Topical application of ivermectin for the treatment of dermatological conditions/afflictions
View Patent ↗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. 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 emulsion which comprises: a thus effective amount of ivermectin; 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 emulsion having lamellar layers of liquid crystals and being chemically stable over a period of 8 weeks.
2. A method for treating rosacea, comprising topically applying onto the affected skin area of an individual in need of such treatment, a topical pharmaceutical emulsion which comprises: a thus effective amount of ivermectin; 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 emulsion having lamellar layers of liquid crystals and being chemically stable over a period of 8 weeks.
3. The method as defined by claim 1 , said topical pharmaceutical emulsion comprising from 0.001% to 10% by weight of ivermectin.
4. The method as defined by claim 1 , wherein said topical pharmaceutical emulsion comprises:
0.1 to 5% of ivermectin;
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.
5. The method as defined by claim 4 , said oily phase comprising a synthetic oil and/or a silicone oil.
6. The method as defined by claim 5 , said synthetic oil and/or silicone oil comprising dimethicone, cyclomethicone, isopropyl palmitate and/or isopropyl myristate.
7. The method as defined by claim 1 , 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.
8. The method as defined by claim 1 , 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-emulsified wax.
9. The method as defined by claim 1 , said one or more gelling agents comprising a carbomer and/or aluminum/magnesium silica.
10. The method as defined by claim 9 , said carbomer being an acrylate C 10-30 alkyl acrylate crosspolymer.
11. A topically applicable, stable pharmaceutical emulsion, said emulsion comprising:
an effective amount of ivermectin;
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 emulsion having lamellar layers of liquid crystals and being chemically stable over a period of 8 weeks.
12. The topically applicable, stable pharmaceutical emulsion as defined by claim 11 , comprising:
0.1 to 5% of ivermectin;
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.
13. The topically applicable, stable pharmaceutical emulsion as defined by claim 11 , 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.
14. The topically applicable, stable pharmaceutical emulsion as defined by claim 11 , comprising from 0.001% to 10% by weight of ivermectin.
15. The topically applicable, stable pharmaceutical emulsion as defined by claim 11 , said oily phase comprising a synthetic oil and/or a silicone oil.
16. The topically applicable, stable pharmaceutical emulsion as defined by claim 15 , said synthetic oil and/or silicone oil comprising dimethicone, cyclomethicone, isopropyl palmitate and/or isopropyl myristate.
17. The topically applicable, stable pharmaceutical emulsion as defined by claim 11 , 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.
18. The topically applicable, stable pharmaceutical emulsion as defined by claim 11 , 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.
19. The topically applicable, stable pharmaceutical emulsion as defined by claim 11 , said one or more gelling agents comprising a carbomer and/or aluminum/magnesium silica.
20. The topically applicable, stable pharmaceutical emulsion as defined by claim 19 , said carbomer being an acrylate C 10-30 alkyl acrylate crosspolymer.