Cationic antiseptic compositions and methods of use
View Patent ↗Antimicrobial compositions, especially those useful when applied topically, particularly to mucosal tissues (i.e., mucous membranes), including a cationic antiseptic such as biguanides and bisbiguanides such as chlorhexidine and its various salts including but not limited to the digluconate, diacetate, dimethosulfate, and dilactate salts; polymeric quaternary ammonium compounds such as polyhexamethylenebiguanide; silver and various silver complexes; small molecule quaternary ammonium compounds such as benzalkoium chloride and alkyl substituted derivatives; di-long chain alkyl (C8-C18) quaternary ammonium compounds; cetylpyridinium halides and their derivatives; benzethonium chloride and its alkyl substituted derivatives; and octenidine. 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).
1. A method of killing or inactivating microorganisms on mammalian tissue, the method comprising contacting the affected area with an antimicrobial composition, the antimicrobial composition comprising:
an antiseptic selected from the group consisting of biguanides, bisbiguanides, polymeric quaternary ammonium compounds, silver and its complexes, small molecule quaternary ammonium compounds, and combinations thereof; wherein the antiseptic is present in a total amount of at least 0.25 percent by weight based on the total weight of the ready to use composition, and wherein when the antiseptic is a biguanide, the composition has a halide salt concentration less than 0.1M;
a hydrophilic component, wherein the hydrophilic component is present in a total amount of at least 4 wt-%;
a surfactant; wherein the surfactant does not reduce or eliminate the antimicrobial activity of the antiseptic component
a hydrophobic component;
water, which is present in the composition in the greatest amount;
a thickener selected from the group consisting of, cationic polymers, zwitterionic polymers, associative polymers, swellable polymers, and combinations thereof;
wherein the cationic polymers are quaternary polymers and/or protonated tertiary amine functional polymers;
wherein the swellable polymers are quaternary, tertiary, secondary, and/or primary amine functional polymers; wherein the swellable polymers are slightly crosslinked polymers; and wherein the swellable polymers are those which at 0.01 to 0.1 wt-% in an aqueous solvent system, after heating for a sufficient time to ensure solubilization of any potentially soluble components, have a detectable number of observable particles greater than 1 micron in particle size, as determined by light scattering measurement; and
wherein the associative polymers are those which have greater than 2 hydrophobic chains per polymer molecule of greater than 12 carbon atoms;
an enhancer component present in a total amount of greater than 0.4 wt-% based upon the total weight of the ready to use composition and comprising an alpha-hydroxyl acid, a beta-hydroxy acid, a chelating agent, a (C1-C4)alkyl carboxylic acid, a (C6-C12)aryl carboxylic acid, a (C6-C12)aralkyl carboxylic acid, a (C6-C12)alkaryl carboxylic acid, a phenolic compound, a (C1-C10)alkyl alcohol, an ether glycol, or combinations thereof; and
less than 20 wt-% of a (C1-C4)alcohol, if present, and wherein the composition achieves at least 2 log reduction in test bacteria in 10 minutes according to the Antimicrobial Efficacy Test.
2. The method of claim 1 wherein the mammalian tissue is at least a portion of the nasal cavity, the anterior nares or the esophageal cavity.
3. The method of claim 1 wherein the small molecule quaternary ammonium compounds are selected from the group consisting of quaternary ammonium compounds having at least one long chain (C6-C18)alkyl, cetylpyridinium halides and their derivatives, benzethonium chloride and its alkyl substituted derivatives, and octenidine.
4. The method of claim 1 wherein the surfactant comprises a sulfonate surfactant, a sulfate surfactant, a phosphonate surfactant, a phosphate surfactant, a poloxamer, a cationic surfactant, or mixtures thereof.
5. The method of claim 1 wherein the hydrophilic component comprises a glycol, a lower alcohol ether, a short chain ester, or combinations thereof, and wherein the hydrophilic component is soluble in water in an amount of at least 20 wt-% at 23° C.
6. The method of claim 1 wherein the hydrophobic component is an organic compound that is liquid, gelatinous, semisolid, or solid at 23° C. and has a solubility in water of less than 5 wt-% at 23° C.
7. The method of claim 1 wherein the microorganisms comprise bacteria and the antimicrobial composition is used in an amount effective to kill one or more bacteria.
8. The method of claim 1 wherein the microorganisms comprise one or more viruses and the antimicrobial composition is used in an amount effective to inactivate one or more viruses.
9. The method of claim 1 wherein the microorganisms comprise one or more fungi and the antimicrobial composition is used in an amount effective to kill one or more fungi.
10. The method of claim 1 wherein the antiseptic is a polybiguanide.
11. The method of claim 10 wherein the polybiguanide is polyhexamethylene biguanide.
12. The method of claim 1 wherein the mammalian tissue comprises skin or mucosal tissue.
13. The method of claim 1 wherein the mammalian tissue is present in the middle ear, tympanic membrane, and/or Eustachian tube of a subject.
14. The method of claim 1 wherein the mammalian tissue is at least a portion of the respiratory system of a subject.
15. The method of claim 1 wherein the mammalian tissue is present in a wound of a subject.
16. The method of claim 1 wherein the mammalian tissue is present in the nose of a subject.
17. The method of claim 1 wherein the antimicrobial composition is stable physically or chemically.
18. The method of claim 17 wherein the antimicrobial composition is stable physically and chemically.
19. The method of claim 1 wherein the surfactant is a cationic, amphoteric, or nonionic.
20. The method of claim 19 wherein the surfactant is nonionic and is an ethylene oxide/propylene oxide surfactant.