CN101111288A - Oral care composition comprising a phenolic compound and antioxidant vitamins and vitamin derivatives - Google Patents
Oral care composition comprising a phenolic compound and antioxidant vitamins and vitamin derivatives Download PDFInfo
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- CN101111288A CN101111288A CNA2005800476854A CN200580047685A CN101111288A CN 101111288 A CN101111288 A CN 101111288A CN A2005800476854 A CNA2005800476854 A CN A2005800476854A CN 200580047685 A CN200580047685 A CN 200580047685A CN 101111288 A CN101111288 A CN 101111288A
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Abstract
An oral care composition comprises an antibacterial phenolic compound and a vitamin or vitamin derivative component comprising one to a plurality of antioxidant vitamin or vitamin derivatives. In one embodiment the vitamin or vitamin derivative component comprises vitamin E and vitamin E acetate and optionally one or more additional vitamin or vitamin derivatives. In another embodiment the vitamin or vitamin derivative component comprises an antioxidant vitamin or vitamin derivative and a source of vitamin B5. A method of oral care comprises applying a composition as described above to an oral surface of a subject.
Description
The cross reference of related application
The application requires the rights and interests of the U.S. Provisional Patent Application sequence number the 60/632nd, 480 of pro-submission, and it submitted in December in 2004 on the 2nd, by reference its content was bonded to this paper.
Background of invention
Many phenolic compounds have antibiotic and anti-inflammatory property, and oneself knows for example to be suitable in collutory and the dentifrice at oral care composition and does antibiotic and/or antiinflammatory.The example of such phenolic compound comprises carvacrol, eugenol (thoxyphenol), 4-hexylresorcinol (4-hexyl-l, the 3-dihydroxy benzenes), bromine chlorophenol (2,2 '-di-2-ethylhexylphosphine oxide (4-chloro-6-bromophenol)), thymol (2-isopropyl-5-cresol) and triclosan (5-chloro-2-(2, the 4-dichlorophenoxy) phenol).
In addition, oneself it was suggested the composition of antioxidant as oral care composition for example avoid the stabilizing agent that oxidative degradation plays a role as the composition that is easy to oxidation by protection, and/or conduct improved the reagent of oral cavity and/or whole body health.Disclosedly comprise ascorbic acid (vitamin C) as oral care composition component and the chemical compound that is described to antioxidant, beta-carotene, folic acid, alpha-lipoic acid (thioctic acid), lycopene, phylloxanthin (xanthophyll), niacin usp (nicotiamide and/or nicotinic acid), retinol (vitamin A), riboflavin (vitamin B
2), rutin, alpha-tocopherol or vitamin E, 6-hydroxyl 2,5,7,8-tetramethyl chromanane-2-carboxylic acid, ubiquinone (ubiquinone
10).Do not report that such antioxidant has any effect to the anti-inflammatory property of the dentifrice that contains phenolic compound.
The invention summary
A kind of oral care composition that comprises at least a antimicrobial halogenated diphenyl ether compound and antioxidant ingredients is provided now; Wherein (a) at least a halogenated diphenyl ether compound exists with antibiotic effective total amount; (b) antioxidant ingredients comprises a kind of extremely multiple vitamin or vitamin derivative, and the amount of total vitamin or vitamin derivative can effectively improve the anti-inflammatory activity of compositions; (c) at least a vitamin or vitamin derivative are acceptable salt of ascorbic acid or its oral cavity or ester in the antioxidant ingredients, or 2-methyl-6-chromanol chemical compound.
Detailed Description Of The Invention
" the antibiotic phenolic compound " of this paper is to have the chemical compound of phenol moieties as its part molecular structure, demonstrates antibacterial activity when it exists with the acceptable amount in oral cavity in oral care composition.
" vitamin or the vitamin derivative " of this paper be vitamin and/or have the active chemical compound of vitamin-like, comprises natural and synthetic vitamin and vitamin D 3-analogies, derivant, precursor, ester, salt, isomer, racemic modification, enantiomer, tautomer etc.The vitamin of this paper " source " can be that vitamin itself, vitamin maybe produce or discharge the vitamin derivative of vitamin at oral surfaces and/or lower-hierarchy (underlying tissue) when being applied to oral surfaces, or presents the vitamin derivative of the vitamin activity that characterizes vitamin under other situation.This paper " multivitamin or vitamin derivative complex " refers to multivitamin or vitamin derivative.
Unless context needs in addition, term " vitamin E " usually comprises any tocopherol or tocotriene chemical compound in this article, comprises its any enantiomer or racemic modification, any such mixture with the active chemical compound of vitamin E.
When chatting at this paper and " at least a " during, it should be interpreted as that mentioned amount is meant the summation of the single amount of such whole members that exists in said composition for " total amount " in compositions of the component of particular types (for example antibiotic phenolic compound kind or antioxidant vitamin or vitamin-derived species) a member.Except as otherwise noted, the concentration of this paper composition is represented with weight.
This paper comprises any process that causes said composition to contact with this surface with compositions " application " in the step of oral surfaces, comprises flushing, gargles and wash, spraying, wiping, friction, brush, smear, place thin film or band with dental floss cleaning (floss), on this surface, implant and chew.
For example the term of oral tissue inflammation " inhibition " comprises prevention, suppresses (suppression) this paper, minimizing degree or seriousness or improve disease about disease.
Oral care composition of the present invention can adopt any physical form that is suitable for being applied to oral surfaces.In various illustrative embodiments, compositions can be to be suitable for washing, gargling the liquid solution of washing or spraying; Dentifrice is powder, toothpaste or the glue that cleans the teeth for example; Periodontal glue (periodontal gel); Be suitable for being applied in the liquid (for example liquid brightener) of dental surface; Chewing gum; Solubilized, can be partly dissolved or undissolved film or band (for example whitening strips); Thin slice (wafer); Wiping cloth or towelette; Implant; Dental floss; Deng.Compositions can contain additionally in those activity and/or the carrier components of above addressing.
In certain embodiments, compositions is suitable for being applied to small-sized domestic animal, for example the oral surfaces of cat or Canis familiaris L..Such compositions is animal edible or masticable typically, can adopt the form of cat for example or dog food, snacks (treat) or toy.
The present invention partly derive from following discovery, when to antibiotic phenolic compound, particularly have when adding antioxidant vitamin or vitamin derivative in so active halogenated diphenyl ether compound with anti-inflammatory activity, anti-inflammatory activity is enhanced.For example, find in antibiotic phenolic compound triclosan, to add antioxidant vitamin or vitamin derivative with the IC of triclosan in the PGE2 generation cell culture test (a kind of inflammatory model) that IL-1 β stimulates
50Value is reduced to wonderful degree.In this test, find that ascorbic acid, Vitamin E acetate and TROLOX (synthetic alpha-tocopherol analog) have especially effectively improved the anti-inflammatory activity of triclosan.Ascorbyl palmitate and vitamin E present not too significantly and improve; Do not accept opinion and limit, it is believed that solubility limits may reduce their effectiveness in this test.
Therefore, in one embodiment of the invention, provide a kind of compositions that comprises at least a antibiotic halogenated diphenyl ether compound and antioxidant ingredients.In the compositions of this embodiment, at least a halogenated diphenyl ether compound exists with antibiotic effective total amount, antioxidant ingredients comprises a kind of to multiple vitamin or vitamin derivative, and the total vitamin or the amount of vitamin derivative are effectively improved the anti-inflammatory activity of compositions.Discovery based on above summary, at least a vitamin in the antioxidant ingredients or vitamin derivative should be acceptable salt of ascorbic acid or its oral cavity or ester, or 2-methyl-6-chromanol chemical compound (for example vitamin E, Vitamin E acetate or TROLOX ).
At least a antibiotic halogenated diphenyl ether derivant for example can be, triclosan, triclosan monophosphate or 2,2 '-dihydroxy-5,5 '-dibromodiphenyl ether.
According to the present embodiment, at least a halogenated diphenyl ether compound for example, triclosan typically exists with about 0.01% total amount to about 10% weight in compositions.Concentration partly depends on the form of compositions; For example in collutory or mouth rinses, can use low relatively concentration, for example about 0.01% to about 0.5%, and in toothpaste or the glue that cleans the teeth (geldentifrice), find higher a little concentration usually, for example about 0.05% to about 5% is satisfactory.The total concentration of at least a halogenated diphenyl ether compound can be about 0.1% to about 2%, for example about 0.2% to about 1% or about 0.25% to about 0.5% in the toothpaste or the glue that cleans the teeth illustratively.
Vitamin that this paper is useful and vitamin derivative illustratively can be selected from following classification: (a) vitamin C source comprises ascorbic acid; (b) 2-methyl-6-chromanol chemical compound, comprise TROLOX , tocol (2-methyl-2-(4,8,12-trimethyl tridecyl)-the 6-chromanol), alpha-tocopherol ((+)-2,5,7,8-tetramethyl-2-(4,8,12-trimethyl tridecyl)-the 6-chromanol), betatocopherol ((+)-2,5,8-trimethyl-2-(4,8,12-trimethyl tridecyl)-the 6-chromanol), Gamma-Tocopherol ((+)-2,7,8-trimethyl-2-(4,8,12-trimethyl tridecyl)-the 6-chromanol), Delta-Tocopherol ((+)-8-methyl-2-(4,8,12-trimethyl tridecyl)-the 6-chromanol), alpha-tocotrienol (2,5,7,8-tetramethyl-2-(4,8,12-trimethyl-3,7,11-13 hydrocarbon trialkenyl (tridecatrienyl))-the 6-chromanol), β-tocotrienol (2,5,8-trimethyl-2-(4,8,12-trimethyl-3,7,11-tridecatrienyl)-the 6-chromanol) and vitamin E (mixture of any or any two or more tocopherols or tocotrienol); (c) carotenoid comprises retinol (vitamin A), retinal, tretinoin, alpha-carotene, beta-carotene, gamma carotene, δ-Radix Dauci Sativae, phylloxanthin, lycopene, lycophyll, lycoxanthin, rhodoxanthin, astaxanthin and cryptoxanthin; (d) vitamin B source comprises thiamine (vitamin B
1), riboflavin (vitamin B
2), nicotiamide and nicotinic acid (both all are called niacin usp), pantothenic acid (vitamin B
5), pantothenol, pyridoxol (vitamin B
6), 2-methyl-3-hydroxy-4-formyl-5-hydroxymethylpyridine., pyridoxamine, folic acid, dihydrofoilic acid, vitamin B
12And biotin; (e) bioflavonoids comprises rutin, hesperetin, Hesperidin, eriodictyol, Quercetin, quercetagetin and quercetagitrin; (f) quinoid enzyme co-factor comprises ubiquinone (ubiquinone
10) and pyrroloquinoline quinone (PQQ); (g) alpha-lipoic acid source; (h) vitamin D source comprises calciferol and cholecalciferol; And (i) the above acceptable salt in oral cavity, ester (comprise phosphate ester, acetas and long-chain ester, for example, linoleate and cetylate), isomer, enantiomer, racemic modification and tautomer.
The vitamin that this paper is useful and the source of vitamin derivative can be natural or synthetic and can make with extra care form or rough form, for example use with the form of herbaceous plant preparation (herbalpreparation).
According to an aspect of the present embodiment, antioxidant ingredients comprises acceptable salt of ascorbic acid and/or its oral cavity or ester.Illustrative salt comprises sodium salt, calcium salt and the zinc salt of ascorbic acid.Illustrative ester is an ascorbyl palmitate.According to the present embodiment on the other hand, antioxidant ingredients comprises 2-methyl-6-chromanol chemical compound.Illustrative ground, 2-methyl-6-chromanol chemical compound can be the acceptable salt of TROLOX or its oral cavity, or the acceptable ester of vitamin E or its oral cavity, for example Vitamin E acetate.
According to another aspect of the present embodiment, antioxidant ingredients comprises the acceptable salt of (a) ascorbic acid and/or its oral cavity or ester and (b) 2-methyl-6-chromanol, for example, and as mentioned above.
Antioxidant ingredients comprises further that randomly one or more are different from the vitamin or the vitamin derivative of vitamin C source or 2-methyl-6-chromanol chemical compound.Such vitamin or vitamin derivative for example can be, vitamin B source, for example thiamine, riboflavin, niacin usp, vitamin B
5, vitamin B
6Or folic acid, carotenoid for example, beta-carotene, phylloxanthin or lycopene, bioflavonoids, quinoid enzyme co-factor or alpha-lipoic acid source.
The total antibiotic halogenated diphenyl ether compound (one or more) that the amount of included antioxidant ingredients typically provides in the compositions of the present embodiment is about 10: 1 to about 1: 100 with the part by weight of total vitamin or vitamin derivative (one or more), for example about 5: 1 to about 1: 50, or about 2: 1 to about 1: 20, or about 1: 1 to about 1: 10.
The raising of anti-inflammatory activity is not by the unique advantage that provides oral care substance with one or more antibiotic phenolic compounds and one or more antioxidant vitamins or vitamin derivative to obtain.For example, can especially provide complementary benefit with antibacterial and antioxidant common application at oral health in oral surfaces in the periodontal zone.And the vitamin of vitamin or vitamin derivative component or vitamin-like activity can provide above oral cavity and whole body health benefit to be not limited to its antioxidation.Under the situation of vitamin E, discovery need comprise the vitamin of esterification and no esterification form.Do not accept opinion institute and limit, it is believed that having esterification and nonesterified form has strengthened sending and so strengthened its effectiveness as the vitamin of antioxidant.For example, vitamin E can provide of short duration burst effect and Vitamin E acetate provides permanent benefit.
Therefore, provide a kind of oral care composition in another embodiment of the invention, it comprises the antibiotic phenolic compound of at least a antimicrobial effective amount and comprises vitamin E and the vitamin of Vitamin E acetate or vitamin derivative component.In the compositions of this embodiment, at least a phenolic compound and vitamin or vitamin derivative component with about 10: 1 to about 1: 100 gross weight than existing.
Useful in this article phenolic compound comprises that illustratively through determining the oral cavity acceptability, by Dewhirst (1980), Prostaglandins 20 (2), and 209-222 confirms as those with anti-inflammatory activity, but is not limited to wherein.The example of antibiotic phenolic compound comprises 4-pi-allyl catechol, and p-Hydroxybenzoate comprises benzyl p-hydroxybenzoate, butyl p-hydroxybenzoate, ethylparaben, methyl parahydroxybenzoate and propyl p-hydroxybenzoate, the 2-benzylphenol, butylated hydroxyanisole, butylated hydroxytoluene, capsaicin, carvacrol, creosol, eugenol, guaiacol, the halogenated bisphenol that comprises hexachlorophene and bromine chlorophenol, the 4-hexylresorcinol, oxine and its salt, salicylate, comprise menthyl salicylate, methyl salicylate and phenyl salicytate, phenol, pyrocatechol, salicylanilide, thymol, triclosan and triclosan monophosphate.
At least a in one aspect antibiotic phenolic compound is a halogenated diphenyl ether, triclosan for example, and triclosan monophosphate or 2,2 '-dihydroxy-5,5 '-dibromodiphenyl ether.
At least a phenolic compound exists with about 0.01% total amount to about 10% weight.The total concentration of at least a phenolic compound can be about 0.05% to about 5%, for example about 0.1% to about 2%, about 0.2% to about 1% or about 0.25% to about 0.5% in the toothpaste of the present embodiment or the glue that cleans the teeth illustratively.
Vitamin or vitamin derivative component comprise vitamin E, for example, and alpha-tocopherol form, and Vitamin E acetate, for example alpha-tocopherol acetate form.Vitamin E and Vitamin E acetate part can be any suitable weight ratios, for example about 20: 1 to about 1: 10, or about 15: 1 to about 1: 5, or about 5: 1 to about 1: 1.The total concentration of vitamin E and Vitamin E acetate can be about 0.05% to about 5%, for example about 0.1% to about 2.5% or about 0.2% to about 1% in the toothpaste or the glue that cleans the teeth illustratively.
According to an aspect of the present embodiment, vitamin or vitamin derivative component may further include one or more vitamin that is different from vitamin E and Vitamin E acetate or vitamin derivatives.As an example, optional at least a vitamin C source for example ascorbic acid, sodium ascorbate, calcium ascorbate, ascorbic acid zinc or the ascorbyl palmitate of further comprising of said composition.As another example, said composition randomly further comprises at least a carotenoid for example retinol, the acceptable salt of tretinoin or its oral cavity, vitamin A palmitate, beta-carotene, phylloxanthin or lycopene.As another example, said composition randomly further comprises at least a vitamin B source for example thiamine, riboflavin, niacin usp, vitamin B
5, vitamin B
6Perhaps folic acid.As another example, optional for example rutin or derivatives thereof of at least a bioflavonoids, for example rutin sulfuric ester, the sodium salt of further comprising of said composition.As another example, optional at least a quinoid enzyme co-factor for example ubiquinone or the PQQ of further comprising of said composition.As another example, said composition further comprises at least a alpha-lipoic acid source.
Another aspect according to the present embodiment, vitamin or vitamin derivative component can be the complex of multivitamin or vitamin derivative, except that vitamin E and Vitamin E acetate, additionally comprise the multivitamin or the vitamin derivative that are selected from following at least two kinds: (a) vitamin C source; (b) carotenoid; (c) vitamin B source; (d) bioflavonoids; (e) quinoid enzyme co-factor; (f) alpha-lipoic acid source; (g) vitamin D source.
According to the present embodiment, illustrative ground and being not limited thereto, the example of following multivitamin or vitamin derivative complex is useful, wherein with the listed any vitamin of the form of acid can randomly be all or part of be the form of acceptable salt in oral cavity or ester:
1. vitamin E+Vitamin E acetate;
2. vitamin E+Vitamin E acetate+ascorbic acid;
3. vitamin E+Vitamin E acetate+ascorbyl palmitate;
4. vitamin E+Vitamin E acetate+beta-carotene;
5. vitamin E+Vitamin E acetate+lycopene;
6. vitamin E+Vitamin E acetate+ascorbic acid+beta-carotene;
7. vitamin E+Vitamin E acetate+ascorbic acid+beta-carotene+lycopene;
8. vitamin E+Vitamin E acetate+pantothenic acid;
9. vitamin E+Vitamin E acetate+ascorbic acid+pantothenic acid;
10. vitamin E+Vitamin E acetate+vitamin B
6
11. vitamin E+Vitamin E acetate+ascorbic acid+vitamin B
6
12. vitamin E+Vitamin E acetate+ascorbic acid+pantothenic acid+vitamin B
6
13. vitamin E+Vitamin E acetate+ascorbic acid+beta-carotene+lycopene+pantothenic acid+vitamin B
6+ folic acid;
14. vitamin E+Vitamin E acetate+rutin;
15. vitamin E+Vitamin E acetate+ubiquinone;
16. vitamin E+Vitamin E acetate+alpha-lipoic acid;
17. vitamin E+Vitamin E acetate+calciferol;
18. vitamin E+Vitamin E acetate+ascorbic acid+beta-carotene+lycopene+pantothenic acid+vitamin B
6+ folic acid+rutin+ubiquinone+alpha-lipoic acid.
The total antibiotic phenolic compound that the amount of included vitamin or vitamin derivative component provides illustratively in the compositions of the present embodiment is about 5: 1 to about 1: 50 with the weight ratio of total vitamin or vitamin derivative component, for example about 2: 1 to about 1: 20, or about 1: 1 to about 1: 10.
In another embodiment of the present invention, a kind of oral care composition is provided, the antibiotic halogenated diphenyl ether compound that comprises at least a antimicrobial effective amount, with vitamin or vitamin derivative component, it comprises (a), and one or more are selected from ascorbic acid, the antioxidant vitamin of acceptable salt in its oral cavity and ester and 2-methyl-6-chromanol chemical compound or vitamin derivative and (b) at least a vitamin B
5The source.In the context of the present embodiment, will be understood that " one or more antioxidant vitaminses or vitamin derivative " is different from vitamin B
5Source but add in addition.Vitamin B
5Antioxidant can or can not played in the source in compositions.In the compositions of this embodiment, at least a halogenated diphenyl ether compound and vitamin or vitamin derivative component with about 10: 1 to about 1: 100 gross weight than existing.
At least a antibiotic halogenated diphenyl ether compound can be selected from triclosan aptly, triclosan monophosphate and 2,2 '-dihydroxy-5,5 '-dibromodiphenyl ether.
At least a halogenated diphenyl ether compound also exists with about 0.01% total amount to about 10% weight.Illustrative ground, the total concentration of at least a halogenated diphenyl ether compound is about 0.05% to about 5%, for example about 0.1% to about 2%, about 0.2% to about 1% or about 0.25% to about 0.5% in the toothpaste or the glue that cleans the teeth.
Aspect of the present embodiment, vitamin or vitamin derivative component comprise natural or the synthesising complex E source, for example alpha-tocopherol or Vitamin E acetate, for example, the alpha-tocopherol acetate.Randomly vitamin E and Vitamin E acetate all exist, and for example with about 20: 1 to about 1: 10, or about 15: 1 to about 1: 5, or exist to about 1: 1 weight ratio in about 5: 1.Illustrative ground is different from vitamin B in the toothpaste or the glue that cleans the teeth
5The antioxidant vitamin in source or the vitamin derivative for example total concentration in vitamin E source are about 0.05% to about 5%, for example about 0.1% to about 2.5% or about 0.2% to about 1%.
According to the present embodiment, vitamin or vitamin derivative component comprise at least a natural or synthetic vitamin B
5The source, for example acceptable salt of pantothenic acid or its oral cavity or ester, or pantothenol.At least a vitamin B
5The total amount that the source exists illustratively makes vitamin B
5The source be different from vitamin B
5The antioxidant vitamin in source or the weight ratio of vitamin derivative are about 1: 100 to about 1: 1, for example about 1: 50 to 1: 5.The vitamin B of the toothpaste or the glue that cleans the teeth
5The source total concentration is about 0.005% to about 1%, for example about 0.01% to about 0.5% or about 0.02% to about 0.2% illustratively.
According to another aspect of the present embodiment, vitamin or vitamin derivative component can be multivitamin or vitamin derivative complex, comprise vitamin B
5Source (for example, acceptable salt of pantothenic acid or its oral cavity or ester) and be selected from the multivitamin or the vitamin derivative of following at least two kinds: (a) vitamin E source; (b) vitamin C source; (c) carotenoid; (d) be different from vitamin B
5The vitamin B source; (e) bioflavonoids; (f) quinoid enzyme co-factor; (g) alpha-lipoic acid source; (h) vitamin D source; Wherein at least a in multivitamin or the vitamin derivative is antioxidant.
According to this embodiment, illustrative ground and being not limited thereto, the example of following multivitamin or vitamin derivative complex is useful, wherein with the listed any vitamin of the form of acid can randomly be all or part of be the form of acceptable salt in oral cavity or ester:
1. vitamin E+pantothenic acid;
2. vitamin E+ascorbic acid+pantothenic acid;
3. ascorbic acid+pantothenic acid;
4. vitamin E+pantothenic acid+beta-carotene;
5. vitamin E+pantothenic acid+lycopene;
6. vitamin E+ascorbic acid+pantothenic acid+beta-carotene;
7. vitamin E+ascorbic acid+pantothenic acid+beta-carotene+lycopene;
8. vitamin E+pantothenic acid+vitamin B
6
9. ascorbic acid+pantothenic acid+vitamin B
6
10. vitamin E+ascorbic acid+pantothenic acid+vitamin B
6
11. vitamin E+ascorbic acid+pantothenic acid+beta-carotene+lycopene+vitamin B
6+ folic acid;
12. vitamin E+pantothenic acid+rutin;
13. vitamin E+pantothenic acid+ubiquinone;
14. vitamin E+pantothenic acid+alpha-lipoic acid;
15. vitamin E+pantothenic acid+calciferol;
16. vitamin E+ascorbic acid+pantothenic acid+beta-carotene+lycopene+vitamin B
6+ folic acid+rutin+ubiquinone+alpha-lipoic acid.
How the pantothenol in illustrative Multivitamin or the vitamin derivative complex (having another name called pantothenylol, for example the DL-pantothenylol) of going up in office can randomly completely or partially substitute pantothenic acid or its salt or ester.
The total antibiotic halogenated diphenyl ether compound that the amount of included vitamin or vitamin derivative component provides illustratively in the present embodiment compositions is about 5: 1 to about 1: 50 with total vitamin or vitamin derivative components by weight, for example about 2: 1 to about 1: 20, or about 1: 1 to about 1: 10 amount.
Illustrative ground, the compositions of the above any embodiment is collutory or gargles lotion, mouthspray, dentifrice, oral cavity bar, liquid brightener or chewing gum.Irrigation comprises and being suitable for by means of installing for example liquid of high-pressure water jet flushing.Dentifrice includes but not limited to toothpaste, gel and powder.This paper's " liquid brightener " comprise semi-liquid composition example gel and flowable liquid, as long as can said composition be applied to dental surface by smearing with hairbrush or other suitable device.In this paper context, " smear " applied in very thin layers that refers to compositions to dental surface.In one embodiment, said composition is the toothpaste or the glue that cleans the teeth.
Compositions of the present invention can also comprise one or more activating agents (" active matter ") except that at least a antibiotic phenols (for example halogenated diphenyl ether) chemical compound and vitamin or vitamin derivative or antioxidant ingredients as defined above.
Useful active matter is those solutions (addressing), the active matter of tooth outward appearance and structural change without limitation,, treatment and pre-preventing dental plaque, tartar, dental caries, dental cavity, abscess, inflammation and/or gingival hemorrhage, gingivitis, oral cavity infection and/or common inflammatory conditions, dental hyperesthesia, halitosis or the like.Therefore, compositions of the present invention can contain antibacterial that one or more active matters for example also can contain beyond the brightening agent, fluoride sources, at least a antibiotic phenols (for example halogenated diphenyl ether) chemical compound, desensitizer, anti-tartar (tartar control) agent, stannous ion source, zinc ion source, salivator, flavorants, antiplaque agent, except that any antiinflammatory phenolic compound of existence extra antiinflammatory, periodontal agent (periodontalagents), except that at least a vitamin or vitamin derivative extra analgesic and nutrient.Active matter should be selected so that it is compatible and compatible with other composition of compositions mutually.
When compositions repeated use as described herein, the activating agent that this paper is useful exists with selected safety and effective amount in compositions usually, it is the benefit that its consumption is enough to provide needs, for example treat, prevention, nutrition or dressing effect, and there is not for example toxicity of over-drastic side effect, stimulate or anaphylaxis, match with rational interests/risk ratio.Such safety and effective amount are common in the scope of the administrative organization's approval that is fit to, but not necessarily.The safety of concrete condition and effective dose depend on many factors, comprise needs particular benefits or treat or the disease of seeking to prevent, specific use or be applied the frequency of patient, compositions, use and persistent period or the like.Activating agent typically with composition weight about 0.01% to about 80%, for example about 0.05% to about 60%, about 0.1% to about 50%, or about 0.5% to about 40% total amount exists.
One or more activating agents comprise that the antibacterial of this paper and/or vitamin or vitamin derivative component can randomly exist with the encapsulation form in compositions.For example, the bead that comprises one or more activating agents is suitable for breaking in the process so that activating agent (one or more) is released into oral surfaces brushing or chew.Additionally, compositions of the present invention can comprise any existence or the conventional component of needs in oral care product.For example, compositions can comprise brightening agent, for example per-compound, chlorine dioxide, chlorite and hypochlorite, polymer-peroxide complex, polyvinylpyrrolidone-hydrogen peroxide (PVP-H
2O
2) complex; Fluoride sources (mono-fluor phosphate and fluosilicate), antibacterial.Activating agent for example antibacterial can comprise, for example comprises those are listed in No. the 5th, 776,435, people's such as Gaffar United States Patent (USP) those, and its content is incorporated herein by reference.Said composition may further include tooth anti-sensitizer, salivator (saliva stimulant), flavorants, antiplaque or dental plaque cracking agent.
The optional useful carrier that comprises is diluent, abrasive material, bicarbonate, pH regulator agent, surfactant, foam modifier, thickening agent, viscosity modifier, wetting agent, sweeting agent, spice and coloring agent in the present composition.Can randomly there be a kind of carrier material or more than a kind of carrier material of identical or different kind.Water is preferable absorbent, for example can be in collutory and the whitening fluid in some compositions with other solvent, and alcohol for example, for example, ethanol.
Said composition can comprise abrasive material, pH regulator agent, surfactant, foam modifier, thickening agent, viscosity modifier, wetting agent, sweeting agent, spice, coloring agent.
The present invention further provides the method for mouth care, comprised the step that compositions as described herein is applied to patient's oral surfaces.In one embodiment, said composition is the toothpaste or the glue that cleans the teeth, and applying step comprises with dentifrice brushes this surface, for example the periodontal surface adjacent with it, the surface of tooth.
According to the working of an invention scheme, further provide the method that suppresses patient's oral tissue inflammation.The method of the present embodiment comprises the oral surfaces that compositions of the present invention is applied to contiguous this tissue.The method that promotes patient's oral health is provided in another embodiment.The method of the present embodiment comprises the oral surfaces that compositions of the present invention is applied to the patient.
The enforcement of the inventive method can promote any aspect or the many aspects of oral health.As an example, such method can promote periodontal and/or gums health, for example by reducing bacterial infection and/or inflammation.As another example, such method can provide the benefit of breath freshening, for example passes through antioxidant activity.As another example, such method can improve the tooth maintenance, for example by minimizing or caries prevention and the destruction that prevents from tooth is retained in the bone matrix of original position.As another example, such method can provide the antiplaque benefit.As another example, such method can help the patient resist oral cancer and pre-cancer disease defense mechanism.As another example, such method can reduce free radical, comprises the infringement of the radical pair oral cavity tissue that occurs owing to contact tobacco smoke or contaminated air.
Health is advanced in the well-known oral cavity of improving, and bacterial infection that particularly improves and reduce and/or the associated periodontal of inflammation and/or gums health can produce general or whole health advantages.Send vitamin by oral surfaces and can be further usually improve general health as provided herein by replenishing with supporting one's family of absorbing of food.
The systemic disorders that takes a turn for the better owing to the improvement of oral health after implementing method of the present invention is a cardiovascular disease, comprises atherosclerosis, coronary heart disease (CHD) and apoplexy; Diabetes; Respiratory tract infection, comprise bacterial pneumonia; The premature labor low birth weight; Gastric ulcer; Bacteremia; Infective endocarditis; Prosthetic appliance infects; Chronic obstructive pulmonary disease (COPD); Behavior and social mentality's obstacle; And brain abscess.
The enforcement of this method is made up of single application as described herein, maybe can comprise the application that repetition is such.In one embodiment, be in and/or in program or scheme that specialty or clinical setting carry out, repeat method as described herein termly, twice of every day or once for example, or twice or once weekly, every month twice or once.
How the patient in the above method in office can be people or non-human mammal, for example Canis familiaris L., cat, horse or adventive mammal.The patient is small-sized domestic animal in certain embodiments, and for example cat or Canis familiaris L. can be with foods, and the compositions of snacks or toy form gives animal chew.
By can further understanding the present invention with reference to following non-limiting example.
Embodiment
Embodiment 1
Preparation has the dentifrice composition of composition as shown in table 1.Comparative composition 1Z is the toothpaste based on glycerol/Sorbitol that contains Silicon stone abrasive material, PVME/MA (GANTREZ ) anticalculus agents, sodium fluoride and other conventional ingredients for preparing routinely.Triclosan exists with 0.3% amount.Compositions 1A of the present invention is substantially the same, except add Vitamin E acetate and DL-pantothenylol as noted in Table 1 at final blend step.
Table 1: dentifrice composition (percetage by weight)
| Composition | Composition no | |
| 1Z | ?1A | |
| Toothpaste matrix 1 | 99.70 | ?99.55 |
| Triclosan | 0.30 | ?0.30 |
| Vitamin E acetate | ?0.10 | |
| The DL-pantothenylol | ?0.05 | |
1Toothpaste matrix comprises following composition: silica powder, glycerol, Sorbitol, water, GANTREZ , sodium lauryl sulphate, sodium hydroxide, titanium dioxide, spice, CMC sodium, t-carrageenin, sodium fluoride, saccharin sodium
Embodiment 2
Preparation has the dentifrice composition of composition as shown in table 2.Comparative composition 2Z is the toothpaste based on Sorbitol that contains Silicon stone abrasive material, PVME/MA (GANTREZ ) anticalculus agents, sodium fluoride and other conventional ingredients for preparing routinely.Triclosan exists with 0.3% amount.Compositions 2A of the present invention is substantially the same, except add Vitamin E acetate and DL-pantothenylol as noted in Table 2 at final blend step.
Table 2: dentifrice composition (percetage by weight)
| Composition | Composition no | |
| ?2Z | ?2A | |
| Toothpaste matrix 2 | ?99.70 | ?99.55 |
| Triclosan | ?0.30 | ?0.30 |
| Vitamin E acetate | ?0.10 | |
| The DL-pantothenylol | ?0.05 | |
2Toothpaste matrix comprises following composition: Sorbitol, water, silica powder, GANTREZ , sodium lauryl sulphate, sodium hydroxide, titanium dioxide, spice, t-carrageenin, glycerol, sodium fluoride, saccharin sodium
Embodiment 3
Preparation has the dentifrice composition of composition as shown in table 3.Comparative composition 3Z is the toothpaste based on glycerol/Sorbitol that contains Silicon stone abrasive material, PVME/MA (GANTREZ ) anticalculus agents, sodium fluoride and other conventional ingredients for preparing routinely.Triclosan exists with 0.3% amount.Compositions 3A-3F of the present invention is substantially the same, except adding vitamin as noted in Table 3 at final blend step.
Table 3: dentifrice composition (percetage by weight)
| Composition | Composition no | ||||||
| 3Z | ?3A | ?3B | ?3C | ?3D | ?3E | ?3F | |
| Toothpaste matrix 3 | 99.70 | ?97.40 | ?98.40 | ?99.15 | ?99.30 | ?98.45 | ?99.10 |
| Triclosan | 0.30 | ?0.30 | ?0.30 | ?0.30 | ?0.30 | ?0.30 | ?0.30 |
| Vitamin E acetate | ?0.20 | ?0.20 | ?0.20 | ?0.20 | ?0.20 | ?0.20 | |
| Vitamin E | ?2.00 | ?1.00 | ?0.30 | ?0.10 | ?1.00 | ?0.30 | |
| The DL-pantothenylol | ?0.05 | ?0.05 | ?0.05 | ?0.05 | ?0.05 | ?0.05 | |
| Vitamin C | ?0.05 | ?0.05 | ?0.05 | ?0.05 | |||
3Toothpaste matrix comprises following composition: water, silica powder, Sorbitol, glycerol, GANTREZ , sodium lauryl sulphate, sodium hydroxide, CMC sodium, propylene glycol, titanium dioxide, saccharin sodium, sodium fluoride
Embodiment 4
Preparation has the dentifrice composition of composition as shown in table 4.Comparative composition 4Z is the toothpaste based on Sorbitol that contains Silicon stone abrasive material, PVME/MA (GANTREZ ) anticalculus agents, sodium fluoride and other conventional ingredients for preparing routinely.Triclosan exists with 0.3% amount.Compositions 4A of the present invention is substantially the same, except add Vitamin E acetate, vitamin E and DL-pantothenylol as noted in Table 4 at final blend step.
Table 4: dentifrice composition (percetage by weight)
| Composition | Composition no | |
| ?4Z | ?4A | |
| Toothpaste matrix 4 | ?99.70 | ?99.55 |
| Triclosan | ?0.30 | ?0.30 |
| Vitamin E acetate | ?0.10 | |
| Vitamin E | ?0.30 | |
| The DL-pantothenylol | ?0.05 | |
4Toothpaste matrix comprises following composition: Sorbitol, water, silica powder, propylene glycol, GANTREZ , sodium lauryl sulphate, sodium hydroxide, t-carrageenin, titanium dioxide, saccharin sodium, sodium fluoride.
Claims (37)
1. an oral care composition comprises antimicrobial halogenated diphenyl ether compound and antioxidant ingredients, and wherein antioxidant ingredients comprises one or more vitamin or vitamin derivative; Wherein at least a in one or more vitamin or the vitamin derivative is ascorbic acid, its salt or ester, or 2-methyl-6-chromanol.
2. the compositions of claim 1, wherein the halogenated diphenyl ether compound is a triclosan.
3. the compositions of claim 1, wherein the halogenated diphenyl ether compound exists with about 0.01% to about 10% amount of composition weight.
4. the compositions of claim 1 is the toothpaste or the glue form that cleans the teeth.
5. the compositions of claim 5, wherein at least a halogenated diphenyl ether compound exists with about 0.05% total amount to about 5% weight.
6. the compositions of claim 1, wherein antioxidant ingredients comprises acceptable salt of ascorbic acid and/or its oral cavity or ester.
7. the compositions of claim 1, wherein antioxidant ingredients comprises at least a 2-methyl-6-chromanol chemical compound.
8. the compositions of claim 8, wherein at least a 2-methyl-6-chromanol chemical compound is selected from 6-hydroxyl-2,5,7, the acceptable salt of 8-tetramethyl chromanane-2-carboxylic acid and oral cavity thereof, the acceptable vitamin-e ester in vitamin E and oral cavity.
9. the compositions of claim 1, wherein antioxidant ingredients comprises the acceptable salt of ascorbic acid and/or its oral cavity or ester and at least a 2-methyl-6-chromanol chemical compound.
10. the compositions of claim 10, wherein at least a 2-methyl-6-chromanol chemical compound is selected from 6-hydroxyl-2,5,7, the acceptable salt of 8-tetramethyl chromanane-2-carboxylic acid and oral cavity thereof, the acceptable vitamin-e ester in vitamin E and oral cavity.
11. the compositions of claim 1, wherein antioxidant ingredients further comprise at least a be selected from vitamin B source, carotenoid, bioflavonoids, quinoid enzyme co-factor, alpha-lipoic acid source, and composition thereof vitamin or vitamin derivative.
12. the compositions of claim 1, wherein at least a halogenated diphenyl ether compound and vitamin or vitamin derivative with about 10: 1 to about 1: 100 gross weight than existing.
13. the compositions of claim 1, wherein at least a halogenated diphenyl ether compound and vitamin or vitamin derivative with about 1: 1 to about 1: 10 gross weight than existing.
14. an oral care composition comprises the antibiotic phenolic compound of at least a antimicrobial effective amount and comprises vitamin E and the vitamin of Vitamin E acetate or vitamin derivative component; Wherein at least a phenolic compound and vitamin or vitamin derivative component with about 10: 1 to about 1: 100 gross weight than existing.
15. the compositions of claim 15, its form are to be suitable for washing, gargling the liquid solution of washing or spraying; Powder, toothpaste or the glue that cleans the teeth; Periodontal glue; Be suitable for being applied in the liquid of dental surface; Chewing gum; Solubilized, can be partly dissolved or insoluble film or band; Thin slice; Wiping cloth or towelette; Implant; Or dental floss.
16. the compositions of claim 15 is hog edible or masticable.
17. the compositions of claim 15, wherein at least a phenolic compound is selected from 4-pi-allyl catechol, P-hydroxybenzoic acid benzyl ester, the 2-benzylphenol, bromochlorobenzene, butylated hydroxyanisole, butylated hydroxytoluene, butyl p-hydroxybenzoate, capsaicin, carvacrol, creosol, aethyl parabenum, eugenol, guaiacol, hexachlorophene, the 4-hexylresorcinol, oxine and its salt, menthyl salicylate, methyl parahydroxybenzoate, methyl salicylate, phenol, phenyl salicytate, propyl parabene, pyrocatechol, N-phenylsalicylamide, thymol, triclosan and triclosan monophosphate and composition thereof.
18. the compositions of claim 15, wherein at least a phenolic compound is a halogenated diphenyl ether.
19. the compositions of claim 15, wherein at least a phenolic compound is a triclosan.
20. the compositions of claim 15, wherein at least a phenolic compound exists with about 0.01% total amount to about 10% weight.
21. the compositions of claim 15 is the toothpaste or the glue form that cleans the teeth.
22. the compositions of claim 22, wherein at least a phenolic compound exists with about 0.05% total amount to about 5% weight.
23. the compositions of claim 23, wherein vitamin E and Vitamin E acetate exist with about 0.05% total amount to about 5% weight.
24. the compositions of claim 15, wherein vitamin E is the form of alpha-tocopherol, and Vitamin E acetate is the form of alpha-tocopherol acetate.
25. the compositions of claim 15, wherein vitamin E and Vitamin E acetate existed to about 1: 10 weight ratio with about 10: 1.
26. the compositions of claim 15, wherein vitamin or vitamin derivative component further comprise at least a vitamin C source.
27. the compositions of claim 15, wherein vitamin or vitamin derivative component further comprise at least a carotenoid.
28. the compositions of claim 15, wherein vitamin or vitamin derivative component further comprise at least a vitamin B source.
29. the compositions of claim 15, wherein vitamin or vitamin derivative component further comprise at least a bioflavonoids.
30. the compositions of claim 15, wherein vitamin or vitamin derivative component further comprise at least a quinoid enzyme co-factor.
31. the compositions of claim 15, wherein vitamin or vitamin derivative component further comprise at least a alpha-lipoic acid source.
32. the compositions of claim 15, wherein vitamin or vitamin derivative component are multivitamin or vitamin derivative complex, and it comprises vitamin E, Vitamin E acetate and be selected from (a) vitamin C source; (b) carotenoid; (C) vitamin B source; (d) bioflavonoids; (e) quinoid enzyme co-factor; (f) alpha-lipoic acid source; (g) at least two kinds multiple vitamin or vitamin derivative in the vitamin D source.
33. oral care composition, the antibiotic halogenated diphenyl ether compound that comprises at least a antimicrobial effective amount, with vitamin or vitamin derivative component, it comprises (a), and one or more are selected from ascorbic acid, acceptable salt in its oral cavity and ester, with the antioxidant vitamin of 2-methyl-6-chromanol chemical compound or vitamin derivative and (b) at least a vitamin B
5The source; Wherein at least a halogenated diphenyl ether compound and vitamin or vitamin derivative component with about 10: 1 to about 1: 100 gross weight than existing.
34. an oral care method comprises compositions is applied to patient's oral surfaces, said composition comprises at least a antibiotic halogenated diphenyl ether compound and antioxidant ingredients; Wherein (a) at least a halogenated diphenyl ether compound exists with antibiotic effective total amount; (b) antioxidant ingredients comprises a kind of extremely multiple vitamin or vitamin derivative, and the amount of total vitamin or vitamin derivative can effectively improve the anti-inflammatory activity of compositions; (c) at least a vitamin or vitamin derivative are acceptable salt of ascorbic acid or its oral cavity or ester in the antioxidant ingredients, or 2-methyl-6-chromanol chemical compound.
35. a method that suppresses patient's oral tissue inflammation, this method comprises the oral surfaces that compositions is applied to close on this tissue, and said composition comprises at least a antibiotic halogenated diphenyl ether compound and antioxidant ingredients; Wherein (a) at least a halogenated diphenyl ether compound exists with antibiotic effective total amount; (b) antioxidant ingredients comprises a kind of extremely multiple vitamin or vitamin derivative, and the amount of total vitamin or vitamin derivative can effectively improve the anti-inflammatory activity of compositions; (c) at least a vitamin or vitamin derivative are acceptable salt of ascorbic acid or its oral cavity or ester in the antioxidant ingredients, or 2-methyl-6-chromanol chemical compound.
36. method that promotes patient's oral health, this method comprises compositions is applied to patient's oral surfaces, said composition comprises the antibiotic phenolic compound of at least a antimicrobial effective amount and comprises vitamin E and the vitamin of Vitamin E acetate or vitamin derivative component; Wherein at least a phenolic compound and vitamin or vitamin derivative component with about 10: 1 to about 1: 100 gross weight than existing.
37. method that promotes patient's oral health, this method comprises compositions is applied to patient's oral surfaces, said composition comprises the antibiotic halogenated diphenyl ether compound of at least a antimicrobial effective amount, with vitamin or vitamin derivative component, it comprises (a), and one or more are selected from ascorbic acid, the antioxidant vitamin of acceptable salt in its oral cavity and ester and 2-methyl-6-chromanol chemical compound or vitamin derivative and (b) at least a vitamin B
5The source; Wherein at least a halogenated diphenyl ether compound and vitamin or vitamin derivative component with about 10: 1 to about 1: 100 gross weight than existing.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US63248004P | 2004-12-02 | 2004-12-02 | |
| US60/632,480 | 2004-12-02 | ||
| US11/238,522 | 2005-09-29 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2013103511767A Division CN103462817A (en) | 2004-12-02 | 2005-11-10 | Oral care composition comprising a phenolic compound and antioxidant vitamins and vitamin derivatives |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101111288A true CN101111288A (en) | 2008-01-23 |
Family
ID=39042999
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA2005800476854A Pending CN101111288A (en) | 2004-12-02 | 2005-11-10 | Oral care composition comprising a phenolic compound and antioxidant vitamins and vitamin derivatives |
Country Status (2)
| Country | Link |
|---|---|
| CN (1) | CN101111288A (en) |
| ZA (1) | ZA200705001B (en) |
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102365550A (en) * | 2009-04-01 | 2012-02-29 | 高露洁-棕榄公司 | Anti bone-loss and anti attachment-loss effects of an oral composition |
| CN102652712A (en) * | 2011-03-04 | 2012-09-05 | 全球生技股份有限公司 | Antibacterial oral care composition and preparation method thereof |
| CN103520060A (en) * | 2013-10-22 | 2014-01-22 | 易金阳 | Composition for eliminating bad breath, protecting gum, strengthening teeth, stopping bleeding and adjusting cold, hotness, sour and sweetness |
| CN106511169A (en) * | 2016-12-01 | 2017-03-22 | 李妍 | Mouthwash capable of preventing formation of dental plaque |
| CN109593026A (en) * | 2018-12-13 | 2019-04-09 | 东莞理工学院 | A kind of phenol color inhibition composition and its application |
| CN109651026A (en) * | 2018-12-28 | 2019-04-19 | 淮南皖淮机电股份有限公司 | A kind of new use for explosive type stimulation medicament and preparation method thereof |
-
2005
- 2005-11-10 CN CNA2005800476854A patent/CN101111288A/en active Pending
-
2007
- 2007-06-01 ZA ZA200705001A patent/ZA200705001B/en unknown
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102365550A (en) * | 2009-04-01 | 2012-02-29 | 高露洁-棕榄公司 | Anti bone-loss and anti attachment-loss effects of an oral composition |
| CN102652712A (en) * | 2011-03-04 | 2012-09-05 | 全球生技股份有限公司 | Antibacterial oral care composition and preparation method thereof |
| CN103520060A (en) * | 2013-10-22 | 2014-01-22 | 易金阳 | Composition for eliminating bad breath, protecting gum, strengthening teeth, stopping bleeding and adjusting cold, hotness, sour and sweetness |
| CN106511169A (en) * | 2016-12-01 | 2017-03-22 | 李妍 | Mouthwash capable of preventing formation of dental plaque |
| CN109593026A (en) * | 2018-12-13 | 2019-04-09 | 东莞理工学院 | A kind of phenol color inhibition composition and its application |
| CN109651026A (en) * | 2018-12-28 | 2019-04-19 | 淮南皖淮机电股份有限公司 | A kind of new use for explosive type stimulation medicament and preparation method thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| ZA200705001B (en) | 2008-10-29 |
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