Pharmaceutical foam
View Patent ↗The present invention provides various pharmaceutically active topical delivery compositions. In particular, compositions of the present invention are present in a pressurized container comprising a quick-breaking alcoholic foaming agent, such that when the composition is released, i.e., dispensed, from the pressurized container, a quick-breaking temperature sensitive foam is formed. In addition, the present invention provides various aspects related to such compositions, including methods for modulating a foam characteristic, methods for improving the shelf-life of a pharmaceutically active compound, methods for the percutaneous treatment of various diseases, infections, and illnesses, and methods for evaluating foam characteristics.
1. A topical delivery composition in a pressurized container, said composition comprising:
up to 15% w/w of clindamycin phosphate;
from about 83% to about 97.9% w/w of a quick-breaking foaming agent, wherein said quick-breaking foaming agent comprises a C 1 –C 6 alcohol, a C 14 –C 22 alcohol, water, and a surfactant; and
from about 2% to about 7% w/w of an aerosol propellant selected from the group consisting of a hydrocarbon, a chlorofluorocarbon, dimethyl ether, hydrofluorocarbons and a mixture thereof,
a base; and
wherein said composition is a quick-breaking temperature sensitive foam after release from said container.
2. The composition of claim 1 , wherein the ratio of said C 1 –C 6 alcohol to water is from about 1:7 to about 1:16.
3. The composition of claim 2 , wherein the ratio of said C 1 –C 6 alcohol to water is about 1:7.
4. The composition of claim 2 , wherein the ratio of said C 1 –C 6 alcohol to water is about 1:16.
5. The composition of claim 1 , wherein the foam breaking temperature of said quick-breaking temperature sensitive foam is from about 30° C. to about 36° C.
6. The composition of claim 1 , wherein the ratio of said C 1 –C 6 alcohol to water is about 1.7:1.
7. The composition of claim 1 , wherein said surfactant is present in an amount of from about 0.1% to about 10 % w/w.
8. The composition of claim 7 , wherein said surfactant is selected from the group consisting of an ethoxylated non-ionic surfactant, an ethoxylated ionic surfactant, and a mixture thereof.
9. The composition of claim 7 , wherein said surfactant is a polysorbate.
10. The composition of claim 1 , further comprising an emollient.
11. The composition of claim 10 , wherein said emollient is a polyol.
12. The composition of claim 11 , wherein said polyol is selected from the group consisting of propylene glycol, glycerol, and a mixture thereof.
13. The composition of claim 1 , wherein the amount of said C 1 –C 6 alcohol in said quick-breaking foaming agent is from about 55% to about 65% w/w.
14. The composition of claim 13 , wherein said C 1 –C 6 alcohol is selected from the group consisting of methanol, ethanol, propanol, butanol, and a mixture thereof.
15. The composition of claim 14 , wherein said C 1 –C 6 alcohol is ethanol.
16. The composition of claim 14 , wherein said C 1 –C 6 alcohol is a mixture of ethanol and at least one other C 1 –C 6 alcohol.
17. The composition of claim 1 , wherein the amount of said C 14 –C 22 alcohol in said quick-breaking foaming agent is from about 1% to about 5% w/w.
18. The composition of claim 17 , wherein said C 14 –C 22 alcohol is a C 14 –C 20 alcohol.
19. The composition of claim 18 , wherein said C 14 –C 20 alcohol is selected from the group consisting of cetyl alcohol, stearyl alcohol, and a mixture thereof.
20. The composition of claim 19 , wherein said C 14 –C 20 alcohol is a mixture of cetyl alcohol and stearyl alcohol.
21. The composition of claim 20 , wherein the ratio of cetyl alcohol to stearyl alcohol is from about 60:40 to about 80:20.
22. The composition of claim 21 , wherein the ratio of cetyl alcohol to stearyl alcohol is about 70:30.
23. The composition of claim 1 , wherein said composition comprises water in an amount up to 90% w/w.
24. The composition of claim 1 , wherein said composition comprises water in an amount from about 30% to about 40% w/w.
25. The composition of claim 1 wherein the pH of said composition is from about pH 4.0 to about pH 9.0.
26. The composition of claim 1 wherein the pH of said composition is from about pH 4.0 to about pH 6.5.
27. The composition of claim 1 , wherein said composition comprises:
from about 0.1% to about 10% w/w of clindamycin phosphate;
from about 83% to about 97.9% w/w of a quick-breaking alcoholic foaming agent; and
from about 2% to about 7% w/w of an aerosol propellant selected from the group consisting of a hydrocarbon, a chlorofluorocarbon, and a mixture thereof.
28. A topical delivery composition in a pressurized container for the treatment of acne, said composition comprising:
up to 15% w/w of clindamycin phosphate;
from about 83% to about 97.9% w/w of a quick-breaking foaming agent, wherein said quick-breaking foaming agent comprises a C 1 –C 6 alcohol, a C 14 –C 22 alcohol, water, and a surfactant;
a base; and
from about 2% to about 7% w/w of an aerosol propellant selected from the group consisting of a hydrocarbon, a chlorofluorocarbon, dimethyl ether, hydrofluorocarbons and a mixture thereof,
wherein said composition is a quick-breaking temperature sensitive foam after release from said container.
29. The composition of claim 1 , wherein the ratio of said C 1 –C 6 alcohol to water is from about 1.5:1 to about 1:16.
30. The composition of claim 29 , wherein the ratio of said C 1 –C 6 alcohol to water is about 1.6:1.
31. A topical delivery composition in a pressurized container, said composition comprising:
up to 15% w/w of clindamycin phosphate;
from about 83% to about 97.9% w/w of a quick-breaking foaming agent, wherein said quick-breaking foaming agent comprises a C 1 –C 6 alcohol, a C 14 –C 22 alcohol, water, and a surfactant, wherein said C 1 –C 6 alcohol is selected from the group consisting of methanol, ethanol, propanoL butanol, and a mixture thereof;
a base;
from about 2% to about 7% w/w of an aerosol propellant selected from the group consisting of a hydrocarbon, a chiorofluorocarbon, dimethyl ether, hydrofluorocarbons and a mixture thereof; and
wherein said composition is a quick-breaking temperature sensitive foam after release from said container.
32. A topical delivery composition in a pressurized container for the treatment of a bacteria-mediated disease, said composition comprising:
up to 15% w/w of clindamycin phosphate;
from about 83% to about 97.9% w/w of a quick-breaking foaming agent, wherein said quick-breaking foaming agent comprises a C 1 –C 6 alcohol, a C 14 –C 22 alcohol, water, and a surfactant, wherein said surfactant is present from 0% to 10% w/w;
from about 2% to about 7% w/w of an aerosol propellant selected from the group consisting of a hydrocarbon, a chlorofluorocarbon, dimethyl ether, hydrofluorocarbons and a mixture thereof;
a base; and
wherein said composition is a quick-breaking temperature sensitive foam after release from said container.
33. A topical delivery composition in a pressurized container, said composition comprising:
up to 15% w/w of clindamycin phosphate;
from about 83% to about 97.9% w/w of a quick-breaking foaming agent, wherein said quick-breaking foaming agent comprises a C 1 –C 6 alcohol, a C 14 –C 22 alcohol, water, and a surfactant;
a base;
an aerosol propellant selected from the group consisting of a hydrocarbon, a chiorofluorocarbon, dimethyl ether, hydrofluorocarbons and a mixture thereof, wherein the maximum amount of propellant is determined by its miscibility in said composition to form a homogeneous solution; and
wherein said composition is a quick-breaking temperature sensitive foam after release from said container.
34. The composition of claims 1 , 28 , 31 , 32 or 33 , wherein said base is a member selected from the group consisting of a bicarbonate, a carbonate, an alkali hydroxide, an alkaline earth metal hydroxide, and a transition metal hydroxide.
35. The composition of claim 34 , wherein said base is potassium hydroxide.