CN103987364A - Oral care composition comprising polyphenol - Google Patents

Oral care composition comprising polyphenol Download PDF

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Publication number
CN103987364A
CN103987364A CN201280057942.2A CN201280057942A CN103987364A CN 103987364 A CN103987364 A CN 103987364A CN 201280057942 A CN201280057942 A CN 201280057942A CN 103987364 A CN103987364 A CN 103987364A
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compositions
oral cavity
requiring
polyphenol
aforementioned
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CN103987364B (en
Inventor
G·巴纳杰
K·布康斯勒
U·马德哈范
K·K·纳雅克
D·K·劳特
M·T·萨吉
S·A·尤帕德亚亚
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Unilever NV
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Unilever NV
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34Alcohols
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34Alcohols
    • A61K8/342Alcohols having more than seven atoms in an unbroken chain
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34Alcohols
    • A61K8/347Phenols
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/4973Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom
    • A61K8/498Cosmetics 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97Cosmetics 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
    • A61K8/9783Angiosperms [Magnoliophyta]
    • A61K8/9789Magnoliopsida [dicotyledons]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q11/00Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Botany (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Oral & Maxillofacial Surgery (AREA)
  • Cosmetics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

The present invention relates to oral care composition and a method of disinfecting the oral cavity. We have found that oral care composition having a combination of selective antimicrobial agents and polyphenol provides improved antimicrobial benefits. The combination surprisingly shows synergistic effects that are an order of magnitude better than those shown individually by the antimicrobial agents.

Description

The oral care composition that comprises polyphenol
Invention field
The present invention relates to a kind of method in oral care composition and sterilization oral cavity.The present invention is mainly developed for oral care composition and is below being described with reference to these purposes.But, should be appreciated that the present invention is not limited to this specific application area.
Background and correlation technique
Oral hygiene is one of most important aspect in consumer's personal nursing.Consumer is all over the world used dissimilar product for mouth care.People brush teeth with toothbrush and dentifrice composition (it can be toothpaste or dentifrice) common every day at least twice.Can guarantee to keep good oral hygiene by the oral cavity bacterium that reduces to greatest extent between sleep period at night or accumulate in oral cavity daytime when people's feed or during having a drink by means of such brushing teeth.Brush teeth and therefore reduced to greatest extent the problem such as decayed tooth, tartar, gingivitis, dental caries and halitosis (badbreath) (also referred to as halitosis (halitosis)).
Although brush teeth twice every day, many people suffer from one or more of disease of various forms of above names, and this is considered to act on the bacterial of oral mucosa in approximately 12 hours between twice is brushed teeth.
For solving above-mentioned mouth care problem, method is up to now to use synthetic (as triclosan or alcohol), and it is thought that by a lot of consumers to them are zest (harsh).Increasing consumer, especially nearest, prefer to use the product that contains natural materials.In addition,, in many countries, from angle of cultural or other, people are unwilling to use alcohol in their collutory.
Combination at the known antimicrobial in oral care composition field provides improved antimicrobial efficacy.
US2007258996AA (The Sterilex Corporation) discloses a kind of antimicrobial compositions and has been used for the treatment of the method for infected by microbes.The antimicrobial compositions of the synergistic combination that this application instruction contains from oil, dyes and dyestuffs, sulfonate, phenol, ester, fatty acid or the dibenzofurans derivant of sequestering agent, carbohydrate, terpenes, terpenoid, peptide class, alkaloid, plant origin independent three kinds of selecting or more kinds of reagent.At least two kinds in described three kinds or more kinds of reagent is not the compound of same type.
EP1013261A1 (Mitsui & Co.Limited, 2000) discloses a kind of mouthspray compositions, and it is provided for covering for a long time halitosis, and brings significant refreshment (refreshing) effect.This application discloses a kind of compositions that contains tea polyphenols, Menthol and/or 1-carvone.This application discloses a kind of compositions that contains high-level ethanol.Ethanol is one of snap action and effective antimicrobial, but it is believed that it is irritating (harsh).In some culture, it is also considered to unacceptable.
We have found that, the oral care composition that contains the combination of selective antimicrobial and polyphenol provides improved antimicrobial benefit.This combination shows astoundingly than the described antimicrobial synergy of an effective order of magnitude of performance separately.Advantageously, even when the concentration of antimicrobial very hour also can be observed this benefit, thereby avoid due to the problem that uses the possible negative sense organ aspect of this active component of high concentration to produce.Also find, said composition also provides anti-inflammatory benefit simultaneously.
Goal of the invention
An object of the present invention is to overcome or improve at least one shortcoming of the prior art.By reference to this description, other object of the present invention will become apparent for those skilled in the art.
Summary of the invention
According to first aspect, a kind of oral care composition is disclosed, it comprises:
(i) 0.01 to 10wt% antimicrobial, is selected from the quintessence oil active component that comprises thymol or terpinol or eugenol or geraniol; Triclosan or its mixture;
(ii) 0.1 to 5wt% polyphenol; With,
(iii) the acceptable substrate in oral cavity;
Wherein said polyphenol comprises at least 50% catechin.
According to second aspect, a kind of method of the oral cavity of sterilizing is disclosed, it comprises the following steps:
A. the compositions of first aspect present invention is applied to oral cavity; And,
B. cleaning oral cavity is to not basically containing described compositions.
According to the third aspect, the purposes for the oral cavity of sterilizing according to the compositions of first aspect present invention is disclosed.
Detailed Description Of The Invention
By reading following detailed description and appended claims, these and other aspects, features and advantages will become apparent for those of ordinary skill in the art.Ask for exempting to become suspicious, any feature of one aspect of the present invention can be for any other aspect of the present invention.Word " comprises " and means " comprising ", but not necessarily " by ... composition " or " by ... form ".In other words the step of, enumerating or option do not need exhaustive.It should be noted that the example providing is in the following description intended to illustrate the present invention, do not intend the present invention to be limited to these examples itself.Similarly, all percentage ratio is w/w percentage ratio, except as otherwise noted.Except in operation and comparative example, or separately clearly state, represent that in the present specification and claims the physical property of amount of substance or reaction condition, material and/or all numerals of use are interpreted as being modified by word " approximately ".The numerical range representing with form " x to y " is understood to include x and y.In the time describing multiple preferable range for a special characteristic with form " x to y ", be understandable that all scopes of also considering the different end points of combination.
Oral care composition of the present invention comprises the acceptable substrate in antimicrobial, polyphenol and oral cavity.
antimicrobial
Described oral care composition comprises 0.01 to 10wt% antimicrobial, and preferably 0.01 to 5wt%, and more preferably 0.01 to 1wt%, also more preferably 0.01 to 0.5wt% and further preferably 0.01 to 0.2wt%.Described antimicrobial is selected from the quintessence oil active component that comprises thymol or terpinol or eugenol or geraniol; Triclosan (TCN) or its mixture.
Described quintessence oil active component preferably includes thymol or terpinol or eugenol or its mixture.
In compositions of the present invention, can comprise the quintessence oil active component that other are optional.These include but not limited to amyl salicylate, carvacrol, p-Cymene for example paracymene, dihydroeugenol, hexyl eugenol, 1-Hexyl salicylate, isoeugenol, methyleugenol, methylisoeugenol, methyl salicylate, tert-butyl group cresol and vanillin or non-aromatic quintessence oil.The example of the non-aromatic quintessence oil of terpenoid comprises cedrene, eucalyptole, citral (comprising geranial and neral), citronellal, citronellol, eucalyptol is (also referred to as 1, 8 eucalyptoles), to dihydro linalool (paradihydrolinalool), dihydromyrcenol (DH myrcenol), farnesol, geraniol, jasminolene, hydroxycitronellol (hydroxycitronallol), hydroxycitronellal, different citral, limonene, (R)-4-isopropenyl-1-methyl-1-cyclohexene, linalool, longifolene, menthol, nerol, nerolidol (nerolidiol), pinene, for example australene, phellandrene, terpinene, for example α-terpinene and γ-terpinene, terpinol, for example γ-terpinol and 4-terpineol, and 2,6-Dimethyl-2-octanol (THM).
Preferred compositions contains 0.01 to 5wt% terpinol, more preferably 0.01 to 2wt% terpinol; 0.01 to 2wt% thymol, more preferably 0.01 to 0.8wt% thymol and 0.001 to 2wt% eugenol, more preferably 0.002 to 0.1wt% eugenol.
Triclosan is 2 ', 4,4 '-trichlorine, 2-hydroxyl-diphenyl ether.Preferred compositions comprises 0.05 to 0.3wt% triclosan.
polyphenol
Described oral care composition comprises 0.1 to 5wt% at least polyphenol of the catechin of 50wt% that contains, and preferably 0.2 to 4wt%, and more preferably 0.5 to 4wt%, and also more preferably 1 to 3wt%, and the best is 1.0 to 2.5wt% polyphenol.
Polyphenol is one group of chemical substance finding in plant, it is characterized in that existing in each molecule more than one phenol unit or construction unit (building block).Polyphenol is divided into hydrolyzable tannins (epicatechol gallate of saccharide) and Phenylpropanoid Glycosides class (phenylpropanoids) conventionally as lignin (Secoisolariciresinol bioside (secoisolariciresinol diglycoside)), flavone compound, and the tannin of condensation.A maximum class and research the most widely polyphenol are flavone compounds, it comprises several thousand kinds of compounds, comprising flavonols (Quercetin, zingiberol, kaempferol, ampelopsin, resveratrol, rutin), flavonoid (apigenin, luteolin), catechin (epicatechin, catechin and gallate, theaflavin), flavanone (Hesperidin, naringenin, silymarin (Silibenin), eriodictyol), anthocyan (pelargonidin, peonidin, anthocyanidin, delphinidin, malvidin), osajin (daidzein, genistein, Glycitein) and Coumarins (coumestrol).
Preferably, described polyphenol comprises at least 60% catechin, more preferably at least 70%, also more preferably at least 80% and the best be 100% catechin.
Preferably, described catechin comprises at least 25% epigallocatechin gallate (EGCG).
Preferably, described polyphenol extracts from green tea (Camellia sinensis).
The polyphenol of the preferred commercially available catechin that contains at least 60% comprises Sunphenon90LB and Sunphenon80SK (Taiyo Kagaku Co., Ltd).
the acceptable substrate in oral cavity
Described oral care composition comprises the acceptable substrate in oral cavity.The acceptable substrate in described oral cavity depends on the delivery form of described oral care composition.Most suitable form is collutory, toothpaste or dentifrice.
The inventor wishes to utilize easy acquisition and natural active component to realize antimicrobial efficacy, and wishes Min. and use the antimicrobial of zest (harsh), as low-molecular-weight (C 1to C 3) alcohol, for example ethanol.Therefore, according to a preferred aspect of the present invention, described compositions comprises and is less than 2wt%, is more preferably less than 1wt%, is further more preferably less than such alcohol of 0.5wt%, and ideally, does not have low-molecular-weight (C in described compositions 1to C 3) alcohol.
collutory
In the time that said composition is configured to collutory, the acceptable substrate in described oral cavity is water.Low-molecular-weight (C can not used according to the antibiotic effect of the expectation of collutory of the present invention 1to C 3) alcohol, for example, when ethanol or isopropyl alcohol, obtain, described compositions does not basically contain low-molecular-weight alcohol.Term does not basically contain low-molecular-weight alcohol and refers to that this alcohol can exist with the amount of not appreciable impact microorganism killing.Preferably, in compositions of the present invention, exist and be less than 2%, be more preferably less than 1% C 1to C 3alcohol, and most preferably do not exist.
Therefore, according to an aspect of the present invention, provide antimicrobial collutory compositions, the antimicrobial that it comprises (a) 0.01 to 10wt%, is selected from the quintessence oil active component that comprises thymol or terpinol or eugenol or geraniol; Triclosan or its mixture; (b) 0.1 to 5wt% polyphenol, wherein said polyphenol comprises at least 50% catechin; (c) 80 to 99.5wt% water.
Collutory of the present invention preferably includes 0.05 to 10wt%, and more preferably 0.05 to 8wt%, most preferably 0.5 to 5wt% surfactant.That described surfactant is preferably is cationic, anionic or amphoteric ion type, most preferably cationic.
In the time there is anion surfactant, it is preferably from alkali metal or the alkali salt of alkyl sulfonic acid, fatty acid or alkyl ether sulphuric acid.
In the time there is zwitterionic surfactant, it is preferably from betaines, sulfobetaines class (sulphobetains), hydroxyl sulfo betaine class (hydroxyl sulphobetains) or aminocarboxylate.In the time there is cationic surfactant, it is preferably benzalkonium chloride, alkyl pyridinium chloride or quaternary ammonium Shuangzi (gemini) surfactant.
By using after not diluted compositions or dilute with water said composition, collutory compositions of the present invention is used for the oral cavity of sterilizing.In dilution step, the preferred weight ratio of compositions and water is 1: 1 to 1: 200, more preferably 1: 5 to 1: 50, and further more preferably 1: 15 to 1: 30 and be preferably approximately 1: 20.
toothpaste
Described oral care composition can be sent with toothpaste form.In the time that compositions is toothpaste, the acceptable substrate in described oral cavity is abrasive material, and it can be calcium carbonate or abrasive silica.In the time that calcium carbonate is abrasive material, toothpaste is opaque paste form.In the time using abrasive silica, toothpaste is sent with transparent gel form conventionally.
Toothpaste preferably includes 2 to 15wt% surfactant of total composition, and preferably 2.2 to 10wt%, and more preferably 2.5 to 5wt%.Preferred surfactant is anion or amphotericity.Described anion surfactant is preferably alkali metal alkyl sulfate, more preferably sodium lauryl sulfate (SLS).Also can use the mixture of anion surfactant.Described amphoteric surfactant is preferably betanin, and more preferably (wherein alkyl is straight chain C to alkylamide propyl-betaine 10-C 18chain), and cocamido propyl betaine (CAPB) most preferably.Also can use the mixture of amphoteric surfactant.
Opaque toothpaste:
Preferably, in opaque toothpaste, the acceptable substrate in oral cavity comprises 15 to 70wt% calcium carbonate, and more preferably 30 to 60wt%.Calcium carbonate (also referred to as Chalk (chalk)) can obtain in a variety of forms and these forms in some in oral care composition, use.Two kinds of conventional forms are FGNC (fine grinding natural whiting (chalk)) and PCC (winnofil).
In total Chalk (chalk) content in oral care composition, FGNC is conventionally with 35 to 100%, preferably 75 to 100% and especially 95 to 100% existence, and surplus is PCC.Typically, compositions comprises that 30 to 65wt%, preferably 35 to 55wt% and 40 to 55wt% FGNC most preferably.FGNC generally includes heavy base median particle diameter and is preferably 1 to 15 μ m, more preferably 2 to 10 μ m, and the further preferred granule of 4 to 7 μ m.
Described compositions also can comprise that other known " non-Chalk (no-chalk) " abrasive material is to improve abrasive action.Such abrasive material comprises dicalcium phosphate dihydrate (DCPD) and silicon dioxide.
Except calcium carbonate, can also comprise that abrasive silica is for strengthening abrasive action at opaque toothpaste.In the time existing, described compositions comprises that 4 to 15wt%, and preferably 6 to 12wt%, and further more preferably 7 to 10wt% abrasive silica.Alternatively, described compositions can comprise that 0.01 to 2wt%, and preferably 0.1 to 0.8wt%, further more preferably 0.3 to 0.7wt% perlite.
In opaque toothpaste, generally include compositions 15 to 40wt%, preferably 20 to 30wt% water.
Preferred compositions comprises wetting agent, for example xylitol, glycerol or Sorbitol.Glycerol and Sorbitol are particularly preferred.Preferably, described compositions comprises 0.1 to 20wt% wetting agent, and more preferably 1 to 15wt%, and most preferably 5 to 13wt%.
Preferably, described compositions also comprises alkali metal hydrogencarbonate.Preferred described alkali metal hydrogencarbonate is sodium salt.Described compositions preferably includes 1 to 30wt%, more preferably 2 to 20wt% and best 3 to 8wt% alkali metal hydrogencarbonate.
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, described abrasive silica has the weight average particle diameter of 5 to 15 microns, 10 to 100m2/g BET (nitrogen) surface area and the oily absorption value of about 70-150cm3/100g.The typical example of suitable low-refraction abrasive silica is Tixosil63 and 73 (from Rhone Poulenc); Sident10 (from Degussa); Zeodent113 (from Zeofinn); Zeodent124 (from Huber), the Sorbosil AC series being provided by Crosfield is as Sorbosil ACII, Sorbosil AC39 and SorbosilAC35, particularly SorbosilAC77 (from Crosfield Chemicals).The amount of silicon dioxide in gel toothpaste composition is preferably 2 to 60wt%, is generally 2 to 20wt%%, and more preferably 5 to 12wt%.
Thickening silica also can be mixed in gel dentifrice, is generally 4 to 12% of composition weight, and preferably 5 to 10%.The example of the medium thickening silica of preference ranking comprises MFIL (from Madhu Silica India), TC15 (from PQ Corp UK), Zeodent165 (from Huber) or Tixosil43 (from Rhodia).
In gel dentifrice, generally include 8 to 14% of composition weight, preferably 8 to 10% water.These water yields for example do not comprise, from the aqueous solution of other composition (Sorbitol) mixes the water said composition.
Toothpaste opaque or gel type also can comprise caries preventive agent, binding agent, thickening agent, spice, stabilizing agent, polymer, vitamin, buffer agent and anti-tartar agent.
Therefore, according to a preferred aspect of the present invention, provide dentifrice composition, the antimicrobial that it contains (a) 0.01 to 10wt%, is selected from the quintessence oil active component that comprises thymol, terpinol, eugenol, geraniol; Triclosan or its mixture; (b) 0.1 to 5wt% polyphenol, wherein said polyphenol comprises at least 50% catechin; (c) 2 to 70wt% abrasive material, is selected from calcium carbonate or silicon dioxide; (d) 8 to 40wt% water.
dentifrice
Dentifrice contains the abrasive material of very high percentage ratio conventionally, and common 90 to 99.9wt%, and preferably 90 to 95wt%.Chalk (chalk) is (FGNC) most preferred abrasive material, but also can use PCC.
By comprising that at dentifrice composition for example sodium lauryl sulfate of anion surfactant provides the foam of aequum.Preferably, described compositions comprises 2 to 3wt% surfactant.Other composition, as silicon dioxide or sodium monofluorophosphate can be included in compositions to 1wt% with height.
Can comprise that sweeting agent is as xylitol, Sorbitol, glycerol or glucide (sachharin).Spice can comprise with height to the amount of the 1wt% of dentifrice composition as spearmint (spearmint) or Herba Menthae (peppermint).
According to another aspect of the invention, provide dentifrice composition, the antimicrobial that it contains (a) 0.01 to 10wt%, is selected from the quintessence oil active component that comprises thymol, terpinol, eugenol, geraniol; Triclosan or its mixture; (b) 0.1 to 5wt% polyphenol, wherein said polyphenol comprises at least 50% catechin; (c) 90 to 99.5wt% abrasive material, is selected from calcium carbonate or silicon dioxide.
Therefore, in disclosed compositions, the acceptable matrix optimization water in described oral cavity, silicon dioxide or calcium carbonate.
pH buffer agent
Described oral care composition preferably also comprises pH buffer agent." pH buffer agent " refers to the system being made up of a kind of compound or compound combination herein, it is in the time adding strong acid or alkali, and pH value is slightly microvariations only.Therefore,, compared with not containing the same combination of pH buffer agent, the existence of pH buffer agent in compositions keeps longer period its pH value during the shelf life of compositions.Preferably, the pH of described oral care composition is 4 to 7.
Preferred pH buffer agent is selected from citric acid, sodium citrate or its mixture.Preferably, described compositions comprises 0.001 to 15wt% pH buffer agent, and more preferably 0.01 to 10wt%, also more preferably 0.01 to 5% and most preferably 0.1 to 3%.
One aspect of the present invention provides the method in sterilization oral cavity, and it comprises the following steps: (a) compositions of a first aspect of the present invention is applied to oral cavity; And (b) cleaning oral cavity to not basically containing described compositions.Clean and refer to that said composition removes substantially from oral cavity.In the time being liquid form (as collutory), only said composition is spued.In the time that described compositions is powder, paste or gel form, can use appropriate water that described compositions is rinsed out from oral cavity.In the time that described compositions is toothpaste, before rinsing step, conventionally brushed on intraoral tooth or gingiva.Rinsing is conventionally rinsed the mouth or gargled by water intaking and water carries out.
Another aspect of the present invention provides the purposes of disclosed compositions for the oral cavity of sterilizing.
The present invention preferably provides non-treatment benefit.
Embodiment
various collutory compositionss are to the biomembranous effect of Streptococcus mutans
Streptococcus mutans (S.mutans) is a kind of Gram-positive, facultative anaerobic bacteria, conventionally in human oral cavity, finds.Streptococcus mutans is the main cause that causes dental caries (decayed tooth) in the whole world, and is considered to tool cariogenicity in all Streptococcus oralis.Adherence of Streptococcus mutans is in dental surface and rely on diversified carbohydrate existence.In the time of metabolism sugar and other energy, this microorganisms acid, causes tooth decayed tooth.Be prepared as follows collutory compositions.Prepare the buffer of citric acid and sodium citrate with the ratio of 1: 6.In this buffer, add sodium lauryl sulfate (SLS) to obtain the buffering SLS solution of 0.34wt%.Mix by the ratio with 0.5: 1: 0.1 mixture that thymol, terpinol and eugenol are prepared quintessence oil active component.
By adding quintessence oil active component (thymol, terpinol, eugenol, menthol, geraniol) or Sunphenon80SK (the refining polyphenol extract of the green tea extract that contains 60% catechin) prepares Comparative composition in above-mentioned buffering SLS solution.The formula of Comparative composition is presented in table 1.
Prepare according to compositions of the present invention by the above-mentioned quintessence oil mixture of active principles that contains thymol, terpinol and eugenol of 0.05wt% being mixed to buffering SLS surfactant solution.In this mixture, add the Sunphenon80SK of 1.5wt% and add water to supply final composition.In a preferred compositions, the Sunphenon80SK of the triclosan of 0.5wt% and 1.5wt% is joined in buffering SLA surfactant solution and water is supplied final composition.The formula of preferred composition provides in table 2.
Test collutory compositions forms effect of the antimicrobial compositions of bacterium Streptococcus mutans as antibiont film.The Streptococcus mutans ATCC25175 cultivation of going down to posterity in BHI meat soup (Broth-Difco-37 gram every liter of Brain Heart Infusion), and make it at CO 2incubator (5%CO 2) at 37 DEG C, grow 16 hours.The cell density of the culture in the BHI meat soup that contains 2% sucrose is adjusted to 10 8cfu/ml (in 620nm place, optical density~0.3).In first group of embodiment, the culture of Streptococcus mutans 37 DEG C on 6 orifice plates at CO 2incubator (5%CO 2) in growth 24 hours culture period with form biomembrane.In second group of embodiment, the culture growth culture period of 72 hours, to form thick biomembrane.After every 24 hours periods, change culture medium.
After 24/72 hour culture period, remove BHI broth bouillon and also clean with 1X PBS the biomembrane having formed on flat board.Each collutory compositions of 2 milliliters contacts 1 minute with biomembrane.Then remove collutory, and the nertralizer of 2 milliliters is added in biomembrane.Then use the treated biomembrane cell of cell scraper scraping, mix and use D/E nertralizer (Difco-39g/L) serial dilution.Its 1ml is inoculated on BHI agar, and at CO 2in incubator, cultivate 48 hours.Cultivate the bacterium colony that after 48 hours, counting forms.Reduce and provide in table 1 using after Comparative composition clump count object, reduce and provide in table 2 using after preferred composition clump count object, be calculated as log10 (number of bacterium colony in contrast)-log10 (number of bacterium colony after processing).
Table 1-comparative example
Table 2-is according to embodiments of the invention
Table 1 and table 2 show, when quintessence oil active component with contain at least 50% the polyphenol combination of catechin time, in biomembrane, the minimizing of microorganism count improves to some extent, and independent component itself shows significantly less antibacterial minimizing in biomembrane.
each mouthwash formula reduces effect of inflammation
Be prepared as follows collutory compositions.Prepare the buffer of citric acid and sodium citrate with the ratio of 1: 6.In this buffer, add sodium lauryl sulphate (SLS) to prepare the SLS solution (contrast) of 0.34wt%.Prepare the mixture of quintessence oil active component thymol, terpinol and eugenol with the ratio of 0.5: 1: 0.1.
Obtain Comparative composition (Comp h) by adding the mixture of quintessence oil active component in the buffer to containing sodium lauryl sulfate (the SLS solution of 0.34wt%).
By adding mixture and the green tea extract of quintessence oil active component in the buffer to containing sodium lauryl sulfate (the SLS solution of 0.34wt%), and prepare preferred composition (embodiment 7) by adding water finally to supply volume.In table 3, provide various collutory compositionss.
Implement external test method to carry out antiinflammatory research.Extremely contain the vacuum test tube (vacutainer) of heparin by venipuncture, from 3 healthy volunteer's sample of blood, drawn.Dilute each Fresh blood sample by 1ml blood sample being added in Rosewell Park Memorial Institute (RPMI) culture medium of 7.5ml.The blood sample of 0.5ml dilution is allocated in 24 orifice plates.With containing or do not stimulate blood sample finally to obtain contrast or the preferred composition of 1 × concentration containing Comparative composition and the preferred composition (2 ×) of the 0.5ml of inflammatory stimulus thing Escherichia coli LPS (2 ×).After stimulation, sample is at 37 DEG C and 5%CO 2under in incubator, hatch 24 hours.After incubation period, by culture plate at 3000rpm centrifugal 10 minutes; Collect supernatant and be stored in-70 DEG C until further analyze with aliquot.
Cytokine is that the dilute sample of the content culture supernatants of TNF α and IL-6 carries out quantitatively.Owing to producing cytokine with the inflammatory reaction of Escherichia coli LPS.To be that the content of TNF α or IL-6 is lower show that collutory compositions is providing good effect aspect anti-inflammatory benefit to cytokine.
Table 3
Composition (wt%) Contrast Comp*h Embodiment 7
Terpinol - 0.015 0.015
Thymol - 0.03 0.03
Eugenol - 0.003 0.003
Sodium lauryl sulfate 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 that compositions of the present invention (embodiment 7) provides than better anti-inflammatory benefit of Comparative composition (Comp*h).

Claims (15)

1. oral care composition, it comprises:
(i) 0.01 to 10wt% antimicrobial, is selected from the quintessence oil active component that comprises thymol or terpinol or eugenol or geraniol; Triclosan or its mixture;
(ii) 0.1 to 5wt% polyphenol; With,
(iii) the acceptable substrate in oral cavity;
Wherein said polyphenol comprises at least 50% catechin.
2. the compositions requiring in claim 1, wherein said catechin comprises at least 25% epigallocatechin gallate (EGCG).
3. the compositions requiring in claim 1 or claim 2, wherein said quintessence oil active component comprises thymol or terpinol or eugenol or its mixture.
4. the compositions requiring in aforementioned claim any one, it comprises 0.05 to 15wt% surfactant.
5. the compositions requiring in claim 4, wherein said surfactant is cationic surfactant.
6. the compositions requiring in claim 5, wherein said cationic surfactant is benzalkonium chloride or cetyl trimethyl ammonium bromide.
7. the compositions requiring in aforementioned claim any one, it comprises the pH buffer agent that is selected from citric acid or sodium citrate or its mixture.
8. the compositions requiring in aforementioned claim any one, it has 4 to 7 pH value.
9. the compositions requiring in aforementioned claim any one, the acceptable substrate in wherein said oral cavity comprises water, silicon dioxide or calcium carbonate.
10. according to the compositions of claim 9, it is antimicrobial collutory, comprises 80 to 99.5wt% water.
11. according to the compositions of claim 9, and it is toothpaste, comprises 2 to 70wt% the abrasive material that is selected from calcium carbonate or silicon dioxide; And 8 to 40wt% water.
12. according to the compositions of claim 9, and it is dentifrice, comprises 90 to 99.5wt% the abrasive material that is selected from calcium carbonate or silicon dioxide.
The method in 13. sterilization oral cavities, it comprises the following steps:
(i) compositions requiring in aforementioned claim any one is applied to oral cavity; And
(ii) cleaning oral cavity is to not basically containing described compositions.
The method requiring in 14. claim 13, wherein, before rinsing step, brushes described compositions on intraoral tooth or gingiva.
The compositions requiring in 15. aforementioned claim any one is for the purposes in the oral cavity of sterilizing.
CN201280057942.2A 2011-11-25 2012-11-01 Oral care composition comprising polyphenol Expired - Fee Related CN103987364B (en)

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