Pharmacokinetics and pharmacodynamics of a single bolus of propofol 2% in healthy volunteers.
This study was undertaken to assess the bioequivalence between a new formulation of propofol 2% and the commercially available product Diprivan. Secondary objectives were to compare the times to onset of and emergence from hypnosis, the hemodynamic effects, and the safety profiles. Twelve healthy male volunteers were included in a randomized crossover study. Subjects were administered a 2-mg/kg single bolus injection of each formulation separated by a 7- to 10-day washout period. Plasma propofol was determined by reversed-phase liquid chromatography with fluorescence detection. Eleven subjects completed the study, and both formulations were considered bioequivalent. There were no serious or severe adverse events. The concentration-time profiles of all the subjects could adequately be described using a three-compartment model. The mean times to cessation of counting out loud (17 vs. 18 s) and to eye opening (245 vs. 244 s) were not statistically different between treatment groups. Moreover, they seem to show some degree of pharmacodynamic bioequivalence, although a higher number of subjects are necessary to unequivocally demonstrate it.
Service of Clinical Pharmacology, Hospital Universitario de la Princesa, Instituto Teófilo Hernando, Universidad Autónoma de Madrid, Madrid, Spain.
Francisco
F
Abad-Santos
M Angeles
MA
Gálvez-Múgica
M Angeles
MA
Santos
Jesús
J
Novalbos
Sonia
S
Gallego-Sandín
Paloma
P
Méndez
Cesar
C
Casimiro
Fernando
F
Gilsanz
D000328:Adult; D018686:Anesthetics, Intravenous / Q000009:adverse effects / Q000493:pharmacokinetics* / Q000494:pharmacology*; D019540:Area Under Curve; D001682:Biological Availability; D018592:Cross-Over Studies; D006801:Humans; D008297:Male; D015742:Propofol / Q000009:adverse effects / Q000493:pharmacokinetics* / Q000494:pharmacology*; D013810:Therapeutic Equivalency; D013997:Time Factors
D018686:Anesthetics, Intravenous; D015742:Propofol