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目的建立测定大鼠血浆中五味子酚浓度的HPLC方法,并对五味子酚在大鼠体内的药动学特征进行研究。方法血浆样品经甲醇沉淀及乙醚萃取后,用HPLC-DAD进行测定分析。色谱柱为Eclipse XDB-C18Agilent(250 mm×4.6 mm,5μm),流动相为乙腈-水(65∶35),检测波长254 nm;测定大鼠静脉注射五味子酚18 mg/kg后的血药浓度,并利用3P87软件拟合其药动学参数。结果五味子酚的血药浓度在0.1~2.5μg/mL线性关系良好(r2=0.999),最低检测限为10 ng/mL,在3个浓度水平下,方法的回收率为88%~110%,日间和日内RSD小于15%,符合生物样品分析要求。大鼠股静脉注射18 mg/kg后,血药浓度-时间曲线呈二室模型。主要药动学参数t1/2α、t1/2β、V、AUC、MRT分别为(0.22±0.11)h、(1.19±0.22)h、(12.81±2.91)L/kg、(1.32±0.19)μg/mL/h、(1.51±0.24)h。结论该方法简便、快速、稳定可靠,适用于五味子酚的体内分析。
Objective To establish a HPLC method for the determination of the concentration of schisandrin in rat plasma and to study the pharmacokinetics of Schisandra in rats. Methods Plasma samples were precipitated by methanol and extracted with ether, then analyzed by HPLC-DAD. The column was Eclipse XDB-C18 Agilent (250 mm × 4.6 mm, 5 μm) with a mobile phase of acetonitrile-water (65:35) at a detection wavelength of 254 nm. The plasma concentration of 18 mg / kg Schisandra after intravenous injection , And 3P87 software was used to fit its pharmacokinetic parameters. Results The linear range was 0.1-2.5 μg / mL (r2 = 0.999). The detection limit was 10 ng / mL. The recovery of the method was 88% -110% at the three concentration levels. RSD less than 15% during the day and in the day, in line with biological sample analysis requirements. After the rat femoral vein injection of 18 mg / kg, the plasma concentration-time curve showed a two-compartment model. The main pharmacokinetic parameters t1 / 2α, t1 / 2β, V, AUC and MRT were (0.22 ± 0.11) h, (1.19 ± 0.22) h and (12.81 ± 2.91) L / mL / h, (1.51 ± 0.24) h. Conclusion The method is simple, rapid, stable and reliable, suitable for in vivo analysis of schisandrin.