Pharmaceutical compositions based on diclofenac

Abstract

New pharmaceutical compositions for oral use containing Diclofenac together with alkali metal bicarbonates in amounts of from 20 to 80 by weight with respect to Diclofenac are described. These compositions are entirely palatable and free from any unpleasant taste or other side effects; in particular, these formulations permit to obtain in human patients higher C max of the active principle and shorter T max together with a lower coefficient of variation.

1 ) A fast-release diclofenac composition, in the form of a unit dose packet of powder for dissolving or suspending in water, or in the form of a fast release layer in a two layered diclofenac tablet that comprises a fast layer and a slow layer, wherein said composition comprises diclofenac in acid and/or salt form.  
     
     
         2 ) The composition of  claim 1  wherein said diclofenac is present as diclofenac potassium.  
     
     
         3 ) The composition of  claim 1  wherein said diclofenac is present in an amount ranging from about 10 to about 60 mg.  
     
     
         4 ) The composition of  claim 1  in the form of a unit dose packet of powder wherein said diclofenac is present in an amount of about 50 mg.  
     
     
         5 ) The composition of  claim 1  in the form of a unit dose packet of powder wherein said diclofenac is present as diclofenac potassium in an amount of about 50 mg.  
     
     
         6 ) The composition of  claim 1  in the form of a unit dose packet of powder, wherein said composition is capable of yielding an average T max  of diclofenac in a human patient between 5 and 30 minutes after administration of said diclofenac to said patient, said average T max  having a coefficient of variation (CV %) less than about 70%.  
     
     
         7 ) The composition of  claim 1  in the form of a unit dose packet of powder, wherein said composition is capable of yielding an average T max  of diclofenac in a human patient between 13 and 27 minutes after administration of said diclofenac to said patient, said average T max  having a coefficient of variation (CV %) less than about 70%.  
     
     
         8 ) The composition of  claim 1  in the form of a fast release layer in a two layered diclofenac tablet.  
     
     
         9 ) The composition of  claim 1  in the form of a fast release layer, wherein said composition comprises about 15 mg. of diclofenac potassium salt, and said slow release layer comprises about 70 mg. of diclofenac potassium salt.  
     
     
         10 ) The composition of  claim 1 , further comprising means for potentiating the bioavailability of said diclofenac.  
     
     
         11 ) The composition of  claim 10  wherein said means decreases the Tmax of said diclofenac.  
     
     
         12 ) The composition of  claim 10  wherein said means increases the Cmax of said diclofenac.  
     
     
         13 ) The composition of  claim 10  wherein said means decreases the coefficient of variation of the Cmax of said diclofenac.  
     
     
         14 ) The composition of  claim 10  in the form of a unit dose packet of powder wherein said diclofenac is present in an amount of from about 10 to about 60 mg.  
     
     
         15 ) The composition of  claim 10  in the form of a unit dose packet of powder wherein said diclofenac is present in an amount of about 50 mg.  
     
     
         16 ) The composition of  claim 10  wherein said means comprises one or more alkali metal carbonates or bicarbonates.  
     
     
         17 ) The composition of  claim 10  wherein said means comprises one or more alkali metal carbonates or bicarbonates in an amount greater than about 20 wt. % based on the weight of said diclofenac.  
     
     
         18 ) The composition of  claim 10  in the form of a unit dose packet of powder wherein said diclofenac is present in an amount of about 50 mg. and said means comprises one or more alkali metal carbonates or bicarbonates in an amount greater than about 20% based on the weight of said diclofenac.  
     
     
         19 ) The composition of  claim 10  in the form of a unit dose packet of powder wherein said diclofenac is present as diclofenac potassium in an amount of about 50 mg. and said means comprises potassium bicarbonate in an amount greater than about 20% based on the weight of said diclofenac.  
     
     
         20 ) The composition of  claim 10  in the form of a unit dose packet of powder wherein said diclofenac is present as diclofenac potassium in an amount of about 50 mg. and said means comprises potassium bicarbonate in an amount of from about 40 wt. % to about 80 wt. % based on the weight of said diclofenac.  
     
     
         21 ) A fast-release diclofenac composition, in the form of a unit dose packet of powder for dissolving or suspending in water, or in the form of a fast release layer in a two layered diclofenac tablet comprising a fast layer and a slow layer, wherein the composition comprises diclofenac in acid and/or salt form and means for potentiating the bioavailability of said diclofenac.  
     
     
         22 ) The composition of  claim 21  wherein said means comprises greater than about 20 wt. % of one or more alkali metal carbonates or bicarbonates based on the weight of said diclofenac.  
     
     
         23 ) A fast-releasing diclofenac composition, in the form of a unit dose packet of powder for dissolving or suspending in water, comprising about 50 mg. of diclofenac in acid and/or salt form.  
     
     
         24 ) The composition of  claim 23  wherein said diclofenac is present as diclofenac potassium.  
     
     
         25 ) The composition of  claim 23  wherein said diclofenac is present as diclofenac potassium, further comprising from about 40 to about 80 wt. % of potassium bicarbonate.  
     
     
         26 ) A fast-release diclofenac composition, in the form of a fast release layer in a two layered diclofenac tablet comprising a fast layer and a slow layer, comprising from about 10 to about 60 mg. of diclofenac in acid and/or salt form.  
     
     
         27 ) The composition of  claim 26  wherein said diclofenac is present as diclofenac potassium.