葡萄柚汁可改变许多药物的药动学参数,尤其对口服降胆固醇药物辛伐他汀的作用明显。尽管还不能完全确定葡萄柚汁中引起药物相互作用的成分,但推测呋喃香豆素衍生物香柠檬亭(bergamottin)是影响药动学参数的主要活性成分之一。作者通过体外试验,研究了香柠檬亭对辛伐他汀在大鼠和人肝微粒体中代谢的抑制作用。 Grapefruit juice can change the pharmacokinetic parameters of many drugs, especially for the oral cholesterol-lowering drug simvastatin. Although the components that cause drug interactions in grapefruit juice have not been completely determined, it is speculated that bergamottin, a furanocoumarin derivative, is one of the main active ingredients that affect the pharmacokinetic parameters. The authors studied in vitro the inhibitory effect of bergamottin on the metabolism of simvastatin in rat and human liver microsomes.