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Claims for Patent: 8,277,780

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Claims for Patent: 8,277,780

Title:Stable liquid desoximethasone compositions with reduced oxidized impurity
Abstract: The present invention relates to a stable liquid formulation comprising desoximetasone, isopropyl myristate, a C.sub.2-C.sub.4 alcohol and a stabilizing agent. Specifically, the present invention provides a liquid formulation comprising: a) about 0.01 wt % to about 2.5 wt % desoximetasone; b) about 10 wt % to about 70 wt % isopropyl myristate; c) about 20 wt % to about 70 wt % C.sub.2-C.sub.4 alcohol; and d) a stabilizing agent selected from the group consisting of an oleaginous vehicle and a propellant, wherein the stabilizing agent is in an amount sufficient to reduce the formation of less than about 1 wt % 17-carboxy-9.alpha.-fluoro-11.beta.-hydroxy-16a-methyl-androsta-1,4-diene- -3-one under an accelerated storage condition.
Inventor(s): Rao; Srinivasa (Valley Stream, NY), Dixit; Suresh (Fort Worth, TX), Yacobi; Avraham (Englewood, NJ), Bailey; Arthur (Bethel, CT)
Assignee: Taro Pharmaceutical North America, Inc. (Grand Cayman, KY)
Application Number:11/921,106
Patent Claims: 1. A liquid formulation comprising: a) about 0.01 wt % to about 2.5 wt % desoximetasone; b) about 10 wt % to about 70 wt % isopropyl myristate; c) about 20 wt % to about 70 Wt % C.sub.2-C.sub.4 alcohol; and d) a stabilizing agent comprising a mixture of (a) an oleaginous vehicle selected from the group consisting of mineral oil and light mineral oil present in the amount of about 10 wt % to about 60 wt % and (b) a skin conditioning agent selected from one or more of the group consisting of (i) a C.sub.15-C.sub.25 fatty alcohol present in the amount of about 0.5 wt % to about 10 wt % and (ii) an ester of glycerin and a C.sub.15-C.sub.25 fatty acid present in the amount of about 0.5 wt % to about 10 wt %.

2. The liquid formulation of claim 1, wherein the desoximetasone is present in the amount of about 0.1 wt % to about 1 wt %.

3. The liquid formulation of claim 1, wherein the desoximetasone is present in the amount of about 0.25 wt %.

4. The liquid formulation of claim 1, wherein the isopropyl myristate is present in the amount of about 25 wt % to about 55 wt %.

5. The liquid formulation of claim 1, wherein the isopropyl myristate is present in the amount of about 31.35 wt %.

6. The liquid formulation of claim 1, wherein the C.sub.2-C.sub.4 alcohol is ethyl alcohol.

7. The liquid formulation of claim 1, wherein the C.sub.2-C.sub.4 alcohol is isopropanol.

8. The liquid formulation of claim 1, wherein the C.sub.2-C.sub.4 alcohol is present in the amount of about 20 wt % to about 40 wt %.

9. The liquid formulation of claim 1, wherein the C.sub.2-C.sub.4 alcohol is present in the amount of about 23.4 wt %.

10. The liquid formulation of claim 1, wherein the oleaginous vehicle is mineral oil.

11. The liquid formulation of claim 1, wherein the oleaginous vehicle is present in the amount of about 20 wt % to about 50 wt %.

12. The liquid formulation of claim 1, wherein the oleaginous vehicle is present in the amount of about 40 wt %.

13. The liquid formulation of claim 1, wherein the skin conditioning agent comprises a ester of a glycerin and a C.sub.15-C.sub.25 fatty acid.

14. The liquid formulation of claim 13, wherein the ester is a monoester.

15. The liquid formulation of claim 13, wherein the C.sub.15-C.sub.25 fatty acid is oleic acid.

16. The liquid formulation of claim 13, wherein the ester is glyceryl oleate.

17. The liquid formulation of claim 13, wherein the ester is present in the amount of about 1 wt % to about 8 wt %.

18. The liquid formulation of claim 13, wherein the ester is present in the amount of about 0.9 wt %.

19. The liquid formulation of claim 1, wherein the skin conditioning agent comprises a C.sub.15-C.sub.25 fatty alcohol.

20. The liquid formulation of claim 19, wherein the C.sub.15-C.sub.25 fatty alcohol is selected from the group consisting of lauryl alcohol, myristyl alcohol, palmityl alcohol, stearyl alcohol, linoleyl alcohol, and oleyl alcohol.

21. The liquid formulation of claim 19, wherein the C.sub.15-C.sub.25 fatty alcohol is oleyl alcohol.

22. The liquid formulation of claim 19, wherein the C.sub.15-C.sub.25 fatty alcohol is present in the amount of about 1 wt % to about 8 wt %.

23. The liquid formulation of claim 19, wherein the C.sub.15-C.sub.25 fatty alcohol is present in the amount of about 5 wt %.

24. The liquid formulation of claim 1, further comprising a propellant selected from the group consisting of 1,1,1,2-tetrafluoroethane, 1,1,1,2,3,3,3-heptafluoropropane, butane, isobutane, propane, and dimethyl ether.

25. The liquid formulation of claim 24, wherein the propellant is 1,1,1,2-tetrafluoroethane.

26. The liquid formulation of claim 24, wherein the propellant is present in the amount of about 20 wt % to about 95 wt %.

27. The liquid formulation of claim 24, wherein the propellant is present in the amount of about 40 wt % to about 80 wt %.

28. The liquid formulation of claim 24, wherein the propellant is present in the amount of about 20 wt % to about 75 wt %.

29. The liquid formulation of claim 1, further comprising a surfactant.

30. The liquid formulation of claim 29, wherein the surfactant selected from the group consisting of sodium lauryl sulfate, and polysorbate 80.

31. The liquid formulation of claim 29, wherein the surfactant is present in the amount of about 0.5 wt % to about 5 wt %.

32. The liquid formulation of claim 1, further comprising water.

33. The liquid formulation of claim 32, wherein the water is present in the amount of about 1 wt % to about 10 wt %.

34. The liquid formulation of claim 1, wherein the liquid formulation comprises less than about 1 wt % 17-carboxy-9.alpha.-fluoro-11.beta.-hydroxy-16.alpha.-methyl-androsta-1,4- -diene-3-one after storage at 50.degree. C., for 4 weeks.

35. A dosage form comprising the liquid formulation of claim 1, and further comprising a pump delivery system.

36. A dosage form comprising the liquid formulation of claim 1, and further comprising an aerosolized delivery system.

37. The dosage form of claim 36, wherein the aerosolized delivery system comprises a can equipped with a continuous valve.

38. The dosage form of claim 36, wherein the aerosolized delivery system comprises a can equipped with a metered-dosed valve.

39. The liquid formulation of claim 1, wherein the liquid formulation is a foam.

40. The liquid formulation of claim 39, wherein the foam is a quick-break foam.

41. A method of treating a corticosteroid responsive dermatosis in a mammal comprising the step of topical administering to the mammal the aerosolized formulation of claim 1.

42. The method of claim 41, wherein the corticosteroid responsive dermatosis is selected from the group consisting of plaque psoriasis, and atopic dermatitis.

43. A process for preparing a liquid formulation of claim 1 comprising: a) mixing desoximetasone in a C.sub.2-C.sub.4 alcohol to from a mixture; b) adding isopropyl myristate in the mixture; and c) adding stabilizing agent comprising a mixture of (a) an oleaginous vehicle selected from the group consisting of mineral oil and light mineral oil present in the amount of about 10 wt % to about 60 wt % and (b) a skin conditioning agent selected from one or more of the group consisting of (i) a C.sub.15-C.sub.25 fatty alcohol present in the amount of about 0.5 wt % to about 10 wt % and (ii) an ester of glycerin and a C.sub.15-C.sub.25 fatty acid present in the amount of about 0.5 wt % to about 10 wt %.

44. A process for preparing an aerosolized formulation of desoximetasone comprising the step of filling an aerosol formulation into a container equipped with a continuous valve, said aerosol formulation comprising: a) about 0.01 wt % to about 2.5 wt % desoximetasone; b) about 10 wt % to about 70 wt % isopropyl myristate; c) about 20 wt % to about 70 wt % C.sub.2-C.sub.4 alcohol; and d) a stabilizing agent comprising a mixture of (a) an oleaginous vehicle selected from the group consisting of mineral oil and light mineral oil present in the amount of about 10 wt % to about 60 wt % and (b) a skin conditioning agent selected from one or more of the group consisting of (i) a C.sub.15-C.sub.25 fatty alcohol present in the amount of about 0.5 wt % to about 10 wt % and (ii) an ester of glycerin and a C.sub.15-C.sub.25 fatty acid present in the amount of about 0.5 wt % to about 10 wt %.

45. The liquid formulation of claim 1, wherein the stabilizing agent is a mixture of mineral oil and glyceryl oleate.

46. The liquid formulation of claim 1, wherein the stabilizing agent reduces the formation of 17-carboxy-9.alpha.-fluoro-11.beta.-hydroxy-16.alpha.-methyl-androsta-1,4- -diene-3-one after storage at 40.degree. C., 75% relative humidity for 3 months to less than about 1 wt %.
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