Abstract: The present invention relates to high concentration ophthalmic pharmaceutical formulations of the phosphodiesterase-4 inhibitor, roflumilast, which are suitable for intravitreal or other ocular administration to injection sites internal or external to the eye and orbit. The compositions can comprise about 2% to about 5% w/v of roflumilast, a viscosity agent, a tonicity agent, a buffer agent, a surfactant, and water. The pharmaceutical compositions are stable with little to no impurities and can be injected from a 27 Gauge or 30 Gauge syringe with minimal force, resulting in therapeutic levels of pharmaceutical in relevant tissues for the ocular surface, anterior compartment, vitreous/posterior compartments, and tissues or chambers surrounding the eye.

Abstract: The present invention relates to stable, ophthalmic pharmaceutical formulations of the phosphodiesterase-4 inhibitor, roflumilast, and methods of making the same. Novel ophthalmic pharmaceutical formulations of roflumilast can comprise a viscosity agent, a surfactant, and a buffer. In preferred embodiments, the pH of the ophthalmic pharmaceutical composition is between 6.0 and 6.7. Methods of making stable, ophthalmic pharmaceutical formulations of roflumilast can include separate active and inactive ingredient processes. Further, the methods can include clarity filtration to mitigate particle size aggregation and to create an optimized suspension. Further, the methods can include terminal sterilization of the final drug product.