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Claims for Patent: 9,278,105

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Claims for Patent: 9,278,105

Title:Tetracycline compositions
Abstract: The present invention relates to compositions, pharmaceutical compositions, and methods for preparing the same, comprising a tetracycline with improved stability and solubility. Some embodiments include a tetracycline with an excess of a divalent or trivalent cation.
Inventor(s): Griffith; David C. (San Marcose, CA), Boyer; Serge (San Diego, CA), Dudley; Michael N. (San Diego, CA), Hecker; Scott (Del Mar, CA)
Assignee: Rempex Pharmaceuticals, Inc. (San Diego, CA)
Application Number:13/654,018
Patent Claims: 1. A method of treating a bacterial infection in a subject, wherein the method comprises administering a therapeutically effective amount of a composition to a subject in need thereof via an intravenous route of administration, wherein the composition comprises an aqueous solution of a 7-dimethylamino-tetracycline antibiotic and a magnesium cation, wherein the molar ratio of magnesium cation to 7-dimethylamino-tetracycline antibiotic is greater than 3:1 and wherein the solution does not comprise a pharmaceutically acceptable oil, has a pH greater than 4 and less than 7, and has an osmolality less than about 500 mOsmol/kg.

2. The method of claim 1, wherein the solution does not comprise an antioxidant, a pyridine-containing compound, gluconate, an alcohol, glycerol, polyethylene glycol, a pyrrolidone-containing compound, a water-miscible local anaesthetic, urea, lactose, or a dehydrating agent.

3. The method of claim 1, wherein solution does not comprise nicotinamide, procaine, or a dehydrating agent selected from the group consisting of ethyl acetate, acetic anhydride, absolute ethanol, and mixtures thereof.

4. The method of claim 1, wherein the solution has a pH of less than 6.

5. The method of claim 1, wherein the solution has a pH of less than 5.

6. The method of claim 1, wherein the molar ratio of magnesium cation to 7-dimethylamino-tetracycline antibiotic is greater than or equal to 5:1.

7. The method of claim 1, wherein the molar ratio of magnesium cation to 7-dimethylamino-tetracycline antibiotic is greater than 8:1.

8. The method of claim 1, wherein the molar ratio of magnesium cation to 7-dimethylamino-tetracycline antibiotic is greater than or equal to 10:1.

9. The method of claim 1, wherein the osmolality of the solution is less than 400 mOsm/kg.

10. The method of claim 1, wherein the osmolality of the solution is less than 350 mOsm/kg.

11. The method of claim 1, wherein the solution comprises magnesium sulfate.

12. The method of claim 1, wherein the solution comprises magnesium acetate.

13. The method of claim 1, wherein the solution comprises magnesium chloride.

14. The method of claim 1, wherein the solution comprises a buffer.

15. The method of claim 14, wherein the solution comprises acetate.

16. The method of claim 1, wherein the solution comprises a base.

17. The method of claim 16, wherein the base is NaOH.

18. The method of claim 1, wherein the 7-dimethylamino-tetracycline is selected from minocycline, PTK796, and a glycylcycline.

19. The method of claim 18, wherein the glycylcycline is tigecycline.

20. The method of claim 19, wherein the composition comprises 5 mg/ml tigecycline, MgSO.sub.4, and NaOH, wherein the Mg to tigecycline molar ratio is 5:1, and the pH is greater than 5.5 and less than 6.5.

21. The method of claim 19, wherein the composition comprises 5 mg/ml tigecycline, MgSO.sub.4, and NaOH, wherein the Mg to tigecycline molar ratio is 12:1, and the pH is greater than 5.5 and less than 6.5.

22. The method of claim 19, wherein the composition comprises 5 mg/ml tigecycline, MgCl.sub.2, and NaOH, wherein the Mg to tigecycline molar ratio is 5:1, and the pH is greater than 5.5 and less than 6.5.

23. The method of claim 19, wherein the composition comprises 5 mg/ml tigecycline, MgCl.sub.2, and NaOH, wherein the Mg to tigecycline molar ratio is 12:1, and the pH is greater than 5.5 and less than 6.5.

24. The method of claim 19, wherein the composition comprises 5 mg/ml tigecycline, MgSO.sub.4, and NaOH, wherein the Mg to tigecycline molar ratio is 5:1, and the pH is greater than 6.0 and less than 7.0.

25. The method of claim 19, wherein the composition comprises 5 mg/ml tigecycline, MgSO.sub.4, and NaOH, wherein the Mg to tigecycline molar ratio is 12:1, and the pH is greater than 6.0 and less than 7.0.

26. The method of claim 1, wherein the 7-dimethylamino-tetracycline is PTK796.

27. The method of claim 1, wherein the 7-dimethylamino-tetracycline is minocycline.

28. The method of claim 27, wherein the concentration of minocycline is at least 5 mg/ml.

29. The method of claim 27, wherein the concentration of minocycline is at least 10 mg/ml.

30. The method of claim 27, wherein the composition comprises 10 mg/ml minocycline, MgCl.sub.2, and NaOH, wherein the Mg to minocycline molar ratio is 5:1, and the pH is greater than 4.5 and less than 5.5.

31. The method of claim 27, wherein the composition comprises 10 mg/ml minocycline, MgSO.sub.4, and sodium acetate, wherein the Mg to minocycline molar ratio is 5:1, the pH is greater than 4.5 and less than 5.5, and the osmolality is greater than 275 mOsm/kg and less than 375 mOsm/kg.

32. The method of claim 27, wherein the composition comprises 10 mg/ml minocycline and Mg(CH.sub.3O.sub.2).sub.2, wherein the Mg to minocycline molar ratio is 5:1, and the pH is greater than 4.5 and less than 5.5.

33. The method of claim 27, wherein the composition comprises 10 mg/ml minocycline, MgSO.sub.4, and NaOH, wherein the Mg to minocycline molar ratio is 5:1, the pH is greater than 4.5 and less than 5.5, and the osmolality is greater than 150 mOsm/kg and less than 250 mOsm/kg.

34. A method of treating a bacterial infection in a subject, wherein the method comprises: reconstituting a water-soluble solid composition in a pharmaceutically acceptable diluent to form a first solution; diluting the reconstituted solution with a pharmaceutically acceptable diluent to form a second solution; and administering a therapeutically effective amount of the second solution to a subject in need thereof via an intravenous route of administration, wherein the water-soluble solid composition comprises a 7-dimethylamino-tetracycline antibiotic or a salt thereof and a salt comprising a divalent or trivalent metal cation, wherein the molar ratio of divalent or trivalent cation to 7-dimethylamino-tetracycline is greater than 3:1 and wherein the second solution has a pH greater than 4 and less than 7 and an osmolality less than 500 mOsmol/kg.

35. The method of claim 34, wherein the molar ratio of divalent or trivalent metal cation to 7-dimethylamino-tetracycline antibiotic is greater than or equal to 5:1.

36. The method of claim 34, wherein the molar ratio of divalent or trivalent metal cation to 7-dimethylamino-tetracycline antibiotic is greater than 8:1.

37. The method of claim 34, wherein the molar ratio of divalent or trivalent metal cation to 7-dimethylamino-tetracycline antibiotic is greater than or equal to 10:1.

38. The method of claim 34, wherein the water-soluble solid composition is in the form of a lyophile.

39. The method of claim 34, wherein the salt comprising a divalent or trivalent metal cation is magnesium sulfate.

40. The method of claim 34, wherein the salt comprising a divalent or trivalent metal cation is calcium chloride.

41. The method of claim 34, wherein the water-soluble solid composition comprises sodium acetate.

42. The method of claim 34, wherein the water-soluble solid composition comprises NaOH.

43. The method of claim 34, wherein the salt comprising a divalent or trivalent metal cation is selected from magnesium chloride, magnesium bromide, magnesium sulfate, calcium chloride, calcium bromide, zinc chloride, gallium chloride, magnesium malate, magnesium citrate, magnesium acetate, and zinc acetate.

44. The method of claim 34, wherein the water-soluble solid composition does not comprise an antioxidant, a pyridine-containing compound, nicotinamide, or gluconate.

45. The method of claim 34, wherein the 7-dimethylamino-tetracycline is selected from minocycline, PTK796, and a glycylcycline.

46. The method of claim 45, wherein the glycylcycline is tigecycline.

47. The method of claim 34, wherein the 7-dimethylamino-tetracycline is minocycline.

48. The method of claim 34, wherein the 7-dimethylamino-tetracycline is PTK796.

49. The method of claim 1, wherein the molar ratio of magnesium cation to 7-dimethylamino-tetracylcine antibiotic is from 5:1 to 10:1.

50. The method of claim 49, wherein the molar ratio of magnesium cation to 7-dimethylamino-tetracylcine antibiotic is 5:1.

51. The method of claim 34 wherein the molar ratio of divalent or trivalent metal cation to 7-dimethylamino-tetracylcine antibiotic is from 5:1 to 10:1.

52. The method of claim 51, wherein the molar ratio of divalent or trivalent metal cation to 7-dimethylamino-tetracylcine antibiotic is 5:1.

53. The method of claim 1, wherein less than 1000 ml of the solution is administered to the subject.

54. The method of claim 1, wherein less than 500 ml of the solution is administered to the subject.

55. The method of claim 1, wherein less than 200 ml of the solution is administered to the subject.

56. The method of claim 1, wherein less than 110 ml of the solution is administered to the subject.

57. The method of claim 34, wherein less than 1000 ml of the second solution is administered to the subject.

58. The method of claim 34, wherein less than 500 ml of the second solution is administered to the subject.

59. The method of claim 34, wherein less than 200 ml of the second solution is administered to the subject.

60. The method of claim 34, wherein less than 110 ml of the second solution is administered to the subject.
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