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 (C_max) and area under concentration-time curve (AUC_0-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 AUC_0-t 90 % CIs corresponded to 94.90-110.58% and were within the pre-specified acceptance range. C_max 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 C_max 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.

Conflict of interest

V.F. is an employee of IBSA Institut Biochimique SA, L.L., C.L. and M.R. are employees of CROSS Research S.A., which was contracted by IBSA Institut Biochimique SA as CRO for the conduction of this study and received financial support for its services. The authors declare that they have no other relationships or activities that could appear to have influenced the submitted work.

Ethical approval

The study protocol (code 17CH-SDF06) was approved by the Ethics Committee of Canton Ticino, Switzerland, and the Swiss Federal Health Authorities.

Informed consent

All subjects provided written informed consent before enrolment.