山奈酚在家兔体内的药动学研究

目的:研究山奈酚在家兔体内的药动学特征。方法:6只家兔分别静脉注射山奈酚(2.0 mg/kg),分别于给药后1、3、5、10、15、20、40、80、160、240 min采血。采用高效液相色谱(HPLC)法检测家兔血浆中山奈酚质量浓度。色谱柱为Phenomenex C18(100mm×4.6 mm,6μm),流动相为乙腈-水(1∶2,V/V),流速为0.5 ml/min,检测波长为370 nm,柱温为35℃,进样量为80μl。经3p97软件计算药动学参数,并进行统计学分析。结果:山奈酚回归方程为y=1.077 1x-0.044 3(r=0.999 6)。山奈酚质量浓度在0.040¹6.213μg/ml范围内与峰面积和内标峰面积比值呈良好线性关系。静脉注射山奈酚后,t1/2α、t1/2β、CL、AUC0→t分别为(0.957±0.172)min、(6.409±1.584)min、(0.034±0.003)ml/min、(98.459±7.031)μg·min/ml。结论:静脉注射山奈酚后消除加快,提示应改变山奈酚的给药途径。

Pharmacokinetic Study of Keampferol in Rabbits

OBJECTIVE： To investigate the pharmacokinetic characteristics of keampferol in rabbits. METHODS： 6 rabbits were given keampferol（2.0 ml/min） intravenously. The blood samples were collected from the rabbits at 1, 3, 5, 10, 15, 20, 40, 80, 160 and 240 min, respectively. The keampferol concentrations were determined by HPLC. The determination was performed on Phenomenex C18（100mm×4.6 mm, 6 μm）column with mobile phase consisted of acetonitrile-water （1 ： 2, V/V） at the flow rate of 0.5 ml/min. The detection wavelength was set at 370 nm, and the colunm temperature was 35 ℃. The sample size was 80 μl. Phar- macokinetic parameters were calculated by 3p97 program and analyzed statistically. RESULTS： The regression equation of keamp- ferol was y=1.077 lx-0.044 3 （r=0.999 6）. The linear range of keampferol was 0.040-16.213μg/ml. After intravenous injection of keampferol, the main pharmacokinetic parameters were as follows： t1/2α（0.957 ± O.172）min,t1/2β（6.409 ± 1.584）min, CL（0.034 ± 0.003） ml/min and AUC0-t（98.459 ± 7.031 ） μg. min/ml, respectively. CONCLUSIONS： Keampferol is eliminated quickly in rab- bits, which indicate the route of administration should be changed.