초록 ▼

The invention is directed to sublingual spray formulations containing sildenafil. The invention is further directed to methods of treating male sexual dysfunction or pulmonary arterial hypertension by administering sublingual spray formulations containing sildenafil to patients in need of such treat

The invention is directed to sublingual spray formulations containing sildenafil. The invention is further directed to methods of treating male sexual dysfunction or pulmonary arterial hypertension by administering sublingual spray formulations containing sildenafil to patients in need of such treatments.

대표청구항 ▼

1. A sublingual spray formulation comprising: from about 2% w/w to about 35% w/w sildenafil or a salt thereof;from about 0.1% w/w to about 70% w/w of a solvent selected from the group consisting of water, ethanol, glycerin, propylene glycol, polyethylene glycol 400 and a combination thereof; andfrom

1. A sublingual spray formulation comprising: from about 2% w/w to about 35% w/w sildenafil or a salt thereof;from about 0.1% w/w to about 70% w/w of a solvent selected from the group consisting of water, ethanol, glycerin, propylene glycol, polyethylene glycol 400 and a combination thereof; andfrom about 0.1% w/w to about 60% w/w of at least one acid, wherein the formulation has a pH from 3 to about 5 and wherein w/w denotes weight by weight of the formulation. 2. The formulation of claim 1, wherein the formulation is a simple solution. 3. The formulation of claim 1, wherein the sildenafil is a salt selected from the group consisting of citrate, hydrochloride, halide, sulfate, phosphate, acetate, maleate, succinate, ascorbate, carbonate, mesylate and lactate. 4. The formulation of claim 1, wherein the solvent comprises from about 0.1% w/w to about 50% w/w water. 5. The formulation of claim 1, wherein the solvent comprises from about 10% w/w to about 70% w/w ethanol. 6. The formulation of claim 1, wherein the solvent comprises from about 1% w/w to about 30% w/w glycerin or propylene glycol or polyethylene glycol 400 or a combination thereof. 7. The formulation of claim 1, wherein the at least one acid is hydrochloric acid. 8. The formulation of claim 1, wherein the hydrochloric acid may be from 0.1 N to 12N. 9. The formulation of claim 1 wherein the formulation is propellant free. 10. The formulation of claim 1, further comprising a permeation enhancer comprising caprylic acid. 11. The formulation of claim 1, wherein the formulation does not contain a permeation enhancer. 12. The formulation of claim 10, wherein the caprylic acid is at a concentration from about 0.1% w/w to about 10% w/w. 13. The formulation of claim 10, wherein the caprylic acid is at a concentration from about 0.1% w/w to about 5 w/w. 14. The formulation of claim 10, wherein the permeation enhancer further comprises a second compound selected from the group consisting of menthol, limonene, carvone, methyl chitosan, polysorbates, sodium lauryl sulfate, glyceryl oleate, caproic acid, enanthic acid, pelargonic acid, capric acid, undecylenic acid, lauric acid, myristic acid, palmitic acid, oleic acid, stearic acid, linolenic acid, arachidonic acid, benzethonium chloride, benzethonium bromide, benzalkonium chloride (BKC), cetylpyridium chloride, edetate disodium dihydrate, sodium desoxycholate, sodium deoxyglycolate, sodium glycocholate, sodium caprate, sodium taurocholate, sodium hydroxybenzoyal amino caprylate, dodecyl dimethyl aminopropionate, L-lysine, glycerol oleate, glyceryl monostearate, citric acid, peppermint oil and a combination thereof. 15. The formulation of claim 14, wherein the second compound is menthol. 16. The formulation of claim 15, wherein the menthol is at a concentration from about 0.1% w/w to about 5 w/w. 17. The formulation of claim 15, wherein the menthol is at a concentration from about 0.1% w/w to about 1 w/w.