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 . A solid dosage form in tablet or pellet form for oral administration of a PDE 4 inhibitor, comprising:
 between 0.25 and 0.5 mg of a PDE 4 inhibitor of the formula I   
       
         
           
           
               
               
           
         
         in which 
         R1 is difluoromethoxy, 
         R2 is cyclopropylmethoxy and 
         R3 is 3,5-dichloropyrid-4-yl, 
         or a salt thereof; 
         a water-soluble binder; and 
         one or more suitable pharmaceutical excipients, and wherein said dosage form provides immediate release of the PDE 4 inhibitor. 
       
     
     
         13 . The solid dosage form according to  claim 12 , wherein the water-soluble binder is selected from the group consisting of polyvinylpyrrolidone, vinylpyrrolidone-vinyl acetate copolymer, gelatin, corn starch mucilage, preswollen starch, hydroxypropyl-methylcellulose, hydroxypropylcellulose and mixtures thereof. 
     
     
         14 . The solid dosage form according to  claim 12 , wherein the proportion of water-soluble binder is from 0.5 to 20% by weight, based on the finished dosage form. 
     
     
         15 . The solid dosage form according to  claim 12 , wherein the PDE 4 inhibitor is N-(3,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-difluoromethoxybenzamide (roflumilast). 
     
     
         16 . The solid dosage form according to  claim 12 , containing 0.5 mg of roflumilast per dosage unit. 
     
     
         17 . The solid dosage form according to  claim 12 , wherein said excipients are selected from the group consisting of fillers, tablet disintegrants, lubricants, release agents, flavoring substances, buffer substances, preservatives, coloring substances, emulsifiers and combinations thereof. 
     
     
         18 . The solid dosage form according to  claim 12 , wherein the water-soluble binder includes at least polyvinylpyrrolidone and one other water-soluble binder. 
     
     
         19 . The solid dosage form according to  claim 12 , wherein the dosage form is a tablet. 
     
     
         20 . The solid dosage form according to  claim 12 , wherein the pharmaceutical excipients include at least a filler and wherein the proportion of filler is from 40 to 99% by weight, based on the finished dosage form. 
     
     
         21 . The solid dosage form according to  claim 20 , wherein the proportion of filler is from 60 to 97% by weight, based on the finished dosage form. 
     
     
         22 . The solid dosage form according to  claim 20 , wherein the filler is selected from the group consisting of sugar alcohols, starches, saccharides and mixtures thereof. 
     
     
         23 . The solid dosage form according to  claim 20 , wherein the filler is selected from the group consisting of corn starch, microcrystalline cellulose, lactose and mixtures thereof. 
     
     
         24 . The solid dosage form according to  claim 20 , wherein the filler includes corn starch and lactose. 
     
     
         25 . The solid dosage form according to  claim 12 , wherein the pharmaceutical excipients include at least a lubricant or release agent and wherein the lubricant or release agent is selected from the group consisting of sodium stearyl fumarate, magnesium stearate, calcium stearate, stearic acid, talc and colloidal anhydrous silica. 
     
     
         26 . The solid dosage form according to  claim 25 , wherein the lubricant or release agent is magnesium stearate. 
     
     
         27 . The solid dosage form according to  claim 25 , wherein the proportion of lubricant or release agent is between 0.1 and 20% by weight, based on the finished dosage form. 
     
     
         28 . The solid dosage form according to  claim 25  wherein the proportion of lubricant or release agent is between 0.3 and 3% by weight, based on the finished dosage form. 
     
     
         29 . The solid dosage form according to  claim 12 , wherein the pharmaceutical excipients include at least one filler and at least one lubricant or release agent. 
     
     
         30 . The solid dosage form according to  claim 12 , wherein the pharmaceutical excipients include at least a disintegrant and wherein the disintegrant is selected from the group consisting of insoluble polyvinylpyrrolidone, carboxymethylstarch sodium, sodium carboxymethylcellulose; alginic acid, disintegrant starches, and combinations thereof. 
     
     
         31 . The solid dosage form according to  claim 30 , wherein the proportion of disintegrant is between 2 and 35% by weight, based on the finished dosage form. 
     
     
         32 . The solid dosage form according to  claim 30 , wherein the proportion of disintegrant is between 2 and 20% by weight, based on the finished dosage form. 
     
     
         33 . A solid dosage form in tablet or pellet form, for oral administration of roflumilast, comprising 0.5 mg of roflumilast, from 40 to 99% by weight based on the finished dosage form of one or more fillers; from 2 to 35% by weight, based on the finished dosage form of one or more disintegrants, from 0.5 to 20% by weight, based on the finished dosage form of a water-soluble binder; and a lubricant, and wherein the dosage form provides immediate release of said roflumilast. 
     
     
         34 . A solid dosage form in tablet form, for oral administration of roflumilast, comprising 0.5 mg of roflumilast, from 40 to 99% by weight based on the finished dosage form of one or more fillers; from 2 to 35% by weight, based on the finished dosage form of one or more disintegrants, and from 0.5 to 20% by weight, based on the finished dosage form of a water-soluble binder; and wherein the dosage form provides immediate release of said roflumilast.