穗花杉双黄酮在大鼠体内的药动学研究

Pharmacokinetics study on amentoflavone in rats

目的建立测定大鼠血清中穗花杉双黄酮含有量的方法,并计算其药动学参数。方法血清样品甲醇液HPLC分析采用C18色谱柱（250 mm×4.6 mm,5μm）;流动相为乙腈-水（含0.1%三氟乙酸）,梯度洗脱;体积流量1.0m L/min;检测波长330 nm;柱温30℃;进样量20μL。大鼠灌胃给予穗花杉双黄酮（60 mg/kg）后,在不同时间点取血,测定血清中该成分的含有量,并计算其药动学参数。结果穗花杉双黄酮在0.010 04~0.803 2μg/m L范围内的线性关系良好（r^2=0.999 1）,血清中该成分在各质量浓度下的回收率均大于80%,Tmax为90 min,Cmax为（0.469±0.046）μg/m L,AUC0-t为（27.731±1.128）mg/（L·min）,AUC0-∞为（24.944±1.093）mg/（L·min）,t1/2为（57.008±2.765）min,V/F为（198.36±17.422）L/kg,CL/F为（2.408±0.103）L/（min·kg）。结论该方法准确、可靠,可用于大鼠血清中穗花杉双黄酮的测定及药动学研究。

AIM To establish a method for determining amentoflavone in rat serum and calculate its pharmacokinetics parameters. METHODS HPLC analysis of serum methanolic extract of AME was performed on C18column（ 250 mm × 4. 6 mm,5 μm） with acetonitrile-water（ including 0. 1% trifluoroacetic acid） as mobile phase at a flow rate of 1. 0 m L / min,the detection wavelength of 330 nm,the column temperature of 30 ℃ and the sample injection volume of 20 μL. After intragastric administration of amentoflavone（ 60 mg / kg）,rat serum was collected and checked for the plasma concentration at different intervals,then the pharmacokinetics parameters were obtained. RESULTS Amentoflavone had a good linear relationship within the range of 0. 010 04- 0. 803 2 μg / m L（ r^2= 0. 999 1）,whose recovery at different concentrations in rat serum was more than 80%,and the Tmax,Cmax,AUC0- t,AUC0- ∞,t1 /2,V/F and CL/F were 90 min,（ 0. 469 ± 0. 046） μg /m L,（ 27. 731 ± 1. 128） mg /（ L·min）,（ 24. 944 ± 1. 093） mg /（ L·min）,（ 57. 008 ± 2. 765） min,（ 198. 36 ± 17. 422） L/kg and（ 2. 408 ± 0. 103） L/（ min·kg）,respectively. CONCLUSION This accurate and reliable method can be applied to determining amentoflavone and conduct pharmacokinetics research in rat serum.