Solid dispersions of amorphous paroxetine mesylate

Abstract

The invention relates to solid dispersions containing paroxetine mesylate. One solid dispersion contains amorphous paroxetine mesylate and a methacrylic acid-methyl methacrylate copolymer, where the weight ratio of paroxetine mesylate to polymer ranges from about 30:70 to about 90:10. Another solid dispersion contains amorphous paroxetine mesylate and a-vinylpyrrolidone/vinylacetate copolymer (PVP-VA), where the weight ratio of paroxetine mesylate to copolymer ranges from about 30:70 to about 50:50. An amorphous solid dispersion of the invention may have a single glass transition temperature. An amorphous solid dispersion is stable for at least 48 hours at 60° C. and 75% relative humidity. A further embodiment of the invention relates to pharmaceutical compositions of paroxetine mesylate comprising a solid dispersion of the invention and at least one pharmaceutically acceptable excipient. Methods for the treatment using paroxetine mesylate in the form of a solid dispersion according to the invention are also disclosed.

1 . A solid dispersion of amorphous paroxetine mesylate in a methacrylic acid-methyl methacrylate copolymer, wherein the weight ratio of paroxetine mesylate to polymer ranges from about 30:70 to about 90:10. 
     
     
         2 . A solid dispersion of  claim 1 , wherein the weight ratio of paroxetine mesylate to polymer is selected from about 30:70, about 70:30 and about 90:10. 
     
     
         3 . A solid dispersion of  claim 1 , having a single glass transition temperature. 
     
     
         4 . A solid dispersion of  claim 1  being stable for at least 48 hours at 60° C. and 75% relative humidity. 
     
     
         5 . A pharmaceutical composition of paroxetine mesylate comprising a solid dispersion of  claim 1  and at least one pharmaceutically acceptable excipient, wherein the paroxetine mesylate is present in a therapeutically acceptable amount. 
     
     
         6 . A method for treating a male or female suffering from at least one condition or disorder selected from the group consisting of depression, obsessive compulsive disorder, post-traumatic stress disorder, panic disorder, generalized anxiety disorder, social phobia and social anxiety disorders, premenstrual dysphoric disorder, premature ejaculation, compulsive gambling, hot flashes, diabetic neuropathy, tension headache, chronic headaches, tingling in the hands and feet caused by diabetes, male sexual problems, and thermoregulatory dysfunction comprising administering paroxetine to said male or female a therapeutically effective amount of paroxetine mesylate in the form of a solid dispersion according to  claim 1 . 
     
     
         7 . The method of  claim 6 , wherein the paroxetine mesylate is administered in an amount, based on the paroxetine moiety, of about 5 mg/day to about 19.5 mg/day. 
     
     
         8 . The method of  claim 6 , wherein the paroxetine mesylate is administered for treating a patient suffering from thermoregulatory dysfunction in an amount, based on the paroxetine moiety, of about 7.5 mg/day. 
     
     
         9 . A method for treating a male or female suffering from at least one condition or disorder selected from the group consisting of depression, obsessive compulsive disorder, post-traumatic stress disorder, panic disorder, generalized anxiety disorder, social phobia and social anxiety disorders, premenstrual dysphoric disorder, premature ejaculation, compulsive gambling, hot flashes, diabetic neuropathy, tension headache, chronic headaches, tingling in the hands and feet caused by diabetes, male sexual problems, and thermoregulatory dysfunction comprising administering paroxetine to said male or female a therapeutically effective amount of paroxetine mesylate in the form of a solid dispersion according to  claim 5 . 
     
     
         10 .- 21 . (canceled)