Oxymorphone Controlled Release Formulations

Abstract

The invention pertains to a method of relieving pain by administering a controlled release pharmaceutical tablet containing oxymorphone which produces a mean minimum blood plasma level 12 to 24 hours after dosing, as well as the tablet producing the sustained pain relief.

1 . An analgesically effective controlled release composition of oxymorphone for oral delivery comprising a controlled release matrix with a release rate profile designed to provide an adequate blood plasma level of analgesic over at least 12 hours, about 5 mg to 80 mg of oxymorphone or a pharmaceutically acceptable salt thereof as the sole active ingredient, and wherein upon oral administration the blood plasma concentration of oxymorphone comprises a first peak between about 0.5-4 hours after administration and a second peak between about 4-8 hours after administration. 
     
     
         2 . A composition according to  claim 1 , wherein the oral administration to the subject occurs under fasting conditions. 
     
     
         3 . A composition according to  claim 1 , wherein the oral administration to the subject occurs under fed conditions. 
     
     
         4 . A composition according to  claim 1 , wherein the time period between the first peak and the second peak is between about 2 to 3.5 hours. 
     
     
         5 . A composition according to  claim 1 , further comprising a third blood plasma concentration peak between about 10-14 hours after administration. 
     
     
         6 . A composition according to  claim 1 , wherein the first blood plasma concentration peak occurs between about 1-3 hours after administration. 
     
     
         7 . A composition according to  claim 1 , wherein the second blood plasma concentration peak occurs between about 5-7 hours after administration. 
     
     
         8 . A composition according to  claim 5 , wherein the third blood plasma concentration peak occurs at about 12 hours after administration. 
     
     
         9 . An analgesically effective controlled release composition of oxymorphone for oral delivery comprising a controlled release matrix with a release rate profile designed to provide an adequate blood plasma level of analgesic over at least 12 hours, about 5 mg to 80 mg of oxymorphone or a pharmaceutically acceptable salt thereof as the sole active ingredient, and wherein upon oral administration the mean blood plasma concentration of oxymorphone 12 hours after administration is greater than or equal to 36.8% that of the highest mean blood plasma concentration of oxymorphone. 
     
     
         10 . A composition according to  claim 9 , wherein the mean blood plasma concentration of oxymorphone 12 hours after administration is between about 36.8% and 95.8% that of the highest mean blood plasma concentration of oxymorphone. 
     
     
         11 . A composition according to  claim 9 , wherein the mean blood plasma concentration of oxymorphone 12 hours after administration is between about 59.3% and 95.8% that of the highest mean blood plasma concentration of oxymorphone. 
     
     
         12 . A composition according to  claim 9 , wherein the mean blood plasma concentration of oxymorphone 12 hours after administration is between about 74.8% and 95.8% that of the highest mean blood plasma concentration of oxymorphone. 
     
     
         13 . A composition according to  claim 9 , wherein the blood plasma concentration of oxymorphone comprises a first peak between about 0.5-4 hours after administration and a second peak between about 4-8 hours after administration. 
     
     
         14 . A composition according to  claim 9 , wherein the blood plasma concentration of oxymorphone comprises a first peak between about 0.5-4 hours after administration, a second peak between about 4-8 hours after administration and a third peak between about 10-14 hours after administration. 
     
     
         15 . An analgesically effective controlled release composition of oxymorphone for oral delivery comprising a controlled release matrix with a release rate profile designed to provide an adequate blood plasma level of analgesic over at least 12 hours, about 5 mg to 80 mg of oxymorphone or a pharmaceutically acceptable salt thereof as the sole active ingredient, and wherein the mean blood plasma concentration of oxymorphone 12 hours after administration is greater than or equal to 28.5% that of the blood plasma concentration of oxymorphone at Cmax. 
     
     
         16 . A composition according to  claim 15 , wherein the blood plasma concentration of oxymorphone 12 hours after administration is between about 30.5% and 81.9% that of the blood plasma concentration of oxymorphone at Cmax. 
     
     
         17 . A composition according to  claim 15 , wherein the blood plasma concentration of oxymorphone 12 hours after administration is between about 46.6% and 81.9% that of the blood plasma concentration of oxymorphone at Cmax. 
     
     
         18 . A composition according to  claim 15 , wherein the blood plasma concentration of oxymorphone 12 hours after administration is between about 65.6% and 81.9% that of the blood plasma concentration of oxymorphone at Cmax. 
     
     
         19 . A composition according to  claim 15 , wherein the blood plasma concentration of oxymorphone comprises a first peak between about 0.5-4 hours after administration and a second peak between about 4-8 hours after administration. 
     
     
         20 . A composition according to  claim 15 , wherein the blood plasma concentration of oxymorphone comprises a first peak between about 0.5-4 hours after administration, a second peak between about 4-8 hours after administration and a third peak between about 10-14 hours after administration.