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

Abstract

The invention is an increased effectiveness of allylamine drug compounds for topical treatment of fungal infections of skin and skin appendages. The allylamine active ingredient is prepared in an acidic environment; the acidic environment altering the physiochemical properties of the active ingredient resulting in the active ingredient having a positive charge. The positive charge and enhancers used in the formula allow for increased penetration of the active ingredient through skin and skin appendages. The positively charged active ingredients are either dissolved in the vehicle directly or dissolved in a plurality of beads suspended in the vehicle. The bead structure minimizes the molecular diffusion of the positively charged active ingredient and a catalytic species through the bead structure, thus stabilizes the positively charged active ingredient inside the bead by impeding the interaction of the positively charged active ingredient and the catalytic species, and thereby extending the shelf life of the positively charged active ingredient.

What is claimed is: 
     
         1 . An increased effectiveness of allylamine drug compounds for topical treatment of fungal infections of skin and skin appendages comprising:
 a mixture of an active ingredient dissolved in a solubilizer in a closed system added to an acidic environment, an enhancer, an antioxidant, a preservative, a humectant, and a viscosity increasing agent;   the acidic environment altering the physiochemical properties of the active ingredient to form a positively charged active ingredient and combined with the enhancer to increase effectiveness of allylamine drug compounds for topical treatment of fungal infections of skin and skin appendages;   wherein the mixture is added to a vehicle and further contained in a storage container or transferred to a dispenser for application.   
     
     
         2 . The increased effectiveness of allylamine drug compounds for topical treatment of fungal infections of skin and skin appendages of  claim 1 , wherein the mixture is applied to a corneocyte of skin, a trichocyte of hair, an onychocyte of a nail plate or a corneocyte of a nail bed. 
     
     
         3 . The increased effectiveness of allylamine drug compounds for topical treatment of fungal infections of skin and skin appendages of  claim 1 , wherein the active ingredient is an allylamine. 
     
     
         4 . The increased effectiveness of allylamine drug compounds for topical treatment of fungal infections of skin and skin appendages of  claim 1 , wherein the active ingredient is terbinafine hydrochloride. 
     
     
         5 . The increased effectiveness of allylamine drug compounds for topical treatment of fungal infections of skin and skin appendages of  claim 1 , wherein the active ingredient is naftifine hydrochloride. 
     
     
         6 . The increased effectiveness of allylamine drug compounds for topical treatment of fungal infections of skin and skin appendages of  claim 1 , wherein the active ingredient has a concentration of 0.001% to 6%. 
     
     
         7 . The increased effectiveness of allylamine drug compounds for topical treatment of fungal infections of skin and skin appendages of  claim 1 , wherein the acidic environment has a pH of less than 7.5 
     
     
         8 . The increased effectiveness of allylamine drug compounds for topical treatment of fungal infections of skin and skin appendages of  claim 7 , wherein the acidic environment has a pH of 3.5 to 6.0. 
     
     
         9 . The increased effectiveness of allylamine drug compounds for topical treatment of fungal infections of skin and skin appendages of  claim 1 , wherein the increased effectiveness results from the positively charged active ingredient combined with the enhancers. 
     
     
         10 . The increased effectiveness of allylamine drug compounds for topical treatment of fungal infections of skin and skin appendages of  claim 1 , wherein the enhancer is selected from the group consisting of alcohols and alkanols, fatty alcohols, fatty acids, fatty acid esters, polyols, terpenes, amides, cyclic amides, pyrrolidone derivatives, essential oils, phospholipids and surfactants. 
     
     
         11 . The increased effectiveness of allylamine drug compounds for topical treatment of fungal infections of skin and skin appendages of  claim 1 , wherein the positively charged active ingredient and the enhancer is dissolved directly into the vehicle. 
     
     
         12 . The increased effectiveness of allylamine drug compounds for topical treatment of fungal infections of skin and skin appendages of  claim 11 , wherein the vehicle is selected from all conventional dosage forms selected from the group consisting of creams, gels, ointments, lotions, emulsions, solutions, suspensions and pastes. 
     
     
         13 . The increased effectiveness of allylamine drug compounds for topical treatment of fungal infections of skin and skin appendages of  claim 1 , wherein the mixture is encapsulated in microparticles or nanoparticles; said microparticles or nanoparticles having a diameter size of 10 nanometers to 200 micrometers 
     
     
         14 . The increased effectiveness of allylamine drug compounds for topical treatment of fungal infections of skin and skin appendages of  claim 13 , wherein said microparticles or nanoparticles are selected from the group consisting of microspheres, liposomes and microsponges. 
     
     
         15 . The increased effectiveness of allylamine drug compounds for topical treatment of fungal infections of skin and skin appendages of  claim 13 , wherein said microparticles or nanoparticles are further entrapped in a multitude of beads; wherein each bead in the multitude of beads is 0.2 to 10 millimeters 
     
     
         16 . The increased effectiveness of allylamine drug compounds for topical treatment of fungal infections of skin and skin appendages of  claim 1 , wherein the mixture is passed through a tip into a hardening agent to form a bead structure; the bead structure impeding an interaction of the positively charged active ingredient and a catalytic species; the bead structure stabilizing the positively charged active ingredient inside the bead structure by minimizing a molecular diffusion of the positively charged active ingredient and a catalytic species through the bead structure; the bead structure stabilizing the active ingredient inside the bead structure by impeding the interaction of the positively charged active ingredient and the catalytic species, the bead structure being a protective envelop to extend the shelf life of the positively charged active ingredient;
 a plurality of said beads being washed and dried prior to agitation in a delivery vehicle;   wherein the delivery vehicle with plurality of said beads is further contained in a storage container or transferred to a dispenser for application.   
     
     
         17 . The increased effectiveness of allylamine drug compounds for topical treatment of fungal infections of skin and skin appendages of  claim 16 , wherein the viscosity increasing agent is sodium alginate, carrageenan, agar gellan dispersed in polyols. 
     
     
         18 . The increased effectiveness of allylamine drug compounds for topical treatment of fungal infections of skin and skin appendages of  claim 16 , wherein the hardening agent is calcium chloride, barium chloride, magnesium chloride, potassium chloride, lithium gluconate, sodium chloride. 
     
     
         19 . The increased effectiveness of allylamine drug compounds for topical treatment of fungal infections of skin and skin appendages of  claim 16 , wherein the hardening agent has a concentration of 0.1 to 20%. 
     
     
         20 . The increased effectiveness of allylamine drug compounds for topical treatment of fungal infections of skin and skin appendages of  claim 16 , wherein the tip has a diameter of 0.2 to 5 millimeters. 
     
     
         21 . The increased effectiveness of allylamine drug compounds for topical treatment of fungal infections of skin and skin appendages of  claim 16 , wherein the bead structure measures 0.2 to 10 millimeters in size. 
     
     
         22 . The increased effectiveness of allylamine drug compounds for topical treatment of fungal infections of skin and skin appendages of  claim 16 , wherein the bead structure has a hardened outer shell. 
     
     
         23 . The increased effectiveness of allylamine drug compounds for topical treatment of fungal infections of skin and skin appendages of  claim 16 , wherein the bead structure is ruptured by an orifice of the dispenser upon application to skin, skin appendages and nails. 
     
     
         24 . The increased effectiveness of allylamine drug compounds for topical treatment of fungal infections of skin and skin appendages of  claim 16 , wherein the bead structure is ruptured by hand pressure during application to skin, skin appendages and nails.