Abstract: The present invention relates to formulations comprising therapeutically effective amounts of at least one acid-stable, carrier-mediated transport statin, at least one poorly water-soluble, carrier-mediated transport statin, or at least one large molecular weight, carrier-mediated transport statin, such as atorvastatin and rosuvastatin, or a pharmaceutically acceptable salt thereof, and methods of their use. The present formulations and methods are designed to exhibit a controlled-release of a therapeutic amount of the statin in the small intestine, thereby limiting systemic exposure of the statin and maximizing liver-specific absorption of the drug. The formulations and methods of the present invention are particularly useful for treating and/or preventing conditions that are benefited by decreasing levels of lipids and/or cholesterol in the body.

Abstract: Chronotherapeutic formulations of cardiovascular drugs are disclosed. The formulations comprise at least one cardiovascular drug that exhibits an in vivo elimination half-life of less than about 8 hours; wherein the formulation exhibits the following in vivo profile following administration to a subject: a) a delay in release of therapeutic levels of the at least one drug for about 2 to about 8 hours; b) a Tmax at about 8 to about 12 hours; c) a drug plasma level within 50% of the peak for greater than or equal to 12 hours; and d) a peak-to-trough ratio of drug plasma levels greater than or equal to about 4.