A phase I pharmacokinetic and bioavailability study of a sublingual fentanyl wafer in healthy volunteers

Anesthesia and Analgesia
Chin Beng Stephen LimYandi Liu

Abstract

The sublingual administration of opioids is a simple and noninvasive method that provides rapid analgesia. In this phase I study we investigated the pharmacokinetics and bioavailability of a fentanyl wafer in healthy volunteers. The principal study objective was to investigate the pharmacokinetic profile of a new sublingual fentanyl wafer and to establish its absolute bioavailability. Twenty-four healthy volunteers, mean age 23 years, were randomly assigned to receive the equivalent of fentanyl 100 μg by both the sublingual and IV routes. Blood samples were collected in sterile polypropylene tubes for 24 hours after each fentanyl administration. The pharmacokinetic parameters were determined by model-independent pharmacokinetic analyses of the plasma fentanyl concentration-time profiles. The mean absolute bioavailability of the sublingual fentanyl wafer was 78.9% (90% confidence interval [CI] 51.1% to 121.7%). The first detectable plasma fentanyl concentration time ranged from 2 to 10 minutes in all volunteers, and the mean (±SD) time to peak plasma concentration at 0.91 (±0.73) hours after administration. Sublingual administration of fentanyl as a wafer product resulted in rapidly detectable plasma fentanyl concentrations. The...Continue Reading

References

Aug 5, 1998·British Journal of Clinical Pharmacology·L E MatherL G Eltherington
Oct 21, 1998·Journal of Clinical Oncology : Official Journal of the American Society of Clinical Oncology·J M ChristieR K Portenoy
Aug 16, 2001·Journal of Pain and Symptom Management·J Gardner-Nix
Feb 15, 2002·Journal of Pain and Symptom Management·Patrick J CoyneThomas J Smith
Jul 20, 2002·Clinical Pharmacokinetics·Hao ZhangJames B Streisand
Nov 1, 2003·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Susanne BredenbergChrister Nyström
Aug 9, 2005·Pain Medicine : the Official Journal of the American Academy of Pain Medicine·Gerald M AronoffBrian Ginsberg
Dec 22, 2006·Drugs·Stephanie K A Blick, Antona J Wagstaff
Feb 27, 2007·Journal of Clinical Pharmacology·Mona DarwishJohn G Jiang
Feb 9, 2008·Journal of Pain and Symptom Management·Giovambattista Zeppetella
Jun 1, 1993·Der Schmerz·H W StriebelA Rieger
Mar 20, 2010·Journal of Opioid Management·Stein KaasaHans Georg Kress
May 25, 2010·Pain Medicine : the Official Journal of the American Academy of Pain Medicine·Niraj VasishtAndrew L Finn

❮ Previous
Next ❯

Citations

Apr 19, 2013·Drug Design, Development and Therapy·Stephen C B LimYandi Liu

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.