Method of treating pain by administering 24 hour oral opioid formulations exhibiting rapid rate of initial rise of plasma drug level

Abstract

Patients are treated with 24-hour oral sustained release opioid formulations which, upon administration, provide an initially rapid opioid absorption such that the minimum effective analgesic concentration of the opioid is more quickly achieved. These sustained release opioid formulations include an effective amount of at least one retardant material to cause said opioid analgesic to be released at a such a rate as to provide an analgesic effect after oral administration to a human patient for at least about 24 hours, and are characterized by providing an absorption half-life from 1 to about 8 hours. A method of titrating a human patient utilizing these sustained release opioid formulations is also disclosed.

1 - 7 . (canceled) 
   
   
       8 . The formulation of  claim 27 , wherein the amount of hydromorphone consists of from about 2 mg to about 64 mg. 
   
   
       9 - 11 . (canceled) 
   
   
       12 . The sustained release formulation of  claim 27 , wherein said retardant material is selected from the group consisting of an acrylic polymer, an alkylcellulose, shellac, zein, hydrogenated vegetable oil, hydrogenated castor oil, and mixtures of any of the foregoing. 
   
   
       13 - 26 . (canceled) 
   
   
       27 . An oral sustained release opioid formulation comprising a plurality of substrates comprising hydromorphone or a salt thereof,
 wherein the surfaces of the plurality of substrates are coated with a sustained release coating comprising:
 a plasticizer, 
 an anti-tacking material, and 
 an effective amount of at least one retardant material, 
   wherein the retardant material of the sustained release coating produces a weight gain level from about 2 to about 30 percent; and   wherein said formulation provides a maximum plasma concentration (T max ) of hydromorphone in about 2 to about 10 hours and a maximum plasma concentration (C max ) which is more than twice the plasma level of hydromorphone at about 24 hours after administration of the formulation to a human patient.   
   
   
       28 . The formulation of  claim 27 , wherein the plurality of substrates comprises a multiparticulate system that is selected from the group consisting of: beads, spheroids, microspheres, seeds, pellets, and ion-exchange resin beads. 
   
   
       29 . The formulation of  claim 28 , wherein the plurality of substrates is beads. 
   
   
       30 . The formulation of  claim 29 , wherein the beads are inert pharmaceutical beads. 
   
   
       31 . The formulation of  claim 30 , wherein the inert pharmaceutical beads may be from about 8 mesh to about 50 mesh. 
   
   
       32 . The formulation of  claim 27 , wherein said formulation provides effective treatment of pain for about 24 hours or more administration to a human patient. 
   
   
       33 . The formulation of  claim 12 , wherein the retardant material is an acrylic polymer. 
   
   
       34 . The formulation of  claim 33 , wherein the acrylic polymer is an acrylic resin lacquer in the form of an aqueous dispersion. 
   
   
       35 . The formulation of  claim 12 , wherein the retardant material is an alkylcellulose. 
   
   
       36 . The formulation of  claim 35 , wherein the alkylcellulose is ethylcellulose.