ORAL SPRAY FORMULATIONS AD METHODS FOR ADMINISTRATION OF SILDENAFIL
The present disclosure is directed to chemically-stable and pharmaceutically-acceptable sildenafil oral spray formulations for the treatment of male erectile dysfunction, wherein the oral spray formulation has a pH of about 1.5 to less than 3.0. The present disclosure is also directed to methods for treating male erectile dysfunction.
1 . An oral spray formulation for the treatment of erectile dysfunction, comprising sildenafil base or a pharmaceutically acceptable salt thereof, wherein the pH of the formulation is about 1.5 to less than 3.0.
2 . The oral spray formulation of claim 1 , wherein the sildenafil base is present in an amount of about 7 to about 12% w/v of the formulation.
3 .- 5 . (canceled)
6 . The oral spray formulation of claim 1 , wherein the sildenafil salt is sildenafil citrate.
7 . The oral spray formulation of claim 1 , wherein the pH of the formulation is about 1.5 to less than 3.0.
8 . The oral spray formulation of claim 1 , wherein the formulation comprises a polar solvent.
9 . The oral spray formulation of claim 8 , wherein the polar solvent comprises propylene glycol and ethyl alcohol.
10 . The oral spray formulation of claim 9 , wherein the ratio of propylene glycol:ethyl alcohol is about 62.5:37.5% v/v.
11 . The oral spray formulation of claim 1 , wherein the formulation comprises one or more pH-adjusting agents.
12 .- 16 . (canceled)
17 . The oral spray formulation of claim 1 , wherein the formulation comprises a taste-masking agent.
18 .- 20 . (canceled)
21 . A method for the treatment of erectile dysfunction, comprising administering to a patient an oral spray formulation comprising sildenafil base or a pharmaceutically acceptable salt thereof, wherein the pH of the formulation is about 1.5 to less than 3.0.
22 . The method of claim 21 , wherein the sildenafil base is present in an amount of about 7 to about 12% w/v of the formulation.
23 .- 25 . (canceled)
26 . The method of claim 21 , wherein the sildenafil salt is sildenafil citrate.
27 . The method of claim 21 , wherein the pH of the formulation is about 1.5 to less than 3.0.
28 . The method of claim 21 , wherein the formulation comprises a polar solvent.
29 . The method of claim 28 , wherein the polar solvent comprises propylene glycol and ethyl alcohol.
30 . The method of claim 29 , wherein the ratio of propylene glycol:ethyl alcohol is about 62.5:37.5% v/v.
31 . The method of claim 21 , wherein the formulation comprises one or more pH-adjusting agents.
32 .- 36 . (canceled)
37 . The method of claim 21 , wherein the formulation comprises a taste-masking agent.
38 .- 40 . (canceled)
41 . The method of claim 21 , wherein the amount of sildenafil administered per spray is selected from the group consisting of: 10 mg, 20 mg, and 30 mg.
42 . (canceled)
43 . (canceled)
44 . The method of claim 41 , wherein the sildenafil exposure in the patient results in a ln-transformed dose-adjusted to 25 mg geometric mean AUC 0-t (ng-hr/mL) of approximately 299.36.
45 . The method of claim 41 , wherein the sildenafil exposure in the patient results in a ln-transformed dose-adjusted to 25 mg geometric mean AUC 0-t (ng-hr/mL) of approximately 323.16.
46 . The method of claim 41 , wherein the sildenafil exposure in the patient results in a ln-transformed dose-adjusted to 25 mg geometric mean AUC 0-t (ng-hr/mL) of approximately 304.98.
47 . The method of claim 41 , wherein the sildenafil exposure in the patient results in a ln-transformed dose-adjusted to 25 mg geometric mean AUC 0-inf (ng-hr/mL) of approximately 310.60.
48 . The method of claim 41 , wherein the sildenafil exposure in the patient results in a ln-transformed dose-adjusted to 25 mg geometric mean AUC 0-inf (ng-hr/mL) of approximately 331.22.
49 . The method of claim 41 , wherein the sildenafil exposure in the patient results in a ln-transformed dose-adjusted to 25 mg geometric mean AUC 0-inf (ng-hr/mL) of approximately 311.05.
50 . The oral spray formulation of claim 1 , wherein the amount of sildenafil administered per spray is selected from the group consisting of: 10 mg, 20 mg, and 30 mg.
51 . (canceled)
52 . (canceled)
53 . The oral spray formulation of claim 17 , wherein the taste-masking agent comprises mint.
54 . (canceled)
55 . The oral spray formulation of claim 53 , further comprising a fruit and/or chocolate flavor.
56 . The method of claim 37 , wherein the taste-masking agent comprises mint.
57 . (canceled)
58 . The method of claim 56 , further comprising a fruit and/or chocolate flavor.
59 . (canceled)
60 . (canceled)
61 . (canceled)
62 . (canceled)