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Last Updated: November 28, 2020

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Claims for Patent: 9,561,251

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Summary for Patent: 9,561,251
Title:Pharmaceutical compositions
Abstract: Pharmaceutical compositions for oral administration, in particular administration as an oral delivery system to be swallowed directly or capable of disintegration in the oral cavity, comprising iron oxy-hydroxide in high loading.
Inventor(s): Weibel; Ludwig Daniel (Waldstatt, CH), Philipp; Erik (Wittenbach, CH)
Assignee: Vifor Fresenius Medical Care Renal Pharma Ltd. (St. Gallen, CH)
Application Number:12/743,120
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 9,561,251
Patent Claims: 1. A pharmaceutical composition comprising an effective phosphate-adsorbing amount of iron oxy-hydroxide in high loading of 10to 80% (w/w) expressed in relation to the total weight of the pharmaceutical composition, and carbohydrates, said carbohydrates compromising saccharose and starch, in a form suitable for oral administration, wherein the amount of iron oxy-hydroxide per dosage form is at least 500 mg.

2. The composition according to claim 1 as film-coated dosage forms for intact swallowing or as dosage forms capable of disintegration in the oral cavity or in a small amount of liquid prior to ingestion.

3. The composition according to claim 1 wherein the iron oxy-hydroxide contains beta iron oxy-hydroxide.

4. The composition of claim 1 wherein iron oxy-hydroxide is present in an amount of 30 to 65% (w/w) expressed in relation to the total weight of the composition.

5. The composition of claim 1 wherein the carbohydrates are present in a total amount of 1 to 50% (w/w) expressed in relation to the total weight of the composition.

6. The composition of claim 1 further comprising one or more flavouring agent, sweetener, taste-enhancing agent, and/or coloring agent.

7. The composition of claim 6, wherein the sweetener, if present, is natural or unnatural sweetener selected from a polyol, aspartame, sucralose, acesulfamine K, and/or saccharin and the taste-enhancing agent, if present, is selected from glycosides neohesperidin dihydrochalcone, glycyrrhizin, glutamate.

8. The composition of claim 6, wherein the sweetener is present in an amount of 0.01 to 2.5% (w/w), and the taste-enhancing agent in an amount of 0.1 to 10 ppm, each expressed in relation to the total weight of the composition.

9. The composition of claim 6, wherein the flavouring agent, if present, is present in an amount of 0.01 to 10% (w/w) expressed in relation to the total weight of the composition.

10. The composition of claim 1 further comprising one or more excipients.

11. The composition of claim 1 comprising iron oxy-hydroxide in an amount of 10 to 80% (w/w), carbohydrates in a total amount of 1.0 to 50% (w/w), optionally one or more excipients in a total amount of 1.0 to 50% (w/w), one or more taste-enhancing agents in a total amount of 0.1 to 10 ppm, and/or one or more flavouring agents in a total amount of 0.01 to 10% (w/w), each expressed in relation to the total weight of the composition.

12. The composition of claim 11 comprising one or more superdisintegrants in a total amount of 0.1 to 10% by weight (w/w).

13. The composition of claim 1 in a form for intact swallowing or in a form capable of rapid disintegration selected from chewable tablets or pills, dry powders, granules, capsules or sachets containing these granules, wafers, or lozenges.

14. A method for preparing the composition according to claim 1 in a form of a tablet by direct compression or dry granulation.

15. A method for preparing a pharmaceutical composition comprising an effective phosphate-adsorbing amount of iron oxy-hydroxide in high loading of 10 to 80% (w/w) expressed in relation to the total weight of the pharmaceutical composition, and carbohydrates, said carbohydrates comprising saccharose and starch, in a form of a tablet, wherein the amount of iron oxy-hydroxide per dosage form is at least 500 mg, comprising the steps of preparing an aqueous suspension, comprising at least 90% (w/w) of all ingredients, including the iron oxy-hydroxide, based on the total weight of the final composition, then subjecting the aqueous suspension to spray-drying to obtain a flowable powder, which is optionally mixed with the remaining ingredients, and subsequently compressing the powder to obtain a tablet.

16. A tablet, as obtainable by the method of claim 15.

17. A tablet comprising iron oxy-hydroxide in an amount of 30 to 65% (w/w), saccharose in an amount of 5 to 30% (w/w), and starch in an amount of 5 to 30% (w/w), expressed in relation to the total weight of the tablet composition, excluding the weight of an optionally present tablet coating, wherein the amount of iron oxy hydroxide per dosage form is at least 500 mg.

18. The composition of claim 5 wherein the carbohydrates are present in a total amount of 5 to 30% (w/w) expressed in relation to the total weight of the composition.

19. The composition of claim 9, wherein the flavouring agent is present in an amount 0.1 to 5% (w/w) expressed in relation to the total weight of the composition.

20. The composition of claim 19, wherein the flavouring agent is present in an amount 0.1 to 1% (w/w) expressed in relation to the total weight of the composition.

21. The composition of claim 10 wherein the excipients is/are selected from superdisintegrants, glidants, antioxidants.

22. The composition of claim 21, wherein the superdisintegrant, if present, is selected from the group consisting of cross-linked polyvinylpyrrolidones, modified starches, and modified celluloses.

23. The composition of claim 11, wherein the superdisintegrant, if present, is present in an amount of 0.1 to 10% (w/w) expressed in relation to the total weight of the composition.

24. The composition of claim 21, wherein the glidant, if present, is selected from the group consisting of magnesium stearate and silica derivatives selected from colloidal silica, pyrogenic silica, hydrated sodium silicoaluminate, colloidal silicon dioxide, talcum and mixtures thereof.

25. The composition of claim 21, wherein the glidant, if present, is present in an amount of 0.01 to 10% (w/w) expressed in relation to the total weight of the composition.

26. The composition of claim 24, wherein the glidant, if present, is selected from magnesium stearate, colloidal silica or talcum.

27. A method for treating hyperphosphatemia, comprising the steps of orally administering a pharmaceutical composition comprising an effective phosphate-adsorbing amount of iron oxy-hydroxide in high loading of 10 to 80% (w/w) expressed in relation to the total weight of the pharmaceutical composition, and carbohydrates, said carbohydrates comprising saccharose and starch, in a form suitable for oral administration, wherein the amount of iron oxy-hydroxide per dosage form is at least 500 mg, to a patient in need thereof.

28. A method for treating patients with chronic renal insufficiency, comprising administering a pharmaceutical composition of claim 1 to a patient in need thereof.

29. The composition according to claim 1, wherein the iron oxy-hydroxide is essentially non-bioabsorbable.

30. The composition according to claim 1, having an iron release rate of below 2.5% w/w.

31. The composition according to claim 1, wherein the iron oxy-hydroxide is stabilized by a stabilization agent, which stabilization agent is not bound as a complex compound to the iron oxy-hydroxide.

32. The composition according to claim 1, which is a dosage form capable of disintegration in the oral cavity.

33. The composition according to claim 32, wherein dosage form is selected from chewable tablets.

34. The composition according to claim 1, wherein the oral dosage form is capable of rapid disintegration in the oral cavity or in a small amount of liquid prior to ingestion and wherein the iron oxy-hydroxide is present in an amount of 700 to 1700 mg per dosage form.

35. The composition according to claim 34, wherein the iron oxy-hydroxide is present in an amount of about 800 mg per dosage form.

36. The composition according to claim 1, which comprises a mixture of native and pregelatinized starch.

37. The composition according to claim 1, consisting of iron oxy-hydroxide, saccharose, starch, flavour, sweetener, and glidant.

38. A pharmaceutical composition according to claim 1, comprising a mixture of starches.

39. The composition according to claim 1, comprising up to 2000 mg iron oxy-hydroxide per dosage form.

40. The composition according to claim 1, comprising at least 700 mg iron oxy-hydroxide per dosage form.

41. The composition according to claim 40, comprising 700 to 2000 mg iron oxy-hydroxide per dosage form.

42. The method according to claim 15, comprising up to 2000 mg iron oxy-hydroxide per dosage form.

43. The method according to claim 15, comprising at least 700 mg iron oxy-hydroxide per dosage form.

44. The method according to claim 43, comprising 700 to 2000 mg iron oxy-hydroxide per dosage form.

45. The method according to claim 15, comprising 700 to 1700 mg iron oxy-hydroxide per dosage form.

46. The method according to claim 45, comprising about 800 mg iron oxy-hydroxide per dosage form.

47. The tablet according to claim 17, comprising up to 2000 mg iron oxy-hydroxide per dosage form.

48. The tablet according to claim 17, comprising at least 700 mg iron oxy-hydroxide per dosage form.

49. The tablet according to claim 48, comprising 700 to 2000 mg iron oxy-hydroxide per dosage form.

50. The tablet according to claim 17, comprising 700 to 1700 mg iron oxy-hydroxide per dosage form.

51. The tablet according to claim 50, comprising about 800 mg iron oxy-hydroxide per dosage form.

52. The method according to claim 27, comprising up to 2000 mg iron oxy-hydroxide per dosage form.

53. The method according to claim 27, comprising at least 700 mg iron oxy-hydroxide per dosage form.

54. The method according to claim 53, comprising 700 to 2000 mg iron oxy-hydroxide per dosage form.

55. The method according to claim 27, comprising 700 to 1700 mg iron oxy-hydroxide per dosage form.

56. The method according to claim 55, comprising about 800 mg iron oxy-hydroxide per dosage form.

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