Single-dose pharmacokinetics of fentanyl buccal soluble film

Pain Med. 2010 Jul;11(7):1017-23. doi: 10.1111/j.1526-4637.2010.00875.x. Epub 2010 May 18.

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 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.

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.

Publication types

  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Buccal
  • Adult
  • Analgesics, Opioid / administration & dosage*
  • Analgesics, Opioid / pharmacokinetics*
  • Analgesics, Opioid / therapeutic use
  • Area Under Curve
  • Biological Availability
  • Cross-Over Studies
  • Dose-Response Relationship, Drug
  • Female
  • Fentanyl / administration & dosage*
  • Fentanyl / pharmacokinetics*
  • Fentanyl / therapeutic use
  • Humans
  • Male
  • Mouth Mucosa / metabolism
  • Pain / drug therapy*
  • Time Factors
  • Treatment Outcome
  • Young Adult

Substances

  • Analgesics, Opioid
  • Fentanyl