CN103987364B - Oral care composition comprising polyphenol - Google Patents
Oral care composition comprising polyphenol Download PDFInfo
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- CN103987364B CN103987364B CN201280057942.2A CN201280057942A CN103987364B CN 103987364 B CN103987364 B CN 103987364B CN 201280057942 A CN201280057942 A CN 201280057942A CN 103987364 B CN103987364 B CN 103987364B
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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
- A61K8/30—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
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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
- A61K8/30—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
- A61K8/342—Alcohols having more than seven atoms in an unbroken chain
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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
- A61K8/30—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
- A61K8/18—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
- A61K8/4973—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom
- A61K8/498—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom having 6-membered rings or their condensed derivatives, e.g. coumarin
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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
- A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
- A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
- A61K8/9783—Angiosperms [Magnoliophyta]
- A61K8/9789—Magnoliopsida [dicotyledons]
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- 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
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Abstract
The present invention relates to the method in oral care composition and sterilization oral cavity.We have found that, the oral care composition of the combination containing selective antimicrobial and polyphenol provides improved antimicrobial benefit.The combination astoundingly shows the synergy than independent effect what a order of magnitude of performance of the antimicrobial.
Description
Invention field
The present invention relates to the method in-kind of oral care composition and sterilization oral cavity.The present invention is mainly developed for oral cavity
Care composition and will be described with reference to these purposes below.It will be appreciated, however, that the present invention is not limited to this spy
Determine application.
Background and correlation technique
Oral hygiene is one of most important aspect in consumer personal care.Consumer all over the world uses different type
Product be used for MC.Generally with toothbrush and dentifrice composition, (which can be toothpaste or tooth to people at least twice daily
Powder) brushing teeth.By means of it is such brush teeth can ensure that by greatest extent reduce sleeping at night during or daytime when people enter
Food or the oral bacteria that accumulates in oral cavity during having a drink are keeping good oral hygiene.Brush teeth therefore subtract to greatest extent
The problem of such as decayed tooth, tartar, gingivitis, carious tooth and halitosis (bad breath) (also referred to as halitosis (halitosis)) is lacked.
Although brushing teeth daily twice, one or more of disease of many people with various forms of above names, this quilt
It is considered to act on the bacterial of oral mucosa by about 12 hours between brushing teeth twice.
To solve the problems, such as above-mentioned MC, method up to now be using synthetic (such as triclosan or alcohol), its
Thought to them it is to stimulate raw (harsh) by many consumers.Increasing consumer, especially recently, prefers to make
With the product containing natural materials.Additionally, in many countries, from angle of cultural or other, people are unwilling gargling at them
Alcohol used in saliva.
Improved antimicrobial efficacy is provided in the combination of antimicrobial known in oral care composition field.
US2007258996AA (The Sterilex Corporation) discloses a kind of antimicrobial compositions and use
In the method for the treatment of microorganism infection.This application teaching containing from sequestering agent, carbohydrate, terpenes, terpene, peptides,
It is independent in alkaloid, the oil of plant origin, dyes and dyestuffses, sulfonate, phenol, ester, aliphatic acid or dibenzofuran derivative
The antimicrobial compositions of the synergistic combination of three or more reagent for selecting.In described three or more reagent at least
Two kinds be not same type compound.
(Mitsui＆Co.Limited, 2000) discloses-kind of buccal spray compositions to EP1013261 A1, and which provides use
Halitosis is covered in long-time, and brings (refreshing) effect that significantly refreshes the mind.That application discloses one kind and contain tea
The composition of polyphenol, Menthol and/or 1- carvols.That application discloses a kind of composition containing high-level ethanol.Second
Alcohol is one of snap action and effective antimicrobial, but it is believed that it is irritating (harsh).In some culture
In, which is also considered as unacceptable.
We have found that, the oral care composition of the combination containing selective antimicrobial and polyphenol is provided and changed
The antimicrobial benefit entered.The combination astoundingly shows effect what a number than the independent performance of the antimicrobial
The synergy of magnitude.Advantageously, or even when the concentration very hour of antimicrobial also observes that this benefit, so as to
The problem produced in terms of avoiding the possible negative sensory due to this active component using high concentration.Also find simultaneously, should
Composition also provides anti-inflammatory benefit.
Goal of the invention
It is an object of the invention to overcome or improve at least one shortcoming of the prior art.By reference to this explanation
Book, other purposes of the present invention are will become clear from for those skilled in the art.
The content of the invention
According in a first aspect, disclosing a kind of oral care composition, which includes：
The antimicrobial of (i) 0.01 to 10wt%, selected from comprising thymol or terpineol or eugenol or geraniol
Active ingredients of essential oils；Triclosan or its mixture；
(ii) polyphenol of 0.1 to 5wt%；With,
(iii) the acceptable matrix in oral cavity；
Wherein described polyphenol includes at least 50% catechin.
According to second aspect, a kind of method in sterilization oral cavity is disclosed, which comprises the following steps：
A. the composition of first aspect present invention is applied to into oral cavity；And,
B. oral cavity is cleaned to being substantially free of the composition.
According to the third aspect, composition according to a first aspect of the present invention is disclosed for the purposes in oral cavity of sterilizing.
Detailed description of the invention
By reading following detailed description and appended claims, these and other aspects, features and advantages are for this
Field those of ordinary skill will become clear from.For avoidance of doubt, any feature of one aspect of the present invention can be used for
In terms of any other of the present invention.Word "comprising" means " including ", but not necessarily " consist of " or " by ... constitute ".Change
Sentence is talked about, the step of enumerate or option need not exhaustion.It should be noted that the example for being given in the following description is intended to explain
The bright present invention, it is therefore intended that limit the invention to these examples itself.Similarly, all of percentage is w/w
Percentage, unless otherwise stated.Except in operation and comparative example or expressly stated otherwise, in specification and claims
In book represent material amount or reaction condition, the physical property of material and/or using all numerals be interpreted as by word
" about " modify.The number range represented with form " x to y " is understood to include x and y.When for a special characteristic is with form
When " x to y " describes multiple preferred scopes, it is to be appreciated that be also contemplated for combining all scopes of different end points.
The oral care composition of the present invention includes the acceptable matrix in antimicrobial, polyphenol and oral cavity.
Antimicrobial
The oral care composition includes the antimicrobial of 0.01 to 10wt%, preferably 0.01 to 5wt%, more preferably
0.01 to 1wt%, even more preferably from 0.01 to 0.5wt% and further preferred 0.01 to 0.2wt%.The antimicrobial is selected from
Including thymol or the active ingredients of essential oils of terpineol or eugenol or geraniol；Triclosan (TCN) or its mixture.
The active ingredients of essential oils preferably includes thymol or terpineol or eugenol or its mixture.
Other optional active ingredients of essential oils are may include in the present compositions.These include but is not limited to salicylic acid
Pentyl ester, carvacrol, cymene such as p-cymene, dihydroeugenol, hexyl eugenol, 1-Hexyl salicylate, isoeugenol, methyl
Eugenol, methylisoeugenol, gaultherolin, tert-butyl group cresols and vanillic aldehyde or non-aromatic essential oil.Terpenoid it is non-
The example of volatile oil includes cedrene, cineole, citral (including geranial and neral), citronellal, citronellol, volatile oil extracted from eucalyptus' leaves or twigs
Smart (also referred to as 1,8 cineoles), to dihydro linalool (paradihydrolinalool), dihydromyrcenol (DH laurenes
Alcohol), fanesol, geraniol, jasminolene, hydroxycitronellol (hydroxycitronallol), laurine, different lemon
Lemon aldehyde, limonene, (R)-4-isopropenyl-1-methyl-1-cyclohexene, linalool, longifolene, menthol, nerol, nerolidol (nerolidiol), firpene, example
Such as australene, phellandrene, terpinenes, such as α-terpinenes and γ-terpinenes, terpineol, such as γ-terpineol and terpin -4-
Alcohol and 2,6-Dimethyl-2-octanol (THM).
Preferred composition contains the terpineol of 0.01 to 5wt%, the more preferably terpineol of 0.01 to 2wt%；0.01 to
The eugenol of the thymol and 0.001 to 2wt% of the thymol of 2wt%, more preferably 0.01 to 0.8wt%, more preferably 0.002
To the eugenol of 0.1wt%.
Triclosan is 2 ', 4,4 '-trichlorine, 2- hydroxyl-diphenyl ethers.Preferred composition includes 0.05 to 0.3wt%'s
Triclosan.
Polyphenol
The oral care composition includes the polyphenol containing at least catechin of 50wt% of 0.1 to 5wt%, preferably
0.2 to 4wt%, more preferably 0.5 to 4wt%, even more preferably from 1 to 3wt%, and the most preferably polyphenol of 1.0 to 2.5wt%.
Polyphenol is the one group of chemical substance found in plant, it is characterised in that there is more than one phenol in each molecule
Unit or construction unit (building block).Polyphenol be generally divided into hydrolyzable tanninses (gallate of carbohydrate) and
Phenylpropanoid Glycosides class (phenylpropanoids) such as lignin (Secoisolariciresinol bioside
(secoisolariciresinol diglycoside)), flavone compound, and the tannin of condensation.A maximum class and grind
It is flavone compound to study carefully widest polyphenol, and which includes thousand of kinds of compounds, including flavonols (Quercetin, zingiberol,
Kaempferol, myricetin, resveratrol, rutin), flavonoids (apiolin, cyanidenon), catechin (epicatechin, catechin
Gallate, theaflavin), flavanone (aurantiamarin, naringenin, silymarin (Silibenin), eriodictyol), anthocyanidin
Class (pelargonidin, peonidin, anthocyanidin, delphinidin, malvidin), osajin (daidzein, genistein,
Glycitein) and Coumarins (coumestrol).
Preferably, the polyphenol includes at least 60% catechin, more preferably at least 70%, still more preferably at least 80%
And most preferably 100% catechin.
Preferably, the catechin includes at least 25% Epigallo-catechin gallate (EGCG).
Preferably, the polyphenol extracts from green tea (Camellia sinensis).
The preferred commercially available polyphenol containing at least 60% catechin include Sunphenon90LB and
Sunphenon80SK (Taiyo Kagaku Co., Ltd).
The acceptable matrix in oral cavity
The oral care composition includes the acceptable matrix in oral cavity.The acceptable matrix in the oral cavity depends on described
The delivery form of oral care composition.Most suitable form is mouthwash, toothpaste or tooth powder.
The present inventor is desirable with being readily available and natural active component realizes antimicrobial efficacy, and wishes irreducible minimum
Antimicrobial of the degree ground using excitant (harsh), such as low-molecular-weight (C1To C3) alcohol, such as ethanol.Therefore, according to this
A bright preferred aspect, the composition are included and are less than 2wt%, more preferably less than 1wt%, still more preferably less than
Such alcohol of 0.5wt%, and it is desirable that in the composition, there is no low-molecular-weight (C1To C3) alcohol.
Mouthwash
When said composition is configured to mouthwash, the acceptable matrix in the oral cavity is water.It is of the invention to gargle
The desired antibiotic effect of water can not use low-molecular-weight (C1To C3) alcohol, for example ethanol or obtain during isopropanol, i.e., described group
Compound is substantially free of low-molecular-weight alcohol.Term is substantially free of low-molecular-weight alcohol and refers to that the alcohol can be not significantly affect micro- life
The amount that thing is killed is present.Preferably, exist in composition of the invention less than 2%, more preferably less than 1% C1To C3Alcohol, and most
Preferably there is no.
Therefore, according to an aspect of the present invention, there is provided antimicrobial mouthrinse composition, its include (a) 0.01 to
The antimicrobial of 10wt%, selected from the active ingredients of essential oils including thymol or terpineol or eugenol or geraniol；Trichlorine
Raw or its mixture；The polyphenol of (b) 0.1 to 5wt%, wherein the polyphenol includes at least 50% catechin；(c) 80 to
The water of 99.5wt%.
The mouthwash of the present invention preferably includes 0.05 to 10wt%, most preferably more preferably 0.05 to 8wt%, 0.5 to 5wt%
Surfactant.The surfactant is preferably cationic, anionic or amphoteric ion type, most preferably cation
Type.
When there is anion surfactant, which preferably is selected from the alkali metal of alkyl sulfonic acid, aliphatic acid or alkyl ether sulfate
Or alkali salt.
When there is zwitterionic surfactant, which preferably is selected from betaines, sulfobetaines bases
(sulphobetains), hydroxyl sulfo betaine class (hydroxyl sulphobetains) or aminocarboxylate.It is positive when existing
During ionic surface active agent, which is preferably benzalkonium chloride, alkyl pyridinium chloride or quaternary ammonium Shuangzi (gemini) surfactant.
After not diluted composition or dilute with water said composition, the mouthrinse composition of the present invention is used for
Sterilization oral cavity.In dilution step, composition is 1: 1 to 1: 200, more preferably 1: 5 to 1: 50 with the preferred weight ratio of water, further
More preferably 1: 15 to 1: 30 and preferably about 1: 20.
Toothpaste
The oral care composition can be delivered with toothpaste form.When composition is toothpaste, the oral cavity is subjected to
Matrix be abrasive material, which can be calcium carbonate or abrasive silica.When calcium carbonate is abrasive material, toothpaste is opaque paste
Form.When using abrasive silica, toothpaste is generally delivered with transparent gel form.
Toothpaste preferably includes the surfactant of 2 to the 15wt% of total composition, preferably 2.2 to 10wt%, and more preferably 2.5
To 5wt%.Preferred surfactant is anion or amphotericity.The anion surfactant is preferably alkali metal alkane
Base sulfate, more preferably NaLS (SLS).The mixture of anion surfactant can also be used.The both sexes
Surfactant is preferably glycine betaine, and more preferably (wherein alkyl is straight chain C to alkylamide propyl-betaine10-C18Chain), and
And most preferably Cocoamidopropyl betaine (CAPB).The mixture of amphoteric surfactant can also be used.
Opaque toothpaste：
Preferably, in opaque toothpaste, the acceptable matrix in oral cavity includes the calcium carbonate of 15 to 70wt%, more preferably
30 to 60wt%.Calcium carbonate (also referred to as chalk (chalk)) can be obtained in a variety of forms and some in these forms are in mouth
Used in the care composition of chamber.Two kinds of conventional forms are FGNC (fine grinding natural whiting (chalk)) and PCC (precipitation carbonic acid
Calcium).
In total chalk (chalk) content in oral care composition, FGNC generally with 35 to 100%, preferably 75 to
100% and especially 95 to 100% exist, balance of PCC.Typically, composition includes 30 to 65wt%, preferably 35 to
The FGNC of 55wt% and most preferably 40 to 55wt%.FGNC generally includes weight base median particle diameter and is preferably 1 to 15 μm, and more preferably 2
To 10 μm, and further preferred 4 to 7 μm of particle.
The composition may also include other known " non-chalk (no-chalk) " abrasive material to improve abrasive action.So
Abrasive material include dicalcium phosphate dihydrate (DCPD) and silica.
Except calcium carbonate, can be including abrasive silica for strengthening abrasive action in opaque toothpaste.When depositing
When, the composition includes 4 to 15wt%, preferably 6 to 12wt%, and the grinding dioxy of even more preferably 7 to 10wt%
SiClx.Alternatively, the composition may include 0.01 to 2wt%, preferably 0.1 to 0.8wt%, even more preferably 0.3 to
The perlite of 0.7wt%.
In opaque toothpaste, 15 to the 40wt% of composition, the preferably water of 20 to 30wt% are generally included.
Preferred composition includes wetting agent, such as xylitol, glycerine or D-sorbite.Glycerine and D-sorbite are special
Preferably.Preferably, the composition includes the wetting agent of 0.1 to 20wt%, more preferably 1 to 15wt%, most preferably 5 to
13wt%.
Preferably, the composition also includes alkali metal hydrogencarbonate.It is preferred that the alkali metal hydrogencarbonate is sodium salt.Institute
State the alkali metal hydrogencarbonate that composition preferably includes 1 to 30wt%, more preferably 2 to 20wt% and optimal 3 to 8wt%.
Gel dentifrice：
Gel dentifrice preferably includes abrasive silica.Preferred abrasive silica has 1.41 to 1.47 and more preferably
1.435 to 1.445 low-refraction.Preferably, the abrasive silica is with 5 to 15 microns of weight average particle diameter, 10 to
BET (nitrogen) surface areas and the oil absorption value of about 70-150cm3/100g of 100m2/g.Suitable low-refraction grinding titanium dioxide
The typical example of silicon is Tixosil63 and 73 (from Rhone Poulenc)；Sident10 (from Degussa)；
Zeodent113 (from Zeofinn)；Zeodent124 (from Huber), the Sorbosil AC systems provided by Crosfield
Row such as Sorbosil ACII, Sorbosil AC39 and SorbosilAC35, particularly SorbosilAC77 (from
Crosfield Chemicals).Amount of the silica in gel toothpaste composition be preferably 2 to 60wt%, usually 2 to
20wt%%, and more preferably 5 to 12wt%.
Thickening silica can be also mixed in gel dentifrice, usually the 4 to 12% of composition weight, and preferably 5 to 10%.
The example of the medium thickening silica of preference ranking includes MFIL (from Madhu Silica India), TC15 (from PQ
Corp UK), Zeodent165 (from Huber) or Tixosil43 (from Rhodia).
The 8 to 14% of composition weight is generally included in gel dentifrice, preferably 8 to 10% water.These water yields are not wrapped
The water mixed in said composition is included from the aqueous solution of other compositions (such as D-sorbite).
The toothpaste of opaque or gel type may also include caries preventive agent, adhesive, thickener, spices, stabilizer, polymerization
Thing, vitamin, buffer and antitartar agents.
Therefore, according to a preferred aspect of the present invention, there is provided dentifrice composition, which contains (a) 0.01 to 10wt%'s
Antimicrobial, selected from the active ingredients of essential oils for including thymol, terpineol, eugenol, geraniol；Triclosan or its mixing
Thing；The polyphenol of (b) 0.1 to 5wt%, wherein the polyphenol includes at least 50% catechin；The abrasive material of (c) 2 to 70wt%,
Selected from calcium carbonate or silica；(d) water of 8 to 40wt%.
Tooth powder
Tooth powder usually contains the abrasive material of very high percentage, preferably usual 90 to 99.9wt%, 90 to 95wt%.Chalk
(chalk) (FGNC) it is most preferred abrasive material, but can also uses PCC.
By including that anion surfactant such as NaLS is the desired amount of to provide in dentifrice composition
Foam.Preferably, the composition includes the surfactant of 2 to 3wt%.Other compositions, such as silica or single fluorophosphoric acid
Sodium can be included in the composition with up to 1wt%.
Sweetener such as xylitol, D-sorbite, glycerine or saccharin (sachharin) can be included.Spices such as spearmint
Or peppermint (peppermint) can be included with the amount of the 1wt% of up to dentifrice composition (spearmint).
According to another aspect of the invention, there is provided dentifrice composition, which contains the antimicrobial of (a) 0.01 to 10wt%
Agent, selected from the active ingredients of essential oils for including thymol, terpineol, eugenol, geraniol；Triclosan or its mixture；(b)0.1
To the polyphenol of 5wt%, wherein the polyphenol includes at least 50% catechin；(c) abrasive material of 90 to 99.5wt%, is selected from
Calcium carbonate or silica.
Therefore, in disclosed composition, the preferred water of the acceptable matrix in the oral cavity, silica or calcium carbonate.
PH buffer
The oral care composition preferably also includes pH buffer." pH buffer " is being referred herein to by a kind of chemical combination
The system that thing or compound combination are constituted,, when strong acid or alkali is added, pH value only slightly changes for which.Therefore, with without pH buffer
The same combination of agent is compared, and pH buffer presence in the composition causes its pH value to keep during the shelf life of composition
Longer period.Preferably, the pH of the oral care composition is 4 to 7.
Preferred pH buffer is selected from citric acid, sodium citrate or its mixture.Preferably, the composition includes
The pH buffer of 0.001 to 15wt%, more preferably 0.01 to 10wt%, even more preferably from 0.01 to 5% and most preferably 0.1 to 3%.
The method that one aspect of the present invention provides sterilization oral cavity, which comprises the following steps：(a) by the present invention first party
The composition in face is applied to oral cavity；And (b) cleans oral cavity to being substantially free of the composition.Cleaning refers to that said composition is basic
On remove from oral cavity.When in liquid form (such as mouthwash), only said composition is spued.When the composition be powder,
When paste or gel form, it is possible to use the composition is rinsed out from oral cavity by appropriate water.When the composition is tooth
During cream, before rinsing step, generally brushed on intraoral tooth or gum.Rinse and fetch water and clear with water
Wash oral cavity or gargle to carry out.
Another aspect of the invention provides purposes of the disclosed composition for oral cavity of sterilizing.
Present invention preferably provides non-treatment benefit.
Embodiment
Various mouthrinse compositions are to the biomembranous effect of Streptococcus mutans
Streptococcus mutans (S.mutans) is a kind of Gram-positive, facultative anaerobic bacteria, is sent out generally in human oral cavity
It is existing.Streptococcus mutans is the main cause for causing carious tooth (decayed tooth) in the whole world, and be considered as in all Streptococcus oralis most
Cariogenicity.Adherence of Streptococcus mutans is survived in dental surface and by diversified carbohydrate.When metabolism is sugared and which
During his energy, the microorganism produces acid, causes tooth to decay tooth.Mouthrinse composition is prepared as follows.Lemon is prepared with 1: 6 ratio
Acid and the buffer solution of sodium citrate.Add NaLS (SLS) in this buffer solution to obtain buffering SLS of 0.34wt%
Solution.Mix thymol, terpineol and eugenol to prepare the mixing of active ingredients of essential oils by the ratio with 0.5: 1: 0.1
Thing.
By in above-mentioned buffering SLS solution add active ingredients of essential oils (thymol, terpineol, eugenol, menthol,
Geraniol) or Sunphenon80SK (the refined polyphenol extract of the green-tea extract containing 60% catechin) it is right to prepare
Compare composition.The formula of Comparative composition is displayed in table 1.
By the above-mentioned active ingredients of essential oils mixture containing thymol, terpineol and eugenol of 0.05wt% is mixed
Composition of the invention is prepared to buffering SLS surfactant solutions.Add 1.5wt%'s in the mixture
Sunphenon80SK simultaneously adds water to supply final composition.In a preferred composition, by the triclosan of 0.5wt%
Be added in buffering SLA surfactant solutions with the Sunphenon80SK of 1.5wt% and final composition is supplied with water.It is excellent
The formula of composition is selected to be given in Table 2.
The effect of test mouthrinse composition as the antimicrobial compositions of antagonism biofilm-forming bacterium streptococcus mutans.
Streptococcus mutans ATCC25175 is passed in BHI meat soups (Brain Heart Infusion Broth-Difco-37 gram per liters)
Culture, and which is made in CO2Incubator (5%CO2) at 37 DEG C grow 16 hours.By in the BHI meat soups containing 2% sucrose
The cell density of culture be adjusted to 108Cfu/ml (at 620nm, optical density～0.3).In first group of embodiment, become
The streptococcic culture of shape 37 DEG C on 6 orifice plates in CO2Incubator (5%CO2) in the growth culture period of 24 hours forming life
Thing film.In second group of embodiment, culture grows the culture period of 72 hours, to form the biomembrane of thickness.Every 24 hours period
After change culture medium.
After 24/72 hour culture period, BHI broth bouillons the life for having been formed on flat board with 1X PBSs are removed
Thing film.2 milliliters of each mouthrinse composition and biofilm contact 1 minute.Then remove mouthwash, and by 2 milliliters of nertralizer
It is added in biomembrane.Then the biofilm cells of process of learning from else's experience are scraped with cell scraper, is mixed and with D/E nertralizer (Difco-
39g/L) it is serially diluted.Its 1ml is inoculated on BHI agar, and in CO2Cultivate 48 hours in incubator.After culture 48 hours
Count the bacterium colony for being formed.The reduction of colony count after Comparative composition is applied is given in Table 1, after preferred composition is applied
The reduction of colony count is given in Table 2, and is calculated as log10 (number of bacterium colony in control)-log10 (numbers of bacterium colony after process
Mesh).
Table 1- comparative examples
Table 2- embodiments in accordance with the present invention
Tables 1 and 2 shows, when active ingredients of essential oils is combined with the polyphenol containing at least 50% catechin, biological
During the reduction of microorganism count in film improves to some extent, and individually component itself shows biomembrane, significantly less bacterium is reduced.
Each mouthwash formula reduces effect of inflammation
Mouthrinse composition is prepared as follows.The buffer solution of citric acid and sodium citrate is prepared with 1: 6 ratio.To this buffering
Add lauryl sodium sulfate (SLS) in liquid to prepare the SLS solution (control) of 0.34wt%.With 0.5: 1: 0.1 ratio system
The mixture of standby active ingredients of essential oils thymol, terpineol and eugenol.
By adding active ingredients of essential oils in the buffer solution containing NaLS (the SLS solution of 0.34wt%)
Mixture is obtaining Comparative composition (Comp h).
By adding active ingredients of essential oils in the buffer solution containing NaLS (the SLS solution of 0.34wt%)
Mixture and green-tea extract, and finally supply volume to prepare preferred composition (embodiment 7) by addition water.In table 3
Provide various mouthrinse compositions.
Implement vitro assay to carry out anti-inflammatory research.By venipuncture to the vacuum test tube containing heparin
(vacutainer), from 3 healthy volunteer's collection blood samples.By 1ml blood samples are added to 7.5ml's
Each Fresh blood sample is diluted in Rosewell Park Memorial Institute (RPMI) culture mediums.0.5ml is dilute
The blood sample released is allocated in 24 orifice plates.With the contrast of the 0.5ml with or without inflammatory stimulus thing Escherichia coli LPS (2 ×)
Composition and preferred composition (2 ×) stimulate blood sample to finally give contrast or the preferred composition of 1 × concentration.Stimulate
Afterwards, sample is at 37 DEG C and 5%CO2Under in incubator be incubated 24 hours.After incubation period, culture plate is centrifuged into 10 in 3000rpm
Minute；Supernatant is collected with aliquot and -70 DEG C is stored in until further analyzing.
Cell factor is that the content of TNF α and IL-6 is carried out quantitatively with the dilute sample of culture supernatants.Due to large intestine
The inflammatory reaction of bacillus LPS produces cell factor.Cell factor is that the content of TNF α or IL-6 relatively low shows mouthrinse composition
Preferable effect in terms of anti-inflammatory benefit is provided.
Table 3
| Composition (wt%) | Control | Comp*h | Embodiment 7 |
| Terpineol | - | 0.015 | 0.015 |
| Thymol | - | 0.03 | 0.03 |
| Eugenol | - | 0.003 | 0.003 |
| NaLS | 0.34 | 0.34 | 0.34 |
| Citric acid | 0.2 | 0.2 | 0.2 |
| Sodium citrate | 1.2 | 1.2 | 1.2 |
| Sunphenon80SK | - | - | 1.5 |
| Ethanol | - | - | 10 |
| Water | To 100 | To 100 | To 100 |
| TNFα(pmg/ml) | 40 | 20 | 10 |
| IL-6(pmg/rml) | 55 | 52 | 2 |
Table 3 shows the composition (embodiment 7) of the present invention there is provided preferably anti-inflammatory is beneficial than Comparative composition (Comp*h)
Place.
Claims (16)
1. oral care composition, which includes：
（i）The antimicrobial of 0.01 to 10wt%, selected from the active ingredients of essential oils comprising thymol or eugenol or geraniol；
Or its mixture；
（ii）The polyphenol of 0.1 to 5wt%；With,
（iii）The acceptable matrix in oral cavity；
Wherein described polyphenol includes at least 50% catechin.
2. the composition for requiring in claim 1, wherein the catechin does not have comprising at least 25% epigallocatechin
Infanticide acid esters.
3. the composition for requiring in claim 1 or claim 2, wherein the active ingredients of essential oils includes thymol or cloves
Phenol or its mixture.
4. the composition for requiring in claim 1, which includes the surfactant of 0.05 to 15wt%.
5. the composition for requiring in claim 4, wherein the surfactant is cationic surfactant.
6. the composition for requiring in claim 5, wherein the cationic surfactant is benzalkonium chloride or cetyl three
Methyl bromide ammonium.
7. the composition for requiring in claim 1 or 2, which includes and buffers selected from the pH of citric acid or sodium citrate or its mixture
Agent.
8. the composition for requiring in claim 7, which has 4 to 7 pH value.
9. the composition for requiring in claim 1 or 2, wherein the acceptable matrix in the oral cavity includes water, silica or carbon
Sour calcium.
10. composition according to claim 9, which is antimicrobial mouthwash, the water comprising 80 to 99.5wt%.
11. compositions according to claim 9, which is toothpaste, comprising 2 to 70wt% selected from calcium carbonate or the mill of silica
Material；And the water of 8 to 40wt%.
12. compositions according to claim 9, which is tooth powder, comprising 90 to 99.5wt% selected from calcium carbonate or silica
Abrasive material.
13. oral care compositions, which includes：
（i）The antimicrobial of 0.01 to 10wt%, the essential oil selected from the mixture comprising thymol, terpineol and eugenol are lived
Property composition；
（ii）The polyphenol of 0.1 to 5wt%；With,
（iii）The acceptable matrix in oral cavity；
Wherein described polyphenol includes at least 50% catechin.
The non-therapeutic method in 14. sterilization oral cavities, which comprises the following steps：
（i）The composition required in aforementioned any one of claim is applied to into oral cavity；And
（ii）Cleaning oral cavity is to without the composition.
The non-therapeutic method required in 15. claims 14, wherein before rinsing step, by the composition brush in oral cavity
On interior tooth or gum.
Non-therapeutic use of the composition required in 16. aforementioned any one of claim for oral cavity of sterilizing.
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN3330/MUM/2011 | 2011-11-25 | ||
| IN3330MU2011 | 2011-11-25 | ||
| EP12151770 | 2012-01-19 | ||
| EP12151770.0 | 2012-01-19 | ||
| PCT/EP2012/071649 WO2013075920A2 (en) | 2011-11-25 | 2012-11-01 | An oral care composition |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103987364A CN103987364A (en) | 2014-08-13 |
| CN103987364B true CN103987364B (en) | 2017-04-05 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201280057942.2A Expired - Fee Related CN103987364B (en) | 2011-11-25 | 2012-11-01 | Oral care composition comprising polyphenol |
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| Country | Link |
|---|---|
| EP (1) | EP2782550A2 (en) |
| CN (1) | CN103987364B (en) |
| BR (1) | BR112014012497A2 (en) |
| IN (1) | IN2014MN00931A (en) |
| WO (1) | WO2013075920A2 (en) |
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| DE102014221669A1 (en) * | 2014-10-24 | 2016-04-28 | Henkel Ag & Co. Kgaa | Use of Camellia sinensis phenolic extract in oral and dental cleaning products to improve the visual appearance of the gums |
| WO2017048617A1 (en) * | 2015-09-15 | 2017-03-23 | Vizuri Health Sciences Llc | Polyphenol/flavonoid compositions and methods of formulating oral hygienic products |
| JP6715688B2 (en) * | 2016-06-14 | 2020-07-01 | 花王株式会社 | Toothpaste composition |
| CN107028781A (en) * | 2017-04-01 | 2017-08-11 | 泰州优克生物科技有限公司 | A kind of toothpaste containing eugenol and preparation method thereof |
| CN107242993B (en) * | 2017-06-23 | 2020-07-31 | 王会海 | Spearmint enzyme mouthwash and preparation method thereof |
| JP7031253B2 (en) * | 2017-11-29 | 2022-03-08 | ライオン株式会社 | Toothpaste composition |
| WO2021180909A1 (en) * | 2020-03-13 | 2021-09-16 | Unilever Ip Holdings B.V. | A cleaning composition |
| CN114469761A (en) * | 2021-12-28 | 2022-05-13 | 彭氏(惠州)实业发展有限公司 | Oral care compositions and methods of use and preparation thereof |
Citations (1)
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|---|---|---|---|---|
| CN101534823A (en) * | 2006-11-10 | 2009-09-16 | 宝洁公司 | Oral care compositions containing combinations of anti-bacterial and host-response modulating agents |
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| US4548809A (en) * | 1984-03-27 | 1985-10-22 | Fung Paul S T | Method for manufacturing a stomatic gargle |
| US5472684A (en) * | 1993-06-02 | 1995-12-05 | Colgate Palmolive Company | Oral compositions for plaque and gingivitis |
| JP2988928B1 (en) | 1998-12-18 | 1999-12-13 | 三井物産株式会社 | Mouth spray composition |
| US6531115B1 (en) * | 2001-01-03 | 2003-03-11 | Council Of Scientific & Industrial Research | Analgesic and refreshing herbal composition and a process for preparing the same |
| US7030092B1 (en) * | 2001-08-24 | 2006-04-18 | Small Giant L.L.C. | Ultra-high fiber supplement and method of reducing weight cardiovascular risks and ingested toxins. |
| US20060105000A1 (en) * | 2002-11-21 | 2006-05-18 | J.P.M.E.D. Ltd | Compositions for treating infected skin and mucous membrane comprising an anti-microbial agent and an essential oil |
| CN1669576A (en) * | 2004-03-17 | 2005-09-21 | 东莞市朗晨生物技术有限公司 | Anticarious spray agent and producing process thereof |
| PL1781375T3 (en) * | 2004-07-27 | 2013-11-29 | Genprofiler S R L | Mixture of polyphenols for the prevention of the onset of prostate cancer in a person diagnosed with High Grade Prostate Intraepithelial Neoplasia (HGPIN) |
| US7329419B2 (en) * | 2004-09-23 | 2008-02-12 | Herbalife International, Inc. | Herbal supplement to support weight loss |
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| US7943183B2 (en) * | 2005-03-18 | 2011-05-17 | Gardiner Paul T | Compositions and methods for increasing metabolism, thermogenesis and/or muscular definition |
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- 2012-11-01 WO PCT/EP2012/071649 patent/WO2013075920A2/en active Application Filing
- 2012-11-01 CN CN201280057942.2A patent/CN103987364B/en not_active Expired - Fee Related
- 2012-11-01 IN IN931MUN2014 patent/IN2014MN00931A/en unknown
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| CN101534823A (en) * | 2006-11-10 | 2009-09-16 | 宝洁公司 | Oral care compositions containing combinations of anti-bacterial and host-response modulating agents |
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| BR112014012497A2 (en) | 2017-06-06 |
| WO2013075920A3 (en) | 2013-12-12 |
| CN103987364A (en) | 2014-08-13 |
| EP2782550A2 (en) | 2014-10-01 |
| IN2014MN00931A (en) | 2015-04-17 |
| WO2013075920A2 (en) | 2013-05-30 |
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