5-氟尿嘧啶脂质体体内动力学研究

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本文用高压液相色谱仪测定5-氟尿嘧啶(5-FU)脂质体在血和组织中的药物浓度。给动物注射脂质体后所得参数表明。5-FU脂质体在家兔体内的动力学性质属单房室模型,血中半衰期为58.3分钟。按实验用家兔体重2.5kg,依组织液占有20%计算值为0.21/kg,而5-FU脂质体在家兔的分布容积为1.08L/kg,远大于组织容积。表明脂质体从血液向其它组织转移容易,分布较广,5-FU脂质体在肝、肺浓度比5-FU注射液高,持续时间也长,而两者在肾脏浓度均较高,持续时间颇为近似,可能与游离药物在肾中浓度较高有关,经数学处理结果与体内分布实验结果相一致,提示5-FU脂质体以静脉滴注为宜。 In this paper, high-pressure liquid chromatography determination of 5-fluorouracil (5-FU) liposomes in blood and tissue drug concentration. The parameters obtained after injection of liposomes into animals show. The kinetic properties of 5-FU liposomes in rabbits are single-chamber model with a blood half-life of 58.3 minutes. According to the experimental rabbit body weight of 2.5kg, 20% of tissue fluid accounted for 0.21 / kg, while the distribution of 5-FU liposomes in rabbits was 1.08L / kg, much larger than the volume of tissue. The results showed that the liposomes were easy to transfer from blood to other tissues. The distribution of 5-FU liposomes in liver and lung was higher than that of 5-FU injection and the duration was longer. Both of them had higher renal concentration, The duration is quite similar, which may be related to the higher concentration of free drug in the kidney. The results of the mathematical treatment are in good agreement with the experimental results in vivo, which suggests that intravenous infusion of 5-FU liposomes is appropriate.
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