Abstract Context: Hyperlipidaemia and hypertension are often treated together with curcumin and amlodipine. It is necessary to investigate the drug-drug interaction between curcumin and amlodipine. Objective: The interaction between curcumin and amlodipine was investigated in rats and with rat liver microsomes. Methods: The pharmacokinetics of amlodipine (1 mg/kg) was investigated in rats with or without curcumin pre-treatment (2 mg/kg), six rats in each group. The metabolic stability of amlodipine was investigated with rat liver microsomes. Results: Curcumin significantly increased the Cmax (26.19 ± 2.21 versus 17.80 ± 1.56 μg/L), AUC(0-t) (507.27 ± 60.23 versus 238.68 ± 45.59 μg·h/L), and t1/2 (14.69 ± 1.64 versus 11.43 ± 1.20 h) of amlodipine (p < 0.05). The metabolic stability of amlodipine was significantly increased with the half-life time in rat liver microsomes increased from 34.23 ± 3.33 to 44.15 ± 4.12 min, and the intrinsic rate decreased from 40.49 ± 3.26 to 31.39 ± 2.78 μL/min/mg protein. Discussion and conclusions: These results indicated that drug–drug interaction might appear during the co-administration of curcumin and amlodipine. The potential mechanism may be due to the inhibition of CYP3A4 by curcumin. Thus, this interaction should be given special attention in the clinic and needs further experiments to characterize the effect in humans.

中文翻译：

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姜黄素对氨氯地平大鼠药代动力学的影响及其潜在机制

摘要 背景：高脂血症和高血压常与姜黄素和氨氯地平一起治疗。有必要研究姜黄素和氨氯地平之间的药物相互作用。目的：在大鼠和大鼠肝微粒体中研究姜黄素和氨氯地平之间的相互作用。方法：在有或没有姜黄素预处理（2mg/kg）的大鼠中研究氨氯地平（1mg/kg）的药代动力学，每组六只大鼠。用大鼠肝微粒体研究氨氯地平的代谢稳定性。结果：姜黄素显着增加了 Cmax（26.19 ± 2.21 对 17.80 ± 1.56 μg/L）、AUC（0-t）（507.27 ± 60.23 对 238.68 ± 45.59 μg·h/L）和 t1/2（11.69 对 14.69） 11.43 ± 1.20 h) 的氨氯地平 (p < 0.05)。随着大鼠肝微粒体半衰期从34.23±3.33增加到44.15±4.12min，氨氯地平的代谢稳定性显着增加，内在速率从40.49±3.26减少到31.39±2.78μL/min/mg蛋白。讨论和结论：这些结果表明，在姜黄素和氨氯地平的共同给药期间可能会出现药物相互作用。潜在的机制可能是由于姜黄素对 CYP3A4 的抑制作用。因此，这种相互作用在临床上应该特别注意，需要进一步的实验来表征对人类的影响。这些结果表明，在姜黄素和氨氯地平的共同给药过程中可能会出现药物相互作用。潜在的机制可能是由于姜黄素对 CYP3A4 的抑制作用。因此，这种相互作用在临床上应该特别注意，需要进一步的实验来表征对人类的影响。这些结果表明，在姜黄素和氨氯地平的共同给药过程中可能会出现药物相互作用。潜在的机制可能是由于姜黄素对 CYP3A4 的抑制作用。因此，这种相互作用在临床上应该特别注意，需要进一步的实验来表征对人类的影响。