Controlled release oxycodone compositions

Abstract

A method for substantially reducing the range in daily dosages required to control pain in approximately 90% of patients is disclosed whereby an oral solid controlled release dosage formulation having from about 10 to about 40 mg of oxycodone or a salt thereof is administered to a patient. The formulation provides a mean maximum plasma concentration of oxycodone from about 6 to about 60 ng/ml from a mean of about 2 to about 4.5 hours after administration, and a mean minimum plasma concentration from about 3 to about 30 ng/ml from about 10 to about 14 hours after repeated “q12h” (i.e., every 12 hour) administration through steady-state conditions. Another embodiment is directed to a method for substantially reducing the range in daily dosages required to control pain in substantially all patients by administering an oral solid controlled release dosage formulation comprising up to about 160 mg of oxycodone or a salt thereof, such that a mean maximum plasma concentration of oxycodone up to about 2.40 ng/ml from a mean of up to about 2 to about 4.5 hours after administration, and a mean minimum plasma concentration up to about 120 ng/ml from about 10 to about 14 hours after repeated “q12h” (i.e., every 12 hour) administration through steady-state conditions are achieved. Controlled release oxycodone formulations for achieving the above are also disclosed.

1 . A process for the preparation of a controlled release oral dosage form comprising: 
 (a) forming granules comprising oxycodone hydrochloride, alkyl cellulose and polymethacrylate, and    (b) drying said granules.    
     
     
         2 . The process of  claim 1 , further comprising adding aliphatic alcohol and regranulating and compressing said granules into tablets.  
     
     
         3 . The process of  claim 1 , wherein said granules are dried at 50° C.  
     
     
         4 . A process for the preparation of a controlled release oral dosage form comprising: 
 (a) forming spheroids comprising oxycodone hydrochloride, spheronising agent, alkyl cellulose and polymethacrylate and    drying said spheroids    
     
     
         5 . The process of  claim 4 , where the spheronising agent is microcrystalline cellulose.  
     
     
         6 . The process of  claim 4 , further comprising film coating said spheroids.  
     
     
         7 . A process for the preparation of a controlled release oral dosage form comprising: 
 (a) wet granulating oxycodone hydrochloride, alkyl cellulose and polymethacrylate to form granules of said oxycodone hydrochloride,    (b) drying said granules,    (c) adding aliphatic alcohol,    (d) regranulating and compressing said granules into tablets.