Bioequivalence study of a new sildenafil 100 mg orodispersible film compared to the conventional film-coated 100 mg tablet administered to healthy male volunteers

Abstract

A new orodispersible film formulation of the phosphodiesterase type 5 inhibitor, sildenafil, has been developed to examine the advantages of an orally disintegrating film formulation and provide an alternative to the current marketed products for the treatment of erectile dysfunction. The pharmacokinetics of the sildenafil 100 mg orodispersible film (IBSA) was compared to that of the conventional marketed 100 mg film-coated tablet (Viagra®) after single-dose administration to 53 healthy male volunteers (aged 18–51 years) in a randomized, open, two-way crossover bioequivalence study. Each subject received a single oral dose of 100 mg of sildenafil as test or reference formulation administered under fasting conditions at each of the two study periods according to a randomized crossover design. There was a washout interval of ≥7 days between the two administrations of the investigational medicinal products. Blood samples for pharmacokinetic analysis were collected up to 24 h post-dosing. The primary objective was to compare the rate (peak plasma concentration; Cmax) and extent (area under the curve [AUC] from administration to last observed concentration time; AUC0–t) of sildenafil absorption after single-dose administration of test and reference. Secondary endpoints were observed to describe the plasma pharmacokinetic profiles of sildenafil and its metabolite N-desmethyl-sildenafil relative bioavailability and safety profile after single-dose administration. The mean sildenafil and N-desmethyl-sildenafil plasma concentration–time profiles up to 24 h after single-dose administration of sildenafil 100 mg orodispersible film and film-coated tablet were nearly superimposable. The bioequivalence test was fully satisfied for sildenafil and N-desmethyl-sildenafil in terms of rate and extent of bioavailability. Adverse events occurred at similar rates for the two formulations and were of mild-to-moderate severity. The results suggest that the new orodispersible film formulation can be used interchangeably with the conventional film-coated formulation.

Comparative single-dose pharmacokinetics of sildenafil after oral and rectal administration in healthy beagle dogs

“…We performed rectal administration of sildenafil ODF formulation, which is rapidly absorbed in the mucous membranes [ 12 ]. Some studies have reported rectal administration of medication as an alternative route for dogs that are not able to receive medication orally because of seizure [ 13 , 14 ].…”

Orodispersible dosage forms: biopharmaceutical improvements and regulatory requirements

“…Orodispersible tablets 83 ODT present similar in appearance to conventional tablets, the rapid penetration of water through capillary 84 action into the porous framework leads to disintegration in the 30 s -3 min range [5,6]. The main 85 production strategies include lyophilisation, moulding or direct compression using peculiar excipients.…”

Physiologically Based Pharmacokinetic Modeling to Understand the Absorption of Risperidone Orodispersible Film

“…It was found that the sildenafil ODF was bioequivalent to that of the conventional tablet (Viagra ® ). The plasma concentration-time profiles of sildenafil and the metabolite were nearly superimposable between the two dosage forms (Radicioni et al, 2017). However, after sublingual or buccal administration of the ropinirole ODF, a fast absorption was achieved within 15 min.…”