Claims for Patent: 10,695,367

Summary for Patent: 10,695,367

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:	16/200,943
Patent Claims:	1. A pharmaceutical composition comprising iron oxy-hydroxide, saccharose, and starch, wherein the total amount of iron oxy-hydroxide, saccharose, and starch is greater than 70% (w/w) expressed relative 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 700 mg to 1700 mg. 2. The pharmaceutical composition according to claim 1, wherein the iron oxy-hydroxide is stabilized by at least saccharose and/or 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 the starch comprises native starch and pregelatinized starch. 8. The pharmaceutical composition according to claim 7 wherein the iron oxy-hydroxide is stabilized by at least saccharose, native starch, and/or pregelatinized starch. 9. The pharmaceutical composition according to claim 1, wherein the iron oxy-hydroxide comprises beta iron oxy-hydroxide. 10. The pharmaceutical composition according to claim 7, wherein native starch and pregelatinized starch are present in a ratio (native:pregelatinized) in the range of 10:1 to 0.5:1. 11. The pharmaceutical composition according to claim 7, wherein native starch and pregelatinized starch are present in a ratio (native:pregelatinized) in the range of 3:1 to 0.5:1. 12. The pharmaceutical composition according to claim 11, 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. 13. The pharmaceutical composition according to claim 11, 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. 14. The pharmaceutical composition according to claim 11, 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. 15. The pharmaceutical composition according to claim 11, 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. 16. The pharmaceutical composition according to claim 11, 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. 17. The pharmaceutical composition according to claim 11 wherein the iron oxy-hydroxide is stabilized by at least saccharose, native starch, and/or pregelatinized starch. 18. The pharmaceutical composition according to claim 7, wherein native starch and pregelatinized starch are present in a ratio (native:pregelatinized) in the range of 2:1 to 1:1. 19. The pharmaceutical composition according to claim 18, 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. 20. The pharmaceutical composition according to claim 18, 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. 21. The pharmaceutical composition according to claim 18, 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. 22. The pharmaceutical composition according to claim 21, wherein the iron oxy-hydroxide comprises beta iron oxy-hydroxide. 23. The pharmaceutical composition according to claim 18, 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. 24. The pharmaceutical composition according to claim 18, 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. 25. 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. 26. 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. 27. 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. 28. The pharmaceutical composition according to claim 27, wherein the iron oxy-hydroxide comprises beta iron oxy-hydroxide. 29. 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. 30. The pharmaceutical composition according to claim 29 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. 31. The pharmaceutical composition according to claim 30, 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. 32. 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. 33. The pharmaceutical composition according to claim 32, wherein the iron oxy-hydroxide comprises beta iron oxy-hydroxide. 34. The pharmaceutical composition according to claim 1, wherein the total amount of iron oxy-hydroxide, saccharose, and starch is greater than 90% (w/w) expressed relative to the total weight of the composition. 35. The pharmaceutical composition according to claim 34, wherein the iron oxy-hydroxide is stabilized by at least saccharose and/or starch. 36. The pharmaceutical composition according to claim 34 having an iron release rate of below 2.5% w/w. 37. The pharmaceutical composition according to claim 34, wherein the iron oxy-hydroxide is essentially non-bioabsorbable. 38. The pharmaceutical composition according to claim 34 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. 39. The pharmaceutical composition according to claim 38, 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. 40. The pharmaceutical composition according to claim 34, wherein the iron oxy-hydroxide comprises beta iron oxy-hydroxide. 41. The pharmaceutical composition according to claim 34, wherein the starch comprises native starch and pregelatinized starch. 42. The pharmaceutical composition according to claim 41 wherein the iron oxy-hydroxide is stabilized by at least saccharose, native starch, and/or pregelatinized starch. 43. The pharmaceutical composition according to claim 41, wherein native starch and pregelatinized starch are present in a ratio (native:pregelatinized) in the range of 3:1 to 0.5:1. 44. The pharmaceutical composition according to claim 43, 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. 45. The pharmaceutical composition according to claim 43, 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. 46. The pharmaceutical composition according to claim 43, 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. 47. The pharmaceutical composition according to claim 46, wherein the iron oxy-hydroxide comprises beta iron oxy-hydroxide. 48. The pharmaceutical composition according to claim 43, 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. 49. The pharmaceutical composition according to claim 43, 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. 50. The pharmaceutical composition according to claim 49, wherein the iron oxy-hydroxide comprises beta iron oxy-hydroxide. 51. The pharmaceutical composition according to claim 41, wherein native starch and pregelatinized starch are present in a ratio (native:pregelatinized) in the range of 2:1 to 1:1. 52. The pharmaceutical composition according to claim 51, 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. 53. The pharmaceutical composition according to claim 51, 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. 54. The pharmaceutical composition according to claim 51, 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. 55. The pharmaceutical composition according to claim 51, 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. 56. The pharmaceutical composition according to claim 51, 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. 57. The pharmaceutical composition according to claim 34, 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. 58. The pharmaceutical composition according to claim 34, 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. 59. The pharmaceutical composition according to claim 34, 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. 60. The pharmaceutical composition according to claim 59, wherein the iron oxy-hydroxide comprises beta iron oxy-hydroxide. 61. The pharmaceutical composition according to claim 34, 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. 62. The pharmaceutical composition according to claim 61 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. 63. The pharmaceutical composition according to claim 62, 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. 64. The pharmaceutical composition according to claim 61, wherein the iron oxy-hydroxide is stabilized by at least saccharose and/or starch. 65. The pharmaceutical composition according to claim 34, 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. 66. A pharmaceutical composition comprising iron oxy-hydroxide, saccharose, and starch, wherein the total amount of iron oxy-hydroxide, saccharose, and starch is about 87 to about 96% (w/w) expressed relative 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. 67. The pharmaceutical composition according to claim 66, wherein the iron oxy-hydroxide comprises beta iron oxy-hydroxide. 68. The pharmaceutical composition according to claim 66, wherein the iron oxy-hydroxide is stabilized by at least saccharose and/or starch. 69. The pharmaceutical composition according to claim 66 having an iron release rate of below 2.5% w/w. 70. The pharmaceutical composition according to claim 66, wherein the iron oxy-hydroxide is essentially non-bioabsorbable. 71. The pharmaceutical composition according to claim 66 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. 72. The pharmaceutical composition according to claim 71, 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. 73. The pharmaceutical composition according to claim 66, wherein the starch comprises native starch and pregelatinized starch. 74. The pharmaceutical composition according to claim 73, wherein the iron oxy-hydroxide comprises beta iron oxy-hydroxide. 75. The pharmaceutical composition according to claim 73 wherein the iron oxy-hydroxide is stabilized by at least saccharose, native starch, and/or pregelatinized starch. 76. The pharmaceutical composition according to claim 73, wherein native starch and pregelatinized starch are present in a ratio (native:pregelatinized) in the range of 3:1 to 0.5:1. 77. The pharmaceutical composition according to claim 76, 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. 78. The pharmaceutical composition according to claim 76, 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. 79. The pharmaceutical composition according to claim 76, 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. 80. The pharmaceutical composition according to claim 79, wherein the iron oxy-hydroxide comprises beta iron oxy-hydroxide. 81. The pharmaceutical composition according to claim 76, 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. 82. The pharmaceutical composition according to claim 76, 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. 83. The pharmaceutical composition according to claim 73, wherein native starch and pregelatinized starch are present in a ratio (native:pregelatinized) in the range of 2:1 to 1:1. 84. The pharmaceutical composition according to claim 83, 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. 85. The pharmaceutical composition according to claim 83, 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. 86. The pharmaceutical composition according to claim 83, 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. 87. The pharmaceutical composition according to claim 83, 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. 88. The pharmaceutical composition according to claim 83, 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. 89. The pharmaceutical composition according to claim 66, 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. 90. The pharmaceutical composition according to claim 66, 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. 91. The pharmaceutical composition according to claim 66, 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. 92. The pharmaceutical composition according to claim 91, wherein the iron oxy-hydroxide comprises beta iron oxy-hydroxide. 93. The pharmaceutical composition according to claim 66, 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. 94. The pharmaceutical composition according to claim 93 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. 95. The pharmaceutical composition according to claim 94, 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. 96. The pharmaceutical composition according to claim 93, wherein the iron oxy-hydroxide is stabilized by at least saccharose and/or starch. 97. The pharmaceutical composition according to claim 66, 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. 98. A pharmaceutical composition comprising iron oxy-hydroxide, saccharose, starch, and water, wherein the starch comprises 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 total amount of iron oxy-hydroxide, saccharose, starch, and water is about 93 to about 98% (w/w) expressed in relation to the total weight of the composition, wherein the pharmaceutical composition is in a form of a tablet, and wherein the amount of iron oxy-hydroxide per dosage form is about 800 mg. 99. The pharmaceutical composition according to claim 98 wherein the iron oxy-hydroxide is stabilized by at least saccharose, native starch, and/or pregelatinized starch. 100. The pharmaceutical composition according to claim 98 having an iron release rate of below 2.5% w/w. 101. The pharmaceutical composition according to claim 98, wherein the iron oxy-hydroxide is essentially non-bioabsorbable. 102. The pharmaceutical composition according to claim 98, wherein the iron oxy-hydroxide comprises beta iron oxy-hydroxide. 103. The pharmaceutical composition according to claim 98 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. 104. The pharmaceutical composition according to claim 103, 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. 105. The pharmaceutical composition according to claim 98, 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. 106. The pharmaceutical composition according to claim 98, 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, wherein native starch and pregelatinized starch are present in a ratio (native:pregelatinized) in the range of 2:1 to 1:1. 107. The pharmaceutical composition according to claim 1, 66, or 98, 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. 108. The pharmaceutical composition according to claim 107, 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. 109. The pharmaceutical composition according to claim 108, wherein the iron oxy-hydroxide is stabilized by at least saccharose and/or starch. 110. The pharmaceutical composition according to claim 108, 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. 111. The pharmaceutical composition according to claim 1, 66, or 98, further comprising at least one superdisintegrant chosen from cross-linked polyvinylpyrrolidones, modified starches, and modified cellulose. 112. The pharmaceutical composition according to claim 111, 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. 113. The pharmaceutical composition according to claim 112, wherein the iron oxy-hydroxide is stabilized by at least saccharose and/or starch. 114. The pharmaceutical composition according to claim 111, 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.