Fluoropolymer-based emulsions for the intravenous delivery of fluorinated volatile anesthetics

摘要

The present invention provides therapeutic formulations, including therapeutic emulsions and nanoemulsions, and related methods for the delivery of fluorinated therapeutic compounds, including an important class of low boiling point perfluorinated and/or perhalogenated volatile anesthetics. Emulsion-based fluorinated volatile anesthetic formulations compatible with intravenous administration are provided that are capable of delivering and releasing amounts of fluorinated volatile anesthetic compounds effective for inducing and maintaining anesthesia in patients. Intravenous delivery of the present emulsion-based fluorinated volatile anesthetic formulations permits anesthetic levels in a patient to be selectively adjusted very rapidly and accurately without the need to hyperventilate patients and without the use of irritating agents.

主权项

1. A therapeutic formulation comprising:
an aqueous solution; semi-fluorinated block copolymers having a hydrophilic block and a fluorophilic block, wherein said fluorophilic block is a perfluorinated linear alkyl chain having a length of 6 to 16 carbons, and wherein said hydrophilic block is a poly(ethylene glycol) block having a molecular weight selected over the range of 500 g mol−1 to 5,000 g mol−1; a fluorinated anesthetic compound selected from the group consisting of sevoflurane, isoflurane, desflurane, enflurane and methoxyflurane; and a stabilizing additive comprising a perhalogenated fluorocarbon selected from the group consisting of perfluorooctyl bromide and perfluorodecalin; wherein said formulation is a nanoemulsion comprising a continuous phase and a dispersed phase, wherein said continuous phase comprises said aqueous solution and said dispersed phase comprises said semi-fluorinated block copolymers, said fluorinated anesthetic compound and said stabilizing additive; and wherein said fluorinated anesthetic compound is greater than or equal to 5% by volume of said therapeutic formulation, said perhalogenated fluorocarbon is 1% to 20% by volume of said therapeutic formulation; and said semi-fluorinated block copolymers have a concentration selected over the range of 1 mg ml−1 to 45 mg ml−1.