人参总皂苷主要成分大鼠体内药动学研究

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。

In vivo pharmacokinetic study on total saponins from roots of Panax ginseng in rats

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.