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 the treatment of 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, said topical pharmaceutical composition being formulated as an emulsion, the topical pharmaceutical emulsion comprising:
an oily phase comprising dimethicone, cyclomethicone, isopropyl palmitate and/or isopropyl myristate, said oily phase further comprising fatty substances selected from the group consisting of cetyl alcohol, cetostearyl alcohol, stearyl alcohol, palmitostearic acid, stearic acid and self-emulsifiable wax;
at least one surfactant-emulsifier selected from the group consisting of glyceryl/PEG100 stearate, sorbitan monostearate, sorbitan palmitate, Steareth-20, Steareth-2, Steareth-21 and Ceteareth-20;
ivermectin;
a mixture of solvents and/or propenetrating agents selected from the group consisting of propylene glycol, oleyl alcohol, phenoxyethanol and glyceryl triacetate;
acrylate C10-C30 alkyl acrylate crosspolymer gelling agent; and
water;
said emulsion being chemically stable over a period of time of 12 weeks.
2. The method as defined by claim 1 , wherein said at least one surfactant-emulsifier is present in an amount of up to 15% by weight.
3. The method as defined by claim 1 , wherein said ivermectin is present in an amount of 0.1 to 5% by weight.
4. The method as defined by claim 1 wherein said mixture of solvents and/or propenetrating agents is present in an amount of 0.1 to 20% by weight.
5. The method as defined by claim 1 , wherein said one or more gelling agents is/are present in an amount of 0.01 to 5% by weight.
6. A method for the treatment of 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, said topical pharmaceutical composition being formulated as an emulsion, the topical pharmaceutical emulsion comprising:
3 to 50% by weight of an oily phase comprising dimethicone, cyclomethicone, isopropyl palmitate and/or isopropyl myristate, said oily phase further comprising fatty substances selected from the group consisting of cetyl alcohol, cetostearyl alcohol, stearyl alcohol, palmitostearic acid, stearic acid and self-emulsifiable wax;
up to 15% by weight of at least one surfactant-emulsifier selected from the group consisting of glyceryl/PEG100 stearate, sorbitan monostearate, sorbitan palmitate, Steareth-20, Steareth-2, Steareth-21 and Ceteareth-20;
0.1 to 5% by weight of ivermectin;
0.1 to 20% by weight of a mixture of solvents and/or propenetrating agents selected from the group consisting of propylene glycol, oleyl alcohol, phenoxyethanol and glyceryl triacetate;
0.01 to 5% by weight of acrylate C10-C30 alkyl acrylate crosspolymer gelling agent; and
water;
said emulsion being chemically stable over a period of time of 12 weeks.
7. A method for the treatment of 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, said topical pharmaceutical composition being formulated as an emulsion, the topical pharmaceutical emulsion comprising:
6 to 20% by weight of an oily phase comprising dimethicone, cyclomethicone, isopropyl palmitate and/or isopropyl myristate, said oily phase further comprising fatty substances selected from the group consisting of cetyl alcohol, cetostearyl alcohol, stearyl alcohol, palmitostearic acid, stearic acid and self-emulsifiable wax;
up to 15% by weight of at least one surfactant-emulsifier selected from the group consisting of glyceryl/PEG100 stearate, sorbitan monostearate, sorbitan palmitate, Steareth-20, Steareth-2, Steareth-21 and Ceteareth-20;
0.1 to 5% by weight of ivermectin;
0.1 to 20% by weight of a mixture of solvents and/or propenetrating agents selected from the group consisting of propylene glycol, oleyl alcohol, phenoxyethanol and glyceryl triacetate;
0.01 to 5% by weight of acrylate C10-C30 alkyl acrylate crosspolymer gelling agent; and
water;
said emulsion being chemically stable over a period of time of 12 weeks.
8. The method as defined by claim 1 , wherein:
said oily phase comprises dimethicone and isopropyl palmitate, said oily phase further comprising fatty substances selected from the group consisting of cetyl alcohol and stearyl alcohol;
said at least one surfactant-emulsifier is selected from the group consisting of sorbitan monostearate and Ceteareth-20; and
said mixture of solvents and/or propenetrating agents is selected from the group consisting of propylene glycol, oleyl alcohol and phenoxyethanol.
9. The method as defined by claim 1 , wherein:
said oily phase comprises dimethicone, isopropyl palmitate, cetyl alcohol and stearyl alcohol;
said at least one surfactant-emulsifier is sorbitan monostearate and Ceteareth-20; and
said mixture of solvents and/or propenetrating agents is a mixture of propylene glycol, oleyl alcohol and phenoxyethanol.
10. The method as defined by claim 1 , said topical pharmaceutical composition further comprising one or more additives selected from the group consisting of flavor enhancers, preserving agents, stabilizers, humidity regulators, pH regulators, osmotic pressure modifiers, UV-A screening agents, UV-B screening agents and antioxidants.
11. The method as defined by claim 1 , said topical pharmaceutical composition further comprising one or more additives selected from the group consisting of glycerol, methyl para-hydroxybenzoate, disodium EDTA, citric acid monohydrate, propyl para-hydroxybenzoate and sodium hydroxide.
12. A topically applicable stable pharmaceutical emulsion, comprising:
an oily phase comprising dimethicone, cyclomethicone, isopropyl palmitate and/or isopropyl myristate, said oily phase further comprising fatty substances selected from the group consisting of cetyl alcohol, cetostearyl alcohol, stearyl alcohol, palmitostearic acid, stearic acid and self-emulsifiable wax;
at least one surfactant-emulsifier selected from the group consisting of glyceryl/PEG100 stearate, sorbitan monostearate, sorbitan palmitate, Steareth-20, Steareth-2, Steareth-21 and Ceteareth-20;
ivermectin;
a mixture of solvents and/or propenetrating agents selected from the group consisting of propylene glycol, oleyl alcohol, phenoxyethanol and glyceryl triacetate;
acrylate C10-C30 alkyl acrylate crosspolymer gelling agent; and
water;
said emulsion being chemically stable over a period of time of 12 weeks.
13. The topically applicable stable pharmaceutical emulsion as defined by claim 12 , wherein said at least one surfactant-emulsifier is present in an amount of up to 15% by weight.
14. The topically applicable, stable pharmaceutical emulsion as defined by claim 12 , wherein said ivermectin is present in an amount of 0.1 to 5% by weight.
15. The topically applicable, stable pharmaceutical emulsion as defined by claim 12 , wherein said mixture of solvents and/or propenetrating agents is present in an amount of 0.1 to 20% by weight.
16. The topically applicable, stable pharmaceutical emulsion as defined by claim 12 , wherein one or more gelling agents is/are present in an amount of 0.01 to 5% by weight.
17. A topically applicable stable pharmaceutical emulsion, comprising:
3 to 50% by weight of an oily phase comprising dimethicone, cyclomethicone, isopropyl palmitate and/or isopropyl myristate, said oily phase further comprising fatty substances selected from the group consisting of cetyl alcohol, cetostearyl alcohol, stearyl alcohol, palmitostearic acid, stearic acid and self-emulsifiable wax;
up to 15% by weight of at least one surfactant-emulsifier selected from the group consisting of glyceryl/PEG100 stearate, sorbitan monostearate, sorbitan palmitate, Steareth-20, Steareth-2, Steareth-21 and Ceteareth-20;
0.1 to 5% by weight of ivermectin;
0.1 to 20% by weight of a mixture of solvents and/or propenetrating agents selected from the group consisting of propylene glycol, oleyl alcohol, phenoxyethanol and glyceryl triacetate;
0.01 to 5% by weight of acrylate C10-C30 alkyl acrylate crosspolymer gelling agent; and
water;
said emulsion being chemically stable over a period of time of 12 weeks.
18. A topically applicable stable pharmaceutical emulsion, comprising:
6 to 20% by weight of an oily phase comprising dimethicone, cyclomethicone, isopropyl palmitate and/or isopropyl myristate, said oily phase further comprising fatty substances selected from the group consisting of cetyl alcohol, cetostearyl alcohol, stearyl alcohol, palmitostearic acid, stearic acid and self-emulsifiable wax;
up to 15% by weight of at least one surfactant-emulsifier selected from the group consisting of glyceryl/PEG100 stearate, sorbitan monostearate, sorbitan palmitate, Steareth-20, Steareth-2, Steareth-21 and Ceteareth-20;
0.1 to 5% by weight of ivermectin;
0.1 to 20% by weight of a mixture of solvents and/or propenetrating agents selected from the group consisting of propylene glycol, oleyl alcohol, phenoxyethanol and glyceryl triacetate;
0.01 to 5% by weight of acrylate C10-C30 alkyl acrylate crosspolymer gelling agent; and
water;
said emulsion being chemically stable over a period of time of 12 weeks.
19. The topically applicable stable pharmaceutical emulsion as defined by claim 12 , wherein:
said oily phase comprises dimethicone and isopropyl palmitate, said oily phase further comprising fatty substances selected from the group consisting of cetyl alcohol and stearyl alcohol;
said at least one surfactant-emulsifier is selected from the group consisting of sorbitan monostearate and Ceteareth-20; and
said mixture of solvents and/or propenetrating agents is selected from the group consisting of propylene glycol, oleyl alcohol and phenoxyethanol.
20. The topically applicable pharmaceutical emulsion as defined by claim 12 , wherein:
said oily phase comprises dimethicone, isopropyl palmitate, cetyl alcohol and stearyl alcohol;
said at least one surfactant-emulsifier is sorbitan monostearate and Ceteareth-20; and
said mixture of solvents and/or propenetrating agents is propylene glycol, oleyl alcohol and phenoxyethanol.
21. The topically applicable stable pharmaceutical emulsion as defined by claim 12 , further comprising one or more additives selected from the group consisting of flavor enhancers, preserving agents, stabilizers, humidity regulators, pH regulators, osmotic pressure modifiers, UV-A screening agents, UV-B screening agents and antioxidants.
22. The topically applicable stable pharmaceutical emulsion as defined by claim 12 , further comprising one or more additives selected from the group consisting of glycerol, methyl para-hydroxybenzoate, disodium EDTA, citric acid monohydrate, propyl para-hydroxybenzoate and sodium hydroxide.
23. The topically applicable stable pharmaceutical emulsion as defined by claim 20 , further comprising glycerol, methyl para-hydroxybenzoate, disodium EDTA, citric acid monohydrate, propyl para-hydroxybenzoate and sodium hydroxide.