Abstract: A pharmaceutical formulation comprises: (a) a C.sub.12 -C.sub.24 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 C.sub.12 -C.sub.24 fatty acid is formulated for non-sustained release on non-parenteral administration and a portion of the C.sub.12 -C.sub.24 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 absorption redistribution of the active substance(s) from the hepatic portal blood supply to the lymphatic system, thereby avoiding first-pass liver metabolism.