The pharmacokinetic characteristics of amph otericin B liposomes injection compared with market injection in rabbits after intraveno us administration / 北京大学学报(医学版)

ABSTRACT

Objective: To compare the pharmacokinetic c haracteristics of amphoterici n B liposomes injection (LAmB) with market amphotericin B injection (MAmB) in ra bbits by intravenous administration. Methods: LAmB and MAmB wer e intravenously ad ministrated to rabbits at a single dosage of 1 mg*kg －1. The AmB concent rations i n plasma samples were determined by HPLC, and the pharmacokinetic parameters wer e calculated by means of 3P97, and ANOVA were done by means of the Excel softwar e. Results: The concentration- time data of LAmB and MAmB after intravenous administration were best fitted acc ording to three compartment-model with a weight of 1/C and 1 respectively . After a singl e intravenous administra tion, C max　of LAmB and MAmB were 8.4±2.1 and 2.4±0.6 mg*L －1, AUC were 22.5±6.8 and 9.0±1.9 mg*h*L －1, CL were 0.050±0 .024 and 0.114 ±0.022 L*h －1, V c were 0.13±0.04 and 0.46±0.18 L , respectively. Comparing with MAmB, all rabbits showed high plasma levels, large area under the curve values and low cl earance, small apparent volume of distribution of LAmB. Conclusion: There were several striking differences between the pharmacokinetics properties of LAmB and MAmB in jection in rabbits. All changes of the pharmacokinetics properties will be advan tageous to reduce toxicity and improve therapeutic effect.