Darusentan oral dosage form

A - Human Necessities – 61 – K

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A61K 9/20 (2006.01) A61K 31/505 (2006.01)

Patent

CA 2668724

A solid discrete orally deliverable pharmaceutical dosage form comprises darusentan and one or more pharmaceutically acceptable excipients; wherein (a) the darusentan is in solid particulate form having a mean particle size of about 5 to about 200 µm and is present in the dosage form in an amount of about 1 to about 600 mg; and (b) the dosage form exhibits at least about 90% dissolution of the darusentan in 30 minutes in a standard in vitro dissolution test. A method for lowering blood pressure, for example in a patient having resistant hypertension, comprises administering such a dosage form once daily to the patient.

L'invention concerne une forme posologique pharmaceutique solide et discrète à administration orale qui comprend du darusentan et un ou plusieurs excipients pharmaceutiquement acceptable. Dans cette forme de dosage: (a) le darusentan est sous forme de particules solides à dimension de particule moyenne comprise entre environ 5 à 200 µm et est présent dans la forme posologique en quantité comprise entre environ 1 et 600 mg; et (b) la forme posologique présente au moins environ 90% de dissolution du darusentan en 30 minutes dans un test de dissolution in vitro standard. L'invention concerne également un procédé destiné à réduire la pression sanguine, par exemple chez un patient souffrant d'hypertension résistante, qui consiste à administrer quotidiennement une telle forme posologique au patient.

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