A single dose, randomized, open-label, cross-over bioequivalence study of sildenafil citrate tablets in healthy Chinese volunteers .

OBJECTIVE

The present study was designed to evaluate the bioequivalence of a newly developed sildenafil citrate tablet 50 mg (Jinge, Test) and a marketed counterpart (Viagra, 100 mg, Reference) in healthy adult male Chinese volunteers.

METHODS

This single-dose, randomized, open-label, four-period, and two-treatment self-crossover study included two parts: fasting and postprandial studies. In each part of the study, the subjects were randomly assigned to receive test or reference products (100 mg sildenafil) in a 1 : 1 ratio, and then received the alternative products, following a 1-week washout period. Plasma sildenafil concentrations were analyzed by liquid chromatography-tandem mass spectrometry. Tolerability was assessed during the entire study period.

RESULTS

32 healthy volunteers (aged 19 - 30) were enrolled in the study; 31 volunteers completed the fasting study, while 32 volunteers completed the postprandial study. The test formulation was bioequivalent to the marketed formulation as the 90% CIs for the ratio of geometric means of C (fasting: 98.79 - 119.61%; fed: 94.47 - 119.65%), AUC (fasting: 98.70 - 109.71%; fed: 96.39 - 112.89%), and AUC (fasting: 98.45 - 108.87%; fed: 96.36 - 112.74%) were within equivalence limits (80 - 125%) under both fasting and postprandial conditions. When sildenafil was given with high-fat meals, mean C was reduced by 23%, and median tmax ranged from 0.75 to 1.50 hours (p ≤ 0.05). However, both AUC and AUC were comparable between fasting and postprandial conditions. No serious adverse events were found among the subjects.

CONCLUSIONS: This study confirmed that test and reference sildenafil citrate tablets were bioequivalent under fasting and postprandial conditions.
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