PHOSPHOLIPID DEPOT

摘要

The present invention provides a clear depot comprising at least one hydrophilic water-soluble pharmaceutically active agent selected from the group consisting of vancomycin, gentamicin, a pharmaceutically acceptable salt thereof and a mixture thereof, water, a phospholipid, an oil, optionally a pH adjusting agent, and a viscosity modifying agent selected from the group consisting of ethanol, isopropanol, and a mixture thereof, wherein the water present in the depot is no more than about 4 wt % relative to the total weight of the depot and the depot has a pH of between about 3 and about 6, method of making and administering same.

主权项

1. A method for making a depot comprising:
(1) forming an oil-in-water emulsion including a phospholipid, an oil, at least one hydrophilic water-soluble pharmaceutically active agent selected from the group consisting of vancomycin, gentamicin, a pharmaceutically acceptable salt thereof or a mixture thereof and water; (2) homogenizing the emulsion to obtain a primary emulsion; (3) microfluidizing the primary emulsion to obtain a monophasic solution; (4) ensuring the pH of the primary emulsion and/or the monophasic solution is between about 3 to about 6 by adjusting the pH as necessary, (5) lyophilizing the monophasic solution of desired pH to obtain a dry paste, (6) adding a viscosity modifying agent to the dry paste in an amount of about 25 wt % or more of the total weight of a resulting viscosity modified solution, (7) removing at least some of the viscosity modifying agent to obtain a depot having from about 1 wt % to about 20 wt % of the viscosity modifying agent relative to the total weight of the depot, and (8) sterilizing the depot.