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Claims for Patent: 8,486,973

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Claims for Patent: 8,486,973

Title:Sublingual fentanyl spray
Abstract: 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.
Inventor(s): Kottayil; S. George (Phoenix, AZ), Goskonda; Venkat R. (Gurnee, IL), Zhu; Zhongyuan (Vernon Hills, IL), Kattookaran; Linet (Des Plaines, IL), Parikh; Neha (Chicago, IL)
Assignee: Insys Therapeutics, Inc. (Phoenix, AZ)
Application Number:12/221,333
Patent Claims: 1. A method of treating pain comprising administering to a patient in need thereof a propellant-free sublingual spray formulation comprising an effective amount of fentanyl, the formulation providing a mean T.sub.max of about 1.28+/-0.60; and wherein said sublingual spray formulation comprises droplets having a mean diameter of at least about 10 microns; wherein said sublingual spray formulations comprises: from about 0.1% to about 0.8% by weight of fentanyl or a pharmaceutically acceptable salt thereof; from about 50% to about 60% by weight of ethanol; and from about 4% to about 6% by weight of propylene glycol.

2. The method of claim 1, wherein the concentration of fentanyl in the sublingual spray formulation is from about 1 mg/mL to about 8 mg/mL.

3. The method of claim 1, wherein the concentration of fentanyl in the sublingual spray formulation is selected from the group consisting of about 1 mg/mL, about 2 mg/mL, about 4 mg/mL, about 6 mg/mL and about 8 mg/mL.

4. The method of claim 1, which provides a mean C.sub.max of about 0.813 ng/ml+/-0.252 based on a sublingual dose of about 400 mcg fentanyl when administered to humans.

5. The method of claim 1, which provides a dosage amount of fentanyl selected from the group consisting of about 100 mcg, about 200 mcg, about 600 mcg and about 800 mcg, and provides a mean C.sub.max which is substantially dose proportional to the sublingual spray formulation containing 400 mcg fentanyl dosage amount, when administered to humans.

6. The method of claim 1, provides a substantially dose proportional mean C.sub.max based on a mean C.sub.max of about 0.813 ng/ml+/-0.252 for a 400 mcg fentanyl dose when administered to humans.

7. The method of claim 1, which provides a mean T.sub.max when administered to humans selected from the group consisting of: about 1.12 hours when the formulation provides a 100 mcg dose, about 1.04 hours when the formulation provides a 200 mcg dose, about 0.97 hours when the formulation provides a 400 mcg dose, about 0.987 hours when the formulation provides a 600 mcg dose, and about 1.06 hours when the formulation provides a 800 mcg dose.

8. The method of claim 1, which provides a plasma concentration after administration to humans selected from the group consisting of: about 60% of the mean Cmax in about 10 minutes, about 86% of the mean Ciax by about 20 minutes and a combination thereof.

9. The method of claim 1, which provides a plasma concentration after administration to humans that is greater than about 80% of the mean C.sub.max for about 2 hours.

10. The method of claim 1, wherein the sublingual spray formulation comprises 400 mcg of fentanyl, and provides one or more mean pharmacokinetic values selected from the group consisting of: AUC.sub.last 4.863+/-1.70821 hr*ng/mL, AUC.sub.inf 5.761+/-1.916 hr*ng/mL, and AUC.sub.extrap 10.26+/-5.66%, when administered to humans.

11. The method of claim 1, which provides a dosage amount of fentanyl when administered to humans which is substantially dose proportional to the dosage which contains about 400 mcg fentanyl selected from the group consisting of about 100 mcg, about 200 mcg, about 600 mcg, about 800 mcg, and provides one or more pharmacokinetic values selected from the group consisting of: mean AUC.sub.last, mean AUC.sub.inf, and mean AUC.sub.extrap.

12. The method of claim 1, which provides a substantially dose proportional mean AUC.sub.last based on a mean AUC.sub.last of about 4.863+/-1.70821 hr*ng/mL for a 400 mcg fentanyl dose when administered to humans.

13. The method of claim 1, wherein the sublingual spray formulation comprises a 400 mcg dose of fentanyl, providing a geometric mean ln(C.sub.max) of about 0.7865 ng/ml when a dose is administered to humans.

14. The method of claim 1, wherein the sublingual spray formulation comprises a 400 mcg dose of fentanyl, providing a mean F(AUC.sub.last) of about 0.721+/-0.199 ng/mL when a dose is administered to humans.

15. The method of claim 1, wherein the sublingual spray formulation comprises a 400 meg dose of fentanyl when a dose is administered to humans, providing a mean F (bioavailability) selected from the group consisting of: about 71%+/-16%, 0.721+/-0.199 based on AUC.sub.last and about 0.756+/-0.212 based on AUC.sub.inf, or combinations thereof.

16. The method of claim 1, wherein the sublingual spray formulation further comprises water.

17. The method of claim 1 wherein the sublingual formulation provides a substantially dose proportional mean C.sub.max based on a mean C.sub.max of about 0.813 ng/ml+/-0.252 for a 400 mcg fentanyl dose when administered to humans.

18. The method of claim 1 wherein the sublingual formulation provides a substantially dose proportional mean AUC.sub.last based on a mean AUC.sub.last of about 4.863+/-1.70821 hr*ng/mL for a 400 mcg fentanyl dose when administered to humans.

19. A method of manufacturing a sublingual spray formulation comprising an effective amount of fentanyl and at least one pharmaceutically acceptable excipient comprising: admixing fentanyl, purified water and dehydrated alcohol and placing the mixture into a sublingual delivery device; the formulation providing a mean T.sub.max of about 1.28+/-0.60 hours when a dose is administered sublingually to humans and upon delivery, providing a mean aerodynamic particle size of at least about 10 microns; wherein said sublingual spray formulation comprises: from about 0.1% to about 0.8% by weight of fentanyl or a pharmaceutically acceptable salt thereof; from about 50% to about 60% by weight of ethanol; and from about 4% to about 6% by weight of propylene glycol.

20. A method of treating pain comprising administering to a patient in need thereof a propellant-free sublingual spray formulation comprising an effective amount of fentanyl, the formulation providing a mean time to 60% maximum plasma concentration (Tmax) of fentanyl of about 10 minutes; and wherein said sublingual spray formulation comprises droplets having a mean diameter of at least about 10 microns; wherein said sublingual spray formulations comprises: from about 0.1% to about 0.8% by weight of fentanyl or a pharmaceutically acceptable salt thereof; from about 50% to about 60% by weight of ethanol; and from about 4% to about 6% by weight of propylene glycol.
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