Continuous fluorochemical microdispersions for the delivery of lipophilic pharmaceutical agents

A high bioavailability pharmaceutical formulation comprising:

• a substantially homogeneous microdispersion of a pharmaceutically effective amount of at least one lipophilic pharmaceutical agent in a liquid continuous phase, said liquid continuous phase comprising one or more physiologically acceptable lipophilic fluorochemicals, at least one nonfluorinated co-solvent and at least one fluorochemical diluent wherein the fluorochemical diluent is less lipophilic than the lipophilic fluorochemical, said substantially homogeneous microdispersion being formed upon combination of the fluorochemical diluent with the lipophilic fluorochemical.

A method for delivering one or more lipophilic pharmaceutical agents to a physiologic target site, said method comprising the steps of:

• providing a high bioavailability pharmaceutical formulation comprising a substantially homogeneous microdispersion of at least one lipophilic pharmaceutical agent in a liquid continuous phase, said liquid continuous phase comprising one or more lipophilic fluorochemicals, at least one nonfluorinated co-solvent and at least one fluorochemical diluent wherein the fluorochemical diluent is less lipophilic than the lipophilic fluorochemical, said substantially homogeneous microdispersion being formed upon combination of the fluorochemical diluent with the lipophilic fluorochemical;
• and
• introducing a pharmaceutically effective amount of said high bioavailability pharmaceutical formulation to a physiologic target site.

A method for preparing a pharmaceutical material, comprising the steps of:

• providing a pharmaceutical composition comprising a lipophilic first fluorochemical liquid, a nonfluorinated co-solvent and a pharmaceutical agent in a single continuous phase;
• and
• adding to said pharmaceutical composition a sufficient amount of a second fluorochemical liquid less lipophilic than said first fluorochemical liquid that is miscible in said first fluorochemical liquid, thereby causing phase separation of said pharmaceutical agent to form a microdisperse discontinuous phase.

A method for providing a kit for preparing a pharmaceutical preparation, comprising:

• placing a first composition comprising a first lipophilic liquid fluorocarbon, a nonfluorinated co-solvent and a pharmaceutical agent in a single continuous phase in a first container;
• and
• adding a second liquid fluorocarbon miscible with said first lipophilic liquid fluorocarbon to a second container, wherein said second liquid fluorocarbon is less lipophilic than said first lipophilic liquid fluorocarbon, such that upon combination of said first composition and said second liquid fluorocarbon, a phase separation of said pharmaceutical agent occurs to form a microdisperse discontinuous phase comprising said pharmaceutical agent.