【摘要】 目的研究牛蒡子苷代谢动力学与分布。方法单剂量随机灌胃,高效液相色谱法测定大鼠体内牛蒡子苷浓度及其在脏器中的分布,代谢动力学分析采用3P87软件。结果口服牛蒡子苷300 mg/kg在大鼠体内呈二室模型分布,其主要动力学参数为A=(37.374 5±8.964 7)μg·mL-1;B =(6.210 6±1.489 3)μg·mL-1;α=(0.004 3±0.000 9)min-1;β=(0.000 4±0.000 2)min-1;Kα=(0.420 2±0.167 5)min-1;t1/2α=(115.192 6±14.382 4)min ;t1/2β=(1 485.578 1±161.173 3)min;K10=(0.001 0±0.000 4)min-1;K21=(0.001 4±0.000 6)min-1;K12=(0.002 3±0.001 3)min-1;Cmax=(41.786 3±7.521 7)μg·mL-1;Tmax=(9.891 9±4.341 4)min;AUC =(22 503.272 7±4 120.182 8)μg·min·mL-1。牛蒡子苷在心、肝、肾、脑等脏器也有分布,以肝脏中最高。结论高效液相色谱法测定牛蒡子苷在动物体内代谢变化,快速、受杂质干扰小,且稳定性和重现性较好,适合牛蒡子苷代谢产物含量测定。牛蒡子苷在体内吸收很快,消除也快。更多还原

【Abstract】 OBJECTIVE To study the pharmacokinetic and distribution of arctiin in rats. METHODS Each rat was given a single dose at random by oral administration. The arctiin in serum and organs were determined by use of RP-HPLC. All pharmacokinetic parameters were calculated with a 3P87 program. RESULTS After oral administration of arctiin at the dose of 300mg·kg~ -1 , Arctiin plasma C-T curve conform to open two-compartment model. The Pharmacokinetic parameters were as follow: A=(37.374 5± 8.964 7 )μg·mL~ -1 ;B=(6.210 6±1.489 3)μg·mL~ -1 ;α=(0.004 3±0.000 9)min~ -1 ;β=(0.000 4±0.000 2)min~ -1 ;K_ α =( 0.420 2 ± 0.167 5 )min~ -1 ;t_ 1/2α =(115.192 6±14.382 4)min ;t_ 1/2β =(1 485.578 1±161.173 3)min;K_ 10 =(0.001 0± 0.000 4 )min~ -1 ;K_ 21 =( 0.001 4 ± 0.000 6 )min~ -1 ;K_ 12 =(0.002 3±0.001 3)min~ -1 ;C_ max =(41.786 3±7.521 7)μg·mL~ -1 ;T_ max =( 9.891 9 ±4.341 4)min;AUC=(22 503.272 7± 4 120.182 8 )μg·min·mL~ -1 . Liver had the highest concentration of arctiin after oral administration. CONCLUSION RP-HPLC method is rapid, sensitive and specific for the research of arctiin pharmacokinetic and its distribution in rats. Arctiin is distributed and eliminated quickly in rats.更多还原