Topical application of ivermectin for the treatment of dermatological conditions/afflictions

Abstract

Dermatological conditions/afflictions such as rosacea, common acne, seborrheic dermatitis, perioral dermatitis, acneform rashes, transient acantholytic dermatosis, and acne necrotica miliaris, most notably rosacea, are treated by topically applying onto the affected skin area of an individual in need of such treatment, a topical pharmaceutical composition which comprises a thus effective amount of ivermectin.

1 .- 38 . (canceled) 
     
     
         39 . A method for treating rosacea, common acne, seborrheic dermatitis, perioral dermatitis, an acneform rash, transient acantholytic dermatitis or acne necrotica milliaris, comprising topically applying onto the affected skin area of an individual in need of such treatment, a topical pharmaceutical composition which comprises: a thus effective amount of ivermectin of 1% by weight relative to the total weight of the composition; an oily phase; at least one surfactant-emulsifier selected from the group consisting of polyoxyethylenated fatty acid esters and sorbitan esters; a mixture of solvents and/or propenetrating agents for the ivermectin, said solvents and/or propenetrating agents being selected from the group consisting of propylene glycol, ethanol, isopropanol, butanol, N-methyl-2-pyrrolidone, DMSO, polysorbate 80, phenoxyethanol, glyceryl triacetate and oleyl alcohol; one or more gelling agents but excluding aluminum magnesium silicate/titanium dioxide/silica; and water; said composition having lamellar layers of liquid crystals and being chemically stable over a period of 8 weeks; said composition being in a form selected from the group consisting of an ointment, a cream, a milk, a pomade, an impregnated pad, a syndet, a towelette, a gel, a spray, a foam, a lotion, a stick, a shampoo, a suspension of microspheres, a suspension of nanospheres, a suspension of lipid vesicles, a suspension of polymeric vesicles, a polymeric patch, and a hydrogel for controlled release. 
     
     
         40 . The method as defined by  claim 39 , wherein the composition is in the form of a cream, a gel, a foam or a lotion. 
     
     
         41 . A method for treating rosacea, comprising topically applying onto the affected skin area of an individual in need of such treatment, a topical pharmaceutical composition which comprises: a thus effective amount of ivermectin of 1% by weight relative to the total weight of the composition; an oily phase; at least one surfactant-emulsifier selected from the group consisting of polyoxyethylenated fatty acid esters and sorbitan esters; a mixture of solvents and/or propenetrating agents for the ivermectin, said solvents and/or propenetrating agents being selected from the group consisting of propylene glycol, ethanol, isopropanol, butanol, N-methyl-2-pyrrolidone, DMSO, polysorbate 80, phenoxyethanol, glyceryl triacetate and oleyl alcohol; one or more gelling agents selected from the group consisting of carbomers, cellulose derivatives, xanthan gums, guar gums, polyacrylamides, modified starches and aluminum magnesium silicates but excluding aluminum magnesium silicate/titanium dioxide/silica; and water; said composition having lamellar layers of liquid crystals and being chemically stable over a period of 8 weeks; said composition being in a form selected from the group consisting of an ointment, a cream, a milk, a pomade, an impregnated pad, a syndet, a towelette, a gel, a spray, a foam, a lotion, a stick, a shampoo, a suspension of microspheres, a suspension of nanospheres, a suspension of lipid vesicles, a suspension of polymeric vesicles, a polymeric patch, and a hydrogel for controlled release. 
     
     
         42 . The method as defined by  claim 41 , wherein the composition is in the form of a cream, a gel, a foam or a lotion. 
     
     
         43 . The method as defined by  claim 39 , wherein said topical pharmaceutical composition further comprises:
 6 to 20% of said oily phase;   2 to 12% of said surfactant-emulsifier;   0.1 to 20% of said mixture of solvents and/or propenetrating agents;   0.01 to 5% of said gelling agents;   and water;   the amounts being in percents by weight relative to the total weight of the composition.   
     
     
         44 . The method as defined by  claim 43 , said oily phase comprising a synthetic oil and/or a silicone oil. 
     
     
         45 . The method as defined by  claim 44 , said synthetic oil and/or silicone oil comprising dimethicone, cyclomethicone, isopropyl palmitate and/or isopropyl myristate. 
     
     
         46 . The method as defined by  claim 39 , said at least one surfactant-emulsifier comprising sorbitan monostearate, sorbitan palmitate, sorbitan oleate, sorbitan sesquioleate, sorbitan isostearate, Steareth-20, Steareth-2, Steareth-21 and/or Ceteareth-20. 
     
     
         47 . The method as defined by  claim 39 , said oily phase further comprising fatty substances selected from the group consisting of cetostearyl alcohol, cetyl alcohol, stearyl alcohol, stearic acid, palmitostearic acid and self-emulsifiable wax. 
     
     
         48 . The method as defined by  claim 39 , said one or more gelling agents comprising a carbomer and/or aluminum/magnesium silica. 
     
     
         49 . The method as defined by  claim 48 , said carbomer being an acrylate C 10-30  alkyl acrylate crosspolymer. 
     
     
         50 . The method as defined by  claim 41 , wherein said topical pharmaceutical composition further comprises:
 6 to 20% of said oily phase;   2 to 12% of said surfactant-emulsifier;   0.1 to 20% of said mixture of solvents and/or propenetrating agents;   0.01 to 5% of said gelling agents;   and water;   the amounts being in percents by weight relative to the total weight of the composition.   
     
     
         51 . The method as defined by  claim 50 , said oily phase comprising a synthetic oil and/or a silicone oil. 
     
     
         52 . The method as defined by  claim 51 , said synthetic oil and/or silicone oil comprising dimethicone, cyclomethicone, isopropyl palmitate and/or isopropyl myristate. 
     
     
         53 . The method as defined by  claim 41 , said at least one surfactant-emulsifier comprising sorbitan monostearate, sorbitan palmitate, sorbitan oleate, sorbitan sesquioleate, sorbitan isostearate, Steareth-20, Steareth-2, Steareth-21 and/or Ceteareth-20. 
     
     
         54 . The method as defined by  claim 41 , said oily phase further comprising fatty substances selected from the group consisting of cetostearyl alcohol, cetyl alcohol, stearyl alcohol, stearic acid, palmitostearic acid and self-emulsifiable wax. 
     
     
         55 . The method as defined by  claim 41 , said one or more gelling agents comprising a carbomer and/or aluminum/magnesium silica. 
     
     
         56 . The method as defined by  claim 55 , said carbomer being an acrylate C 10-30  alkyl acrylate crosspolymer. 
     
     
         57 . A topically applicable, stable pharmaceutical composition, said composition comprising:
 an effective amount of ivermectin of 1% by weight relative to the total weight of the composition;   an oily phase;   at least one surfactant-emulsifier selected from the group consisting of polyoxyethylenated fatty acid esters and sorbitan esters;   a mixture of solvents and/or propenetrating agents for the ivermectin, said solvents and/or propenetrating agents being selected from the group consisting of propylene glycol, ethanol, isopropanol, butanol, N-methyl-2-pyrrolidone, DMSO, polysorbate 80, phenoxyethanol, glyceryl triacetate and oleyl alcohol;   one or more gelling agents but excluding aluminum magnesium silicate/titanium dioxide/silica;   and water;   said composition having lamellar layers of liquid crystals and being chemically stable over a period of 8 weeks; said composition being in a form selected from the group consisting of an ointment, a cream, a milk, a pomade, an impregnated pad, a syndet, a towelette, a gel, a spray, a foam, a lotion, a stick, a shampoo, a suspension of microspheres, a suspension of nanospheres, a suspension of lipid vesicles, a suspension of polymeric vesicles, a polymeric patch, and a hydrogel for controlled release.   
     
     
         58 . The topically applicable, stable pharmaceutical composition as defined by  claim 57 , said composition being in the form of a cream, a gel, a foam or a lotion. 
     
     
         59 . The topically applicable, stable pharmaceutical composition as defined by  claim 57 , further comprising:
 6 to 20% of said oily phase;   2 to 12% of said surfactant-emulsifier;   0.1 to 20% of said mixture of solvents and/or propenetrating agents;   0.01 to 5% of said gelling agents;   and water;   the amounts being in percents by weight relative to the total weight of the composition.   
     
     
         60 . The topically applicable, stable pharmaceutical composition as defined by  claim 57 , said one or more gelling agents being selected from the group consisting of carbomers, cellulose derivatives, xanthan gums, guar gums, polyacrylamides, modified starches and aluminum magnesium silicates but excluding aluminum magnesium silicate/titanium dioxide/silica. 
     
     
         61 . The topically applicable, stable pharmaceutical composition as defined by  claim 57 , said oily phase comprising a synthetic oil and/or a silicone oil. 
     
     
         62 . The topically applicable, stable pharmaceutical composition as defined by  claim 61 , said synthetic oil and/or silicone oil comprising dimethicone, cyclomethicone, isopropyl palmitate and/or isopropyl myristate. 
     
     
         63 . The topically applicable, stable pharmaceutical composition as defined by  claim 57 , said at least one surfactant-emulsifier comprising sorbitan monostearate, sorbitan palmitate, sorbitan oleate, sorbitan sesquileate, sorbitan isostearate, Steareth-20, Steareth-2, Steareth 21 and/or Ceteareth-20. 
     
     
         64 . The topically applicable, stable pharmaceutical composition as defined by  claim 57 , said oily phase further comprising fatty substances selected from the group consisting of cetostearyl alcohol, cetyl alcohol, stearyl alcohol, stearic acid, palmitostearic acid and self-emulsifiable wax. 
     
     
         65 . The topically applicable, stable pharmaceutical composition as defined by  claim 57 , said one or more gelling agents comprising a carbomer and/or aluminum/magnesium silica. 
     
     
         66 . The topically applicable, stable pharmaceutical composition as defined by  claim 65 , said carbomer being an acrylate C 10-30  alkyl acrylate crosspolymer. 
     
     
         67 . The topically applicable, stable pharmaceutical composition as defined by  claim 66 , said composition being in the form of a cream, a gel, a foam or a lotion.