Antimicrobial compositions and methods

Inactive Publication Date: 2005-03-17
3M INNOVATIVE PROPERTIES CO
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

Compositions of the present invention provide effective topical antimicrobial activity and are accordingly useful in the local treatment and/or prevention of conditions that are caused, or aggravated by, microorganisms (including viruses, bacteria, fungi, mycoplasma, and protozoa) on skin and/or mucous membranes.
Significantly, certain embodiments of the present invention have a very low potential for generating microbial resistance. Thus, such compositions can be applied multiple times over one or more days to

Problems solved by technology

Thus, they may not retard, and can even enhance, wound healing.
Even though presurgical decolonization of the anterior nares using mupirocin has been shown to decrease the risk of surgical site infection by as much as 2 to 10 times (T. Perl et al., Ann. Pharmacother., 32:S7-S 16 (1998)), the high resistance rates to this antibiotic make it unsuitable for routine use.
Not only does resistance eliminate the ability of a medication to treat an affliction, but it can also put the patient at further risk, especially if the antibiotic is one that is routinely used systemically.
This nonspecific activity makes it difficult for resistance to develop to antiseptics.
These compounds, however, need to be used at concentrations that often result in irritation or tissue damage, e

Method used

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  • Antimicrobial compositions and methods
  • Antimicrobial compositions and methods

Examples

Experimental program
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examples

Objects and advantages of this invention are further illustrated by the following examples, but the particular materials and amounts thereof recited in these examples, as well as other conditions and details, should not be construed to unduly limit this invention.

Glossary of Components

AcronymTrade NameDescriptionSource / AddressGMLLAURICIDINGlycerol monolaurateMedChem Laboratories,Inc. / Galena, ILPURACLactic Acid (88%)Purac America / HIPURE 88Lincolnshire, ILMandelic AcidSigma-Aldrich / St. Louis, MOBenzoic acidMallinckrodt BakerInc. / Paris, KYSalicylic acidMallinckrodtBaker Inc.C10H23 glycerin ether(Preparationdescribed inExample 18)Propylene glycolUniquema / monocaprateWilmington, DECRODAPHOSPPG-5 ceteth-10Croda Inc. / SGphosphateParsipanny, NJDOSS,COMPLEMIXDioctylsulfosuccinate,Cytec Industries / 100%sodium salt (Docusate,West Paterson, NJsodium)DOSS,AEROSOL GPGDioctylsulfosuccinate,Cytec Industries70%sodium salt, 70% inethanol / waterPOLYSTEPSodium laureth-4Stepan Company / B12sulfateNorthfiel...

examples 3-7

Antimicrobial compositions were prepared as described in Examples 1-2 using the components shown in Table 2a. Mandelic acid was ground into a fine powder using a mortar and pestle and added to the glycerin and DOSS and heated to about 88° C. for Examples 3 and 4 or added directly to the hot, molten petrolatum at about 82° C. for Examples 5 and 6.

TABLE 2aComponents (weight percent)ExampleMandelicDOSSWhiteNo.GMLAcid(100%)GlycerinPetrolatum33.001.001.0010.0085.0043.030.920.0010.1185.9453.001.001.000.0095.0063.001.000.000.0096.0072.970.900.000.9695.17

Compositions of Examples 3-7 were evaluated using the Antimicrobial Kill Rate Test and the results are shown in Table 2b and 2c.

TABLE 2bMRS A (log reduction)E. coli (log reduction)ExampleAfter 2After 5After 10After 2After 5After 10No.minutesminutesminutesminutesminutesminutes33.65.75.94.05.66.142.83.94.35.75.66.055.05.85.45.45.86.362.42.63.63.23.33.772.33.14.14.03.94.7

TABLE 2cExamplePseudomonas ae. (log reduction)No.After 2 minutesAft...

example 3

contained a hydrophilic component (glycerin) and surfactant (DOSS) in addition to the antimicrobial lipid (GML) and enhancer (mandelic acid). This sample had the best antimicrobial activity overall, achieving greater than 5.9 log reduction against all three organisms at 10 minutes. Example 4 contained no surfactant (no DOSS), which led to a decrease in activity over Example 5 which contained no hydrophilic component had decreased activity over Example 3 but the effect was not as great as elimination of the surfactant. Example 6 containing no hydrophilic component or surfactant showed relatively poor antimicrobial activity. Addition of only 1% hydrophilic component (Example 7) showed an improvement in antimicrobial activity.

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Abstract

Antimicrobial compositions, especially those useful when applied topically, particularly to mucosal tissues (i.e., mucous membranes), including a fatty acid ester, fatty ether, or alkoxide derivative thereof. The compositions can also include an enhancer component, a surfactant, a hydrophobic component, and/or a hydrophilic component. Such compositions provide effective topical antimicrobial activity and are accordingly useful in the treatment and/or prevention of conditions that are caused, or aggravated by, microorganisms (including viruses).

Description

BACKGROUND The use of antimicrobial agents plays an important part in current medical therapy. This is particularly true in the fields of dermatology as well as skin and wound antisepsis, where the most effective course of treatment for skin or mucous membranes (e.g., as in the nasal cavities and in particular the anterior nares), which are afflicted with bacterial, fungal, or viral infections or lesions, frequently includes the use of a topical antimicrobial agent. For decades medicine has relied primarily upon antibiotics to fight systemic as well as topical infections. For example, bacitracin, neomycin sulfate, polymyxin B sulfate, gentamicin, framycetin-gramicidin, lysostaphin, methicillin, rifampin, tobramycin, nystatin, mupirocin, and combinations thereof, as well as many others, have been used with varying success. Antibiotics are generally effective at very low levels and are often safe with very few, if any, side effects. Often antibiotics have little or no toxicity to ma...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/19A61K31/23A61K31/231A61K31/25A61K45/06A61K47/06A61K47/10A61K47/12A61K47/14A61K47/20
CPCA61K9/0014A61K9/0043A61K47/44A61K47/20A61K47/14A61K47/12A61K47/10A61K47/06A61K45/06A61K9/0046A61K9/0053A61K9/007A61K31/19A61K31/23A61K31/231A61K31/25A61K2300/00A61P1/00A61P11/00A61P17/00A61P17/02A61P27/16A61P31/00A61P31/04A61P31/10A61P31/12Y02A50/30
Inventor SCHOLZ, MATTHEW T.GIBBS, DIANNE L.CAPECCHI, JOHN T.ANDREWS, JEFFREY F.
Owner 3M INNOVATIVE PROPERTIES CO
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