积雪草苷在大鼠体内的药动学研究

目的:研究积雪草苷在大鼠体内的药动学特点。方法:用高效液相色谱法,以葫芦素B为内标,甲醇为血浆蛋白沉淀剂,水-乙腈(24∶76)为流动相,测定一次性给大鼠尾静脉注射积雪草苷(42或126mg·kg-1)后SD大鼠血浆中积雪草苷的浓度。采用3p97程序计算药动学参数。结果:积雪草苷在SD大鼠体内的药动学符合二室开放模型,2个剂量组的t1/2α分别为1.89和1.73min,t1/2β分别为27.08和26.81min,K21分别为0.24和0.20min,K10分别为0.039和0.031min,K12分别为0.11和0.13min,AUC分别为1442.11和5749.78mg·min·L-1,CL分别为0.029和0.022mL·g-1·min-1,MRT分别为39.08和38.70min。结论:积雪草苷在SD大鼠体内的分布消除较快,呈一级动力学特征。

Pharmacokinetic Study of Asiaticoside in Rats

OBJECTIVE： To investigate the pharmacokinetic characteristics of asiaticoside in rats. METHODS： HPLC method was used to determine the plasma concentration of asiaticoside in SD rats with single dose of asiaticoside （42 mg·kg^-1 or 126mg·kg^-1） via tail vein. Methanol was used to precipitate the plasma protein and water-acetonitrile （24 ： 76） was used as mobile phase. Cucurbitacin B was applied as internal standard. 3p97 program was used to calculate pharmacokinetic parameters. RESULTS： The pharmacokinetics of asiaticoside in SD rats conformed to two-compartment open model. The main pharmacokinetic parameters of two groups were as follows：t1/2α 1.89 min vs. 1.73 min;t1/2β：27.08 min vs. 26.81 min;K21： 0.24 min^-1 and 0.20 min;K10：0.039 min and 0.031 rain; K12：0.11 min and 0.13 min; AUC： 1 442.1 mg·min·L^-1 vs. 5 749.78 mg·min·L^-1;CL：0.029 mL·g·min^-1 vs, 0.022 mL·g·min^-1;MRT： 39.08 min vs. 38.70 rain, respectively. CONCLUSION： The pharmacokinetics of asiaticoside show a rapid distribution and elimination process in SD rats and is of first-order dynamic characteristics.