IP Library › Granted Patent US 8,598,129

Granted Patent B2

US 8,598,129 · App. 13/851,816 · Granted Dec 3, 2013

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

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Quick Facts

Patent No.: US 8,598,129
App. No.: 13/851,816
Granted: Dec 3, 2013
Kind: B2

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USPTO Patent Center↗ Full Patent PDF↗

Abstract

Dermatological conditions/afflictions such as rosacea, common acne, seborrheic dermatitis, perioral dermatitis, acneform rashes, transient acantholytic dermatosis, and acne necrotica milliaris, 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.

Claims (338)

1. A method for the treatment of common acne, seborrheic dermatitis, perioral dermatitis, an acneform rash, transient acantholytic dermatosis 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, 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 cetostearyl alcohol, cetyl alcohol, stearyl alcohol, stearic acid, palmitostearic 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;

one or more gelling agents selected from the group consisting of carbomers, cellulose gelling agents, xanthan gums, aluminum magnesium silicates but excluding aluminum magnesium silicate/titanium dioxide/silica, guar gums, polyacrylamides and modified starches; and

water;

said emulsion being chemically stable over a period of time of 8 weeks.

2. The method as defined by claim 1 , wherein the topical pharmaceutical emulsion comprises:

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 cetostearyl alcohol, cetyl alcohol, stearyl alcohol, stearic acid, palmitostearic 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 one or more gelling agents selected from the group consisting of carbomers, cellulose gelling agents, xanthan gums, aluminum magnesium silicates but excluding aluminum magnesium silicate/titanium dioxide/silica, guar gums, polyacrylamides and modified starches; and

water;

said emulsion being chemically stable over a period of time of 8 weeks.

3. The method as defined by claim 1 , wherein the topical pharmaceutical emulsion comprises:

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;

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;

water;

said emulsion being chemically stable over a period of time of 8 weeks.

4. 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.

5. The method as defined by claim 1 , and 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.

6. A method for the treatment of common acne, seborrheic dermatitis, perioral dermatitis, an acneform rash, transient acantholytic dermatosis 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, said topical pharmaceutical composition being formulated as an emulsion, the topical pharmaceutical emulsion comprising:

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 8 weeks.

7. A method for the treatment of common acne, seborrheic dermatitis, perioral dermatitis, an acneform rash, transient acantholytic dermatosis 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, said topical pharmaceutical composition being formulated as an emulsion, the topical pharmaceutical emulsion comprising:

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;

water;

said emulsion being chemically stable over a period of time of 8 weeks.

8. The method as defined by claim 7 , wherein the topical pharmaceutical emulsion comprises:

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;

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 aluminum magnesium silicate gelling agent but excluding aluminum magnesium silicate/titanium dioxide/silica; and

water;

said emulsion being chemically stable over a period of time of 8 weeks.

9. The method as defined by claim 8 , wherein the topical pharmaceutical emulsion comprises:

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 palmitostearic acid, self-emulsifiable wax, cetyl alcohol and stearyl alcohol;

2 to 12% by weight of at least one surfactant-emulsifier selected from the group consisting of glyceryl/PEG100 stearate, sorbitan monostearate, Steareth-20 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, glyceryl triacetate, oleyl alcohol and phenoxyethanol;

0.01 to 5% by weight of aluminum magnesium silicate gelling agent but excluding aluminum magnesium silicate/titanium dioxide/silica; and

water;

said emulsion being chemically stable over a period of time of 8 weeks.

10. The method as defined by claim 9 , wherein the topical pharmaceutical emulsion comprises:

6 to 20% by weight of an oily phase comprising dimethicone, isopropyl palmitate, palmitostearic acid and self-emulsifiable wax;

2 to 12% by weight of glyceryl/PEG stearate, sorbitan monostearate and Steareth-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, glyceryl triacetate and phenoxyethanol;

0.01 to 5% by weight of aluminum magnesium silicate gelling agent but excluding aluminum magnesium silicate/titanium dioxide/silica; and

water;

said emulsion being chemically stable over a period of time of 8 weeks.

11. 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.

12. 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.

13. The method as defined by claim 8 , said topical pharmaceutical emulsion comprising:

Ivermectin

1.00

Glycerol

4.0

Aluminum magnesium silicate

1.0

Methyl para-hydroxybenzoate

0.2

Disodium EDTA

0.05

Citric acid monohydrate

0.05

Isopropyl palmitate

4.0

Glyceryl/PEG 100 stearate

3.0

Self-emulsifiable wax

2.0

Palmitostearic acid

2.5

Steareth-20

3.0

Sorbitan stearate

2.0

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.

14. The method as defined by claim 9 , said topical pharmaceutical emulsion comprising:

Ivermectin

1.00

Glycerol

4.0

Aluminum magnesium silicate

1.0

Methyl para-hydroxybenzoate

0.2

Disodium EDTA

0.05

Citric acid monohydrate

0.05

Isopropyl palmitate

4.0

Glyceryl/PEG 100 stearate

3.0

Self-emulsifiable wax

2.0

Palmitostearic acid

3.0

Steareth-20

3.0

Sorbitan stearate

2.0

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.

15. A method for the treatment of common acne, seborrheic dermatitis, perioral dermatitis, an acneform rash, transient acantholytic dermatosis 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, 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.

16. The method as defined by claim 15 , wherein said at least one surfactant-emulsifier is present in an amount of up to 15% by weight.

17. The method as defined by claim 15 , wherein said ivermectin is present in an amount of 0.1 to 5% by weight.

18. The method as defined by claim 15 , wherein said mixture of solvents and/or propenetrating agents is present in an amount of 0.1 to 20% by weight.

19. The method as defined by claim 15 , wherein said one or more gelling agents is/are present in an amount of 0.01 to 5% by weight.

20. A method for the treatment of common acne, seborrheic dermatitis, perioral dermatitis, an acneform rash, transient acantholytic dermatosis 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, 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;

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.

21. The method as defined by claim 15 , 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.

22. The method as defined by claim 15 , 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.

23. The method as defined by claim 15 , 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.

24. The method as defined by claim 15 , 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.

25. A method for the treatment of common acne, seborrheic dermatitis, perioral dermatitis, an acneform rash, transient acantholytic dermatosis 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, 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;

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.

26. The method as defined by claim 25 , wherein the topical pharmaceutical emulsion comprises:

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.

27. The method as defined by claim 25 , wherein the topical pharmaceutical emulsion comprises:

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.

28. The method as defined by claim 25 , wherein the topical pharmaceutical emulsion comprises:

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.

29. The method as defined by claim 26 , 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.

30. The method as defined by claim 26 , 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.

31. The method as defined by claim 27 , 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.

32. The method as defined by claim 27 , 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.

33. The method as defined by claim 28 , 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.

34. The method as defined by claim 28 , 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.

35. The method as defined by claim 28 , further comprising glycerol, methyl para-hydroxybenzoate, disodium EDTA, citric acid monohydrate, propyl para-hydroxybenzoate and sodium hydroxide.

36. The method as defined by claim 26 , 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.

37. A method for the treatment of common acne, seborrheic dermatitis, perioral dermatitis, an acneform rash, transient acantholytic dermatosis or acne necrotica milliaris, comprising topically applying onto the affected skin area of an individual in need of such treatment, the topical pharmaceutical emulsion which comprises:

Ivermectin

1.00

Glycerol

4.0

Acrylate C10-30 alkyl acrylate

0.2

crosspolymer

Methyl para-hydroxybenzoate

0.2

Disodium EDTA

0.05

Citric acid monohydrate

0.05

Isopropyl palmitate

4.0

Cetyl alcohol

3.5

Stearyl alcohol

2.5

Oleyl alcohol

2.0

Ceteareth-20

3.0

Sorbitan monostearate

2.0

Dimethicone 200 20 cs

0.5

Propyl para-hydroxybenzoate

0.1

Propylene glycol

2.0

Phenoxyethanol

1.0

10% sodium hydroxide

qs pH

Water

qs 100

as % by weight relative to the total weight of the emulsion.

38. A method for the treatment of common acne, seborrheic dermatitis, perioral dermatitis, an acneform rash, transient acantholytic dermatosis or acne necrotica milliaris, comprising topically applying onto the affected skin area of an individual in need of such treatment, the topical pharmaceutical emulsion which comprises:

Ivermectin

1.4

Glycerol

4.0

Acrylate C10-30 alkyl acrylate

0.2

crosspolymer

Methyl para-hydroxybenzoate

0.2

Disodium EDTA

0.05

Citric acid monohydrate

0.05

Isopropyl palmitate

4.0

Cetyl alcohol

3.5

Stearyl alcohol

2.5

Oleyl alcohol

2.0

Ceteareth-20

3.0

Sorbitan monostearate

2.0

Dimethicone 200 20 cs

0.5

Propyl para-hydroxybenzoate

0.1

Propylene glycol

2.0

Phenoxyethanol

1.0

10% sodium hydroxide

qs pH

Water

qs 100

as % by weight relative to the total weight of the emulsion.

Assignments (4)

CHANGE OF ADDRESS Recorded Jun 28, 2022

From: GALDERMA HOLDING SA

To: GALDERMA HOLDING SA

Reel/Frame 060541/0374 →

ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 26, 2021

From: MANETTA, VINCENT; WATKINS, GARY R.

To: GALDERMA S.A.

Reel/Frame 056044/0935 →

CHANGE OF NAME Recorded Apr 26, 2021

From: NESTLÉ SKIN HEALTH SA

To: GALDERMA HOLDING SA

Reel/Frame 056045/0088 →

ASSET TRANSFER AGREEMENT Recorded Apr 26, 2021

From: GALDERMA S.A.

To: NESTLÉ SKIN HEALTH SA

Reel/Frame 056048/0065 →