PHARMACOKINETICS OF [6]-GINGEROL AFTER INTRAVENOUS ADMINISTRATION IN RATS WITH ACUTE RENAL OR HEPATIC-FAILURE
PHARMACOKINETICS OF [6]-GINGEROL AFTER INTRAVENOUS ADMINISTRATION IN RATS WITH ACUTE RENAL OR HEPATIC-FAILURE
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DOI：
10.1248/cpb.40.1295
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发表时间：
1992-05-01
影响因子：
1.7
通讯作者：
IWAMOTO, K
中科院分区：
文献类型：
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作者：
NAORA, K;DING, GH;IWAMOTO, K
在双侧肾切除诱导的急性肾衰竭大鼠或单次口服四氯化碳（CCl 4）诱导的急性肝衰竭大鼠中研究了[6]-姜辣素的药代动力学，以阐明肾脏和肝脏对[6]-姜辣素消除过程的贡献。静脉推注给药后，[6]-姜辣素的血药浓度-时间曲线符合二室开放模型。对照组和肾切除大鼠的血药浓度-时间曲线或任何药代动力学参数均无显著差异。因此，这表明，肾脏排泄根本不会导致大鼠血浆中[6]-姜辣素的消失。与此相反，肝中毒与四氯化碳，升高血浆浓度的[6]-姜辣素在终端阶段。其消除半衰期显着增加，从8.5至11.0分钟，在四氯化碳中毒大鼠。[6]-姜辣素与血清蛋白结合的程度超过90%，受CCl 4-中毒的影响很小。这些方面表明，[6]-姜辣素部分由肝脏消除。
The pharmacokinetics of [6]-gingerol were investigated in rats with acute renal failure induced by bilateral nephrectomy, or those with acute hepatic failure induced by a single oral administration of carbon tetrachloride (CCl4), to clarify the contribution of the kidney and liver to the elimination process of [6]-gingerol. After bolus intravenous administration, a plasma concentration-time curve of [6]-gingerol was illustrated by a two-compartment open model. There was no significant difference in either the plasma concentration-time curve or any pharmacokinetic parameters between the control and nephrectomized rats. It is suggested, therefore, that renal excretion does not contribute at all to the disappearance of [6]-gingerol from plasma in rats. In contrast, hepatic intoxication with CCl4, elevated the plasma concentration of [6]-gingerol at the terminal phase. Its elimination half-life increased significantly, from 8.5 to 11.0 min, in CCl4-intoxicated rats. The extent of [6]-gingerol bound to serum protein was more than 90% and was affected very slightly by the CCl4-intoxication. These aspects indicate that [6]-gingerol is eliminated partly by the liver.