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.
| Original language | English |
|---|---|
| Pages (from-to) | 924-934 |
| Number of pages | 11 |
| Journal | Anesthesiology |
| Volume | 106 |
| Issue number | 5 |
| DOIs | |
| Publication status | Published - 2007 May 1 |
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ASJC Scopus subject areas
- Anesthesiology and Pain Medicine
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Pharmacokinetics and pharmacodynamics of propofol microemulsion and lipid emulsion after an intravenous bolus and variable rate infusion. / Kim, Kye Min; Choi, Byung Moon; Park, Si Won; Lee, Soo Han; Christensen, Lane V.; Zhou, Jiaye; Yoo, Byung Hoon; Shin, Hye Won; Bae, Kyun Seop; Kern, Steven E.; Kang, Sung Hong; Noh, Gyu Jeong.
In: Anesthesiology, Vol. 106, No. 5, 01.05.2007, p. 924-934.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Pharmacokinetics and pharmacodynamics of propofol microemulsion and lipid emulsion after an intravenous bolus and variable rate infusion
AU - Kim, Kye Min
AU - Choi, Byung Moon
AU - Park, Si Won
AU - Lee, Soo Han
AU - Christensen, Lane V.
AU - Zhou, Jiaye
AU - Yoo, Byung Hoon
AU - Shin, Hye Won
AU - Bae, Kyun Seop
AU - Kern, Steven E.
AU - Kang, Sung Hong
AU - Noh, Gyu Jeong
PY - 2007/5/1
Y1 - 2007/5/1
N2 - 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.
AB - 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.
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U2 - 10.1097/01.anes.0000265151.78943.af
DO - 10.1097/01.anes.0000265151.78943.af
M3 - Article
VL - 106
SP - 924
EP - 934
JO - Anesthesiology
JF - Anesthesiology
SN - 0003-3022
IS - 5
ER -