PARTICLE FORMULATIONS FOR USE IN PHARMACEUTICAL COMPOSITIONS

• US 20110208168A1
• Filed: 04/21/2011
• Published: 08/25/2011
• Est. Priority Date: 12/19/2002
• Status: Active Grant

• Current Assignee: Intarcia Therapeutics, Inc.
• Original Assignee: Intarcia Therapeutics, Inc.
• Inventors: Zhang, Yuanpeng, Eliaz, Rom Ezer, Junnarkar, Gunjan, Weeks, Eric William, Rohloff, Catherine Manya
• Granted Patent: US 8,398,967 B2
• Time in Patent Office: Days
• US Class Current: 604/892.1
• CPC Class Codes: A61K 31/519 ortho- or peri-condensed with heterocyclic rings
• CPC Class Codes: A61K 38/21 Interferons [IFN]
• CPC Class Codes: A61K 9/0004 Osmotic delivery systems; Sustained release driven by osmosis, thermal energy or gas
• CPC Class Codes: A61K 9/1075 Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers A61K9/0026 takes precedence
• CPC Class Codes: A61K 9/1617 Organic compounds, e.g. phospholipids, fats
• CPC Class Codes: A61K 9/1623 Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: A61P 5/06 of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH

Abstract

A liquid composition in an osmotic drug delivery system and a dosage form in an osmotic drug delivery system is disclosed comprising an amphiphilic molecule, a non-aqueous liquid solvent, and a pharmaceutically active agent.

Claims

1-83. -83. (canceled)

84. A particle formulation for use in a pharmaceutical composition comprising a protein or peptide, sucrose, methionine, and citrate buffer.

85. The particle formulation of claim 84, wherein said protein or peptide is selected from the group consisting of interferon, erythropoietin, human growth hormone, granulocyte macrophage colony stimulating factor, human growth hormone releasing hormone, insulin, infliximab, and glucagon-like peptide-1.

86. The particle formulation of claim 85, wherein the protein or peptide is glucagon-like peptide-1.

87. The particle formulation of claim 85, wherein the protein or peptide is an interferon.

88. The particle formulation of claim 87, wherein the interferon is selected from the group consisting of omega-interferon, alpha-interferon, beta-interferon, and gamma-interferon.

89. The particle formulation of claim 84, wherein the particle formulation comprises the protein or peptide, sucrose, methionine, and citrate buffer in a weight ratio of 1:

2;

1;

2.15.

90. The particle formulation of claim 84, wherein particles of the formulation are made by spray-drying, lyophilization, or supercritical fluid processing.

91. The particle formulation of claim 84, wherein the particle formulation comprises spray-dried particles.

92. The particle formulation of claim 91, wherein the particle size is from about 1 μ

m to about 10 μ

m in diameter.

93. An implantable osmotic delivery device, comprising

a capsule having a first chamber containing a viscous liquid pharmaceutical composition and a second chamber containing an osmotic agent, the first chamber having an opening through which the pharmaceutical composition can be delivered from the first chamber to a location external of the first chamber;

a movable piston positioned in the capsule between the first chamber and the second chamber;

a wall of the second chamber comprising a fluid permeable membrane portion;

and an incompressible fluid additive located within the second chamber and substantially surrounding the osmotic agent;

wherein the viscous liquid pharmaceutical composition comprises the particle formulation of claim 84 dispersed in a suspending vehicle, and the suspending vehicle comprising a solvent selected from the group consisting of benzyl benzoate, lauryl lactate, and lauryl alcohol.

94. The implantable osmotic delivery device of claim 93, wherein the solvent is benzyl benzoate.

95. The implantable osmotic delivery device of claim 93, wherein the solvent is lauryl lactate.

96. The implantable osmotic delivery device of claim 93, wherein the solvent is lauryl alcohol.

97. The implantable osmotic delivery device of claim 93, wherein the suspending vehicle further comprises a lipid.

98. The implantable osmotic delivery device of claim 93, wherein the particle formulation comprises the protein or peptide, sucrose, methionine, and citrate buffer in a weight ratio of 1:

2;

1;

2.15.

99. The implantable osmotic delivery device of claim 93, wherein particles of the formulation are made by spray-drying, lyophilization, or supercritical fluid processing.

100. The implantable osmotic delivery device of claim 93, wherein the particle formulation comprises spray-dried particles.

101. The implantable osmotic delivery device of claim 100, wherein the particle size is from about 1 μ

m to about 10 μ

m in diameter.

102. The implantable osmotic delivery device of claim 93, wherein the osmotic agent is a tablet comprising NaCl.

103. The implantable osmotic delivery device of claim 102, wherein the incompressible fluid additive comprises PEG.