CN103037940B - New application - Google Patents

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Publication number
CN103037940B
CN103037940B CN201180015772.7A CN201180015772A CN103037940B CN 103037940 B CN103037940 B CN 103037940B CN 201180015772 A CN201180015772 A CN 201180015772A CN 103037940 B CN103037940 B CN 103037940B
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CN
China
Prior art keywords
zinc
purposes
sddbs
mottle
compositions
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
CN201180015772.7A
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Chinese (zh)
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CN103037940A (en
Inventor
G·C·艾特肯
D·R·丘奇利
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Glaxo Group Ltd
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Glaxo Group Ltd
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Publication date
Priority claimed from GBGB1004981.5A external-priority patent/GB201004981D0/en
Application filed by Glaxo Group Ltd filed Critical Glaxo Group Ltd
Publication of CN103037940A publication Critical patent/CN103037940A/en
Application granted granted Critical
Publication of CN103037940B publication Critical patent/CN103037940B/en
Expired - Fee Related legal-status Critical Current
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Abstract

The present invention relates to the purposes that dodecylbenzene sodium sulfonate (SDDBS) is adapted to assist in the mottle of prevention or removing natural teeth and dental case surface deposition, and the oral care composition comprising SDDBS for this purposes.

Description

New application
The present invention relates to dodecylbenzene sodium sulfonate (SDDBS) be used for resisting (i.e. help prevention or remove) natural teeth and tooth The purposes of the mottle of dummy surface deposition, and the oral care composition comprising SDDBS for this purposes.Suitably group Compound includes collutory and dentifrice composition.
Some factors make tooth discoloration, but be sure of three principal elements: i) dental surface forms plaque and tartar substrate, Then (entrap) mottle, ii are retained down) in tooth forming process, taken in some drugs, and iii) formed at enamel Cheng Zhong, due to oral wounds, then blood stains thing penetrates into the mineralizing surface of tooth and makes its variable color.Present invention primarily contemplates tooth discoloration First factor or reason, the i.e. natural sediment mottle on tooth.
Have been developed for OTC (over-the-counter) brightener for tooth, it is desirable to provide recover surface trapped substance and cause the adamantine light of variable color Many cosmetic advantages in pool.Although all of collutory and dentifrice composition all comprise some abluents and polishing agent, some teeth Surface deposits may become difficult to process, and can not be completely removed by these reagent under normal usage.These preparations Be likely to be not use completely remove due to be excessively exposed to coloring agent formed mottle and variable color amount required for reagent use Amount and type are prepared.Such as, smoker generally develop into enamel decolouring because exhalation smoke from cigarette in tar and Particle deposition is on tooth.Further, abundance of food can make enamel play mottle and decolouring, and Folium Camelliae sinensis is the example of a kind of beverage, its Tannic acid in middle tea is deposited on enamel.Some medicinal reagents can cause mottle or variable color via retaining, although this is not The most common reason of this kind of mottle.
The mode that the most commonly used three kinds of enamels brighten.They be all based on use abrasive, use oxidant or Hydrolysate is utilized to decompose coloring thing, such as enzyme based products.
SDDBS is a kind of for many oral cavities and the anion surfactant of personal care product.
The present invention has been based on the discovery that SDDBS has antiplaque activity.In particular, it was found that SDDBS is prevented by it The ability suppression mottle that food mottle absorbs on model surface is formed.In addition, SDDBS is shown to remove in vitro color Speckle.
Therefore, at first aspect, the present invention provides a kind of for resisting (i.e. contribute to prevention or remove) dental surface (ratio Such as natural teeth surface or dental case surface) the oral care composition of mottle, wherein said composition comprises SDDBS.
At second aspect, the present invention provides SDDBS preparing the oral care composition for anti-dental surface mottle In purposes.
At the 3rd aspect, the present invention provides a kind of method for anti-dental surface mottle, and described method includes to tooth Tooth surface uses the oral care composition of the SDDBS comprising effective dose.
Suitably, amount is total composition weight the 0.1% to 10.0% of SDDBS, such as 0.2% to 5.0% with On, or be more suitably 0.25% to 2.0%.
It is from Pilot Chemical Company, 2744 East Kemper for the SDDBS of the present invention Rd.Cincinnati, Ohio 45241 is obtainable with trade name Calsoft F90.
The oral care composition of the present invention can comprise one or more activity being generally used for oral care composition Agent, such as fluoride source, desensitizer, anti-plaque agent;Anticalculus agent, halitosis agent (oral malodour agent), antiinflammatory or The mixture that at least a part of which is two kinds.Such reagent can be included to provide the level of expectation therapeutic effect.
Suitably, the compositions of the present invention comprises zinc ion source further.Zinc ion has antibacterial properties, is adapted to assist in pre- Prevent, suppress and/or treat oral hygiene disease that is bacterial present in oral cavity or that increase the weight of, including periodontal (gingiva) disease Disease, dental caries, halitosis, dental plaque and tartar.
Suitably, zinc ion source, when the zinc part as corresponding salt defines, amount is total composition weight 0.01% to 2.50%, such as 0.04% to 0.70%.
Suitably, zinc ion source is zinc salt, such as zinc chloride, zinc citrate, zinc acetate, zinc sulfate, zinc gluconate, water Poplar acid zinc, zinc lactate, MALEIC ACID, ZINC SALT, malic acid zinc, zinc tartrate, zinc carbonate, zinc phosphate, zinc oxide or zinc sulfate.Additionally Zinc salt is described in United States Patent (USP) 4,022,880 (Vinson et al.).
A kind of preferably zinc salt is zinc chloride.
Suitably, the compositions of the present invention comprises 4-isopropyl-3-methylphenol (IPMP) further.IPMP has antibacterial Anti-inflammatory activity, is adapted to assist in prevention, suppresses and/or treats oral hygiene disease that is bacterial present in oral cavity or that increase the weight of Sick.
Suitably, amount is total composition weight the 0.005% to 1.00% of IPMP, such as 0.01% to 0.20% Or 0.05% to 0.10%.
The oral care composition of the combination comprising IPMP, zinc salt and SDDBS demonstrates the antibacterial activity of enhancing, Yi Jiyou Anti-inflammatory activity and resisted mottle benefit.
The oral care composition of the present invention is normally configured to toothpaste, spray, collutory, rinse liquid (mouthrinse), gel, lozenge, chewing gum, tablet, pastille, instant powder (instant powders), refreshing tablets (oral strips), buccal patch, wound dressing and dental cement.
In one embodiment, the compositions of the present invention is dentifrice composition, and more suitably, it can connect for comprising oral cavity The carrier being subject to or the mouthrinse composition of excipient.
The oral care composition of the present invention should comprise other reagent preparation, lives in such as abrasive, thickening agent, surface Property agent, wetting agent, flavoring agent, sweeting agent, opacifier or coloring agent, preservative and water, selected from the mouth for such purpose In the hygiene composition of chamber normally used those.
Suitably oral care active agents and oral cavity acceptable carrier or excipient (the most above-mentioned reagent preparation) is described in Such as in US 2007/0053849 (Procter & Gamble).
Compositions according to the present invention can be prepared by mixing the composition of appropriate relative amounts with order the most easily, If it is necessary, regulation pH is to obtain final desired value.
When the form that compositions is toothpaste, it is be applicable to being contained in such as laminated tube commonly used in the art or pump and therefrom Distribution.
Now, by following embodiment and data, the present invention is described.
Embodiment
1. hydroxyapatite mottle prophylaxis model (HASP)
Method
With the most non-be excited people's saliva (whole unstimulated human saliva) (100 μ l/ hole) 37 DEG C/ The microtitration plate of 96 hole hydroxyapatite coatings is processed under 100rpm.After 1 hour, by any to remove for the washing of described plate Unconjugated component, by every kind of 200 μ l test activating agent and positive and negative control (respectively 5% Sodium triphosphate (STP) and Water) transfer to the plate of each row, and plate is put back in incubator.After 10 min, plate is cleaned again, and by applying 200 μ The newly picked and processed tea leaves solution (deionized water of 1 tea bag (PG tips)/50ml) of l makes plate play mottle.After again cultivating 10 minutes, move Except tea, and wash plate.Finally, by using the 2.5M citric acid/hole of 200 μ l to make the mottle desorption of combination.Minimum 12 little Time after, the tea/citric acid solution of 180 μ l is transferred to clean, normal (not having HA to be coated with) 96 hole microtitration plate, and Measure under 405nm and absorb.
2. the dark brown speckle of hydroxyapatite removes model (HATSR)
Method
96 hole hydroxy-apatites are processed with the tea/hole (deionized water of 1 tea bag (PG Tips)/50ml) of 100 μ l aliquots The microtitration plate of stone coating, and under 37 DEG C/100rpm, cultivate described plate.After 10 min, plate is washed with deionized water Wash, and be dried overnight at 37 DEG C.Test activating agent (200 μ l/ hole) is joined the plate of tea coating of each column with positive and cloudy Property comparison (respectively 5% Sodium triphosphate (STP) and water), and plate is put back to incubator.After 10 min, plate is washed again Wash, by using the 2.5M citric acid/hole of 200 μ l to make the mottle desorption of combination.After minimum 12 hours, by 180 μ l's Tea/citric acid solution transfers to clean, normal (not having HA to be coated with) 96 hole microtitration plate, and measures absorption under 405nm.
Result
3.1. solution
All solution are all in 7 times tests of pH.
Fig. 1. in HASP model (n=8), concentration range 0.1%10% time, the mottle preventive dose of the SDDBS of test Reaction.
Conclusion
The result display SDDBS prevention food mottle of Fig. 1 absorbs on HASP model oral surfaces.All of SDDBS is dense Degree is the most statistically better than water negative control, except 0.1% (it is only that orientation is better than), but neither one and positive control STP (a kind of known stainblocker used in many whitening toothpastes) is the most effective.
Fig. 2. in HASP model (n=8), under concentration range 0.1%-10%, the mottle of the SDDBS of test removes dosage Reaction.
Conclusion
The result of the HATSR model test in Fig. 2 shows that SDDBS removes mottle with dosage-dependent manner.All of SDDBS concentration is the most statistically better than water negative control, except concentration 0.125%, but neither one and positive control STP ( A kind of known stainblocker used in many whitening toothpastes) the most effective.
Fig. 3. in HASP model (n=8), SDDBS/SLS's combination (total surfactant level: 1%) of test Mottle prevention data.
Conclusion
The result of the HASP model test of Fig. 3 shows that, under equivalent concentration, SDDBS is statistically better than lauryl sulphate acid Sodium (SLS).
Keeping the constant concentration of surfactant 1%, it is effective that the combination of SDDBS and SLS is shown without 1%SDDBS, But still better than single SLS.The process of all SDDBS of comprising is better than water, but not with positive control STP (in many A kind of known stainblocker used in whitening toothpaste) the most effective.
Embodiment preparation
In HASP (Fig. 4) and HATSR (Fig. 5) model, also evaluate for a large amount of commercially available obtainable products and comprise SDDBS Mouthwash formulations.
Fig. 4. in HASP model (n=8), the test preparation comprising 0.5%SDDBS of test obtains relative to commercially available The mottle prevention data of product.
Fig. 5. in HASP model (n=8), the test preparation comprising 0.5%SDDBS of test obtains relative to commercially available The mottle of product removes data.
Conclusion
Prevent deposition and the removing aspect of food mottle in vitro, comprise all 3 kinds of test collutorys of 0.5%SDDBS (MW1, MW2 and MW3) all demonstrates and is statistically better than commercially available obtainable product.With commercially available prod (except Listerine Outside (Original and Total Care)) different, these preparations do not comprise can be in conjunction with mottle chromophore and enhancing mottle Cationic antimicrobial agent, such as cetylpyridinium chloride (CPC) and chlorhexidine.
MW embodiment preparation 1-3 (as shown in above-mentioned Figure 4 and 5)

Claims (8)

1. dodecylbenzene sodium sulfonate (SDDBS) protects for the oral cavity of anti-dental surface mottle in preparation as sole active agent Purposes in reason compositions.
Purposes the most according to claim 1, wherein said compositions comprises zinc ion source further.
Purposes the most according to claim 2, wherein said zinc ion source selected from zinc chloride, zinc citrate, zinc acetate, zinc sulfate, Zinc gluconate, zinc salicylate, zinc lactate, malic acid zinc, MALEIC ACID, ZINC SALT, zinc tartrate, zinc carbonate, zinc phosphate, zinc oxide or Zinc sulfate.
Purposes the most according to claim 3, wherein said zinc ion source is zinc chloride.
5., according to the purposes any one of Claims 1-4, wherein said compositions comprises 4-isopropyl-3-methyl further Phenol (IPMP).
6., according to the purposes any one of Claims 1-4, wherein said compositions is collutory or toothpaste.
7., according to the purposes any one of Claims 1-4, wherein said compositions is collutory.
8., for a method for anti-dental surface mottle, described method includes using to dental surface comprising effective dose The oral care composition of SDDBS, wherein SDDBS is used as the sole active agent for anti-dental surface mottle, Qi Zhongsuo Method of stating is for non-treatment purpose.
CN201180015772.7A 2010-03-24 2011-03-22 New application Expired - Fee Related CN103037940B (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB1004981.5A GB201004981D0 (en) 2010-03-24 2010-03-24 Novel use
GB1004981.5 2010-03-24
PCT/EP2011/054291 WO2011117216A2 (en) 2010-03-24 2011-03-22 Novel use

Publications (2)

Publication Number Publication Date
CN103037940A CN103037940A (en) 2013-04-10
CN103037940B true CN103037940B (en) 2016-11-30

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Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0870492A1 (en) * 1997-04-11 1998-10-14 Carter-Wallace, Inc. Oral composition comprising aluminium hydroxide, silica and an anionic surfactant

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0870492A1 (en) * 1997-04-11 1998-10-14 Carter-Wallace, Inc. Oral composition comprising aluminium hydroxide, silica and an anionic surfactant

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Termination date: 20170322