Claims for Patent: 10,322,186

Summary for Patent: 10,322,186

Title:	Topical tetracycline compositions
Abstract:	A topical therapeutic hydrophobic breakable composition includes a carrier comprising (a) about 60% to about 99% by weight of at least one hydrophobic oil; (b) at least one viscosity-modifying agents selected from the group consisting of a fatty alcohol, a fatty acid and a wax; and (c) a tetracycline antibiotic, characterized in that at least part of the tetracycline antibiotic is suspended in the composition; the viscosity of the composition is at least about 30% higher than the viscosity of the carrier without the tetracycline antibiotic; and is higher than the viscosity or the hydrophobic oil and the tetracycline antibiotic without the viscosity modifying agents. The tetracycline is chemically stable in the composition for at least six months; wherein more than about 90% of the tetracycline has not broken down. The composition is packaged as a breakable foam that breaks easily upon application of shear force.
Inventor(s):	Dov Tamarkin, Elana Gazal, Irakliy PAPIASHVILI, Yohan HAZOT, David Schuz, Rita KEYNAN
Assignee:	Journey Medical Corp
Application Number:	US16/235,964
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 10,322,186
Patent Claims:	1. A method of treating rosacea, comprising administering a waterless foam composition comprising a minocycline and a foamable carrier, the carrier comprising: a) at least one hydrophobic oil; and b) an agent comprising (i) at least one fatty alcohol and at least one wax; (ii) at least one fatty acid and at least one wax; (iii) at least one fatty alcohol, at least one fatty acid, and at least one wax; (iv) a wax comprising a hydrogenated oil; or (v) a combination of two or more waxes; wherein the composition does not contain one or more minocycline incompatible substance selected from the group consisting of dimethyl sulfoxide (DMSO), dimethylformamide (DMF), acetonitrile, acetone, methyl ethyl ketone, 1,4-dioxane, tetrahydrofuran (THF), N-methylpyrrolidone, pyridine, piperidine, N-methyl-2-pyrrolidone and 1-methyl-2-pyrrolidinone), azone (1-dodecylazacycloheptan-2-one), dimethyl isosorbide, glycerin, ethanol, propylene glycol, butylene glycol, PEG 200, hexylene glycol, PEG 400, diethylene glycol monoethyl ether, pomegranate seed oil, isostearic acid, and ethylcellulose; wherein the composition does not contain a surfactant; and wherein the composition does not contain a polyol. 2. The method of claim 1, wherein the at least one hydrophobic oil comprises a mineral oil, a cocoglyceride, a silicone oil, a liquid paraffin, a caprylic/capric triglyceride, a coconut oil, a soybean oil, a cyclomethicone, disopropyl adipate isododecane, cetearyl octanoate, a gelled mineral oil, isopropyl myristate, PPG 15 stearyl ether, octyl dodecanol, a petrolatum, a calendula oil, a grape seed oil, an almond oil, a jojoba oil, an avocado oil, a peanut oil, a wheat germ oil, or a mixture of any two or more thereof. 3. The method of claim 1, wherein at least one or both of the fatty alcohol and the fatty acid has at least 12 carbon atoms in its carbon backbone. 4. The method of claim 1, wherein the agent comprises at least one fatty alcohol, at least one fatty acid, and at least one wax, wherein the at least one wax comprises a beeswax, a hydrogenated oil, or both. 5. The method of claim 1, wherein the composition contains less than 0.4% by weight of a protic solvent, a polar aprotic solvent, and a silicone thickening agent, or wherein the composition contains less than 0.4% by weight of a polymeric gelling agent, a short chain alcohol, and a silicone thickening agent. 6. The method of claim 1, wherein the minocycline is minocycline hydrochloride. 7. The method of claim 1, wherein the foamable carrier comprises: a) 45% to 55% by weight of a soybean oil; b) 21.2% to 26% by weight of a coconut oil; c) 4.5% to 5.5% by weight of a cyclomethicone; d) 0.85% to 4.8% by weight of a light mineral oil; e) 3.2% to 3.9% by weight of cetostearyl alcohol; f) 2.7% to 3.3% by weight of stearic acid; g) 2.3% to 2.8% by weight of myristyl alcohol; h) 1.8% to 2.2% by weight of hydrogenated castor oil; i) 1.8% to 2.2% by weight of beeswax; j) 1.4% to 1.7% by weight of stearyl alcohol; and k) 1% to 1.2% by weight of behenyl alcohol. 8. The method of claim 1, wherein the minocycline is present at about 1% to about 10% of the composition. 9. The method of claim 1, wherein the minocycline is present at about 1.5% or about 3% of the composition. 10. The method of claim 1, wherein the composition is free of or comprises less than 10% petrolatum by weight of the composition. 11. The method of claim 1, wherein the at least one hydrophobic oil is about 60% to about 99% by weight of the composition. 12. The method of claim 1, wherein the composition is administered at least once daily. 13. The method of claim 1, wherein the composition is administered at least once daily and the minocycline is present at about 1.5% or about 3% of the composition. 14. The method of claim 1, wherein the foam composition is produced with a liquefied or compressed gas propellant. 15. The method of claim 1, wherein the at least one hydrophobic oil comprises a hydrocarbon oil, an ester oil, an ester of a dicarboxylic acid, a triglyceride oil, an unsaturated or polyunsaturated oil, an essential oil, a canola oil, a castor oil, a corn oil, a cotton oil, a cottonseed oil, glycerol, an olive oil, a palm oil, a dimethicone, a fatty acid-modified silicone oil, or a mixture of any two or more thereof. 16. A method of treating rosacea, comprising administering a waterless composition comprising a carrier and 1% to 10% by weight of the composition of a minocycline, wherein the carrier comprises: a) at least one hydrophobic oil; and b) an agent comprising (i) at least one fatty alcohol and at least one wax; (ii) at least one fatty acid and at least one wax; (iii) at least one fatty alcohol, at least one fatty acid, and at least one wax; (iv) a wax comprising a hydrogenated oil; or (v) a combination of two or more waxes; wherein the composition does not contain a surfactant; and wherein the composition does not contain a polyol. 17. The method of claim 16, wherein the minocycline is minocycline hydrochloride and is present at an amount of about 1.5% or about 3% by weight of the composition. 18. The method of claim 16, wherein the agent comprises at least one fatty alcohol, at least one fatty acid, and at least one wax. 19. The method of claim 16, wherein the composition is a foam composition, and wherein the foam composition is produced upon addition of a liquefied or compressed gas propellant to the carrier. 20. The method of claim 16, wherein the carrier comprises: a) 45% to 55% by weight of a soybean oil; b) 21.2% to 26% by weight of a coconut oil; c) 4.5% to 5.5% by weight of a cyclomethicone; d) 0.85% to 4.8% by weight of a light mineral oil; e) 3.2% to 3.9% by weight of cetostearyl alcohol; f) 2.7% to 3.3% by weight of stearic acid; g) 2.3% to 2.8% by weight of myristyl alcohol; h) 1.8% to 2.2% by weight of hydrogenated castor oil; i) 1.8% to 2.2% by weight of beeswax; j) 1.4% to 1.7% by weight of stearyl alcohol; and k) 1% to 1.2% by weight of behenyl alcohol. 21. A method of treating rosacea, comprising administering a foam produced from a foamable composition comprising a carrier and a liquified or compressed gas propellant, the carrier comprising: a) a tetracycline antibiotic; b) a combination of two or more hydrophobic oils, wherein at least one of the hydrophobic oils is a light mineral oil and the other hydrophobic oil comprises a heavy mineral oil, soybean oil, and/or coconut oil; and c) a combination of two or more fatty alcohols, wherein at least one of the fatty alcohols is stearyl alcohol; wherein the hydrophobic oils are present at between about 70% and 95% by weight of the carrier; and wherein the ratio of the carrier to the propellant is between about 100:1 and about 100:25. 22. The method of claim 21, wherein the foamable composition further comprises stearic acid, wherein the ratio of the fatty alcohols to stearic acid is between about 4:1 and 1:4. 23. The method of claim 21, wherein the tetracycline antibiotic comprises minocycline. 24. The method of claim 23, wherein the minocycline is present at about 1.5% to about 3% by weight of the carrier. 25. The method of claim 21, wherein the carrier further comprises at least one wax, wherein the wax is selected from the group consisting of a beeswax, a hydrogenated castor oil, a paraffin 58-62° C. wax, a paraffin 51-53° C. wax, a paraffin 42-44° C. wax, and a mixture of two or more thereof. 26. The method of claim 25, wherein the fatty alcohols and the wax are present at a ratio between about 4:1 and 3:2. 27. The method of claim 21, wherein the combination of the hydrophobic oils comprises a light mineral oil, a soybean oil, a coconut oil, and cyclomethicone. 28. The method of claim 21, wherein the combination of the fatty alcohols comprises stearyl alcohol, cetostearyl alcohol, behenyl alcohol, and myristyl alcohol. 29. A method of treating rosacea, comprising administering a foam produced from a foamable composition comprising a carrier and a liquified or compressed gas propellant, the carrier comprising: a) a minocycline; b) a combination of two or more hydrophobic oils, wherein at least one of the hydrophobic oils is a light mineral oil and the other hydrophobic oil comprises a heavy mineral oil, soybean oil, and/or coconut oil; c) a combination of two or more fatty alcohols, wherein at least one of the fatty alcohols is stearyl alcohol; and d) at least one wax; wherein the hydrophobic oils are present at between about 70% and 95% by weight of the carrier; wherein the fatty alcohols and the wax are present at a ratio between about 4:1 and 3:2; and wherein the ratio of the carrier to the propellant is between about 100:1 and about 10025. 30. The method of claim 29, wherein the carrier further comprises a stearic acid and wherein the ratio of the fatty alcohols to stearic acid is between about 4:1 and 1:4.