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Non-halogenated naphthol compounds, antimicrobial compositions containing the same, and methods of using the same

a technology of non-halogenated naphthol and antimicrobial composition, which is applied in the field of antimicrobial compounds, can solve the problems of limited success rate, high toxicity, and substantial incidence of infections, and achieve the effect of reducing the presence of microorganisms and reducing the incidence of infections

Inactive Publication Date: 2005-03-03
HARPER DAVID SCOTT +4
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

"The present invention is about non-halogenated naphthol compounds that have effective antimicrobial activity. These compounds can be used in antimicrobial compositions to reduce the presence of microorganisms on surfaces or in fluids. The invention also provides oral antimicrobial compositions for use in the mouth to prevent dental plaque and promote oral health. The non-halogenated naphthol compounds have specific formulas and can be selected from a variety of options. The invention also includes an effective carrier for the antimicrobial agents."

Problems solved by technology

Although such infections are more common in third world areas, there is also a substantial incidence of the infections in developed areas where a high level of personal hygiene exists.
Such therapies are disadvantageous because they exhibit a limited rate of success, are contraindicated and / or have undesirable drug interactions, produce elevated levels of toxicity, and / or are expensive.
Even with good oral hygiene, it has been shown that microorganisms (include those responsible for plaque formation) rapidly multiply and build up in the oral cavity, and many individuals have difficulty in maintaining good plaque control with brushing and flossing alone.
Quite often the use of dentifrices such as toothpaste, and / or toothbrushes, dental flosses, and cosmetic mouthrinses, is insufficient to control the undesirable microorganisms.
The persistence of these microorganisms in such environments greatly increases the risk of plaque and calculus build-up, which in turn presents a danger of gingival inflammation and more advanced forms of periodontal disease.
In addition, the production of malodorous volatile compounds by accumulated populations of anaerobic microorganisms in dental plaque or on the tongue dorsum may lead to perceptible oral malodor.
However, many mouthrinses have only been effective in masking halitosis.
The attachment and subsequent interaction with the cell surface disrupts the cell membrane structure, causing leakage of the intracellular fluids, eventually killing the microorganism.
However, such materials are generally not effective when formulated in combination with anionic materials and when other cationic minerals and organic molecules present in hard water which may interfere with attraction and subsequent attachment of the cationic materials to the negatively-charged moieties.
These chemical interactions may thereby reduce the overall antimicrobial efficacy of this class of compounds.
However, halogenated compounds may present safety issues.
However, such essential oil formulations possess lower antimicrobial potency than those containing triclosan.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

Mouthrinse Formulation Containing Antimicrobial Compounds of Formula (III)

A mouthrinse composition containing the ingredients and the amounts shown in Table 1 is prepared by mixing the alcohol soluble ingredients 2 and 3 with ethanol. Water is added to the mixture. Water soluble ingredients 4 through 9 are then added and blended thoroughly to the mixture. About 1000 ml of water are added to the mixture to adjust the final volume to yield the mouthrinse composition.

TABLE 1Ingredients% by weight1)Alcohol, USP152)Antimicrobial Agents of Formula (III)0.053)Flavoring oil0.14)Glycerine35)Sodium lauryl methyl cocoyl taurate0.36)Sodium citrate0.087)Citric acid0.028)Saccharin sodium0.19)FD&C Green #30.000210)Water, USPQS to 100

example 2

Dentifrice Composition Containing Antimicrobial Compounds of Formula (III)

A dentifrice composition containing the ingredients and the amounts shown in Table 2 is prepared by combining water, a portion of the humectant, the sweetener, the fluoride, and the water soluble buffers together. The remainder of the humectant is separately combined with the gum and then added to the initial mixture. Titanium oxide and silicas are blended and then added to the mixture. The colorant, flavor oil, antimicrobial compounds of Formula (III) and the surfactant are added and blended with the mixture.

TABLE 2Ingredients% by weight1)Glycerine62)Sodium carboxymethylcellulose1.23)Sorbitol404)Sodium monofluoriphosphate, USP0.765)Saccharin sodium16)Sodium phosphate, dibasic0.037)Sodium phosphate, monobasic0.258)Silicon dioxide, hydrated159)Titanium dioxide0.210)Flavor oil211)Antimicrobial Agents of Formula (III)0.512)FD&C Green #30.000213)Water, deionizedQS to 100

example 3

Deodorant Composition Containing Antimicrobial Compounds of Formula (II)

A deodorant composition containing the ingredients and the amounts shown in Table 3 is prepared by mixing together the polar solvent, volatile nonpolar solvent, and the antimicrobial compounds of Formula (II). Gellants are added to the resulting mixture and agitated. The mixture is heated to a temperature in the range from about 75Ε to 100Ε C until the gellants melted and formed a substantially clear and translucent liquid. The resulting liquid mixture is slightly cooled prior to adding the fragrance. The resulting liquid mixture is poured into a suitable container and cooled to yield a solid form composition.

TABLE 3Ingredients% by weight1)Propylene glycol302)Glycerine2.53)Butyl stearate204)Antimicrobial Agents of Formula (II)0.55)Propylene glycol monostearate156)Water32

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Abstract

An antimicrobial compound, composition containing such compound, and method of use of the same for reducing the presence of microorganism on a substrate or in a fluid environment comprising an antimicrobial effective carrier and one or more essential antimicrobial compounds including non-halogenated naphthol compounds.

Description

FIELD OF THE INVENTION The present invention relates to antimicrobial compounds, and compositions containing such compounds, and more particularly to non-halogenated naphthol compounds exhibiting antimicrobial activity, antimicrobial compositions containing non-halogenated naphthol compounds, and methods of using such compositions. BACKGROUND OF THE INVENTION Recently, attention has focused on personal hygiene in light of mounting concerns about public health. There is a growing awareness of various microorganisms and microbial pathogens such as yeast, fungi, bacteria, molds and viruses, that can cause disease upon access and entry into the body such as through the eyes, ears, nose, mouth and skin. These microbes are generally transmitted from a source (e.g. a contaminated surface) by the hands to a person's body. Thus, a number of illnesses may easily be prevented by decontamination of the skin and the hands. In a related vein, the control of pathogenic or otherwise undesirable m...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K8/34A61K9/68A61K31/05A61K31/075A61K31/12A61K31/22A61Q11/00C07C39/12C07C39/14C07C39/23C07C43/20C07C49/83
CPCA61K8/347A61Q11/00C07C49/83C07C39/23C07C39/14
Inventor HARPER, DAVID SCOTTCOBURN, ROBERT A.SOSHINSKY, ANDREGEORGIADES, CONSTANTINEHUNTLEY, MARIANNE D.
Owner HARPER DAVID SCOTT