Single-Dose Pharmacokinetics of Fentanyl Buccal Soluble Film

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.