Pharmacokinetics and pharmacodynamics of propofol microemulsion and lipid emulsion after an intravenous bolus and variable rate infusion

Kye Min Kim, Byung Moon Choi, Si Won Park, Soo Han Lee, Lane V. Christensen, Jiaye Zhou, Byung Hoon Yoo, Hye Won Shin, Kyun Seop Bae, Steven E. Kern, Sung Hong Kang, Gyu Jeong Noh

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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 languageEnglish
Pages (from-to)924-934
Number of pages11
JournalAnesthesiology
Volume106
Issue number5
DOIs
Publication statusPublished - 2007 May 1

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Intravenous Fat Emulsions
Propofol
Pharmacokinetics
Unconsciousness
Safety
Therapeutic Equivalency
Korea
Emulsions
Consciousness

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 journalArticle

Kim, KM, Choi, BM, Park, SW, Lee, SH, Christensen, LV, Zhou, J, Yoo, BH, Shin, HW, Bae, KS, Kern, SE, Kang, SH & Noh, GJ 2007, 'Pharmacokinetics and pharmacodynamics of propofol microemulsion and lipid emulsion after an intravenous bolus and variable rate infusion', Anesthesiology, vol. 106, no. 5, pp. 924-934. https://doi.org/10.1097/01.anes.0000265151.78943.af
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. / Pharmacokinetics and pharmacodynamics of propofol microemulsion and lipid emulsion after an intravenous bolus and variable rate infusion. In: Anesthesiology. 2007 ; Vol. 106, No. 5. pp. 924-934.
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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{\circledR}; 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{\circledR}. CONCLUSIONS: The efficacy and safety of Aquafol were not different from those of Diprivan{\circledR} within the dose range in this study.",
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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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