title: Pharmacokinetics and pharmacodynamics of propofol microemulsion and lipid emulsion after an intravenous bolus and variable rate infusion.
abstract: BACKGROUND
  The aim of this trial was to evaluate the induction and recovery characteristics of microemulsion propofol (Aquafol; Daewon Pharmaceutical Co., Ltd., Seoul, Korea). Pharmacokinetics, pharmacodynamics, and safety profile were investigated. Lipid emulsion propofol (Diprivan; AstraZeneca, London, United Kingdom) was used as a comparator.
  
  
  METHODS
  Thirty-one healthy volunteers aged 20-79 yr were given an intravenous bolus of propofol 2 mg/kg, followed by variable rate infusion for 60 min. Each volunteer was studied twice with different formulations at an interval of 1 week. Arterial concentrations of propofol were measured, and Bispectral Index was used as a surrogate measure of propofol effect. The induction and recovery characteristics including bioequivalence were evaluated by noncompartmental analysis. The pharmacokinetics and pharmacodynamics were investigated using a population approach with mixed effects modeling. The rate, severity, and causal relation of adverse events were analyzed.
  
  
  RESULTS
  Both formulations were bioequivalent. The observed time to peak effect after a bolus of both formulations was 1.5 min. Plasma concentration of propofol at loss of consciousness, time to loss of consciousness after a bolus, and time to recovery of consciousness after discontinuation of infusion did not show significant differences. The population pharmacokinetics and pharmacodynamics revealed a variety of differences between two formulations. Aquafol showed similar safety profile to Diprivan.
  
  
  CONCLUSIONS
  The efficacy and safety of Aquafol were not different from those of Diprivan within the dose range in this study.
authors: Department of Anesthesiology and Pain Medicine, Sanggye Paik Hospital, Inje University College of Medicine, Seoul, Korea.
authors: Kye-Min
authors: KM
authors: Kim
authors: Byung-Moon
authors: BM
authors: Choi
authors: Si-Won
authors: SW
authors: Park
authors: Soo-Han
authors: SH
authors: Lee
authors: Lane V
authors: LV
authors: Christensen
authors: Jiaye
authors: J
authors: Zhou
authors: Byung-Hoon
authors: BH
authors: Yoo
authors: Hye-Won
authors: HW
authors: Shin
authors: Kyun-Seop
authors: KS
authors: Bae
authors: Steven E
authors: SE
authors: Kern
authors: Sung-Hong
authors: SH
authors: Kang
authors: Gyu-Jeong
authors: GJ
authors: Noh
mesh_terms: D000328:Adult; D000368:Aged; D018686:Anesthetics, Intravenous / Q000008:administration & dosage*; D018592:Cross-Over Studies; D004655:Emulsions; D005217:Fat Emulsions, Intravenous; D005260:Female; D006801:Humans; D007262:Infusions, Intravenous; D007275:Injections, Intravenous; D008297:Male; D008875:Middle Aged; D015742:Propofol / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology; D012449:Safety
chemical_list: D018686:Anesthetics, Intravenous; D004655:Emulsions; D005217:Fat Emulsions, Intravenous; D015742:Propofol