Process for manufacturing ophthalmic oil-in-water emulsions

摘要

The present invention relates to new processes for the preparation of oil-in-water emulsions useful in ophthalmic applications. In particular, processes are provided that include preparing a pre-concentrate of the oil-in-water emulsion, and diluting the pre-concentrate obtained to form the desired oil-in-water emulsion. The present invention also provides pharmaceutical compositions comprising an oil-in-water emulsion prepared by an inventive process, and methods of using these compositions for the treatment of an eye disease or condition.

主权项

1. A process for manufacturing a cationic ophthalmic oil-in-water emulsion, said process comprising steps of:
manufacturing a pre-concentrate of a cationic ophthalmic oil-in-water emulsion, said manufacturing comprising a step of emulsifying an oil phase with an aqueous phase and at least one surface-active agent to obtain the pre-concentrate, wherein the oil phase comprises at least one oil suitable for ophthalmic use, and wherein the pre-concentrate obtained is a cationic emulsion having a content in oil of between 6% and 50% v/v; and diluting one volume of the pre-concentrate with between 2 and 50 volumes of a diluting aqueous solution, wherein said emulsifying step comprises using a device selected from the group consisting of a colloid mill, a rotor/stator homogenizer, a high pressure homogenizer, and a sonicating homogenizer to obtain said emulsion, wherein the at least one surface-active agent is tyloxapol.