Pharmacological Sciences Unit, iMed.UL, University of Lisbon, Faculty of Pharmacy, Portugal; Department of Bioengineering and Therapeutic Sciences, University of California, San Francisco, USA.
Adv Drug Deliv Rev. 2013 Oct;65(10):1340-56. doi: 10.1016/j.addr.2012.09.042. Epub 2012 Oct 4.
The importance of drug transporters as one of the determinants of pharmacokinetics has become increasingly evident. While much research has been conducted focusing the role of drug transporters in the liver and kidney less is known about the importance of uptake and efflux transporters identified in the intestine. Over the past years the effects of intestinal transporters have been studied using in vivo models, in situ organ perfusions, in vitro tissue preparations and cell lines. This review aims to describe up to date findings regarding the importance of intestinal transporters on drug absorption and bioavailability, highlighting areas in need of further research. Wu and Benet proposed a Biopharmaceutics Drug Disposition Classification System (BDDCS) that allows the prediction of transporter effects on the drug disposition of orally administered drugs. This review also discusses BDDCS predictions with respect to the role of intestinal transporters and intestinal transporter-metabolizing enzyme interplay on oral drug pharmacokinetics.
药物转运体作为决定药物动力学的因素之一的重要性已日益明显。虽然已经进行了大量研究，重点关注药物转运体在肝脏和肾脏中的作用，但对于在肠道中发现的摄取和外排转运体的重要性知之甚少。在过去的几年中，使用体内模型、原位器官灌注、体外组织制剂和细胞系研究了肠道转运体的作用。本综述旨在描述有关肠道转运体对药物吸收和生物利用度的重要性的最新发现，突出需要进一步研究的领域。Wu 和 Benet 提出了生物药剂学药物处置分类系统（BDDCS），该系统允许预测口服药物的药物处置中转运体的作用。本综述还讨论了 BDDCS 预测与肠道转运体以及肠道转运体-代谢酶相互作用对口服药物药代动力学的关系。
