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 regime or regimen 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 cetostearyl alcohol, cetyl alcohol, stearyl alcohol, stearic acid, palmitostearic acid and self-emulsifiable wax;
2 to 12% 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;
1 to 10% 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 one or more gelling agents selected from the group consisting of carbomers; and
water;
said emulsion being chemically stable over a period of time of 12 weeks.
2. A regime or regimen 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, isopropyl palmitate and/or isopropyl myristate, said oily phase further comprising fatty substances selected from the group consisting of cetyl alcohol, stearyl alcohol, palmitostearic acid and self-emulsifiable wax;
2 to 12% 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;
1 to 10% 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.
3. A regime or regimen 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 and isopropyl palmitate, said oily phase further comprising fatty substances selected from the group consisting of cetyl alcohol and stearyl alcohol;
2 to 12% by weight of at least one surfactant-emulsifier selected from the group consisting of sorbitan monostearate and Ceteareth-20;
0.1 to 5% by weight of ivermectin;
1 to 10% by weight of a mixture of solvents and/or propenetrating agents selected from the group consisting of propylene glycol, oleyl alcohol and phenoxyethanol;
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.
4. A regime or regimen 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, isopropyl palmitate, cetyl alcohol and stearyl alcohol;
2 to 12% by weight of sorbitan monostearate and Ceteareth-20 as surfactant emulsifiers;
0.1 to 5% by weight of ivermectin;
1 to 10% by weight of a mixture of the solvents and/or propenetrating agents propylene glycol, oleyl alcohol and phenoxyethanol;
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.
5. The regime or regimen 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.
6. The regime or regimen 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.
7. The regime or regimen as defined by claim 2 , 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.
8. The regime or regimen as defined by claim 2 , 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.
9. The regime or regimen as defined by claim 2 , said topical pharmaceutical emulsion comprising:
Ivermectin
1.00
Glycerol
4.0
Acrylate C10-30 alkyl acrylate
0.15
crosspolymer
Methyl para-hydroxybenzoate
0.2
Disodium EDTA
0.05
Citric acid monohydrate
0.05
Isopropyl myristate
4.0
Cetyl alcohol
3.0
Stearyl alcohol
2.0
Self-emulsifiable wax
0.8
Palmitostearic acid
0.5
Steareth-20
2.0
Sorbitan palmitate
1.0
Dimethicone 20
0.5
Propyl para-hydroxybenzoate
0.1
Propylene glycol
4.0
Glyceryl triacetate
1.0
Phenoxyethanol
0.5
10% sodium hydroxide
qs pH
Water
qs 100
as % by weight relative to the total weight of the composition.
10. The regime or regimen as defined by claim 3 , 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 regime or regimen as defined by claim 3 , 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. The regime or regimen as defined by claim 4 , 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.
13. The regime or regimen as defined by claim 4 , 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.
14. The regime or regimen as defined by claim 4 , further comprising glycerol, methyl para-hydroxybenzoate, disodium EDTA, citric acid monohydrate, propyl para-hydroxybenzoate and sodium hydroxide.
15. 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 cetostearyl alcohol, cetyl alcohol, stearyl alcohol, stearic acid, palmitostearic acid and self-emulsifiable wax;
2 to 12% 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;
1 to 10% 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 one or more gelling agents selected from the group consisting of carbomers; and
water;
said emulsion being chemically stable over a period of time of 12 weeks.
16. A topically applicable stable pharmaceutical emulsion, comprising:
6 to 20% by weight of an oily phase comprising dimethicone, isopropyl palmitate and/or isopropyl myristate, said oily phase further comprising fatty substances selected from the group consisting of cetyl alcohol, stearyl alcohol, palmitostearic acid and self-emulsifiable wax;
2 to 12% 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;
1 to 10% 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.
17. A topically applicable, stable pharmaceutical emulsion, comprising:
6 to 20% by weight of an oily phase comprising dimethicone and isopropyl palmitate, said oily phase further comprising fatty substances selected from the group consisting of cetyl alcohol and stearyl alcohol;
2 to 12% by weight of at least one surfactant-emulsifier selected from the group consisting of sorbitan monostearate and Ceteareth-20;
0.1 to 5% by weight of ivermectin;
1 to 10% by weight of a mixture of solvents and/or propenetrating agents selected from the group consisting of propylene glycol, oleyl alcohol and phenoxyethanol;
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 at least 12 weeks.
18. A topically applicable, pharmaceutical emulsion, comprising:
6 to 20% by weight of an oily phase comprising dimethicone, isopropyl palmitate, cetyl alcohol and stearyl alcohol;
2 to 12% by weight of sorbitan monostearate and Ceteareth-20 as surfactant emulsifiers;
0.1 to 5% by weight of ivermectin;
1 to 10% by weight of a mixture of the solvents and/or propenetrating agents propylene glycol, oleyl alcohol and phenoxyethanol;
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 15 , 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.
20. The topically applicable, stable pharmaceutical emulsion as defined by claim 15 , 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.
21. The topically applicable, stable pharmaceutical emulsion as defined by claim 16 , 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 16 , 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 16 , comprising:
Ivermectin
1.00
Glycerol
4.0
Acrylate C10-30 alkyl acrylate
0.15
crosspolymer
Methyl para-hydroxybenzoate
0.2
Disodium EDTA
0.05
Citric acid monohydrate
0.05
Isopropyl myristate
4.0
Cetyl alcohol
3.0
Stearyl alcohol
2.0
Self-emulsifiable wax
0.8
Palmitostearic acid
0.5
Steareth-20
2.0
Sorbitan palmitate
1.0
Dimethicone 20
0.5
Propyl para-hydroxybenzoate
0.1
Propylene glycol
4.0
Glyceryl triacetate
1.0
Phenoxyethanol
0.5
10% sodium hydroxide
qs pH
Water
qs 100
as % by weight relative to the total weight of the composition.
24. The topically applicable, stable pharmaceutical emulsion as defined by claim 17 , 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.
25. The topically applicable, stable pharmaceutical emulsion as defined by claim 17 , 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.
26. The topically applicable, stable pharmaceutical emulsion as defined by claim 18 , 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.
27. The topically applicable, stable pharmaceutical emulsion as defined by claim 18 , 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.
28. The topically applicable, stable pharmaceutical emulsion as defined by claim 18 , further comprising glycerol, methyl para-hydroxybenzoate, disodium EDTA, citric acid monohydrate, propyl para-hydroxybenzoate and sodium hydroxide.