Formulations

Abstract

The present invention relates to pharmaceutical compositions for oral administration of active compounds.

1 . Oral pharmaceutical composition containing at least two separate formulations:
 a first formulation, which contains an active compound selected from 2-[4-(diphenylmethyl)-1-piperazinyl]-acetic acids and their amides having the general formula I   
       
         
           
           
               
               
           
         
       
       wherein 
       R 1  is a —COOH group or a —CONH 2  group, and 
       X 1  and X 2 , taken separately, each represent a hydrogen atom, a halogen atom, a straight-chain or branched C 1 -C 4  alkoxy group or a trifluoromethyl group as well as their pharmaceutically acceptable salts, geometrical isomers, enantiomers, diastereomers and mixtures thereof, and which first formulation does not contain polyols having a molecular weight of less than 300 in a molar ratio between the polyol and active compound of formula I above 10; and
 a second formulation, which contains one or more solid polyol(s) with a molecular weight of less than 3000 and is free of any drug, 
 wherein the pharmaceutical formulation is a dry syrup prepared from a mixture of two types of granules wherein one type of granules is made by compaction of the first formulation and the other type of granules is made by compaction of the second formulation. 
 
     
     
         2 . The composition according to  claim 1  wherein the first formulation does not contain polyols having a molecular weight of less than 950 in a molar ratio between polyol and active compound of formula I above 10, with the exception of lactose. 
     
     
         3 . The composition according to  claim 1  wherein the first formulation does not contain polyols having a molecular weight of less than 300 in a molar ratio between polyol and active compound of formula I above 5. 
     
     
         4 . The composition according to  claim 1  wherein the first formulation does not contain polyols having a molecular weight of less than 300. 
     
     
         5 . The composition according to  claim 1  wherein the first formulation does not contain polyols having a molecular weight of less than 950 in a molar ratio between polyol and active compound of formula I above 5, with the exception of lactose. 
     
     
         6 . The composition according to  claim 1  wherein the first formulation does not contain polyols having a molecular weight of less than 950, with the exception of lactose. 
     
     
         7 . The composition according to  claim 1  wherein the formulations are prepared in the form of powders, granules, solutions or suspensions. 
     
     
         8 . The composition according to  claim 1  wherein the polyol in the second formulation is mannitol. 
     
     
         9 . The composition according to  claim 1  wherein the polyol in the second formulation is a polysaccharide. 
     
     
         10 . The composition according to  claim 1  wherein at least one of the formulations further contains an alcalinizing agent. 
     
     
         11 . The composition according to  claim 10  wherein the alcalinizing agent is sodium citrate. 
     
     
         12 . The composition according to  claim 1  wherein the first formulation further contains one or more excipients selected from cyclodextrins, colloidal anhydrous silica, microcristalline cellulose, magnesium stearate, flavors or colorants. 
     
     
         13 . The composition according to  claim 1  wherein the first formulation further contains non-polyol sweetening agents such as acesulfame K, aspartame, saccharine, saccharine sodium or cyclamate. 
     
     
         14 . The composition according to  claim 1  wherein the active compound in the first formulation is cetirizine dihydrochloride, levocetirizine dihydrochloride or efletirizine dihydrochloride. 
     
     
         15 - 22 . (canceled)