水飞蓟素的药动学及药物相互作用

Pharmacokinetics and herb-drug interactions of silymarin

水飞蓟素是水飞蓟种子中提取的黄酮多酚类混合物。在体内经一相和二相代谢后大部分经胆汁排泄,可降低CYP450酶、葡萄糖醛酸转移酶(UCT)的活性;抑制P糖蛋白(P-gP)、OATP1B1与BCRP的转运,从而影响相应酶与转运体底物的药动学参数,因此发生药物相互作用的风险较高。本文综述了近年来水飞蓟素的药动学及药物相互作用研究。

Silymarin is a mixture of polyphenoic fiavonoids extracted from the seeds of milk thistle. It undergoes phase Ⅰ and phase Ⅱ metabolism and is primarily excreted from the body by bile and urine. Silymarin can decrease the activity of CYP450 and UDP-glucuronosyhransferase （UGT） enzyme. It can also inhibit the transportation of P-glycoprotein （P-gp）, OATP1B1 as well as BCRP, and affect the pharmacokinetics of several drugs in vivo. Therefore, the risk of drug-drug interaction is high. This paper reviewed the recent studies on the herb-drug interaction for silymarin.