The Pharmacokinetic Characteristics of Sildenail Citrate Chewable Tablets Compared to Film-Coated Tablets in Healthy Male Subjects

Abstract

UI14SDF100CW is a chewable tablet of sildenafil citrate, which was developed to improve compliance through convenient administration. The purpose of this study was to evaluate the pharmacokinetic properties of sildenafil citrate chewable tablets compared with conventional sildenafil citrate film-coated tablets. A randomized, open-label, single dose, two-treatment, two-period, two-way crossover study was conducted in 60 healthy male volunteers. In each period, subjects received a single oral dose of UI14SDF100CW or sildenafil citrate film-coated tablet (both tablets contain 140.45mg of sildenafil citrate which is 100 mg as sildenafil). Serial blood samples were collected up to 24 hours post-dose for pharmacokinetic (PK) analysis. Plasma concentration of sildenafil was determined using a validated LC-MS/MS assay. PK parameters of sildenafil was calculated using non-compartmental methods. This study was approved by Institutional Review Board of Chungnam National University Hospital. (No. CNUH 2012-01-021) The plasma sildenafil concentration – time profiles of two formulation is similar.. For UI14SDF100CW, the Cmax and the AUClast of sildenafil were 1068.69 ± 458.25 (mean ± standard deviation) mg/L and 3580.59 ± 1680.29 h*mg/L, and their corresponding values for sildenafil citrate film-coated tablet were 1146.84 ± 501.70 mg/L and 3406.35 ± 1452.31 h*mg/L, respectively. The geometric mean ratios (90% confidence intervals) of UI14SDF100CW to sildenafil citrate film-coated tablet for Cmax and AUClast were 0.933 (0.853 – 1.021) and 1.034 (0.969 – 1.108), respectively, which met the bioequivalence criteria of Korean regulatory agency. UI14SDF100CW has similar pharmacokinetic properties compared to a conventional sildenafil citrate film-coated tablet. Therefore, UI14SDF100CW can be an alternative treatment option for sildenafil citrate film-coated tablet, providing better compliance.