Suspensions of cyclosporin a form 2

Abstract

Disclosed herein are methods of formulating cyclosporin A Form 2.

What is claimed is: 
     
         1 . A nanosuspension formulation comprising
 particles of cyclosporin A form 2 and   a vehicle,   wherein the average size (d90) of the particles is less than about 10 μm.   
     
     
         2 . The formulation of  claim 1 , wherein the vehicle comprises at least one surfactant and at least one stabilizer. 
     
     
         3 . The formulation of  claim 2 , wherein cyclosporin is at a concentration of about 0.01% to about 10%. 
     
     
         4 . The formulation of  claim 3 , wherein the vehicle comprises one or more surfactants selected from the group consisting of polyoxyethylene (20) sorbitan monooleate, polyethylene glycol 660 hydroxystearate, polyoxyethylene (40) stearate Myrj 52, pluronic F68, polyoxyethylene sorbitan monolaurate, and sodium glycocholate. 
     
     
         5 . The formulation of  claim 3 , wherein the vehicle comprises one or more surfactants selected from the group consisting of polyoxyethylene (20) sorbitan monooleate at a concentration of about 0.1% to about 5% (w/v), polyethylene glycol 660 hydroxystearate at a concentration of about 0.1% to about 5% (w/v), polyoxyethylene (40) stearate Myrj 52 at a concentration of about 0.1% to about 5% (w/v), pluronic F68 at a concentration of about 0.1% to about 5% (w/v), polyoxyethylene sorbitan monolaurate at a concentration of about 0.1% to about 5% (w/v), and sodium glycocholate at a concentration of about 0.1% to about 5% (w/v). 
     
     
         6 . The formulation of  claim 4 , wherein the vehicle comprises at least one stabilizer selected from the group consisting of hydroxy propyl cellulose, hydroxypropylmethyl cellulose, hydroxyethylcellulose, polyvinyl pyrolidone, and carboxymethylcellulose. 
     
     
         7 . The formulation of  claim 5 , wherein the vehicle comprises one or more stabilizers each selected from the group consisting of hydroxypropyl cellulose at a concentration of about 0.1% to about 5% (w/v), hydroxypropylmethyl cellulose at a concentration of about 0.1% to about 5% (w/v), hydroxyethylcellulose at a concentration of about 0.1% to about 5% (w/v), and polyvinyl pyrolidone at a concentration of about 0.1% to about 5% (w/v), and carboxymethylcellulose at a concentration of about 0.1% to about 5% (w/v). 
     
     
         8 . The formulation of  claim 7 , wherein the vehicle further comprises one or more ingredients selected from glycerin, mannitol, Pemulen TR-2, sodium citrate dihydrate, potassium chloride, boric acid, sodium borate decahydrate, and water. 
     
     
         9 . The formulation of  claim 7 , wherein the vehicle further comprises one or more ingredients selected from glycerin at concentration of about 1.0% to about 2.2%, mannitol at concentration of about 0.5%, Pemulen TR-2 at concentration of about 0.01% to about 0.1%, sodium citrate dihydrate at concentration of about 0.4%, potassium chloride at concentration of about 0.14%, boric acid at concentration of about 0.25%, sodium borate decahydrate at concentration of about 0.41%, and water. 
     
     
         10 . The formulation of  claim 1 , wherein the average size of the particles is less than about 1 μm.