Sublingual ondansetron spray
View Patent ↗The invention is directed to sublingual spray formulations containing ondansetron, a pharmaceutically acceptable salt thereof, and a solvent consisting of ethanol and glycerin, suitable for administration to humans, and methods for treatment with sublingual formulations.
1. A sublingual spray formulation comprising:
from about 3% to about 11% w/w ondansetron;
from about 30% to about 60% w/w ethanol;
from about 20% to about 48% w/w glycerin;
from about 0.05% to about 0.5% w/w menthol; and
from about 0.5% to about 5% w/w caprylic acid, wherein w/w denotes weight by total weight of the formulation.
2. The formulation of claim 1 wherein the formulation is a liquid.
3. The formulation of claim 1 wherein the formulation is substantially free of water.
4. The formulation of claim 1 wherein the formulation is free of propellant.
5. The formulation of claim 1 further comprising water.
6. The formulation of claim 1 further comprising a pharmaceutically acceptable sweetener.
7. The sublingual spray formulation of claim 1 wherein the formulation is capable of producing a droplet size distribution wherein:
a) the mean Dv(10) is from about 10 to about 35 microns during administration;
b) the mean Dv(50) is from about 40 to about 200 microns during administration; and
c) the mean Dv(90) is from about 150 to about 700 microns during administration.
8. The sublingual spray formulation of claim 1 wherein the formulation is capable of producing a spray plume wherein:
a) the mean ovality ratio is from about 1.0 to about 2.0 and
b) the mean angle is from about 25 to about 65 degrees.
9. A sublingual spray formulation comprising:
ondansetron at a concentration of about 4.24% w/w;
ethanol at a concentration of about 50% w/w;
glycerin at a concentration of about 30% w/w;
menthol at a concentration of about 0.5% w/w; and
caprylic acid at a concentration of about 2% w/w, wherein w/w denotes weight by total weight of the formulation.
10. The sublingual formulation of claim 9 further comprising:
about 0.6% w/w sucralose;
about 0.001% w/w edetate disodium dihydrate;
about 0.01% w/w benzalkonium chloride; and
about 0.08% w/w of strawberry flavor.
11. A method for treating or preventing nausea and emesis in humans associated with chemotherapy, radiation or surgery for cancer treatment comprising administering the formulation of claim 1 to a patient in need thereof.
12. The method of claim 11 wherein from about 50 to about 400 μL of the formulation of claim 1 is administered to the patient in need thereof.
13. The method of claim 12 wherein from about 100 to about 200 μL of the formulation of claim 1 is administered to the patient in need thereof.
14. A method for treating or preventing nausea and emesis in humans associated with chemotherapy, radiation or surgery for cancer treatment comprising administering the formulation of claim 4 to a patient in need thereof.
15. The method of claim 14 wherein from about 50 to about 400 μL of the formulation of claim 1 is administered to the patient in need thereof.
16. The method of claim 15 wherein from about 100 to about 200 μL of the formulation of claim 1 is administered to the patient in need thereof.