PHARMACEUTICAL COMPOSITION COMPRISING POROUS DRY MATRIX

• US 20100036002A1
• Filed: 12/25/2007
• Published: 02/11/2010
• Est. Priority Date: 12/26/2006
• Status: Abandoned Application

• Current Assignee: MedRx Co., Ltd.
• Original Assignee: MedRx Co., Ltd.
• Inventors: Ishibashi, Masaki, Hamamoto, Hidetoshi, Kobayashi, Katsunori
• Application Number:
  US12/520,678
• Publication Number:
  US 20100036002A1
• Time in Patent Office: Days
• US Class Current: 514/781
• CPC Class Codes: A61K 31/795 Polymers containing sulfur
• CPC Class Codes: A61K 47/30 Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
• CPC Class Codes: A61K 9/2013 Organic compounds, e.g. phospholipids, fats
• CPC Class Codes: A61K 9/2018 Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
• CPC Class Codes: A61K 9/2027 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose

Abstract

The invention provides a porous dry matrix preparation comprising at least a polymeric thickener and an excipient ingredient, wherein (1) the content of the polymeric thickener is down to 0.5 w/w % and up to 14 w/w %, (2) the content of the excipient ingredient is down to 30 w/w % and up to 80 w/w %, (3) the void ratio is not less than 20%, and (4) the water activity is not more than 0.55, or water content is not more than 10 w/w %.

Claims

1-52. -52. (canceled)

53. A porous dry matrix preparation comprising at least a polymeric thickener and polystyrenesulfonate, wherein

(1) the content of the polymeric thickener is down to 0.5 w/w % and up to 14 w/w %,

(2) the content of the polystyrenesulfonate is down to 30 w/w % and up to 80 w/w %,

(3) the void ratio is not less than 20% and not more than 70%, and

(4) the water activity is not more than 0.55, or water content is not more than 10 w/w %.

54. The porous dry matrix preparation of claim 53, wherein the preparation completes water absorption within 15 minutes to become a hydrated composition that does not collapse when impregnated with water.

55. The porous dry matrix preparation of claim 53, wherein the polymeric thickener comprises carboxymethylcellulose and/or a salt thereof.

56. The porous dry matrix preparation of claim 55, wherein the carboxymethylcellulose salt is carboxymethylcellulose sodium or carboxymethylcellulose calcium.

57. The porous dry matrix preparation of claim 55, wherein the carboxymethylcellulose salt is carboxymethylcellulose sodium.

58. The porous dry matrix preparation of claim 53, wherein the polystyrenesulfonate is calcium polystyrenesulfonate or sodium polystyrenesulfonate.

59. The porous dry matrix preparation of claim 55, wherein the polystyrenesulfonate is calcium polystyrenesulfonate or sodium polystyrenesulfonate.

60. The porous dry matrix preparation of claim 53, wherein the void ratio is not less than 25%.

61. The porous dry matrix preparation of claim 54, wherein the void ratio is not less than 25%.

62. The porous dry matrix preparation of claim 53, comprising an edible oil/fat.

63. The porous dry matrix preparation of claim 53, comprising a sugar and/or a sugar alcohol.

64. The porous dry matrix preparation of claim 53, further comprising an edible oil/fat and a sugar and/or a sugar alcohol, wherein the polymeric thickener comprises carboxymethylcellulose and/or a salt thereof.

65. The porous dry matrix preparation of claim 53, further comprising an edible oil/fat and a sugar and/or a sugar alcohol, wherein the polymeric thickener comprises carboxymethylcellulose sodium, and the polystyrenesulfonate comprises calcium polystyrenesulfonate or sodium polystyrenesulfonate.

66. A method of producing the porous dry matrix preparation of claim 53, comprising subjecting a mixed composition obtained by mixing and molding at least a polymeric thickener, polystyrenesulfonate, and water to thermal drying under normal pressure, wherein the total content of the polymeric thickener and the polystyrenesulfonate before thermal drying is 15 w/w % to 45 w/w %, and wherein the water content before thermal drying is not less than 25 w/w %.

67. The production method of claim 66, wherein the polymeric thickener comprises carboxymethylcellulose and/or a salt thereof.

68. The production method of claim 67, wherein the carboxymethylcellulose salt is carboxymethylcellulose sodium or carboxymethylcellulose calcium.

69. The production method of claim 66, wherein the carboxymethylcellulose salt is carboxymethylcellulose sodium.

70. The production method of claim 67, wherein the polystyrenesulfonate is calcium polystyrenesulfonate or sodium polystyrenesulfonate.

71. The production method of claim 68, wherein the polystyrenesulfonate is calcium polystyrenesulfonate or sodium polystyrenesulfonate.

72. The production method of claim 66, wherein the void ratio is not less than 25%.

73. The production method of claim 66, wherein the mixed composition comprises an edible oil/fat.

74. The production method of claim 66, wherein the mixed composition comprises a sugar and/or a sugar alcohol.

75. The production method of claim 66, wherein the polymeric thickener comprises carboxymethylcellulose and/or a salt thereof, and the mixed composition comprises an edible oil/fat and a sugar and/or a sugar alcohol.

76. The production method of claim 66, wherein the polymeric thickener comprises carboxymethylcellulose sodium, the polystyrenesulfonate comprises calcium polystyrenesulfonate or sodium polystyrenesulfonate, and the mixed composition comprises an edible oil/fat and a sugar and/or a sugar alcohol.

77. The production method of claim 66, wherein the thermal drying under normal pressure is performed at a temperature of 100°

C. to 200°

C.

78. A method of producing the porous dry matrix preparation of claim 54, comprising subjecting a mixed composition obtained by mixing and molding at least a polymeric thickener, polystyrenesulfonate, and water to thermal drying under normal pressure, wherein the total content of the polymeric thickener and the polystyrenesulfonate before thermal drying is 15 w/w % to 45 w/w %, and wherein the water content before thermal drying is not less than 25 w/w %.

79. The production method of claim 78, wherein the polymeric thickener comprises carboxymethylcellulose and/or a salt thereof.

80. The production method of claim 78, wherein the carboxymethylcellulose salt is carboxymethylcellulose sodium.

81. The production method of claim 78, wherein the polystyrenesulfonate is calcium polystyrenesulfonate or sodium polystyrenesulfonate.