Controlled release dosage forms

Abstract

The invention provides stable controlled release monolithic coating compositions for use in coating pharmaceutical oral dosage forms comprising a polyglycol having a melting point greater than 55° C. and an aqueous dispersion of a neutral ester copolymer lacking functional groups.

1 . A controlled release oral dosage form, comprising:
 (1) about 1000 mg of metformin hydrochloride, wherein said oral dosage form further comprises   (2) means for releasing said metformin hydrochloride to provide a T max  of said metformin hydrochloride after administration to a patient.   
     
     
         2 . The controlled release oral dosage form of  claim 1 , wherein said T max  ranges from about 6 hours to about 12 hours. 
     
     
         3 . The controlled release oral dosage form of  claim 2 , wherein said T max  is about 9 hours. 
     
     
         4 . A controlled release oral dosage form, comprising:
 (1) about 1000 mg of metformin hydrochloride, wherein said oral dosage form further comprises   (2) means for releasing said metformin hydrochloride to provide a C max  of said metformin hydrochloride after administration to a patient.   
     
     
         5 . The controlled release oral dosage form of  claim 4 , wherein said C max  of said metformin hydrochloride is about 1252±321 ng/mL. 
     
     
         6 . The controlled release oral dosage form of  claim 4 , wherein said C max  is about 1210 ng/mL. 
     
     
         7 . A controlled release oral dosage form, comprising:
 (1) about 1000 mg of metformin hydrochloride, wherein said oral dosage form further comprises   (2) means for releasing said metformin hydrochloride to provide an AUC(0 to t) of said metformin hydrochloride after administration to a patient.   
     
     
         8 . The controlled release oral dosage form of  claim 7 , wherein said AUC(0 to t) is about 11644±2808 (ng)(hr)/mL. 
     
     
         9 . The controlled release oral dosage form of  claim 7 , wherein said AUC(0 to t) is about 11313 (ng)(hr)/mL. 
     
     
         10 . A controlled release oral dosage form, comprising:
 (1) about 1000 mg of metformin hydrochloride, wherein said oral dosage form further comprises   (2) means for releasing said metformin hydrochloride to provide an AUC(0 to infinity) after administration to a patient.   
     
     
         11 . The controlled release oral dosage form of  claim 10 , wherein said AUC(0 to infinity) of said metformin hydrochloride is about 11812±2822 (ng)(hr)/mL. 
     
     
         12 . The controlled release oral dosage form of  claim 11 , wherein said AUC(0 to infinity) is about 11482 (ng)(hr)/mL. 
     
     
         13 . The controlled release oral dosage form of  claim 1 , wherein said means for releasing said metformin hydrochloride further provides an in-vitro release rate of the metformin hydrochloride when tested by the USP Apparatus II (Paddle Apparatus) method at 50 rpm, in 900 mL water and at about 37° C., such that about 20% or less of the metformin hydrochloride is released after about 1 hour, about 48% or less of the metformin hydrochloride is released after about 3 hours, and not less than about 87% of the metformin hydrochloride is released after about 10 hours. 
     
     
         14 . The controlled release oral dosage form of  claim 1 , wherein said means for releasing said metformin hydrochloride further provides an in-vitro release rate of the metformin hydrochloride when tested by the USP Apparatus I (Basket Apparatus) method at 100 rpm, in 900 mL simulated gastric fluid USP and at about 37° C., such that between about 18% and about 39% of the metformin hydrochloride is released after about 2 hours, between about 34% and about 59% of the metformin hydrochloride is released after about 4 hours, and between about 67% and about 85% of the metformin hydrochloride is released after about 8 hours.