Mechanistic understanding of the different effects of Wuzhi Tablet (Schisandra sphenanthera extract) on the absorption and first-pass intestinal and hepatic metabolism of Tacrolimus (FK506)
Mechanistic understanding of the different effects of Wuzhi Tablet (Schisandra sphenanthera extract) on the absorption and first-pass intestinal and hepatic metabolism of Tacrolimus (FK506)
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DOI：
10.1016/j.ijpharm.2010.01.025
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发表时间：
2010-04-15
影响因子：
5.8
通讯作者：
Huang, Min
中科院分区：
文献类型：
--
作者：
Qin, Xiao Ling;Bi, Hui Chang;Huang, Min
我们最近报道了他克莫司（FK506）在大鼠血药浓度显著增加后，摄入中药制剂五脂片（WZ，五味子提取物）。为了确定FK506水平升高的潜在机制，我们在体外和体内研究了WZ对FK506吸收和首过肠道和肝脏代谢的影响。与WZ联合给药时，口服FK506的AUC（0-∞）值提高了2.1倍，口服生物利用度（F-oral）从5.4%提高到13.2% (p = 0.0002), （F-abs × F-G）为111.4% （p = 0.0002）
We recently reported that the blood concentrations of Tacrolimus (FK506) in rats were markedly increased following the intake of a Chinese herbal preparation, Wuzhi Tablet (WZ, Schisandra sphenanthera extract). In order to identify the underlying mechanisms of the increase in FK506 level, we investigated the effects of WZ on the absorption and first-pass intestinal and hepatic metabolism of FK506 in vitro and in vivo. When co-administered with WZ, the AUC(0-infinity) value after oral FK506 dosing was increased by 2.1 fold, the oral bioavailability (F-oral) was increased from 5.4% to 13.2% (p = 0.0002), and the (F-abs x F-G) was 111.4% (p