Formulations and dosage forms of oxidized phospholipids

摘要

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 compositions 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.

主权项

1. A pharmaceutical composition comprising an oxidized phospholipid having a structure according to Formula (1): wherein R1 is C14-C20 straight or branched alkyl; R3 is selected from the group consisting of phosphorylethanolamine, phosphorylcholine, phosphorylethanolamine-N-glutaric acid, and phosphorylserine; R5 is selected from the group consisting of H, a negative charge, methyl, and ethyl; and X1 is C4 or C5 alkylene,the composition further comprising a thermosoftening carrier and an anti-adherent agent, wherein said thermosoftening carrier has a melting point from about 40° C. to about 100° C., wherein the weight ratio of said anti-adherent agent to said oxidized phospholipid is about 1:5 to about 5:1, wherein said thermosoftening carrier is a poloxamer or a polyethylene glycol, and wherein said anti-adherent agent is selected from the group consisting of talc, magnesium stearate, cellulose, cellulose derivatives, lactose, gelatin, alginates, aluminum hydroxide, magnesium oxide, clays, attapulgite, bentonite, carrageenan, copovidone, hectorite, polymethacrylates, sodium docusate, erythritol, povidones, croscarmellose sodium, dextrates, starches, iron oxide, kaolin, silicates, corn flour, sugars, calcium carbonate, magnesium carbonate, calcium phosphate, calcium sulfate, bicarbonates, citrate salts, and titanium dioxide.