Department of Emergency, Yidu Central Hospital of Weifang, Weifang, Shandong, China.
Department of Cardiovascular Medicine, Yidu Central Hospital of Weifang, Weifang, Shandong, China.
Pharm Biol. 2020 Dec;58(1):465-468. doi: 10.1080/13880209.2020.1764060.
Hyperlipidaemia and hypertension are often treated together with curcumin and amlodipine. It is necessary to investigate the drug-drug interaction between curcumin and amlodipine. The interaction between curcumin and amlodipine was investigated in rats and with rat liver microsomes. 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. Curcumin significantly increased the (26.19 ± 2.21 versus 17.80 ± 1.56 μg/L), (507.27 ± 60.23 versus 238.68 ± 45.59 μg·h/L), and (14.69 ± 1.64 versus 11.43 ± 1.20 h) of amlodipine ( < 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. 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.
高脂血症和高血压常联合使用姜黄素和氨氯地平进行治疗。有必要研究姜黄素和氨氯地平之间的药物相互作用。在大鼠和大鼠肝微粒体中研究了姜黄素和氨氯地平之间的相互作用。在有或没有姜黄素预处理（2 mg/kg）的情况下，每组 6 只大鼠，研究了大鼠体内氨氯地平（1 mg/kg）的药代动力学。用大鼠肝微粒体研究了氨氯地平的代谢稳定性。姜黄素显著增加了氨氯地平的（26.19 ± 2.21 对 17.80 ± 1.56 μg/L）、（507.27 ± 60.23 对 238.68 ± 45.59 μg·h/L）和（14.69 ± 1.64 对 11.43 ± 1.20 h）（<0.05）。氨氯地平在大鼠肝微粒体中的代谢稳定性显著增加，半衰期从 34.23 ± 3.33 增加到 44.15 ± 4.12 min，内在清除率从 40.49 ± 3.26 降低到 31.39 ± 2.78 μL/min/mg 蛋白。这些结果表明，姜黄素和氨氯地平联合用药可能会出现药物相互作用。潜在的机制可能是由于姜黄素抑制了 CYP3A4。因此，在临床中应特别注意这种相互作用，并需要进一步的实验来表征其在人体中的作用。
