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.


METHODS
Open-label, randomized, four-period, Latin-square crossover pharmacokinetic study.


METHODS
Inpatient phase 1 unit.


METHODS
Twelve healthy volunteers. Interventions. Injectable fentanyl citrate (200 microg) administered by intravenous infusion, injectable fentanyl citrate (800 microg/16 mL) administered orally, and fentanyl buccal soluble film (800 microg) administered as a single film and as four separate 200 microg films simultaneously.


METHODS
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.
Vasisht
Niraj
N
BioDelivery Sciences International, Inc., Raleigh, North Carolina 27607, USA.
Gever
Larry N
LN
Tagarro
Ignacio
I
Finn
Andrew L
AL
D000278:Administration, Buccal; D000328:Adult; D000701:Analgesics, Opioid / Q000008:administration & dosage* / Q000493:pharmacokinetics* / Q000627:therapeutic use; D019540:Area Under Curve; D001682:Biological Availability; D018592:Cross-Over Studies; D004305:Dose-Response Relationship, Drug; D005260:Female; D005283:Fentanyl / Q000008:administration & dosage* / Q000493:pharmacokinetics* / Q000627:therapeutic use; D006801:Humans; D008297:Male; D009061:Mouth Mucosa / Q000378:metabolism; D010146:Pain / Q000188:drug therapy*; D013997:Time Factors; D016896:Treatment Outcome; D055815:Young Adult
D000701:Analgesics, Opioid; D005283:Fentanyl