目的 研究人参总皂苷中9种人参皂苷Rb₁、Rb₂/Rb₃、Rc、Rd、Re、Rf、Rg₁和Rh₁在大鼠体内的药动学。方法 大鼠ig 200 mg/kg人参总皂苷后于不同时间点眼底静脉丛取血。生物样本采用正丁醇液-液萃取,经C₁₈柱,应用梯度洗脱程序进行色谱分离(体积流量0.2 mL/min),应用液质联用(LC-MS)技术检测。结果 大鼠ig人参总皂苷后,血浆中可测得6种人参皂苷(Rb₁、Rb₂/Rb₃、Rc、Rd、Re和Rg₁),其中二醇型的人参皂苷(Rb₁、Rb₂/Rb₃、Rc和Rd)的体内暴露程度及半衰期显著高于三醇型的人参皂苷(Re和Rg₁)。结论 建立的人参皂苷血药浓度测定方法简便、灵敏、特异,适用于大鼠血浆中各人参皂苷的测定及人参总皂苷的药动学研究。

Objective To study the pharmacokinetic profiles of the nine ginsenosides from the roots of Panax ginseng in rats, such as ginsenosides Rb₁, Rb₂/Rb₃, Rc, Rd, Re, Rf, Rg₁, and Rh₁. Methods After different time points of ig administration of 200 mg/kg ginsenosides, the blood was taken from the venous plexus of fundus. The biological samples were extracted with n-butanol. Chromatographic separation was performed on a C₁₈ column using a gradient elution program at the flow rate of 0.2 mL/min. The LC-MS system was operated using an electro-spray ionization probe in the negative ion model. After the oral administration of 200 mg/kg ginsenosides to rats, plasma was collected and analyzed under the above conditions. The pharmacokinetic parameters were calculated by non-compartment model. Results After the oral administration of ginsenosides to rats, six ginsenosides were detected in plasma which included Rb₁, Rb₂/Rb₃, Rc, Rd, Re, and Rg₁. Among these ginsenosides, the protopanaxatriol ginsenoside Rg₁ and Re were quickly eliminated. However, the pharmacokinetic behaviors of protopanaxadiol ginsenoside Rb₁, Rb₂/Rb₃, Rc, and Rd were markedly different from those of ginsenosides Rg₁ and Re in rats with the significantly longer half-life of the protopanaxadiol ginsenosides. Conclusion The method is accurate, stable, and reliable, and can be used for profiling total ginsenosides' pharmacokinetic properties in rats.

国家自然科学基金资助项目(81202983);江苏高校优势学科建设工程资助项目;天然药物活性组分与功效国家重点实验室(中国药科大学)资助项目(SKLNMKF201209)