Premium
A randomized, open‐label 3‐way crossover study to investigate the relative bioavailability and bioequivalence of crushed sildenafil 20 mg tablets mixed with apple sauce, extemporaneously prepared suspension (EP), and intact sildenafil 20 mg tablets in healthy volunteers under fasting conditions
Author(s) -
Gao Xiang,
Ndongo MarieNoella,
Checchio Tina M.,
Cook Jack,
Duncan Barbara,
LaBadie Robert R.
Publication year - 2014
Publication title -
clinical pharmacology in drug development
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.711
H-Index - 22
eISSN - 2160-7648
pISSN - 2160-763X
DOI - 10.1002/cpdd.146
Subject(s) - bioequivalence , bioavailability , sildenafil , medicine , crossover study , pharmacokinetics , pharmacology , dosage form , chromatography , chemistry , alternative medicine , pathology , placebo
The relative bioavailability and bioequivalence of 20‐mg doses of a pediatric formulation of sildenafil extemporaneous preparation suspension (EP; 10 mg/mL), the sildenafil 20‐mg intact tablet and the crushed sildenafil 20‐mg tablet mixed with apple sauce were assessed in a single‐dose, randomized, open‐label, 3‐way crossover study with 18 healthy adult volunteers. Blood samples were collected at predefined times and analyzed for sildenafil plasma concentrations. Natural log‐transformed sildenafil pharmacokinetic parameters (C max , AUC last , and AUC inf ) were used to estimate relative bioavailability and construct 90% confidence intervals (CI) using a mixed‐effects model. Bioequivalence was concluded among the three formulations with one exception, in which the EP suspension showed a 15% decrease in C max with a lower 90% CI of 76% compared with the intact tablet. The 15% decrease in sildenafil C max is not considered to be clinically relevant. Therefore, the EP suspension is considered to be an appropriate pediatric formulation. All 3 formulations were well tolerated in healthy adult volunteers.