Rhein or diacerein compositions

Abstract

The invention relates to pharmaceutical compositions comprising rhein or diacerein or salts or esters or prodrugs thereof, optionally with one or more pharmaceutically acceptable excipients. The invention also relates to the methods for preparing such compositions.

1 - 36 . (canceled) 
     
     
         37 . A pharmaceutical composition comprising rhein or diacerein or salts or esters or prodrugs thereof and one or more sugar alcohols, wherein the composition exhibits a dissolution profile such that more than 75% of diacerein is released within 30 minutes, wherein the release rate is measured in Apparatus 2 (USP, Dissolution, paddle, 75 rpm) using 1000 ml of pH 5.7 phosphate buffer at 37° C.±0.5° C. 
     
     
         38 . The pharmaceutical composition of  claim 37 , wherein the diacerein can be present in an amount relative to the sugar alcohol, such that a molar ratio between the diacerein and the sugar alcohol is from about 1:1 to 1:10. 
     
     
         39 . The pharmaceutical composition of  claim 37 , wherein the composition comprises one or more of a tablet, capsule, powder, disc, caplet, granules, pellets, granules in capsule, minitablets, minitablets in capsule, pellets in capsule, and sachet. 
     
     
         40 . The pharmaceutical composition of  claim 37 , wherein the composition further comprises one or more pharmaceutically acceptable excipients comprising fillers, binders, lubricants, glidants, disintegrants, surfactants, sweeteners, coloring and flavoring agents. 
     
     
         41 . The pharmaceutical composition of  claim 37 , wherein the diacerein is present in the form of admixture with sugar alcohol, complex with sugar alcohol or adsorbed on sugar alcohol. 
     
     
         42 . The pharmaceutical composition of  claim 37 , wherein the pharmaceutical composition comprising rhein or diacerein or salts or esters or prodrugs thereof adsorbed on one or more sugar alcohol matrix characterized by the crystallographic data shown in  FIG. 1 . 
     
     
         43 . The pharmaceutical composition of  claim 42 , wherein the pharmaceutical composition comprising rhein or diacerein or salts or esters or prodrugs thereof adsorbed on one or more sugar alcohol matrix having X-ray diffraction peaks at angle 2 theta of 9.6 and 13.52 degrees. 
     
     
         44 . A method of improving the solubility of diacerein or salts thereof, wherein the rhein or diacerein or salts or esters or prodrugs there of is associated with one or more sugar alcohols. 
     
     
         45 . A process for the preparation of a pharmaceutical composition, the process comprising spraying a solution of rhein or diacerein or salts or esters or prodrugs thereof in one or more organic solvents, with sugar alcohols and/or one or more pharmaceutically acceptable excipients in a flow of a fluid under supercritical pressure to form particles and collecting the particles. 
     
     
         46 . The process of  claim 45 , wherein the supercritical fluid comprises one or more of carbon dioxide, water, ethane and xenon.