【摘要】 目的:研究氢溴酸高乌甲素在小鼠体内的药动学。方法:小鼠单剂量静脉注射氢溴酸高乌甲素3．33 mg·kg-1,用HPLC法测定给药后不同时间的血浆药物浓度。色谱条件:Microsorb-MV 100-5 C18色谱柱(250 mm×4．6 mm,5μm),流动相为甲醇-0．1 mol·L-1磷酸二氢钠溶液(50:50),流速0．6 mL·min-1,检测波长252 nm,柱温40℃。结果:氢溴酸高乌甲素血浆浓度在0．5～15μg·mL-1范围内呈良好的线性关系,日内精密度(CV)<12％,日间CV<16％,方法回收率为69．57％～83．08％。小鼠按3．33 mg·kg-1单剂量静脉注射给药,主要药动学参数为:t1/2β= 4．726 h,总清除率(CLB)=0．318 L·kg-1·h-1,VC=0．341 L·kg-1,VB=2．167 L·kg-1,AUC0→∞=10．476μg·h·mL-1。结论:氢溴酸高乌甲素静注后在小鼠体内的药时过程符合二室开放模型,原药主要分布于周边室,消除速度适中。更多还原

【Abstract】 Objective:To analyze pharmacokinetic profile of lappaconite hydrobromide (LH) in mice. Methods:The mice were intravenously injected with a single dose of lapaconite hydrobromide 3. 33 mg·kg-1 . The plasma concentration of LH in mice were measured by HPLC consisted of Microsorb MV 100-5 C18 column (250 mm×4. 6 mm, 5μm) with the column temperature at 40℃, a mobile phase of methanol-0. 1 mol·L-1 monosodium phosphate (50: 50) with a flow rate of 0. 6 mL·min-1, and detection wavelength at 252 nm. Results:The linearity of LH concentration was within 0. 5～15μg·mL-1. The within-day and among-day RSD was < 12% versus < 16%. The recovery rate of LH was in a range of 69. 57%～83. 08% . The main PK parameters were t1/2β= 4. 726 h, VC = 0. 341 L·kg-1, VB = 2. 167 L·kg-1, and AUC0→∞=10. 476μg·h·mL-1. Conclusion:The PK profile of LH for injection in mice obeyed a two-compartment open model with a distribution of peripheral compartment and moderate elimination.更多还原