肠道细胞色素P450和P-糖蛋白对口服药物生物利用度的影响

Effects of Intestinal Cytochrome P450 and P-glycoprotein on Oral Drug Bioavailability

目的综述肠道细胞色素P450和P-糖蛋白(P-gp)对口服药物生物利用度的影响,包括CYP450、Pgp的作用及CYP与Pgp的联合作用。方法收集、阅读并分析近十年来关于肠道细胞CYP450和Pgp影响口服药物生物利用度的文献。结果 CYP450和Pgp在胃肠道均具有高表达,且两者的底物具有显著的重叠性,所以肠道细胞CYP450对已吸收药物的生物转化作用和肠道细胞中Pgp对已吸收药物的主动外排作用是影响口服药物生物利用度的重要因素。结论肠道细胞CYP450和Pgp对药物的口服生物利用度具有重要影响。

Objective The effects of intestinal cytochrome P450（CYP450） and P-glycoprotein（P-gp） on oral drug bioavailability including the effects of CYP450,Pgp and the combined effects of them were rebiewed.Methods Collect,read and analyse literatures about the effects of intestinal CYP450 and Pgp on oral drug bioavailability.Results CYP450 and Pgp exhibited high expression in gastrointestinal tract.In addition,they possessed overlapping substrate specificities.Therefore,biotransformation of absorbed drug by intestinal CYP450 and active efflux by intestinal Pgp were the main factors affecting oral drug bioavailability.Conclusion Intestinal CYP450 and Pgp showed significant effect on oral drug bioavailability.