Claims for Patent: 10,682,376

Summary for Patent: 10,682,376

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 (Arbon, CH)
Assignee:	Vifor Fresenius Medical Care Renal Pharma Ltd (St. Gallen, CH)
Application Number:	16/170,650
Patent Claims:	1. A pharmaceutical composition comprising iron oxy-hydroxide, saccharose, native starch, and pregelatinized starch, wherein the iron oxy-hydroxide is present in an amount of 10 to 80% (w/w) expressed in relation to the total weight of the composition, wherein the pharmaceutical composition is in a form of a chewable tablet for oral administration, and wherein the amount of iron oxy-hydroxide per dosage form is 700 mg to 1700 mg. 2. The pharmaceutical composition according to claim 1 wherein the iron oxy-hydroxide is stabilized by at least saccharose, native starch, and/or pregelatinized starch. 3. The pharmaceutical composition according to claim 1 having an iron release rate of below 2.5% w/w. 4. The pharmaceutical composition according to claim 1, wherein the iron oxy-hydroxide is essentially non-bioabsorbable. 5. The pharmaceutical composition according to claim 1 further comprising at least one additional component chosen from flavouring agents, sweeteners, taste-enhancing agents, and coloring agents, and optionally at least one excipient chosen from superdisintegrants, glidants, and antioxidants. 6. The pharmaceutical composition according to claim 5, wherein the sweeteners, if present, is/are present in an amount of 0.01 to 2.5% (w/w), wherein the taste-enhancing agents, if present, is/are present in an amount of 0.1 to 50 ppm, wherein the flavouring agents, if present, is/are present in an amount of 0.01 to 10% (w/w), wherein the superdisintegrants, if present, is/are present in an amount of 0.1 to 10% (w/w), and/or wherein the glidants, if present, is/are present in an amount of 0.01 to 10% (w/w), each expressed in relation to the total weight of the composition. 7. The pharmaceutical composition according to claim 1, wherein native starch and pregelatinized starch are present in a ratio (native:pregelatinized) in the range of 10:1 to 0.5:1. 8. The pharmaceutical composition according to claim 1, wherein native starch and pregelatinized starch are present in a ratio (native:pregelatinized) in the range of 3:1 to 0.5:1. 9. The pharmaceutical composition according to claim 8 wherein the iron oxy-hydroxide is stabilized by at least saccharose, native starch, and/or pregelatinized starch. 10. The pharmaceutical composition according to claim 1, wherein native starch and pregelatinized starch are present in a ratio (native:pregelatinized) in the range of 2:1 to 1:1. 11. The pharmaceutical composition according to claim 1, wherein the iron oxy-hydroxide is present in an amount of 30 to 65% (w/w) expressed in relation to the total weight of the composition. 12. The pharmaceutical composition according to claim 11, wherein native starch and pregelatinized starch are present in a ratio (native:pregelatinized) in the range of 10:1 to 0.5:1. 13. The pharmaceutical composition according to claim 11, wherein native starch and pregelatinized starch are present in a ratio (native:pregelatinized) in the range of 3:1 to 0.5:1. 14. The pharmaceutical composition according to claim 11, wherein native starch and pregelatinized starch are present in a ratio (native:pregelatinized) in the range of 2:1 to 1:1. 15. The pharmaceutical composition according to claim 1, wherein the iron oxy-hydroxide is present in an amount of about 30 to about 35% (w/w) expressed in relation to the total weight of the composition. 16. The pharmaceutical composition according to claim 15, wherein the iron oxy-hydroxide comprises beta iron oxy-hydroxide. 17. The pharmaceutical composition according to claim 15, wherein native starch and pregelatinized starch are present in a ratio (native:pregelatinized) in the range of 10:1 to 0.5:1. 18. The pharmaceutical composition according to claim 15, wherein native starch and pregelatinized starch are present in a ratio (native:pregelatinized) in the range of 3:1 to 0.5:1. 19. The pharmaceutical composition according to claim 15, wherein native starch and pregelatinized starch are present in a ratio (native:pregelatinized) in the range of 2:1 to 1:1. 20. The pharmaceutical composition according to claim 1, wherein the iron oxy-hydroxide is present in an amount of about 27 to about 35% (w/w) expressed in relation to the total weight of the composition. 21. The pharmaceutical composition according to claim 20, wherein the iron oxy-hydroxide comprises beta iron oxy-hydroxide. 22. The pharmaceutical composition according to claim 20, wherein native starch and pregelatinized starch are present in a ratio (native:pregelatinized) in the range of 10:1 to 0.5:1. 23. The pharmaceutical composition according to claim 20, wherein native starch and pregelatinized starch are present in a ratio (native:pregelatinized) in the range of 3:1 to 0.5:1. 24. The pharmaceutical composition according to claim 20, wherein native starch and pregelatinized starch are present in a ratio (native:pregelatinized) in the range of 2:1 to 1:1. 25. The pharmaceutical composition according to claim 1, wherein the iron oxy-hydroxide is present in an amount of about 29 to about 32% (w/w) expressed in relation to the total weight of the composition. 26. The pharmaceutical composition according to claim 25, wherein the iron oxy-hydroxide comprises beta iron oxy-hydroxide. 27. The pharmaceutical composition according to claim 25 further comprising at least one additional component chosen from flavouring agents, sweeteners, taste-enhancing agents, and coloring agents, and optionally at least one excipient chosen from superdisintegrants, glidants, and antioxidants. 28. The pharmaceutical composition according to claim 27, wherein the sweeteners, if present, is/are present in an amount of 0.01 to 2.5% (w/w), wherein the taste-enhancing agents, if present, is/are present in an amount of 0.1 to 50 ppm, wherein the flavouring agents, if present, is/are present in an amount of 0.01 to 10% (w/w), wherein the superdisintegrants, if present, is/are present in an amount of 0.1 to 10% (w/w), and/or wherein the glidants, if present, is/are present in an amount of 0.01 to 10% (w/w), each expressed in relation to the total weight of the composition. 29. The pharmaceutical composition according to claim 25, wherein native starch and pregelatinized starch are present in a ratio (native:pregelatinized) in the range of 10:1 to 0.5:1. 30. The pharmaceutical composition according to claim 25, wherein native starch and pregelatinized starch are present in a ratio (native:pregelatinized) in the range of 3:1 to 0.5:1. 31. The pharmaceutical composition according to claim 30 wherein the iron oxy-hydroxide is stabilized by at least saccharose, native starch, and/or pregelatinized starch. 32. The pharmaceutical composition according to claim 30 further comprising at least one additional component chosen from flavouring agents, sweeteners, taste-enhancing agents, and coloring agents, and optionally at least one excipient chosen from superdisintegrants, glidants, and antioxidants. 33. The pharmaceutical composition according to claim 32, wherein the sweeteners, if present, is/are present in an amount of 0.01 to 2.5% (w/w), wherein the taste-enhancing agents, if present, is/are present in an amount of 0.1 to 50 ppm, wherein the flavouring agents, if present, is/are present in an amount of 0.01 to 10% (w/w), wherein the superdisintegrants, if present, is/are present in an amount of 0.1 to 10% (w/w), and/or wherein the glidants, if present, is/are present in an amount of 0.01 to 10% (w/w), each expressed in relation to the total weight of the composition. 34. The pharmaceutical composition according to claim 25, wherein native starch and pregelatinized starch are present in a ratio (native:pregelatinized) in the range of 2:1 to 1:1. 35. The pharmaceutical composition according to claim 1, wherein the iron oxy-hydroxide is present in an amount of about 27 to about 32% (w/w) expressed in relation to the total weight of the composition. 36. The pharmaceutical composition according to claim 35, wherein the iron oxy-hydroxide comprises beta iron oxy-hydroxide. 37. The pharmaceutical composition according to claim 35, wherein native starch and pregelatinized starch are present in a ratio (native:pregelatinized) in the range of 10:1 to 0.5:1. 38. The pharmaceutical composition according to claim 35, wherein native starch and pregelatinized starch are present in a ratio (native:pregelatinized) in the range of 3:1 to 0.5:1. 39. The pharmaceutical composition according to claim 35, wherein native starch and pregelatinized starch are present in a ratio (native:pregelatinized) in the range of 2:1 to 1:1. 40. A pharmaceutical composition comprising iron oxy-hydroxide, saccharose, and starch, wherein the iron oxy-hydroxide is present in an amount of 10 to 80% (w/w) expressed in relation to the total weight of the composition, wherein the pharmaceutical composition is in a form of a chewable tablet, and wherein the amount of iron oxy-hydroxide per tablet is about 800 mg. 41. The pharmaceutical composition according to claim 40, wherein the iron oxy-hydroxide is stabilized by at least saccharose and/or starch. 42. The pharmaceutical composition according to claim 40 having an iron release rate of below 2.5% w/w. 43. The pharmaceutical composition according to claim 40, wherein the iron oxy-hydroxide is essentially non-bioabsorbable. 44. The pharmaceutical composition according to claim 40 further comprising at least one additional component chosen from flavouring agents, sweeteners, taste-enhancing agents, and coloring agents, and optionally at least one excipient chosen from superdisintegrants, glidants, and antioxidants. 45. The pharmaceutical composition according to claim 44, wherein the sweeteners, if present, is/are present in an amount of 0.01 to 2.5% (w/w), wherein the taste-enhancing agents, if present, is/are present in an amount of 0.1 to 50 ppm, wherein the flavouring agents, if present, is/are present in an amount of 0.01 to 10% (w/w), wherein the superdisintegrants, if present, is/are present in an amount of 0.1 to 10% (w/w), and/or wherein the glidants, if present, is/are present in an amount of 0.01 to 10% (w/w), each expressed in relation to the total weight of the composition. 46. The pharmaceutical composition according to claim 40, wherein the iron oxy-hydroxide is present in an amount of 30 to 65% (w/w) expressed in relation to the total weight of the composition. 47. The pharmaceutical composition according to claim 40, wherein the iron oxy-hydroxide is present in an amount of about 30 to about 35% (w/w) expressed in relation to the total weight of the composition. 48. The pharmaceutical composition according to claim 40, wherein the iron oxy-hydroxide is present in an amount of about 27 to about 35% (w/w) expressed in relation to the total weight of the composition. 49. The pharmaceutical composition according to claim 48, wherein the iron oxy-hydroxide comprises beta iron oxy-hydroxide. 50. The pharmaceutical composition according to claim 40, wherein the iron oxy-hydroxide is present in an amount of about 29 to about 32% (w/w) expressed in relation to the total weight of the composition. 51. The pharmaceutical composition according to claim 50 further comprising at least one additional component chosen from flavouring agents, sweeteners, taste-enhancing agents, and coloring agents, and optionally at least one excipient chosen from superdisintegrants, glidants, and antioxidants. 52. The pharmaceutical composition according to claim 51, wherein the sweeteners, if present, is/are present in an amount of 0.01 to 2.5% (w/w), wherein the taste-enhancing agents, if present, is/are present in an amount of 0.1 to 50 ppm, wherein the flavouring agents, if present, is/are present in an amount of 0.01 to 10% (w/w), wherein the superdisintegrants, if present, is/are present in an amount of 0.1 to 10% (w/w), and/or wherein the glidants, if present, is/are present in an amount of 0.01 to 10% (w/w), each expressed in relation to the total weight of the composition. 53. The pharmaceutical composition according to claim 50, wherein the iron oxy-hydroxide is stabilized by at least saccharose and/or starch. 54. The pharmaceutical composition according to claim 40, wherein the iron oxy-hydroxide is present in an amount of about 27 to about 32% (w/w) expressed in relation to the total weight of the composition. 55. The pharmaceutical composition according to claim 54 further comprising at least one additional component chosen from flavouring agents, sweeteners, taste-enhancing agents, and coloring agents, and optionally at least one excipient chosen from superdisintegrants, glidants, and antioxidants. 56. The pharmaceutical composition according to claim 55, wherein the sweeteners, if present, is/are present in an amount of 0.01 to 2.5% (w/w), wherein the taste-enhancing agents, if present, is/are present in an amount of 0.1 to 50 ppm, wherein the flavouring agents, if present, is/are present in an amount of 0.01 to 10% (w/w), wherein the superdisintegrants, if present, is/are present in an amount of 0.1 to 10% (w/w), and/or wherein the glidants, if present, is/are present in an amount of 0.01 to 10% (w/w), each expressed in relation to the total weight of the composition. 57. The pharmaceutical composition according to claim 54, wherein the iron oxy-hydroxide is stabilized by at least saccharose and/or starch. 58. The pharmaceutical composition according to claim 1 or 40, further comprising at least one glidant chosen from magnesium stearate and silica derivatives, wherein said silica derivatives are chosen from colloidal silica, pyrogenic silica, hydrated sodium silicoaluminate, colloidal silicon dioxide, and talcum. 59. The pharmaceutical composition according to claim 58, wherein the glidants is/are present in an amount of 0.1 to 5% (w/w) expressed in relation to the total weight of the composition. 60. The pharmaceutical composition according to claim 59, wherein the iron oxy-hydroxide is stabilized by at least saccharose and/or starch. 61. The pharmaceutical composition according to claim 59, wherein the glidants is/are present in an amount of 1 to 2% (w/w) expressed in relation to the total weight of the composition. 62. The pharmaceutical composition according to claim 1 or 40, further comprising at least one superdisintegrant chosen from cross-linked polyvinylpyrrolidones, modified starches, and modified cellulose. 63. The pharmaceutical composition according to claim 62, wherein the superdisintegrants is/are present in an amount of 0.5 to 8% (w/w) expressed in relation to the total weight of the composition. 64. The pharmaceutical composition according to claim 63, wherein the iron oxy-hydroxide is stabilized by at least saccharose and/or starch. 65. The pharmaceutical composition according to claim 62, further comprising at least one glidant chosen from magnesium stearate and silica derivatives, wherein said silica derivatives are chosen from colloidal silica, pyrogenic silica, hydrated sodium silicoaluminate, colloidal silicon dioxide, and talcum.