Pharmaceutical formulations comprising paclitaxel, derivatives and pharmaceutically acceptable salts thereof

Abstract

The invention concerns paclitaxel solubilizers and formulations thereof with a high propensity to dissolve paclitaxel. The formulations of the invention reduce or obviate the need for the disadvantageous excipient Cremophor® EL. The formulations of the invention are useful for administering paclitaxel, its derivatives, or pharmaceutically acceptable salts of such derivatives to patients in need thereof. The formulations of the invention are suitable for parenteral, oral, local, or transdermal administration to mammals including humans, particularly for intravenous delivery.

1 . A pharmaceutical formulation for administration to a mammal comprising: 
 (a) paclitaxel, a derivative, or a pharmaceutically acceptable salt thereof; and    (b) one or more of a PEG-glyceryl fatty ester, a quaternary ammonium salt or a PEG-fatty alcohol.    
     
     
         2 . The pharmaceutical formulation of  claim 1 , wherein the formulation is cremophor free.  
     
     
         3 . The pharmaceutical formulation of  claim 1 , further comprising an additional active.  
     
     
         4 . The pharmaceutical formulation of  claim 3 , wherein the additional active is cisplatin, carboplatin, tamoxifen, epirubicin, leuprolide, bicalutamide, goserelin implant, irinotecan, gemcitabine, or sargramostim or a pharmaceutically acceptable salt thereof.  
     
     
         5 . The pharmaceutical formulation of  claim 1 , wherein the formulation is suitable for dissolution in an aqueous medium.  
     
     
         6 . The pharmaceutical formulation of  claim 1 , wherein the formulation is in a form of a solid, semisolid, gel, suspension, or emulsion.  
     
     
         7 . The pharmaceutical formulation of  claim 1 , wherein the formulation is in liquid form.  
     
     
         8 . The pharmaceutical formulation of  claim 1 , wherein the formulation is in liquid-concentrate form.  
     
     
         9 . The pharmaceutical formulation of  claim 8 , further comprising ethanol.  
     
     
         10 . The pharmaceutical formulation of  claim 6 , wherein the solid is a lyophilized solid.  
     
     
         11 . The pharmaceutical formulation of  claim 1 , further comprising an aqueous medium.  
     
     
         12 - 153 . (canceled)