CN105748305A - Oral treatment composition - Google Patents
Oral treatment composition Download PDFInfo
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- CN105748305A CN105748305A CN201610139490.2A CN201610139490A CN105748305A CN 105748305 A CN105748305 A CN 105748305A CN 201610139490 A CN201610139490 A CN 201610139490A CN 105748305 A CN105748305 A CN 105748305A
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- oral cavity
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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
- A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
- A61K8/44—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
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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
- A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
-
- 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
- A61K8/24—Phosphorous; Compounds thereof
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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
- A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
- A61K8/27—Zinc; Compounds 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
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
- A61K8/81—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions involving only carbon-to-carbon unsaturated bonds
- A61K8/8164—Compositions of homopolymers or copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and at least one being terminated by a carboxyl radical, and containing at least one other carboxyl radical in the molecule, or of salts, anhydrides, esters, amides, imides or nitriles thereof; Compositions of derivatives of such polymers, e.g. poly (methyl vinyl ether-co-maleic anhydride)
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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
Abstract
The invention discloses an oral treatment composition which is applied to treatment of various oral disorders.The composition is capable of realizing blocking of dentinal canals while having anti-microbial and dental caries prevention functions.The composition comprises free arginine or arginine salt, membrane attachable polymers and at least one of pyrophosphate, zinc salt, sylvite, strontium salt and mixture thereof.
Description
The application is Application No. 201080067593.3 (international application no PCT/US2010/039677), filing date
On June 23rd, 2010, the divisional application of application for a patent for invention of invention entitled " treatment oral cavity composition ".
Technical field
The present invention relates to treatment oral cavity composition useful in treating multiple oral disorders, wherein said compositions can
Dentine pipe close is provided, antibacterial and anti-caries efficacy is provided simultaneously.
Background technology
Three mineralized tissues of tooth are enamel, cementum and dentin.In the tooth of people, enamel covers crown
Dentin, and cementum covers root face dentin.Successively, the dental pulp of dentin encapsulating tooth, dental pulp provides blood vessel for dentin
With nerve support.Being different from enamel and cementum, Dentinal transverse section is made up of many tubules.Tubule wall comprises dentin
Calcified matrix, and tubule space is filled with the fluid (dentin liquid) coming from pulp tissue's fluid and serum.Matrix minerals matter
Mainly comprising synthos, hydroxyapatite, it is neutral poor, when pH becomes the most acid with dissolubility under alkaline pH
Time, its dissolubility is become better and better.
Due to the wall of its rigidity, fill the fluid of narrow Dentinal tubule make cold, sense of touch, evaporation and permeability thorn
Swash and can be transferred to dental pulp with the form of fluid motion by dentin.The motion of this dentin liquid is perceived as the play of short-term
Bitterly.When the odontoblast of dental pulp terminal of tubule is charged in interference, cause this kind of pain, and as result, have stimulated
Adhere to the mechanical type sensor of its pulpal nerve fibers.Nerves reaction is commonly referred to as Dentinal pain and involved
Dentin refers to hypersensitive dentine.
When protectiveness enamel or cover Dentinal cementum lose time, produce Dentinal allergy.Dentale
Matter is easier to destroy, because cementum is thinner and is easier to by acid attack than enamel.But, at gingival recession and root surface
Before being exposed to oral environment, it is impossible to cemental destruction occurs.When there is the cementum of destruction and suffering from dentin hypersensitiveness
During the food of the individuality of disease, the exposed area of its tooth touches cold air or heat and cold liquid or sweet or acid, or
During touching metal, usually experience pain.
The approach occurring cementum to lose (and adamantine situation is the most identical) is the process via dental caries.Acid is to make
Produce for the end product of bacterial degradation of fermentable carbohydrate, and hydroxyapatite are dissolved in these acid, after
Person is as the same with enamel in dentin, is main calcium phosphate mineral, and it constitutes the major part of cemental mineral.Separately
One source is acidic food, if frequently and over a long time taken in, will promote tooth demineralisation.These acidic foods include
Fruit juice and many Alcoholics and non-alcoholic beverages.Other acidizers causing chemical to be corroded include that multiple human mouth is protected
Reason product.Many of which is commercially available gargarism and some toothpaste.Grinding agent toothpaste and violent brushing teeth can help
Corrosion process.Another approach of cementum and enamel cover layer that Dentinal tubule loses their protectiveness is, logical
Cross the program implemented in dental clinic by dentist or oral hygiene teacher.This includes that preparation is for filling up the tooth repaired with other
The cavities of tooth and crown preparation.It is also included within by periodontist or oral hygiene teacher implement scrape calculus and root of the tooth was planished
Removal cementum in journey.
Have been made by many effort, but at the Dentinal tubule of blocking exposure, thus reduce or stop stimulation to arrive tooth
Marrow obtains limited success with the ability aspect causing pain.Have attempted to or single or combination multiple material produces and has
The stopper of effect.It is common means by form calcium phosphate precipitating the closing to tubule.This includes making soluble calcium salt with solvable
Acid phosphate mixes, and immediately by this combined administration in open tubule.Or, also use a kind of salt, use another afterwards
Plant salt, to attempt the precipitate obtaining being formed in tubule.
Having utilized is not the material of calcium phosphate.Such as, U.S. Patent number 3,683,006 describes use potassium nitrate, nitre
Acid lithium or sodium nitrate.Another example is little or large-sized calcium oxalate granule.Use protein denaturant, such as ethanol, surface
Activating agent or chaotropic salt (chaotropic salt), it is possible to the Dentinal tubule that blocking exposes, because at Dentinal tubule
In there is protein material, and degeneration may sometimes result in tubule part or completely plugged.But yet another fiercer means
It is Dental Erosion part to be placed in affected region or covers this region with adhesive material.U.S. Patent number 5,139,768
It is described in lasting hydrophobic polymer the finishing varnish (varnish) used containing strontium salt.Adhere and leak from tubule without fluid
The most always it is easily achieved, because it is difficult for adhering to wettable surfaces, it is contemplated that dentin liquid is from the outflow of tubule continuous print or lets out
Leakage, and implant or binding agent dispose and are difficult to stop.
Effort not by blocking treatment dentin hypersensitiveness has been directed to god important for neural impulse transmits
Depolarization through fibrous membrane.Potassium salt, particularly potassium nitrate, the most for this purpose.Such as, U.S. Patent number 4,751,
072 and 4,631,185 describe use potassium bicarbonate and potassium chloride.U.S. Patent number 6,524,558 discloses containing arginine and calcium
Salt, the oral cavity composition for the treatment of dentin allergy.
Arginine and other basic amino acids have been proposed for mouth care, and believe tackle dental cavity formation and
Dentin hypersensitiveness has notable benefit.But, by these basic amino acids and the mineral with oral care benefits, such as fluorine
Compound and calcium combine, to form the oral care product with acceptable long-time stability, it was demonstrated that challenging.Especially
It is that basic amino acid can raise pH and promote calcium ion to dissociate, and it can react with fluoride ion, forms infusible precipitate.This
Outward, higher pH has the potentiality causing stimulation.But, when neutral pH or acid pH, system utilizes arginine bicarbonate
Salt (it is lectured by this area is preferred) releasable carbon dioxide, causes container to expand and explosion.Additionally, it is anticipated that reduce pH
To lower effect of said preparation to neutral or acid condition, because arginine can form insoluble arginine-calcium complexes, it is right
The affinity of dental surface is worse, and the pH reduced also by lower said preparation be likely to be of cariogenic to buffering in mouth
Any effect of lactic acid.It is used together antimicrobial with arginine and salt and also results in difficulty.Commercially available arginine-
Based toothpastes, such as ProClude and DenClude, such as, containing arginine bicarbonate and calcium carbonate, but not fluoride
Also without any antimicrobial.
Gargarism and mouthwash formulations are also familiar with for this area.Various preparations include antibacterial, spice, coloring agent, sweet taste
Agent, flavorants etc..And plurality of reagents can be included in rinse or rinse preparation, their synergistic application is not likely to be feasible
, due to the interaction between each reactant, untoward reaction, cause loss of activity.Gargarism or mouthrinse composition are provided
For treating multiple minor illness, including such as, dentin allergy, dental caries, halitosis, dental plaque formation, tartar control, prevent
Dye/brighten, xerostomia, burn into gingivitis etc. will be desirable.
Summary of the invention
The feature of embodiment of the present invention is to provide treatment oral cavity composition, and it is super quick that said composition is used for treating dentin
Reaction, dental caries, halitosis, bacterial plaque formed, tartar control, prevention dye/brighten, xerostomia, burn into gingivitis etc..Combination is provided
Thing is inventive feature, and described compositions can be as by utilizing calcium and phosphonium ion present in dentin liquid to realize inherence
Dentinal canals blocks, and provides antibacterial and anti-caries efficacy at the same time, improves xerostomia and treatment corrosion and gingivitis.Combination is provided
Thing is also the feature of embodiment of the present invention, and said composition provides the waterpower showing as the improvement that flow reduces greater than about 50% to pass
Lead (hydraulic conductance).
According to these and other features of embodiment, provided herein is the oral care composition according to claim 1, its
Comprise free or the arginine of salt form, mucoadhesive polymer and be selected from pyrophosphate compound, zinc salt, potassium salt, strontium salt
And at least one composition of mixture.Preferably, said composition is gargarism.
Another embodiment of the invention includes the method for the foundation claim 11 of following one or more aspects: reduce
The allergy of tooth;Reduce or the formation of suppression dental caries;Reduce or suppress the demineralized of tooth and promote remineralization;Reduce or
Suppression gingivitis;In suppression oral cavity, microbial biofilm is formed;Reduce the gathering of dental plaque;Treatment xerostomia;Reduce tooth
Corrosion;Enamel after protection erosion challenges;With cleaning and/or whitening teeth and cleaning oral cavity, described method includes oral cavity
Care composition is applied to the oral cavity of the patient needed, and said composition comprises free or the arginine of salt form, mucoadhesive
Polymer and selected from pyrophosphate compound, zinc salt, potassium salt, strontium salt and at least one composition of mixture thereof.
People will be readily apparent from these and other features from the summary of the detailed description of following preferred embodiment.
Detailed description of the invention
Guide defined below and non-limiting must consider in looking back description of the invention in this paper.Make herein
Title (such as " background " and " summary ") and subtitle (such as " compositions " and " method ") be intended only to be suitable to the present invention's
The normal tissue (general organization) of the topic in Gong Kai and be not intended to be limited to the present invention or its any aspect
Open.Particularly, the theme disclosed in " background " can include the technical elements within scope of the invention, and can not be formed in
The narration of first technology.Theme disclosed in " summary " be the full scope of the present invention or its any embodiment be not limit
Or disclose completely.For convenience's sake, carried out the Sorting Materials in the chapters and sections of this specification or discussion, described material
As having special effectiveness (such as " active " or " carrier " composition), and should not draw inference, i.e. when using it for times
Time in the compositions what is given, according to it in classification herein, material must necessarily or individually function.
Be not intended that to those lists of references it is the accreditation in first technology quoting of here by reference, or do not approve right
Patentability in present invention disclosed herein has any association.Any discussion of the content of the list of references quoted in introduction
It is intended only to provide the General Introduction to the opinion made by the author of list of references, and is not intended that about such reference literary composition
The accreditation of the correctness of the content offered.
Describe and special embodiment, while instruction embodiment of the present invention, it is intended to be used merely to explain purpose, and also
It is not intended to limit scope of the invention.Additionally, the narration of the embodiment of multiple features set forth is not intended to repulsion and has
Additionally other embodiments of feature, or integrate other embodiments of the various combination of described feature.In order to illustrate how system
Standby and use the present composition and the purpose of method, it is provided that specific embodiment, unless otherwise expressly provided outside, be not intended to
Showing, the embodiment that the present invention gives or has not yet been prepared or has tested.
As used in this article, word " preferably " and " preferably " refer to provide some interests in some cases
Embodiment of the present invention.But, other embodiments equally or are being alternatively preferably in the case of other.And, a kind of
Or the narration of multiple preferred embodiment is not meant to that other embodiments are not useful, and it is not intended to implement other
Scheme excludes from scope.It addition, compositions and method may be included in elements described herein, substantially by this
The key element that literary composition describes forms or is formed by elements described herein.
As used in the whole text, scope is used as shorthand to describe each and each value in its scope.May select
Any value in its scope is as the end points of scope.It addition, in all references cited herein at this by reference in full
It is incorporated into herein.If genetic definition conflict in the disclosure and cited list of references, it is as the criterion with the disclosure.
Unless otherwise specified, in all percents herein and expressed in its elsewhere of this specification and amount, it should be appreciated that
For referring to percetage by weight.The amount be given is effective weight based on material.In narration to occurrence herein, no matter referring to all
The respective amount of composition, or other features of embodiment, it is intended to represent the value of the degree of variation considering measurement error that adds deduct.
Such as, the amount of 10% can include 9.5% or 10.5%, and the degree of the error in given measurement will have common skill for this area
Personnel are appreciated and understood by.
As used herein, " antibacterial activity " means herein as by acceptable external or internal antibacterial any
Analyze or test the activity measured." anti-inflammatory activity " means herein as by acceptable external or In vivo analysis any
Or the activity that test, the such as generation of suppression prostaglandin or the analysis of peroxidase activity or test are measured." antioxidant is lived
Property " activity as measured is meant by acceptable external or internal antioxidant analysis any or test herein.
In this article, " discharge surface " includes any soft or hard surface in mouth, and it includes tongue, firmly glues with soft palate, buccal
Film, the surface of gums and tooth surface.In this article, " tooth surface " is surface or the hard table of artificial denture of born tooth
Face, including corona, tooth cap, implant, bridge, artificial tooth, dental implant etc..Herein, term " suppresses " to relate to disease, such as
During inflammation in oral cavity tissue, reduce or the alleviation of disease including prevention, suppression, scope or the order of severity.
The oral care composition of preferred embodiment includes free or the arginine of salt form, mucoadhesive polymerization
Thing, optionally at least one antibacterial and selected from pyrophosphate compound, zinc salt, potassium salt, strontium salt and mixture thereof at least one
Composition.Described compositions preferably presents the form of gargarism or collutory.In addition to these compositions, gargarism or collutory can wrap
Include sweeting agent, pH adjusting agent, acid, salt, anti-caries agent and other conventional gargarism.Described compositions is preferred for the total of oral cavity
Body or all treat, including allergy, dental caries, halitosis, dental plaque is formed, tartar controls, prevention is dyeed/brightened, xerostomia,
The treatment of burn into gingivitis etc..
Although being not intended to be limited to any theory of operation, it is believed by the inventor herein that the use in conjunction of the most all compositions,
Offer tubule obturation effect of coating enhancing in its surface, delivers and retains useful reagent to surface.Said composition
Thering is provided mucosa-adherent (mucoadhesivity) and thin film Formation and characteristics, it can be used for process allergy, xerostomia, acid are supported
Anti-, demineralization etc..
Compositions described herein is containing free or the arginine of salt form.Suitable arginine compounds, derivant and salt
Such as, disclosed in U.S. Patent Application Publication No. 2005/0031551,2009/0202465 and 2009/0202454, it is open
By in full with reference to being incorporated into herein.Arginine can exist with itself, and can include arginine and D thereof and L-shaped formula.Arginine
(or as arginic derivant) can also be there is by salt form.Arginic any salt can be used in the present invention, if its energy
Discharge arginine in the solution.Suitable arginine salt includes arginine and the salt of one or more following materials: (a) is sour
Property polymer;The conjugate acid of (b) anionic surfactant salt;(c) polynary phosphoric acid or polyphosphonic acid;Or (d) is acid anti-micro-
Biological agent.Arginine salt is preferably arginine and the salt of dodecanoyl sulphuric acid.
The conjugate acid of anionic surfactant salt is selected from the water-soluble of (i) higher fatty acid monoglyceride ester one sulfate
Property salt is (such as the salt one sulfate monoglyceride of hydrogenated coconut fatty acid oil, such as N-methyl N-cocoyl sodium taurocholate, cocos nucifera oil
Acid monoglyceride sodium sulfate (sodium cocomo-glyceride sulfate));(ii) higher alkyl sulfates, such as Laurel
Base sodium sulfate;(iii) senior alkyl-ether sulfate, such as formula CH3(CH2)mCH2(OCH2CH2)nOSO3The salt of H, wherein m is 6-
16, such as 10, n is 1-6, as 2,3 or 4 and X is Na or K (such as laureth (laureth)-2 sodium sulfate (CH3(CH2)10
(CH2(OCH2CH2)2OSO3Na));(iv) higher alkyl aryl sulfonates (such as dodecylbenzene sodium sulfonate (lauryl benzene sulphur
Acid sodium));(v) higher alkyl sulfoacetates (such as lauryl sulfoacetate sodium (sodium lauryl sulfoacetate), 1,2 2
The high-grade aliphatic ester of hydroxypropanesulfonic acid salt.Sulfo group laurate (sulfocolaurate) (N-2-Ethyl Lauroyl acid potassium altogether
Sulfo group acetamide) and sodium lauryl sarcosinate);(vi) and its mixture, as wherein " senior alkyl " refers to C6-30Alkyl, example
Such as C8-18。
Arginine salt can include arginine polyphosphoric acids or polyphosphinates, including, such as, arginine and polyvinylphosphonic acid
The salt of the salt of the salt of salt, arginine and polyphosphoric acid, arginine and hexa metaphosphoric acid, arginine and pyrophosphoric acid, arginine and trimerization
The salt of phosphoric acid and mixture thereof.
Arginine salt may also comprise the salt of arginine and antimicrobial acid.In particularly preferred embodiment of the present invention, it is provided that
Arginine and benzoic salt, described benzoic acid optionally by carboxyl and/or one or more, as 1,2 or 3 hydroxyls replace, such as benzene
Formic acid, phthalandione, salicylic acid or trihydroxybenzoic acid, such as, gallic acid.
Free or salt form arginine can be present in the amount of 0.1 wt. % to 20 wt. % of the gross weight of compositions
In compositions described herein, described amount is preferably from 0.25 wt. % to 5 wt. % of total composition weight, such as based on group
The weight meter of the gross weight of compound is from 0.4% to 2.5% or from 0.5% to 2% or from 0.6% to 1% or from 0.75% to 0.9%.
The compositions of the present invention also contains mucoadhesive polymer.Mucoadhesive polymer is generally known and can
Acceptable polyvinyl methyl ether/maleic anhydride (PVME/MA) copolymer, acrylic acid/methacrylic acid selected from oral cavity
Ester/styrene/2-acrylamido-2-methyl propane sulfonic acid copolymer (Lupasol FF4243/Lupasol DVFR), poly-
One or more in (vinyl pyrrolidone) (PVP), carboxymethyl cellulose (CMC), xanthan gum and mixture thereof.Mucosa
Tack polymer exist amount, in terms of gross weight based on compositions, be preferably from 0.1% to 20%, such as from 0.25% to
10% weight, more preferably from 0.4% to 2.5% or from 0.5% to 2% or from 0.6% to 1% weight.
Preferably mucoadhesive polymer be the delivery of those Contrast agents and reservation and reservation himself at discharge surface
On material.For such reagent of the present invention disclosed in U.S. Patent number 5,188,821 and 5,192,531.Suitable
Polyvinyl methyl ether/maleic anhydride (PVME/MA) copolymer include those in the copolymer methyl vinyl ether with suitable
Anhydride maleique ratio is from the copolymer of 1:4 to 4:1, and the mean molecule quantity that this copolymer has is 30, and 000 to 1,000,
000, such as 30,000 to 500,000.Preferably PVME/MA copolymer includes that those are from ISP (Bound Brook, N.
J., 08805) trade mark is the copolymer of GANTREZ.If there is antibacterial enhancing effective amount, PVME/MA copolymer also may be used
Work as antimicrobial enhancing agent.GANTREZ copolymer can include, such as, can from ISP Technologies, Inc.,
GANTREZ AN 139 (M.W. 500,000), the GANTREZ AN that Bound Brook, N. J. 08805 obtains
119 (M.W. 250,000) and preferably GANTREZ S-97 pharmaceutical grade (M.W. 700,000).
Mucoadhesive polymer for the oral care composition of the present invention also includes one or more polymer, all
As PVP (PVP), Polyethylene Glycol, polyvinyl methyl ether acid/maleic acid copolymers, polysaccharide (as
Cellulose derivative, such as carboxymethyl cellulose or polysaccharide gum, such as xanthan gum or carrageenan gum).Can with they
The water-soluble alkali (such as potassium and sodium) of free acid or neutralization partially or completely or ammonium salts provide acidic polymer, such as
Polyacrylate gel.
Other polymer worked include those polymer, such as maleic anhydride and ethyl acrylate, methyl-prop
The 1:1 copolymer of olefin(e) acid hydroxyl ethyl ester, NVP or ethylene, the latter can conduct, such as Monsanto EMA compile
Number 1103, M.W. 10,000 and EMA Grade 61, and acrylic acid and methyl methacrylate or hydroxyethyl methylacrylate,
The 1:1 copolymer of acrylic acid methyl ester. or ethyl acrylate, IVE or NVP and obtain.
The ene-type of the general polymerization desirably containing carbon-extremely-carbene double bond and at least one carboxyl activated or ethylene type
Unsaturated carboxylic acid, i.e. containing being prone to the acid of alkene double bond worked in the polymerization, because it is present in monomer molecule, or
In the alpha-beta position relative to carboxyl, or the part as composition terminal methylene.Illustrative such acid is acrylic acid, first
Base acrylic acid, ethylacrylic acid, α-chloro-acrylicacid .beta.-methylacrylic acid, β-acryloxy propionic, sorbic acid, alpha-chloro sorbic acid
(α-chlorsorbic), cinnamic acid, β-styrene acrylic, viscous furancarboxylic acid (muconic), itaconic acid, citraconic acid, mesaconic acid,
Glutaconate, equisetic acid, atropic acid, 2 benzyl acrylic acid, 2-cyclohexylacrylic, angelic acid, umbellic acid, anti-butylene
Diacid, maleic acid and acid anhydride.Vinyl acetate, chlorine can be included from other different alkene monomers of such carboxylic acid monomer's copolymerization
Ethylene, dimethyl maleate etc..Copolymer is containing enough water-soluble carboxylic acid's salt groups.
The polymerization agent of another class includes the homopolymer containing substituted acrylamide and/or undersaturated sulfonic acid and salt thereof
The compositions of homopolymer, polymer the most therein is based on undersaturated sulfonic acid, and it is selected from acrylamido alkane
(alykane) sulfonic acid, such as 2-acrylamide 2 methyl propane sulfonic acid, its molecular weight is about 1, and 000 to about 2,000,000, in U.S.
State's patent No. 4, described in 842,847, it is open by full with reference to being incorporated into herein.In this, particularly preferred polymerization
Thing is acrylic acid/methacrylate/styrene/2-acrylamido-2-methyl propane sulfonic acid copolymer (Lupasol
FF4243/Lupasol DVFR).Lupasol FF4243 is containing 20% acrylic acid, 20% acrylic acid methyl ester., 59% 2-acrylamide
2 methyl propane sulfonic acid and 1% cinnamic copolymer.Another kind of useful polymerization agent includes polyamino acid, particularly those
Containing the aminoacid of a certain proportion of anion surface active, such as aspartic acid, glutamic acid and phosphoserine, as special in the U.S.
Profit number 4, described in 866,161, it is open by full with reference to being incorporated into herein.
The compositions of preferred embodiment also can optionally contain one or more antibacterial.Antibacterial is selected from the two of halogenation
Phenyl ether (such as triclosan), herb extracts and quintessence oil are (such as Herba Rosmarini Officinalis extract, tea extract, extract of magnolia, Herba thymi vulgaris
Phenol, menthol, eudesmol, geraniol, carvacrol, citral, chamenol, catechol, methyl salicylate, table GC do not have
Infanticide acid esters, table GC (epigallocatechin), gallic acid, Meath watt gram (miswak) extract, Fructus Hippophae carry
Take thing), biguanides preservative (such as chlorhexidine, alexidine or octenidine), quaternary ammonium compound is (such as cetylpyridinium chloride (CPC), benzene
Prick oronain, TPC (TPC), TDEPC (TDEPC)), phenols anticorrosion
Agent, hexetidine, octenidine, Sanguinarine, povidone iodine, delmopinol (delmopinol), the positive decoyl-3 of 5-'-fluoroform
Base phenyl salicylic amide (salifluor), metal ion are (such as zinc salt, such as, zinc citrate, zinc oxide, pink salt, mantoquita, ferrum
Salt), Sanguinarine propolis and oxidant (such as hydrogen peroxide, the Dexol of buffering or sodium carbonate peroxide), phthalandione and salt thereof, single mistake
Phthalandione (monoperthalic acid) and salt thereof and ester, ascorbyl stearate, N-Oleoylsarcosine, alkyl sulfate, sulphur
Base dioctyl succinate, N-phenylsalicylamide, Bradosol Bromide, delmopinol, octapinol (octapinol) and other piperidinos
Derivant, nicin prepared product, chlorite;Mixture with aforementioned any material.Antibacterial is not the most triclosan, and can
For CPC, chlorhexidine, zinc citrate, zinc oxide, and mixture.If used, for gross weight based on compositions, antibacterial
The amount that agent preferably exists be by weight from 0.01% to 10%, such as from 0.025% to 5%, more preferably from 0.05% to 1%, or
By weight from 0.075% to 0.5%.
The compositions of preferred embodiment also includes selected from pyrophosphate compound, zinc salt, potassium salt, strontium salt and mixing thereof
At least one or more composition of thing.Pyrophosphate for this compositions includes pyrophosphoric acid two alkali metal salt, pyrophosphoric acid four alkali gold
Belong to salt, and mixture.In the unhydrated and Sodium Acid Pyrophosphate (Na of hydrated form2H2P2O7), tetrasodium pyrophosphate
(Na4P2O7) and tetrapotassium pyrophosphate (K4P2O7) it is preferred kind.In the present compositions, pyrophosphate can three kinds of sides
One of formula exists: main lysed pyrophosphate, main undissolved pyrophosphate or dissolving and undissolved pyrophosphate
Mixture.With different protonated states (such as HP2O7 -3) pyrophosphate ions that exists also can exist, this depends on compositions
If pH and being partly dissolved of tetrasodium pyrophosphate.Gross weight meter based on compositions, pyrophosphate can be from 0.1% to 5%
Weight, preferably with from 0.2% to 2% weight with more preferably to exist from the amount of 0.4 to 2% weight.The group of all pyrophosphates can be used
Close.
Zinc salt for embodiment includes, such as, any physiologically acceptable zinc compound includes water miscible
(including that shipwreck is molten) organic and inorganic zinc compounds.Water-soluble zinc compound (at least 1% solubilized) is preferred.Can use
The example of suitable zinc compound includes: zinc acetate, zinc fluoride, zinc sulfate ammonium, zinc formate, zinc bromide, zinc iodide, zinc chloride,
Zinc oxide, zinc nitrate, zinc chromate, zinc phenolsulfonate, zinc citrate, zinc salicylate, dithionic acid zinc, zinc sulfate, Zinc fluosilicate,
Zinc gluconate, zinc tartrate, zinc succinate, zinc glycerophosphate, and mixture.Disclosed in U.S. Patent number 4,138,477
The zinc ion that the dissolubility that has of other zinc compounds is at least every ml water about 0.01 mg, by with reference to being incorporated into herein.Base
In the gross weight meter of compositions, zinc salt more preferably can be deposited with the amount from 0.1-1% zinc salt weight with scope from 0.01-5% weight
?.
Suitable nitrate and carbonate include, such as, for any physiologically acceptable salt of collut.Nitric acid
Salt includes above-mentioned zinc nitrate and potassium nitrate and sodium nitrate.Suitable carbonate includes, such as, and calcium carbonate, alkali metal carbonic acid
Salt, sodium carbonate etc..Nitrate and carbonate typically in terms of this composition weight from 0.1% to 30%, preferably from 1% to 10% and
The more preferably amount from 1.5% to 5% exists.
In addition to arginine, mucoadhesive polymer and salt, the oral cavity composition described according to embodiment can contain allusion quotation
It is applied to the conventional ingredient of oral cavity composition type.Such as, liquid gargarism can contain solvent, such as distilled water or deionized water and
Ethanol;Sweeting agent, such as saccharin, aspartame, sorbitol, mannitol and xylitol;And flavoring agent, such as Oleum menthae and Liu Lan
Oleum sesami (see U.S. Patent number 4,226,851 and 4,606,912, it is open by full with reference to being incorporated into herein).Toothpaste can
Contain, such as, conventional grinding agent, such as resin, silicon dioxide and the insoluble alkali metal of the standard volume with 20% to 60% weight
Metaphosphate;Binding agent, such as hydroxyethyl cellulose, xanthan gum and sodium carboxymethyl cellulose, its standard volume scope is from 0.05%
To 5.0% weight;Foaming agent, such as sodium lauryl sulphate, cocos nucifera oil coconut monoglyceride and N-methyl-N-palmityl cattle sulphur
Acid sodium, its standard volume scope is from 0.5% to 3.0% weight;Flavoring agent;Sweeting agent;Appointing needed for preservative and particular composition
What his composition, and as will be recognized by those of skill the art (see U.S. Patent number 4,177,258 and 4,721,614, it is open logical
Cross in full with reference to being incorporated into herein).Tablet and powder can contain, such as, vehicle, such as lactose and mannitol, binding agent, such as
Corn starch and carboxymethyl cellulose and disintegrating agent.
Be applied topically to sensitive teeth position, the cemental dentifrice of breeched of the such as root surface that oral cavity exposes or
Toothpaste, can be dentifrice that is that a combination thereof thing more simplifies (simpler) and that use with soft giver or toothpaste.Such dentifrice
Or toothpaste can contain or can be free of grinding agent, foaming agent and the flavoring agent of routine.Local location, such as the tooth of Dental Erosion
Dentin after body preparation is directed to the compositions that more simplifies and includes the filler for dental pulp capping, hole, dental chamber
Wadding and cementing material and those skilled in the art think compositions any other composition necessary (Craig etc., 1989,
Restorative Dental Materials. Mosby, St. Louis, pp. 189-225).Such as, zinc oxide and fourth
Fragrant phenol level (respectively 20 and 25%) will be suitable for dentistry cementing material compositions.
Embodiments herein also provides for the article manufactured, including packaging material and this paper in being included in packaging material
The oral cavity composition described.Oral cavity composition is effective delaying or preventing in dentin quencher reaction.Packaging material are preferred
It is effective label including instruction oral cavity composition in delaying or preventing dentin quencher to react.For encompassing oral cavity composition
Packaging material can include glass, plastics, metal or any other suitable inert material.Such as, the tooth containing oral cavity composition
Cream can be included in dentifrice tube, typically aluminium soft tube, lead matter-liner hose or plastic tube, or extrusion pump or pressurization allotter
To measure out content, or include in tearable pouch (tearable sachet).Also compositions can be included in typically
In the plastic bottle distributing liquid.
Also the oral cavity composition of the embodiment in small-sized dental container can be used for for polishing tooth or treat quick
Sense tooth or prevention are scraped calculus, root of the tooth planing by dentist or oral hygiene teacher or remove the development of sensitive teeth after mottle
In preventative toothpaste, such as make the rotary attachment of dentist's small tool (dental hand-pieces) for dental hospital
(rotary attachments) is prone to the container being arranged according to size of access.
The oral care composition of the present invention can take to be suitable for being applied to any liquid or the gel form of discharge surface.?
In multiple illustrative embodiment, compositions can be the liquid solution being suitable for rinsing, rinse or spraying;Toothpaste, such as dentistry
Use gel;Periodontal gel;It is suitable for smearing the liquid (such as liquid brightener) of tooth surface;Collutory, foam etc..More than except
Outside those of statement, compositions can contain activity and/or carrier components.
Preferably oral care composition include selected from toothpaste, gargarism, oral cavity band (oral strips), lozenge,
Pearl (beads), liposome, micelle, reverse micelle, micro--or the container of nanometer-encapsulation, enzyme, albumen, gel, collosol and gel, water
Gel, silica gel, organic zeolite, inorganic silica gel those, be such as found in those following products: toothpaste, smears (paint-
Ons), oral cavity paster, polymer, spray, smoke inhalation device, foam, mouth balosam, from the back side of head toothbrushes or pass through tooth
Brush, oil or for oral hygiene or other products beneficial to oral cavity.These products may also comprise for dental care,
Food, liquid and the Li Sheng element that inherence comprises or can mix with extinction material (photoabsorbing species)
(probiotics)。
In multiple embodiments, compositions comprises the acceptable fluoride ion source in oral cavity as anti-caries agent.Can deposit
In one or more such sources.Suitable fluoride ion source includes fluoride, mono-fluor phosphate and fluosilicate and fluorine
Change amine, including olaflur (olaflur) (N'-n-octadecane base trimethylene diamine-N, N, N'-tri-(2-ethanol)-dihydro fluorine
Hydrochlorate) and stannous fluoride.Can use other anti-caries agents, such as arginine and arginine derivative are (such as Ethyl Lauroyl acyl arginine
(ELAH))。
As anti-caries agent, optionally to provide 100-20 altogether, 000 ppm, 200-5,000 ppm or 500-2,500 ppm
There is the salt of one or more release fluorides in the amount of fluoride ion.When sodium fluoride is the salt of the release fluoride of single existence
Time, illustratively the sodium fluoride of the amount of by weight 0.01% to 5%, 0.02% to 1% or 0.04% to 0.5% of property may be present in
In compositions.
Can use phenolic compound, and include being subjected to the mensuration that oral cavity is acceptable, those phenolic compounds by
Dewhirst (1980), Prostaglandins 20 (2), 209-222 are defined as having anti-inflammatory activity, but are not limited to this.
The example of antibacterial phenolic compound include 4-pi-allyl catechol, include benzyl p-hydroxybenzoate, butyl p-hydroxybenzoate,
The p-hydroxy Benzoic Acid ester of ethylparaben, methyl parahydroxybenzoate and propyl p-hydroxybenzoate, 2-benzyl benzene
Phenol, butylated hydroxyanisole, butylated hydroxytoluene, capsaicin, carvacrol, creosol, eugenol, guaiacol, the bisphenols chemical combination of halogenation
Thing, including hexachlorobenzene and bromo chlorobenzene, 4-hexyl resorcin, 8-hydroxyquinoline and salt thereof, include menthol salicylate,
Methyl salicylate and the salicylate of phenyl salicylate, phenol, pyrocatechol, N-phenylsalicylamide and thymol.These phenols
Compound typically exists with one or more natural extracts described above.
In another embodiment, said composition comprises, and such as, is adapted to assist in minimizing gingivitis, dental plaque, tooth knot
The acceptable stannous ion source in oral cavity of stone, dental caries or Sensitive disease.One or more such sources can be there are.Suitable stannous ion source
Include, but are not limited to stannous fluoride, other halogenation stannous, such as stannous chloride dihydrate, ditin diphosphate, organic carboxyl acid Asia
Pink salt, such as formic acid stannous, stannous acetate, gluconic acid stannous, lactic acid stannous, stannous tartrate, stannous oxalate, malonic acid stannous
With stannous citrate, stannum ethylene glyoxide (stannous ethylene glyoxide) etc..One or more stannous ion sources are appointed
Selection of land and illustratively in terms of composition weight 0.01% to 5%, the total amount of such as 0.03% to 2% or 0.05% to 1% exists.
In another embodiment, said composition comprises the acceptable flavorants in oral cavity.One or more are so
Flavorants effective total amount of breath freshening can be made to exist.Suitable flavorants includes, but are not limited to zinc salt, all
Such as zinc gluconate, zinc citrate and zinc chlorite, α-ionone etc..
In another embodiment, said composition comprises the acceptable anti-plaque including making bacterial plaque disintegrate in oral cavity
Agent.One or more such antiplaque agents can effectively antiplaque total amount exist.Suitable ascoxal includes, but not
It is limited to stannum, copper, magnesium and strontium salt, dimethicone copolyol (copolyols), such as Cetyl dimethicone
Copolyol, papain, glucoamylase, glucose oxidase, carbamide, calcium lactate, calcium glycerophosphate, polyacrylic acid strontium and chela
Mixture, such as citric acid and tartaric acid and alkali metal salt thereof.
In another embodiment, said composition comprises the acceptable antiinflammatory in oral cavity.One or more are such anti-
Scorching agent can exist with the total amount of effective antiinflammatory.Suitable antiinflammatory includes, but are not limited to steroid dose, such as fluocinolone acetonide
And hydrocortisone and on-steroidal agent (NSAIDs), such as ketorolac, flurbiprofen, ibuprofen, Nabumetone (flucinolone)
Life, indomethacin, diclofenac, etodolac, indomethacin, sulindac, tolmetin, ketoprofen, fenoprofen, pyrrole sieve former times
Health, nabumetone, aspirin, diflunisal, meclofenamic acid, mefenamic acid, oxyphenbutazone and Phenylbutazone.In compositions optionally
There is the antiinflammatory of one or more effective antiinflammatory amounts.
The present composition is optionally containing other compositions, such as enzyme, vitamin and anti-sticker.Enzyme, such as albumen can be added
Enzyme is for anti-dyeing and other effects.The limiting examples of vitamin includes vitamin C, vitamin E, vitamin B5 and leaf
Acid.In multiple embodiments, vitamin has antioxidant properties.Anti-sticker includes Ethyl Lauroyl acyl arginine
(ELAH), Nipagin ester (solbrol), ficin, silicon resin copolymer and derivant and quorum sensing (quorum
Sensing) inhibitor.
Optionally include in the useful carrier in the present composition be diluent, grinding agent, bicarbonate, pH adjusting agent,
Surfactant, foam modifier, thickening agent, viscosity modifier, wetting agent, sweeting agent, flavoring agent and coloring agent.Can optionally deposit
Carrier material in the identical or different classification of a kind of carrier material or more than one.Each other with compositions should be selected to produce
It is mutually adapted the carrier adaptive with other compositions.
Water is preferred diluent, and at some compositions, in such as gargarism and whitening fluid, usually companion's alcohol, such as second
Alcohol.In gargarism compositions, water is generally 1:1 to 20:1 with the weight ratio of alcohol, such as 3:1 to 20:1 or 4:1 to 10:1.Increasing
In white liquor, in water can be above scope with the weight ratio of alcohol or less than above scope, such as 1:10 to 2:1.
In further embodiment, the compositions of the present invention comprises at least one pH adjusting agent.Such regulation
Agent includes that acidulant is to reduce pH, basifier to raise pH and buffer agent to regulate and control the pH scope at needs.Such as, it may include choosing
From one or more compounds of acidulant, basifier and buffer agent, to provide the pH of 2-10, or multiple exemplary embodiment party
The pH of 2-8,3-9,4-8,5-7,6-10,7-9 etc. in case.The acceptable pH adjusting agent in any oral cavity can be used, including but not
It is limited to carboxylic acid, phosphoric acid and sulfonic acid, hydrochlorate (such as sodium dihydrogen citrate, disodium citrate, malic acid one sodium etc.), citric acid, alkali metal
Hydroxide, such as sodium hydroxide, carbonate, such as sodium carbonate, sodium bicarbonate, sodium sesquicarbonate, sodium borate, sodium silicate, phosphorus
Acid sodium (such as monosodium phosphate, tertiary sodium phosphate, pyrophosphate etc.), imidazoles etc..Optionally effectively to maintain compositions acceptable in oral cavity
PH scope in total amount there are one or more pH adjusting agents.
In further embodiment, the present composition comprises at least one surfactant, and it is such as used for
Other adaptive compositions of compositions, and therefore the stability of enhancing is provided, to help cleaning tooth surface by detergent action, and
Foam is provided, as during brushing teeth with the dentifrice composition of the present invention when agitation.Any oral cavity can be used acceptable
Surfactant, major part therein is anionic, nonionic or both sexes.Suitable anion surfactant bag
Include, but be not limited to C8–20The water soluble salt of alkyl sulfate, C8–20The sulfonated monoglyceride of fatty acid, sarcosinate, cattle sulphur
Hydrochlorate etc..The illustrative example of these and other kinds includes sodium lauryl sulfate, cocos nucifera oil coconut monoglyceride, lauryl flesh
Propylhomoserin sodium, sodium lauryl isethionate (sodium lauryl isoethionate), laureth carboxylic acid sodium and 12
Sodium alkyl benzene sulfonate.Suitable nonionic surfactant includes, but are not limited to poloxamer, polyoxyethylene sorbitol acid anhydride
Ester, alcohol ethoxylate, alkylphenol ethoxylate, tertiary amino oxides, phosphine oxides, dialkyl sulfoxide etc..Suitably
Amphoteric surfactant include, but are not limited to the C with anionic group8–20Aliphatic secondary amine and the derivant of tertiary amine, such as
Carboxylate, sulfate, sulfonate, phosphate or phosphonate.Suitable example is cocamidopropyl betaine.A kind of or many
Planting surfactant 0.01% to 10% optionally based on the weight of compositions, the total amount of such as 0.05% to 5% or 0.1% to 2% is deposited
?.
In further embodiment, the compositions of the present invention comprises at least one foam modifier, and it is used for example
As increased by the amount of produced foam, consistency or stability during agitation compositions.The acceptable bubble in any oral cavity can be used
Foam regulator, includes, but are not limited to Polyethylene Glycol (PEGs), it is also known that for polyoxyethylene.High molecular weight PEGs s is suitable, bag
Include those mean molecule quantities about 200,000 to about 7,000,000, e.g., from about 500,000 to about 5,000,000 or about 1,000,
The PEGs of 000 to about 2,500,000.One or more PEGs optionally based on the weight of compositions about 0.1% to about 10%, such as
About 0.2% to about 5% or about 0.25% to about 2% total amount exist.
In further embodiment, compositions described herein can comprise at least one thickening agent, and it is used for example
As given the denseness required for compositions and/or mouthfeel.The acceptable thickening agent in any oral cavity can be used, include but not limited to card
Ripple nurse, it is also known that for CVP Carbopol ETD2050, carrageenin, it is also known that for Irish moss, and more particularly ι-carrageenin
(ι-carrageenin), cellulosic polymers, such as hydroxyethyl cellulose, carboxymethyl cellulose (CMC) and salt thereof, as CMC sodium,
Natural gum, such as POLY-karaya, xanthan gum, Radix Acaciae senegalis and Tragacanth, colloid silicic acid magnalium, silica sol etc..
The thickening agent of preferred classes or gellant include what a class acrylic acid and the alkyl ether of tetramethylolmethane or the alkyl ether of sucrose cross-linked
Homopolymer, or carbomer.Can be with Carbopol series from the B. commercially available carbomer of F. Goodrich.Particularly preferred poly-
Carbonyl ethylene (Carbopols) include carbopol 934,940,941,956,974P, and mixture.One or more thickening agents
Optionally 0.01% to 15% based on the weight of compositions, the total amount of such as 0.1% to 10% or 0.2% to 5% exists.
In further embodiment, this compositions can include at least one viscosity modifier, and it is for such as pressing down
Make deposition or the separation of all compositions, or promote the redispersibility when stirring fluid composition.Any oral cavity can be used to can accept
Viscosity modifier, they include, but are not limited to mineral oil, vaseline, clay and organically-modified clay, silicon dioxide etc..One
Kind or multiple viscosity modifier optionally based on the weight of compositions 0.01% to 10%, the total amount of such as 0.1% to 5% exists.
In further embodiment, this compositions can include at least one wetting agent, and it is for such as preventing
When being exposed to air, toothpaste is hardening.The acceptable wetting agent in any oral cavity can be used, include but not limited to polyhydroxy-alcohol, such as third
Triol, sorbitol, xylitol or low-molecular-weight PEGs.Most of wetting agents also play the effect of sweeting agent.One or more moisturizings
Agent optionally based on the weight of compositions 1% to 70%, the total amount of such as 1% to 50%, 2% to 25% or 5% to 15% exists.
In further embodiment, this compositions can include at least one sweeting agent, and it is used for such as enhancing group
The taste of compound.Any oral cavity can be used acceptable natural or artificial sweetener, include but not limited to dextrose, sucrose, wheat
Bud sugar, dextrin, dry Nulomoline, mannose, xylose, ribose, fructose, levulose, galactose, corn syrup (include that high fructose is beautiful
Rice syrup and corn-syrup solids), the starch of partial hydrolysis, the starch hydrolysate of hydrogenation, sorbitol, mannitol, xylitol,
Maltose alcohol, different Fructus Hordei Germinatus (isomalt), aspartame, Xin Temu (neotame), saccharin and salt thereof, dipeptides-base intense sweetness
Agent, cyclamate etc..One or more sweeting agents are optionally to depend strongly on selected concrete sweeting agent (s)
Total amount exist, but they typically in terms of the weight of compositions 0.005% to 5% existence.
In further embodiment, this compositions can include at least one flavoring agent, and it is used for such as enhancing group
The taste of compound.Can use the acceptable naturally occurring or synthetic flavoring agent in any oral cavity, they include, but are not limited to vanillin, Mus
Tail grass, Origanum majorana L., parsley oil, Oleum Menthae Rotundifoliae, Oleum Cinnamomi, wintergreen oil (methyl salicylate), Oleum menthae, Oleum Caryophylli, laurel fat, fennel
Celery oil, Eucalyptus oil, orange oil, fruit oil and essence, including those come from Fructus Citri Limoniae, orange, Citrus aurantium Linn., Fructus Citri grandis, Fructus Pruni, Fructus Musae, Fructus Vitis viniferae, Fructus Mali pumilae,
The essence of Fructus Fragariae Ananssae, Fructus Pruni pseudocerasi, Fructus Ananadis comosi etc., come from bean-and nut-spice, such as coffee, cocoa, laughable tree, Semen arachidis hypogaeae, Semen Armeniacae Amarum
Deng, the adsorbed and flavoring agent etc. of encapsulation.Also include having of flavoring agent herein in fragranced is provided in mouth and/or includes cooling
Or the composition of other sensory effects of thermogenetic effect.Such composition illustratively includes that menthol, menthyl acetate, lactic acid are thin
Lotus ester, Camphora, Eucalyptus oil, eudesmol, anethole, eugenol, Cortex Cinnamomi, raspberry ketone (oxanone), α-ionone, propylene
Base guaethol (propenyl guaiethol), thymol, linalool, benzaldehyde, cinnamic aldehyde, N-ethyl-p-thin
Lotus alkane (menthan)-3-Methanamide, N, 2,3-trimethyl-2-butanamide, 3-(1-terpane epoxide
(menthoxy))-propane-1,2-glycol, cinnamic aldehyde glycerineacetal (CGA), menthone glycerine acetal (MGA) etc..A kind of
Or multiple flavoring agent optionally in terms of the weight of compositions 0.01% to 5%, the total amount of such as 0.1% to 2.5% exists.
In further embodiment, this compositions can comprise at least one coloring agent.Coloring agent herein includes
Pigment, dyestuff, color lake and give special gloss or reflexive reagent, such as pearling agent.Coloring agent can play multiple effect, including
Such as provide white or light coating, the indicator effectively contacting tooth surface location as compositions and/or modification to tooth surface
Outward appearance, the most colored and/or opaque compositions, to improve the captivation to consumer.Any oral cavity can be used to can accept
Coloring agent, they include, but are not limited to Pulvis Talci, Muscovitum, magnesium carbonate, calcium carbonate, magnesium silicate, Magnesiumaluminumsilicate, silicon dioxide,
Titanium dioxide, zinc oxide, redness, yellow, brown and black iron oxide, ferric ferrocyanide ammonium (ferric ammonium
Ferrocyanide), manganese violet, ultramarine, the Muscovitum (titaniated mica) of titanium dioxide, bismuth oxychloride etc..One or more
Coloring agent optionally in terms of the weight of compositions 0.001% to 20%, the total amount of such as 0.01% to 10% or 0.1% to 5% exists.
In multiple embodiments, the present invention provides a mouthful balosam compositions, and it comprises more than gum base and effective dose
The combination of the extract discussed.Mouthful balosam preparation is the most typically containing one or more plasticisers, at least one sweeting agent and at least
A kind of flavoring agent.The carrier preferably employing transparent clear prepares mouth balosam preparation, to provide the mouth balosam compositions of transparent clear.
Gum base material is that this area is familiar with and includes naturally occurring or synthetic gum base or its mixture.Representational
Natural gum or lactoprene include tunny gum (chicle), natural rubber, gelutong (jelutong), Ba Lata tree
Glue (balata), gutta-percha (guttapercha), Lai Kaiou glue (lechi caspi), rope horse glue (sorva),
Guttakay, hat glue (crown gum) and perillo.The representative of paragutta or lactoprene includes that butadiene-styrene is altogether
Polymers, polyisobutylene and isobutylene-isoprene copolymer.With the concentration of 10-40% and preferred 20-35%, gum base is mixed
In mouth balosam product.
In other embodiments, this oral cavity composition includes comprising one or more polymerism film former and effective dose
The edible oral cavity band of the combination of extract discussed above.One or more polymer film-forming agents can connect selected from oral cavity
The polymer being subject to, such as amylopectin (pullulan), cellulose derivative and other soluble polymers include that this area is ripe
Those known.Further, this polymeric tapes is preferably transparent clear.
The present embodiment relates to the method for following one or more aspects: reduce the allergy of tooth;Reduce or
The formation of suppression dental caries;Reduce or suppress the demineralization of tooth and promote remineralization;Reduce or suppression gingivitis;In suppression oral cavity
Microbial biofilm is formed;Reduce the gathering of dental plaque;Treatment xerostomia;Reduce the corrosion of tooth;After protection erosion challenges
Enamel;With cleaning and/or whitening teeth and cleaning oral cavity, these are all by will be according to any embodiment described herein
Oral cavity composition be applied to oral cavity realize.Preferably, by compositions periodically (the most once a day, the most twice daily,
It is applied to three times a day) oral cavity schedule to last from 1 day to more than 6 months, more preferably at least 2 weeks.
It is more fully described preferred embodiment referring now to following non-limiting example.
The special embodiment of the present invention
Embodiment 1
In order to test the desensitization characteristic of compositions described herein, using at U.S. Patent number 5,589,159 (it is open passes through
Quote in full and be incorporated into herein) described in method, multiple oral cavity compositions are tested.The waterpower of the method detection material passes
Lead, it is provided that reduce the relevant objective reduction of fluid flow to fluid flow in Dentinal tubule.In this method, with metallurgy
Saw blade is perpendicular to the major axis of tooth and is cut by the intact people's molar being not suffering from dental caries and reparation, to form thin slice section or circle
Dish, thickness is mm from about 0.4 to about 0.8.Select there is no adamantine fragment for testing containing dentin, then use citric acid
Solution corrodes to remove smear layer (smear layer).Every disk is positioned into splitting into the device (split of chamber
Chambered device) in, this device is described in the J. Dent. Research, 57:187 (1978), and it is a kind of special
The chamber of other leakproof, with containing tissue culture fluid, pressurization fluid reservoir be connected.By using pressurized nitrogen and titanium dioxide
The mixture of carbon gas, can prepare fluid under physiological pH.In order to further ensure that accuracy, with artificial saliva, (phosphate delays
Rush liquid, PBS) disk is moistened condition to approximation oral cavity.This instrument includes coupling flow transducer (FLODEC, DeMarco
Engineering SA, Geneva) capillary glass tube.By bubble implantation glass capillary tube.By detecting the letter as the time
The displacement of the bubble of number, can detect the fluid flow by dentin disk.Fluid flow is equal to dentin ferrule.
Before using gargarism (baseline) and afterwards, detect dentin ferrule.The maximum of Baseline detection reflection pipe is opened
Mouthful, it causes higher permeability.After the baseline fluid flow of detection dentin disk, with micropipet by the group of 400uL
Compound is applied to its outer surface.After the time of 10 minutes, wash away the compositions on surface for 6 times with 400uL PBS rinse.Can calculate
Being reduced by the percentage flow caused by experimental compositions-treated, flow reduces the most, then inaccessible effect of compositions is the biggest.Will
Pipe obturation is calculated as flow and reduces or the percent ((baseline flow measurement treatment flow/baseline flow measurement) * 100) of permeability reduction.Excellent
Choosing, the present composition makes flow reduce by more than 50%, preferably greater than 56% and even more preferably more than 60%.
Table 1 below includes gargarism preparation:
Detection sample I-IV and comparison A and the hydraulic conductivity of comparison B.Value is reported in table 2 below.
Upper table discloses, and when comparing with collutory A and B compareed, the compositions of the present invention provides excellent flow to reduce.Although
All samples shows inaccessible effect, and flow reduces by more than 40%, but the sample of the present invention is respectively provided with the hydraulic conductivity more than 60%
Flow reduces.These examples disclose, and the compositions of the present invention provides outstanding result.
Embodiment 2
Preparing other mouthwash formulations (table 3), change is the type of used salt, and presence or absence mucosa is attached
The property polymer and arginine.
Table 3
Detecting the hydraulic conductivity of these samples, result is shown in table 4 below.
The data of table 4 disclose, when mucoadhesive polymer is combined with arginine (comparative example F), and not salt adding,
Being similar to the preparation disclosed in the embodiment of U.S. Patent Application Publication No. 2009/0202454, hydraulic conductivity is tested
(hydraulic conductance test) only provides 30% flow to reduce.And comparative example A and the B performance obturation in table 1
Effect, reduces by more than 40% with flow, and flow reduces remote inferior to the flow minimizing realized according to the present invention.Certainly, embodiment
VII includes adding pyrophosphate, and other is identical with comparative example F.Embodiment VII provides and subtracts more than double flow
Few, reach the flow of 65% reduce (with only 30% comparative example F compare).Similarly, add in embodiment VIII little
The calcium salt (use with calcium carbonate abrasives substantial amounts of, that will not produce calcium salt is made comparisons) of amount, even makes flow reduce and carries
High more, the flow reaching 79% reduces.
By reference to exemplary embodiment, invention has been described, it is understood that, the present invention does not limit to
In disclosed embodiment.Change that those skilled in the art will make after reading this specification and amendment, also include this in
In the range of invention, described scope limits in the appended claims.
Claims (18)
1. an oral care composition, described compositions comprises at least one free or arginine compounds of salt form, extremely
Few a kind of mucoadhesive polymer and pyrophosphate compound,
Wherein said arginine compounds is rendered as D or L-shaped formula or as the salt with dodecanoyl sulphuric acid;
The amount that wherein said arginine compounds exists is in 0.5% to 2% weight range;
Wherein when using hydraulic conductivity testing inspection, described compositions provides the flow more than 50% to reduce;
Wherein said mucoadhesive polymer is the group of polyvinyl methyl ether/maleic anhydride (PVME/MA) copolymer
Close, and additionally comprise CMC and/or xanthan gum;And
Wherein said compositions comprises the zinc salt selected from zinc oxide and/or zinc citrate the most further.
2., such as the compositions required in claim 1, the amount that arginine compounds therein exists is in 0.75% to 0.9% weight
In the range of.
3., such as the compositions required in claim 1, mucoadhesive polymer therein also comprises acrylic acid/metering system
Acid esters/styrene/2-acrylamido-2-methyl propane sulfonic acid copolymer, PVP (PVP), carboxymethyl
One or more in cellulose (CMC), xanthan gum and mixture thereof.
4., such as the compositions required in claim 1, mucoadhesive polymer therein is polyvinyl methyl ether/suitable fourth
Enedioic acid acid anhydride (PVME/MA) copolymer.
5., such as the compositions required in claim 1, the amount that mucoadhesive polymer therein exists is at 0.6% to 1% weight
In weight range.
6., such as the compositions required in claim 1, it also comprises antibacterial.
7., such as the compositions required in claim 1, pyrophosphate therein is selected from Sodium Acid Pyrophosphate (Na2H2P2O7)、
Tetrasodium pyrophosphate (Na4P2O7), tetrapotassium pyrophosphate (K4P2O7) and mixture.
8., such as the compositions required in claim 1, compositions therein is to use selected from gargarism, dental gel, periodontal
Presented in gel and being suitable for is applied in the liquid of tooth surface.
9., such as the compositions required in claim 8, compositions therein is gargarism.
10. comprise free or the arginine of salt form, mucoadhesive polymer and be selected from pyrophosphate compound, zinc salt, potassium
The oral cavity composition of at least one composition of salt, strontium salt and mixture thereof is used for selected from following one or more aspects in preparation
Purposes in medicine: reduce the allergy of tooth;Reduce or the formation of suppression dental caries;Reduce or suppression tooth demineralized and
Promote the remineralization of tooth;Reduce or suppression gingivitis;In suppression oral cavity, microbial biofilm is formed;Reduce the poly-of dental plaque
Collection;Treatment xerostomia;Reduce the corrosion of tooth;Enamel after protection erosion challenges;With cleaning and/or whitening teeth and cleaning
Oral cavity, arginine compounds therein is rendered as D or L-shaped formula or as the salt with lauryl sulphate acid, and essence ammonia therein
The amount that acid compound exists is in 0.6% to 1% weight range.
11. such as the purposes required in claim 10, wherein to this medicine of oral administration at least one times, continue at least two every day
Week.
12. such as the purposes required in claim 10, the amount that arginine compounds therein exists is in 0.75% to 0.9% weight
In the range of.
13. such as the purposes that require in claim 10, mucoadhesive polymer therein is selected from polyvinyl methyl ether/suitable
Anhydride maleique (PVME/MA) copolymer, acrylic acid/methacrylate/styrene/2-acrylamido-2-methylpropane
In sulfonic acid copolymer, PVP (PVP), carboxymethyl cellulose (CMC), xanthan gum and mixture thereof one
Plant or multiple.
14. such as the purposes required in claim 13, mucoadhesive polymer therein is polyvinyl methyl ether/maleic
Dicarboxylic anhydride (PVME/MA) copolymer.
15. such as the purposes required in claim 10, the amount that mucoadhesive polymer therein exists is at 0.6% to 1% weight
In weight range.
16. such as the purposes required in claim 10, wherein said compositions also comprises antibacterial.
17. 1 kinds of article including packaging material and the compositions as required in claim 1, packaging material therein include
Instruction oral cavity composition is delaying or is preventing effective label in dentin allergy.
The compositions of 18. foundation claim 1, it is selected from method of following aspect for one or more: reduce the super of tooth
Quick reaction;Reduce or the formation of suppression dental caries;Reduce or suppress the demineralized of tooth and promote the remineralization of tooth;Reduce or press down
Gingivitis processed;In suppression oral cavity, microbial biofilm is formed;Reduce the gathering of dental plaque;Treatment xerostomia;Reduce the corruption of tooth
Erosion;Enamel after protection erosion challenges;With cleaning and/or whitening teeth and cleaning oral cavity, described method includes oral cavity group
Compound is applied to oral cavity.
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CN201610139490.2A CN105748305A (en) | 2010-06-23 | 2010-06-23 | Oral treatment composition |
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CN201610139490.2A CN105748305A (en) | 2010-06-23 | 2010-06-23 | Oral treatment composition |
Related Parent Applications (1)
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CN2010800675933A Division CN102946841A (en) | 2010-06-23 | 2010-06-23 | Therapeutic oral composition |
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CN105748305A true CN105748305A (en) | 2016-07-13 |
Family
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CN201610139490.2A Pending CN105748305A (en) | 2010-06-23 | 2010-06-23 | Oral treatment composition |
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CN104721226A (en) * | 2013-12-19 | 2015-06-24 | 高露洁-棕榄公司 | Oral care composition |
CN110051444A (en) * | 2019-03-12 | 2019-07-26 | 温宏兴 | A kind of tooth membrane module and preparation method thereof for straightening of teeth |
CN110573131A (en) * | 2017-04-27 | 2019-12-13 | 荷兰联合利华有限公司 | Oral care compositions |
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CN108210355B (en) * | 2013-12-19 | 2022-02-18 | 高露洁-棕榄公司 | Oral care compositions |
CN110573131A (en) * | 2017-04-27 | 2019-12-13 | 荷兰联合利华有限公司 | Oral care compositions |
CN110051444A (en) * | 2019-03-12 | 2019-07-26 | 温宏兴 | A kind of tooth membrane module and preparation method thereof for straightening of teeth |
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