Abstract

1. Morin, a natural flavonol, is present in many plants. It has anti-inflammatory and immunomodulatory activities and is often used as an adjuvant treatment for arthritis. Diclofenac sodium is the first-choice drug in the treatment of rheumatoid arthritis. However, the herb-drug interaction (HDI) between morin and diclofenac sodium remains unclear.

2. The aim of the present research was to investigate whether and how morin affect the pharmacokinetic profile of diclofenac sodium.

3. The enzyme kinetic and pharmacokinetic studies showed that morin significantly accelerated the metabolism and reduced systemic exposure of diclofenac sodium. Interestingly, the effect of morin on the pharmacokinetic profile of diclofenac sodium was not in a dose-dependent manner. Therefore, the effect of morin on P-glycoprotein (P-gp) was further investigated.

4. The results implied that the influence mechanism of morin on the pharmacokinetic of diclofenac sodium might be related to CYP2C9 and P-gp. Attention should be paid to the risk of HDI between morin and diclofenac sodium in clinical practice.

摘要

1. Morin，一种天然黄酮醇，存在于许多植物中。它具有抗炎和免疫调节活性，常被用作关节炎的辅助治疗。双氯芬酸钠是治疗类风湿性关节炎的首选药物。然而，桑椹和双氯芬酸钠之间的草药-药物相互作用（HDI）仍不清楚。

2. 本研究的目的是研究桑椹素是否以及如何影响双氯芬酸钠的药代动力学特征。

3.酶动力学和药代动力学研究表明，桑椹显着加速双氯芬酸钠的代谢，减少全身暴露。有趣的是，morin 对双氯芬酸钠药代动力学特征的影响不是剂量依赖性的。因此，进一步研究了桑椹素对P-糖蛋白（P-gp）的影响。

4.结果提示桑椹素对双氯芬酸钠药代动力学的影响机制可能与CYP2C9和P-gp有关。临床上应注意桑椹与双氯芬酸钠之间发生HDI的风险。