【摘要】 目的　建立测定大鼠血浆中灯盏乙素浓度的反相高效液相色谱法,研究灯盏花素及其β环糊精包合物(灯盏花素βCD)大鼠灌胃后体内药代动力学行为。方法　以甲醇水醋酸盐缓冲液为流动相,Shim packC18为固定相; 12只大鼠随机均分为2组,分别灌胃灯盏花素及其包合物后,检测血浆药物浓度。药时数据采用3P97药代计算程序处理。结果　线性范围10-400ng·mL-1,方法回收率95.32% -98. 81%;灯盏花素和包合物的Cmax分别为(154±18)ng·mL-1和(328±31)ng·mL-1;AUC0-12h分别为(710±126)ng·h·mL-1和(1. 093±200)ng·h·mL-1,经t检验两者有极显著性差异(P<0 .01)。结论　该法准确、灵敏,适用于灯盏乙素血浆浓度的测定;制备的灯盏花素包合物与灯盏花素相比吸收显著增加。更多还原

【Abstract】 Aim To establish RP-HPLC method for determination of plasma scutellarin concentration and study of the pharmacokinetic behavior of scutellarin in rat after ig administration of breviscapine and its β-cyclodextrin complex (breviscapine-β-CD). Methods Mobile phase composed of methanol and acetate buffer. The column was Shim-pack C ~18.Twelve rats randomized into 2 groups were separately given breviscapine and breviscapine-β-CD at single dose of 10.8 mg·kg~-1. Drug in plasma was extracted and determined by HPLC. The pharmacokinetic parameters were calculated by 3P97 software. Results Linearity was obtained over the range of 10-400 ng·mL~-1. The recovery was 95.32%-98.81%. C ~max and AUC ~0-12 h of breviscapine were (154±18) ng·mL~-1 and (710±126) ng·h·mL~-1. For breviscapine-β-CD, C ~max and AUC ~0-12 h were (328±31) ng·mL~-1 and (1 093±200) ng·h·mL~-1, respectively. There were significant differences of AUC ~0-12 h between breviscapine and breviscapine-β-CD (P<0.01). Conclusion The assay method was suitable for the determination of scutellarin plasma concentration in rat. Brevescapine-β-CD showed greater absorption compared with that of brevescapine.更多还原