Solid pharmaceutical compositions containing pregabalin

Abstract

A solid pharmaceutical composition containing pregabalin is described. The composition includes a matrix forming agent and a swelling agent and is suitable for once daily oral administration. Exemplary matrix forming agents include mixtures of polyvinyl acetate and polyvinylpyrrolidone, and exemplary swelling agents include cross-linked polymers of polyvinylpyrrolidone.

1 . A pharmaceutical composition comprising an active pharmaceutical ingredient and excipients, the active pharmaceutical ingredient comprising pregabalin, or a pharmaceutically acceptable complex, salt, solvate or hydrate thereof, and the excipients comprising a matrix forming agent and a swelling agent, the matrix forming agent comprising polyvinyl acetate and polyvinylpyrrolidone, and the swelling agent comprising cross-linked polyvinylpyrrolidone, wherein the pharmaceutical composition is adapted for once-daily oral dosing.  
   
   
       2 . The pharmaceutical composition according to  claim 1 , wherein the pharmaceutical composition expands to a size of about 9 mm or greater when contacting water.  
   
   
       3 . The pharmaceutical composition according to  claim 1 , wherein the pharmaceutical composition is retained in the stomach of a subject following oral dosing for about 3 hours to about 14 hours.  
   
   
       4 . The pharmaceutical composition according to  claim 1 , wherein the active pharmaceutical ingredient is released over a period of time that is about 4 hours to about 6 hours longer than the time the pharmaceutical composition is retained in the stomach of a subject following oral dosing.  
   
   
       5 . The pharmaceutical composition according to  claim 1 , wherein the active pharmaceutical ingredient is released over a period of time of about 12 hours to about 20 hours.  
   
   
       6 . The pharmaceutical composition according to  claim 1 , in which the active pharmaceutical ingredient exhibits an in vivo steady-state C MAX  of about 9 μg/mL or less, or an in vivo steady-state C MIN  of about 0.7 μg/mL or greater, or an in vivo steady-state C MAX  of about 9 μg/mL or less and an in vivo steady-state C MIN  of about 0.7 μg/mL or greater.  
   
   
       7 . The pharmaceutical composition according to  claim 1 , wherein the swelling agent further comprises polyethylene oxide.  
   
   
       8 . The pharmaceutical composition according to  claim 1 , wherein the pharmaceutical composition is bioequivalent to an immediate release formulation comprising pregabalin, lactose monohydrate, maize starch, and talc.  
   
   
       9 . A method of treating a condition or disorder in a subject which is responsive to pregabalin, the method comprising administering to the subject a pharmaceutical composition as in  claim 1 , wherein the pharmaceutical composition is administered orally once daily.  
   
   
       10 . The method according to  claim 9 , wherein the condition or disorder is selected from epilepsy, pain, diabetic peripheral neuropathy, postherpetic neuralgia, physiological conditions associated with psychomotor stimulants, inflammation, gastrointestinal damage, alcoholism, insomnia, fibromyalgia, anxiety, depression, mania, and bipolar disorder.  
   
   
       11 . A method of treating a condition or disorder in a subject which is responsive to pregabalin, the method comprising administering to the subject once daily a pharmaceutical composition comprising an active pharmaceutical ingredient and excipients, the active pharmaceutical ingredient comprising pregabalin, or a pharmaceutically acceptable complex, salt, solvate or hydrate thereof, and the excipients comprising a matrix forming agent and a swelling agent.  
   
   
       12 . The method according to  claim 11 , wherein the condition or disorder is selected from epilepsy, pain, diabetic peripheral neuropathy, postherpetic neuralgia, physiological conditions associated with psychomotor stimulants, inflammation, gastrointestinal damage, alcoholism, insomnia, fibromyalgia, anxiety, depression, mania, and bipolar disorder.  
   
   
       13 . The method according to  claim 11 , in which the active pharmaceutical ingredient exhibits an in vivo steady-state C MAX  of about 9 μg/mL or less.  
   
   
       14 . The method according to  claim 11 , in which the active pharmaceutical ingredient exhibits an in vivo steady-state C MIN  of about 0.7 μg/mL or greater.  
   
   
       15 . The method according to  claim 11 , in which the active pharmaceutical ingredient exhibits an in vivo steady-state C MAX  of about 9 μg/mL or less and an in vivo steady-state C MIN  of about 0.7 μg/mL or greater.