Pharmaceutical solution of asenapine for sublingual or buccal use
A kit for treating psychosis by administering a pharmaceutically acceptable liquid composition of Asenapine to oral mucosa includes a formulation having Asenapine, or a pharmaceutically acceptable salt or hydrate thereof, ethanol, and water and a multidose pump filled with the formulation. The Asenapine compositions are stable for an extended period of time at normal storage conditions.
1. A pharmaceutically acceptable liquid composition of Asenapine for sublingual or buccal delivery comprising:
Asenapine, or a pharmaceutically acceptable salt or hydrate thereof;
ethanol; and
water,
wherein the composition is free of a polyol and is stable for an extended period of time at normal storage conditions.
2. The composition of claim 1 , wherein the composition comprises greater than about 10% by volume of ethanol.
3. The composition of claim 2 , wherein the composition comprises about 10% to about 80% by volume of ethanol.
4. The composition of claim 3 , wherein the composition comprises about 50% to about 70% by volume of ethanol.
5. The composition of claim 1 , wherein the Asenapine, or a pharmaceutically acceptable salt or hydrate thereof, is Asenapine maleate.
6. The composition of claim 1 , further comprising pharmaceutically acceptable excipients selected from one or more of preservatives, buffers, taste modifiers, flavors or combinations thereof.
7. The composition of claim 6 , wherein the composition comprises EDTA.
8. The composition of claim 6 , wherein the composition comprises L-Methionine.
9. The composition of claim 1 , wherein the composition exhibits less than 0.3% weight loss after storage at 25° C./60% RH for up to 35 days.
10. The composition of claim 9 , wherein the composition exhibits less than 0.07% weight loss after storage at 25° C./60% RH for up to 35 days.
11. A pharmaceutically acceptable liquid composition of Asenapine for sublingual or buccal delivery comprising:
Asenapine, or a pharmaceutically acceptable salt or hydrate thereof;
greater than about 10% ethanol; and
water; wherein the composition is free of a polyol.
12. The composition of claim 11 , wherein the Asenapine, or a pharmaceutically acceptable salt or hydrate thereof, is Asenapine maleate.
13. The composition of claim 11 , wherein the composition comprises about 10% to about 80% by volume of ethanol.
14. The composition of claim 13 , wherein the composition comprises about 50% to about 70% by volume of ethanol.
15. The composition of claim 11 , further comprising pharmaceutically acceptable excipients selected from one or more of preservatives, buffers, taste modifiers, flavors or combinations thereof.
16. A method of treating psychosis by administering a therapeutically effective amount of a composition of claim 1 to a patient in need thereof.
17. The method of claim 16 , wherein about 2.5 mg to about 10 mg Asenapine is delivered to the patient's mouth.
18. The method of claim 17 , wherein an average dispensed volume of about 140 μL of the composition is administered to the patient by spraying the composition into the patient's mouth.
19. A kit for treating psychosis by administering a pharmaceutically acceptable liquid composition of Asenapine to oral mucosa comprising:
a formulation including Asenapine, or a pharmaceutically acceptable salt or hydrate thereof, ethanol, and water; and
a multidose pump filled with the formulation; wherein the composition is free of a polyol.