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ABSTRACT AIM: It is generally assumed that only unbound drugs can reach the site of action by diffusing across the membranes and exerting pharmacological effects by interacting with
receptors. Recent research has shown that the percentage of free drugs may depend on the total drug concentration. The aim of the paper is to verify whether the mentioned dependence reported
for propofol also takes place in plasma and human serum albumin samples in the presence of intralipid — the medium used as a vehicle for propofol infusions and a parenteral nutrition agent.
METHODS: Artificial plasma samples and human plasma were spiked with intralipid or ethanolic solutions of propofol. The samples were then assayed for free propofol concentration using
ultrafiltration and high performance liquid chromatography with fluorimetric detection. RESULTS: The decrease of the total drug concentration results in free propofol fraction increase,
irrespectively of the used type of propofol solvent and sample type. The addition of intralipid causes the lowering of the overall free drug fraction with respect to the samples spiked with
ethanolic solutions of the drug. CONCLUSION: The presence of intralipid does not influence the phenomenon of free propofol fraction rise at low total drug concentration. Such a rise cannot
be ignored in clinical conditions when the drug is applied for sedative, antiemetic or other low-dosage purposes. SIMILAR CONTENT BEING VIEWED BY OTHERS DEVELOPMENT OF EXTENDED
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SEQUESTRATION BY INTRAVENOUS LIPID EMULSION USING BIOLOGICALLY RELEVANT IN VITRO MODELS OF DRUG DISTRIBUTION Article Open access 04 November 2022 ARTICLE PDF REFERENCES * Mehta AC .
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AUTHORS AND AFFILIATIONS * Department of Chromatographic Methods, Maria Curie-Sklodowska University, Lublin, 20 031, PL, Poland Rafal Kalitynski, Andrzej L Dawidowicz & Jacek Poszytek
Authors * Rafal Kalitynski View author publications You can also search for this author inPubMed Google Scholar * Andrzej L Dawidowicz View author publications You can also search for this
author inPubMed Google Scholar * Jacek Poszytek View author publications You can also search for this author inPubMed Google Scholar CORRESPONDING AUTHOR Correspondence to Andrzej L
Dawidowicz. RIGHTS AND PERMISSIONS Reprints and permissions ABOUT THIS ARTICLE CITE THIS ARTICLE Kalitynski, R., Dawidowicz, A. & Poszytek, J. Influence of intralipid on free propofol
fraction assayed in human serum albumin solutions and human plasma. _Acta Pharmacol Sin_ 27, 1637–1641 (2006). https://doi.org/10.1111/j.1745-7254.2006.00454.x Download citation * Received:
11 April 2006 * Accepted: 16 June 2006 * Issue Date: 01 December 2006 * DOI: https://doi.org/10.1111/j.1745-7254.2006.00454.x SHARE THIS ARTICLE Anyone you share the following link with will
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content-sharing initiative KEYWORDS * propofol * unbound drugs * human serum albumin * drug binding * intralipid * plasma