Chronotherapeutic formulations of diltiazem and the...

A - Human Necessities – 61 – K

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A61K 31/554 (2006.01) A61K 9/16 (2006.01) A61K 9/22 (2006.01) A61K 9/50 (2006.01) A61K 9/52 (2006.01) A61K 31/55 (2006.01) A61P 9/00 (2006.01)

Patent

CA 2292247

A controlled-release Galenical preparation of pharmaceutically acceptable Diltiazem including the pharmaceutically acceptable salts thereof, suitable for evening dosing every 24 hours containing from about 120 mg to about 540 mg or more of the form of Diltiazem with excipients to provide controlled (sustained) release of the form of Diltiazem from the preparation for providing a Cmax of Diltiazem in the blood at between about 10 hours and about 15 hours (Tmax) after administration of the preparation, the preparation being in a sustained- release dosage form in which the Diltiazem is adapted to be control released after administration of the preparation over a period of time and being adapted to release the Diltiazem (i) into an aqueous medium at the following rates measured using the method of United States Pharmacopoeia No. XXIII at 100 rpm in 900 ml of water: (a) between about 1% and about 15% after 2 hours; (b) between about 7% and about 35% after 4 hours; (c) between about 30% and about 58% after 8 hours; (d) between about 55% and about 80% after 14 hours; and (e) and in excess of about 75% after 24 hours. and/or (ii) into a buffered medium having a pH between about 5.5 and about 6.5, at the following rates measured using the method of United States Pharmacopoeia No. XXIII at 100 rpm in 900ml of the buffered medium: (a) between about 1% and about 25% after about 2 hours; (b) between about 7% and about 45% after about 4 hours; (c) between about 30% and about 68% after about 8 hours; (d) in excess of about 75% after about 24 hours.

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