Topical application of ivermectin for the treatment of dermatological conditions/afflictions
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 topically applicable, stable pharmaceutical emulsion, comprising, by weight relative to the total weight of the emulsion:
1% of ivermectin;
6 to 20% of an oily phase comprising fatty substances;
2 to 12% of at least one surfactant-emulsifier selected from polyoxyethylenated fatty acid esters and sorbitan esters;
0.1 to 20% of a mixture of solvents and/or propenetrating agents for the ivermectin selected from propylene glycol, ethanol, isopropanol, butanol, N-methyl-2-pyrrolidone, DMSO, polysorbate 80, phenoxyethanol, glyceryl triacetate, and oleyl alcohol;
0.01 to 5% of one or more gelling agents, but excluding aluminum magnesium silicate/titanium dioxide/silica; and
30% to 95% of water;
wherein the ivermectin is chemically stable in the emulsion over a period of 8 weeks.
2. The emulsion as defined by claim 1 , wherein the oily phase comprises dimethicone, cyclomethicone, isopropyl palmitate, isopropyl myristate, or mixtures thereof.
3. The emulsion as defined by claim 2 , wherein the fatty substances are selected from cetostearyl alcohol, cetyl alcohol, stearyl alcohol, stearic acid, palmitostearic acid, and a self-emulsifiable wax.
4. The emulsion as defined by claim 1 , wherein the sorbitan esters are selected from sorbitan monostearate, sorbitan palmitate, sorbitan oleate, sorbitan sesquioleate, and sorbitan isostearate; and the polyoxyethylenated fatty acid esters are selected from steareth-20, steareth-2, steareth-21, and ceteareth-20.
5. The emulsion as defined by claim 4 , wherein the at least one surfactant-emulsifier is present in an amount of from 2% to 6% by weight relative to the total weight of the emulsion.
6. The emulsion as defined by claim 1 , wherein the one or more gelling agents are selected from carbomers, cellulose derivatives, xanthan gums, guar gums, polyacrylamides, modified starches, and aluminum magnesium silicates.
7. The emulsion as defined by claim 6 , wherein the one or more gelling agents are present in the emulsion in an amount of from 0.1% to 3% by weight relative to the total weight of the emulsion.
8. The emulsion as defined by claim 1 , wherein the emulsion is chemically stable over a period of 12 weeks.
9. The emulsion as defined by claim 1 , wherein the mixture of solvents and/or propenetrating agents are present in an amount of from 1% to 10% by weight relative to the total weight of the emulsion.
10. The emulsion as defined by claim 1 , wherein the ivermectin is chemically stable in the emulsion over a period of two months at a pH of about 4.
11. The emulsion as defined by claim 1 , wherein the ivermectin is chemically stable in the emulsion over a period of two months at a pH of about 5.
12. The emulsion as defined by claim 1 , wherein the ivermectin is chemically stable in the emulsion over a period of two months at a pH of about 6.
13. The emulsion as defined by claim 1 , wherein the water is from 60% to 80% by weight relative to the total weight of the emulsion.
14. The emulsion as defined by claim 1 , wherein the emulsion has lamellar layers of liquid crystals.
15. A topically applicable, stable pharmaceutical emulsion, comprising, by weight relative to the total weight of the emulsion:
0.001% to 1.4% of ivermectin;
6 to 20% of an oily phase comprising fatty substances;
2 to 12% of at least one surfactant-emulsifier selected from polyoxyethylenated fatty acid esters and sorbitan esters;
0.1 to 20% of a mixture of solvents and/or propenetrating agents for the ivermectin selected from propylene glycol, ethanol, isopropanol, butanol, N-methyl-2-pyrrolidone, DMSO, polysorbate 80, phenoxyethanol, glyceryl triacetate, and oleyl alcohol;
0.01 to 5% of one or more gelling agents, but excluding aluminum magnesium silicate/titanium dioxide/silica; and
30% to 95% of water;
wherein the ivermectin is chemically stable in the emulsion over a period of 8 weeks.
16. The emulsion as defined by claim 15 , wherein the oily phase comprises dimethicone, cyclomethicone, isopropyl palmitate, isopropyl myristate, or mixtures thereof.
17. The emulsion as defined by claim 16 , wherein the fatty substance is selected from cetostearyl alcohol, cetyl alcohol, stearyl alcohol, stearic acid, palmitostearic acid, and a self-emulsifiable wax.
18. The emulsion as defined by claim 15 , wherein the sorbitan esters are selected from sorbitan monostearate, sorbitan palmitate, sorbitan oleate, sorbitan sesquioleate, and sorbitan isostearate; and the polyoxyethylenated fatty acid esters are selected from steareth-20, steareth-2, steareth-21, and ceteareth-20.
19. The emulsion as defined by claim 18 , wherein the at least one surfactant-emulsifier is present in an amount of from 2% to 6% by weight relative to the total weight of the emulsion.
20. The emulsion as defined by claim 15 , wherein the one or more gelling agents are selected from carbomers, cellulose derivatives, xanthan gums, guar gums, polyacrylamides, modified starches, and aluminum magnesium silicates.
21. The emulsion as defined by claim 20 , wherein the one or more gelling agents is present in the emulsion in an amount of from 0.01% to 5% 0.1% to 3% by weight relative to the total weight of the emulsion.
22. The emulsion as defined by claim 15 , wherein the emulsion is chemically stable over a period of 12 weeks.
23. The emulsion as defined by claim 15 , wherein the mixture of solvent and/or propenetrating agent is present in an amount of from 1% to 10% by weight relative to the total weight of the emulsion.
24. The emulsion as defined by claim 15 , wherein the ivermectin is chemically stable in the emulsion over a period of two months at a pH of about 4.
25. The emulsion as defined by claim 15 , wherein the ivermectin is chemically stable in the emulsion over a period of two months at a pH of about 5.
26. The emulsion as defined by claim 15 , wherein the ivermectin is chemically stable in the emulsion over a period of two months at a pH of about 6.
27. The emulsion as defined by claim 15 , wherein the water is from 60% to 80% by weight relative to the total weight of the emulsion.
28. The emulsion as defined by claim 15 , wherein the emulsion has lamellar layers of liquid crystals.
29. A topically applicable, stable pharmaceutical emulsion, comprising, by weight relative to the total weight of the emulsion:
1% of ivermectin;
6 to 20% of an oily phase comprising fatty substances;
2 to 12 at least one surfactant-emulsifier selected from polyoxyethylenated fatty acid esters and sorbitan esters;
0.1 to 20% of at least two of the following solvents and/or propenetrating agents for the ivermectin: propylene glycol, ethanol, isopropanol, butanol, N-methyl-2-pyrrolidone, DMSO, polysorbate 80, phenoxyethanol, glyceryl triacetate, and oleyl alcohol;
0.01 to 5% of one or more gelling agents, but excluding aluminum magnesium silicate/titanium dioxide/silica; and
30% to 95% of water;
wherein the ivermectin is chemically stable in the emulsion over a period of 8 weeks.
30. The emulsion as defined by claim 29 , wherein the oily phase comprises dimethicone, cyclomethicone, isopropyl palmitate, isopropyl myristate, or mixtures thereof.
31. The emulsion as defined by claim 28 , wherein the fatty substances are selected from cetostearyl alcohol, cetyl alcohol, stearyl alcohol, stearic acid, palmitostearic acid, and a self-emulsifiable wax.
32. The emulsion as defined by claim 29 , wherein the sorbitan esters are selected from sorbitan monostearate, sorbitan palmitate, sorbitan oleate, sorbitan sesquioleate, and sorbitan isostearate; and the polyoxyethylenated fatty acid esters are selected from steareth-20, steareth-2, steareth-21, and ceteareth-20.
33. A topically applicable, stable pharmaceutical emulsion, comprising, by weight relative to the total weight of the emulsion:
0.001% to 1.4% of ivermectin;
6 to 20% of an oily phase comprising fatty substances;
2 to 12% of at least one surfactant-emulsifier selected from polyoxyethylenated fatty acid esters and sorbitan esters;
0.1 to 20% of at least two of the following solvents and/or propenetrating agents for the ivermectin: propylene glycol, ethanol, isopropanol, butanol, N-methyl-2-pyrrolidone, DMSO, polysorbate 80, phenoxyethanol, glyceryl triacetate, and oleyl alcohol;
0.01 to 5% of one or more gelling agents, but excluding aluminum magnesium silicate/titanium dioxide/silica; and
30% to 95% of water;
wherein the ivermectin is chemically stable in the emulsion over a period of 8 weeks.
34. The emulsion as defined by claim 33 , wherein the oily phase comprises dimethicone, cyclomethicone, isopropyl palmitate, isopropyl myristate, or mixtures thereof.
35. The emulsion as defined by claim 34 , wherein the fatty substances are selected from cetostearyl alcohol, cetyl alcohol, stearyl alcohol, stearic acid, palmitostearic acid, and a self-emulsifiable wax.
36. The emulsion as defined by claim 33 , wherein the sorbitan esters are selected from sorbitan monostearate, sorbitan palmitate, sorbitan oleate, sorbitan sesquioleate, and sorbitan isostearate; and the polyoxyethylenated fatty acid esters are selected from steareth-20, steareth-2, steareth-21, and ceteareth-20.