Drug – bio-affecting and body treating compositions – Dentifrices – Plant extract of undetermined constitution
Reexamination Certificate
2000-05-10
2002-12-31
Rose, Shep K. (Department: 1614)
Drug, bio-affecting and body treating compositions
Dentifrices
Plant extract of undetermined constitution
C424S049000, C424S195110
Reexamination Certificate
active
06500409
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Field of the Invention
This invention relates to a antiplaque combination of a noncationic halogenated hydroxydiphenyl ether antibacterial agent and an extract of Magnolia Officinalis and more particularly to an oral composition containing such combination which exhibits increased antigingivitis effect due to synergistic antibacterial effect against plaque bacteria.
2. The Prior Art
It is difficult to predict the antiplaque efficacy of antibacterial compounds when incorporated in a delivery vehicle and particularly in oral compositions. For example, dental plaque is a soft deposit which forms on teeth as opposed to calculus which is a hard calcified deposit on teeth. Unlike calculus, plaque may form on any part of the tooth surface, particularly at the gingival margin and is implicated in the occurrence of gingivitis. Cationic antibacterial compounds such as chlorhexidine, benzothonium chloride and cetyl pyridinium chloride have been used by the art as antibacterial antiplaque agents in oral compositions. However, such agents are generally not effective when there is also present in the oral composition an anionic surfactant required for the effective performance of oral compositions such as toothpaste and mouthrinses.
Noncationic antibacterial materials are compatible with anionic surfactants in oral compositions and noncationic halogenated hydroxydiphenyl ethers such as Triclosan have been effectively employed in commercial oral compositions as antiplaque agents when mixed with neutral ingredients such as humectants, abrasives and thickeners conventionally used in the formulation of oral compositions. Nothwithstanding the efficacy of halogenated hydroxydiphenyl ethers such as Triclosan, there is a continuing interest in the oral care field for agents which improve the efficacy of such noncationic halogenated hydroxydiphenyl ethers.
Recently, interest has been displayed in the medicinal properties of herbal preparations for use in oral compositions. Herbal preparations are considered “more natural” and are therefore viewed as more acceptable antibacterial ingredients to the consumer.
Extracts of Magnolia Cortex (barks of Magnolia officinalis) are known to have antibacterial efficacy. For example, it has been reported in “Dental caries Prevention by Traditional Chinese Medicines”, T. Namba et al, J. Medicinal Plant Res., vol. 44, pp. 100-106(1982) that some active principles of these extracts, identified to be magnolol and honokiol, were bactericidal against
S. mutans
in the in vitro test Minimal Inhibitory Concentration (MIC) but was not found to be inhibitory to plaque adherence to teeth in vitro tests designed to determine the therapeutic efficacy of antiplaque antigingivitis.
The dental art is continuously seeking synergistic enhancement of antiplaque/antigingivitis of non-herbal, antibacterial compositions such as halogenated biphenylether using herbal compositions in which the non-herbal ingredient has high antibacterial activity alone, while the herbal ingredient has little or no antiplaque activity, wherein the two ingredients have far higher antiplaque activity than could be expected from their individual activities, thus displaying synergism. The advantage of such synergism is that the effectiveness of the non-herbal antiplaque agent is greatly increased, without a concomitant increase in the dosage level or rate of administration so that lower quantities of the non-herbal antiplaque agent can be administered, yet still achieve the desired therapeutic effect. Such synergistic combinations are particularly important in the treatment of delicate or sensitive tissues, such as the oral mucosa, where the ability to reduce the level of the non-herbal antiplaque agent in the oral composition would be beneficial.
There is thus a recognized need for, and it would be highly advantageous to have a antiplaque dentifrice in which a combination of a non-herbal antiplaque agent and a herbal ingredient exhibited synergistic antiplaque activity resulting into enhanced effectiveness against gingivitis.
SUMMARY OF THE INVENTION
In accordance with the present invention it has been unexpectedly discovered that a combination of a nonionic halogenated hydroxydiphenyl ether such as Triclosan and phenolic compound selected from magnolol and honokiol and mixtures thereof extracted from the cortex of Magnolia Officinalas hereinafter referred to as “Magnolia Extract”, are synergistically effective in inhibiting the growth of plaque causing bacteria whereby enhanced antiplaque activity in substantial excess of the additive antibacterial effect of the individual noncationic halogenated hydroxydiphenyl ether or Magnolia Extract is exhibited by the combination of these agents.
The fact that halogenated hydroxydiphenyl ether compounds such as Triclosan have been approved as safe and effective for use in oral care products and that the Magnolia Extract is a widely used herbal extract, particularly in Chinese medicine, suggests that these compounds will both be commercially acceptable as ingredients in oral hygiene products such as dentifrice, mouth rinse, chewing gum and lozenge formulations.
DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS
The Magnolia Extract of the present invention is a dried cortex extract of Magnolia officinalis which belongs to the family Magnoliaceae. As used herein, “extracting” or “extraction” of a solid or liquid material means contacting the material, which if solid is preferably dried and crushed or ground, with an appropriate solvent to remove the substance(s) desired to be extracted from the material. Such an extraction may be carried out by conventional means; for example, by using an extraction apparatus, such as a Soxhlet apparatus, which retains the solid material in a holder and allows the solvent to flow through the material; or by blending the solvent and material together and then separating the liquid and solid phases or two immiscible liquid phases, such as by filtration or by settling and decanting.
Preferred Magnolia Extracts used in the practice of the present invention are made from dried Magnolia plant bark and can be prepared by extracting the bark using an appropriate solvent. Preferred solvents include methanol, ethanol, methylene chloride, hexane cyclohexane, pentane, petroleum ether, chloroform and ethylene dichloride, one part of plant tissue (dry basis) is extracted with from about 5 to about 50 parts, preferably from about 15 parts to about 30 parts of solvent using an extraction apparatus where the solvent is contacted with the bark to obtain a concentrated paste which is then subjected to one or more additional extraction steps with different solvents to further concentrate the originally obtained paste over an extended period of time, preferably from about 6 hours to abut 1-2 days, more preferably for about 1 day.
In one method of extraction, the dried, crushed Magnolia bark in the form of a powder is sequentially contacted with ethanol, methylene chloride, and cyclohexane to form in each step a concentrated paste, the last paste form being dissolved in heated petroleum either at about 50°-60° C. and then dried under vacuum, the final extraction yielding an extract containing about 5 to about 10% by weight honokiol and about 15 to about 25% by weight magnolol.
Magnolol and honokiol are hydroxybiphenyl compounds, the structures of which being represented as follows:
In the practice of the present invention, the antiplaque efficacy of an oral composition containing a noncationic antiplaque agent such as Triclosan, is synergistically enhanced by the presence in the oral composition of an amount of Magnolia Extract which will yield to the oral composition about 0.001 to about 50% by weight of magnolol and preferably about 0.01 to about 0.3 by weight and about 0.02 to about 0.1% by weight of honokiol and preferably about 0.024 to about 20% by weight.
These amounts of magnolol and honokiol are yielded to the oral composition when the Magnolia Extract about 1 to about 20% by weight of magnolol about 2 to about 50%
Gaffar Abdul
Herles Susan M.
Scherl Dale S.
Xu Tao
Colgate - Palmolive Company
Rose Shep K.
Shapiro Paul
LandOfFree
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