CN101027033A - Oral cavity composition - Google Patents
Oral cavity composition Download PDFInfo
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- CN101027033A CN101027033A CN 200580026168 CN200580026168A CN101027033A CN 101027033 A CN101027033 A CN 101027033A CN 200580026168 CN200580026168 CN 200580026168 CN 200580026168 A CN200580026168 A CN 200580026168A CN 101027033 A CN101027033 A CN 101027033A
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- dentifrice composition
- composition according
- citric acid
- zinc
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Abstract
An opaque toothpaste composition and method for making such, the toothpaste comprising water, a zinc salt, a chelating agent for the zinc salt, the chelating agent having a log Ks1 as herein defined of from 3.0 to 7.0, and an abrasive present at from 10% to 70% by weight of the composition, said abrasive comprising calcium carbonate.
Description
The present invention relates to a kind of opaque dentifrice composition, comprise the bioactive zinc salt that is contained in the chalk formulation.The invention still further relates to the method for preparing said composition.
EP-A1-0740 932 (Unilever) discloses the limpid gel-type dentifrice of a kind of vision, comprise a kind of zinc salt more soluble in water than zinc citrate, a kind of can with the bonded aminoacid of zinc and a kind of low-refraction type abrasive silica.
US 5 470 561 (Klugkist) discloses a kind of plaque mouthwash, comprises a kind of zinc salt and triclosan.Compositions also comprises glycine and pH between 4 to 8, and between preferred 5 to 7, more preferably pH is 6.
GBA-2 052 978 (Unilever) discloses a kind of toothpaste, comprise and contain zinc salt and glycine, and pH is 4.5 to 8.0.
US 5 632 972 (Williams) discloses a kind of method, and its second kind of composition by discharging the zinciferous first kind of composition of bag and comprising bicarbonate reduces to minimum with the infringement of gums and periodontal tissue.
US 4 425 325 (Sapone etc.) discloses a kind of oral cavity composition, comprises biological activity zinc ion and glycine, and has the pH about 4.5 to 9.4 that has regulated.
GB 1 319 247 (Beecham INC) discloses the anticalculous tooth composite of a kind of nonfluid, comprises zinc, cupric or the zirconium composite of a kind of dental vehicle and a kind of fluorizated beta-diketon.
US 4 325 939 (Shah) discloses a kind of zinc citric acid alkali metal or zinc citric acid ammonium salt, is used for preparing dental composition, especially mouthwash agent composition.
US 5 188 820 (Cummins etc.) discloses for example dentifrice of a kind of oral cavity composition, comprises for example stannous fluoride or ditin diphosphate and the zinc salt mixture of zinc citrate for example of tin salt.
Yet, never attempt to make a kind of dentifrice composition that contains a kind of zinc salt and calcium carbonate as grinding agent in the prior art.This is to be attributed to occur in the untoward reaction that forms carbon dioxide between calcium carbonate and the zinc ion.When longer-term storage a period of time, between for example making and using, the gas that produces in this reaction expands the closed container of storage sets compound, and will finally cause explosion.In addition, the generation of carbon dioxide has reduced the bioavailability as the zinc ion of antimicrobial, thereby reduces the effectiveness of zinc salt.
Of the present invention aspect first in, a kind of opaque dentifrice composition is provided, described compositions comprises the chelating citric acid of zinc salt, water, zinc salt, the chelating citric acid has 3.0 to 7.0 logKs1 of this paper definition, account for 10% to 70% grinding agent of dentifrice composition weight, described grinding agent comprises calcium carbonate.
The invention provides the suitableeest a kind of balance, promptly produce competent biological activity zinc ion and can and antibacterial interact and do not generate the suitableeest balance between the carbon dioxide of harmful amount.Therefore the danger that this has just reduced any bubble in the storage composition container, allow zinc salt stably to be present in the calcium carbonate composition, for example at memory period over a period to come.
Zinc salt accounts for 0.01% to 5% of dentifrice composition weight, preferably accounts for 0.5% to 3.0% of composition weight.Zinc salt for example zinc citrate is sl. sol., contains the log K of the cheland of zinc ion
s1 is worth, and is equal to or greater than the log K of the zinc ion of acidic anionic and microsolubility zinc salt
s1.Yet, preferred water-soluble zinc salt.The zinc salt that is fit to comprises zinc chloride, zinc sulfate and zinc fluoride.In such preparation, preferred zinc salt is a zinc sulfate, and the suitableeest above-mentioned balance is provided.
Preferably, the log K of the chelating citric acid of zinc salt
s1 is 4.0 to 6.0.In zinc of the present invention, log K
sThe 1st, the logarithm of primary stability constant, it is meant specific ligand and the ionic binding affinity of special metal (being zinc in the present invention).For example, when the chelating citric acid was glycine, primary stability constant was the binding affinity of a glycine ligand and free zinc ion, and in order to give a definition: K
s1=[ML]/[M] .[L], wherein [ML] is the concentration of metal-ligand complex, [M] is the concentration of free metal ion, and [L] is the concentration of free ligand.[L] is the function of pH value of solution, because the initial deprotonation effect of essential part as datum mark (reference point), is therefore write down described log K in pH7.4
s1 value.
The chelating citric acid accounts for 0.001 to 6% of composition weight, preferably accounts for 0.5 to 4.0% of composition weight.Preferred chelating citric acid comprises the alkali metal salt of citric acid, alanine, glycine and serine.Glycine most preferably, it can prevent to provide the suitableeest balance between zinc salt hydrolysis (causing carbon dioxide to generate) and its solubility of maintenance and the biological utilisation in the Chalk system.Abrasive system accounts for 10 to 70% of dentifrice composition weight, and is preferred 20 to 60%, most preferably accounts for 35 to 45% of dentifrice composition weight.
The abrasive system of Shi Yonging is based on calcium carbonate in the present invention.This does not repel for example use of silicon dioxide, tungsten carbide and carborundum of non-calcium carbonate abrasives.
In a preferred embodiment, abrasive system comprises the calcium carbonate of at least 50% weight, more preferably the calcium carbonate of at least 75% weight, the most preferably calcium carbonate of at least 95% weight.Although can be the mixture of calcium carbonate and other grinding agent, in the most preferred embodiment of the present invention, abrasive system comprises the calcium carbonate of 100% weight.
Because itself and the good stability of zinc salt interaction, preferably calcium carbonate comprises fine ground natural chalk.Term fine ground natural chalk (FGNC) is the term that this area crowd knows, and discloses suitable embodiment in US 2003/0072721Al (Riley), quotes the content of its definition about FGNC, type and grade herein, as a reference.Yet FGNC is interpreted as the Chalk by grinding stone lime stone or marble deposits acquisition.Preferably, to comprise heavy basic median particle diameter be that 1-15um and BET surface area are 0.5-3m to FGNC
2The particulate matter of/g.
Thing combined according to the invention also preferably comprises fluoride sources, for example the alkali metal salt of MFP, preferably sodium monofluorophosphate.This fluoride sources exists so that 100-2000ppm, the preferred ionic amount of 900-1500ppm free fluorine can be provided.
Dentifrice composition is included in the common more composition in this area according to the present invention, for example:
Antimicrobial, for example chlorhexidine, Sanguinarine extract, metronidazole, quaternary ammonium compound cetylpyridinium chloride for example; Biguanides is chlorhexidine gluconate, hexetidine, octenidine, alexidine for example; With the halogenated bisphenol chemical compound, 2,2 ' methylene two-(4-chloro-6-bromophenol) for example;
Antiinflammatory, for example ibuprofen, Flurbiprofen, aspirin, indomethacin etc.;
Dental caries agent, for example sodium fluoride and stannous fluoride, amine fluoride, sodium monofluorophosphate, sodium trimetaphosphate and casein;
Dental plaque buffer agent, for example urea, calcium lactate, calcium glycerophosphate and polyacrylic acid strontium;
Vitamin is vitamin A, C and E for example;
Plant extract;
Desensitizer, for example potassium citrate, potassium chloride, Soluble tartar., potassium bicarbonate, potassium oxalate, potassium nitrate and strontium salt;
Anticalculus agent, for example alkali metal pyrophosphate, the polymer that contains hypophosphites, organic phosphonate and phosphoric acid citrate etc.;
Biomolecule, for example bacteriocin, antibody, enzyme etc.;
Flavoring agent, for example Herba Menthae and Oleum menthae;
Protein material, for example collagen protein;
Antiseptic;
Opacifier;
Coloring agent;
The pH regulator agent;
Sweeting agent;
Pharmaceutically acceptable carrier, for example starch, sucrose, water or water/ethanol system etc.;
Surfactant, for example anion, nonionic, cation and amphion or amphoteric surfactant;
The microgranule abrasive material, for example silicon dioxide, aluminium oxide, calcium carbonate, calcium hydrogen phosphate, calcium pyrophosphate, hydroxyapatite, trimetaphosphate, insoluble hexametaphosphate etc., comprise agglomerant microgranule abrasive material, be generally 3 to 60% weight of dentifrice composition weight.Preferred abrasive material is Chalk and silicon dioxide, more preferably fine ground natural chalk.
Wetting agent, for example glycerol, sorbitol, propylene glycol, xylitol, lactose etc.;
Binding agent and thickening agent, for example sodium carboxymethyl cellulose, hydroxyethyl-cellulose (Natrosol
), xanthan gum, Radix Acaciae senegalis etc., and synthetic polymer polyacrylate and carboxy vinyl polymer Carbopol for example for example
Also can comprise the polymer that energy enhanced activity composition discharges, for example antimicrobial;
The pH of buffering dentifrice composition and the buffer agent and the salt of ionic strength; With
Other optional members that can contain are, bleach for example, and peroxide peroxide diphosphonic acid potassium for example for example, effervescent system is sodium bicarbonate/citric acid sodium system for example, toning system etc.
Liposome also can be used to promote the release or the stability of active component.
In another aspect of this invention, a kind of method of making the opaque dentifrice composition of first aspect is provided, may further comprise the steps: form chelates of zinc solution,, pH is buffered to the pH that is equal to or higher than calcium carbonate in the aqueous suspension with before the calcium carbonate of suspendible mixes.The material that can in final mixture, add other, for example flavouring agent.
Remove operation and comparative examples, or outside other clearly indicated, all numerals in this description should be understood to the amount with word " pact " modification.
Term " comprises " and means and be not any key element of explanation subsequently of restriction, but comprises the non-appointment key element of more or less critical function.In other words, the step of listing, key element or choosing do not need detailed mutually.When using " comprising " or " containing ", these term meanings were equal to above-mentioned definition " comprising ".
By means of non-limiting example, embodiment of the present invention are further elaborated.
Embodiment 1
Following example formulation is one embodiment of the present invention.Preparation at first mixes Zinc vitriol with glycine (with other submember) by the following method, and regulating pH with sodium hydroxide is 8.5 to 9.5.In zinc-chelating mixture, add calcium carbonate, surfactant and excipient then.Add flavoring agent at last.
| Composition | ％(w/w) |
| Fine ground natural chalk (Addon 1015) | 40.00 |
| Sorbitol (70%aq) | 15.00 |
| Thickening property silicon dioxide | 3.00 |
| Sodium carboxymethyl cellulose | 0.90 |
| Flavoring agent | 1.10 |
| Sweeting agent | 0.23 |
| Sodium lauryl sulfate | 2.50 |
| Zinc vitriol | 2.745 |
| Glycine | 3.584 |
| Sodium hydroxide | 1.12 |
| Formalin | 0.10 |
| Sodium monofluorophosphate | 0.76 |
| Water | To 100 |
| 100.00 |
Embodiment 2
As shown in the table, when the ratio that adopts zinc with acetic acid that plays the part effect or glycine is when protecting zinc at 1: 3, the pH of the sedimentary upper water solution of no zinc hydroxide that can reach.
| The mol ratio of zinc and part | Acetic acid | Glycine |
| Zinc-part (log K s1) | 1.03 | 5.16 |
| PH during the zinc hydroxide precipitation | 5.82 | ＞10 |
In other words, be that 1: 3 and part are the situation of acetate at the ratio of zinc and part, when the pH of compositions just reaches 6 when following, will generate zinc hydroxide.Contain the pH of calcium carbonate, generally be low to moderate 8 as the dentifrice composition of grinding agent, most of on 8, even up to 10.
Therefore, in acetic acid and glycine, only glycine can form because only such part just can prevent zinc hydroxide as the part of zinc in the chalk toothpaste, and prevents the calcium reaction in gained carbon dioxide and the Chalk.
Claims (12)
1. opaque dentifrice composition, described compositions comprises the chelating citric acid of water, zinc salt, zinc salt, and the chelating citric acid has 3.0 to 7.0 log K of this paper definition
sL and account for 10% to 70% grinding agent of dentifrice composition weight, described grinding agent comprises calcium carbonate.
2. opaque dentifrice composition according to claim 1, wherein the pH of compositions is 8.0-10.0.
3. require described opaque dentifrice composition according to any aforesaid right, wherein calcium carbonate is a fine ground natural chalk.
4. require described opaque dentifrice composition according to any aforesaid right, wherein compositions comprises fluoride sources.
5. require described opaque dentifrice composition according to any aforesaid right, wherein zinc salt is a water-soluble zinc salt.
6. require described opaque dentifrice composition according to any aforesaid right, wherein zinc salt is a zinc sulfate.
7. require described opaque dentifrice composition according to any aforesaid right, wherein the chelating citric acid is a glycine.
8. require described opaque dentifrice composition according to any aforesaid right, wherein the chelating citric acid is a serine.
9. require described opaque dentifrice composition according to any aforesaid right, wherein the chelating citric acid is an alanine.
10. require described opaque dentifrice composition according to any aforesaid right, wherein the chelating citric acid is an alkali metal citrates.
11. require described opaque dentifrice composition according to any aforesaid right, described compositions comprises and is selected from following material: dental caries agent, anticalculus agent, halitosis agent, brightener for tooth, resist gingivitis agent and composition thereof.
12. a method for preparing opaque dentifrice composition, this dentifrice composition comprise the chelating citric acid of water, zinc salt, zinc salt, the chelating citric acid has 3.0 to 7.0 log K of this paper definition
sL and account for 10% to 70% grinding agent of dentifrice composition weight, this grinding agent comprises calcium carbonate, and described method comprises:
-form chelates of zinc solution, with before calcium carbonate mixes, pH is buffered to the pH that is equal to or higher than calcium carbonate in the aqueous suspension, choose in any step adding other materials arbitrarily wantonly.
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP04254662.2 | 2004-08-02 | ||
| EP04254662 | 2004-08-03 | ||
| EP04254661.4 | 2004-08-03 | ||
| EP04257064.8 | 2004-11-15 | ||
| EP04257063.0 | 2004-11-15 | ||
| EP05250131.9 | 2005-01-13 | ||
| EP05250642.5 | 2005-01-26 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101027033A true CN101027033A (en) | 2007-08-29 |
Family
ID=34930539
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200580026168 Pending CN101027033A (en) | 2004-08-03 | 2005-07-13 | Oral cavity composition |
| CN 200580026177 Pending CN1993100A (en) | 2004-08-03 | 2005-07-13 | Oral composition |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200580026177 Pending CN1993100A (en) | 2004-08-03 | 2005-07-13 | Oral composition |
Country Status (1)
| Country | Link |
|---|---|
| CN (2) | CN101027033A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108883315A (en) * | 2016-03-31 | 2018-11-23 | 荷兰联合利华有限公司 | Dentifrice composition |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2838826C (en) * | 2011-06-17 | 2016-01-05 | Colgate-Palmolive Company | Oral care compositions |
| AU2017351069B2 (en) * | 2016-10-24 | 2019-09-12 | Colgate-Palmolive Company | Oral care compositions and methods of use |
-
2005
- 2005-07-13 CN CN 200580026168 patent/CN101027033A/en active Pending
- 2005-07-13 CN CN 200580026177 patent/CN1993100A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108883315A (en) * | 2016-03-31 | 2018-11-23 | 荷兰联合利华有限公司 | Dentifrice composition |
| CN108883315B (en) * | 2016-03-31 | 2022-05-24 | 联合利华知识产权控股有限公司 | Toothpaste composition |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1993100A (en) | 2007-07-04 |
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|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
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| C12 | Rejection of a patent application after its publication | ||
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Application publication date: 20070829 |