Sublingual fentanyl spray and methods of treating pain
View Patent ↗The present invention is directed to sublingual formulations containing fentanyl, a pharmaceutically acceptable salt thereof, or derivative thereof, suitable for administration to a patient, and methods for treatment with the formulations.
1. A sublingual formulation comprising discrete liquid droplets of an effective amount of fentanyl or a fentanyl derivative selected from the group consisting of sufentanil, carfentanil, lofentanil and alfatenil, a free base or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable liquid carrier; said droplets having a mean diameter of from about 30 to about 70 microns.
2. A non-propellant sublingual fentanyl formulation comprising discrete liquid droplets of an effective amount of fentanyl a free base, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable liquid carrier, wherein the sublingual fentanyl formulation comprises:
from about 0.001% to about 15% by weight fentanyl free base;
from about 50% to about 60% by weight of ethanol; and
from about 4% to about 6% by weight of propylene glycol; said droplets having a mean diameter of at least about 10 microns.
3. A non-propellant sublingual fentanyl formulation comprising discrete liquid droplets of an effective amount of fentanyl a free base, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable liquid carrier, wherein the sublingual fentanyl formulation consists essentially of:
from about 0.001% to about 15% by weight fentanyl free base;
from about 50% to about 60% by weight of ethanol; and
from about 1% to about 30% by weight of propylene glycol; said droplets having a mean diameter of at least about 10 microns.
4. A multi-dose device for sublingual administration of a drug comprising:
a reservoir containing the liquid formulation comprising fentanyl, or a fentanyl derivative selected from the group consisting of sufentanil, carfentanil, lofentanil and alfatenil, a free base or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable liquid carrier; and
the device having an actuator which when actuated delivers a therapeutically effective dose of the liquid formulation in the form of liquid droplets having a mean diameter of from about 30 to about 70 microns.
5. A method of treating pain comprising sublingually administering an effective amount of the sublingual formulation according to claim 1 to a human patient experiencing pain.