The intestine has important gate-keeping functions that can profoundly affect the systemic blood exposure of orally administered drugs. Thus, characterizing a new molecular entity's (NME) disposition within the intestine is of utmost importance in drug development. While currently used in vitro systems, such as Ussing chamber, precision-cut intestinal slices, immortalized cell lines, and primary enterocytes provide substantial knowledge about drug absorption and the intestinal first-pass effect, they remain sub-optimal for quantitatively predicting this process and the oral bioavailability of many drugs. Use of novel in vitro systems such as intestinal organoids and intestinal microphysiological systems have provided substantial advances over the past decade, expanding our understanding of intestinal physiology, pathology, and development. However, application of these emerging in vitro systems in the pharmaceutical science is in its infancy. Preliminary work has demonstrated that these systems more accurately recapitulate the physiology and biochemistry of the intact intestine, as it relates to oral drug disposition, and thus they hold considerable promise as preclinical testing platforms of the future. Here we review currently used and emerging in vitro models of the human intestine employed in pharmaceutical science research. We also highlight aspects of these emerging tools that require further study.

肠道具有重要的把关功能，可以深刻影响口服药物的全身血液暴露。因此，表征新分子实体（NME）在肠道内的分布对于药物开发至关重要。虽然目前使用的体外系统，如尤斯室、精确切割的肠切片、永生化细胞系和原代肠上皮细胞提供了有关药物吸收和肠道首过效应的大量知识，但它们对于定量预测这一过程仍然不是最佳的，并且许多药物的口服生物利用度。肠道类器官和肠道微生理系统等新型体外系统的使用在过去十年中取得了实质性进展，扩大了我们对肠道生理学、病理学和发育的理解。然而，这些新兴的体外系统在制药科学中的应用还处于起步阶段。初步工作表明，这些系统更准确地概括了完整肠道的生理学和生物化学，因为它与口服药物处置有关，因此它们作为未来的临床前测试平台具有相当大的前景。在这里，我们回顾了药物科学研究中当前使用的和新兴的人体肠道体外模型。我们还强调了这些新兴工具需要进一步研究的方面。