Bisphosphocin gel formulations and uses thereof
Inventors
Kates, Steven A. • Johnson, Keith Arthur
Assignees
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Publication Number
US-11096954-B2
Publication Date
2021-08-24
Expiration Date
Abstract
Gel formulations including a Bisphosphocin having antimicrobial activity are disclosed. Methods of using the gel formulations including a Bisphosphocin are further disclosed.
Core Innovation
Disclosed gel formulations are suitable for topical administration and comprise Nu-3, or a pharmaceutically acceptable salt thereof, to provide antimicrobial activity. The formulations are designed to maintain a pH of about pH 1 to about pH 3, and the disclosure emphasizes formulation challenges associated with low pH requirements and ionic incompatibility with typical polymers and emulsifiers.
The gel formulations include a fatty alcohol thickening agent and a nonionic polymer emulsifier, together with a diluent, in specified weight/weight ranges. Example components are selected from cetyl alcohol, lauryl alcohol, stearyl alcohol, cetostearyl alcohol, myristyl alcohol, docosanol alcohol, oleyl alcohol, polysorbate 20, polysorbate 60, polysorbate 80, ceteareth-12, ceteareth-20, ceteareth 30, ceteth-10, ceteth-20, steareth-10, steareth-20, steareth-40, steareth-100, and combinations thereof.
The disclosure further describes topical gel formulations associated with antimicrobial activity and relevance to treating infections and biofilms. Documented uses include diabetic foot ulcers, burn wounds, venous leg ulcers, acne vulgaris, otitis externa, onychomycosis, conjunctivitis, and other infections, as well as disinfectant or sterilization-related concepts and combinations or monotherapy concepts.
Claims Coverage
The document provides three independent claims directed to topical gel formulations. Each independent claim contains multiple inventive features, including defined weight/weight ranges for Nu-3, specified gel-forming components, and a required low pH of about pH 1 to about pH 3.
Low-pH Nu-3 gel formulation for topical administration
A gel formulation suitable for topical administration comprising from about 1% to about 30% (weight/weight) of a Nu-3, or a pharmaceutically acceptable salt thereof, and wherein the formulation has a pH of about pH 1 to about pH 3.
Nu-3 gel with fatty alcohol thickening agent and nonionic polymer emulsifier
A gel formulation comprising from about 1% to about 30% (weight/weight) of Nu-3, from about 1% to about 20% (weight/weight) of a fatty alcohol thickening agent selected from cetyl alcohol, lauryl alcohol, stearyl alcohol, cetostearyl alcohol, myristyl alcohol, docosanol alcohol, oleyl alcohol, and combinations thereof, and from about 0.25% to about 15% (weight/weight) of a nonionic polymer emulsifier selected from polysorbate 20, polysorbate 60, polysorbate 80, ceteareth-12, ceteareth-20, ceteareth 30, ceteth-10, ceteth-20, steareth-10, steareth-20, steareth-40, steareth-100, and combinations thereof, with a diluent and a pH of about pH 1 to about pH 3.
Acid-containing low-pH Nu-3 gel formulation
A gel formulation comprising from about 1% to about 30% (weight/weight) of a Nu-3, from about 1% to about 10% (weight/weight) of a fatty alcohol thickening agent, from about 0.5% to about 5% (weight/weight) of a nonionic polymer emulsifier, from about 1% to about 10% (weight/weight) of an acid selected from hydrochloric acid, hydrobromic acid, hydroiodic acid, nitric acid, carbonic acid, sulfuric acid, and phosphoric acid, and from about 1% to about 45% (weight/weight) of a diluent, wherein the formulation has a pH of about pH 1 to about pH 3.
Defined composition Nu-3 topical gel with cetostearyl alcohol, ceteareth-20, hydrochloric acid, and water
A topical gel formulation comprising from about 1% to about 30% (weight/weight) of Nu-3, from about 1% to about 10% (weight/weight) of cetostearyl alcohol, from about 0.5% to about 5% (weight/weight) of ceteareth-20, from about 1% to about 10% (weight/weight) of hydrochloric acid, and from about 1% to about 45% (weight/weight) of water, wherein the formulation has a pH of about pH 1 to about pH 3.
Across the independent claims, the inventive coverage focuses on topical gel formulations containing Nu-3 in specified weight/weight ranges, formulated with fatty alcohol thickening agents and nonionic polymer emulsifiers, with one independent claim additionally requiring a specified acid, and constrained to a low pH of about pH 1 to about pH 3.
Stated Advantages
Documented Applications
No documented applications found
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