Pharmacokinetics of Amphotericin B in Patients Receiving Repeated Intravenous High Doses of Amphotericin B Entrapped into Sonicated Liposomes

Autor:	Chantal Laduron, Jean-Paul Sculier, Cathy Hollaert, Claude Delcroix, Christiane Brassinne, André Coune
Rok vydání:	1989
Předmět:	Liposome Chromatography food.ingredient Cholesterol Pharmaceutical Science Pharmacology Lecithin Dissociation constant chemistry.chemical_compound food chemistry Pharmacokinetics Amphotericin B medicine Distribution (pharmacology) Liberation medicine.drug
Zdroj:	Journal of Liposome Research. 1:151-166
ISSN:	1532-2394 0898-2104
DOI:	10.3109/08982108909035988
Popis:	Repeated high doses (2-4 mg/kg/day) of amphotericin B entrapped in sonicated liposomes made of egg yolk lecithin, cholesterol, and stearylamine in the molar ratio 4:3:1 were given intravenously to cancer patients with fungal complications. High levels of the drug were measured in the serum. Pharmacokinetic analysis showed that amphotericin B distribution followed a nonlinear bicompartmental model incorporating a liposome-free drug subsystem. This model allowed us to define the Michaelis-Menten dissociation constant of uptake of the drug entrapped in the liposomes by the storage compartment, the maximal liberation rate and fractional liberation rate of free amphotericin B, and the number of binding sites in the ampholiposome storage compartment. the levels of free amphotericin B in the serum and the kinetics of saturation of the uptake of ampholiposomes by the storage compartment were also calculated.
Databáze:	OpenAIRE
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