The absolute bioavailability of racemic ketamine from a novel sublingual formulation
MetadataShow full item record
AIM: The principal study objective was to investigate the pharmacokinetic characteristics of a new sublingual ketamine wafer and to establish its absolute bioavailability and local tolerability. METHODS: The study was of open label, two way randomized crossover design in eight healthy male volunteers. Each participant received either a single 10 mg intravenous dose as a constant rate 30 min infusion or a 25 mg sublingual dose of ketamine wafer in two treatment periods with a 7 day wash out. Pharmacokinetic blood sampling and local tolerability and safety assessments were carried out during 24 h following both dosing occasions. Plasma concentrations were analyzed by non-compartmental methods and local tolerability was assessed using modified Likert scales. RESULTS: The median (90% CI lower, upper limit) absolute bioavailability of sublingual ketamine was 29% (27, 31%). The first quantifiable plasma ketamine concentration was observed within 5 min for all eight participants for both routes of administration and the median (min–max) time of the peak plasma concentration was 0.75 h (0.25–1.0 h) after sublingual administration. The ketamine wafer had very good local tolerability. CONCLUSION: Sublingual administration of the ketamine wafer resulted in rapid absorption. The ketamine wafer has comparable bioavailability with other oral transmucosal formulations of ketamine but with markedly reduced inter-subject variability, warranting further evaluation as analgesic adjunct.
Showing items related by title, author, creator and subject.
A Phase I Pharmacokinetic and Bioavailability Study of a Sublingual Fentanyl Wafer in Healthy VolunteersLim, Stephen; Schug, Stephan; Sunderland, Bruce; Paech, Michael; Liu, Yandi (2012)Background: 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 ...
Low-Dose Sublingual Ketamine Does Not Modulate Experimentally Induced Mechanical Hyperalgesia in Healthy SubjectsSlater, Helen; Graven-Neilsen, T.; Wright, Anthony; Schug, S. (2012)Objective: Musculoskeletal pain has been associated with N-methyl-d-aspartate (NMDA) receptor-mediated mechanisms. This randomized controlled trial (RCT) investigated the effect of the NMDA receptor antagonist ketamine ...
Robson, T.; Stevens, Jason; Dixon, Kingsley; Reid, N. (2017)Recent studies suggest sulfur-accumulators (thiophores and gypsophiles) produce foliar gypsum (CaSO4 2H2O) as a novel biomineralogical tolerance mechanism against sulfate salinity and excess soluble calcium (e.g. gypsic ...