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Absolute and Relative Bioavailability of Fentanyl Buccal Tablet and Oral Transmucosal Fentanyl Citrate
Author(s) -
Darwish Mona,
Kirby Mary,
Robertson Philmore,
Tracewell William,
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 - 10.1177/0091270006297749
Subject(s) - medicine , fentanyl , buccal administration , crossover study , bioavailability , pharmacokinetics , breakthrough pain , anesthesia , pharmacology , oral administration , opioid , alternative medicine , receptor , pathology , placebo
This study assessed the absolute and relative bioavailabilities and transmucosal and gastrointestinal absorbency of fentanyl buccal tablet (FBT) and oral transmucosal fentanyl citrate (OTFC). In a randomized crossover design, 26 healthy subjects received FBT 400 μg (transmucosal), FBT 800 μg (oral), OTFC 800 μg (transmucosal), and fentanyl 400 μg (intravenous). The transmucosal FBT had the highest absolute bioavailability (0.65) compared with the oral FBT (0.31) or transmucosal OTFC (0.47). More fentanyl was absorbed transmucosally from FBT than OTFC (48% vs 22%). Median t max values were shorter following the transmucosal FBT (47 minutes) than the oral FBT (90 minutes) or the transmucosal OTFC (91 minutes). Transmucosal administration of FBT compared with dose‐normalized OTFC resulted in higher total systemic fentanyl exposure, higher early systemic exposure, and higher C max . The rate and extent of fentanyl absorption were greater following administration of FBT compared to OTFC. An approximately 30% smaller dose of FBT achieved systemic exposures comparable to OTFC.