIDs were dried and the final batch was weighed as 152.7 grams. This is an increase of 56.0% by weight indicating the amount of dry formulation impregnated in the EID. The present invention has been described in detail, including preferred embodiments thereof. However, it will be appreciated that those skilled in the art, upon consideration of the present disclosure, may make modifications and / or improvements in this invention yet be within the scope and spirit of this invention as set forth in the following claims.
Claims (1)
- CLAIMS 1. - A treatment composition, selected from the group consisting of compositions for oral treatment, compositions for treatment of the throat, compositions for the treatment of the esophagus, compositions for the treatment of the stomach and intestine, where said composition contains a dispersion of high effort cutting, water-free, or ULTRAMULSION ™, formed by heating a mixture of surfactant and silicone, and then mixing with high shear; where to. the silicone is insoluble in the surfactant, has a viscosity of greater than about 100,000 and has an average particle size of up to about 10 microns; b. the surfactant to silicone ratio in the ULTRAMULSION dispersion is approximately between 400: 1 and 1: 1, and the surfactant has an orientation effect on the silicone; c. the ULTRAMULSION dispersion forms stable dispersions in water content treatment compositions; and d. the treatment composition exhibits increased substantivity for the surface of the mouth, throat, esophagus, stomach and intestines; wherein the ULTRAMULSION coating functions as a reservoir for various ingredients of the lipid soluble and lipid dispersible treatment composition, which are available to be released from the coating reservoir on the surface being treated. 2. A treatment composition according to claim 1, further characterized in that the ULTRAMULSION dispersion comprises a poloxamer, nonionic surfactant, and polydimethylsiloxane; where to. the polydimethylsiloxane has the chemical composition (CH3) 2SiO [SiO (CH3) 2] nSi (CH3) 3, where n is an integer; b. said surfactant has the chemical composition: CH3 I OH - (CH2CH2) X- (CH3CHO) and- (CH3CH30) x-H where X, Y and X 'are integers; c. the viscosity of the polydimethylsiloxane ranges from about 2.5 million to 50 million is; d. the particle size of the majority of the polydimethylsiloxane in the ULTRAMULSION dispersion is approximately between 0.1 and 10 microns; and. substantially all of the polydimethylsiloxane particles in the ULTRAMULSION dispersion is less than about 10 microns; F. the nonionic surfactant is a polyoxyethylene-polyoxypropylene block copolymer, having a molecular weight of between about 1,100 and about 150,000; g. the ratio of surfactant to polydimethylsiloxane is approximately between 400: 1 and 1: 2; and h. when the ULTRAMULSION dispersion is dispersed in the aqueous base treatment composition, it is stable. 3. - A method for manufacturing suitable U LTRAMULSION dispersions for treatment compositions, characterized in that said method comprises: heating the mixture of surfactant and silicone in a heated and agitated container, substantially. free of water, and then subjecting the mixture to dispersion with high shear stress; where to. the silicone is insoluble in the surfactant, has a viscosity ranging from more than 100,000 is to about 50 million, and has a particle size of up to about 10 microns; b. the surfactant to silicone ratio in the high shear dispersion is about 400: 1 to 1: 1, and the surfactant has a guiding effect on the silicone; c. the silicone is oriented, exhibits increased substantivity for the surfaces of the oral cavity, and functions as a reservoir for various active ingredients. 4. - A method according to claim 3, further characterized in that the heated container is provided with an inert gas front. 5. - A method according to claim 3, further characterized in that the dispersing medium of high shear stress is equipped with a small hole. 6. - A method according to claim 3, further characterized in that the dispersing means of high shear stress comprises an ultrasound means. 7. - A stable, water-based treatment composition selected from the group consisting of: composition for treatment of the mouth, composition for the treatment of the throat, composition for the treatment of the esophagus, composition for the treatment of the stomach and composition for bowel treatment; wherein the composition contains dispersed therein, a ULTRAM ULSION dispersion consisting of a nonionic poloxamer surfactant and a polydimethylsiloxane insoluble in the surfactant; where to. the polydimethylsiloxane has the chemical composition (CH3) 3SiO [SiO (CH3) 2] nSi (CH3) 3, where n is an integer; b. The surfactant has the chemical composition: CH3 I OH - (CH2CH2) x - (CH3CHO) and - (CH3CH30) x - H where x, y and x 'are integers; c. the viscosity of the polydimethylsiloxane varies approximately between 1 00,000 is and 50 million is; d. the particle size of the polydimethylsiloxane in the U LTRAM ULSION dispersion is approximately between 0.1 and 10 microns; and. substantially all of the polydimethylsiloxane particles in the ULTRAMU LSION dispersions are approximately between 1 and 10 microns; F. the polydimethylsiloxane in the dispersion of U LTRAMULSION is not curled and oriented; g. the nonionic surfactant is a polyoxyethylene-polyoxypropylene block copolymer having an approximate molecular weight between 1,000,000 and 150,000; h. the ratio of surfactant to polydimethylsiloxane is approximately between 400: 1 and 1: 2; and i. When dispersed in water, the ULTRAMULSION dispersion is stable. 8. - A treatment composition according to claim 7, further characterized in that the ratio of surfactant to silicone is 9: 1 and 90% of the silicone particles have between about 1 and 3 microns. 9. - A treatment composition according to claim 7, further characterized in that the ratio of the surfactant to the silicone is 2: 1 and 1 00 percent of the silicone dispersion has less than 10 microns. 1 0.- A treatment composition according to claim 7, further characterized in that the ratio of the surfactant to the silicone is 1: 1, and the silicone particles in the ULTRAMULSION dispersion have less than 10 microns. 1 - An aqueous-based antacid containing a ULTRAMULSION dispersion comprising a non-ionic poioxamer surfactant and an insoluble polydimethylsiloxane in the surfactant; where to. the polydimethylsiloxane has the chemical composition (CH3) 3S iO [SiO (CH3) 2) n Si (CH3) 3; where n is an integer; b. the surfactant has the chemical composition: CH3 I OH- (CH2CH2) x- (CH3CHO) y- (CH3CH30) x.- H where x, y and x 'are integers; c. the viscosity of the polydimethylsiloxane varies approximately between 1.5 million and 4 million is; d. the particle size of the majority of the polyethylene oxide in the dispersion of ULTRAMULSION is approximately between 0.1 and 10 microns; and. about 80 to 95 percent of the polydimethylsiloxane particles in the dispersions of U LTRAMULSION are between about 1 and about 10 microns; F. the polydimethylsiloxane in the dispersion of U LTRAMULSION is not curled and is oriented; g. the nonionic surfactant is a polyoxyethylene-polyoxypropylene block copolymer, having an approximate molecular weight of between 1, 100 and 150,000; h. the ratio of surfactant to polydimethylsiloxane is approximately between 400: 1 and 1: 2; and i. when dispersed in the water-based antacid composition, the dispersion of U LTRAMULSION is stable. 12. - A treatment composition according to claim 1, further characterized in that the silicone is polydimethylsiloxane, not curled and oriented, with the oxygen portions generally oriented in a plane different from that of the methyl portions. 13. - A treatment composition according to claim 1, further characterized in that the surfactant is selected from the group consisting of fluids capable of flowing, with varying viscosities; pastes, pills and molded solids. 14. - A method according to claim 3, further characterized in that the dispersion is obtained with high shear stress, through high shear dispersant media, selected from the group consisting of superfine dispersion media and dispersion media. ultrasonic 15. - A liquid composition for oral treatment, according to claim 7, further characterized in that the ratio of surfactant to polydimethylsiloxane is 1: 1 and at least 80 percent of the dispersed polydimethylsiloxane particles are between 1 and 9 micras 16. - A syrup composition for throat treatment, according to claim 1, further characterized in that the ratio of surfactant to polydimethylsiloxane is 9: 1, and about 90 percent of the dispersed polydimethylsiloxane particles have between 1 and 3 microns 17. - A lip balm composition according to claim 1, further characterized in that the ratio of surfactant to polydimethylsiloxane is 2: 1, and about 90 percent of the dispersed polydimethylsiloxane particles have between 1 and 3 microns. 18. An antacid composition, selected from the group consisting of tablets and liquids, according to claim 7, further characterized in that the ratio of surfactant to polydimethylsiloxane is 4: 1, and approximately 90 percent of the dispersed particles of polydimethylsiloxane have between 1 and 9 microns. 19. - A liquid antacid composition according to claim 7, further characterized in that the ratio of surfactant to polydimethylsiloxane is 9.5: 0.5, and about 100 percent of the dispersed polydimethylsiloxane particles have between 1 and 9 microns. 20. - A liquid composition for treatment of esophagus, according to claim 7, further characterized in that the polydimethylsiloxane has a viscosity of 2.5 million is, and the surfactant is solid at room temperature. 21. - A composition for treatment of duodenum, according to claim 1, further characterized in that the discontinuous silicone contains a suitable active ingredient to treat an infection attributed to Helicobacter pylori. RESU IN The present invention is directed to oral care products based on ULTRAMULSION ™, including toothpastes, treated dental threads and dental stimulators, interdental coating substances, oral rinses, internal treatment products that condition mouth / throat and anti-gingivitis products. All these products are improved when using a ULTRAMULSION ™ dispersion containing silicone and a surfactant as taught herein. The ULTRAMULSION ™ dispersions of the present invention combine certain emulsion characteristics with certain aspects of microemulsions. As conventional emulsions, they are two-phase systems comprising a silicone dispersed in a continuous surfactant phase, wherein the silicone is insoluble in the surfactant. Unlike conventional emulsions, but like microemulsions, these dispersions are stable. Unlike microemulsions, but like conventional emulsions, mechanical work is required to form ULTRAMULSION ™ dispersions; they do not form spontaneously. Unlike microemulsions, but like conventional emulsions, ULTRAMULSION ™ dispersions do not contain a cosolvent commonly found in microemulsions.
Applications Claiming Priority (8)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US08/462,599 US5665374A (en) | 1995-06-05 | 1995-06-05 | Ultramulsion containing interdental delivery devices |
| US08/461,698 US5733529A (en) | 1995-06-05 | 1995-06-05 | Ultramulsion based antigingivitis toothpaste compositions |
| US08/462,203 US5651959A (en) | 1995-06-05 | 1995-06-05 | Ultramulsion based oral care compositions |
| US08/464,403 US5711936A (en) | 1995-06-05 | 1995-06-05 | Ultramulsion based ingestible compositions |
| US08/462,930 US5645841A (en) | 1995-06-05 | 1995-06-05 | Ultramulsion based oral care rinse compositions |
| PCT/US1996/008714 WO1996039116A1 (en) | 1995-06-05 | 1996-06-04 | Oral care ultramulsion based products |
| DE19630837.2 | 1996-07-31 | ||
| DE19640556.4 | 1996-10-01 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MXPA97005771A MXPA97005771A (en) | 1998-11-12 |
| MXPA02005771A true MXPA02005771A (en) | 2005-02-22 |
Family
ID=27541677
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MXPA02005771A MXPA02005771A (en) | 1995-06-05 | 1996-06-04 | Oral care ultramulsion based products. |
| MX9709735A MX9709735A (en) | 1995-06-05 | 1997-12-05 | Oral care ultramulsion based products. |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX9709735A MX9709735A (en) | 1995-06-05 | 1997-12-05 | Oral care ultramulsion based products. |
Country Status (8)
| Country | Link |
|---|---|
| EP (1) | EP0831762A4 (en) |
| JP (1) | JPH11506769A (en) |
| CN (1) | CN1190342A (en) |
| AU (1) | AU712266B2 (en) |
| BR (1) | BR9608343A (en) |
| CA (1) | CA2222407A1 (en) |
| MX (2) | MXPA02005771A (en) |
| WO (1) | WO1996039116A1 (en) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0955836B1 (en) * | 1996-07-25 | 2003-10-29 | Whitehill Oral Technologies Inc. | Toothbrush with improved cleaning and abrasion efficiency |
| DE19721590A1 (en) * | 1997-05-23 | 1998-11-26 | Henkel Ecolab Gmbh & Co Ohg | Non-drying, viscous surface treatment agent |
| US6190706B1 (en) * | 1997-12-23 | 2001-02-20 | Wm. Wrigley Jr. Company | Chewing gum and gum bases having reduced adhesion to environmental surfaces and method for making |
| US6596298B2 (en) * | 1998-09-25 | 2003-07-22 | Warner-Lambert Company | Fast dissolving orally comsumable films |
| BR0101911A (en) * | 2001-04-30 | 2002-12-24 | Johnson & Johnson Ind Com | Composition for oral hygiene |
| ES2390162T3 (en) * | 2003-06-30 | 2012-11-07 | Nihon Pharmaceutical Co., Ltd. | Method for preparing a stabilized menthol emulsion |
| WO2009067605A2 (en) * | 2007-11-21 | 2009-05-28 | The Procter & Gamble Company | Preparations, methods and kits useful for treatment of cough |
| TWI392514B (en) | 2010-01-29 | 2013-04-11 | Colgate Palmolive Co | A dentifrice with high microbial efficacy and no fluoride and anionic surfactant |
| US20130230469A1 (en) * | 2010-11-12 | 2013-09-05 | Colgate-Palmolive Company | Oral Care Product and Methods of Use and Manufacture Thereof |
| US9149528B2 (en) | 2011-10-13 | 2015-10-06 | Premier Dental Products Company | Topical vitamin D oral supplement compositions |
| US9877930B2 (en) | 2012-10-12 | 2018-01-30 | Premier Dental Products Company | Topical ubiquinol oral supplement compositions with amorphous calcium phosphate |
| CN109908157A (en) * | 2012-10-12 | 2019-06-21 | 第一牙科产品公司 | Vitamin D oral cavity supplement composition locally |
| US9724542B2 (en) * | 2012-10-12 | 2017-08-08 | Premier Dental Products Company | Remineralizing and desensitizing compositions, treatments and methods of manufacture |
| WO2014059143A1 (en) | 2012-10-12 | 2014-04-17 | Premier Dental Products Company | Topical vitamin d and ubiquinol oral supplement compositions |
| CN103646763A (en) * | 2013-11-28 | 2014-03-19 | 宝电电子(张家港)有限公司 | Transformer |
| CN106456515A (en) * | 2014-04-11 | 2017-02-22 | 第牙科产品公司 | Enamel protectant and repair toothpaste |
| JP2015224233A (en) * | 2014-05-29 | 2015-12-14 | サンメディカル株式会社 | Composition for tooth cleaning treatment |
| CN106573055B (en) | 2014-06-09 | 2021-03-23 | 广东科洛克生物医药集团有限公司 | Silicone-based biophotonic compositions and uses thereof |
| US10639242B1 (en) * | 2018-11-05 | 2020-05-05 | Inspired Material Solutions, LLC | Dimethicone-based oral varnish |
| EP3902523A1 (en) | 2018-12-29 | 2021-11-03 | 3M Innovative Properties Company | Oral articles and methods of use |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5057306A (en) * | 1983-11-06 | 1991-10-15 | Hill Ira D | Method of manufacturing oral hygiene gels |
| US5057307A (en) * | 1986-11-06 | 1991-10-15 | Hill Ira D | Method of relieving gum discomfort |
| US5098711A (en) * | 1988-11-14 | 1992-03-24 | Ira Hill | Method of treating the oral cavity with dental floss containing chemotherapeutic agents |
| US5380530A (en) * | 1992-12-29 | 1995-01-10 | Whitehill Oral Technologies | Oral care composition coated gum |
-
1996
- 1996-06-04 BR BR9608343A patent/BR9608343A/en not_active Application Discontinuation
- 1996-06-04 WO PCT/US1996/008714 patent/WO1996039116A1/en not_active Ceased
- 1996-06-04 CA CA 2222407 patent/CA2222407A1/en not_active Abandoned
- 1996-06-04 MX MXPA02005771A patent/MXPA02005771A/en unknown
- 1996-06-04 EP EP96917114A patent/EP0831762A4/en not_active Withdrawn
- 1996-06-04 CN CN96195388A patent/CN1190342A/en active Pending
- 1996-06-04 AU AU59787/96A patent/AU712266B2/en not_active Ceased
- 1996-06-04 JP JP9501219A patent/JPH11506769A/en active Pending
-
1997
- 1997-12-05 MX MX9709735A patent/MX9709735A/en not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| BR9608343A (en) | 1999-01-05 |
| CA2222407A1 (en) | 1996-12-12 |
| MX9709735A (en) | 1998-10-31 |
| EP0831762A1 (en) | 1998-04-01 |
| AU712266B2 (en) | 1999-11-04 |
| JPH11506769A (en) | 1999-06-15 |
| EP0831762A4 (en) | 1999-08-11 |
| CN1190342A (en) | 1998-08-12 |
| AU5978796A (en) | 1996-12-24 |
| WO1996039116A1 (en) | 1996-12-12 |
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