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Oral care product and methods of use and manufacture thereof

Inactive Publication Date: 2009-08-13
COLGATE PALMOLIVE CO
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0006]It is now surprisingly discovered that a basic amino acid such as arginine in combination with an anionic surfactant can reduce bacterial attachment and biofilm formation and additionally dramatically enhance solubility, delivery, retention and antibacterial effectiveness of an antibacterial agent such as triclosan.
[0007]The invention thus encompasses oral care compositions and methods of using the same that are effective in inhibiting or reducing the accumulation of plaque, reducing levels of acid producing (cariogenic) bacteria, remineralizing teeth, and inhibiting or reducing gingivitis. The invention also encompasses compositions and methods to clean the oral cavity and provide improved methods of promoting oral health and / or systemic health, including cardiovascular health, e.g., by reducing potential for systemic infection via the oral tissues.

Problems solved by technology

Combining these basic amino acids with minerals having oral care benefits, e.g., fluoride and calcium, to form an oral care product having acceptable long term stability, however, has proven challenging.
Moreover, the higher pH has the potential to cause irritation.
At neutral pH or acidic pH, however, a system utilizing arginine bicarbonate (which the art teaches is preferred) may release carbon dioxide, leading to bloating and bursting of the containers.
Moreover, it might be expected that lowering the pH to neutral or acidic conditions would reduce the efficacy of the formulation because the arginine may form an insoluble arginine-calcium complex that has a poorer affinity for the tooth surface, and moreover that lowering the pH would reduce any effect the formulation might have on buffering cariogenic lactic acid in the mouth.
Partly because of these unaddressed formulation hurdles and partly because arginine has generally been viewed in the art as a potential alternative to fluoride rather than a co-active, there has been little motivation to make oral care products comprising both arginine and fluoride.
Additional hurdles are potentially posed by addition of an antimicrobial agent.
These agents however are challenging to deliver in effective amounts to the teeth and gums, and their solubility, delivery and retention on the teeth is formulation dependent.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

Availability and Delivery of Antibacterial in Arginine Formulations

[0095]Formulations are prepared using commercial toothpaste comprising, i.a., 0.3% by weight of triclosan, 0.243% by weight of sodium fluoride, sodium lauryl sulfate, and a copolymer of methyl vinyl ether and maleic anhydride (PVM / MA), to which is added 0, 1%, 3%, and 5% L-arginine hydrochloride (pH 7.0).

[0096]Incorporation of L-arginine in the commercial formulation enhances the amount of soluble triclosan available from the formulation, from about 70% (0% arginine) to about 80% (1% arginine), 85% (3% arginine), and 95% (5% arginine).

[0097]The formulations are tested in vitro in an artificial mouth model designed to measure bacterial attachment to toothpaste-treated hydroxyapatite (HAP) disks over a 24 hour period, generally as described by Gaffar, A. et al. American Journal of Dentistry, vol. 3, September 1990, with the modification that the saliva-coated hydroxyapatite disks are treated with the dentifrice slurry ...

example 2

Delivery of Antibacterial in Silica Based Formulations Comprising Arginine

[0099]Toothpaste formulations comprising 5% arginine in a silica base are prepared as follows:

FormulaFormulaFormulaFormulaFormula IFormula IIIIIIVFormula VVIVIIIngredientWt %Wt %Wt %Wt %Wt %Wt %Wt %L-Arginine5.005.005.005.005.005.005.00Hydrochloric Acid——2.002.002.00——Silica21.5021.5021.5023.5023.5023.5023.50Sodium Fluoride0.2430.2430.243———.0243Glycerin20.0020.0020.0020.0020.0020.0020.00Sorbitol20.8520.8520.8520.8520.8520.8520.85Propylene Glycol0.500.500.50———2.00Tetrasodium———2.002.00—2.00PyrophosphateZinc Lactate,———1.4———DihydrateSodium————3.00——TripolyphosphateSodium Lauryl1.501.501.501.501.50—1.50SulfatePoloxomer 407—————1.01—(Pluronic F-127)Cocamidopropyl———1.011.01—1.01Betaine (30%solutionHydroxy Ethyl———1.501.501.50—CelluloseSodium1.101.101.10———1.10carboxymethylcelluloseCarrageenan0.40.40.4———0.40PVM / MA2.002.002.00————copolymerSodium———0.760.760.76—MonollurophosphateFlavor1.001.001.001.001.001.001.00...

example 3

Delivery of Antibacterial in Formulations Comprising Precipitated Calcium Carbonate

[0102]Formulations comprising 2% arginine bicarbonate are prepared as follows:

RAW MATERIALWEIGHT %Formula ADeionized Water32.42070% Sorbitol23.000Carboxymethyl cellulose0.940Xanthan gum0.210Sodium saccharin0.450Sodium silicate0.800Sodium bicarbonate0.500Arginine bicarbonate2.000Precipitated calcium carbonate36.000Sodium monofluorophosphate0.760Flavor1.000Triclosan0.300Sodium lauryl sulfate1.620TOTAL100.000Formula BDeionized Water23.20070% Sorbitol23.000Xylitol2.500Carboxymethyl cellulose0.940Xanthan gum0.210Sodium saccharin0.450Sodium silicate0.800Sodium bicarbonate0.500Arginine bicarbonate2.000Precipitated calcium carbonate42.000Sodium monofluorophosphate1.100Flavor1.000Triclosan0.300Sodium lauryl sulfate2.000TOTAL100.000Formula CDeionized Water34.42070% Sorbitol23.000Carboxymethyl cellulose0.940Xanthan gum0.210Sodium saccharin0.450Sodium silicate0.800Sodium bicarbonate0.500Arginine bicarbonate0.000P...

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Abstract

This invention relates to oral care compositions comprising an effective amount of a basic amino acid in free or salt form, together with an anionic surfactant, and to methods of using and of making such compositions.

Description

[0001]This application claims the benefit of U.S. Ser. No. 61 / 027,432 filed Feb. 8, 2008, U.S. Ser. No. 61 / 027,431 filed Feb. 8, 2008 and U.S. Ser. No. 61 / 027,420 filed Feb. 8, 2008, the contents of which are incorporated herein by reference.FIELD OF THE INVENTION[0002]This invention relates to oral care compositions comprising a basic amino acid in free or salt form, an anionic surfactant, and optional additional agents, and to methods of using and of making these compositions.BACKGROUND OF THE INVENTION[0003]Arginine and other basic amino acids have been proposed for use in oral care and are believed to have benefits in combating cavity formation and tooth sensitivity. Combining these basic amino acids with minerals having oral care benefits, e.g., fluoride and calcium, to form an oral care product having acceptable long term stability, however, has proven challenging. In particular, the basic amino acid may raise the pH and facilitate dissociation of calcium ions that can react w...

Claims

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Application Information

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IPC IPC(8): A61K8/30A61K8/19A61K8/66A61Q11/00
CPCA61K8/19A61K8/21A61Q11/00A61K8/44A61K31/198A61K8/24A61K8/27A61K8/347A61K2800/28A61K2800/5424A61K2800/596A61P1/02A61P31/02A61P31/04A61P37/04A61P9/00
Inventor PRENCIPE, MICHAELCUMMINS, DIANESUBRAMANAYAM, RAVISULLIVAN, RICHARD J.SANTARPIA, III, RALPH PETERMELLO, SARITA V.ZAIDEL, LYNETTECHOPRA, SUMANWANG, QINTAMBS, GARY EDWARDBARNES, VIRGINIA MONSULWU, DONGHUIMORGAN, ANDRE M.KOHLI, RAJNISHROBINSON, RICHARD SCOTTLEITE, SERGIOSIMON, ERIC A.
Owner COLGATE PALMOLIVE CO
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