汉黄芩素固体脂质纳米粒在大鼠体内的药动学及组织分布

Study on Pharmacokinetics and Distribution of Wogonin Solid Lipid Nanoparticles in Rats

目的:研究汉黄芩素固体脂质纳米粒在大鼠体内的药动学及组织分布情况。方法:大鼠随机分成汉黄芩素注射液组和汉黄芩素固体脂质纳米粒组,分别于给药后不同时间采血测定汉黄芩素含量,并测定两组大鼠心、肝、脾、肺、肾中汉黄芩素含量,计算靶向效率以评价其在大鼠体内的组织分布及靶向性。结果:汉黄芩素固体脂质纳米粒在大鼠体内的药动学模型符合二室模型,主要药动学参数为:t_(1/2α)=(0.551 0±0.124 7)h,t_(1/2β)=(14.589 1±1.563 8)h,CL=(0.006 4±0.0014)ml·h·Kg^(-1),AUC_(0→8)=(125.76±9.5728)mg·h·L^(-1),其在肝脏、脾脏、心脏、肺脏及肾脏的靶向效率分别为2.003、1.789、0.634、0.707、0.259。结论:与汉黄芩素溶液相比,汉黄芩素固体脂质纳米粒能提高对肝脏、脾脏的趋向性,有利于提高其治疗作用。

Objective： To study the pharmacokinetics and distribution of wogonin solid lipid nanoparticles （SLN） in rats. Method： The plasma concentration of wogonin in rats was determined by HPLC and the pharmacokinetic parameters were calculated by soft- ware program 3P97. The targeting efficiency （To） was used to evaluate the tissue targeting of wogonin SLN. Result： The pharmacoki- netic property fitted a two - compartment model, and the main pharmacokinetic parameters of wogonin SLN were as follows： tl/2α of （0.5510＋0.1247）h, t1/2β of （14.589 1＋1.5638）h, CL of （0.0064＋0.001 4） ml .h .kg^-1 and AUC0→8 of （125.76 ＋ 9.572 8 ） mg ·h ·L ^- 1. Compared with that of wogonin solution, the To of live, spleen, heart, hung and kidney of wogonin SLN were 2. 003,1. 789,0. 634,0. 707 and 0. 259, respectively. Conclusion： Compared with wogonin solution, wogonin SLN show remarkable sustained-release property, and can enhance wogonin bioavailability in rats.