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Last Updated: December 7, 2021

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Claims for Patent: 10,130,640


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Summary for Patent: 10,130,640
Title:Pharmaceutical spray composition comprising a vitamin D analogue and a corticosteroid
Abstract: The present invention relates to a topical spray composition comprising a biologically active vitamin D derivative or analog and a corticosteroid, and its use in the treatment of dermal diseases and conditions.
Inventor(s): Lind; Marianne (Bagsv.ae butted.rd, DK), Rasmussen; Gritt (Virum, DK), Sonne; Mette Rydahl (Brondby Strand, DK), Hansen; Jens (Virum, DK), Petersson; Karsten (Ballerup, DK)
Assignee: Leo Pharma A/S (Ballerup, DK)
Application Number:14/707,733
Patent Claims: 1. A sprayable, storage stable, substantially anhydrous topical composition comprising a therapeutically effective amount of calcipotriol or calcipotriol monohydrate and a therapeutically effective amount of betamethasone dipropionate, wherein the calcipotriol or calcipotriol monohydrate and the betamethasone dipropionate are dissolved in a pharmaceutically acceptable propellant comprising at least one of dimethyl ether or methylethyl ether, or propellant mixture comprising a first propellant comprising at least one of dimethyl ether or methylethyl ether and a second propellant comprising at least one of a C.sub.3-5 alkane, hydrofluoroalkane, hydrochloroalkane, fluoroalkane or chlorofluoroalkane, the composition further comprises a pharmaceutically acceptable lipid carrier solubilized or suspended in said propellant or propellant mixture, the lipid carrier comprises one or more paraffins wherein said lipid carrier upon application on skin and evaporation of the propellant or propellant mixture forms a semi-solid and occlusive layer at the site of application, the composition optionally comprises non-evaporating oily co-solvent, and wherein a supersaturated solution of the calcipotriol or calcipotriol monohydrate and the betamethasone dipropionate is formed on the skin after application of the composition and evaporation of the propellant or propellant mixture.

2. The composition according to claim 1, wherein the propellant is present in an amount from 45-95% w/w.

3. The composition according to claim 2, wherein the propellant is present in an amount from 50-90% w/w.

4. The composition according to claim 3, wherein the propellant is present in an amount from 55-70% w/w.

5. The composition according to claim 1, wherein the propellant is a mixture of dimethylether and C.sub.3-5 alkane.

6. The composition according to claim 5, wherein the C.sub.3-5 alkane is n-propane, isopropane, n-butane and/or isobutane.

7. The composition according to claim 6, wherein the C.sub.3-5 alkane is n-butane and/or isobutane.

8. The composition according to claim 7, wherein the C.sub.3-5 alkane is n-butane.

9. The composition according to claim 7, wherein the ratio of n-butane and/or isobutane to dimethyl ether is in the range of 6:1-0:1 v/v.

10. The composition of claim 7, wherein the ratio of n-butane and/or isobutane to dimethyl ether is in the range of 5:1-1:2 v/v.

11. The composition of claim 7, wherein the ratio of n-butane and/or isobutane to dimethyl ether is in the range of 4:1-1:1 v/v.

12. The composition of claim 7, wherein the ratio of n-butane and/or isobutane to dimethyl ether is in the range of 4:2-4:3 v/v.

13. The composition of claim 7, wherein the ratio of n-butane and/or isobutane to dimethyl ether is in the range of 4:3-1:1 v/v.

14. A composition according to claim 1, comprising (a) about 0.00001-0.05% w/w calcipotriol or calcipotriol monohydrate, (b) about 0.0005-1% w/w betamethasone dipropionate, (c) about 5-55% w/w of the lipid carrier, and (d) about 45-95% w/w of the propellant.

15. The composition according to claim 1, wherein the amount of calcipotriol or calcipotriol monohydrate is 0.00001-0.05% w/w of the composition.

16. The composition according to claim 15, wherein the amount of calcipotriol or calcipotriol monohydrate is 0.001 or 0.002% w/w of the composition.

17. The composition according to claim 1, wherein the amount of betamethasone dipropionate is 0.0005-1% w/w of the composition.

18. The composition according to claim 17, wherein the amount of betamethasone dipropionate is 0.006, 0.02, 0.026 or 0.03% w/w of the composition.

19. The composition according to claim 1, wherein the amount of betamethasone dipropionate is 0.026% w/w and the amount of calcipotriol monohydrate is 0.002% w/w or the corresponding amount of calcipotriol.

20. The composition according to claim 1, further comprising a non-evaporating oily co-solvent selected from at least one of the following solvent classes (a) a compound of general formula I H(OCH.sub.2C(CH.sub.3)H).sub.xOR.sup.1 wherein R.sup.1 is straight or branched chain C.sub.1-20 alkyl, and x is an integer of 2-60; (b) an isopropyl ester of a straight or branched chain C.sub.10-18 alkanoic or alkenoic acid; (c) a propylene glycol diester of a C.sub.8-14 alkanoic or alkenoic acid; (d) a straight or branched C.sub.8-24 alkanol or alkenol; (e) highly purified vegetable oils such as medium chain triglycerides or long chain triglycerides; and (f) N-alkylpyrrolidone or N-alkylpiperidone.

21. The composition according to claim 20, wherein the compound of general formula I is polyoxypropylene-15-stearyl ether, polyoxypropylene-11-stearyl ether, polyoxypropylene-14-butyl ether, polyoxypropylene-10-cetyl ether or polyoxypropylene-3-myristyl ether.

22. The composition according to claim 20, wherein the isopropyl ester of a straight or branched chain C.sub.10-18 alkanoic or alkenoic acid is isopropyl myristate, isopropyl palmitate, isopropyl isostearate, isopropyl linolate or isopropyl monooleate.

23. The composition according to claim 20, wherein the propylene glycol diester of a C.sub.8-14 alkanoic acid is propylene glycol dipelargonate.

24. The composition according to claim 20, wherein the straight C.sub.8-24 alkanol or alkenol is capryl, lauryl, cetyl, stearyl, oleyl, linoelyl or myristyl alcohol, or wherein the branched C.sub.8-24 alkanol is a branched C.sub.18-24 alkanol.

25. The composition according to claim 20, wherein the N-alkylpyrrolidone is N-methylpyrrolidone.

26. The composition according to claim 1, comprising 10-50% w/w of the lipid carrier.

27. The composition according to claim 26, comprising 15-45% w/w of the lipid carrier.

28. The composition according to claim 27, comprising 20-40% w/w of the lipid carrier.

29. The composition according to claim 1, wherein the paraffin is selected from paraffins consisting of hydrocarbons with chain lengths from C.sub.5 to C.sub.60, the chain lengths peaking at C.sub.14-16, C.sub.18-22, C.sub.20-22, C.sub.20-26, C.sub.28-40, and C.sub.40-44 (as determined by gas chromatography).

30. The composition according to claim 29, further comprising a lipophilic viscosity-increasing agent capable of imparting to the lipid carrier the property of forming a semi-solid and occlusive layer on skin on application and evaporation of the propellant, said viscosity-increasing agent being selected from the group consisting of microcrystalline wax, silicone wax and hydrogenated castor oil, or mixtures thereof, and an isoparaffin.

31. The composition according to claim 1, comprising 0.1-10% w/w of the oily co-solvent.

32. The composition of claim 31, comprising 1-2.5% w/w or 1.5-2% w/w of the oily co-solvent.

33. The composition according to claim 20, wherein the oily co-solvent is medium chain triglycerides.

34. The composition according to claim 22, wherein the isopropyl ester of a straight or branched chain C.sub.10-18 alkanoic or alkenoic acid is isopropyl myristate.

35. The composition according to claim 24, wherein the straight C.sub.8-24 alkanol or alkenol is oleyl alcohol.

36. The composition according to claim 1, wherein the amount of calcipotriol in said composition without the propellant corresponds to about 0.005% w/w calcipotriol and the amount of betamethasone dipropionate in the composition without the propellant is about 0.064% w/w.

37. The composition according to claim 1, wherein the amount of calcipotriol in said composition without the propellant corresponds to about 0.005 w/w calcipotriol and the amount of betamethasone dipropionate in the composition without the propellant is about 0.064% w/w and wherein the propellant is a mixture of dimethyl ether and one or more C.sub.3-5 alkanes.

38. The composition according to claim 1, wherein the amount of calcipotriol in the composition without the propellant corresponds to about 0.005% w/w calcipotriol and the amount of betamethasone dipropionate in the composition without the propellant is about 0.064% w/w and wherein the propellant is a mixture of n-butane and/or isobutane and dimethyl ether and wherein the ratio of n-butane and/or isobutane to dimethyl ether is in the range of 6:1-0:1 v/v.

39. The composition of claim 38, wherein the propellant is a mixture of n-butane or isobutane and dimethyl ether and the ratio of n-butane and/or isobutane to dimethyl ether is in the range of 5:1-1:2 v/v.

40. The composition of claim 39, wherein the ratio of n-butane and/or isobutane to dimethyl ether is in the range of 4:1-1:1 v/v.

41. The composition of claim 39, wherein the ratio of n-butane and/or isobutane to dimethyl ether is in the range of 4:2-1:1 v/v.

42. The composition of claim 39, wherein the ratio of n-butane and/or isobutane to dimethyl ether is in the range of 4:2-4:3 v/v.

43. The composition of claim 39, wherein the ratio of n-butane and/or isobutane to dimethyl ether is in the range of 4:3-1:1 v/v.

44. The composition according to any one of claims 36 to 43, wherein the propellant consists of a mixture of dimethyl ether and n-butane.

45. The composition according to any one of claims 36 to 43, wherein the amount of propellant is 45-95% w/w.

46. The composition of claim 45 wherein the amount of propellant is 45-90 w/w.

47. The composition of claim 45 wherein the amount of propellant is 45-70% w/w.

48. The composition of claim 45 wherein the amount of propellant is 50-70 w/w.

49. The composition according to claim 1, wherein the amount of calcipotriol in the composition without the propellant corresponds to about 0.005% w/w calcipotriol and the amount of betamethasone dipropionate in the composition without the propellant is about 0.064% w/w and wherein the lipid carrier which upon application on the skin and evaporation of the propellant form a semi-solid and occlusive layer at the site of application comprises petrolatum and liquid paraffin.

50. The composition according to claim 1, wherein the amount of calcipotriol in the composition without the propellant corresponds to about 0.005% w/w calcipotriol and the amount of betamethasone dipropionate in the composition without the propellant is about 0.064% w/w and wherein the propellant is a mixture of dimethyl ether and one or more C.sub.3-5 alkanes and wherein the lipid carrier which upon application on the skin and evaporation of the propellant form a semi-solid and occlusive layer at the site of application comprises petrolatum and liquid paraffin.

51. The composition according to claim 1, wherein the amount of calcipotriol in the composition without the propellant corresponds to about 0.005 w/w calcipotriol and the amount of betamethasone dipropionate in the composition without the propellant is about 0.064% w/w, wherein the propellant is a mixture of n-butane and/or isobutane and dimethyl ether where the ratio of n-butane and/or isobutane to dimethyl ether is in the range of 6:1-0:1 v/v and wherein the lipid carrier which upon application on the skin and evaporation of the propellant form a semi-solid and occlusive layer at the site of application comprises petrolatum and liquid paraffin.

52. The composition of claim 51, wherein the propellant is a mixture of n-butane and/or isobutane and dimethyl ether and the ratio of n-butane and/or isobutane to dimethyl ether is in the range of 5:1-1:2 v/v.

53. The composition of claim 51, wherein the ratio of n-butane and/or isobutane to dimethyl ether is in the range of 4:1-1:1 v/v.

54. The composition of claim 51, wherein the ratio of n-butane and/or isobutane to dimethyl ether is in the range of 4:2-1:1 v/v.

55. The composition of claim 51, wherein the ratio of n-butane and/or isobutane to dimethyl ether is in the range of 4:2-4:3 v/v.

56. The composition of claim 51, wherein the ratio of n-butane and/or isobutane to dimethyl ether is in the range of 4:3-1:1 v/v.

57. The composition of any one of claims 49 to 56, wherein the propellant consists of dimethyl ether and n-butane.

58. The composition of any one of claims 49 to 56, wherein the amount of propellant is 45-95% w/w.

59. The composition of claim 58 wherein the amount of propellant is 45-90% w/w.

60. The composition of claim 59 wherein the amount of propellant is 45-70% w/w.

61. The composition of claim 60 wherein the amount of propellant is 50-70 w/w.

62. The composition of claim 1 wherein the amount of calcipotriol in the composition without the propellant corresponds to about 0.005% w/w calcipotriol and the amount of betamethasone dipropionate in the composition without the propellant is about 0.064% betamethasone w/w and wherein propellant is a mixture of dimethyl ether and one or more C.sub.3-5 alkanes and the amount of propellant is 45-70% w/w.

63. The composition of claim 62 wherein the propellant is a mixture of n-butane and/or isobutane, and dimethyl ether; and the ratio of n-butane and/or isobutane to dimethyl ether is in the range of 4:2-4:3 v/v.

64. The composition of claim 62 wherein the propellant is a mixture of n-butane and/or isobutane, and dimethyl ether; and the ratio of n-butane and/or isobutane to dimethyl ether is in the range of 4:3-1:1 v/v.

65. The composition according to claim 62, wherein the lipid carrier comprises petrolatum and liquid paraffin.

66. The composition according to claim 2 wherein the amount of propellant is 45-70% w/w.

67. The composition according to claim 1, wherein the propellant is a mixture of dimethylether and one or more C.sub.3-5 alkanes, and the lipid carrier consists essentially of petrolatum and liquid paraffin.

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