大鼠血浆中岩白菜素含量分析方法的建立及其体内药动学

Development and validation of a method for quantification of bergenin in rat plasma: application to a pharmacokinetic study

目的建立血浆中岩白菜素的HPLC的测定方法,研究岩白菜素及岩白菜素磷脂复合物在大鼠体内的药动学行为。方法采用Odyssil C18色谱柱（250 mm×4.6 mm,5μm）,流动相为甲醇-乙腈-质量分数为0.2%的磷酸水溶液（体积比为4∶16∶80）,流速为0.8 mL·min^-1,检测波长为220 nm。应用液-液萃取法处理血浆,测定两只大鼠分别口服岩白菜及其磷脂复合物后不同时刻血浆中岩白菜素的质量浓度。结果岩白菜素质量浓度在0.01-5 mg·L^-1内线性关系良好,定量下限为0.01 mg·L^-1;提取回收率均在78.6%-90%之间;日内、日间精密度均小于13.7%。结论该方法准确度高、灵敏度强、专属性好,可作为测定大鼠血浆岩白菜素质量浓度的方法,为探讨岩白菜素的药动学行为提供方法依据。

Objective To establish a rapid and sensitive method for the determination of bergenin and bergenin phospholipid complex in rat plasma by HPLC for pharmacokinetics study. Methods Chromatographic separation of bergenin was performed on a Odyssil C18column（ 250 mm × 4. 6 mm,5 μm）with a mobile phase of methanol-acetonitrile- 0. 2%（ w） phosphorous acid（ V ∶ V ∶ V = 4∶ 16∶ 80） at a flow-rate of 0. 8 m L·min^-1 and the operating temperature of 25 ℃,and UV detection was set at 220 nm. The plasma samples were pretreated by liquid-liquid extraction. Two SD male rats were given a single dose of bergenin and bergenin phospholipid complex. Results The calibration curve exhibited good linearity over the range of0. 01- 5 mg·L^-1,and the LLOQ was 0. 01 mg·L^-1; The overall recoveries were within 78. 6%- 90%; The intra-day and inter-day precision were validated by RSD,which is less than 13. 7%. Conclusions This method is rapid and sensitive which can be applied to investigate the pharmacokinetics of bergenin in rats.