Cyclosporin compositions

• US 20070015691A1
• Filed: 07/13/2005
• Published: 01/18/2007
• Est. Priority Date: 07/13/2005
• Status: Abandoned Application

• Current Assignee: Saint Regis Mohawk Tribe
• Original Assignee: Allergan Incorporated (Abbvie Incorporated)
• Inventors: Chang, James, Firestone, Bruce, Olejnik, Orest
• Application Number:
  US11/181,409
• Publication Number:
  US 20070015691A1
• Time in Patent Office: Days
• US Class Current: 514/20.500
• CPC Class Codes: A61K 38/13 Cyclosporins
• CPC Class Codes: A61K 47/32 Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers , poly(meth)acrylates, or polyvinyl pyrrolidone
• CPC Class Codes: A61K 47/34 Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers A61K47/10 takes precedence
• CPC Class Codes: A61K 47/38 Cellulose; Derivatives thereof
• CPC Class Codes: A61K 47/44 Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin synthetic glycerides, e.g. medium-chain triglycerides, A61K47/14
• CPC Class Codes: A61K 9/0048 Eye, e.g. artificial tears
• CPC Class Codes: A61K 9/107 Emulsions ; Emulsion preconcentrates; Micelles composition of emulsions A61K47/00
• CPC Class Codes: A61P 27/02 Ophthalmic agents

Abstract

A composition is disclosed herein comprising from about 0.001% to about 0.4% cyclosporin A, castor oil, and a surfactant selected from the group consisting of alcohol ethoxylates, alcohols, alkyl glycosides, alkyl polyglycosides, alkylphenol ethoxylates, amine oxides, block polymers, carboxylated alcohol or alkylphenol ethoxylates, carboxylic acids/fatty acids, cellulose derivatives, ethoxylated alcohols, ethoxylated alkylphenols, ethoxylated aryl phenols, ethoxylated fatty acids, ethoxylated fatty acids, ethoxylated fatty esters and oils, fatty alcohols, fatty esters, glycol esters, lanolin-based derivatives, lecithin and lecithin derivatives, lignin and lignin derivatives, methyl esters, monoglycerides and derivatives , phosphalipids, polyacrylic acids, polyethylene glycols, polyethylene oxide-polypropylene oxide copolymers, polyethylene oxides, polymeric surfactants, polypropylene oxides, propoxylated alcohols, propoxylated alkyl phenols, propoxylated fatty acids, protein-based surfactants, sarcosine derivatives, silicone-based surfactants, sorbitan derivatives, stearates, sucrose and glucose esters and derivatives, and combinations thereof.

Claims

1. A composition comprising from about 0.001% to about 0.4% cyclosporin A, castor oil, and a surfactant selected from the group consisting of alcohol ethoxylates, alcohols, alkyl glycosides, alkyl polyglycosides, alkylphenol ethoxylates, amine oxides, block polymers, carboxylated alcohol or alkylphenol ethoxylates, carboxylic acids/fatty acids, cellulose derivatives, ethoxylated alcohols, ethoxylated alkylphenols, ethoxylated aryl phenols, ethoxylated fatty acids, ethoxylated fatty acids, ethoxylated fatty esters and oils, fatty alcohols, fatty esters, glycol esters, lanolin-based derivatives, lecithin and lecithin derivatives, lignin and lignin derivatives, methyl esters, monoglycerides and derivatives, phosphalipids, polyacrylic acids, polyethylene glycols, polyethylene oxide-polypropylene oxide copolymers, polyethylene oxides, polymeric surfactants, polypropylene oxides, propoxylated alcohols, propoxylated alkyl phenols, propoxylated fatty acids, protein-based surfactants, sarcosine derivatives, silicone-based surfactants, stearates, sucrose and glucose esters and derivatives, and combinations thereof, wherein the surfactant is not a sorbitan derivative wherein said composition is an ophthalmically acceptable emulsion.

2. The composition of claim 1 comprising from about 0.005% to about 0.05% cyclosporin A.

3. The composition of claim 2 comprising about 0.05% cyclosporin A.

5. The composition of claim 2 comprising from about 0.005% to about 0.05% cyclosporin A, castor oil, and a stearate.

6. The composition of claim 2 comprising from about 0.005% to about 0.05% cyclosporin A, castor oil, and glyceryl stearate.

7. The composition of claim 2 comprising from about 0.005% to about 0.05% cyclosporin A, castor oil, and isopropyl stearate.

8. The composition of claim 2 comprising from about 0.005% to about 0.05% cyclosporin A, castor oil, and polyethylene glycol.

9. The composition of claim 2 comprising from about 0.005% to about 0.05% cyclosporin A, castor oil, and polyethylene oxide.

10. The composition of claim 2 comprising from about 0.005% to about 0.05% cyclosporin A, castor oil, and a polyethylene oxide-polypropylene oxide copolymer.

11. The composition of claim 2 comprising from about 0.005% to about 0.05% cyclosporin A, castor oil, and an alcohol ethoxylate.

12. The composition of claim 2 comprising from about 0.005% to about 0.05% cyclosporin A, castor oil, and an alkylphenol ethoxylate.

13. The composition of claim 2 comprising from about 0.005% to about 0.05% cyclosporin A, castor oil, and an alkyl glycoside.

14. The composition of claim 2 comprising from about 0.005% to about 0.05% cyclosporin A, castor oil, and alkyl polyglycoside.

15. The composition of claim 2 comprising from about 0.005% to about 0.05% cyclosporin A, castor oil, and a fatty alcohol.

16. The composition of claim 2 comprising from about 0.005% to about 0.05% cyclosporin A, castor oil, and hydroxypropylmethyl cellulose.

17. The composition of claim 2 comprising from about 0.005% to about 0.05% cyclosporin A, castor oil, and carboxymethyl cellulose.

18. The composition of claim 2 comprising from about 0.005% to about 0.05% cyclosporin A, castor oil, and a polyacrylic acid.

19. The composition of claim 2 comprising from about 0.005% to about 0.05% cyclosporin A, castor oil, and a Carbomer.

20. The composition of claim 2 comprising from about 0.005% to about 0.05% cyclosporin A, castor oil, and a phosphalipid.

4. (Canceled)

21. A composition comprising from about 0.001% to about 0.4% cyclosporin A, castor oil, and an ethoxylated fatty acid surfactant, wherein said composition is an ophthalmically acceptable emulsion.

34. A composition comprising from about 0.001% to about 0.4% cyclosporin A, castor oil, and an ethoxylated fatty acid surfactant, wherein said composition is an ophthalmically acceptable emulsion, and PEG 200 monolaurate, PEG 200 dilaurate, PEG 400 monolaurate, PEG 400 dilaurate, PEG 600 mololaurate, PEG 600 dilaurate, PEG 200 monooleate, PEG 200 dioleate, PEG 400 monooleate, PEG 400 dioleate, PEG 600 monooleate, PEG 600 dioleate, PEG 200 monotallate, PEG 200 ditallate, PEG 400 monotallate, PEG 400 ditallate, PEG 600 monotallate, PEG 600 ditallate, and combinations thereof.

22. The composition of claim 34 comprising from about 0.005% to about 0.05% cyclosporin A.

23. The composition of claim 22 comprising about 0.05% cyclosporin A.

24. The composition of claim 22 wherein the ethoxylated fatty acid surfactant is Aldo PGHMS®

.

25. The composition of claim 22 wherein the ethoxylated fatty acid surfactant is Alkamuls TO-15/HR®

.

26. The composition of claim 22 wherein the ethoxylated fatty acid surfactant is Armotan AL-69-66®

.

27. The composition of claim 22 wherein the ethoxylated fatty acid surfactant is Cerasynt 840®

, Cerasynt 945®

, or a combination thereof.

28. The composition of claim 22 wherein the ethoxylated fatty acid surfactant is Crystal Inhibitor No. 5®

.

29. The composition of claim 22 wherein the ethoxylated fatty acid surfactant is DeThox Acid L-9®

, DeThox Acid S-8®

, or a combination thereof.

30. The composition of claim 22 wherein the ethoxylated fatty acid surfactant is Ethofat 242/25®

.

31. The composition of claim 22 wherein the ethoxylated fatty acid surfactant is Hydropalat 65®

.

32. The composition of claim 22 wherein the ethoxylated fatty acid surfactant is selected from Lipo EGMS®

, Lipopeg 2 DL®

, Lipopeg 4 DL®

, Lipopeg 4-L®

, Lipopeg 39-S®

, Lipopeg 4-S®

, Lipopeg 10-S®

, Lipopeg 100-S®

, Lipopeg 6000 DS®

, and combinations thereof.

33. The composition of claim 22 wherein the ethoxylated fatty acid surfactant is selected from Lumulse 40-L®

, Lumulse 40-S®

, Lumulse 42-L®

, Lumulse 42-S®

, Lumulse 100-S®

,Lumulse 602-S®

, and combinations thereof.

35. The composition of claim 22 wherein the ethoxylated fatty acid surfactant is Mapeg S-40K®

.

36. The composition of claim 22 wherein the ethoxylated fatty acid surfactant is Marlowet OTS®

.

37. The composition of claim 22 wherein the ethoxylated fatty acid surfactant is Naturechem PGR®

.

38. The composition of claim 22 wherein the ethoxylated fatty acid surfactant is PG No. 4®

.

39. The composition of claim 22 wherein the ethoxylated fatty acid surfactant is Renex 20®

.

40. The composition of claim 22 wherein the ethoxylated fatty acid surfactant is Ritox 52®

, Ritox 53®

, Ritox 59®

, or a combination thereof.

41. The composition of claim 22 wherein the ethoxylated fatty acid surfactant is Surfax 8916/A®

.

42. The composition of claim 22 wherein the ethoxylated fatty acid surfactant is Tego Acid S 40 P®

.

43. The composition of claim 22 wherein the ethoxylated fatty acid surfactant is Tego Acid S 100 P®

.

44. The composition of claim 22 wherein the ethoxylated fatty acid surfactant is Tween 20®

.

45. The composition of claim 22 wherein the ethoxylated fatty acid surfactant is Volpo 131®

.

46. The composition of claim 34 wherein the ethoxylated fatty acid surfactant is PEG 200 monolaurate.

47. The composition of claim 34 wherein the ethoxylated fatty acid surfactant is PEG 200 dilaurate.

48. The composition of claim 34 wherein the ethoxylated fatty acid surfactant is PEG 400 monolaurate.

49. The composition of claim 34 wherein the ethoxylated fatty acid surfactant is PEG 400 dilaurate.

50. The composition of claim 34 wherein the ethoxylated fatty acid surfactant is PEG 600 mololaurate.

51. The composition of claim 34 wherein the ethoxylated fatty acid surfactant is PEG 600 dilaurate.

52. The composition of claim 34 wherein the ethoxylated fatty acid surfactant is PEG 200 monooleate.

53. The composition of claim 34 wherein the ethoxylated fatty acid surfactant is PEG 200 dioleate.

54. The composition of claim 34 wherein the ethoxylated fatty acid surfactant is PEG 400 monooleate.

55. The composition of claim 34 wherein the ethoxylated fatty acid surfactant is PEG 400 dioleate.

56. The composition of claim 34 wherein the ethoxylated fatty acid surfactant is PEG 600 monooleate.

57. The composition of claim 34 wherein the ethoxylated fatty acid surfactant is PEG 600 dioleate.

58. The composition of claim 34 wherein the ethoxylated fatty acid surfactant is PEG 200 monotallate.

59. The composition of claim 34 wherein the ethoxylated fatty acid surfactant is PEG 200 ditallate.

60. The composition of claim 34 wherein the ethoxylated fatty acid surfactant is PEG 400 monotallate.

61. The composition of claim 34 wherein the ethoxylated fatty acid surfactant is PEG 400 ditallate.

62. The composition of claim 34 wherein the ethoxylated fatty acid surfactant is PEG 600 monotallate.

63. The composition of claim 34 wherein the ethoxylated fatty acid surfactant is PEG 600 ditallate.