Compositions for delivery of reboxetine

Abstract

Described herein are methods for the administration of reboxetine, or a pharmaceutically acceptable salt thereof, to a human being in need thereof, resulting in a first maximum plasma concentration and a second maximum plasma concentration, wherein the two maxima are separated by a time period of about 2 hours to about 6 hours.

1 . A pharmaceutical product comprising a single dosage form and a label, wherein the single dosage form comprises a first release component and a second release component, wherein the first release component contains 1 mg to 10 mg of reboxetine, and the second release component contains 0.1 mg to 10 mg of reboxetine and is coated with a polymer that delays release of reboxetine in the second release component;
 wherein the single dosage form has a property that, when administered to a fasted human subject:   1) the reboxetine in the first release component provides a first local maximum in reboxetine plasma concentration, and   2) the reboxetine in the second release component provides a second local maximum in reboxetine plasma concentration,   wherein the first local maximum in reboxetine plasma concentration occurs about 2 hours to about 6 hours prior to the second local maximum in reboxetine plasma concentration; and   wherein the label states that the single dosage form is to be administered once a day.   
     
     
         2 . The pharmaceutical product of  claim 1 , wherein the polymer that delays release of reboxetine in the second release component comprises an acrylic acid or an acrylate polymer. 
     
     
         3 . The pharmaceutical product of  claim 1 , wherein the polymer that delays release of reboxetine in the second release component comprises a quaternary ammonium compound. 
     
     
         4 . The pharmaceutical product of  claim 1 , wherein the polymer that delays release of reboxetine in the second release component comprises a cellulose derivative. 
     
     
         5 . The pharmaceutical product of  claim 1 , wherein the first release component is free of any polymer that controls or delays release of reboxetine. 
     
     
         6 . The pharmaceutical product of  claim 1 , wherein the second release component comprises an inner core containing the reboxetine and the first release component comprises an outer coating layer containing the reboxetine. 
     
     
         7 . The pharmaceutical product of  claim 6 , wherein the polymer that delays release of reboxetine in the second release component is disposed between the inner core containing the reboxetine and the first release component. 
     
     
         8 . The pharmaceutical product of  claim 1 , wherein the first release component comprises a first controlled release layer and the second release component comprises a second controlled release layer, and the first controlled release layer and the second controlled release layer together form a bi-layer structure. 
     
     
         9 . The pharmaceutical product of  claim 8 , wherein the first controlled release layer provides immediate release of reboxetine. 
     
     
         10 . The pharmaceutical product of  claim 1 , wherein the first release component comprises a first release layer and the second release component comprises a second release layer, wherein the first release layer is not physically bound to the second release layer. 
     
     
         11 . The pharmaceutical product of  claim 10 , wherein the first release layer provides immediate release of reboxetine. 
     
     
         12 . The pharmaceutical product of  claim 1 , wherein the reboxetine is in the free base form. 
     
     
         13 . The pharmaceutical product of  claim 1 , wherein the reboxetine is in a salt form. 
     
     
         14 . The pharmaceutical product of  claim 1 , wherein the reboxetine is in the form of mesylate salt. 
     
     
         15 . The pharmaceutical product of  claim 1 , wherein the single dosage form is in the form of a pill, a tablet, a capsule, a caplet, or a cachou. 
     
     
         16 . The pharmaceutical product of  claim 1 , wherein the single dosage form further comprises a binder. 
     
     
         17 . The pharmaceutical product of  claim 1 , wherein the single dosage form further comprises a lubricant. 
     
     
         18 . The pharmaceutical product of  claim 1 , wherein the single dosage form further comprises an inert excipient. 
     
     
         19 . The pharmaceutical product of  claim 1 , wherein the first release component contains 3 mg to 7 mg of reboxetine. 
     
     
         20 . The pharmaceutical product of  claim 1 , wherein the second release component contains 0.1 mg to 7 mg of reboxetine.