【摘要】 目的:研究静脉注射山柰酚后大鼠体内药动学特点。方法:将60只大鼠随机分为10个时间组,每组6只。均静脉注射给药,给药容积0.1mL·kg-1,剂量5mg·kg-1。于给药后1、3、5、10、20、40、80、120、180、240min分别从相应时间组每只大鼠取血0.5mL(n=6),采用高效液相色谱法检测大鼠血浆中山柰酚浓度;色谱柱为PhenomenexC1(8100mm×4.6mm,6μm),预柱为DikmaEasyⅡGuardC18Kit(8mm×4mm),流动相为乙腈-水(1∶2,V/V),流速为0.5mL·min-1,检测波长为370nm,柱温为35℃,进样量为80μL;采用3p97软件计算药动学参数。结果:大鼠静脉注射山柰酚的浓度-时间曲线符合二室模型,t1/2α=(0.95±0.35)min;t1/2β=(5.68±0.94)min;AUC0～t=(155.10±7.43)μg·min·mL-1;AUC0～∞=(199.84±14.07)μg·min·mL-1;CL=(45.90±1.90)mL·kg-1·min-1。结论:山柰酚原型在大鼠体内消除迅速,血药浓度下降快,30min后消除95%以上。更多还原

【Abstract】 OBJECTIVE: To investigate the pharmacokinetic characteristics of kaempferol in rats with intravenous administration. METHODS:60 rats were randomly divided into 10 time groups with 6 rats in each group. They were given medicine 5 mg·kg-1 intravenously(0.1 mL·kg-1). The blood samples 0.5 mL were collected from the rats at 1, 3, 5, 10, 20, 40, 80, 120, 180 and 240 min in each time group(n=6). The plasma level of kaempferol was determined by HPLC. The determination was performed on Phenomenex C18(100 mm×4.6 mm,6 μm) column and Dikma EasyⅡGuard C18 Kit (8 mm×4 mm) pre-column with mobile phase consisted of acetonitrile-water (1:2,V/V) at the flow rate of 0.5 mL·min-1. The detection wavelength was set at 370 nm and column temperature was 35 ℃. The injection volume was 80 μL. Pharmacokinetic parameters were calculated with 3p97 software. RESULTS: The plasma concentration-time curves of kaempferol were presented by two-compartment model in rats. The main pharmacokinetic parameters were as follows:t1/2α=(0.95±0.35) min;t1/2β=(5.68±0.94) min;AUC0→t=(155.10±7.43) μg·min·mL-1; AUC0→∞=(199.84±14.07) μg·min·mL-1;CL=(45.90±1.90) mL·kg-1·min-1. CONCLUSION: Original kaempferol is eliminated quickly in rats, and the concentration of drug decrease immediately after administration. More than 95% of the original kaempferol is eliminated in 30 min.更多还原