IMMEDIATE-RELEASE TABLET FORMULATIONS OF A THROMBIN RECEPTOR ANTAGONIST
First Claim
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1. A solid pharmaceutical formulation for oral administration comprising COMPOUND 1 or a pharmaceutically acceptable salt or solvate thereof and at least one disintegrant, wherein the amount of COMPOUND 1 is less than about 10% of the weight of the formulation.
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Abstract
Immediate-release formulations for oral administration of a thrombin receptor antagonist are provided. Certain formulations of higher API loading demonstrate sufficient moisture uptake after storage at stressed conditions to retard dissolution. The formulations of the present invention incorporate either lower API loading or elevated disintegrant-to-API ratios, found necessary to achieve disintegration rates required for immediate-release performance.
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Citations
38 Claims
- 1. A solid pharmaceutical formulation for oral administration comprising COMPOUND 1 or a pharmaceutically acceptable salt or solvate thereof and at least one disintegrant, wherein the amount of COMPOUND 1 is less than about 10% of the weight of the formulation.
- 25. A solid pharmaceutical formulation for oral administration comprising about 40 mg of Compound 1 or a pharmaceutically acceptable salt thereof and at least about 5 wt percent of a disintegrant.
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29. A solid pharmaceutical formulation for oral administration comprising:
Ingredient Amount (mg) COMPOUND 1 Bisulfate 40 Lactose Monohydrate 383 Microcrystalline Cellulose 120 Croscarmellose Sodium 36 Povidone 18 Magnesium Stearate 3.
- 30. A solid pharmaceutical formulation for oral administration comprising about 2.5 mg of Compound 1 or a pharmaceutically acceptable salt thereof and at least about 5 weight percent of a disintegrant.
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34. A solid pharmaceutical formulation for oral administration comprising:
Ingredient Amount (mg) COMPOUND 1 Bisulfate 2.5 Lactose Monohydrate 68 Microcrystalline Cellulose 20 Croscarmellose Sodium 6 Povidone 3 Magnesium Stearate 0.5.
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35. An immediate-release tablet formulation of a thrombin receptor antagonist that results in a 30-minute dissolution of said thrombin receptor antagonist of at least about 80%, wherein said thrombin receptor antagonist is selected from the group consisting of:
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or a pharmaceutically acceptable isomer, salt or solvate thereof.
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Specification