Details for Patent: 9,433,680

Title:	Topical compositions and methods for making and using same
Abstract:	The present invention relates to improved topical gel compositions comprising an active agent, and uses thereof.
Inventor(s):	Hardas; Bhushan (Summerville, NC), Dalton; Donna (High Point, NC), Scheppler; Petra (Mainz, DE), Hensche; Anja (Eschborn, DE), Boderke; Peter (Schwalbach, DE)
Assignee:	MERZ PHARMACEUTICALS, LLC (Raleigh, NC)
Filing Date:	Jul 12, 2013
Application Number:	13/941,201
Claims:	1. A gel composition comprising from about 0.01 wt % to about 0.5 wt % fluticasone, or a pharmaceutically acceptable salt or ester thereof, from about 15 wt % to about 25 wt % of a glycol solvent, from about 0.75 wt % to about 2.25 wt % of a hydroxyl cellulose, from about 1 wt % to less than about 10 wt % of a polysorbate solubilizing agent, from about 1 wt % to less than about 10 wt % of a second solubilizing agent, optionally a third solubilizing agent, and optionally one or more of: a diluent, a pH adjuster, a chelating agent, a preservative, a fragrance, and a coloring agent; wherein the gel composition contains no alkyl alcohol, and wherein the composition contains no active agent in addition to the fluticasone, or a pharmaceutically acceptable salt thereof. 2. The gel composition of claim 1, comprising from about 0.01 wt % to about 0.1 wt % fluticasone, or a pharmaceutically acceptable salt or ester thereof, from about 15 wt % to about 25 wt % of a glycol solvent, from about 0.75 wt % to about 2.25 wt % of a hydroxy cellulose, from about 3 wt % to about 8 wt % of a polysorbate solubilizing agent, from about 1 wt % to less than about 10 wt % of a second solubilizing agent, optionally a third solubilizing agent, and optionally one or more of: a diluent, a pH adjuster, a chelating agent, a preservative, a fragrance, and a coloring agent. 3. The gel composition of claim 1, comprising from about 0.01 wt % to about 0.1 wt % fluticasone, or a pharmaceutically acceptable salt or ester thereof, from about 15 wt % to about 25 wt % propylene glycol, from about 0.75 wt % to about 2.25 wt % hydroxyethyl cellulose, from about 3 wt % to about 8 wt % Polysorbate 20, from about 1 wt % to less than about 10 wt % of a second solubilizing agent, optionally a third solubilizing agent, and optionally one or more of: a diluent, a pH adjuster, a chelating agent, a preservative, a fragrance, and a coloring agent. 4. The gel composition of claim 1, comprising from about 0.01 wt % to about 0.1 wt % fluticasone, or a pharmaceutically acceptable salt or ester thereof, from about 15 wt % to about 25 wt % propylene glycol, from about 1.5 wt % to about 2.0 wt % hydroxyethyl cellulose, from about 3 wt % to about 8 wt % Polysorbate 20, from about 1 wt % to less than about 10 wt % of a second solubilizing agent selected from an alcohol or glycol ether solubilizing agent, optionally from about 1 wt % to less than about 10 wt % of a third solubilizing agent, and optionally one or more of: a diluent, a pH adjuster, a chelating agent, a preservative, a fragrance, and a coloring agent. 5. The gel composition of claim 1, wherein the fluticasone or a pharmaceutically acceptable salt or ester thereof is present in an amount of from about 0.01 wt % to about 0.1 wt %. 6. The gel composition of claim 1, wherein the glycol solvent is present in an amount of about 18 wt % to about 22 wt %. 7. The gel composition of claim 6, wherein the glycol solvent is propylene glycol. 8. The gel composition of claim 1, wherein the hydroxy cellulose is present in an amount of from about 1.5 wt % to about 2.0 wt %. 9. The gel composition of claim 1, wherein the hydroxy cellulose is hydroxyethyl cellulose. 10. The gel composition of claim 1, wherein the polysorbate solubilizing agent is present in an amount of from about 3 wt % to about 8 wt %. 11. The gel composition of claim 1, wherein the polysorbate solubilizing agent is Polysorbate 20. 12. The gel composition of claim 1, wherein the polysorbate solubilizing agent is Polysorbate 80. 13. The gel composition of claim 1, wherein the fluticasone, or pharmaceutically acceptable salt or ester thereof, is fluticasone propionate. 14. The gel composition of claim 1, wherein the preservative is benzyl alcohol. 15. The gel composition of claim 14, wherein the benzyl alcohol is present in an amount of about 1.0 wt %. 16. The gel composition of claim 1, comprising from about 0.01 wt % to about 0.075 wt % fluticasone, or a pharmaceutically acceptable salt or ester thereof, from about 15 wt % to about 25 wt % propylene glycol, from about 1.5 wt % to about 2.0 wt % hydroxyethyl cellulose, from about 3 wt % to about 8 wt % Polysorbate 20, from about 1 wt % to less than about 10 wt % of a second solubilizing agent selected from an alcohol or glycol ether solubilizing agent, optionally from about 1 wt % to less than about 10 wt % of a third solubilizing agent selected from an alcohol or glycol ether solubilizing agent, and optionally one or more of: a diluent, a pH adjuster, a chelating agent, a preservative, a fragrance, and a coloring agent. 17. The gel composition of claim 16, wherein the second solubilizing agent is a glycol ether solubilizing agent. 18. The gel composition of claim 17, wherein the second solubilizing agent is diethylene glycol monoethylether. 19. The gel composition of claim 18, wherein the diethylene glycol monoethylether is present in an amount of about 1 wt % to about 3 wt %. 20. The gel composition of claim 19, wherein the fluticasone or pharmaceutically acceptable salt or ester thereof is fluticasone propionate. 21. The gel composition of claim 20, wherein the preservative is benzyl alcohol. 22. The gel composition of claim 21, wherein the benzyl alcohol is present in an amount of about 1.0 wt %. 23. The gel composition of claim 1, comprising about 0.025 wt % fluticasone, or a pharmaceutically acceptable salt or ester thereof, about 20 wt % propylene glycol, about 1.5 wt % to about 2.0 wt % hydroxyethyl cellulose, from about 3 wt % to about 8 wt % Polysorbate 20, from about 1 wt % to about 3 wt % of a glycol ether solubilizing agent, and optionally one or more of: a diluent, a pH adjuster, a chelating agent, a preservative, a fragrance, and a coloring agent. 24. The gel composition of claim 1, comprising about 0.025 wt % fluticasone, or a pharmaceutically acceptable salt or ester thereof, about 20 wt % propylene glycol, about 1.75 wt % hydroxyethyl cellulose, about 5 wt % Polysorbate 20, about 1.5 wt % diethylene glycol monoethylether, water, 0.02 wt % ethylenediaminetetracetic acid (EDTA) or a salt thereof, and optionally a preservative, a pH adjuster, a fragrance, and a coloring agent. 25. The gel composition of claim 24, wherein the fluticasone or pharmaceutically acceptable salt or ester thereof is fluticasone propionate. 26. The gel composition of claim 25, wherein the preservative is benzyl alcohol. 27. The gel composition of claim 26, wherein the benzyl alcohol is present in an amount of about 1.0 wt %.