| 1 | Pharmacokinetics and disposition of monoterpene glycosides derived from Paeonia lactiflora roots (Chishao) after intravenous dosing of antiseptic XueBiJing injection in human subjects and rats显示文摘瞄准:从 Paeonia lactiflora 根(Chishao ) 导出的 Monoterpene glycosides 被相信为防腐草药的注射 XueBiJing pharmacologically 重要。这研究被设计描绘 monoterpene glycosides.Methods 的 pharmacokinetics 和布置:到 Chishao monoterpene glycosides 的全身的暴露在收到静脉内的注入和 XueBiJing 注射的多重注入的人的题目被估计,由对主要传播混合物的 pharmacokinetics 的评价列在后面。支持的老鼠研究也被执行。膜渗透和血浆蛋白质绑定在 vitro.Results 被估计:18 monoterpene glycosides 的一个总数在 XueBiJing 注射被检测(内容层次, 0.001-2.47 mmol/L ) ,并且 paeoniflorin 说明了检测的 monoterpene glycosides 的 85.5% 全部的剂量。在人的题目,未改变的 paeoniflorin 与 1.2-1.3 h 的消除一半生活展出了全身的暴露的可观的层次;没有重要代谢物被检测。Oxypaeoniflorin 和 albiflorin 展出了低暴露层次,并且留下的次要的 monoterpene glycosides 可以忽略或未被发现。Glomerular-filtration-based 肾的排泄是 paeoniflorin 的主要消除小径,它血浆蛋白质糟糕一定。在老鼠,当剂量被增加, paeoniflorin 的全身的暴露水平按比例增加了。老鼠肺,心,和 paeoniflorin 的肝暴露层次比血浆水平低,与肾水平的例外,它是比血浆水平大的 4.3 褶层;大脑穿入被差的膜 permeability.Conclusion 限制:由于它的重要全身的暴露和适当 pharmacokinetic 侧面,以及以前报导了防腐性质, paeoniflorin 是治疗学的重要性的有希望的 XueBiJing 成分。 | Chen CHENG Jia-zhen LIN Li LI Jun-ling YANG Wei-wei JIA Yu-hong HUANG Fei-fei DU Feng-qing WANG Mei-juan LI Yan-fen LI Fang XU Na-ting ZHANG Olajide E. OLALEYE Yan SUN Jian LI Chang-hai SUN Gui-ping ZHANG Chuan LI | 2016 | Acta Pharmacologica Sinica2016，37，4： | 15 |
| 2 | Multiple circulating saponins from intravenous ShenMai inhibit OATPIBs in vitro: potential joint precipitants of drug interactions显示文摘ShenMai, an intravenous Injection prepared from steamed Hanax ginseng roots (Hongshen) and Ophiopogon japonicus roots (Maidong), is used as an add-on therapy for coronary artery disease and cancer;saponins are its bioactive constituents. Since many saponins inhibit human organic anion-transporting polypeptides (OATP11B, this investigation determined the inhibition potencies of circulating ShenMai saponins on the transporters and the joint potential of these compounds for ShenMai drug interaction. Circulating saponins and their pharmacokinetics were charaaerized in rats receiving a 30-min infusion of ShenMai at 1OmL/kg. Inhibition of human OATP1B1/1B3 and rat Oatplb2 by the individual saponins was investigated in vitro;the compounds, joint inhibition was also assessed in vitro and the data was processed using the Chou-Talalay method. Plasma protein binding was assessed by equilibrium dialysis. Altogether, 49 saponins in ShenMai were characterized and graded into: 10-1OOμmol/day (compound doses from ShenMai;7 compounds), 1-10 μmol/day (17 compounds), and <1μmol/day (25 compounds, including Maidong ophiopogonins). After dosing, circulating saponins were protopanaxadiol-type ginbenosides Rbi, Rb2r Rc, Rd, Rg2, and Ra3, protopanaxatriol-type ginsenosides Rg1, Re, Rg2, and Rf, and ginsenoside Ro. The protopanaxadiol-type ginsenosides exhibited maximum plasma concentrations of 2.1-46.6 μmol/L, plasma unbound fractions of 0.4-1.0% and terminal half-lives of 15.6-28.5 h (ginsenoside Rg3f 1.9 h), while the other ginsenosides exhibited 0.1-77 μmol/L, 20.8-99.2%, and 0.2-0.5 h, respectively. The protopanaxadiol-type ginsenosides, ginsenosides without any sugar attachment at C-20 (except ginsenoside Rf), and ginsenoside Ro inhibited OATP1B3 more potently (IC50, 0.2-3.5 (μmol/L) than the other ginsenosides (≥22.6 μmol/L). Inhibition of OATP1B1 by ginsenosides was less potent than OATP1B3 inhibition. Ginsenosides Rb1;Rb2, Rc, Rd, Ro, Ra1, Re, and Rg2 likely contribute the major part of OATP1B3-mediated ShenMai-drug interaction potential, in an additive and time-related manner. | Olajide E. Olaleye Wei Niu Fei-fei Du Feng-qing Wang Fang Xu Salisa Pintusophon Jun-lan Lu Jun-ling Yang Chuan Li | 2019 | Acta Pharmacologica Sinica2019，40，6： | 7 |
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