Comparison of pharmacokinetic characteristics of sildenafil citrate chewable tablets and film-coated tablets in healthy male subjects.

Abstract

UI14SDF100CW is a chewable tablet of sildenafil citrate, which was developed to improve compliance through convenience of administration. The purpose of this study was to compare the pharmacokinetic (PK) properties of sildenafil citrate chewable tablets (UI14SDF100CW) and conventional sildenafil citrate film-coated tablets (Viagra®, Pfizer). A randomized, open-label, single dose, two-treatment, two-period, two-way crossover study was conducted in 60 healthy male volunteers. In each period, the subjects received a single oral dose of UI14SDF100CW or Viagra® (both tablets contain 140.45 mg of sildenafil citrate, which is equivalent to 100 mg of sildenafil). Serial blood samples were collected up to 24 h post-dose for PK analysis. The plasma concentration of sildenafil was determined using a validated HPLC-MS/MS assay. PK parameters of sildenafil were calculated using non-compartmental methods. The plasma concentration-time profiles of sildenafil in both formulations were similar. For UI14SDF100CW, the Cmax and AUClast of sildenafil were 1068.69 ± 458.25 (mean ± standard deviation) mg/L and 3580.59 ± 1680.29 h·mg/L, and the corresponding values for Viagra® were 1146.84 ± 501.70 mg/L and 3406.35 ± 1452.31 h·/L, respectively. The geometric mean ratios (90% confidence intervals) of UI14SDF100CW to Viagra® 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. In conclusion, UI14SDF100CW and Viagra® showed similar PK properties. Therefore, UI14SDF100CW can be an alternative to sildenafil for the treatment of erectile dysfunction, providing better compliance.