【摘 要】
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Background 20(S)-Ginsenoside Rh2 (20(S)-Rh2) is an inhibitor of P-glycoprotein (P-gp), while ritonavir (RITV) is a substrate of P-gp.The pbarmacokinetic interaction between 20(S)-Rh2 and RITV were stu
【机 构】
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Key Laboratory of Drug Metabolism and Pharmacokinetics, State Key Laboratory of Natural Medicines, C
【出 处】
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第十届全国药物和化学异物代谢学术会议暨第三届国际ISSX/CSSX联合学术会议
论文部分内容阅读
Background 20(S)-Ginsenoside Rh2 (20(S)-Rh2) is an inhibitor of P-glycoprotein (P-gp), while ritonavir (RITV) is a substrate of P-gp.The pbarmacokinetic interaction between 20(S)-Rh2 and RITV were studied.Methods and Results 20(S)-Rh2 enhanced the uptake of RITV in Caco-2 and MDCK-MDR1 Cell lines, and exhibited a concentration-dependent effect on inhibiting RITV efflux across Caco-2 and MDCK-MDR1 Monolayers.Yet, 20(S)-Rh2 did not significantly alter RITV uptake and transport when tested on MDCK-WT cells.These results suggest 20(S)-Rh2 inhibits RITV etflux via P-gp.Further in vivo analysis of 20(S)-Rh2 on the pharmacokinetics of RITV showed that intragastric administration of 20(S)-Rh2 did not significantly alter plasma profile of RITV in Wistar rats, although intravenous injection of 20(S)-Rh2 markedly increased plasma exposure of RITV.Conclusion and Perspective 20(S)-Rh2 did not show significant effect on P-gp in intragastric gut of rats, although it inhibited RITV efflux via P-gp in cell lines.The differentiating effects of 20(S)-Rh2 on plasma profiles of RITV in rats in response to intragastric or intravenous administration of 20(S)-Rh2 indicate that other transporters or P-gp in the.specific tissue/organ are involved in the pbarmacokinetic interaction between 20(S)-Rh2 and RITV.
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