Influence of intralipid on free propofol fraction assayed in human serum albumin solutions and human

来源 :Acta Pharmacologica Sinica | 被引量 : 0次 | 上传用户:yanji0708
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Aim:It is generally assumed that only unbound drugs can reach the site of actionby diffusing across the membranes and exerting pharmacological effects by inter-acting with receptors.Recent research has shown that the percentage of freedrugs may depend on the total drug concentration.The aim of the paper is toverify whether the mentioned dependence reported for propofol also takes placein plasma and human serum albumin samples in the presence of intralipid-themedium used as a vehicle for propofol infusions and a parenteral nutrition agent.Methods:Artificial plasma samples and human plasma were spiked with intralipidor ethanolic solutions of propofol.The samples were then assayed for free propofolconcentration using ultrafiltration and high performance liquid chromatographywith fluorimetric detection.Results:The decrease of the total drug concentrationresults in free propofol fraction increase,irrespectively of the used type of propofolsolvent and sample type.The addition of intralipid causes the lowering of theoverall free drug fraction with respect to the samples spiked with ethanolic solu-tions of the drug.Conclusion:The presence of intralipid does not influence thephenomenon of free propofol fraction rise at low total drug concentration.Such arise cannot be ignored in clinical conditions when the drug is applied for sedative,antiemetic or other low-dosage purposes. Aim: It is generally assumes that only unbound drugs can reach the site of action by diffusing across the membranes and exerting pharmacological effects by inter-acting with receptors. Researchers have shown that the percentage of freedrugs may depend on the total drug concentration. of the paper is toverify whether the mentioned dependence reported for propofol also takes placein 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 intralipidor ethanolic solutions of propofol.The samples were then assayed for free propofolconcentration 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 and sample type.The addition of intralipid c auses the lowering of theoverall free drug fraction with respect to the samples spiked with ethanolic solu-tions of the drug. Confc: The presence of intralipid does not influence the phenomenon of free propofol fraction rise at low total drug concentration. Sud ch can can not be ignored in clinical conditions when the drug is applied for sedative, antiemetic or other low-dosage purposes.
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