Single-dose pharmacokinetics of fentanyl buccal soluble film

Abstract

Objective. The objectives of the study were to determine the absolute bioavailability of fentanyl from fentanyl buccal soluble film, estimate the percentage of a fentanyl dose absorbed through the buccal mucosa, and compare the bioavailability of equivalent doses administered either as single or multiple dose units. Design. Open-label, randomized, four-period, Latin-square crossover pharmacokinetic study. Setting. Inpatient phase 1 unit. Patients. Twelve healthy volunteers. Interventions. Injectable fentanyl citrate (200 μg) administered by intravenous infusion, injectable fentanyl citrate (800 μg/16 mL) administered orally, and fentanyl buccal soluble film (800 μg) administered as a single film and as four separate 200 μg films simultaneously. Outcome Measures. Plasma concentrations after fentanyl dosing; pharmacokinetic parameters. Results. The two buccal film treatments were bioequivalent and both had an absolute bioavailability of 71%. The percentage of an administered dose absorbed through the buccal mucosa was calculated to be 51%. Conclusions. Fentanyl buccal soluble film effectively delivers a high percentage of the administered fentanyl dose and nearly identical plasma profiles are obtained when equivalent doses are delivered by single or multiple dosage units. © 2010 American Academy of Pain Medicine.