Objective: To investigate the in vivo pharmacokinetics and distribution of sophoridine nanoliposomes in rats. Methods: Sophoridine injection and sophoridine nanoliposome were administered by intravenous injection in rats. The plasma sophoridine concentration was measured by high-efficiency liquid chromatography (HPLC) to assess their pharmacokinetics. The concentrations of sophoridine in the heart, liver, spleen, lung and kidney were determined by HPLC, respectively. The distribution of sophoridine in tissue was analyzed. Results: The AUC of sophoridine nanoliposome was 2. 42 times as much as that of sophoridine injection, meanwhile the MRT was prolonged. The concentrations of sophoridine in tissues increased initially and decreased thereafter. Compared with sophoridine injection, the average concentration of sophoridine in liver and spleen increased 4 h after intravenous injection of sophoridine liposomes, while that in other tissues decreased. Conclusion: Sophoridine liposomes can increase the distribution of sophoridine in liver and spleen indicating liver and spleen targeting properties, especially the liver targeting property.%目的:研究槐定碱纳米脂质体静脉给药后在大鼠体内药代动力学及组织分布.方法:大鼠尾静脉注射给药后,采用HPLC法测定血浆药物浓度,比较盐酸槐定碱注射液、槐定碱纳米脂质体的药代动力学；另HPLC法测定各组大鼠心脏、肝、脾、肺、肾中4h内的槐定碱浓度,分析药物组织分布情况.结果:槐定碱纳米脂质体的大鼠药时曲线AUC是普通注射液的2.42倍,体内滞留时间延长；各组织中槐定碱浓度均在0.5h达最高后开始降低；与槐定碱注射液比较,静脉注射槐定碱纳米脂质体后4h内的平均浓度在肝、脾中均升高,在其他组织中的浓度均降低.结论:槐定碱纳米脂质体能提高药物在肝、脾中的分布,具有肝、脾靶向性,尤其是肝靶向性.
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