Formulations of 14-EPI-Analogues of Vitamin D

Abstract

The present invention provides new formulations of 14-epi-analogues of vitamin D, such as inecalcitol, providing improved absorption profile.

1 . An oral formulation of a 14-epi-analogue of vitamin D, characterized by an improved absorption profile over the Medium Chain Triglycerides (MCT) formulation of said 14-epi-analogues of vitamin D. 
     
     
         2 . An oral formulation of a 14-epi-analogue of vitamin D for use for improving the absorption of said 14-epi-analogue over the formulation in medium chain triglyceride. 
     
     
         3 . The oral formulation according to  claim 1 , wherein it is characterized by a higher peak concentration (Cmax) and optionally a higher overall absorption (AUC 0-24h ) than the corresponding formulation in MCT. 
     
     
         4 . The oral formulation according to  claim 1 , wherein said formulation is a dry formulation which comprises:
 at least one 14-epi-analogue of vitamin D,   carboxymethylcellulose (CMC),   and one or more optional pharmaceutically acceptable excipient(s).   
     
     
         5 . The oral formulation according to  claim 4 , which comprises between 0.1% and 50% (weight) of CMC. 
     
     
         6 . The oral formulation according to  claim 1 , wherein said formulation is a soft gelatin capsule comprising:
 at least one 14-epi-analogue of vitamin D,   at least one Long Chain Triglyceride (LCT),   and one or more optional pharmaceutically acceptable excipient(s).   
     
     
         7 . The oral formulation according to  claim 6 , wherein the concentration (weight) of LCT is comprised between 1% and qsp. 
     
     
         8 . The oral formulation according to  claim 1 , wherein said formulation is a solution comprising:
 at least one 14-epi-analogue of vitamin D,   propylene glycol,   and one or more optional pharmaceutically acceptable excipient(s).   
     
     
         9 . The oral formulation according to  claim 8 , wherein the concentration (weight) of propylene glycol is comprised between 1% and qsp. 
     
     
         10 . The oral formulation according to  claim 1 , wherein said 14-epi-analogue of vitamin D is inecalcitol. 
     
     
         11 . The oral formulation according to  claim 1 , wherein the concentration of said 14-epi-analogue in said formulation is comprised between 0.001 and 50% (weight). 
     
     
         12 . The oral formulation according to  claim 1  in a unit dose. 
     
     
         13 . The oral formulation according to  claim 1 , which comprises from 0.5 to 20 mg of said 14-epi-analogue. 
     
     
         14 . A method for the prevention and/or treatment of rickets, osteoporosis, osteomalacia, psoriasis, autoimmune diseases such as multiple sclerosis or type I diabetes, hyperparathyroidism, benign prostate hyperplasia, any type of cancer or any vitamin D associated disease comprising administering the oral formulation according to  claim 1 .