Pharmacokinetics and dose proportionality of fentanyl sublingual spray: a single-dose 5-way crossover study.

Background: Fentanyl sublingual spray is a novel formulation of fentanyl for sublingual delivery that was designed to enhance the rate and extent of absorption of fentanyl for management of breakthrough cancer pain (BTCP).

Objectives: The primary objective of this study was to determine the pharmacokinetics and dose proportionality of 5 different doses (100, 200, 400, 600, and 800 μg) of fentanyl sublingual spray in healthy subjects under fasted conditions (part A); the secondary objective was to assess the effects of temperature and pH in the oral cavity on relative bioavailability of fentanyl (part B).

Methods: Analyses were performed on venous blood samples drawn 5 min to 36 h after administration of fentanyl sublingual spray (Subsys(®), Insys Therapeutics, Inc.

Single-dose pharmacokinetics of fentanyl sublingual spray and oral transmucosal fentanyl citrate in healthy volunteers: a randomized crossover study.

Background: Fentanyl sublingual spray (FSS) is a novel fentanyl formulation recently developed for the treatment of breakthrough cancer pain, which is characterized by a fast onset and a relatively short duration.

Objective: To compare rate of absorption and systemic bioavailability between FSS and oral transmucosal fentanyl citrate (OTFC) in healthy volunteers.

Methods: This randomized 3-way crossover study involved 29 healthy volunteers (25 men and 4 women; mean age, 35 years) who received single doses of FSS (400 μg), OTFC (400 μg), and intravenous fentanyl citrate (100 μg) separated by washout periods of ≥7 days.