Solid pharmaceutical compositions containing benzofuran derivatives

Abstract

The present invention relates to a solid pharmaceutical composition for oral administration characterized in that it comprises a benzofuran derivative with antiarrhythmic activity, or one of the pharmaceutically acceptable salts thereof, as an active principle, and a pharmaceutically acceptable nonionic hydrophilic surfactant optionally in combination with one or more pharmaceutical excipients.

What is claimed is: 
     
         1 . A solid pharmaceutical composition for oral administration comprising dronedarone, or a pharmaceutically acceptable salt thereof, as an active principle, and a pharmaceutically acceptable nonionic hydrophilic surfactant optionally in combination with one or more pharmaceutical excipients, wherein said pharmaceutical composition has a pharmacokinetic profile wherein the maximum plasmatic concentration of active principle following a single oral administration in a non-fasted human is less than about five times the maximum concentration of active principle following a single oral administration in a fasted human. 
     
     
         2 . The pharmaceutical composition according to  claim 1 , wherein the active principle is dronedarone hydrochloride. 
     
     
         3 . The pharmaceutical composition according to  claim 1 , wherein the nonionic hydrophilic surfactant is selected from the group consisting of poloxamer 124, poloxamer 188, poloxamer 237, poloxamer 338, poloxamer 407, and polyethylene hydroxystearate 660. 
     
     
         4 . The pharmaceutical composition according to  claim 1 , wherein the nonionic hydrophilic surfactant is poloxamer 407. 
     
     
         5 . The pharmaceutical composition according to  claim 1 , which is in a tablet or a gelatin capsule form, wherein the nonionic hydrophilic surfactant is present in a proportion of from 1% to 50% by weight of the active principle in base form. 
     
     
         6 . A solid pharmaceutical composition for oral administration comprising dronedarone, or a pharmaceutically acceptable salt thereof, as an active principle, and a pharmaceutically acceptable nonionic hydrophilic surfactant optionally in combination with one or more pharmaceutical excipients, wherein said pharmaceutical composition exhibits a mean AUC of the active principle following a single oral administration in a non-fasted human which is less than about five times the mean AUC of the active principle following a single oral administration of the pharmaceutical composition in a fasted human. 
     
     
         7 . The pharmaceutical composition according to  claim 6 , wherein the active principle is dronedarone hydrochloride. 
     
     
         8 . The pharmaceutical composition according to  claim 6 , wherein the nonionic hydrophilic surfactant is selected from the group consisting of poloxamer 124, poloxamer 188, poloxamer 237, poloxamer 338, poloxamer 407, and polyethylene hydroxystearate 660. 
     
     
         9 . The pharmaceutical composition according to  claim 6 , wherein the nonionic hydrophilic surfactant is poloxamer 407. 
     
     
         10 . The pharmaceutical composition according to  claim 6 , which is in a tablet or a gelatin capsule form, wherein the nonionic hydrophilic surfactant is present in a proportion of from 1% to 50% by weight of the active principle in base form. 
     
     
         11 . A solid pharmaceutical composition for oral administration comprising 200 to 400 mg of dronedarone hydrochloride, calculated in base form, and poloxamer 407, optionally in combination with one or more pharmaceutical excipients. 
     
     
         12 . A method of treating a patient comprising orally administering a solid pharmaceutical composition comprising dronedarone, or a pharmaceutically acceptable salt thereof, as an active principle, and a pharmaceutically acceptable nonionic hydrophilic surfactant optionally in combination with one or more pharmaceutical excipients, wherein the bioavailability of the composition following a single oral administration in the not fasted state is less than about five times the bioavailability of the composition following a single oral administration in the fasted state. 
     
     
         13 . The method according to  claim 12 , wherein the active principle is dronedarone hydrochloride.