Sublingual naloxone spray
View Patent ↗The invention provides storage stable sublingual formulations containing naloxone, a pharmaceutically acceptable salt or a derivative thereof. The invention further provides methods for treating opioid dependence, opioid overdose, and congenital insensitivity to pain with anhidrosis by administering the sublingual formulations of the present invention to a patient in need thereof.
1. A storage stable sublingual spray formulation comprising:
from about 1% to about 10% w/w naloxone, or a pharmaceutically acceptable salt thereof;
from about 30% to about 40% w/w water;
from about 50% to about 60% w/w ethanol;
from about 3% to about 7% w/w propylene glycol;
from about 0.005% to about 0.08% w/w of an antioxidant; and
from about 0.002% to 0.008% of a chelating agent,
wherein the % w/w is of the total formulation.
2. The sublingual spray formulation of claim 1 , wherein the chelating agent is edetate disodium dihydrate.
3. The sublingual spray formulation of claim 2 , wherein the antioxidant is selected from the group consisting of butylated hydroxyanisole, butylated hydroxytoluene, sodium ascorbate, sodium thiosulfate, and a combination thereof.
4. A method of treating opioid dependence comprising administering the sublingual spray formulation of claim 1 to a patient in need thereof.
5. A method of treating opioid overdose comprising administering the sublingual spray formulation of claim 1 to a patient in need thereof.
6. A method of treating congenital insensitivity to pain with anhidrosis comprising administering the sublingual spray formulation of claim 1 to a patient in need thereof.