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 m L/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 m L/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.