CN1095263A - The oral composition that contains antiplaque, the agent of anti-tooth dirt - Google Patents
The oral composition that contains antiplaque, the agent of anti-tooth dirt Download PDFInfo
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- CN1095263A CN1095263A CN 93119922 CN93119922A CN1095263A CN 1095263 A CN1095263 A CN 1095263A CN 93119922 CN93119922 CN 93119922 CN 93119922 A CN93119922 A CN 93119922A CN 1095263 A CN1095263 A CN 1095263A
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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
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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
- A61K8/24—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
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/36—Carboxylic acids; Salts or anhydrides thereof
- A61K8/365—Hydroxycarboxylic acids; Ketocarboxylic acids
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
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- Birds (AREA)
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- Inorganic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
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- Oral & Maxillofacial Surgery (AREA)
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Abstract
The present invention relates to be used for the treatment of or prevent the compositions of dental plaque, tooth dirt and gingivitis or halitosis, it contains:
A) zinc ion source of (i) safety and effective dose; (ii) a kind of source of citrate ion; (iii) one or more anti-tooth dirt agent are selected from pyrophosphate, phosphonate, and diphosphate and general formula are (P
nO
(3n+1))
(n+2)-The polyphosphate of pharmaceutically acceptable linear condensation, wherein n is 2 to 21 integer;
Zinc wherein: the mol ratio of citrate is at most 1: 1; The mol ratio of zinc: Pgro is at most 1: 1; With
B) a kind of pharmaceutically useful local mouth carrier.
The invention still further relates to treatment or prevention dental plaque, tooth dirt and gingivitis, or the method for halitosis, comprise this compositions of oral administration to people or other animals.
Description
The present invention relates to be used for the treatment of or prevent the oral composition of dental plaque, tooth dirt and gingivitis and halitosis, for example dentifrice and mouth solution.
The oral cavity is bacterial growth and moves living place that in the oral cavity, gum, lip, oral mucosa (cheek), palate, tongue and tooth provide the surface that supplies bacterial colonization and accumulate.In the oral cavity, because tooth is hard, it is unique naked surface, and on its surface, antibacterial and product thereof (dental plaque) can obviously be accumulated, particularly at proximal surface with along gingiva seam place.
Dental plaque is the coarse adhesive film of tooth last layer, and it is to be made of saliva, antibacterial and the food particle of tight adhesion in irregular place of tooth or breakpoint.Within behind the cleaning of teeth several hours, form one deck sialomucin on the tooth, this sialomucin mainly is made up of albumen.Various oral cavity bacteriums move and give birth on the mucin and breeding, form one deck dental plaque.The polysaccharide food chip adheres to mucin and by the bacterial digestion of several generation dental plaques.This digestion has produced the by-product that is added on dental plaque, has also produced the adamantine acid of corrosion.The bacterial by-products that produces in the oral cavity also comprises the unpleasant gas that causes the oral cavity stink.
Antibacterial in mouthful on the dental plaque comprises many Gram-positives and gram negative bacteria, and they are embedded in the insoluble polysaccharide of chamber epimatrix, is attached to tooth and other oral surfaces firmly.The bacterial colonization of formation dental plaque is followed some aerobic strains that have earlier (mainly being the Gram-positive streptococcus) and is moved the ecological model of odontiasis enamel surfaces.The antibacterial complicated stage of this dental plaque by increasing further develops.Usually the ripe dental plaque of finding in protected tooth regions mainly contains anaerobe, and this zone is as slit, adjacent area and gingiva seam.Fluid is the nutrient source of dental plaque in saliva and the seam.Local condition influences the metabolic activity and the composition of dental plaque.
If do not prevented and remove, dental plaque will embed in the inorganic salt of calcic and phosphate radical, form hard shelly deposit, tooth dirt or tartar on tooth.The tartar color is a white or xanchromatic, perhaps can be through outside agent dyeing or decolouring.Tartar is seen than the more difficult quilt of dental plaque and is also more difficultly removed from tooth.Toxin in dental plaque and the tartar can stimulate and is covered in periodontal gingiva tissue, causes the damage of various focusing depths represented, and the damage of various focusing depths represented can cause other complication.
Zinc is the agent of a kind of anti-tooth dirt; Yet zinciferous compositions has astringent taste and undesirable bitterness usually.The same with biological activity with its chemistry, the undesirable mouthfeel of zinc ion is a dose dependent; The zinc of high concentration shows relatively poor mouthfeel; Therefore, increasing free zinc concentration will be that cost increases effect to sacrifice mouthfeel.Ambivalent behavior between this effect and mouthfeel has limited the application of zinc in oral composition.Pyrophosphate also is the agent of a kind of anti-tooth dirt, yet it has undesirable taste, and this taste becomes stronger when pyrophosphate concentration increases.Through preparing the compositions that contains zinc and pyrophosphate in earnest, the applicant is surprised to find the level that can increase zinc in mouthful compositions, improves its corresponding anti-tooth dirt effect thus, and does not increase the undesirable mouthfeel of said composition largely.
Be surprised to find that to separate this effect and the mouthfeel contain Zn composition be possible.When with a certain proportion of zinc: citrate and zinc: pyro preparation zinc just may be avoided the common unhappy mouthfeel relevant with zinc ion during with citrate and pyro.
An object of the present invention is to provide and stop the compositions that the tooth dirt forms in the oral cavity.
A further object of the invention provides and stops the compositions that dental plaque forms in the oral cavity.
Another object of the present invention provides and stops the method that the tooth dirt forms in the oral cavity.
A further object of the invention provides and stops the method that dental plaque forms in the oral cavity.
The present invention relates to the compositions of a kind of treatment or prevention dental plaque, tooth dirt and gingivitis or halitosis, it comprises:
(a) (ⅰ) a kind of zinc ion source of safe and effective amount;
(ⅱ) a kind of source of citrate ion; (ⅲ) one or more anti-tooth dirt agent, being selected from pyrophosphate, phosphonate, diphosphate and general formula is (PnO
(3n+1))
(n+2)-The pharmaceutically acceptable linear condensation polyphosphate of (wherein n is 2 to 21 integer);
Zinc wherein: the mol ratio of citrate was up to about 1: 1; The mol ratio of zinc: pyro is about 1: 1 at the most; With
(b) pharmaceutically useful local mouth carrier.
The invention still further relates to the method for treatment or prevention dental plaque, tooth dirt and gingivitis or halitosis, it comprises to people or other this compositions of animal oral administration.
The invention provides the compositions of effective antiplaque formation, the formation of tooth dirt, gingivitis and halitosis.
" pharmaceutically acceptable local mouth carrier " used herein refers to the carrier of reactive compound of the present invention (after this with " active substance " expression), it comprises solid or liquid filler diluent, and these diluent are applicable to and contact with the oral cavity of people and rudimentary animal and do not have (suitable reasonably useful/dangerous ratios) such as excessive toxicity, incompatibility, unstability, zest, anaphylaxiss.When using carrier to mix for this type of local mouthful, obtain being locally applied to the compositions in oral cavity with active substance of the present invention.Preferably this based composition is kept a period of time in the oral cavity, yet spue substantially rather than swallow.This based composition comprises collutory, dentilave liquid, oral spray, tooth treatment liquid, toothpaste, tooth glue, dentifrice, preventative toothpaste, lozenge, chewing gum etc., and these will more fully be described hereinafter.Toothpaste and collutory are preferred compositions.
" pyro " used herein is meant pyrophosphate; Phosphonate; Diphosphate and pharmaceutically acceptable polyphosphate, it is (PnO that the latter includes but is not limited to general formula
(3n+1))
(n+2)-, the polyphosphate of the linear condensation of (wherein n is 2 to 21 integer).
" free pyro " used herein is meant and do not combine with transition metal zinc or the pyro of chelating.
" free zinc " used herein is meant the zinc cation of hydration, for example Zn(H
2O)
2+ 6
Except as otherwise noted, the listed percent of this paper is the weight fraction of compositions.
The amount of pyro and citrate with oral composition in zinc content recently the expression.In mole, when the molal quantity of zinc was 1, being at least 1(with respect to the amount of the citrate of zinc is zinc: the mol ratio of citrate was about 1: 1 at the most); And the molal quantity at zinc is 1 o'clock, and be at least 1(promptly, zinc with respect to the amount of the pyro of zinc: the mol ratio of pyro was up to about 1: 1).Preferred zinc: the ratio of citrate is about 1: 1 to about 1: 20; More preferably from about 1: 1 to about 1: 4; Most preferably from about 1: 1 to about 1: 3.The ratio of preferred zinc: pyro is about 1: 1 to about 1: 20, more preferably from about 1: 1 to about 1: 8, and most preferably from about 1: 1.5 to about 1: 6.Again when the proportional of zinc is 1, zinc: citrate: the ionic molar ratio of citrate and pyro is counted sum and is preferably about 2 to about 9 in the pyro ratio, and more preferably from about 3 to about 9.
The zinc content that is suitable for the object of the invention is about 0.005% to about 5%Zn; More preferably from about 0.03% arrive about 3%Zn; Most preferably from about 0.05% arrive about 2%Zn.In dentifrice composition, preferred zinc content is about 0.1% to about 2%, more preferably from about 0.25% to about 1%.In rinse liquid, dentilave liquid, oral spray and toothwash liquid, preferred zinc content is about 0.005% to about 1%, more preferably from about 0.05% to about 0.5%.
The content that is suitable for the citrate of the object of the invention is about 0.015% to about 25% citrate.In the dentifrice composition, the content of citrate ion is preferably about 0.2% to about 17%, and more preferably from about 0.7% to about 12%, and most preferably from about 1.5% to about 5%.In rinse liquid, dentilave liquid, oral spray and the toothwash liquid, the content of citrate anion is preferably about 0.01% to about 12%, and more preferably from about 0.1% to about 6%, and most preferably from about 0.15% to about 1%.
The pyro ion concentration that is suitable for the object of the invention is about 0.015% to about 25%Pyro.In dentifrice composition, the ionic content of Pyro is preferably 0.25% to about 16%, and more preferably from about 0.6% to about 11%.In rinse liquid, dentilave liquid, oral spray and toothwash liquid, the content of pyro is preferably about 0.01% to about 11%, and more preferably from about 0.1% to about 5%.
Suitable zinc ion source comprises zinc oxide, zinc halogenide, zinc-strong acid coordination compound, Zn(NO
3)
2, Zn(ClO
4)
2, ZnSO
4Receive with organic acid zinc source such as zinc lactate, Tartaric acid zinc, citric acid zinc salt, citric acid zinc salt trihydrate and zinc citrate.Unacceptable zinc source is ethylenediaminetetraacetic acid zinc (ZnEDTA) and nitrilotriacetic acid(NTA) zinc (ZnNTA).Preferred zinc ion source comprises zinc oxide (ZnO) and zinc citrate; More preferably ZnO.
Suitable source of citrate ion comprises zinc citrate; Citric acid; Alkali metal citrates, particularly citric acid are received and potassium citrate; Above-mentioned any pharmaceutically acceptable water compound and dehydration salt; And above-mentioned any mixture of ingredients.
Suitable pyro ion source is disclosed in Parran ﹠amp; The United States Patent (USP) 4,885 of Sakkab, the 155(1989 December was published on the 5th); People's such as Widder United States Patent (USP) 3,678,154(1972 published July 18); People's such as Francis United States Patent (USP) 3,737,522(1973 published June 5); With people's such as Gaffer United States Patent (USP) 4,627, the 977(1986 December was published on the 9th); Above-mentioned patent all is incorporated herein by reference.Suitable pyro ion source comprises that tetrasodium pyrophosphate, pyrophosphoric acid two receive (Na
2H
2P
2O
7), tetrapotassium pyrophosphate (K
4P
2O
7); Phosphate includes but is not limited to the polyphosphate of linear condensation: its general formula is M
(n+2)PnO
(3n+1),, wherein M is Na or K, and n is from 2 to 21 integer; Phosphonic acids and di 2 ethylhexyl phosphonic acid, as EHDP(ethane-1-hydroxyl-1,1-di 2 ethylhexyl phosphonic acid and AHP(azepan-2,2-di 2 ethylhexyl phosphonic acid); The pharmaceutically acceptable alkali metal salt of pyrophosphoric acid, polyphosphoric acid, phosphonic acids and di 2 ethylhexyl phosphonic acid; And above-mentioned mixture.Preferred pyro ion is a pyrophosphate ion; Preferred multi-phosphate ion is 6,13 and 21 multi-phosphate ion for n in those following formulas.Owing to the dissolubility reason, preferred alkali metal is sodium and potassium; Also available bases metal salt mixture.
The PH of oral composition of the present invention is crucial, but variation to a certain degree can be arranged.The PH of this oral composition is preferably about 6 to about 9, and more preferably from about 6.25 to about 8.75, and most preferably from about 7.5 to about 8.5.
In preparation compositions process of the present invention, should make the condition that adds each component perfect as far as possible, so that any moment of the PH of mixture between the each component mixing period is not less than the PH of prescription.
" safety and effective dose " used herein means in correct medical care evaluation scope, be enough to induce chemical compound or the amount of composition that curing the desease disease is produced obvious positive regulating action, and this amount is low to being enough to avoid serious adverse (reasonably useful/risk-benefit risks).The safety of this chemical compound or compositions and effective dose will with the particular disorder of being treated, seriousness, treatment phase or same period of the patient's age of curing and physiological condition, disease treat characteristics, used particular compound or compositions, used specific factors such as pharmaceutically suitable carrier change.
Term used herein " contains " to mean in the compositions of the present invention and can together add various additional ingredients.
Be used for local mouthful of oral composition of the present invention with carrier component be fit to be applied to people or lower animal oral cavity and can with a kind of in addition with other component; Particularly compatible with active substance.
Term used herein " compatible " means component can be mixed with the interaction mode that can not reduce oral composition effect (under normally used condition) greatly mutually with a kind of other components.
Preferred local mouthful provides desirable characteristics with carrier to collutory, dentilave liquid, oral spray, tooth treatment liquid, toothpaste, tooth glue, dentifrice, preventative toothpaste, lozenge, chewing gum etc.Local mouthful of the present invention comprises with carrier and well known to a person skilled in the art the component that is used for this based composition.This type of component includes, but is not limited to dental caries agent, antiplaque agent, the agent of anti-tooth dirt, tooth abrasive material, surfactant, flavoring agent, sweeting agent, binding agent, wetting agent, thickening agent, buffer agent, antiseptic, coloring agent and dyestuff, ethanol and water.
Water is that local mouthful of the selectivity component with carrier, the used water of the commercial suitable compositions of preparation preferably contain low ion component, and do not contain organic impurity in the present composition.In the present composition, water content is preferably about 2% to about 99%, and more preferably from about 20% to about 95%.When being toothpaste form, said composition preferably contains 2% to about 80% the water of having an appointment, more preferably from about 30% to about 60% water; And rinse liquid preferably contain have an appointment 45% about 98%, 75% to about 98% water more preferably from about.
Comprise many different materials as local mouthful of tooth abrasive material in the present composition with carrier.Selected material must be a kind of can be compatible and excessively do not denude the material of tooth with this composition beneficial.These materials comprise for example silicon dioxide (comprising colloid and precipitate), calcium carbonate, dicalcium orthophosphate dihydrate, calcium pyrophosphate, tricalcium phosphate, many granule condensation products of phosphorus calcium, insoluble many Polymeric sodium metaphosphate ies, hydrated alumina and resin abrasive material such as urea and formaldehyde partially, and people's such as other material such as Cooley United States Patent (USP) 3,070, the publication on the 25th of 510(1962 December) disclosed material in, this patent is incorporated herein by reference.Also can use the mixture of abrasive material.
Various types of Silicon stone tooth abrasive materials have unique superior advantage and can excessively not denude enamel or dentine the cleaning and the burnishing action of tooth.Owing to this reason, this paper preferably uses these abrasive materials.
Be used for silicon dioxide polishing material and other abrasive material of this paper, general mean particle size range is between about 0.1 and 30 micron, preferably between about 5 and 15 microns.This abrasive silica can be precipitated silica or silica gel, as the silica xerogel described in the following patent: people's such as Pader United States Patent (USP) 3,538,230(1970 published March 2) and the United States Patent (USP) 3 of DiGiulio, 862,307(1975 published June 21), these two pieces of patents all are incorporated herein artificial reference.Preferably commodity are called Syloid
Commercially available silica xerogel, by W.R.Grace ﹠amp; Company Davidson Chemical Division produces.The preferred precipitated material comprises that those commodity of being sold by J.M.Huber Corporation are called those of Zeodent, particularly have Zeodent 119
The silicon dioxide of brand.The United States Patent (USP) 4,340 of Wason, 583(1982 published July 20) in these abrasive silica have been described, this patent is incorporated herein by reference.
Can use the mixture of abrasive material.When cleaning agent was toothpaste, the content range of abrasive material was about 6% to about 70%, preferred about 15% to about 50% in the compositions as herein described.If said composition is a dentifrice, can use higher content, as up to 90%.
Also flavoring agent can be added in the compositions of the present invention, so that theirs is better to eat.Suitable flavoring agent comprises menthol, wintergreen oil, Oleum menthae, Oleum Menthae Rotundifoliae, Sassafras oil and Oleum Caryophylli.The amount of the flavoring agent that contains in the present composition is usually 0% to about 3%, and preferred about 0.04% to about 2% weight.
Can in the present composition, add coloring agent to improve outward appearance.If contain coloring agent, its content is generally about 0.001% to about 0.5% weight.
Also preferably contain sweeting agent in the compositions of the present invention, so that its taste is more pleasant.Spendable sweeting agent comprises aspartame, acesulfame potassium, saccharin salt, dextrose, glucose, levulose, thaumation, D-tryptophan, dihydrochalcone and cyclamate.Preferred saccharin salt.Levels of sweetener commonly used is 0% to about 6% in the present composition, and preferred about 0.005% to about 5% weight.
Oral composition also can contain surfactant.Suitable surfactant is that those are suitably stable and form foamy surfactant in the extensive PH scope of cyclophon, comprises non-soap anionic, non-ionic, cationic, zwitterionic and both sexes organic synthesis detergent and compatible mixture thereof.People's such as Gieske United States Patent (USP) 4,051, the 234(1977 JIUYUE was published on the 27th) and Agricola, Briner, the United States Patent (USP) 3 of Granger and Widder, 959,458(1976 published May 25) the suitable surfactant of many these classes is disclosed, the two is incorporated herein by reference in the lump.The surfactant level that contains in the present composition typically is 0% to about 20%, and is preferred about 0.1, and more preferably from about 1% to about 4% weight.Surfactant also can be used as solubilizing agent and helps keep the slightly soluble component, and (as some flavoring agent) is in solution.Be suitable for this purpose surfactant and comprise Spheron MD 30/70 and Poloxamers.Preferred surfactants is to be nonionic under the prescription PH of said composition.
In the preparation present composition, particularly adding binding agent and/or thickening agent are ideal so that required denseness to be provided in dentifrice composition.The binding agent suitable to these compositionss is natural gum, as POLY-karaya, arabic gum and Tragacanth; Polysaccharide glue; As xanthan gum; With other natural product, as carrageenin; The natural product of chemical modification such as those are the ester of raw material with the cellulose, i.e. carboxymethyl cellulose (CMC), hydroxyethyl-cellulose (HEC) and hydroxypropyl cellulose (HPC); With composite adhesives such as polyvinylpyrrolidone; And water soluble salt such as the sodium carboxymethyl cellulose and the carboxymethyl hydroxyethyl cellulose sodium of cellulose ether.The carboxy vinyl polymer binding is not ideal, but also can use.Collodial silica magnalium or the very thin Silicon stone of pulverizing can be used as the part thickening agent with the further structure of improving.The admixture of suitable binders and mixture can obviously improve the feature with its compositions for preparing.Preferred adhesive is cellulose such as the CMC or the HEC of chemical modification; More preferably HEC.The binding agent that contains in the present composition and the amount of thickening agent are generally about 0.1% to about 10%, and preferred about 0.25% to about 7.5%, and more preferably from about 0.5% to about 3.5%.
The mouth of another selectable present composition is a wetting agent with carrier component.Wetting agent avoids dentifrice composition to be exposed in the air and hardening, and makes collutory and toothpaste have the mouth-moistening sense.Some wetting agent can also make collutory and toothpaste have sweet taste.The wetting agent that the compositions of this paper contains (coming in pure wetting agent) is generally 0% to about 70%, and preferred about 2% to about 55% weight.Be applicable to that the wetting agent in the present composition comprises edible polyhydric alcohol such as glycerol, sorbitol, xylitol, Polyethylene Glycol and propylene glycol, particularly sorbitol and glycerol.
Also opacifier can be used in the toothpaste of the present invention so that toothpaste is opaque.Suitable opacifier comprises titanium dioxide and some abrasive material, comprises for example Magnesiumaluminumsilicate.The opacifier that the compositions of this paper contains usually is 0% to about 4%, and preferred about 0.5% to about 3%(accounts for the weight of this paper compositions).
Other selectable component is an antiseptic in the present composition.Antiseptic can be avoided the bacterial growth in the compositions.Suitable antiseptic comprises methyl butex, propylparaben, benzoate (or vinegar) and ethanol.If antiseptic is an ethanol, then contain 0% in the compositions of this paper usually to about 35% weight, preferred about 5% to about 15% ethanol.The amount that contains other antiseptic in the compositions of this paper is generally 0% to about 5% weight, preferred about 0.1% to about 2%.
Also optionally contain antibiotic antiplaque agent in the oral composition of the present invention, condition is that they can be compatible with active substance.This type of medicament comprises (but being not limited to) The Merck Index 11th Ed.(1989), P
1520(go into hide number 9573) described triclosan, 2,4,4 '-three chloro-2 '-hydroxy diphenyl ether; Chlohexidine, (MerckIndex, No.2090); Win-21904 (Merck Index, NO.222); Triocil (MerckIndex No.4624); Sanguinarine (Merck Index No.8320); Benasept (Merck Index No.1066); N-phenylsalicylamide (Merck Index No.8299); The bromo methylpentynol (Merck Index, No.3411); Hexadecylpyridinium chloride (CPC) (Merck Index, No.2024); Four decyl pyridinium chlorides, (TPC) N-four decyls-4-ethyl pyridinium chloride (TDEPC); Octenidine; Delmopinol, Octapinol and other sub-base derivatives of piperidine; The nicin preparation; Antibiotic such as amoxicillin one clavulanic acid, amoxicillin, tetracycline, doxycycline, diformazan ammonia tetracycline, and metronidazole; And peroxide such as peroxidating cylium, hydrogen peroxide and monoperphthalic acid magnesium and analog thereof (as U.S. Patent No. 4,670, described in 252); And the analog and the salt of above-mentioned antibiotic antiplaque agent.If contain antibiotic antiplaque agent in the compositions of the present invention, then its content is 0% to about 6%, and preferred about 0.1% to about 5%(accounts for the weight of the present composition).
Also can contain bleach in the oral composition of the present invention.Suitable bleach comprises organic and inorganic oxidizer such as hydrogen peroxide, alkali-metal peroxide and superoxides and organic peroxide such as monoperphthalic acid salt (or ester) and benzylhydroperoxide derivant.If compositions of the present invention contains bleach, its content is 0% to about 6%, and preferred about 1% to about 5%(weight).
Also can contain nutrient in the oral composition of the present invention, condition is that they can be compatible with active substance.This class nutrient can comprise folate, retinoid (vitamin A), vitamin C, vitamin E.If contain nutrient in the compositions of the present invention, then its content is generally about 0.001% and accounts for composition weight of the present invention to about 10%().
Other selectable component comprises the fluoride sources of safety and effective dose, is typically the form of water-soluble fluorine chemical compound.The amount of the water-soluble fluorine chemical compound that typically contains in the compositions of the present invention is enough to provide 0.0025% fluorinion concentration to about 5.0% weight, and preferred about 0.005% to about 2.0%(weight).This sodium fluoride of preferred fluorine source, acidifying phosphoric acid fluoride and sodium monofluorophosphate.People's such as Widder United States Patent (USP) 3,678,154(1972 published July 18) this class salt and other material are disclosed, this patent is incorporated herein by reference.
Preferred compositions of the present invention is that dentifrice forms, especially toothpaste, the component of toothpaste generally includes tooth abrasive material (about 10% to about 50%), surfactant (about 0.5% to about 10%), thickening agent (about 0.1% to about 5%), wetting agent (about 10% to about 55%), flavoring agent (about 0.04% to about 2%), sweeting agent (about 0.1% to about 3%), coloring agent (about 0.01% to about 0.5%) and water (about 2% to about 45%).
Other preferred compositions of the present invention is dentilave liquid, collutory and oral spray.The component of this class collutory and oral spray comprises water (about 45% to about 95%), ethanol (about 0% to about 25%), wetting agent (0% to about 50%), surfactant (about 0.01% to about 7%), flavoring agent (about 0.04% to about 2%), sweeting agent (about 0.1% to about 3%) and coloring agent (about 0.001% to about 0.5%).Also can add antiplaque agent (about 0.1% to about 5%) in this type of dentilave liquid, collutory and the oral spray.
Other preferred composition of the present invention is a toothwash liquid.The component of this class toothwash liquid contains water (about 90% to about 99%), antiseptic (about 0.01% to about 0.5%), thickening agent (about 0% to about 5%), flavoring agent (about 0.04% to about 2%), sweeting agent (about 0.1% to about 3%) and surfactant (about 0% to about 5%) usually.
Another aspect of the present invention relates to the compositions that contains safety and effective dose active substance by using to oral cavity tissue, the method for the gingivitis of treatment or prevention halitosis, dental plaque, tartar.This based composition has above been described.
These methods relate to the active substance to oral administration safety and effective dose, pass through to oral administration oral composition of the present invention as indicated above typically.Usually the amount that contains at least about the compositions of 0.001g active substance is effective.Tooth and other oral cavity tissues are exposed in this active substance.
When the very moment compositions is toothpaste, apparatus as, the amount of paste that is coated with usefulness on the toothbrush typically is about 0.3 and restrains about 15 grams, preferred about 0.5 restrains about 5 grams, more preferably from about 1 restrains about 2 grams.Then with this apparatus so that oral composition and oral cavity tissue particularly the mode that contacts with gingiva of tooth contact with oral surfaces.Can further utilize this apparatus that oral composition is distributed in tooth surface, for example moving by brush.This using preferred lasting about 15 seconds to about 10 minutes, more preferably from about 30 seconds to about 3 minutes, most preferably from about 1 minute to about 2 minutes.After this, by with the acceptable liquid in a kind of oral cavity, be typically water, cleaning also spues from the oral cavity, and the toothpaste residue is removed from dental surface.
When the very moment compositions was collutory, this amount of introducing the liquid collutory that contains the antiplaque active substance in oral cavity typically was about 1ml to about 20ml, and preferred 2ml is to about 15ml, and most preferably from about 10ml is to about 15ml.Stir this collutory then in the oral cavity, so that this collutory is distributed in oral cavity tissue better, the stirring time is about 10 seconds to about 10 minutes, preferred 15 seconds to about 3 minutes, and more preferably from about 30 seconds to about 2 minutes.After the stirring, be typically collutory is spued from the oral cavity.
Frequency of utilization preferably about weekly 3 times to every day approximately 4 times, more preferably from about arrive pact every day 3 times once a day, most preferably about 1 to 2 time of every day.This type of treatment phase usually can be from about 1 day to all one's life.
Routine non-limiting example has further described and has illustrated the preferred embodiment in the scope of the invention down.The embodiment that provides only is used for explanation and is not construed as limiting the invention, and in the scope that does not deviate from spirit of the present invention, many variations of the present invention are possible.
The method that employing is generally used for producing the oral cavity health care product can prepare the present composition.
Embodiment I-XI
Followingly be the embodiment of Dentrifice composition of the present invention, they prepare with conventional method.The number of listing is the percetage by weight of compositions.Prepare during the various compositionss, minimum PH remains 7.5.
Slurry PH:7.1 to 7.3
Slurry pH:7.5 to 8.5
Embodiment XII-X VI
Classify the example of collutory of the present invention and dentilave fluid composition down as, they prepare with conventional method.Listed content is the percetage by weight of compositions.During the preparation, the PH of following compositions remains on minimum 7.5.
Though described specific embodiments of the present invention, for a person skilled in the art, do not deviated under spirit of the present invention and the scope.To this show effect various variations and adjustment is conspicuous.In appending claims, with whole these class adjustment that cover within the scope of the invention.
Claims (30)
1, a kind of compositions that is used for the treatment of or prevents dental plaque, tooth dirt and gingivitis or halitosis is characterized in that wherein containing:
(a) (i) zinc ion source of a kind of safety and effective dose; (ii) a kind of source of citrate ion; (iii) one or more anti-tooth dirt agent, being selected from pyrophosphate, phosphonate, diphosphate and general formula is (PnO
(3n+1))
(n+2)-The polyphosphate of pharmaceutically acceptable linear condensation, wherein n is 2 to 21 integer.
Wherein, zinc: the mol ratio of citrate was up to about 1: 1; The mol ratio of zinc: pyro is at most 1: 1; With
(b) a kind of pharmaceutically useful local mouth carrier.
2, according to the compositions of claim 1, zinc ion wherein: the mol ratio of citrate ion is about 1: 1 to about 1: 20, and the mol ratio of zinc ion and the agent of anti-tooth dirt is about 1: 1 to about 1: 20.
3, according to the compositions of claim 2, zinc ion wherein: the mol ratio of citrate ion is about 1: 1 to about 1: 5, the mol ratio of zinc ion and anti-tooth dirt agent is about 1: 1 to about 1: 5, and the mol ratio of citrate ion and the dirty agent of anti-tooth to count sum be about 2 to about 9.
4, according to the compositions of claim 2, zinc ion wherein: the mol ratio of citrate ion is about 1: 1 to about 1: 4, and the mol ratio of zinc ion and the agent of anti-tooth dirt is about 1: 1 to about 1: 8.
5, according to the compositions of claim 4, wherein the PH of said composition is about 6 to about 9.
6, according to the compositions of claim 5, wherein the PH of said composition be about 7.5 to about 8.5 and the mol ratio of citrate ion and the agent of anti-tooth dirt to count sum be about 3 to about 9.
7, the compositions of claim 1, it is the dentifrice form.
8, according to the compositions of claim 7, zinc ion wherein: the mol ratio of citrate ion is about 1: 1 to about 1: 20; Zinc ion: the mol ratio of anti-tooth dirt agent is about 1: 1 to about 1: 20; And wherein, pharmaceutically useful local mouthful contains the tooth abrasive material with carrier.
9, compositions according to Claim 8, wherein the mol ratio of zinc ion and citrate ion is about 1: 1 to about 1: 4; And zinc ion: the mol ratio of anti-tooth dirt agent is about 1: 1 to about 1: 8.
10, according to the compositions of claim 9, wherein PH is about 6 to about 9.
11, according to the compositions of claim 10, it contains 0.1% zinc ion to about 2% weight of having an appointment in addition, and the agent of anti-tooth dirt to be selected from pyrophosphate, EHDP, AHP and general formula be (PnO
(3n+1))
(n+2)-, the polyphosphate of linear condensation, wherein n is 6,13 or 21.
12, according to the compositions of claim 11, it contains 0.25% zinc ion to about 1% weight of having an appointment in addition.
13, according to the compositions of claim 11, it contains a kind of fluoride sources in addition, can obtain about 0.0025% fluorion to about 5% weight.
14, according to the compositions of claim 13, wherein the PH of said composition is about 7.5 to about 8.5.
15, according to the compositions of claim 14, the agent of wherein anti-tooth dirt is a pyrophosphate.
16, according to the compositions of claim 1, it is the mouth rinse form.
17, according to the compositions of claim 16, zinc ion wherein: the mol ratio of citrate ion is about 1: 1 to about 1: 20; Zinc ion: the mol ratio of anti-tooth dirt agent is about 1: 1 to about 1: 20; And wherein pharmaceutically useful local mouthful contains a kind of material that is selected from wetting agent, ethanol and a kind of non-ionic surface active agent with carrier.
18, according to the compositions of claim 17, zinc ion wherein: the mol ratio of citrate ion is about 1: 1 to about 1: 4, and zinc ion: the mol ratio of anti-tooth dirt agent is about 1: 1 to about 1: 8.
19, according to the compositions of claim 18, PH wherein is about 6 to about 9.
20, according to the compositions of claim 19, wherein contain in addition and have an appointment 0.005% to the zinc ion of about 1% weight, and the agent of anti-tooth dirt to be selected from pyrophosphate, EHDP, AHP and general formula be (PnO
(3n+1))
(n+2)-The polyphosphate of linear condensation, wherein n is 6,13 or 21.
21, according to the compositions of claim 20, it contains 0.05% zinc ion to about 0.5% weight of having an appointment in addition.
22, according to the compositions of claim 20, wherein the PH of said composition about 7.5 to about 8.5.
23, according to the compositions of claim 22, it contains a kind of fluoride sources in addition, to obtain about 0.0025% fluorion to about 5% weight.
24, according to the compositions of claim 23, the agent of wherein anti-tooth dirt is a pyrophosphate.
25, the method for a kind of treatment or prevention dental plaque, tooth dirt or halitosis comprises the compositions to the claim 1 of the oral administration safety of people or lower mammal and effective dose.
26, the method for a kind of treatment or prevention dental plaque, tooth dirt or halitosis comprises the compositions to the claim 5 of the oral administration safety of people or lower mammal and effective dose.
27, the method for a kind of treatment or prevention dental plaque, tooth dirt or halitosis comprises the compositions of using the claim 7 of safety and effective dose to people or lower mammal.
28, the method for a kind of treatment or prevention dental plaque, tooth dirt or halitosis comprises the compositions of using the claim 6 of safety and effective dose to people or lower mammal.
29, the method for a kind of treatment or prevention dental plaque, tooth dirt or halitosis comprises the compositions of using the claim 16 of safety and effective dose to people or lower mammal.
30, the method for a kind of treatment or prevention dental plaque, tooth dirt or halitosis comprises the compositions of using the claim 22 of safety and effective dose to people or lower mammal.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US148,776 | 1980-05-12 | ||
| US99333692A | 1992-12-18 | 1992-12-18 | |
| US993,336 | 1992-12-18 | ||
| US14877693A | 1993-11-16 | 1993-11-16 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1095263A true CN1095263A (en) | 1994-11-23 |
Family
ID=26846152
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 93119922 Pending CN1095263A (en) | 1992-12-18 | 1993-12-18 | The oral composition that contains antiplaque, the agent of anti-tooth dirt |
Country Status (10)
| Country | Link |
|---|---|
| EP (1) | EP0675706A1 (en) |
| JP (1) | JPH08505843A (en) |
| CN (1) | CN1095263A (en) |
| AU (1) | AU5740094A (en) |
| BR (1) | BR9307688A (en) |
| CA (1) | CA2151913A1 (en) |
| CZ (1) | CZ156795A3 (en) |
| HU (1) | HUT72041A (en) |
| MX (1) | MX9400053A (en) |
| WO (1) | WO1994014407A1 (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100360109C (en) * | 2001-05-15 | 2008-01-09 | 宝洁公司 | Oral care compositions |
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| US5302373A (en) * | 1993-06-10 | 1994-04-12 | Church & Dwight Co., Inc. | Liquid mouthwash containing a particulate bicarbonate suspension |
| CN1145583A (en) * | 1993-12-22 | 1997-03-19 | 史密斯克莱恩-比彻姆公司 | Tooth whitening preparations |
| US5599527A (en) * | 1994-11-14 | 1997-02-04 | Colgate-Palmolive Company | Dentifrice compositions having improved anticalculus properties |
| US5833955A (en) * | 1996-11-14 | 1998-11-10 | The Research Foundation Of State University Of New York | Diagnostic tests to assess a persons oral malodor capacity and potential for developing periodontitis |
| US6190644B1 (en) * | 1996-11-21 | 2001-02-20 | The Procter & Gamble Company | Dentifrice compositions containing polyphosphate and monofluorophosphate |
| US5939052A (en) * | 1996-11-21 | 1999-08-17 | The Procter & Gamble Company | Dentifrice compositions containing polyphosphate and fluoride |
| US6713049B1 (en) | 1999-11-12 | 2004-03-30 | The Procter & Gamble Company | Oral compositions providing optimal surface conditioning |
| DK176196B1 (en) | 1997-10-07 | 2007-01-08 | Ejvind Jersie Pedersen | Oral hygiene composition for the treatment of halitosis and the use of a chelate comprising a metal ion moiety and an amino acid moiety as a component of the composition |
| JPH11246376A (en) * | 1998-02-27 | 1999-09-14 | Sunstar Inc | Composition for oral cavity |
| US6846478B1 (en) * | 1998-02-27 | 2005-01-25 | The Procter & Gamble Company | Promoting whole body health |
| US6350438B1 (en) * | 1998-02-27 | 2002-02-26 | The Procter & Gamble Company | Oral care compositions comprising chlorite and methods |
| ES2225260T3 (en) | 1999-11-12 | 2005-03-16 | THE PROCTER & GAMBLE COMPANY | STANNED DOUBLE PHASE COMPOSITIONS IMPROVED. |
| CA2389174C (en) | 1999-11-12 | 2007-01-23 | The Procter & Gamble Company | Improved stannous oral compositions |
| US10470985B2 (en) | 1999-11-12 | 2019-11-12 | The Procter & Gamble Company | Method of protecting teeth against erosion |
| US20040146466A1 (en) | 1999-11-12 | 2004-07-29 | The Procter & Gamble Company | Method of protecting teeth against erosion |
| JP2001151651A (en) * | 1999-11-26 | 2001-06-05 | Earth Chem Corp Ltd | Composition for oral cavity |
| DE60134855D1 (en) * | 2000-06-30 | 2008-08-28 | Procter & Gamble | ORAL PREPARATIONS CONTAINING ANTIMICROBIAL ACTIVE SUBSTANCES FOR PREVENTING SYSTEMIC DISEASES |
| WO2002092027A2 (en) * | 2001-05-15 | 2002-11-21 | The Procter & Gamble Company | Confectionery compositions |
| WO2002092037A1 (en) * | 2001-05-15 | 2002-11-21 | The Procter & Gamble Company | Oral care confectionery compositions |
| JP3957293B2 (en) * | 2003-01-27 | 2007-08-15 | 花王株式会社 | Oral composition |
| DE10311171A1 (en) * | 2003-03-12 | 2004-09-23 | Henkel Kgaa | Oral and dental care composition with antitartar, antiplaque and anti-discoloration action, containing cationic antibacterial agent, aza-cycloalkane-diphosphonic acid and xanthan gum or carboxymethyl cellulose |
| GB0319566D0 (en) * | 2003-08-20 | 2003-09-24 | Unilever Plc | Use of oral care composition |
| TWI531379B (en) * | 2005-12-21 | 2016-05-01 | 美國棕欖公司 | Improved oral compositions comprising zinc citrate and/or tocopherol agents |
| ES2326382T3 (en) | 2006-03-22 | 2009-10-08 | The Procter And Gamble Company | ORAL COMPOSITIONS OF CINC. |
| RU2448680C2 (en) | 2007-11-09 | 2012-04-27 | Дзе Проктер Энд Гэмбл Компани | Oral compositions containing tin |
| MX347064B (en) | 2009-10-29 | 2017-04-11 | Colgate-Palmolive Company * | Dentifrice comprising stannous fluoride plus zinc citrate and low levels of water. |
| US10123953B2 (en) | 2012-06-21 | 2018-11-13 | The Procter & Gamble Company | Reduction of tooth staining derived from cationic antimicrobials |
| JP2018002660A (en) * | 2016-07-01 | 2018-01-11 | Ｎｓファーファ・ジャパン株式会社 | Oral composition |
| CN113747948B (en) | 2019-04-26 | 2023-12-15 | 宝洁公司 | Reduction of dental discoloration from cationic antimicrobial agents |
| JP2022099625A (en) * | 2020-12-23 | 2022-07-05 | 小林製薬株式会社 | Composition for oral cavity |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH0747531B2 (en) * | 1986-06-27 | 1995-05-24 | ライオン株式会社 | Oral composition |
| AU1746088A (en) * | 1987-06-12 | 1988-12-15 | Unilever Plc | Oral compositions |
| AU2090488A (en) * | 1987-08-28 | 1989-03-02 | Avantgarde S.P.A. | Chewing gum having antitartar activity |
| US4869898A (en) * | 1988-01-25 | 1989-09-26 | Colgate-Palmolive Co. | Anticalculus oral composition |
| GB8804817D0 (en) * | 1988-03-01 | 1988-03-30 | Unilever Plc | Anticalculas oral compositions |
| GB8922434D0 (en) * | 1989-10-05 | 1989-11-22 | Unilever Plc | Oral compositions |
| WO1992010994A1 (en) * | 1990-12-18 | 1992-07-09 | The Procter & Gamble Company | Oral compositions effective against plaque and gingivitis |
| US5240697A (en) * | 1991-10-17 | 1993-08-31 | Colgate-Palmolive Company | Desensitizing anti-tartar dentifrice |
-
1993
- 1993-12-06 WO PCT/US1993/011787 patent/WO1994014407A1/en not_active Application Discontinuation
- 1993-12-06 JP JP6515185A patent/JPH08505843A/en active Pending
- 1993-12-06 CZ CZ951567A patent/CZ156795A3/en unknown
- 1993-12-06 CA CA 2151913 patent/CA2151913A1/en not_active Abandoned
- 1993-12-06 HU HU9501784A patent/HUT72041A/en unknown
- 1993-12-06 AU AU57400/94A patent/AU5740094A/en not_active Abandoned
- 1993-12-06 BR BR9307688-6A patent/BR9307688A/en not_active Application Discontinuation
- 1993-12-06 EP EP94903459A patent/EP0675706A1/en not_active Withdrawn
- 1993-12-18 CN CN 93119922 patent/CN1095263A/en active Pending
-
1994
- 1994-01-03 MX MX9400053A patent/MX9400053A/en unknown
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100360109C (en) * | 2001-05-15 | 2008-01-09 | 宝洁公司 | Oral care compositions |
Also Published As
| Publication number | Publication date |
|---|---|
| MX9400053A (en) | 1994-07-29 |
| CA2151913A1 (en) | 1994-07-07 |
| EP0675706A1 (en) | 1995-10-11 |
| CZ156795A3 (en) | 1996-01-17 |
| JPH08505843A (en) | 1996-06-25 |
| HUT72041A (en) | 1996-03-28 |
| HU9501784D0 (en) | 1995-08-28 |
| WO1994014407A1 (en) | 1994-07-07 |
| AU5740094A (en) | 1994-07-19 |
| BR9307688A (en) | 1999-09-08 |
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