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. Issue 1 (30th October 2014)

• Record Type: Journal Article
• Authors: Gao, Xiang; Ndongo, Marie‐Noella; Checchio, Tina M.; Cook, Jack; Duncan, Barbara; LaBadie, Robert R.
• Is Part Of: Clinical pharmacology in drug development. Volume 4:Issue 1(2015:Jan./Feb.)
• Page Start: 74
• Page End: 80
• Publication Date: 2014-10-30
• Subjects: Drugs -- Testing -- Periodicals; Drug development -- Periodicals; Clinical pharmacology -- Periodicals; 615.580724
• DOI: 10.1002/cpdd.146
• Languages: English
• ISSNs: 2160-7648

Abstract

<abstract abstract-type="main" xml:lang="en"> <title>Abstract</title> <sec id="cpdd146-sec-0001" sec-type="section"> <p>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.</p> </sec> </abstract>