Drug – bio-affecting and body treating compositions – Dentifrices
Reexamination Certificate
2000-10-11
2002-09-17
Rose, Shep K. (Department: 1614)
Drug, bio-affecting and body treating compositions
Dentifrices
Reexamination Certificate
active
06451291
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Field of the Invention
The present invention relates to an oral composition containing an antibacterial compound for the inhibition of bacterial plaque accumulation on dental tissue and more particularly to an oral composition containing an antibacterial compound and a mixed anionic/zwitterionic surfactant system which promotes significantly higher uptake of the antibacterial compound on dental tissue.
2. The Prior Art
Dental plaque is a soft deposit which forms on teeth and is comprised of an accumulation of bacteria and bacterial by-products. Plaque adheres tenaciously at the points of irregularity or discontinuity, e.g., on rough calculus surfaces, at the gum line and the like. Besides being unsightly, plaque is implicated in the occurrence of gingivitis and other forms of periodontal disease.
A wide variety of antibacterial agents have been suggested in the art to retard plaque formation and the oral infections and dental disease associated with plaque formation. For example, halogenated hydroxydiphenyl ether compounds such as triclosan are well known to the art for their antibacterial activity and have been used in oral compositions to counter plaque formation by bacterial accumulation in the oral cavity. The effectiveness of the antibacterial agent is dependent upon its delivery to and uptake by teeth and soft tissue areas of the gums.
There is therefore a need in the art to provide means whereby the delivery to and uptake by dental tissue of antibacterial compounds contained in oral compositions can be promoted so as to enhance the therapeutic efficacy of the antibacterial agent.
SUMMARY OF THE INVENTION
In accordance with this invention there is provided an oral composition comprising in an orally acceptable vehicle, an effective antiplaque amount of an halogenated diphenyl ether or phenolic antibacterial compound, and an amount of a mixed anionic/zwitterionic surfactant system present at specific weight concentrations in the vehicle effective to increase the delivery and uptake of the antibacterial compound to oral surfaces so as to enhance the therapeutic efficacy of the administered compound.
As will hereinafter be demonstrated, the presence of the mixed surfactant system results in uptake and bioavailability of the antibacterial agent which is unexpectedly higher than for comparable compositions in which the anionic/zwitterionic surfactant system ingredients are outside the scope of the present invention.
DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS
The term “oral composition” is used herein to designate products which, in the ordinary course of usage, are retained in the oral cavity for a time sufficient to contact substantially all of the dental surfaces but are not intentionally ingested. Such products include, for example, dentifrices such as toothpaste and gels, mouthwashes, chewing gums and lozenges.
It is essential and critical that the antibacterial containing oral composition of the present invention contain a mixed anionic/zwitterionic surfactant system present at a concentration of about 1.5 to about 4% by weight and preferably about 2 to about 3% by weight wherein the anionic surfactant is the major constituent, the weight concentration being in the range of about 0.5 to about 3.0% by weight and preferably about 1.5 to about 2.50% by weight and the zwitterionic surfactant being present in the oral composition at a concentration of about 0.30 to about 0.1% by weight and preferably about 0.35 to about 0.50% by weight.
Halogenated diphenyl ether antibacterial compounds useful for the preparation of the oral care compositions of the present invention particularly desirable from considerations of antiplaque effectiveness and safety include 2,4,4′-trichloro-2′-hydroxy-diphenyl ether (triclosan) and 2,2′-dihydroxy-5,5′-dibromo-diphenyl ether.
Phenolic compounds useful in the practice of the present invention include phenol and its homologs, mono and polyalkyl and aromatic halophenols, resorcinol and its derivatives and bisphenolic compounds, such phenolic compounds being more fully disclosed in U.S. Pat. No. 5,368,844, the disclosure of which is incorporated herein by reference. Preferred phenolic compounds are n-hexyl resorcinol and 2,2′-methylene bis (4-chloro-6-bromophenol).
The halogenated diphenyl ether or phenolic antibacterial compound is present in the oral composition of the present invention in an effective antiplaque amount, typically about 0.05% to about 2.0% by weight, and preferably about 0.1% to about 1% by weight of the oral composition.
Anionic surfactants useful in the practice of the present invention include the higher fatty acid monoglyceride monosulfates, such as the sodium salts of the monosulfated monoglycerides of hydrogenated coconut oil fatty acid; higher alkyl sulfates, such as sodium lauryl sulfate; higher alkyl aryl sulfonates, such as sodium linear dodecyl benzene sulfonate; higher olefin sulfonates, such as sodium higher olefin sulfonate in which the olefin group is 12 to 21 carbon atoms; higher alkyl alkali sulfoacetates such as sodium lauryl sulfoacetate; higher fatty acid esters of 1,2-dihydroxypropane sulfonates; the substantially saturated higher aliphatic acyl amides of lower aliphatic aminocarboxylic acid alkali metal salts, such as those having 12 to 16 carbon atoms in the fatty acyl radicals; higher alkyl poly-lower alkoxy (of 10 to 100 alkoxies) sodium sulfates; higher fatty acid sodium and potassium soaps of coconut oil and tallow, and the like. The anionic surfactant, sodium lauryl sulfate, is preferred in the practice of the present invention.
Zwitterionic surfactants useful in the practice of the present invention include betaine compounds such as alkyl amido betaines, alkyl amido propyl betaines, alkyl dimethyl betaines, sulpho betaines and alkyl betaines. The alkyl amido propyl betaine, cocoamido propyl betaine is a preferred zwitterionic surfactant for use in the practice of the present invention.
In the preparation of an oral composition in accordance with the practice of the present invention, an orally acceptable vehicle including a water-phase with humectant is present. The humectant is preferably glycerine, sorbitol, and/or propylene glycol. Water is present typically in amount of at least about 10% by weight, generally about 30 to 60% by weight and the humectant concentration typically totals about 40-60% by weight of the oral composition.
Dentifrice compositions such as toothpastes and gels also typically contain polishing materials including crystalline silica, having a particle size of up to about 20 microns, such as commercially available Zeodent 115, silica gel or colloidal silica, complex amorphous alkali metal aluminosilicates, hydrated alumina, sodium metaphosphate as well as sodium bicarbonate, calcium carbonate, calcium pyrophosphate, dicalcium phosphate and dicalcium phosphate dihydrate. Typically, the polishing material is included in semi-solid or pasty dentifrice compositions of the present invention in an amount of from about 15 to about 60% by weight and preferably from about 20 to about 55%.
Pyrophosphate salts having antitartar efficacy such as a dialkali or tetraalkali metal phosphate salts such as Na
4
P
2
O
7
, K
4
P
2
O
7
, Na
2
K
2
P
2
O
7
, Na
2
H
2
P
2
O
7
and K
2
H
2
P
2
O
7
, long chain polyphosphates such as sodium hexametaphosphate and cyclic phosphate such as sodium trimetaphosphate may be incorporated in oral compositions of the present invention preferably at concentration of about 0.5 to about 8.0% by weight and preferably about 0.5 to about 3.0% by weight. In liquid oral preparations, the pyrophosphate salts are incorporated at a concentration of about 0.1 to about 2% by weight.
Dentifrices prepared in accordance with the present invention typically contain a natural or synthetic thickener in proportions of about 0.1 to about 5% by weight, preferably about 0.5 to about 2% by weight. Suitable thickeners include Irish moss, i-carrageenan, gum tragacanth, starch, polyvinylpyrrolidone, hydroxyethypropyl cellul
Liu Xiaoyan
Subramanyam Ravi
Williams Malcolm
Colgate - Palmolive Company
Rose Shep K.
Shapiro Paul
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