高效液相色谱法测定益母草碱大鼠血浆浓度及其药代动力学研究

摘要

Objective To establish the HPLC method to detect the mass concentration of leonurine in rat plasma,and the pharmacoki-netics was evaluated.Methods The mass concentration of leonurine in 8 rats was detected after intravenous injection of 20 mg/kg leonurine by HPLC.The mobile phase was acetonitrile-0.02 moL/L mono potassium phosphate(adjusting to pH=4.0 with phosphoric acid)=60 ∶40,at the flow rate of 1.0 mL/min and detected at 277 nm,the column temperature was 30 ℃.Results The process of leonurine in rats fit two-compartment model.The main pharmacokinetic parameters were followed:t1 /2α was (0.46 ±0.13)h,t1 /2β was (2.90 ±1.41)h,V was(0.46 ±0.07)L/kg,AUC(0-t) was (70.65 ±12.39)mg/(h·L).Conclusion This method was accurate,stable and sensitive,which can be used for the determination and pharmacokinetic of Leonurine.%目的：建立测定大鼠血浆中益母草碱质量浓度的高效液相色谱（HPLC ）法，并研究益母草碱在大鼠体内的药代动力学特征。方法8只SD大鼠尾静脉注射益母草碱后，采用HPLC法测定血浆中益母草碱的质量浓度，流动相为乙腈-0．02 moL／L磷酸二氢钾（磷酸调pH＝4．0）＝60∶40，波长为277 nm，流速为1 mL／min，柱温为30℃。结果益母草碱在大鼠体内分布符合二室模型，主要药代动力学参数消除半衰期(t1／2α)为（0．46±0．13）h，t1／2β为（2．90±1．41）h，中心室分布容积(V)为（0．46±0．07）L／kg，药时曲线下面积(AUC0-t)为（70．65±12．39）mg／（h·L）。结论该方法简便、快速，可用于体内益母草碱的测定及药代动力学研究。