CN112822993A - Remineralization promoter for teeth and liquid oral composition containing same - Google Patents
Remineralization promoter for teeth and liquid oral composition containing same Download PDFInfo
- Publication number
- CN112822993A CN112822993A CN201980066451.6A CN201980066451A CN112822993A CN 112822993 A CN112822993 A CN 112822993A CN 201980066451 A CN201980066451 A CN 201980066451A CN 112822993 A CN112822993 A CN 112822993A
- Authority
- CN
- China
- Prior art keywords
- liquid oral
- oral composition
- oil
- moles
- ethylene oxide
- Prior art date
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- 239000007788 liquid Substances 0.000 title claims abstract description 58
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- PUZPDOWCWNUUKD-UHFFFAOYSA-M sodium fluoride Chemical compound [F-].[Na+] PUZPDOWCWNUUKD-UHFFFAOYSA-M 0.000 claims abstract description 26
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- IUVKMZGDUIUOCP-BTNSXGMBSA-N quinbolone Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H]([C@]4(C=CC(=O)C=C4CC3)C)CC[C@@]21C)C1=CCCC1 IUVKMZGDUIUOCP-BTNSXGMBSA-N 0.000 description 1
- AZJPTIGZZTZIDR-UHFFFAOYSA-L rose bengal Chemical compound [K+].[K+].[O-]C(=O)C1=C(Cl)C(Cl)=C(Cl)C(Cl)=C1C1=C2C=C(I)C(=O)C(I)=C2OC2=C(I)C([O-])=C(I)C=C21 AZJPTIGZZTZIDR-UHFFFAOYSA-L 0.000 description 1
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- 239000000377 silicon dioxide Substances 0.000 description 1
- 239000001509 sodium citrate Substances 0.000 description 1
- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 1
- AJPJDKMHJJGVTQ-UHFFFAOYSA-M sodium dihydrogen phosphate Chemical group [Na+].OP(O)([O-])=O AJPJDKMHJJGVTQ-UHFFFAOYSA-M 0.000 description 1
- 229940080264 sodium dodecylbenzenesulfonate Drugs 0.000 description 1
- 229940075560 sodium lauryl sulfoacetate Drugs 0.000 description 1
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 1
- 159000000000 sodium salts Chemical class 0.000 description 1
- 229960000776 sodium tetradecyl sulfate Drugs 0.000 description 1
- UAJTZZNRJCKXJN-UHFFFAOYSA-M sodium;2-dodecoxy-2-oxoethanesulfonate Chemical compound [Na+].CCCCCCCCCCCCOC(=O)CS([O-])(=O)=O UAJTZZNRJCKXJN-UHFFFAOYSA-M 0.000 description 1
- UPUIQOIQVMNQAP-UHFFFAOYSA-M sodium;tetradecyl sulfate Chemical compound [Na+].CCCCCCCCCCCCCCOS([O-])(=O)=O UPUIQOIQVMNQAP-UHFFFAOYSA-M 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
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- 239000000600 sorbitol Substances 0.000 description 1
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- 235000019721 spearmint oil Nutrition 0.000 description 1
- 235000019411 steviol glycoside Nutrition 0.000 description 1
- 229930182488 steviol glycoside Natural products 0.000 description 1
- 150000008144 steviol glycosides Chemical class 0.000 description 1
- 235000019202 steviosides Nutrition 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 150000005846 sugar alcohols Chemical class 0.000 description 1
- BDHFUVZGWQCTTF-UHFFFAOYSA-M sulfonate Chemical compound [O-]S(=O)=O BDHFUVZGWQCTTF-UHFFFAOYSA-M 0.000 description 1
- 239000002344 surface layer Substances 0.000 description 1
- 239000008399 tap water Substances 0.000 description 1
- 235000020679 tap water Nutrition 0.000 description 1
- 229940104261 taurate Drugs 0.000 description 1
- 229960000790 thymol Drugs 0.000 description 1
- UAXOELSVPTZZQG-UHFFFAOYSA-N tiglic acid Natural products CC(C)=C(C)C(O)=O UAXOELSVPTZZQG-UHFFFAOYSA-N 0.000 description 1
- 229940034610 toothpaste Drugs 0.000 description 1
- 239000000606 toothpaste Substances 0.000 description 1
- MBDOYVRWFFCFHM-UHFFFAOYSA-N trans-2-hexenal Natural products CCCC=CC=O MBDOYVRWFFCFHM-UHFFFAOYSA-N 0.000 description 1
- 229960002622 triacetin Drugs 0.000 description 1
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- 239000011782 vitamin Substances 0.000 description 1
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- 239000000811 xylitol Substances 0.000 description 1
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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
- A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
- A61K8/20—Halogens; Compounds thereof
- A61K8/21—Fluorides; Derivatives thereof
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/39—Derivatives containing from 2 to 10 oxyalkylene groups
-
- 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
- A61K8/86—Polyethers
-
- 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)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Birds (AREA)
- Oral & Maxillofacial Surgery (AREA)
- Emergency Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Inorganic Chemistry (AREA)
- Cosmetics (AREA)
Abstract
The invention provides a tooth remineralization promoter which efficiently exerts tooth remineralization promotion effect by fluorine, and a liquid oral composition containing the same. A liquid oral composition comprising (A) sodium fluoride and (B) one or more selected from polyoxyethylene lauryl ethers in which the average molar number of addition of ethylene oxide is 10 to 25 moles and polyoxyethylene alkyl ethers in which the average molar number of addition of ethylene oxide is 7 to 17 moles and the carbon number of an alkyl group is 14 to 16, and the liquid oral composition further comprising (C) polyoxyethylene hydrogenated castor oil in which the average molar number of addition of ethylene oxide is 40 to 100. An agent for promoting tooth remineralization which comprises the components (A) and (B) and is used in a liquid oral composition, and an agent for promoting tooth remineralization which further comprises the component (C).
Description
Technical Field
The present invention relates to a tooth remineralization promoter which efficiently and sufficiently exerts a tooth remineralization promoting effect by fluorine, and a liquid oral composition containing the same.
Background
Fluorine-containing compounds such as sodium fluoride have an effect of promoting remineralization of teeth by fluorine, and are widely used in oral compositions such as dentifrice compositions. In order to effectively act on teeth and prevent dental caries, it is important to retain fluorine ions on teeth, and for example, a mode of blending a polymer compound is used in a dentifrice composition such as toothpaste in order to improve retention. However, when a polymer compound is added to a liquid oral composition such as a mouth wash, the feeling of use and stability of the preparation may be impaired, and therefore, it is difficult to adopt a method using a polymer compound, and a technique for efficiently exhibiting a tooth remineralization promoting effect by fluorine of a fluorine-containing compound without depending on a polymer compound has been desired.
Patent document 1 (jp 2009-155218 a) proposes that by adding a silica-based abrasive and a polyoxyethylene alkyl ether having an average molar number of addition of ethylene oxide of 15 to 25 or a polyoxyethylene hydrogenated castor oil having an average molar number of addition of ethylene oxide of 40 to 80 to a dentifrice composition containing sodium fluoride at a specific ratio, and adding a specific cellulose derivative such as hydroxyethyl cellulose, the retention in the oral cavity of sodium fluoride is improved, and moldability and liquid separation stability are obtained. Patent document 2 (jp 2015-117215 a) proposes a dentifrice composition in which sodium fluoride, a hydroxyethylcellulose dimethyldiallylammonium salt (ヒドロキシエチルセルロースジメチルジアリルアンモニウム salt), and a polyoxyethylene hydrogenated castor oil having an average molar number of addition of 10 to 30 of ethylene oxide and a polyoxyethylene alkyl ether having an average molar number of addition of 8 or less of ethylene oxide are mixed in a specific ratio in combination to improve retention of fluorine ions in the oral cavity.
Documents of the prior art
Patent document
Patent document 1: japanese laid-open patent publication No. 2009-155218
Patent document 2: japanese patent laid-open publication No. 2015-117215
Patent document 3: japanese laid-open patent publication No. 2009-46449
Patent document 4: japanese examined patent publication (Kokoku) No. 7-96492
Patent document 5: japanese laid-open patent publication No. 11-209254
Patent document 6: japanese patent laid-open publication No. 2016-199473
Disclosure of Invention
Problems to be solved by the invention
The present invention has been made in view of the above circumstances, and an object thereof is to provide a tooth remineralization promoter which efficiently and sufficiently exerts a tooth remineralization promoting effect by fluorine, and a liquid oral composition containing the same.
Means for solving the problems
The present inventors have made intensive studies to achieve the above object, and as a result, have found that when sodium fluoride (a) as a fluorine-containing compound is used in combination with a specific polyoxyethylene alkyl ether (B) described below, the remineralization promoting effect of the component (a) is efficiently exhibited, and the above effect is improved and excellent, and by using the components (a) and (B) in combination and blending the components in a liquid oral composition, the remineralization promoting effect of teeth is excellent, and the feeling of use and the stability of appearance can be secured, and have completed the present invention.
More specifically, the present inventors have made studies on surfactants as an important factor for improving the retention of fluorine on teeth by a liquid oral composition without depending on a polymer compound. As a result, although the nonionic surfactant polyoxyethylene alkyl ether hardly shows a tooth remineralization promoting effect, it has been found that, surprisingly, when the component (B) having an average molar number of addition of ethylene oxide within a specific range is used in combination with the component (a) as a polyoxyethylene alkyl ether for a liquid oral composition, the retention of the component (a) on teeth is improved and a tooth remineralization promoting effect by fluorine is efficiently and sufficiently exhibited by the component (B), and the remineralization rate can be improved. In this case, when a polyoxyethylene alkyl ether, which is not suitable in terms of the average addition mole number of ethylene oxide although it is a polyoxyethylene alkyl ether, is used in combination with the component (a), the following problems occur: the remineralization promoting effect of teeth is low and cannot be improved; further, the refreshing feeling after the oral administration and discharge is reduced, or turbidity is generated after storage, and the appearance stability is also deteriorated. However, when the component (B) is used in combination with the component (a), the remineralization promoting effect of teeth can be improved while maintaining the feeling of use and the appearance stability by preventing the decrease in refreshing feeling and the generation of turbidity as described above. In addition, this can provide an excellent remineralization promoting effect even in a liquid oral composition in which fluorine is less likely to accumulate on teeth.
As shown in comparative examples described later, in comparative examples 1 to 4 in which a polyoxyethylene lauryl ether or polyoxyethylene cetyl ether having an inappropriate average addition mole number of ethylene oxide was used in combination with component (a), the remineralization acceleration effect was low, and was at the same level as that of comparative example 5 in which component (a) was not contained, and the feeling of use (feeling of freshness) was poor and the appearance stability (degree of opaqueness of turbidity) was not good. On the other hand, as shown in examples, the liquid oral composition of the present invention containing the components (a) and (B) is excellent in remineralization promoting effect and also good in feeling of use (refreshing feeling) and appearance stability (degree of opaqueness).
In patent documents 3 to 5 (Japanese patent laid-open publication No. 2009-46449, Japanese patent publication No. 7-96492, and Japanese patent laid-open publication No. 11-209254), the stability of dextranase and the effect of inhibiting tartar formation, the bactericidal activity of cetylpyridinium chloride, and the like are improved by polyoxyethylene alkyl ether having an average number of moles of ethylene oxide added of 10 or more in a liquid oral composition. In patent document 6 (jp 2016-199473) the adhesion of isopropylmethylphenol to a container in a dentifrice composition containing isopropylmethylphenol and a nonionic surfactant is suppressed by a fluorine compound. In contrast, the present invention can provide a liquid oral composition having an excellent effect of enhancing the tooth remineralization promotion effect of the component (a) by the component (B) and having an excellent remineralization promotion effect.
Accordingly, the present invention provides the following liquid oral composition and dental remineralization promoter.
[ 1] A liquid oral composition comprising:
(A) sodium fluoride, and
(B) one or more selected from polyoxyethylene lauryl ether having an average addition mole number of ethylene oxide of 10 to 25 moles, and polyoxyethylene alkyl ether having an average addition mole number of ethylene oxide of 7 to 17 moles and a carbon number of an alkyl group of 14 to 16.
[ 2] the liquid oral composition according to [ 1], wherein,
(B) the component (A) is selected from polyoxyethylene lauryl ether with the average addition mole number of ethylene oxide being 15-25 moles and polyoxyethylene cetyl ether with the average addition mole number of ethylene oxide being 10-15 moles.
[ 3] the liquid oral combination according to [ 1] or [ 2], wherein,
the liquid oral composition contains 0.01-0.2% by mass of component (A) and 0.05-0.3% by mass of component (B).
[ 4] the liquid oral composition according to any one of [ 1] to [ 3], wherein,
and (B)/(A) is 2-15 by mass ratio.
[ 5] the liquid oral composition according to any one of [ 1] to [ 4], wherein,
the liquid oral composition further contains (C) 0.1-0.4 mass% of polyoxyethylene hydrogenated castor oil with an average addition mole number of ethylene oxide of 40-100 moles.
[ 6 ] the liquid oral composition according to any one of [ 1] to [ 5], wherein,
the liquid oral composition is a mouthwash composition.
[ 7 ] A tooth remineralization promoter for a liquid oral composition, which comprises:
(A) sodium fluoride, and
(B) one or more selected from polyoxyethylene lauryl ether having an average addition mole number of ethylene oxide of 10 to 25 moles, and polyoxyethylene alkyl ether having an average addition mole number of ethylene oxide of 7 to 17 moles and a carbon number of an alkyl group of 14 to 16.
[ 8 ] the dental remineralization promoter according to [ 7 ], wherein,
and (B)/(A) is 2-15 by mass ratio.
[ 9 ] the dental remineralization promoter according to [ 7 ] or [ 8 ], wherein,
the tooth remineralization promoter further contains (C) polyoxyethylene hydrogenated castor oil with the average addition mole number of ethylene oxide of 40-100 moles.
Effects of the invention
The present invention can provide a tooth remineralization promoter that efficiently exerts a tooth remineralization promoting effect by fluorine, and a liquid oral composition containing the same. The liquid oral composition of the present invention can provide excellent tooth remineralization promoting effects while maintaining the feeling of use and the stability of appearance, and is effective for preventing or inhibiting dental caries.
Detailed Description
The present invention will be described in more detail below, and in the present invention, one or more selected from the group consisting of (a) sodium fluoride and (B) polyoxyethylene lauryl ether having an average number of moles of ethylene oxide added (hereinafter abbreviated as E.O) of 10 to 25 moles and polyoxyethylene alkyl ether having 7 to 17 moles of e.o. and having 14 to 16 carbon atoms in the alkyl group are used in combination. In this case, the components (a) and (B) function as effective components for promoting remineralization of teeth.
In the present invention, the components (a) and (B) can be used in combination as an effective component for promoting tooth remineralization, and a tooth remineralization promoter comprising these effective components can be used, and the tooth remineralization promoter can be obtained by blending two components, but if necessary, other known components for oral use other than these components may be contained within a range not to impair the effects of the present invention.
The above tooth remineralization promoter can be incorporated into a liquid oral composition, particularly a mouth wash.
The liquid oral composition of the present invention contains the components (a) and (B), and the remineralization promoting effect of teeth is enhanced by using these components in combination.
(A) The amount of sodium fluoride is preferably 0.01 to 0.2% by mass of the entire composition (hereinafter the same applies). The larger the amount of the composition, the more the effect of promoting tooth remineralization is improved, but when the composition is too much, the risk of eating by mistake increases, and when the composition is 0.2% or less, the risk of eating by mistake can be sufficiently prevented.
(B) The component (A) is selected from polyoxyethylene lauryl ether with E.O. of 10-25 mol and polyoxyethylene alkyl ether with E.O. of 7-17 mol and alkyl with 14-16 carbon atoms. Examples of the polyoxyethylene alkyl ether having an alkyl group with 14 to 16 carbon atoms include polyoxyethylene cetyl ether and polyoxyethylene tetradecyl ether. These may be used singly or in combination of two or more.
Here, the polyoxyethylene lauryl ether has an e.o. of 10 to 25 mol, preferably 15 to 25 mol, and more preferably 15 to 20 mol, from the viewpoint of the effect of promoting remineralization of teeth. Further, the E.O. of the polyoxyethylene alkyl ether having 14 to 16 carbon atoms in the alkyl group is 7 to 17 moles, preferably 10 to 15 moles, and more preferably 15 moles, from the viewpoint of the effect of promoting remineralization of teeth. When the e.o. content is within the above range, the tooth remineralization promoting effect is excellent, and when the e.o. content is less than the lower limit value or exceeds the upper limit value, the tooth remineralization promoting effect is not excellent. In addition, the appearance stability is impaired or the feeling in use is reduced.
(B) The component (c) is particularly preferably polyoxyethylene lauryl ether and polyoxyethylene cetyl ether each having an e.o. value within the above range, and among them, polyoxyethylene cetyl ether is preferable in terms of not showing any unpleasant odor when it is contained in the mouth.
As the component (a), specifically, EMALEX710, 712, 715, 720, 725, 107, 110, 112, 115, 117 manufactured by NIHON emulosion co.
(B) The amount of the component (B) is preferably 0.05 to 0.3%, more preferably 0.1 to 0.2% of the total composition. When the content is 0.05% or more, a sufficient tooth remineralization promoting effect is obtained, and the appearance stability can be sufficiently maintained. When the content is 0.3% or less, the remineralization promoting effect can be sufficiently maintained, and the feeling of use can be sufficiently maintained. If the content exceeds 0.3%, the remineralization promoting effect may be reduced, and the refreshing feeling after discharge may be impaired.
In the present invention, (B)/(A) representing the ratio of the amounts of the component (A) and the component (B) in terms of mass ratio is preferably 2 to 15, and more preferably 3 to 10. When the amount is within the above range, the tooth remineralization promoting effect is more excellent, and the feeling of use and the appearance stability are sufficiently maintained. When the amount is less than 2, the tooth remineralization promoting effect may be reduced, and when the amount is more than 15, the refreshing feeling after discharge may be reduced, and the feeling of use may not be maintained.
The liquid oral composition of the present invention preferably further contains (C) polyoxyethylene hydrogenated castor oil.
As the polyoxyethylene hydrogenated castor oil (C), polyoxyethylene hydrogenated castor oil having an e.o. of 40 to 100 moles can be used from the viewpoint of the feeling of use and the appearance stability, and among them, polyoxyethylene hydrogenated castor oil having an e.o. of 60 to 100 moles is preferable.
As the component (C), NIKKOL HCO-40, 60, 80 and 100 manufactured by Nikkol chemical Co., Ltd can be specifically used.
When the component (C) is used, the amount of the component (C) is preferably 0.1 to 0.4% of the total composition. When the amount is within the above range, the appearance stability is further improved, and the remineralization promoting effect of teeth is not impaired. When the content is 0.4% or less, the feeling of use can be sufficiently maintained. When the amount of the additive is too large, the refreshing feeling after the discharge may be reduced.
In addition to the components (B) and (C), surfactants other than these may be blended, and for example, an anionic surfactant may be blended.
Specific examples of the anionic surfactant include: alkyl sulfates such as sodium lauryl sulfate and sodium tetradecyl sulfate; n-acyl sarcosinates such as N-lauroyl sarcosinate sodium and N-myristoyl sarcosinate sodium; n-acyl glutamates such as sodium dodecylbenzenesulfonate, sodium hydrogenated coconut fatty acid monoglyceride monosulfate, sodium lauryl sulfoacetate, and sodium N-palmitoyl glutamate; sodium N-methyl-N-acyl taurate, sodium N-methyl-N-acyl alanine and sodium alpha-olefin sulfonate. The anionic surfactant can be blended within a range that does not impair the remineralization promoting effect of teeth and the feeling of use, and the preferred blending amount is 0.05 to 0.3%, particularly 0.1 to 0.2%, of the entire composition.
The liquid oral composition of the present invention uses purified water as a solvent, and may be mixed with a lower monohydric alcohol such as ethanol. In particular, the content of ethanol is 10% or less, particularly preferably 8% or less, of the total composition from the viewpoint of suppressing irritation, and may not be blended, that is, the content of ethanol is 0%. Preparations substantially free of lower monohydric alcohols, particularly ethanol (the content of ethanol is 0.1% or less, preferably 0.01% or less of the total composition) are suitable as low-irritation type preparations. In the present invention, even in the case of a liquid oral composition containing substantially no ethanol at a low ethanol concentration, the composition can maintain the stability of appearance and has an excellent effect of promoting tooth remineralization.
The liquid oral compositions of the present invention can be prepared and used as mouthwashes, liquid dentifrices, mouth fresheners, and are particularly suitable as mouthwash compositions. Further, according to the form of the preparation, the purpose of use, and the like, it is possible to incorporate, as necessary, an appropriate known component other than the above components. Specifically, a humectant, a preservative, a sweetener, a colorant, a perfume, a pH adjuster, an active ingredient, and the like are blended. In general, insoluble solid components such as abrasives are not blended in liquid oral compositions such as mouth washes.
The liquid oral composition of the present invention can provide an excellent effect of promoting tooth remineralization even if it does not contain a polymer compound, and from the viewpoint of feeling of use, when a water-soluble polymer compound such as a cellulose derivative is added, the content thereof is preferably 0.1% or less, and more preferably not added (the content is 0%).
Examples of the wetting agent include: sugar alcohols such as sorbitol, xylitol and erythritol, and polyols such as glycerol, ethylene glycol and polyethylene glycol having an average molecular weight of 160 to 400 (average molecular weight described in ministerial drug substance standard 2006). The amount of the wetting agent is usually 5 to 50%.
Examples of the preservative include: parabens, benzoic acid or its sodium salt, and the like. Examples of the sweetener include: sodium saccharin, steviol glycosides, and the like.
Examples of the colorant include: highly safe water-soluble coloring matters such as blue No. 1, green No. 3, yellow No. 4, and red No. 105.
As the flavor, the following known flavor materials for oral compositions can be used in combination, but the flavor is not limited to those described in examples: natural flavors such as peppermint oil, spearmint oil, fennel oil, eucalyptus oil, wintergreen oil, cinnamon oil, clove oil, thyme oil, sage oil, lemon oil, orange oil, peppermint oil, cardamom oil, coriander oil, orange peel oil, lime berry oil, lavender oil, rosemary oil, bay oil, chamomile oil, caraway oil, marjoram oil, mandarin oil, lemongrass oil, oregano oil, pine leaf oil, orange flower oil, rose oil, jasmine oil, grapefruit oil, platinum grapefruit oil, iris extractum, mint essential oil, rose essential oil, orange flower oil, and the like; the natural perfume is processed (pre-fraction removal, post-fraction removal, fractionation, liquid-liquid extraction, essence, powdery perfume, etc.); and unit flavors such as menthol, carvone, anethole, eucalyptol, methyl salicylate, cinnamaldehyde, eugenol, 3-l-menthoxypropane-1, 2-diol, thymol, linalool, linalyl acetate, limonene, menthone, menthyl acetate, N-substituted-p-menthane-3-carboxamide, pinene, octanal, citral, pulegone, carvone acetate, anisaldehyde, ethyl acetate, ethyl butyrate, allyl cyclohexanepropionate, methyl anthranilate, ethyl methylphenylglycidylate, vanillin, undecalactone, hexanal, butanol, isoamyl alcohol, hexenol, dimethyl sulfide, cyclamic acid, furfural, trimethyl pyrazine, ethyl lactate, ethyl thioacetate; and blending flavors such as strawberry flavor, apple flavor, banana flavor, pineapple flavor, grape flavor, mango flavor, butter flavor, milk flavor, fruit mix flavor, tropical fruit flavor, and the like.
The amount of the perfume is not particularly limited, and the above perfume raw material is preferably used in an amount of 0.000001 to 1% in the composition, and an aromatizing perfume using the above perfume raw material in an amount of 0.1 to 2% in the composition.
In the present invention, the pH at 25 ℃ is preferably adjusted to 5.5 to 8.0, and a composition of sodium dihydrogen phosphate and sodium monohydrogen phosphate, or citric acid and sodium citrate may be added as a pH adjusting agent in the vicinity thereof.
As the optional active ingredients, there may be mentioned: examples of the pharmaceutically effective components other than the component (A) include allantoin, water-soluble vitamins, and water-soluble anti-inflammatory agents. The amount of these additives is an effective amount in a range not to impair the effects of the present invention.
The tooth remineralization promoter of the present invention comprises a combination of (A) sodium fluoride and (B) one or more members selected from the group consisting of polyoxyethylene lauryl ether having 10 to 25 moles of E.O. and polyoxyethylene alkyl ether having 7 to 17 moles of E.O. and 14 to 16 carbon atoms in the alkyl group, as effective components for promoting tooth remineralization.
In this case, the details of the components (a) and (B), for example, the details of the specific substances used, the ratio of the amounts, the amounts to be blended, and the like, are preferably the same as those described above with respect to the liquid oral composition. The details of other components that can be further blended are the same as those described above with respect to the liquid oral composition.
The present invention will be specifically described below by way of examples, comparative examples and formulation examples, but the present invention is not limited to the following examples. In the following examples, unless otherwise specified,% represents% by mass.
[ examples and comparative examples ]
Liquid oral compositions (mouthwashes) having compositions shown in tables 1 to 3 were prepared by a conventional method and evaluated by the following method. The results are also shown in the table.
POE is an abbreviation for polyoxyethylene, and the value in () described later is the number of moles of e.o.
< evaluation method >
(1) Method for evaluating remineralization promoting effect
According to journal of oral hygiene society (oral student )54 authored by escort-yi et al: 2-8, 2004, the following experiments were carried out.
1. Preparation of demineralized samples
The enamel portion of the bovine tooth was cross-divided by a hard tissue cutter (ISOMET 2000, manufactured by Buehler Co., Ltd.) to make 4 enamel blocks per tooth. The enamel surfaces of these blocks were mirror ground, covered with nail polish, and exposed about a 4mm x 4mm window (test face). The enamel block was immersed in a demineralizing solution having the following composition, and allowed to stand at 37 ℃ for 3 days to form an artificial skinned demineralizing lesion, thereby obtaining a demineralizing sample.
Composition of the demineralization solution: (pH4.5)
(1L in distilled water in such a manner as to attain the above concentration.)
2. Preparation of remineralized samples
The demineralised samples (5 pieces in each group) were immersed in the test composition (liquid oral composition) for 5 minutes 2 times per day (about 9 and 18 points). For the demineralized samples after impregnation, after a Window face was brushed with a toothbrush (PC CLINICA LION BRUSS standard, manufactured by LION king corporation) for about 10 strokes, the sample was washed with running tap water for about 30 seconds, and then the pieces were immersed one by one in 10mL of a remineralization solution having the following composition and maintained at 37 ℃. The remineralizing solution consisted of plaque solution similar to that after 30 minutes of sucrose intake, supplemented with an acid phosphatase with MFPase activity (from P-3627 wheat), prepared and replaced 2 times per day. This series of operations was continued for 14 days, thereby preparing a remineralization-treated sample.
Composition of remineralizing solution: (pH6.0)
(1L in distilled water in such a manner as to attain the above concentration.)
3. Determination of mineral loss by Contact microradiopraph (CMR, Soft X-ray Generator)
< preparation of measurement section >
The non-demineralized, and remineralized samples were resin-embedded with N ═ 3 (rigalac 2004: permak N: PROMOTER E ═ 120: 1: 1, manufactured by Okenshoji co., ltd.) and cured, and then cut from the test surface in a vertical direction with a thickness of 300 μm using a hard tissue cutter (ISOMET 2000, manufactured by Buehler), and the cut surfaces were ground using an automatic grinder (SPEED WRAP (スピードラップ) ML-150DC, marto INSTRUMENT co., ltd.), thereby producing cut pieces with a thickness of about 150 μm.
< measurement of mineral loss amount >
CMR imaging was performed using a soft X-ray generator (CMR-III, manufactured by Softex Co., Ltd.) along with a standard sample for measuring a mineral amount for image analysis (aluminum ladder: 15 th) under conditions of a current of 3mA, a voltage of 20kV, and an X-ray irradiation time of 20 minutes from the cross-sectional direction of each slice (SO-343, manufactured by Kodak Co., Ltd.). The image pickup was performed by taking a CMR image including a region from the surface layer of the test surface to the subsurface demineralization part with a camera (HD camera model HQ-130, manufactured by Nikon, Ltd.) under a microscope (Optiphoto T2, manufactured by Nikon, Ltd.). The image was directly inputted to a computer, and the image was analyzed by image analysis software (WinRoof V3.0, manufactured by Mitani Co., Ltd.),the method of Angmar is performed based on the gray scale values in a region 50 μm wide (direction parallel to the test surface) and 300 μm long (depth direction from the test surface) after the gray scale processing (256 gray scales)*The mineral loss (. DELTA.Z; vol%. mu.m) was calculated. In the above calculation, the gradation values of the background and undemineralized samples were set to 0 vol% and 100 vol%, respectively, for analysis.
A first step of; method of Angmar
Angmar,B.,Carlstrome,D.and Glas,J.E.:Studies on the ultrastructure of dental enamel.IV.The mineralization of normal human enamel.J Ultrastructural Res,8:12~23,1963.
4. Calculation of the remineralization Rate
The mineral loss amount Δ Za of the demineralized sample and the mineral loss amount Δ Zb of the remineralized sample were measured, and the remineralization rate X (%) was calculated from these values by the following formula, and the remineralization promoting effect was evaluated according to the following evaluation criteria. The results were rated as "O" or more.
X=(ΔZa-ΔZb)/ΔZa×100
Evaluation criteria:
very good: the remineralization rate is more than 60 percent;
o: the remineralization rate is more than 50% and less than 60%;
and (delta): the remineralization rate is more than 40% and less than 50%;
x: the remineralization rate is lower than 40 percent.
(2) Method for evaluating feeling of use (refreshing feeling)
About 10mL of a test sample (liquid oral composition) was put into the mouth of 10 subjects, and the refreshing feeling at the time of spitting was evaluated according to the following 4-point scale. The average score of 10 persons was obtained and expressed as ∈,. smallcircle,. DELTA.. times.according to the following criteria.
Grading standard:
and 4, dividing: after the spitting, a strong refreshing feeling was felt.
And 3, dividing: the user feels a little refreshing feeling after spitting.
And 2, dividing: after the spitting, the refreshing feeling was hardly felt.
1 minute: no refreshing feeling was felt after the discharge.
And (3) judging standard:
very good: the average score is more than 3.5 and less than 4.0;
o: the average score is more than 3.0 and less than 3.5;
and (delta): the average score is more than 2.0 and less than 3.0;
x: the average score was less than 2.0.
(3) Evaluation method of appearance stability
450mL of a test specimen (liquid oral composition) was filled in a colorless transparent PET container (manufactured by Jiye industries) filled with 500mL of the test specimen and stored in a thermostatic bath at 50 ℃ for one month, and then the degree of opaqueness of turbidity was visually judged by the following 4-degree scale. The 3 samples were evaluated to obtain average scores, and evaluated according to the following evaluation criteria, expressed as "excellent", "Δ", and "x". It is to be noted that the liquid oral composition just prepared is clear.
Grading standard:
and 4, dividing: there was no turbidity at all.
And 3, dividing: there was substantially no turbidity.
And 2, dividing: there was little turbidity.
1 minute: there was a lot of turbidity.
Evaluation criteria:
very good: the average score is more than 3.5 and less than 4.0;
o: the average score is more than 3.0 and less than 3.5;
and (delta): the average score is more than 2.0 and less than 3.0;
x: the average score was less than 2.0.
TABLE 1
TABLE 2
TABLE 3
Next, formulation examples are shown. The liquid oral composition (mouth wash) of the formulation example was excellent in the effect of promoting remineralization, and also good in the feeling of use (refreshing feeling) and the stability of appearance. As described later, the evaluation results of the liquid oral composition (mouthwash) using flavors B to E instead of flavor a were also good.
Formulation example 1 mouthwash
(B) (A) (mass ratio) 5
Formulation example 2 mouthwash
(B) (A) (mass ratio) 5
[ formulation example 3] mouthwash
(B) (A) (mass ratio) 5
[ formulation example 4] mouthwash
(B) (A) (mass ratio) 5
[ formulation example 5] mouthwash
(B) (A) (mass ratio) 5
The fragrances A to E shown in tables 4 to 12 were used as the fragrances.
TABLE 4
TABLE 5
Essence 1 | Mass portion of |
Linalool | 1 |
Menthol furans | 1 |
Anethole | 1 |
Menthones | 1 |
Menthyl acetate | 1 |
Total up to | 5 |
TABLE 6
Essence 2 | Mass portion of |
Orange oil | 1 |
Orange essential oil (80% removal of front cut) | 1 |
Lemon oil | 1 |
Lemon essential oil (front cut 95% removed) | 1 |
Pear berry oil | 1 |
Orange peel oil | 1 |
Pomelo oil | 1 |
Citral | 1 |
Decanal | 1 |
Total up to | 9 |
TABLE 7
Essence 3 | Mass portion of |
Fennel oil | 1 |
Eucalyptus oil | 1 |
Cinnamon oil | 1 |
Clove oil | 1 |
Thyme oil | 1 |
Sage oil | 1 |
Cardamom oil | 1 |
Coriander oil | 1 |
Rosemary oil | 1 |
Laurel oil | 1 |
Chrysanthemum oil | 1 |
Carex oil | 1 |
Basil oil | 1 |
Total up to | 13 |
TABLE 8
Essence 4 | Mass portion of |
Wintergreen oil | 1 |
Mastic oil | 1 |
Lavender oil | 1 |
Bitter orange flower oil (neroli oil) | 1 |
LemonGrass oil | 1 |
Jasmine oil | 1 |
Rose oil | 1 |
Iris oil | 1 |
Vanilla | 1 |
Total up to | 9 |
TABLE 9
Essence 5 | Mass portion of |
3-1-menthoxypropane-1, 2-diol | 1 |
Menthyl glyceryl ethers | 1 |
Herba Cancriniae Lasiocarpae extract (containing 70% of herba Cancriniae Lasiocarpae alcohol) | 1 |
Linalool oxide | 1 |
Vanillyl butyl ether | 1 |
Isopulegol | 1 |
Capsicum extract | 1 |
Ginger extract | 1 |
Pepper extract | 1 |
Total up to | 9 |
Watch 10
Essence 6 | Mass portion of |
Maltol | 1 |
Ethyl maltol | 1 |
Vanillin | 1 |
Ethyl vanillin | 1 |
Furanones | 1 |
Ethyl cyclopentenolone | 1 |
3-hydroxy-4, 5-dimethylfuran-2-one | 1 |
Cyclodulcin | 1 |
2-methyl butyric acid | 1 |
Acetic acid | 1 |
Propionic acid | 1 |
Total up to | 11 |
TABLE 11
Essence 7 | Mass portion of |
p-methoxy cinnamic aldehyde | 1 |
Cis-3-hexenol | 1 |
Trans-2-hexenal | 1 |
Undecalactones | 1 |
Decanolide | 1 |
Butyric acid ethyl ester | 1 |
Acetic acid isoamyl ester | 1 |
Benzaldehyde | 1 |
Acetic acid hexyl ester | 1 |
2-methyl butyric ester | 1 |
Benzyl alcohol | 1 |
Alpha-terpineol | 1 |
Linalyl acetate | 1 |
Phenyloxirane carboxylic acid ethyl ester | 1 |
Phenylethyl alcohol | 1 |
Allyl caproate | 1 |
Octanol (I) | 1 |
Cinnamic acid methyl ester | 1 |
Heptynecarboxylic acid methyl ester | 1 |
Ionones | 1 |
Beta-methylthio-lactic acid acetic acid | 1 |
Cis-6-nonenol | 1 |
7-methyl-3, 5-dihydro-2H-benzodiazepine-3-ones | 1 |
Jasmonic acid methyl ester | 1 |
Total up to | 24 |
TABLE 12
Solvent(s) | Mass portion of |
Ethanol | 1 |
Propylene glycol | 1 |
Glycerin fatty acid ester | 1 |
Triacetin | 1 |
Total up to | 4 |
Claims (9)
1. A liquid oral composition comprising:
(A) sodium fluoride, and
(B) one or more selected from polyoxyethylene lauryl ether having an average addition mole number of ethylene oxide of 10 to 25 moles, and polyoxyethylene alkyl ether having an average addition mole number of ethylene oxide of 7 to 17 moles and a carbon number of an alkyl group of 14 to 16.
2. The liquid oral composition of claim 1,
(B) the component (A) is selected from polyoxyethylene lauryl ether with the average addition mole number of ethylene oxide being 15-25 moles and polyoxyethylene cetyl ether with the average addition mole number of ethylene oxide being 10-15 moles.
3. The liquid oral composition of claim 1 or 2,
the liquid oral composition contains 0.01-0.2% by mass of component (A) and 0.05-0.3% by mass of component (B).
4. The liquid oral composition according to any one of claims 1 to 3,
and (B)/(A) is 2-15 by mass ratio.
5. The liquid oral composition of any one of claims 1 to 4,
the liquid oral composition further contains (C) 0.1-0.4 mass% of polyoxyethylene hydrogenated castor oil with an average addition mole number of ethylene oxide of 40-100 moles.
6. The liquid oral composition of any one of claims 1 to 5,
the liquid oral composition is a mouthwash composition.
7. A tooth remineralization promoter for a liquid oral composition comprising:
(A) sodium fluoride, and
(B) one or more selected from polyoxyethylene lauryl ether having an average addition mole number of ethylene oxide of 10 to 25 moles, and polyoxyethylene alkyl ether having an average addition mole number of ethylene oxide of 7 to 17 moles and a carbon number of an alkyl group of 14 to 16.
8. The dental remineralization promoter according to claim 7, wherein,
and (B)/(A) is 2-15 by mass ratio.
9. The dental remineralization promoter according to claim 7 or 8, wherein,
the tooth remineralization promoter further contains (C) polyoxyethylene hydrogenated castor oil with the average addition mole number of ethylene oxide of 40-100 moles.
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JP2018-190612 | 2018-10-09 | ||
JP2018190612 | 2018-10-09 | ||
PCT/JP2019/038888 WO2020075586A1 (en) | 2018-10-09 | 2019-10-02 | Tooth remineralization-promoting agent and liquid composition for oral cavity comprising same |
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CN112822993B CN112822993B (en) | 2024-01-26 |
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JP (1) | JP7405087B2 (en) |
KR (1) | KR20210071934A (en) |
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JP7405087B2 (en) | 2023-12-26 |
WO2020075586A1 (en) | 2020-04-16 |
KR20210071934A (en) | 2021-06-16 |
CN112822993B (en) | 2024-01-26 |
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