a School of Pharmacy, Lanzhou University , Lanzhou , China.
b Key Laboratory for Prevention and Remediation of Plateau Environmental Damage , Lanzhou General Hospital , Lanzhou , China.
Drug Metab Rev. 2018 Aug;50(3):357-368. doi: 10.1080/03602532.2018.1497647. Epub 2018 Sep 19.
Gut microbiota, one of the determinants of pharmacokinetics, has long been underestimated. It is now generally accepted that the gut microbiota plays an important role in drug metabolism during enterohepatic circulation either before drug absorption or through various microbial enzymatic reactions in the gut. In addition, some drugs are metabolized by the intestinal microbiota to specific metabolites that cannot be formed in the liver. More importantly, metabolizing drugs through the gut microbiota prior to absorption can alter the systemic bioavailability of certain drugs. Therefore, understanding intestinal flora-mediated drug metabolism is critical to interpreting changes in drug pharmacokinetics. Here, we summarize the effects of gut microbiota on drug pharmacokinetics, and propose that the influence of intestinal flora on pharmacokinetics should be organically related to the therapeutic effects and side effects of drugs. More importantly, we could rationally perform the strategy of intestinal microflora-mediated metabolism to design drugs.
肠道微生物群是决定药代动力学的因素之一，长期以来一直被低估。现在普遍认为，肠道微生物群在药物吸收前的肠肝循环或通过肠道中的各种微生物酶反应中，在药物代谢中起着重要作用。此外，一些药物被肠道微生物群代谢为特定的代谢物，这些代谢物在肝脏中无法形成。更重要的是，通过肠道微生物群在吸收前代谢药物会改变某些药物的全身生物利用度。因此，了解肠道菌群介导的药物代谢对于解释药物药代动力学的变化至关重要。在这里，我们总结了肠道菌群对药物药代动力学的影响，并提出肠道菌群对药代动力学的影响应该与药物的治疗效果和副作用有机地联系起来。更重要的是，我们可以合理地进行肠道微生物群介导的代谢策略来设计药物。
