NL9000639A - Caries inhibiting tooth-paste, mouth-wash etc. - contg. cpds. with at least one phosphate gp. and alkyl gp. with at least 12 carbon atoms - Google Patents
Caries inhibiting tooth-paste, mouth-wash etc. - contg. cpds. with at least one phosphate gp. and alkyl gp. with at least 12 carbon atoms Download PDFInfo
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- NL9000639A NL9000639A NL9000639A NL9000639A NL9000639A NL 9000639 A NL9000639 A NL 9000639A NL 9000639 A NL9000639 A NL 9000639A NL 9000639 A NL9000639 A NL 9000639A NL 9000639 A NL9000639 A NL 9000639A
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- Prior art keywords
- oral care
- phosphate
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- carbon atoms
- care agent
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- 229910019142 PO4 Inorganic materials 0.000 title claims abstract description 8
- 239000010452 phosphate Substances 0.000 title claims abstract description 8
- 239000000606 toothpaste Substances 0.000 title claims description 18
- 229940034610 toothpaste Drugs 0.000 title claims description 13
- 125000004432 carbon atom Chemical group C* 0.000 title claims description 11
- 239000002324 mouth wash Substances 0.000 title claims description 6
- 229940051866 mouthwash Drugs 0.000 title claims description 4
- 208000002925 dental caries Diseases 0.000 title abstract description 10
- 125000000217 alkyl group Chemical group 0.000 title abstract description 5
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 title abstract description 4
- 230000002401 inhibitory effect Effects 0.000 title description 5
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerol Natural products OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims abstract description 10
- -1 glycol ester Chemical class 0.000 claims abstract description 7
- 239000004386 Erythritol Substances 0.000 claims abstract description 5
- 229940009714 erythritol Drugs 0.000 claims abstract description 5
- 239000001177 diphosphate Substances 0.000 claims abstract description 4
- LYCAIKOWRPUZTN-UHFFFAOYSA-N ethylene glycol Natural products OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims abstract description 4
- WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 claims abstract description 3
- UNXHWFMMPAWVPI-UHFFFAOYSA-N Erythritol Natural products OCC(O)C(O)CO UNXHWFMMPAWVPI-UHFFFAOYSA-N 0.000 claims abstract 2
- 235000019414 erythritol Nutrition 0.000 claims abstract 2
- 150000001875 compounds Chemical class 0.000 claims description 23
- 239000008375 oral care agent Substances 0.000 claims description 16
- 125000002467 phosphate group Chemical group [H]OP(=O)(O[H])O[*] 0.000 claims description 12
- 239000002562 thickening agent Substances 0.000 claims description 8
- KRHYYFGTRYWZRS-UHFFFAOYSA-M Fluoride anion Chemical compound [F-] KRHYYFGTRYWZRS-UHFFFAOYSA-M 0.000 claims description 7
- 230000000675 anti-caries Effects 0.000 claims description 4
- 235000011180 diphosphates Nutrition 0.000 claims description 4
- 239000000203 mixture Substances 0.000 claims description 4
- 239000000654 additive Substances 0.000 claims description 2
- 239000011230 binding agent Substances 0.000 claims description 2
- XPPKVPWEQAFLFU-UHFFFAOYSA-J diphosphate(4-) Chemical compound [O-]P([O-])(=O)OP([O-])([O-])=O XPPKVPWEQAFLFU-UHFFFAOYSA-J 0.000 claims description 2
- 239000000499 gel Substances 0.000 claims 2
- LAYXSTYJRSVXIH-UHFFFAOYSA-N LysoPA(18:0/0:0) Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)COP(O)(O)=O LAYXSTYJRSVXIH-UHFFFAOYSA-N 0.000 claims 1
- 239000008365 aqueous carrier Substances 0.000 claims 1
- 239000008135 aqueous vehicle Substances 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 abstract description 4
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 abstract 1
- PUZPDOWCWNUUKD-UHFFFAOYSA-M sodium fluoride Chemical compound [F-].[Na+] PUZPDOWCWNUUKD-UHFFFAOYSA-M 0.000 description 12
- 230000000694 effects Effects 0.000 description 7
- 239000000796 flavoring agent Substances 0.000 description 7
- 235000019634 flavors Nutrition 0.000 description 7
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 7
- 239000011775 sodium fluoride Substances 0.000 description 6
- 235000013024 sodium fluoride Nutrition 0.000 description 6
- XGRSAFKZAGGXJV-UHFFFAOYSA-N 3-azaniumyl-3-cyclohexylpropanoate Chemical compound OC(=O)CC(N)C1CCCCC1 XGRSAFKZAGGXJV-UHFFFAOYSA-N 0.000 description 5
- 229940091249 fluoride supplement Drugs 0.000 description 5
- 229960004711 sodium monofluorophosphate Drugs 0.000 description 5
- 239000000126 substance Substances 0.000 description 5
- QZTLXVHLRNYBHP-UHFFFAOYSA-N (1,2-dihydroxy-4-oxohenicosan-3-yl) dihydrogen phosphate Chemical compound P(=O)(O)(O)OC(C(O)CO)C(CCCCCCCCCCCCCCCCC)=O QZTLXVHLRNYBHP-UHFFFAOYSA-N 0.000 description 4
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 4
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical group [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 4
- 238000002360 preparation method Methods 0.000 description 4
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 4
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- 210000003298 dental enamel Anatomy 0.000 description 3
- 150000002222 fluorine compounds Chemical class 0.000 description 3
- 239000004088 foaming agent Substances 0.000 description 3
- 150000003013 phosphoric acid derivatives Chemical class 0.000 description 3
- 208000006558 Dental Calculus Diseases 0.000 description 2
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 description 2
- 239000003082 abrasive agent Substances 0.000 description 2
- 229940112822 chewing gum Drugs 0.000 description 2
- 235000015218 chewing gum Nutrition 0.000 description 2
- 235000003599 food sweetener Nutrition 0.000 description 2
- 239000003906 humectant Substances 0.000 description 2
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 description 2
- 210000000214 mouth Anatomy 0.000 description 2
- 229910052814 silicon oxide Inorganic materials 0.000 description 2
- 239000003765 sweetening agent Substances 0.000 description 2
- YUOWTJMRMWQJDA-UHFFFAOYSA-J tin(iv) fluoride Chemical compound [F-].[F-].[F-].[F-].[Sn+4] YUOWTJMRMWQJDA-UHFFFAOYSA-J 0.000 description 2
- 239000000811 xylitol Substances 0.000 description 2
- 235000010447 xylitol Nutrition 0.000 description 2
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 description 2
- 229960002675 xylitol Drugs 0.000 description 2
- NOOLISFMXDJSKH-UTLUCORTSA-N (+)-Neomenthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@@H]1O NOOLISFMXDJSKH-UTLUCORTSA-N 0.000 description 1
- NCKMMSIFQUPKCK-UHFFFAOYSA-N 2-benzyl-4-chlorophenol Chemical compound OC1=CC=C(Cl)C=C1CC1=CC=CC=C1 NCKMMSIFQUPKCK-UHFFFAOYSA-N 0.000 description 1
- DDFHBQSCUXNBSA-UHFFFAOYSA-N 5-(5-carboxythiophen-2-yl)thiophene-2-carboxylic acid Chemical compound S1C(C(=O)O)=CC=C1C1=CC=C(C(O)=O)S1 DDFHBQSCUXNBSA-UHFFFAOYSA-N 0.000 description 1
- 108010011485 Aspartame Proteins 0.000 description 1
- 206010006326 Breath odour Diseases 0.000 description 1
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 description 1
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 1
- GHXZTYHSJHQHIJ-UHFFFAOYSA-N Chlorhexidine Chemical compound C=1C=C(Cl)C=CC=1NC(N)=NC(N)=NCCCCCCN=C(N)N=C(N)NC1=CC=C(Cl)C=C1 GHXZTYHSJHQHIJ-UHFFFAOYSA-N 0.000 description 1
- 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 1
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 1
- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 description 1
- YCKRFDGAMUMZLT-UHFFFAOYSA-N Fluorine atom Chemical compound [F] YCKRFDGAMUMZLT-UHFFFAOYSA-N 0.000 description 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
- 229920002125 Sokalan® Polymers 0.000 description 1
- XEFQLINVKFYRCS-UHFFFAOYSA-N Triclosan Chemical compound OC1=CC(Cl)=CC=C1OC1=CC=C(Cl)C=C1Cl XEFQLINVKFYRCS-UHFFFAOYSA-N 0.000 description 1
- 230000009471 action Effects 0.000 description 1
- WNROFYMDJYEPJX-UHFFFAOYSA-K aluminium hydroxide Chemical compound [OH-].[OH-].[OH-].[Al+3] WNROFYMDJYEPJX-UHFFFAOYSA-K 0.000 description 1
- PNEYBMLMFCGWSK-UHFFFAOYSA-N aluminium oxide Inorganic materials [O-2].[O-2].[O-2].[Al+3].[Al+3] PNEYBMLMFCGWSK-UHFFFAOYSA-N 0.000 description 1
- 239000000605 aspartame Substances 0.000 description 1
- IAOZJIPTCAWIRG-QWRGUYRKSA-N aspartame Chemical compound OC(=O)C[C@H](N)C(=O)N[C@H](C(=O)OC)CC1=CC=CC=C1 IAOZJIPTCAWIRG-QWRGUYRKSA-N 0.000 description 1
- 235000010357 aspartame Nutrition 0.000 description 1
- 229960003438 aspartame Drugs 0.000 description 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 description 1
- 229910052794 bromium Inorganic materials 0.000 description 1
- JUNWLZAGQLJVLR-UHFFFAOYSA-J calcium diphosphate Chemical compound [Ca+2].[Ca+2].[O-]P([O-])(=O)OP([O-])([O-])=O JUNWLZAGQLJVLR-UHFFFAOYSA-J 0.000 description 1
- 239000001506 calcium phosphate Substances 0.000 description 1
- 229910000389 calcium phosphate Inorganic materials 0.000 description 1
- 235000011010 calcium phosphates Nutrition 0.000 description 1
- 229940043256 calcium pyrophosphate Drugs 0.000 description 1
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 1
- 230000000248 cariostatic effect Effects 0.000 description 1
- 239000000679 carrageenan Substances 0.000 description 1
- 235000010418 carrageenan Nutrition 0.000 description 1
- 229920001525 carrageenan Polymers 0.000 description 1
- 229940113118 carrageenan Drugs 0.000 description 1
- 229920006184 cellulose methylcellulose Polymers 0.000 description 1
- 229960003260 chlorhexidine Drugs 0.000 description 1
- AZSFNUJOCKMOGB-UHFFFAOYSA-K cyclotriphosphate(3-) Chemical compound [O-]P1(=O)OP([O-])(=O)OP([O-])(=O)O1 AZSFNUJOCKMOGB-UHFFFAOYSA-K 0.000 description 1
- 230000009849 deactivation Effects 0.000 description 1
- 239000008121 dextrose Substances 0.000 description 1
- 235000019821 dicalcium diphosphate Nutrition 0.000 description 1
- 235000019820 disodium diphosphate Nutrition 0.000 description 1
- GYQBBRRVRKFJRG-UHFFFAOYSA-L disodium pyrophosphate Chemical compound [Na+].[Na+].OP([O-])(=O)OP(O)([O-])=O GYQBBRRVRKFJRG-UHFFFAOYSA-L 0.000 description 1
- 239000000975 dye Substances 0.000 description 1
- UNXHWFMMPAWVPI-ZXZARUISSA-N erythritol Chemical class OC[C@H](O)[C@H](O)CO UNXHWFMMPAWVPI-ZXZARUISSA-N 0.000 description 1
- 229910052731 fluorine Inorganic materials 0.000 description 1
- 239000011737 fluorine Substances 0.000 description 1
- 229960001031 glucose Drugs 0.000 description 1
- 230000006872 improvement Effects 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 230000002701 inhibitory effect on caries Effects 0.000 description 1
- 229910052500 inorganic mineral Inorganic materials 0.000 description 1
- 229910052816 inorganic phosphate Inorganic materials 0.000 description 1
- 239000001525 mentha piperita l. herb oil Substances 0.000 description 1
- 239000001683 mentha spicata herb oil Substances 0.000 description 1
- 229940041616 menthol Drugs 0.000 description 1
- 125000005341 metaphosphate group Chemical group 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 239000011707 mineral Substances 0.000 description 1
- 235000010755 mineral Nutrition 0.000 description 1
- 210000003739 neck Anatomy 0.000 description 1
- ZVVSSOQAYNYNPP-UHFFFAOYSA-N olaflur Chemical compound F.F.CCCCCCCCCCCCCCCCCCN(CCO)CCCN(CCO)CCO ZVVSSOQAYNYNPP-UHFFFAOYSA-N 0.000 description 1
- 229960001245 olaflur Drugs 0.000 description 1
- 239000006072 paste Substances 0.000 description 1
- 235000019477 peppermint oil Nutrition 0.000 description 1
- 239000000049 pigment Substances 0.000 description 1
- 230000007505 plaque formation Effects 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- CVHZOJJKTDOEJC-UHFFFAOYSA-N saccharin Chemical compound C1=CC=C2C(=O)NS(=O)(=O)C2=C1 CVHZOJJKTDOEJC-UHFFFAOYSA-N 0.000 description 1
- 235000019204 saccharin Nutrition 0.000 description 1
- 229940081974 saccharin Drugs 0.000 description 1
- 239000000901 saccharin and its Na,K and Ca salt Substances 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- FQENQNTWSFEDLI-UHFFFAOYSA-J sodium diphosphate Chemical compound [Na+].[Na+].[Na+].[Na+].[O-]P([O-])(=O)OP([O-])([O-])=O FQENQNTWSFEDLI-UHFFFAOYSA-J 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 235000019721 spearmint oil Nutrition 0.000 description 1
- 230000000638 stimulation Effects 0.000 description 1
- 150000005846 sugar alcohols Polymers 0.000 description 1
- 229920003002 synthetic resin Polymers 0.000 description 1
- 239000000057 synthetic resin Substances 0.000 description 1
- RYCLIXPGLDDLTM-UHFFFAOYSA-J tetrapotassium;phosphonato phosphate Chemical compound [K+].[K+].[K+].[K+].[O-]P([O-])(=O)OP([O-])([O-])=O RYCLIXPGLDDLTM-UHFFFAOYSA-J 0.000 description 1
- 235000019818 tetrasodium diphosphate Nutrition 0.000 description 1
- 229920001187 thermosetting polymer Polymers 0.000 description 1
- XROWMBWRMNHXMF-UHFFFAOYSA-J titanium tetrafluoride Chemical compound [F-].[F-].[F-].[F-].[Ti+4] XROWMBWRMNHXMF-UHFFFAOYSA-J 0.000 description 1
- 230000009466 transformation Effects 0.000 description 1
- 238000000844 transformation Methods 0.000 description 1
- 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 description 1
- 229960003500 triclosan Drugs 0.000 description 1
- 239000000341 volatile oil Substances 0.000 description 1
- 239000000230 xanthan gum Substances 0.000 description 1
- 235000010493 xanthan gum Nutrition 0.000 description 1
- 229920001285 xanthan gum Polymers 0.000 description 1
- 229940082509 xanthan gum Drugs 0.000 description 1
- 150000003752 zinc compounds Chemical class 0.000 description 1
- UHVMMEOXYDMDKI-JKYCWFKZSA-L zinc;1-(5-cyanopyridin-2-yl)-3-[(1s,2s)-2-(6-fluoro-2-hydroxy-3-propanoylphenyl)cyclopropyl]urea;diacetate Chemical compound [Zn+2].CC([O-])=O.CC([O-])=O.CCC(=O)C1=CC=C(F)C([C@H]2[C@H](C2)NC(=O)NC=2N=CC(=CC=2)C#N)=C1O UHVMMEOXYDMDKI-JKYCWFKZSA-L 0.000 description 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
- A61K8/55—Phosphorus compounds
-
- 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
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)
- Oral & Maxillofacial Surgery (AREA)
- Birds (AREA)
- Epidemiology (AREA)
- Cosmetics (AREA)
Abstract
Description
MondverzorgingsmiddelOral care product
De uitvinding heeft betrekking op een mondverzorgingsmiddel omvattende een fysiologisch aanvaardbare drager, en een hoeveelheid van een verbinding, die in staat is de cariësprogressie tegen te gaan.The invention relates to an oral care agent comprising a physiologically acceptable carrier and an amount of a compound capable of inhibiting caries progression.
Onder mondverzorgingsmiddelen worden die produkten verstaan, die die bij normaal gebruik niet of nauwelijks worden ingeslikt, maar wel gedurende enige tijd in de mondholte verblijven, waarbij het middel met vrijwel alle tandvlakken in intensief contact komt. Voorbeelden van dergelijke middelen zijn tandpasta's, tandpolishes, kauwgom, mondwaters en mondpoeders.Oral care products are those products that are not or hardly swallowed during normal use, but which remain in the oral cavity for some time, whereby the product comes into intensive contact with almost all dental surfaces. Examples of such agents are toothpastes, dental polishes, chewing gum, mouthwashes and mouth powders.
Het is bekend, dat het mogelijk is de cariësprogressie tegen te gaan door toevoeging van diverse verbindingen aan mondverzorgingsmiddelen. De meest bekende verbindingen zijn die welke fluoride ionen leveren, zoals NaF, tinfluoride, aminfluoride met lange keten en natriummonofluorfosfaat. De werking van dergelijke fluoride verbindingen berust op stimulatie van minerale transformaties in het tand-email.It is known that it is possible to combat caries progression by adding various compounds to oral care products. The most well-known compounds are those which provide fluoride ions, such as NaF, tin fluoride, long chain amine fluoride and sodium monofluorophosphate. The action of such fluoride compounds is based on stimulation of mineral transformations in the tooth enamel.
Ook is het bekend fosfaatverbindingen toe te voegen aan mondverzorgingsmiddelen. Bekende anorganische fosfaatverbindingen zijn trimetafosfaat en calciumfosfaat. Ook is het bekend organische fosfaatverbindingen toe te voegen aan mondverzorgingsmiddelen. Deze stoffen hechten sterk aan het tandglazuur, waarbij de oppervlaktespanning verlaagd wordt.It is also known to add phosphate compounds to oral care products. Known inorganic phosphate compounds are trimetaphosphate and calcium phosphate. It is also known to add organic phosphate compounds to oral care products. These substances adhere strongly to the tooth enamel, whereby the surface tension is reduced.
Dit zou de hechting van plaque aan het tandglazuur verminderen. Tevens zijn er indicaties, dat dergelijke verbindingen een cariostatische werking hebben.This would reduce the adhesion of plaque to the enamel. There are also indications that such compounds have a cariostatic effect.
Door Borggreven et al (Caries Res.15, 1989, pp 238-242) is aangegeven, dat 2-0-stearoyl-glycerol 1,3-difosfaat in vitro een remmende werking heeft op cariës. Gevonden is nu, dat verwante verbindingen een aanzienlijk betere werking vertonen.Borggreven et al (Caries Res.15, 1989, pp 238-242) indicate that 2-0-stearoyl-glycerol 1,3-diphosphate inhibits caries in vitro. It has now been found that related compounds exhibit a considerably better effect.
De onderhavige uitvinding beoogt een mondverzorgingsmiddel te verschaffen, waarin een verbinding is opgenomen met een goede werking tegen cariësprogressie. Tevens wordt beoogd een mondverzorgingsmiddel te verschaffen, dat een werking heeft tegen plaque, tegen tandsteen, slechte adem en/of tegen gevoeligheid van de tandhalzen voor pijnprikkels.The present invention contemplates providing an oral care agent incorporating a compound having good activity against caries progression. It is also intended to provide an oral care agent that has an effect against plaque, against tartar, bad breath and / or against the sensitivity of the dental necks to pain stimuli.
De uitvinding omvat derhalve een mondverzorgingsmiddel waarin is opgenomen een fysiologisch aanvaardbare drager en een tegen cariës effectieve hoeveelheid van ten minste één verbinding die voorzien is van ten minste één fosfaatgroep en ten minste één alkylrest met ten minste 12 koolstofatomen, waarbij het aantal fosfaatgroepen per molecuul ten hoogste gelijk is aan het aantal alkylresten met ten minste 12 koolstofatomen.The invention therefore encompasses an oral care agent incorporating a physiologically acceptable carrier and an anti-caries effective amount of at least one compound having at least one phosphate group and at least one alkyl radical with at least 12 carbon atoms, the number of phosphate groups per molecule highest is equal to the number of alkyl radicals with at least 12 carbon atoms.
Verrassenderwijs is gebleken, dat dergelijke verbindingen met een fosfaatgroep en een alkylrest met ten minste 12 koolstof atomen, en meer in het bijzonder tussen 16 en 22 koolstofatomen, een uitgesproken remmende werking hebben op cariës. Bij voorkeur worden verbindingen toegepast waarin het aantal fosfaatgroepen en het aantal alkylresten met ten minste 12 koolstof atomen gelijk is. Het was geenszins te verwachten dat door deze nadere definitie van de onderlinge verhouding van de alkyl- en de fosfaatgroepen een zo sterke verbetering van de cariës remmende werking verkregen zou kunnen worden, terwijl ook geen deactivering van de verbinding in het mondverzorgingsmiddel optreedt.Surprisingly, it has been found that such compounds with a phosphate group and an alkyl radical with at least 12 carbon atoms, and more particularly between 16 and 22 carbon atoms, have a pronounced inhibitory effect on caries. Preferably, compounds are used in which the number of phosphate groups and the number of alkyl radicals having at least 12 carbon atoms is equal. It was by no means to be expected that this further definition of the mutual ratio of the alkyl and the phosphate groups could achieve such a marked improvement in the anti-caries effect, nor would deactivation of the compound occur in the oral care product.
Geschikte verbindingen voor toepassing volgens de uitvinding zijn glycol-, glycerol- en erythritol-esters met fosfaat en alkylresten, zoals 2S,3S-0-distearoyl-erythritol 1,4 difosfaat, 2-0-stearoyl-propyleen-glycol-3-fosfaat en 1-0-stearoyl-glycerol-3-fosfaat.Suitable compounds for use according to the invention are glycol, glycerol and erythritol esters with phosphate and alkyl radicals, such as 2S, 3S-0-distearoyl-erythritol 1,4 diphosphate, 2-0-stearoyl-propylene-glycol-3-phosphate and 1-0-stearoyl-glycerol-3-phosphate.
Gebleken is, dat door toepassing van een fluoride bron in de mondverzorgingsmiddelen volgens de uitvinding nog een versterking van de werking van het middel verkregen kan worden. Daartoe kan men de gangbare fluoride leverende verbindingen toepassen in de daartoe bekende hoeveelheden.It has been found that by using a fluoride source in the oral care preparations according to the invention, an enhancement of the effect of the preparation can still be obtained. For this purpose, the conventional fluoride-providing compounds can be used in the amounts known for that purpose.
Een overzicht van de gangbare fluoride-leverende verbindingen is bij voorbeeld vermeld in EP-A 97476, waarvan de inhoud bij wijze van referentie hierin opgenomen is. Meer in het bijzonder past men natriumfluoride en/of natriummonofluorfosfaat toe, aangezien deze een goede werking vertonen. Eventueel kunnen ook andere fluoridebronnen worden toegepast, zoals tinfluoride, organische fluoriden, ammoniumfluoride, titaantetrafluoride en combinaties van twee of meer van de genoemde fluoriden.An overview of the common fluoride-providing compounds is given, for example, in EP-A 97476, the contents of which are incorporated by reference herein. More in particular, sodium fluoride and / or sodium monofluorophosphate are used, since they show good activity. Optionally, other fluoride sources may also be used, such as tin fluoride, organic fluorides, ammonium fluoride, titanium tetrafluoride and combinations of two or more of the said fluorides.
De hoeveelheid fluoride leverende verbinding wordt zodanig gekozen, dat in het mondverzorgingsmiddel 50 tot 3000 ppm aan fluoride berekend als F bevat. Het uiteindelijke gehalte aan fluor wordt ook bepaald door de aard van de drager. In tandpasta's past men liefst 1000-2000 ppm toe, in medicinale pasta's 1000-3000 ppm, in kindertandpasta's 50-1000 ppm, in mondwaters 100-1500 ppm en in kauwgom 50-500 ppm.The amount of the fluoride-providing compound is selected so that in the oral care agent contains 50 to 3000 ppm of fluoride calculated as F. The final fluorine content is also determined by the nature of the support. 1000-2000 ppm is used in toothpastes, 1000-3000 ppm in medicinal pastes, 50-1000 ppm in children's toothpastes, 100-1500 ppm in mouthwashes and 50-500 ppm in chewing gum.
In het mondverzorgingsmiddel kunnen desgewenst andere actieve verbindingen opgenomen worden.zoals pyrofosfaten of zinkverbindingen, welke de tandsteenvorming tegengaan. Bij voorkeur wordt een mengsel van tetrakalium-pyrofosfaat en tetranatriumpyrofosfaat of dinatrium-diwaterstofpyrofosfaat toegepast in hoevelheden van 0,1 tot 20 gew.%. Ook kunnen stoffen toegevoegd worden die de plaque vorming tegengaan, zoals xylitol, broom chlorofeen, triclosan, chloorhexidine en mengsels van twee of meer van deze stoffen in hoeveelheden van 0,1 tot 30 gew.%.If desired, other active compounds can be included in the oral care agent, such as pyrophosphates or zinc compounds, which counteract tartar formation. Preferably, a mixture of tetrapotassium pyrophosphate and tetrasodium pyrophosphate or disodium dihydrogen pyrophosphate is used in amounts from 0.1 to 20% by weight. Substances that prevent plaque formation can also be added, such as xylitol, bromine chlorophene, triclosan, chlorhexidine and mixtures of two or more of these substances in amounts of 0.1 to 30% by weight.
Als het mondverzorgingsmiddel een tandpasta is, bevat het ook een hoeveelheid schuurmiddel. Deze hoeveelheid kan variëren van ca. 10 tot ca. 70 gew.%. Als schuurmiddelen kunnen in principe alle geschikte schuurmiddelen toegepast worden, zoals silica, onoplosbare metafosfaten, calciumpyrofosfaat, thermohardende kunststofharsen, gehydrateerd alumina en dergelijke.If the oral care product is a toothpaste, it also contains an amount of abrasive. This amount can vary from about 10 to about 70% by weight. In principle, all suitable abrasives can be used as abrasives, such as silica, insoluble metaphosphates, calcium pyrophosphate, thermosetting synthetic resins, hydrated alumina and the like.
In tandpasta's wordt liefst ook 0,001 tot 5 gew.% schuimmiddel opgenomen. Een veel gebruikt schuimmiddel is natriumlaurylsulfaat, maar ook andere schuimmiddelen, zoals sarcosinaten kunnen worden toegepast.Preferably, 0.001 to 5% by weight of foaming agent is also included in toothpastes. A commonly used foaming agent is sodium lauryl sulfate, but other foaming agents, such as sarcosinates, can also be used.
Afhankelijk van de aard van het mondverzorgingsmiddel kunnen ook andere componenten aanwezig zijn, zoals, smaakstoffen, zoetstoffen, kleurstoffen en pigmenten.Depending on the nature of the oral care agent, other components may also be present, such as, flavors, sweeteners, dyes and pigments.
Geschikte smaakstoffen zijn bijvoorbeeld etherische oliën zoals pepermuntolie en kruizemuntolie. Tevens kan gebruik gemaakt worden van synthetische smaakstoffen zoals menthol. Zoetstoffen die toegepast kunnen worden zijn onder meer saccharine, dextrose, aspartaam en dergelijke. De hoeveelheden van deze stoffen zijn afhankelijk van de gewenste smaak en kunnen eenvoudig vastgesteld worden.Suitable flavors are, for example, essential oils such as peppermint oil and spearmint oil. Synthetic flavors such as menthol can also be used. Sweeteners that can be used include saccharin, dextrose, aspartame and the like. The amounts of these substances depend on the desired taste and can be easily determined.
Andere eventueel aanwezige componenten zijn polyhydrische alcoholen zoals glycerol, sorbitol, xylitol, propyleenglycol en dergelijke in hoeveelheden van 0,1 tot 50 gew,%.Other optional components are polyhydric alcohols such as glycerol, sorbitol, xylitol, propylene glycol and the like in amounts from 0.1 to 50% by weight.
In bepaalde gevallen kan het gewenst zijn een verdikkingsmiddel toe te passen. Dit kan gebruikt worden in een hoeveelheid die in het algemeen 5 gew.% niet zal overschrijden. Geschikte verdikkingsmiddelen zijn CMC, xanthaangom, carrageenan, en carboxyvinylpolymeren.In some cases it may be desirable to use a thickener. This can be used in an amount which will generally not exceed 5% by weight. Suitable thickeners are CMC, xanthan gum, carrageenan, and carboxyvinyl polymers.
De drager van de mondverzorgingsmiddelen volgens de uitvinding wordt verder gevormd door water, eventueel gecombineerd met ethanol. De diverse componenten worden opgelost en/of gedispergeerd in het water, ter verkrijging van het gewenste produkt. De hoeveelheid water variëert van minder dan 5 gew.% tot 95 gew.%. Meer in het bijzonder is deze hoeveelheid gelegen tussen 10 en 60 gew.%.The carrier of the oral care preparations according to the invention is further formed by water, optionally combined with ethanol. The various components are dissolved and / or dispersed in the water to obtain the desired product. The amount of water ranges from less than 5 wt% to 95 wt%. More particularly, this amount is between 10 and 60% by weight.
Volgens een voorkeursuitvoeringsvorm van de uitvinding bestaat het mondverzorgingsmiddel uit 0,001 tot 5 gew.delen verbinding die voorzien is van ten minste één fosfaatgroep en ten minste één alkylrest met ten minste 12 koolstofatomen, 5 tot 95 gew.delen fysiologisch aanvaardbare drager, 50 tot 3000 ppm fluoride berekend als F 0 tot 70 gew.delen slijpmiddel, 0 tot 5 gew.delen verdikkingsmiddel, 0 tot 40 gew.delen vochtbindmiddel en 0 tot 10 gew.delen andere toevoegsels.According to a preferred embodiment of the invention, the oral care agent consists of 0.001 to 5 parts by weight of compound containing at least one phosphate group and at least one alkyl radical with at least 12 carbon atoms, 5 to 95 parts by weight of physiologically acceptable carrier, 50 to 3000 ppm fluoride calculated as F 0 to 70 parts by weight of abrasive, 0 to 5 parts by weight of thickener, 0 to 40 parts by weight of moisture binder and 0 to 10 parts by weight of other additives.
De diverse stoffen die toegepast kunnen worden in de mondverzorgingsmiddelen volgens de uitvinding zijn in het algemeen in de handel verkrijgbare produkten. De verbinding die ten minste één alkylgroep en ten minste één fosfaatgroep bevat kan op eenvoudige wijze bereid worden, bijvoorbeeld analoog aan de methode beschreven door Borggreven in de reeds geciteerde publicatie.The various substances which can be used in the oral care preparations according to the invention are generally commercially available products. The compound containing at least one alkyl group and at least one phosphate group can be prepared in a simple manner, for example, analogous to the method described by Borggreven in the cited publication.
De uitvinding wordt nu toegelicht aan de hand van enkele voorbeelden, echter zonder daartoe beperkt te zijn.The invention is now elucidated by means of a few examples, but without being limited thereto.
VOORBEELD 1EXAMPLE 1
Een tandpasta werd bereid uitgaande van de in de tabel opgegeven componenten. Deze tandpasta werd vervolgens beproefd ten aanzien van de cariës remmende werking, welke duidelijk verbeterd bleek te zijn in vergelijking met een tandpasta die niet de stearoyl-glycerol-fosfaat bevatte.A toothpaste was prepared from the components listed in the table. This toothpaste was then tested for its caries inhibiting effect, which was found to be clearly improved compared to a toothpaste that did not contain the stearoyl glycerol phosphate.
TABEL 1TABLE 1
Aluminiumhydroxide 35 %Aluminum hydroxide 35%
Natriumlaurylsulfaat 2 %Sodium lauryl sulfate 2%
Humectant 20 %Humectant 20%
Natriumfluoride 0,24 %Sodium fluoride 0.24%
Natriummonofluorfosfaat 0,76 5Sodium monofluorophosphate 0.76 5
Aroma 1 % l-O-stearoyl-glycerol-3-fosfaat 0,7 %Flavor 1% l-O-stearoyl-glycerol-3-phosphate 0.7%
Verdikkingsmiddelen 5 %Thickeners 5%
Water tot 100 % VOORBEELD 2Water up to 100% EXAMPLE 2
Een tandpasta werd bereid uitgaande van de in de tabel opgegeven componenten. Deze tandpasta werd vervolgens beproefd ten aanzien van de cariës remmende werking, welke duidelijk verbeterd bleek te zijn in vergelijking met een tandpasta die niet de stearoyl-glycerol-fosfaat bevatte.A toothpaste was prepared from the components listed in the table. This toothpaste was then tested for its caries inhibiting effect, which was found to be clearly improved compared to a toothpaste that did not contain the stearoyl glycerol phosphate.
TABEL 2TABLE 2
Siliciumoxide 20 %Silicon oxide 20%
Natriumlaurylsulfaat 2 %Sodium lauryl sulfate 2%
Verdikkingsmiddelen 5 %Thickeners 5%
Natriumfluoride 0,24 %Sodium fluoride 0.24%
Natriummonofluorfosfaat 0,76 %Sodium monofluorophosphate 0.76%
Pyrofosfaten 8 % l-0-stearoyl-glycerol-3-fosfaat 1 %Pyrophosphates 8% l-0-stearoyl-glycerol-3-phosphate 1%
Aroma 2 %Flavor 2%
Water tot 100 % VOORBEELD 3Water up to 100% EXAMPLE 3
Een transparante tandpasta werd bereid uitgaande van de in de tabel opgegeven componenten. Deze tandpasta werd vervolgens beproefd ten aanzien van de cariës remmende werking, welke duidelijk verbeterd bleek te zijn in vergelijking met een tandpasta die geen stearoyl-glycerol-fosfaat bevatte.A transparent toothpaste was prepared from the components listed in the table. This toothpaste was then tested for its caries inhibiting effect, which was found to be clearly improved compared to a toothpaste containing no stearoyl glycerol phosphate.
TABEL 3TABLE 3
Siliciumoxide 20 %Silicon oxide 20%
Natriumlaurylsulfaat 2 %Sodium lauryl sulfate 2%
Humectant 35 %Humectant 35%
Natriumfluoride 0,24 %Sodium fluoride 0.24%
Natriummonofluorfosfaat 0,76 %Sodium monofluorophosphate 0.76%
Aroma 1,5 % l-O-stearoyl-glycerol-3-fosfaat 0,7 %Flavor 1.5% l-O-stearoyl-glycerol-3-phosphate 0.7%
Verdikkingsmiddelen 1,5 %Thickeners 1.5%
Water tot 100 % VOORBEELD 4Water up to 100% EXAMPLE 4
Een mondspoelmiddel werd bereid uitgaande van de in de tabel opgegeven componenten. Dit middel werd vervolgens beproefd ten aanzien van de cariës remmende werking, welke duidelijk verbeterd bleek te zijn in vergelijking met een middel dat geen stearoyl-glycerol-fosfaat bevatte.A mouthwash was prepared from the components listed in the table. This agent was then tested for its anti-caries effect, which was found to be clearly improved compared to an agent which did not contain stearoyl glycerol phosphate.
TABEL 4TABLE 4
Aroma 1 %Flavor 1%
Natriumfluoride 0,05 %Sodium fluoride 0.05%
Conserveringsmiddelen 0,5 % l-O-stearoyl-glycerol-3-fosfaat 0,2 % Alcohol 10 %Preservatives 0.5% l-O-stearoyl-glycerol-3-phosphate 0.2% Alcohol 10%
Water tot 100 %Water up to 100%
Claims (9)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| NL9000639A NL9000639A (en) | 1990-03-20 | 1990-03-20 | Caries inhibiting tooth-paste, mouth-wash etc. - contg. cpds. with at least one phosphate gp. and alkyl gp. with at least 12 carbon atoms |
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| NL9000639 | 1990-03-20 | ||
| NL9000639A NL9000639A (en) | 1990-03-20 | 1990-03-20 | Caries inhibiting tooth-paste, mouth-wash etc. - contg. cpds. with at least one phosphate gp. and alkyl gp. with at least 12 carbon atoms |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| NL9000639A true NL9000639A (en) | 1991-10-16 |
Family
ID=19856773
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NL9000639A NL9000639A (en) | 1990-03-20 | 1990-03-20 | Caries inhibiting tooth-paste, mouth-wash etc. - contg. cpds. with at least one phosphate gp. and alkyl gp. with at least 12 carbon atoms |
Country Status (1)
| Country | Link |
|---|---|
| NL (1) | NL9000639A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005039518A1 (en) * | 2003-10-16 | 2005-05-06 | Cerestar Holding B.V. | Oral compositions comprising erythritol for the treatment of dental-plaque and oral infections |
| EP1325737A4 (en) * | 2000-10-12 | 2005-07-27 | Kao Corp | Skin pore minimizers and skin elasticity improvers |
-
1990
- 1990-03-20 NL NL9000639A patent/NL9000639A/en not_active Application Discontinuation
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1325737A4 (en) * | 2000-10-12 | 2005-07-27 | Kao Corp | Skin pore minimizers and skin elasticity improvers |
| US7968607B2 (en) | 2000-10-12 | 2011-06-28 | Koa Corporation | Skin pore minimizers and skin elasticity improvers |
| WO2005039518A1 (en) * | 2003-10-16 | 2005-05-06 | Cerestar Holding B.V. | Oral compositions comprising erythritol for the treatment of dental-plaque and oral infections |
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