■人参在东方文化中被认为是一种具有神奇功效的珍贵药草。人参的主要化学成分是皂苷,人参皂苷的生理活性决定了其食用和药用价值。本研究的目的是全面系统地研究20(S)-原人参二醇(PPD)在大鼠和犬体内的动力学过程,以促进人参作为药物和膳食成分的合理结合。
■给予PPD,采用液相色谱串联质谱(LC/MS/MS)和放射性示踪法检测不同生物样品中的药物浓度。药代动力学参数,如吸收,生物利用度,组织分布,血浆蛋白结合率,排泄率,并计算了累积排泄量,以及主要代谢物的推断。
■这项研究系统地研究了吸收,分布,新陈代谢,PPD在大鼠和犬中的排泄(ADME)为首次。PPD的生物利用度相对较低,口服吸收几乎完全,大多数人经历了首过代谢。PPD具有高的血浆蛋白结合率并且在体内相对均匀地分布。口服后,PPD经历了广泛的代谢,可能涉及一个结构转变和三个羟基化反应。代谢产物主要通过粪便和尿液排出,表明存在肝肠循环。静脉内给药后PPD的药代动力学过程与三室模型吻合良好。相比之下,经胃给药后,它更适合两个隔间的模型,符合线性药代动力学和比例消除。在PPD方面,大鼠和狗之间存在明显的种间差异,但是这种药物在同一物种中的个体差异很小。
■本研究系统研究了大鼠PPD的动力学过程,并首次研究了犬PPD的动力学特征。这些发现为进一步研究PPD的膳食营养和药理作用奠定了基础。
UNASSIGNED: Ginseng has been regarded as a precious medicinal herb with miraculous effects in Eastern culture. The primary chemical constituents of ginseng are saponins, and the physiological activities of ginsenosides determine their edible and medicinal value. The aim of this study is to comprehensively and systematically investigate the kinetic processes of 20(S)-protopanaxadiol (PPD) in rats and dogs, in order to promote the rational combination of ginseng as a drug and dietary ingredient.
UNASSIGNED: PPD was administered, and drug concentration in different biological samples were detected by liquid chromatography tandem mass spectrometry (LC/MS/MS) and radioactive tracer methods. Pharmacokinetic parameters such as absorption, bioavailability, tissue distribution, plasma protein binding rate, excretion rate, and cumulative excretion were calculated, along with inference of major metabolites.
UNASSIGNED: This study systematically investigated the absorption, distribution, metabolism, excretion (ADME) of PPD in rats and dogs for the first time. The bioavailabilities of PPD were relatively low, with oral absorption nearly complete, and the majority underwent first-pass metabolism. PPD had a high plasma protein binding rate and was relatively evenly distributed in the body. Following oral administration, PPD underwent extensive metabolism, potentially involving one structural transformation and three hydroxylation reactions. The metabolites were primarily excreted through feces and urine, indicating the presence of enterohepatic circulation. The pharmacokinetic processes of PPD following intravenous administration aligned well with a three-compartment model. In contrast, after gastric administration, it fitted better with a two-compartment model, conforming to linear
pharmacokinetics and proportional elimination. There were evident interspecies differences between rats and dogs regarding PPD, but individual variations of this drug were minimal within the same species.
UNASSIGNED: This study systematically studied the kinetic process of PPD in rats and also investigated the kinetic characteristics of PPD in dogs for the first time. These findings lay the foundation for further research on the dietary nutrition and pharmacological effects of PPD.