Pharmacokinetics and Bioequivalence Evaluation of Two Different Aildenafil Citrate Tablet Formulations in Healthy Chinese Male Subjects Under Fasting and Fed Conditions.

Abstract

Aildenafil citrate is a novel and potent phosphodiesterase type 5 inhibitor for the treatment of erectile dysfunction (ED). This study evaluates the pharmacokinetics and bioequivalence of 2 formulations of aildenafil citrate tablets (30 and 60 mg) in healthy Chinese male subjects under both fasting and fed conditions. A single-center, randomized, open-label, 2-period crossover design was employed, with 78 participants enrolled, including 30 in the fasting condition and 48 in the fed condition. Blood samples were collected at multiple time points for pharmacokinetic analysis, which included C_max, AUC_0-t, and AUC_0-∞ as the primary parameters. The results demonstrated that the pharmacokinetic profiles of the test and reference formulations were comparable in both the fasting and fed states, with 90% confidence intervals for the geometric mean ratios of C_max, AUC_0-t, and AUC_0-∞ falling within the 80%-125% range, confirming bioequivalence. Although food intake slightly delayed the time to peak concentration and reduced the absorption rate, it did not significantly affect the overall bioavailability. Both formulations were well tolerated, with adverse events being mild and resolving spontaneously. This study provides evidence supporting the bioequivalence of the 2 aildenafil citrate formulations and their interchangeability for clinical use in treating ED.