Increased effectiveness of allylamine drug compounds for topical treatment of fungal infections of the skin and skin appendages

摘要

The present invention provides compositions comprising allylamine drug compounds for topical treatment of fungal infections of the skin and skin appendages. In some embodiments a positive charge and enhancers are used in the compositions to allow for increased penetration of the active ingredient through skin and skin appendages. In some embodiments the positively charged active ingredients are either dissolved in the vehicle directly or dissolved in a plurality of beads suspended in the vehicle. The present invention also provides methods for making compositions comprising an allylamine drug compound, and methods of using such compositions for the treatment of fungal infections of the skin and skin appendages.

主权项

1. A method for topical treatment of onychomycosis in a subject in need thereof, wherein the method comprises applying to a nail of the subject a composition comprising:
(a) about 1% weight/weight positively charged terbinafine, (b) about 1% to about 20% weight/weight phospholipid, (c) at least one solubilizer selected from the group consisting of water, ethanol, polyols, glycols, surfactants, phospholipids, polysorbate 20, polysorbate 80, and complexing agents, (d) at least one enhancer selected from the group consisting of ethanol, alkanols, fatty alcohols, fatty acids, fatty acid esters, polyols, polysorbate 20, polysorbate 80, propylene glycol, 1,3-butanediol, terpenes, amides, cyclic amides, pyrrolidone derivatives, essential oils, phospholipids and surfactants, (e) at least one antioxidant, (f) at least one preservative, (g) at least one humectant selected from the group consisting of 1,3-butanediol, propylene glycol, glycerin, sorbitol, lactic acid, methyl gluceth-10, aloe vera extract, sodium PCA, and polyethylene glycol, and (h) at least one viscosity increasing agent, wherein the composition has a pH in the range of about 3.5 to about 7.0.