Biphasic release formulations for lipophilic drugs

Details Biphasic release formulations for lipophilic drugs Biphasic release formulations for lipophilic drugs

A - Human Necessities

61

K

A61K 47/12 (2006.01) A61K 9/22 (2006.01) A61K 9/48 (2006.01) A61K 9/52 (2006.01)

Patent

CA 2093206

A pharmaceutical formulation comprises: (a) a C12-C24 fatty acid, which may be saturated or mono- or poly-unsaturated, such as oleic or linoleic acid; and (b) a generally lipophilic pharmaceutically active substance. A portion of the C12-C24 fatty acid is formulated for non- sustained release on non-parenteral administration and a portion of the C12-C24 fatty acid and at least a portion of the pharmaceutically active substance are formulated for sustained release on non-parenteral administration. The pharmaceutically active substance may be a cardiovascular drug such as propranolol, verapamil, nifedipine, diltiazem, metoprolol, nicardipine or labetolol. Such formulations promote absorbtion redistribution of the active substance(s) from the hepatic portal blood supply to the lymphatic system, thereby avoiding first-pass liver metabolism. Formulations of this type will have a predictable dose response in patients, achieved with a lower chemical load, with which therapeutic efficacy is maintained.

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