Oral Dosage Form Containing A PDE 4 Inhibitor as an Active Ingredient and Polyvinylpyrrolidon as Excipient

Abstract

Dosage forms for oral administration of a PDE 4 inhibitor whose solubility is slight are described. They contain PVP as binder.

1 .- 11 . (canceled) 
     
     
         12 . An immediate release solid dosage form in tablet or pellet form for oral administration of N-(3,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-difluoromethoxybenzamide (roflumilast), comprising:
 (a) between 0.25 and 0.5 mg of roflumilast;   (b) a binder; and   (c) one or more suitable pharmaceutical excipients selected from the group consisting of fillers, tablet disintegrants, lubricants, release agents, flavoring substances, buffer substances, preservatives, coloring substances and emulsifiers,   
       wherein approximately 78% of the roflumilast is released after 15 minutes. 
     
     
         13 . The solid dosage form according to  claim 12 , wherein quantitative release of roflumilast is observed after approximately 60 minutes. 
     
     
         14 . The solid dosage form according to  claim 12 , wherein the disintegration time of the dosage form is approximately 7 minutes. 
     
     
         15 . The solid dosage form according to  claim 12 , wherein the dosage form is a tablet. 
     
     
         16 . The solid dosage form according to  claim 12 , wherein said binder is present in a proportion of about 0.5% to about 20% by weight based on the finished dosage form. 
     
     
         17 . The solid dosage form according to  claim 12 , wherein said roflumilast is in the form of a solid solution in said binder, said solid solution having an amorphous structure. 
     
     
         18 . The solid dosage form according to  claim 12 , wherein said roflumilast is in the form of a molecular dispersion in said binder. 
     
     
         19 . The solid dosage form according to  claim 12 , comprising 0.5 mg of roflumilast. 
     
     
         20 . The solid dosage form according to  claim 12 , wherein said dosage form provides a mean T max  of less than 1.5 hr. 
     
     
         21 . The solid dosage form according to  claim 20 , wherein said mean T max  is less than 1 hour. 
     
     
         22 . The solid dosage form according to  claim 20 , wherein said mean T max  is less than 30 minutes. 
     
     
         23 . An immediate release solid dosage form in tablet or pellet form for oral administration of N-(3,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-difluoromethoxybenzamide (roflumilast), comprising:
 (a) between 0.25 and 0.5 mg of roflumilast;   (b) a binder; and   (c) one or more suitable pharmaceutical excipients selected from the group consisting of fillers, tablet disintegrants, lubricants, release agents, flavoring substances, buffer substances, preservatives, coloring substances and emulsifiers,   
       wherein quantitative release of roflumilast is observed after approximately 60 minutes. 
     
     
         24 . The solid dosage form according to  claim 23 , wherein approximately 78% of the roflumilast is released after 15 minutes. 
     
     
         25 . The solid dosage form according to  claim 23 , wherein the disintegration time of the dosage form is approximately 7 minutes. 
     
     
         26 . The solid dosage form according to  claim 23 , wherein said binder is present in a proportion of about 0.5% to about 20% by weight based on the finished dosage form. 
     
     
         27 . The solid dosage form according to  claim 23 , wherein said roflumilast is in the form of a solid solution in said binder, said solid solution having an amorphous structure. 
     
     
         28 . The solid dosage form according to  claim 23 , wherein said roflumilast is in the form of a molecular dispersion in said binder. 
     
     
         29 . The solid dosage form according to  claim 23  comprising 0.5 mg of roflumilast. 
     
     
         30 . The solid dosage form according to  claim 23 , wherein said dosage form provides a mean T max  of less than 1.5 hr. 
     
     
         31 . The solid dosage form according to  claim 30 , wherein said mean T max  is less than 1 hour. 
     
     
         32 . The dosage form according to  claim 30 , wherein said mean T max  is less than 30 minutes. 
     
     
         33 . An immediate release solid dosage form in tablet or pellet form for oral administration of N-(3,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-difluoromethoxybenzamide (roflumilast), comprising:
 (a) between 0.25 and 0.5 mg of roflumilast;   (b) a binder; and   (c) one or more suitable pharmaceutical excipients selected from the group consisting of fillers, tablet disintegrants, lubricants, release agents, flavoring substances, buffer substances, preservatives, coloring substances and emulsifiers,   
       wherein the disintegration time of the dosage form is approximately 7 minutes. 
     
     
         34 . The solid dosage form according to  claim 33 , wherein approximately 78% of the roflumilast is released after 15 minutes. 
     
     
         35 . The solid dosage form according to  claim 33 , wherein quantitative release of roflumilast is observed after approximately 60 minutes. 
     
     
         36 . The solid dosage form according to  claim 33 , wherein said binder is present in a proportion of about 0.5% to about 20% by weight based on the finished dosage form. 
     
     
         37 . The solid dosage form according to  claim 33 , wherein said roflumilast is in the form of a solid solution in said binder, said solid solution having an amorphous structure. 
     
     
         38 . The solid dosage form according to  claim 33 , wherein said roflumilast is in the form of a molecular dispersion in said binder. 
     
     
         39 . The solid dosage form according to  claim 33 , wherein said dosage form provides a mean T max  of less than 1.5 hr. 
     
     
         40 . The solid dosage form according to  claim 39 , wherein said mean T max  is less than 1 hour. 
     
     
         41 . The solid dosage form according to  claim 39 , wherein said mean T max  is less than 30 minutes.