Preparation of solid cyclodextrin complexes for ophthalmic active pharmaceutical ingredient delivery

Abstract

The present disclosure relates to ophthalmic compositions comprising solid complexes of active pharmaceutical ingredients, in particular kinase inhibitors and cyclodextrin, and to their uses in the treatment of posterior ocular conditions. More specifically, the disclosure relates to an aqueous composition comprising drug/cyclodextrin complexes of a tyrosine kinase inhibitor or a salt thereof, and a cyclodextrin, wherein said complexes have a complexation efficacy (CE) of more than 0.01, preferably more than 0.1 in the aqueous composition, and/or the tyrosine kinase inhibitor or a salt thereof has a ratio of the half maximal inhibitory concentration (IC50) of the epidermal growth factor receptors (EGFR) to the half maximal inhibitory concentration (IC50) of the vascular endothelial growth factor receptors (VEGFR2) that is greater than 2000, preferably greater than 5000.

Dependencies are inferred from the claim text.