Drug – bio-affecting and body treating compositions – Dentifrices
Reexamination Certificate
2002-07-29
2004-02-10
Rose, Shep K. (Department: 1614)
Drug, bio-affecting and body treating compositions
Dentifrices
C424S048000, C424S058000, C424S435000, C424S440000
Reexamination Certificate
active
06689342
ABSTRACT:
FIELD OF THE INVENTION
The present invention is related generally to oral care compositions, more particularly to oral care compositions comprising substituted tropolone compounds and essential oils, and methods of using the same for oral care.
BACKGROUND OF THE INVENTION
Oral malodor, plaque, gingivitis, periodontal disease, and discoloration of the teeth, are all undesirable conditions that affect many people. First malodor of the oral cavity also known as halitosis or bad breath, has been broadly estimated to afflict 20 to 90 million individuals in the US. It is generally believed that the presence of anaerobic bacteria, especially gram-negative anaerobic bacteria, in the mouth contributes to this condition. Other oral conditions caused by microorganisms include periodontal disease, tooth decay, inflammation and the like.
Periodontal disease is a major cause of tooth loss in adults, and can manifest itself in people as young as age 12. Periodontal disease affects the periodontum, which is the investing and supporting tissues surrounding a tooth (i.e., the periodontal ligament, the gingiva, and the alveolar bone). Gingivitis and periodontatitis are disorders of the gingiva and the deeper periodontal tissues, respectively. Periodontal disease is generally associated with the accumulation of plaque on the teeth. The teeth are coated with a salivary proteinaceous material (pellicle) and thereafter streptococci adhere to this coating. Gingivitis is generally caused by dental plaque, and periodontatitis is caused by the infection spreading to the periodontal pocket or space between the gingival and the tooth root.
Many of the current oral care compositions including toothpastes, mouthwashes, rinses and tooth gels are formulated to clean the oral cavity and kill pathogenic microbes. Such oral care compositions are typically formulated with one or more antimicrobial agents to suppress the microorganisms that contribute both to the initiation and progression of oral malodor, periodontal disease and other undesirable oral conditions. Current oral care compositions comprise antimicrobial agents and are formulated to maximize the kinetics of the antimicrobial agent. The antimicrobial agents are dissolved to provide effective prevention of bad breath, eradication of oral microbes, and penetration, reduction, and elimination of plaque and gingivitis.
One well-known antiseptic agent is thymol, also known as an essential oil, which is utilized for its antimicrobial activity in a range of oral care preparations. In particular, thymol has been utilized in oral hygiene compositions such as mouthwashes in sufficient quantities to provide desired beneficial therapeutic effects. LlSTERINE® Brand mouth rinse is a well-known antiseptic mouthwash that has been used by millions of people for over one hundred years and has been proven effective in killing microbes in the oral cavity that are responsible for plaque, gingivitis, and bad breath. Thymol and other essential oils, such as methyl salicylate, menthol, and eucalyptol, are active ingredients (e.g., antimicrobial agents) in antiseptic mouth rinses such as LISTERINE®. Even in small amounts, these essential oils are effective antimicrobial agents. Without being restricted to any specific theory, it is believed that the efficacy and taste of antiseptic mouthwashes such as LISTERINE® may be due to the dissolution and delivery kinetics of these four active agents.
There is still a need to provide efficacious oral care compounds and oral care compositions such as mouthwashes or rinses containing the same having favorable antimicrobial kinetics while exhibiting chemical stability and solubility favorable for efficient delivery and antiseptic effectiveness. There is still a need to provide oral care compositions and compounds that are effective for the prevention or treatment of diseases and conditions of the oral cavity in warm-blooded animals including humans by eliminating or suppressing the presence of pathogenic oral microorganisms responsible for plaque, gingivitis and other undesirable oral conditions in the oral cavity.
SUMMARY OF THE INVENTION
The present invention relates to oral care compositions and methods of using the same for preventing or treating diseases or conditions of the oral cavity in warm-blooded animals including humans. Generally, the oral care composition comprises substituted tropolone compounds in combination with one or more essential oils in amounts effective for suppressing or eliminating the presence of harmful pathogenic oral microorganisms in the oral cavity. The oral care compositions provide a high level of antimicrobial kinetics and efficacy useful for preventing, among others, plaque, gum disease, and oral malodor. In addition, the oral care composition can be formulated into a range of oral care products including, but not limited to, toothpastes, tooth gels, tooth powders, mouthwashes, lozenges, chewing gums, tooth strips, dental floss, orally consumable film and mouth spray.
In one particular aspect of the present invention, there is provided an oral care composition comprising:
(a) an oral care effective amount of at least one compound of Formula
wherein R
1
, R
2
, R
3
, R
4
, and R
5
are each independently selected from the group consisting of hydrogen, hydroxy, an alkyl group, a hydroxyalkyl group, an alkoxyalkyl group, an alkylene group, an alkenylene group, an alkaryl group, an alkcycloalkyl group, an alkoxy group, an alkenyl group, an alkynyl group, an aryl group, a cycloalkyl group, a cycloalkenyl group, an aliphatic group optionally substituted with 1 to 3 halogens, an aromatic group optionally substituted with 1 to 3 halogens and a carbonyl group, and isomers and pharmaceutically acceptable salts thereof;
(b) at least one essential oil; and
(c) a pharmaceutically acceptable oral carrier.
In a preferred embodiment of the present invention, the oral care composition comprises an oral care effective amount of at least one compound of Formula (I) wherein R
2
, R3, and R
5
are each independently selected from the group consisting of hydrogen, an alkyl group having 1 to 6 carbons, a hydroxyalkyl group having 1 to 6 carbons, and an alkoxyalkyl group wherein the “alkoxy” portion and the “alkyl” portion each have from 1 to 6 carbons, and R
1
and R
4
are each hydrogen.
Preferably the essential oil is selected from the group consisting of thymol, eucalyptol, menthol, methyl salicylate, and combinations thereof.
In another aspect of the present invention, there is provided a method for preventing or treating diseases or conditions of the oral cavity, comprising administering an oral care effective amount of the oral care composition of the present invention to a warm-blooded animal including humans.
DETAILED DESCRIPTION OF THE INVENTION
The present invention is directed to oral care compositions with antimicrobial efficacy against microorganisms, particularly oral microorganisms responsible for producing undesirable diseases or conditions in the oral cavity, including oral malodor, plaque build-up, and the like, and the resulting tooth and gum diseases that may follow. The oral care compositions may be in a form selected from, for example, mouthwashes, toothpastes, tooth powders, dental creams, dental flosses, liquids, gels, chewing gums, liquid center filled gums, mints, lozenges, orally consumable films and the like. One preferred aspect of the present invention is directed to an oral care composition containing an effective amount of at least one substituted tropolone compound having antimicrobial activity in combination with one or more essential oils. In a particularly preferred aspect of the present invention, there is provided an oral care composition, preferably a mouthwash, containing an effective amount of at least one substituted tropolone compound in combination with at least one essential oil.
Essential oils are volatile aromatic oils which may be synthetic or may be derived from plants by distillation, expression or extraction, and which usually carry the odor or flavor of the plant from which
Arvanitis Georgia
Berardini Michael
Finnegan Marybeth
Pan Pauline
Soshinsky Andre
Rose Shep K.
Warner-Lambert & Company
Watov & Kipnes P.C.
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