In addition to not requiring water for administration, orodispersible films share the advantages of tablet formulations (accurate dosage and ease of administration) with those of liquid dosing forms (ease of swallowing and rapid bioavailability due to bypassing the hepatic first-pass effect when the absorption of active substance occurs mainly through the oral mucosae).Although orodispersible formulations have particular relevance by improving compliance in special patient populations, such as children, geriatric patients, and dysphasic patients who have difficulty in swallowing tablets or capsules, their convenience, superior dosing accuracy, and rapid onset of action contribute to strong patient preference over conventional solid dosage forms across a wide range of patient groups.Keywords: sildenafil, pharmacokinetics, bioequivalence, orodispersible film, PDE5 inhibitor, N-desmethyl-sildenafil Introduction The first-in-class selective inhibitor of cyclic guanosine monophosphate-specific phosphodiesterase type 5 (PDE5), sildenafil, has become well established as a safe and effective treatment for male erectile dysfunction since the approval of Viagra (Pfizer Ltd, Tadworth, UK) by the US Food and Drug Administration (FDA) in 1998.
Accepted for publication 14 December 2016 Published 11 April 2017 Volume 20 Pages 1183—1192 DOI https://doi.org/10.2147/DDDT.
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.
More than 25 years of clinical experience has confirmed the risk/benefit profile of sildenafil and established it as an effective treatment option for erectile dysfunction.
Sildenafil could also be taken by men with comorbidities, such as hypertension, stable coronary artery disease, congestive heart failure, diabetes mellitus, traumatic spinal cord injury, obstructive sleep apnea, multiple sclerosis, renal dysfunction, prostate cancer, Parkinson’s disease, depression, and traumatic stress disorders.
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 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.