Difference in oral absorption of ginsenoside Rg1 between in vitro and in vivo models
Difference in oral absorption of ginsenoside Rg1 between in vitro and in vivo models作者机构：Department of Pharmaceutics School of Pharmacy Fudan University Shanghai China
出 版 物：《Acta Pharmacologica Sinica》 (中国药理学报(英文版))
年 卷 期：2006年第27卷第4期
页 面：499-505页
核心收录：
学科分类：1008[医学-中药学(可授医学、理学学位)] 1006[医学-中西医结合] 100602[医学-中西医结合临床] 10[医学]
主 题：ginsenoside Rgl Panax Caco-2 bioavailability pharmacokinetics
摘 要：Aim:To clarify the cause of poor oral absorption of ginsenoside Rg1(Rg1),theactive ingredient in Panax notoginseng saponins(PNS)used for ***:Caco-2 cell monolayers were used as an in vitro model tostudy the transport mechanism of Rg1across the intestinal ***,the serum concentration-time profiles after peroral(po),intraduodenal(id),portalvenous(pv)and tail venous(iv)administration of Rg1in rats were compared toevaluate the first-pass effects in the stomach,intestine,and ***:Up-take of Rg1by Caco-2 cell monolayers was temperature-dependent,but was notinfluenced by cyclosporin *** change in the apical pH produced no obviouseffect on the uptake of *** uptake and transport of Rg1was non-saturable;whereas the flux from the apical compartment to the basolateral compartment(A-B)increased in a linear manner with the increase in concentration,indicatingpassive *** apparent permeability coefficient of(2.59±0.17)×10-7cm/s(C0=1 mg/mL)predicted incomplete absorption.A significant difference was ob-served between the po(Fpowas 3.29% at a dose of 1500 mg/kg),id(Fidwas 6.60%at a dose of 1200 mg/kg)and pv(Fpvwas 50.56%)administration methods,and thebarrier function of the intestine was more significant than those of the stomachand liver in the absorption ***:Elimination in the stomach,largeintestine and liver contributed to the low oral bioavailability of Rg1,but low mem-brane permeability might be a more important factor in determining the extent ofabsorption.
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