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Generated: September 25, 2017

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Title: Pharmaceutical compositions comprising cyclosporins
Abstract:Pharmaceutical compositions comprising a cyclosporin, e.g. Ciclosporin or [Nva].sup.2 -Ciclosporin, in "microemulsion pre-concentrate" and microemulsion form. The compositions typically comprise (1.1) a C.sub.1-5 alkyl or tetrahydrofurfuryl di- or partial-ether of a low molecular weight mono- or poly-oxy-alkane diol, e.g. Transcutol or Glycofurol, as hydrophilic component. Compositions are also provided comprising a cyclosporin and (1.1) and, suitably, also a saccharide monoester, e.g. raffinose or saccharose monolaurate. Dosage forms include topical formulations and, in particular, oral dosage forms.
Inventor(s): Hauer; Birgit (Lahr, DE), Meinzer; Armin (Munzingen, DE), Posanski; Ulrich (Freiburg, DE), Richter; Friedrich (Schonbush-Urtenen, CH)
Assignee: Novartis AG (Basel, CH)
Application Number:08/812,073
Patent Claims: 1. A pharmaceutical composition comprising about 5 to about 25% by weight of cyclosporin A, about 0.5 to about 90% by weight of a hydrophilic component, other than a polyoxyethylene glycolated natural or hydrogenated vegetable oil and other than water, about 0.5 to about 90% by weight of a triglyceride lipophilic component and about 0.5 to about 90% by weight of a polyoxyethylene glycolated natural or hydrogenated vegetable oil surfactant, all weight percents being based on the total weight of the composition, wherein said composition, upon dilution with water to a ratio of 1 part by weight of composition to 5 parts by weight of water, spontaneously forms an oil-in-water microemulsion having particles of less than 2,000 .ANG..

2. The composition of claim 1 wherein the particles have a maximum size of less than 1,500 .ANG..

3. The composition of claim 1 wherein the maximum size of the particles is from 100 to 1,000 .ANG..

4. The composition of claim 1 comprising about 2 to about 45% by weight of said lipophilic component, based on the total weight of the composition.

5. The composition of claim 1 comprising about 20 to about 90% by weight of said surfactant, based on the total weight of the composition.

6. The composition of claim 1 comprising about 0.5 to about 90% by weight of said hydrophilic component, about 2 to about 45% by weight of said lipophilic component and about 20 to about 90% by weight of said surfactant, all weights based on the total weight of the composition.

7. The composition of claim 1 wherein said surfactant comprises a polyoxyethylene glycolated hydrogenated castor oil.

8. The composition of claim 1 wherein said triglyceride is a medium chain fatty acid triglyceride.

9. The composition of claim 1 additionally comprising a monoglyceride.

10. The composition of claim 9 wherein said monoglyceride is a glycerol monooleate.

11. The composition of claim 1 additionally comprising an anti-oxidant.

12. The composition of claim 11 wherein said anti-oxidant is alpha-tocopherol.

13. A pharmaceutical composition comprising about 5 to about 25% by weight of cyclosporin A, about 0.5 to about 90% by weight of a hydrophilic component other than a polyoxyethylene glycolated natural or hydrogenated vegetable oil and other than water, about 0.5 to about 90% by weight of a triglyceride lipophilic component and about 0.5 to about 90% by weight of a polyoxyethylene glycolated natural or hydrogenated vegetable oil surfactant, all weight percents being based on the total weight of the composition, wherein said composition, upon dilution with water to a ratio of 1 part by weight of composition to 5 parts by weight of water, spontaneously forms an oil-in-water microemulsion having an average particle size of less than about 1,500 .ANG..

14. The composition of claim 13 wherein the average particle size is less than about 1,000 .ANG..

15. The composition of claim 14 wherein the average particle size is from about 150 to less than about 1,000 .ANG..

16. The composition of claim 13 comprising about 2 to about 45% by weight of said lipophilic component, based on the total weight of the composition.

17. The composition of claim 13 comprising about 20 to about 90% by weight of said surfactant, based or, the total weight of the composition.

18. The composition of claim 13 comprising about 0.5 to about 90% by weight of said hydrophilic component, about 2 to about 45% by weight of said lipophilic component and about 20 to about 90% by weight of said surfactant, all weights based on the total weight of the composition.

19. The composition of claim 13 wherein said surfactant is a polyoxyethylene glycolated hydrogenated castor oil.

20. The composition of claim 13 wherein said triglyceride is a medium chain fatty acid triglyceride.

21. The composition of claim 13 additionally comprising a monoglyceride.

22. The composition of claim 21 wherein said monoglyceride is a glycerol monooleate.

23. The composition of claim 13 additionally comprising an anti-oxidant.

24. The composition of claim 23 wherein said anti-oxidant is alpha-tocopherol.

25. An oil-in water microemulsion composition having particles of less than 2,000 .ANG. comprising water, about 5 to about 25% by weight of cyclosporin A, about 0.5 to about 90% by weight of a hydrophilic component other than a polyoxyethylene glycolated natural or hydrogenated vegetable oil and other than water, about 0.5 to about 90% by weight of a triglyceride lipophilic component, about 0.5 to about 90% by weight of a polyoxyethylene glycolated natural or hydrogenated vegetable oil surfactant, all weight percents being based on the total weight of the cyclosporin A, hydrophilic component, lipophilic component and surfactant.

26. The composition of claim 25 wherein the particles have a maximum size of less than 1,500 .ANG..

27. The composition of claim 25 wherein the maximum size of the particles is from 100 to 1,000 .ANG..

28. The composition of claim 25 comprising about 2 to about 45% by weight of said lipophilic component, based on the total weight of the cyclosporin A, hydrophilic component, lipophilic component and surfactant.

29. The composition of claim 25 comprising about 20 to about 90% by weight of said surfactant, based on the total weight of the cyclosporin A, hydrophilic component, lipophilic component and surfactant.

30. The composition of claim 25 comprising about 0.5 to about 90% by weight of said hydrophilic component, about 2 to about 45% by weight of said lipophilic component and about 20 to about 90% by weight of said surfactant, all weights based on the total weight of the cyclosporin A, hydrophilic component, lipophilic component and surfactant.

31. The composition of claim 25 wherein said surfactant is a polyoxyethylene glycolated hydrogenated castor oil.

32. The composition of claim 25 wherein said triglyceride is a medium chain fatty acid triglyceride.

33. The composition of claim 25 additionally comprising a monoglyceride.

34. The composition of claim 33 wherein said monoglyceride is a glycerol monooleate.

35. The composition of claim 25 additionally comprising an anti-oxidant.

36. The composition of claim 35 wherein said anti-oxidant is alpha-tocopherol.

37. An oil-in-water microemulsion composition having an average particle size of less than about 1,500 .ANG. comprising water, about 5 to about 25% by weight of cyclosporin A, about 0.5 to about 90% by weight of a hydrophilic component other than a polyethylene glycolated natural or hydrogenated vegetable oil and other than water, about 0.5 to about 90% by weight of a triglyceride lipophilic component, about 0.5 to about 90% by weight of a polyoxyethylene glycolated natural or hydrogenated vegetable oil surfactant, all weight percents being based on the total weight of the cyclosporin A, hydrophilic component, lipophilic component and surfactant.

38. The composition of claim 37 wherein the average particle size is less than about 1,000 .ANG..

39. The composition of claim 37 wherein the average particle size is from about 150 to less than about 1,000 .ANG..

40. The composition of claim 37 comprising about 2 to about 45% by weight of said lipophilic component, based on the total weight of the cyclosporin A, hydrophilic component, lipophilic component and surfactant.

41. The composition of claim 37 comprising about 20 to about 90% by weight of said surfactant, based on the total weight of the cyclosporin A, hydrophilic component, lipophilic component and surfactant.

42. The composition of claim 37 comprising about 0.5 to about 90% by weight of said hydrophilic component, about 2 to about 45% by weight of said lipophilic component and about 20 to about 90% by weight of said surfactant, all weights based on the total weight of the cyclosporin A, hydrophilic component, lipophilic component and surfactant.

43. The composition of claim 37 wherein said surfactant is a polyoxyethylene glycolated hydrogenated castor oil.

44. The composition of claim 37 wherein said triglyceride is a medium chain fatty acid triglyceride.

45. The composition of claim 37 additionally comprising a monoglyceride.

46. The composition of claim 45 wherein said monoglyceride is a glycerol monooleate.

47. The composition of claim 37 additionally comprising an anti-oxidant.

48. The composition of claim 47 wherein said anti-oxidant is alpha-tocopherol.

49. A method of reducing the influence of bile acids and salts on the bioavailability of cyclosporin A in a patient's gastrointestinal system during cyclosponn therapy, said method comprising orally administering a pharmaceutical composition comprising about 5 to about 25% by weight of cyclosporin A, about 0.5 to about 90% by weight of a hydrophilic component, about 0.5 to about 90% by weight of a lipophilic component and about 0.5 to about 90% by weight of a surfactant, all weights based on the total weight of the composition, the relative proportion of said cyclosporin A, hydrophilic component, lipophilic component and surfactant being such that upon dilution with water to a ratio of 1 part by weight of composition to 5 parts by weight of water, an oil-in-water microemulsion having particles of less than 2,000 .ANG. is spontaneously formed.

50. The method of claim 49 wherein the particles have a maximum size of less than 1,500 .ANG..

51. The method of claim 50 wherein the maximum size of the particles is from 100 to 1,000 .ANG..

52. The method of claim 49 wherein the dilution with water is to a ratio of 1 part by weight of composition to 1 part by weight of water.

53. The method of claim 49 comprising about 2 to about 45% by weight of lipophilic component, based on the total weight of the composition.

54. The method of claim 49 comprising about 20 to about 90% by weight of surfactant, based on the total weight of the composition.

55. The method of claim 49 comprising about 0.5 to about 90% by weight of hydrophilic component, about 2 to about 45% by weight of lipophilic component and about 20 to about 90% by weight of surfactant, all weights based on the total weight of the composition.

56. The method of claim 49 wherein the cyclosporin therapy comprises liver transplant therapy.

57. A method of reducing the influence of bile acids and salts on the bioavailability of cyclosporin A in a patient's gastrointestinal system during cyclosporin therapy, said method comprising orally administering a pharmaceutical composition comprising about 5 to about 25% by weight of cyclosporin A, about 0.5 to about 90% by weight of a hydrophilie component, about 0.5 to about 90% by weight of a lipophilic component and about 0.5 to about 90% by weight of a surfactant, all weights based on the total weight of the composition, the relative proportion of said cyclosporin A, hydrophilic component, lipophilic component and surfactant being such that upon dilution with water to a ratio of 1 part by weight of composition to 5 parts by weight of water, an oil-in-water microomulsion having an average particle size of less than about 1,500 .ANG. is spontaneously formed.

58. The method of claim 57 wherein the average particle size is less than about 1,000 .ANG..

59. The method of claim 58 wherein the average particle size is fom about 150 to less than about 1,000 .ANG..

60. The method of claim 57 wherein the dilution with water is to a ratio of 1 part by weight of composition to 1 part by weight of water.

61. The method of claim 57 comprising about 2 to about 45% by weight of lipophilic component, based on the total weight of the composition.

62. The method of claim 57 comprising about 20 to about 90% by weight of surfactant, based on the total weight of the composition.

63. The method of claim 57 comprising about 0.5 to about 90% by weight of hydrophilic component, about 2 to about 45% by weight of lipophilic component and about 20 to about 90% by weight of surfactant, all weights based on the total weight of the composition.

64. The method of claim 57 wherein the cyclosporin therapy comprises liver transplant therapy.
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