Formulations and Dosage Forms of Oxidized Phospholipids

Abstract

The current disclosure provides pharmaceutical compositions containing an oxidized phospholipid, such as 1-hexadecyl-2-(4′-carboxybutyl)-glycero-3-phosphocholine (VB-201) and a thermosoftening carrier, e.g., a poloxamer. The pharmaceutical competitions may further comprise an anti-adherent agent, such as talc and/or a thixotropic agent. The current disclosure further provides processes for preparing the pharmaceutical compositions. The disclosure further provides capsules containing the pharmaceutical compositions. Uses of such pharmaceutical compositions and capsules in treating inflammatory disorders are also disclosed.

1 - 122 . (canceled) 
     
     
         123 . A pharmaceutical composition comprising an oxidized phospholipid, a thermosoftening carrier, and an anti-adherent agent,
 wherein the weight ratio of said anti-adherent agent to said oxidized phospholipid is about 1:5 to about 5:1,   wherein said oxidized phospholipid is 1-hexadecyl-2-(4′-carboxybutyl)-glycero-3-phosphocholine (VB-201),   wherein said thermosoftening carrier is a poloxamer with a molecular weight from about 7000 to 10000 daltons or a polyethylene glycol with a molecular weight from about 2000 to 8000 daltons, and   wherein said anti-adherent agent is talc.   
     
     
         124 . The pharmaceutical composition of  claim 123 , wherein said thermosoftening carrier is a poloxamer with a molecular weight from about 7000 to 10000 daltons. 
     
     
         125 . The pharmaceutical composition of  claim 124 , wherein said poloxamer is poloxamer 188. 
     
     
         126 . The pharmaceutical composition of  claim 123 , wherein said thermosoftening carrier is a polyethylene glycol with a molecular weight from about 2000 to 8000 daltons. 
     
     
         127 . The pharmaceutical composition of  claim 123 , wherein said weight ratio of said anti-adherent agent to said oxidized phospholipid is from about 1:4 to about 1:1. 
     
     
         128 . The pharmaceutical composition of  claim 123 , further comprising a thixotropic agent. 
     
     
         129 . The pharmaceutical composition of  claim 128 , wherein said thixotropic agent is selected from the group consisting of fumed silica, kieselguhr, gums, cellulose derivatives, starches, polymers, emulsifiers, and clay derivatives, attapulgite, mica, synthetic magnesium phyllosilicates, layered silicates, modified smectites, hectorite, and sepiolite. 
     
     
         130 . The pharmaceutical composition of  claim 129 , wherein said thixotropic agent is a fumed silica. 
     
     
         131 . The pharmaceutical composition of  claim 130 , wherein said thermosoftening carrier is poloxamer 188. 
     
     
         132 . The pharmaceutical composition of  claim 123 , wherein said pharmaceutical composition is a liquid-fill composition. 
     
     
         133 . The pharmaceutical composition of  claim 126 , wherein the polyethylene glycol has a molecular weight of about 6000 daltons. 
     
     
         134 . The pharmaceutical composition of  claim 127 , wherein said weight ratio of said anti-adherent agent to said oxidized phospholipid is about 1:4. 
     
     
         135 . The pharmaceutical composition of  claim 133 , wherein said weight ratio of said anti-adherent agent to said oxidized phospholipid is about 1:4. 
     
     
         136 . The pharmaceutical composition of  claim 123 , wherein said thermosoftening carrier is poloxamer 188, and wherein said weight ratio of said anti-adherent agent to said oxidized phospholipid is about 1:4. 
     
     
         137 . The pharmaceutical composition of  claim 136 , further comprising a thixotropic agent. 
     
     
         138 . The pharmaceutical composition of  claim 137 , wherein said thixotropic agent is a fumed silica. 
     
     
         139 . A method of treating an inflammatory disease or disorder comprising administering to a subject in need thereof a therapeutically effective amount of the pharmaceutical composition of  claim 123 . 
     
     
         140 . The method of  claim 139 , wherein the inflammatory disease or disorder is Crohn's disease. 
     
     
         141 . The method of  claim 139 , wherein the inflammatory disease or disorder is hepatic cirrhosis. 
     
     
         142 . The method of  claim 139 , wherein the inflammatory disease or disorder is an autoimmune disease or disorder.