Pharmacokinetics of a Novel Sildenafil Orodispersible Film Administered by the Supralingual and the Sublingual Route to Healthy Men.

BACKGROUND: Sildenafil was the first selective drug available on the market as oral therapy for erectile dysfunction (ED). A novel sildenafil orodispersible film (ODF) for ED treatment, containing sildenafil citrate, has recently been marketed. OBJECTIVES: Study objective was to investigate sildenafil bioavailability of the novel ODF formulation after sublingual and supralingual administration. METHODS: In this randomised, two-way cross-over study, 12 healthy male volunteers received a single 50 mg sildenafil dose by the sublingual and supralingual administration routes. Plasma sildenafil was determined up to 12 h post-dose. Peak concentration (Cmax) and area under concentration-time curve (AUC0-t) were calculated and compared between the two administration routes by analysis of variance (ANOVA). RESULTS: Sublingual and supralingual administration can be claimed equivalent regarding the extent of sildenafil exposure since AUC0-t 90 % CIs corresponded to 94.90-110.58% and were within the pre-specified acceptance range. Cmax 90% CIs (79.92-125.57%) were only slightly outside the 80.00-125.00% limits, due to the small sample size, while the time to achieve Cmax did not differ between treatments (p = 0.9277). Rate of exposure of the two administration routes was therefore similar. Reported treatment-related adverse events were mild to moderate headache (33.3% of subjects) and vomiting (8.3%). CONCLUSIONS: In healthy men, sublingual and supralingual administration of sildenafil ODF resulted in a remarkably similar pharmacokinetic profile and confirmed the safety of both study treatments. The recently marketed sildenafil ODF, administered by both investigated routes, can provide a valuable alternative to the marketed solid oral forms (tablets) in ED treatment.