Pharmacokinetics of a New Orodispersible Tablet Formulation of Vardenafil: Results of Three Clinical Trials

Background: Vardenafil is a potent and highly selective oral phosphodiesterase type 5 (PDE-5) inhibitor that has been shown in numerous clinical trials and post-marketing surveillance studies to be safe and effective for improving erectile function in men with erectile dysfunction (ED). Until recently, the drug was only available as a film-coated tablet (FCT). A new orodispersible tablet (ODT) formulation of vardenafil has been developed that disintegrates in the subject’s mouth without the need for water or other liquids. Objective: To characterize the pharmacokinetics of a new 10 mg ODT formulation of vardenafil. Methods: Three clinical trials were conducted: (i) a randomized 4-fold crossover study to assess the effect of food and water on the pharmacokinetics of vardenafil ODT, compared with vardenafil FCT, in healthy men; (ii) a phase I study to assess single and multiple doses of vardenafil ODT, compared with a single dose of vardenafil FCT, in young and elderly men with ED; and (iii) a pharmacokinetic substudy of a phase III trial in men of broad age range with ED. Results: Vardenafil ODT was rapidly absorbed after oral administration without water, with a similar pharmacokinetic profile to vardenafil FCT, except that the ODT exhibited significantly greater bioavailability. After a single dose, the geometric mean area under the plasma concentration-time curve from time zero to infinity (AUC ∞ ) of vardenafil ODT increased by 21–44% compared with the FCT. There was no consistent difference in geometric mean maximum vardenafil plasma concentration (C max ) between the two formulations. Geometric mean AUC∞ and C max were increased by 41% and 24%, respectively, in men with ED aged ≥65 years compared with those aged