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Single‐Dose and Steady‐State Pharmacokinetics of Fentanyl Buccal Tablet in Healthy Volunteers
Author(s) -
Darwish Mona,
Kirby Mary,
Robertson Philmore,
Hellriegel Edward,
Jiang John G.
Publication year - 2007
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1177/0091270006294129
Subject(s) - fentanyl , pharmacokinetics , buccal administration , medicine , anesthesia , naltrexone , pharmacology , opioid , receptor
This study evaluated the single‐dose and steady‐state pharmacokinetics of fentanyl buccal tablet 400 μg in healthy adult volunteers. After receiving naltrexone 50 mg to block opioid receptor–mediated effects of fentanyl, subjects received fentanyl buccal tablet 400 μg on day 1, then every 6 hours from day 4 to day 9 (21 doses). Naltrexone 50 mg was administered every 12 hours throughout the study. Plasma fentanyl concentrations were determined for 72 hours after administration of fentanyl buccal tablet 400 μg on day 1 and the last dose of fentanyl buccal tablet 400 μg on day 9. Following single‐ and multiple‐dose administration of fentanyl buccal tablet, the median time to maximum concentration (t max ) was 52.2 and 49.8 minutes, respectively. Peak plasma concentration of fentanyl (C max ) was 0.88 ng/mL for the single‐dose regimen and 1.77 ng/mL for the multiple‐dose regimen. Steady state was reached within 5 days, consistent with the observed median half‐life of approximately 22 hours following multiple doses. Observed accumulation of fentanyl after multiple doses of fentanyl buccal tablet was slightly greater than would be expected based on the single‐dose data. This was attributed to the redistribution of fentanyl from a deep tissue compartment into the plasma. This study indicates that fentanyl buccal tablet has predictable pharmacokinetics following multiple‐dose administration.