冬凌草甲素固态类脂纳米粒在小鼠体内的组织分布及兔体内的药代动力学

目的考察冬凌草甲素固态类脂纳米粒在动物体内的组织分布及药代动力学特性。方法建立生物样品中冬凌草甲素的HPLC测定法，比较冬凌草甲素普通注射液和固态类脂纳米粒注射液的体内分布特点与药代动力学参数。结果冬凌草甲素固态类脂纳米粒在肝、脾、肺、心及肾中的相对摄取率分别为4.25%，3.44%，1.19%，0.52%和0.60%。静脉注射后的药-时曲线表明体内过程符合三室模型，其各相半衰期分别为T_1/2π=0.087 h，T_1/2α=1.65 h，T_1/2β=32.36 h，中心分布容积V_C=0.66 mL·kg^-1。结论冬凌草甲素固态类脂纳米粒能够增强药物的肝脾靶向性，提高药物生物利用度，并在一定程度上延长药物在动物体内的循环时间。固态类脂纳米粒可能成为冬凌草甲素的一种新型药物载体。

The tissue distribution in mice and pharmacokinetics in rabbits of oridonin-solid lipid nanoparticles

AIM: To investigate the tissue distribution and pharmacokinetics of oridonin-solid lipid nanoparticles in animals. METHODS: HPLC method was established to determine the concentration of oridonin in serum of rabbits and in different tissues of mice. The results after tail iv administration of oridonin and oridonin solid lipid nanoparticles were compared. RESULTS: The relative tissue content of oridonin of solid lipid nanoparticles in the liver, spleen, lung, heart and kidney were 4.25%, 3.44%, 1.19%, 0.52% and 0.60%, respectively. The concentration-time curves of oridonin and oridonin solid lipid nanoparticles were both fitted to the three-compartment model. T(1/2)pi = 0.087 h, T(1/2)alpha = 1.65 h, T(1/2)beta = 32.36 h, V(C) = 0.66 mL.kg(-1). CONCLUSION :Solid lipid nanoparticles could increase the hepatic and lienic targeting efficiency of oridonin in mice and improve its bioavailability. Solid lipid nanoparticles were helpful for oridonin to reach a long circulation time and were hopeful to be its novel drug carrier.