| 引用本文: | 潘旭旺,王福根,方红英,庄让笑.18α-甘草酸固体脂质纳米粒的药动学研究[J].中国现代应用药学,2014,31(9):1086-1089. |
| PAN Xuwang,WANG Fugen,FANG Hongying,ZHUANG Rangxiao.Pharmacokinetics Study of 18α-GL Solid Lipid Nanoparticles[J].Chin J Mod Appl Pharm(中国现代应用药学),2014,31(9):1086-1089. |
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| 摘要: |
| 目的 对18α-GL固体脂质纳米粒(18α-GL-SLN)的药动学进行研究。方法 在大鼠股静脉和肝脏同时植入探针，尾静脉给药后，同步微透析采样10 h，HPLC测定透析液中18α-GL的浓度，推算血液及肝脏中真实18α-GL药物浓度，拟合药-时曲线，计算药动学参数，并进行统计分析。结果 大鼠尾静脉给予18α-GL-SLN和18α-GL后血液和肝脏的主要药动学参数Cmax、AUC0→T(n)、AUCextra和MRT差异均有统计学意义。与18α-GL水溶液相比，18α-GL-SLN的血液Cmax显著降低，肝脏Cmax显著升高，MRT显著延长，AUC显著增高。结论 18α-GL-SLN给药后药物在大鼠肝脏中的浓度显著升高，存留时间显著延长，提示18α-GL-SLN具有显著的肝脏靶向特性。 |
| 关键词: 18α-甘草酸 固体脂质纳米粒 药动学 微透析 |
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| 基金项目:杭州市医药卫生科技计划项目(2008A019)；卫生部医药卫生科技项目(2008101166) |
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| Pharmacokinetics Study of 18α-GL Solid Lipid Nanoparticles |
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PAN Xuwang, WANG Fugen, FANG Hongying, ZHUANG Rangxiao
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Manufacturing Laboratory, Xixi Hospital of Hangzhou, Hangzhou 310023, China
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| Abstract: |
| OBJECTIVE To study the pharmacokinetics of 18α-GL solid lipid nanoparticles(18α-GL-SLN). METHODS Implanted microdialysis probes into the femoral vein and liver of rats, and sampling at the same time for 10 h after 18α-GL-SLN and 18α-GL solution administration. Dialysate was determined with HPLC and real 18α-GL drug concentration in blood and liver was calculated. Drug-time curve was fitted, pharmacokinetics parameters were calculated and these parameters were compared by statistical analysis. RESULT Pharmacokinetics parameters of Cmax, AUC0→T, AUCextra and MRT were significantly different in blood and liver after 18α-GL-SLN and 18α-GL administration. Compared wih 18α-GL solution, 18α-GL-SLN had lower Cmax in blood, higher Cmax, longer MRT and higher AUC in liver. CONCLUSION Concentration of 18α-GL in liver increases significantly and the MRT becomes longer after 18α-GL-SLN administration. Experiment shows that 18α-GL-SLN has distinguished liver target characteristics. |
| Key words: 18α-GL solid lipid nanoparticles pharmacokinetics microdialysis |
