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替加氟磁性长循环脂质体在大鼠体内的药代动力学和靶向性
引用本文:曾昭武,王小丽,张阳德. 替加氟磁性长循环脂质体在大鼠体内的药代动力学和靶向性[J]. 中国药理学与毒理学杂志, 2009, 23(1): 51-54. DOI: 10.3867/j.issn.1000-3002.2009.01.010
作者姓名:曾昭武  王小丽  张阳德
作者单位:1. 中南大学国家卫生部肝胆肠外科研究中心,中南大学生物医学工程研究院,湖南,长沙,410008
2. 宜春学院,江西,宜春,336000
摘    要:
目的研究替加氟磁性长循环脂质体经肝动脉给药的药代动力学和组织靶向性。方法采用高效液相色谱仪检测大鼠生物样品中替加氟的浓度。结果磁控并加热的替加氟磁性长循环脂质体组的肝内8h药时曲线下面积(AUC)是游离替加氟组的17.4倍,是替加氟长循环脂质体组的3.9倍;其肝外组织血浆和肾的AUC比游离替加氟组低。其肝靶向效率达到73.9%。结论替加氟磁性长循环脂质体经肝动脉给药能显著增加药物的肝脏靶向性,可能降低其肾毒性。

关 键 词:替加氟  脂质体  药代动力学  肝靶向性
收稿时间:2008-08-05

Pharmacokinetics and liver targeting of tegafur magnetic long-circulating liposomes in rats
ZENG Zhao-Wu,WANG Xiao-Li,ZHANG Yang-De. Pharmacokinetics and liver targeting of tegafur magnetic long-circulating liposomes in rats[J]. Chinese Journal of Pharmacology and Toxicology, 2009, 23(1): 51-54. DOI: 10.3867/j.issn.1000-3002.2009.01.010
Authors:ZENG Zhao-Wu  WANG Xiao-Li  ZHANG Yang-De
Affiliation:ZENG Zhao-Wu1, WANG Xiao-Li2, ZHANG Yang-De1
Abstract:
AIM To study liver targeting and pharmacokinetics of tegafur magnetic long-circulating liposomes (TMLCL) which were given rats by hepatic artery. METHODS The concentration in biological specimens of rats was detected with high performance liquid chromatography. RESULTS Area under concentration-time curve of 8 h at liver in TMLCL group was 17.4 times of that in tegafur group, and 3.9 times of that in tegafur long-circulating liposome group. Tegafur concentrations in plasma and kidney were lower than those in tegafur group and its liver-targeted ratio was 73.9%. CONCLUSION TMLCL by hepatic artery can markedly increase the liver targeting for tegafur and decrease nephrotoxicity in rats.
Keywords:tegafur  liposomes  pharmacokinetics  liver targeting
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