Formulations of thiophene compounds
AssigneeVertex Pharmaceuticals Incorporated
InventorsNicholas Cardoso, Chong-Hui Gu, Peter A. Ojakovo, Tapan Sanghvi, Eric A. Simone, Marinus J. Verwijs
Life of this patent
Estimating the term…
Abstract
A pharmaceutical composition comprises: a) polymorphic form M or tromethamine salt of Compound (1) represented by the following structural formula: and b) a filler. A method of preparing a pharmaceutical composition comprises: providing a mixture of Compound (1) and a filler to form the composition of Compound (1). A method of treating a HCV infection in a subject comprises administering to the subject a therapeutically effective amount of the pharmaceutical composition.
Claims78
A pharmaceutical composition comprising:
- a) polymorphic form M or tromethamine salt of Compound (1) represented by the following structural formula:
- and
- b) a filler.
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A pharmaceutical composition comprising polymorphic form M of Compound (1) by weight of the composition, wherein Compound (1) is represented by the following structural formula:
- wherein the composition has a dissolution rate represented by the following equation:
- dissolution
-
-
- rate
-
-
- (
-
- M
-
- t
- )
- =
- z
- ×
- M
- 0
-
- (
- M
- 0
- -
- M
- M
- 0
- )
- 2
- 3
- ×
- (
- C
- s
- -
- M
- V
- )
- wherein M is a dissolved mass of Compound (1), M0 is an initial mass of Compound (1), t is a dissolution time, Cs is a solubility of Compound (1) in a fed state simulated intestinal fluid, V is volume of the fed state simulated intestinal fluid, and z is a dissolution rate factor, wherein the composition has a z value greater than 0.025 ml/mg/minute.
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A pharmaceutical composition comprising:
- a) polymorphic form M or tromethamine salt of Compound (1) represented by the following structural formula:
- b) a complexing agent;
- and
- c) a buffering agent
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A method of preparing a pharmaceutical composition, comprising:
- providing a mixture that includes a polymorphic form M or tromethamine salt of Compound (1) and a filler to form the pharmaceutical composition, wherein Compound (1) is represented by the following structural formula:
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The method of 57, wherein the mixing of the binder solution and the pre-granulation composition includes feeding the pre-granulation composition into a twin screw extruder and introducing the binder solution into the twin screw extruder.
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Dependencies are inferred from the claim text.