Pharmaceutical formulations

Abstract

The present invention relates to formulations including compounds of Formula (I), or prodrug, or a pharmaceutically acceptable salt thereof.

1 . An orally administrable pharmaceutical formulation comprising
 (a) compound of Formula (I)   
       
         
           
           
               
               
           
         
       
       wherein
 R 1  is halo, cyano, optionally substituted lower alkyl, or optionally substituted lower alkoxyl; and 
 R 2  is optionally substituted aryl, or optionally substituted heterocyclyl; 
 or a prodrug, or pharmaceutically acceptable salt thereof; 
 
       (b) at least one diluent or filler; 
       (c) optionally at least one disintegrant; 
       (d) optionally at least one binder; and 
       (e) optionally at least one lubricant; 
       wherein 
       the compound of formula (I) is present in an amount within the range of from about 1% to about 80% by weight; 
       the diluent or filler is present in an amount within the range of from about 10% to about 95% by weight; 
       the disintegrant, if present, is present in an amount within the range of from about 0.1% to about 20% by weight;
 the binder, if present, is present in an amount within the range of from about 0.1% to about 20% by weight; and 
 the lubricant, if present, is present in an amount within the range of from about 0.1% to about 5% by weight, all of the above % by weight being based on the weight of the formulation. 
 
     
     
         2 . The pharmaceutical composition of  claim 1  wherein
 R 1  is a halogen atom, or a lower alkyl group; and 
 R 2  is phenyl optionally substituted by 1 to 3 substituents selected from the group consisting of a halogen atom, a cyano group, a lower alkyl group, a halo-lower alkyl group, a lower alkoxy group, a halo-lower alkoxy group, a methylenedioxy group, an ethyleneoxy group, a mono- or di-lower alkylamino group, a carbamoyl group, and a mono- or di-lower alkylcarbamoyl group. 
 
     
     
         3 . The pharmaceutical composition of  claim 1  wherein the compound of Formula (I) is the compound of formula (I-S): 
       
         
           
           
               
               
           
         
         or a prodrug, or pharmaceutically acceptable salt thereof. 
       
     
     
         4 . The pharmaceutical composition of  claim 3 , wherein the compound is present in an amount of about 25 mg to about 600 mg. 
     
     
         5 . The pharmaceutical composition of  claim 3 , wherein the compound is present in an amount of about 50 mg to about 300 mg. 
     
     
         6 . The pharmaceutical composition of  claim 3 , wherein the compound is present in an amount of about 100 mg. 
     
     
         7 . The pharmaceutical composition of  claim 3 , wherein the compound is present in an amount of about 300 mg. 
     
     
         8 . The pharmaceutical composition of  claim 1 , wherein the compound is 1-(β-D-glucopyranosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl]benzene)hemihydrate. 
     
     
         9 . The pharmaceutical composition of  claim 1 , wherein the formulation is a tablet. 
     
     
         10 . A method for treating a sodium-dependent glucose transporter mediated disorder, said method comprising administering to a patient in need thereof, the pharmaceutical composition of  claim 3 . 
     
     
         11 . The method of  claim 10  wherein the compound is administered at a dose of from about 50 mg to about 300 mg once daily. 
     
     
         12 . The method of  claim 10  wherein the compound is administered at a dose of about 100 mg per day. 
     
     
         13 . The method of  claim 10  wherein the compound is administered at a dose of about 300 mg per day. 
     
     
         14 . An orally administrable pharmaceutical formulation comprising
 (a) a compound of Formula (I-S)   
       
         
           
           
               
               
           
         
         or a prodrug or pharmaceutically acceptable salt thereof present in an amount within the range of from about 40% to about 60% by weight; 
         (b) at least one diluent or filler present in an amount within the range of from about 30% to about 50% by weight; 
         (c) at least one disintegrant in an amount within the range of from about 3% to about 10% by weight; 
         (d) at least one binder present in an amount within the range of from about 0.5% to about 5% by weight; and 
         (e) at least one lubricant present in an amount within the range of from about 0.5% to about 2% by weight; 
         wherein the % by weight is based on the weight of the formulation. 
       
     
     
         15 . The pharmaceutical composition of  claim 14 , wherein the compound is 1-(β-D-glucopyranosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl]benzene)hemihydrate. 
     
     
         16 . The pharmaceutical composition of  claim 14 , wherein the formulation is a tablet. 
     
     
         17 . The pharmaceutical composition of  claim 15 , wherein the formulation is a tablet.