Liquid formulation of cabazitaxel

Abstract

The present invention relates to a stable liquid formulation of cabazitaxel. The formulation comprises cabazitaxel, and at least one solubilizer. Typically, formulations are in the form of ready-to-use solutions or concentrates.

1 . A stable, liquid pharmaceutical composition, comprising cabazitaxel or a pharmaceutically acceptable salt thereof, at least one solubilizer and a solvent. 
     
     
         2 . The stable, liquid pharmaceutical composition of  claim 1 , wherein the composition is in the form of a nanodispersion comprising nanoparticles having a mean size less than 500 nm, preferably less than 300 nm. 
     
     
         3 . The stable, liquid pharmaceutical composition of  claim 1 , wherein the composition is a ready to use formulation. 
     
     
         4 . The stable, liquid pharmaceutical composition of  claim 1 , wherein the solubilizer is selected from the group comprising of benzyl alcohol, tertiary-butyl alcohol, isopropyl alcohol, acetic acid, glycols, polysorbates, polyoxyethylene glycol esters, polyoxyethylene castor oil derivatives and suitable mixtures thereof. 
     
     
         5 . The stable, liquid pharmaceutical composition of  claim 4 , wherein the solubilizer is Polyethylene glycol. 
     
     
         6 . The stable, liquid pharmaceutical composition of  claim 1 , wherein the solvent is ethanol. 
     
     
         7 . The stable, liquid pharmaceutical composition of  claim 1 , wherein the composition further comprises at least one stabilizer selected from the group comprising of chelating agents, phospholipids and sterols. 
     
     
         8 . The stable, liquid pharmaceutical composition of  claim 1 , wherein the composition further comprises one or more pharmaceutically acceptable excipients selected from the group comprising co-solvents, buffers, tonicity adjusting agents, emulsifying agents, pH adjusters, antioxidants, preservatives, and mixtures thereof. 
     
     
         9 . The stable, liquid pharmaceutical composition of  claim 1 , wherein the composition is suitable for parenteral administration. 
     
     
         10 . A method of preparation of the stable, liquid pharmaceutical composition of  claim 1 , comprising the steps of:
 i. dissolving or mixing solubilizer, stabilizer, co-solvent, antioxidant, tonicity adjusting agents, buffers and preservatives in a solvent or mixture of solvents;   ii. dissolving cabazitaxel in the solution obtained in step (i), and adjusting the pH if required;   iii. filtering the solution obtained in step (ii) through suitable sterile grade membrane filter   iv. purging pure nitrogen into the filtered final solution; and   v. filling measured volume of the solution in vials and purging pure nitrogen in the headspace of vials before closing with rubber stopper.