Physicochemical properties, pharmacokinetics, and pharmacodynamics of a reformulated microemulsion propofol in rats

Anesthesiology
Eun-Ho LeeGyu-Jeong Noh

Abstract

A newly developed microemulsion propofol consisted of 10% purified poloxamer 188 and 0.7% polyethylene glycol 660 hydroxystearate. The authors studied the physicochemical properties, aqueous free propofol concentration, and plasma bradykinin generation. Pharmacokinetics and pharmacodynamics were also evaluated in rats. The pH, particle size, and osmolarity of microemulsion propofol were measured using a pH meter, particle size analyzer, and cryoscopic osmometer, respectively. The aqueous free propofol and plasma bradykinin were measured by a dialysis method and radioimmunoassay, respectively. Microemulsion propofol was administered by zero-order infusion of 0.5, 1.0, and 1.5 mg . kg . min for 20 min in 30 rats. The electroencephalographic approximate entropy was used as a surrogate measure of propofol effect. The pH, osmolarity, and particle size of microemulsion propofol are 7.5, 280 mOsm/l, and 67.0 +/- 28.5 nm, respectively. The aqueous free propofol concentration in microemulsion propofol was 63.3 +/- 1.2 mug/ml. When mixed with human blood, microemulsion propofol did not generate bradykinin in plasma. Although microemulsion propofol had nonlinear pharmacokinetics, a two-compartment model with linear pharmacokinetics best d...Continue Reading

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Citations

Mar 1, 2012·International Journal of Clinical Pharmacology and Therapeutics·Michael Bewernitz, Hartmut Derendorf
Dec 7, 2013·Therapeutic Delivery·Bharti SapraAshok Tiwary
Aug 26, 2014·Journal of Pharmacokinetics and Pharmacodynamics·Soo-Han LeeGyu-Jeong Noh
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Jan 24, 2012·International Journal of Pharmaceutics·Guiling LiMei Li
Feb 18, 2009·British Journal of Clinical Pharmacology·Ji-Yeon SimGyu-Jeong Noh
Jun 26, 2010·Biopharmaceutics & Drug Disposition·Timothy E MoreyDonn M Dennis
Mar 15, 2012·Veterinary Anaesthesia and Analgesia·Joanne N MichouJacqueline C Brearley
Mar 25, 2015·Advanced Biomedical Research·Poupak RahimzadehMohammad Reza Ghodrati
Mar 11, 2011·Korean journal of anesthesiology·Dong Hun ChungHee-Kyung Jo
May 26, 2010·Korean journal of anesthesiology·Hye-Joo KangMyoung-Ae Lee
Dec 10, 2013·Acta Cirúrgica Brasileira·Cristian Durço PaçoLuiz Antonio Vane
Feb 1, 2012·The Journal of International Medical Research·Y-J ChaeH-B Cho
Apr 15, 2017·Computational Intelligence and Neuroscience·Kab-Mun ChaHyun-Chool Shin
Nov 15, 2016·Computational Intelligence and Neuroscience·Kyung-Jin YouHyun-Chool Shin

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