PDE-5 inhibitors for transmucosal delivery

摘要

A pharmaceutical formulation for the transmucosal delivery of a phopshodiesterase-5 (PDE-5) inhibitor comprises a PDE-5 inhibitor and a carrier in which the PDE-5 inhibitor is soluble or forms a suspension or emulsion. The PDE-5 inhibitor may be hydrophilic, preferably selected from sildenafil mesylate or a salt of vardenafil, where the carrier may be an aqueous solution, such that the PDE5 inhibitor is solubilised in the carrier. Alternatively, the PDE-5 inhibitor may be hydrophobic, preferably selected from sildenafil, sildenafil citrate, vardenafil or tadalafil or a salt thereof, where the carrier may be an aqueous solution, such that the PDE5 inhibitor is suspended or emulsified in the carrier. Alternatively, the PDE-5 inhibitor may be lipophobic, preferably, selected from sildenafil, vardenafil or tadalafil or a salt thereof, where the carrier may be an oil that comprises a glyceride, such that the PDE5 inhibitor is suspended or emulsified in the carrier. Preferably the oil carrier is a medium chain triglyceride. Preferably the formulation is delivered buccally or sublingually. A pharmaceutical composition comprising a PDE5 inhibitor for use in inhibiting PDE5 activity in vivo wherein the composition is delivered via the transmucosal route is also outlined. Preferably the composition is for use in treating a disease or condition responsive to a PDE5 inhibitor in particular, erectile dysfunction or pulmonary arterial hypertension.