Population Pharmacokinetics/Pharmacodynamics (PK/PD) of Microemulsion Propofol in Healthy Volunteers
Status:
Completed
Trial end date:
2011-06-01
Target enrollment:
Participant gender:
Summary
AquafolTM (Daewon Pharmaceutical Co., Ltd., Seoul, Korea) is a microemulsion propofol that
has been developed for eliminating lipid solvent-related adverse events of long chain
triglyceride emulsion (LCT) propofol (Diprivan®; AstraZeneca, London, United Kingdom), such
as infection, fat embolism, hypertriglyceridemia and pancreatitis. Originally, AquafolTM was
formulated with 8% polyethylene glycol 660 hydroxystearate (Solutol HS 15, BASF Company Ltd.,
Seoul, Korea) and 5% tetrahydrofurfuryl alcohol polyethylene glycol ether (Glycofurol, Roche,
Basle, Switzerland). A phase 1 study to assess the safety and tolerability of polymeric
vehicles of this formulation in healthy volunteers showed dose-limiting toxicity.
Subsequently, it was reformulated with 10% purified poloxamer 188 (PP188) as a nonionic block
copolymer surfactant and 0.7% polyethylene glycol 660 hydroxystearate as a nonionic
surfactant. Alterations in propofol formulation may result in altered pharmacokinetic,
pharmacodynamic characteristics.
The aim of this study was to compare the pharmacokinetics and pharmacodynamics of propofol
microemulsion and lipid emulsion, using noncompartmental analysis and population analysis
with mixed effects modeling.