紫杉醇纳米制剂在小鼠体内的药代动力学研究  

Pharmacokinetics of SWCNTs-Paclitaxel in mice

作　　者：张艳艳[1] 付旭东[2] 赵继敏[1] 张晓艳[1] 赵明耀[1] 张振中[3] 

机构地区：[1]郑州大学基础医学院病理生理学教研室,河南郑州450001 [2]郑州大学第五附属医院,河南郑州450052 [3]郑州大学药学院,河南郑州450001

出　　处：《中国现代医学杂志》2013年第31期6-11,共6页China Journal of Modern Medicine

基　　金：国家自然科学基金(No:037167781910)

摘　　要：目的通过测定紫杉醇浓度,进行紫杉醇纳米制剂(SWCNTs-PTX)在小鼠体内的药代动力学研究,并考察其在体组织分布情况。方法紫杉醇的血药浓度及在各组织的药物浓度均采用高效液相色谱法测定,色谱柱为Eclipse XDB-C18(150 mm×4.6 mm,5μm);流动相为乙腈∶水=60∶40,流速为1 mL/min,检测波长为227 nm。用3p87程序和SPSS 13.0统计软件处理和分析数据,计算相关药代动力学参数。结果紫杉醇及其纳米制剂在静脉注射后在小鼠体内代谢符合二房室模型,日间和日内RSD均小于10%。紫杉醇纳米制剂在肝脏和瘤体的分布明显比单纯紫杉醇注射液较多(P<0.05);其它组织中两者分布基本相近(P>0.05)。结论紫杉醇制成纳米制剂(SWCNTs-PTX)后,体内药代行为发生明显变化,其组织分布快,有肝和肿瘤组织靶向趋势,值得对紫杉醇纳米制剂作进一步的研究。【Objective】To investigate the pharmacokinetics and tissue distribution of Paclitaxel-carbon nanotubes in mice. 【Methods】The concentration of paclitaxel in plasma and different tissues was determined by high perfor- mance liquid chromatography（HPLC）. Chromatographic column was Eclipse XDB-C18（150 mm ×4.6 mm,5 μm）; moving phase was acetonitrile and water（60：40）, flow rate was 1 mL/min, detection wavelength was 227 nm. The pharmacokinetic parameters were calculated and analyzed by 3p87 program and SPSS13.0 statistical software.【Re- sult】The result of pharmacokinetics of Paclitaxel and SWCNTs- PTX was fitted to two-compartmentmode in mice. RSDs of within-day and between-day was less than 10%. The distribution of SWCNTs-PTXin liver and tumor was more than Paclitaxe（P 0.05）, and the distribution was similar in other tissue（P 0.05）.【Conclusion】The pharma- cokinetic action was different between SWCNTs-PTX and Paclitaxel. The liver and tumor targeting of SWCNTs-PTX was more obviously than Paclitaxel and the tissue distribution of SWCNTs- PTX was faster.

关 键 词：紫杉醇 单壁碳纳米管 高效液相色谱法 药代动力学 

分 类 号：R917[医药卫生—药物分析学] R-332[医药卫生—药学]