Ta Wenjing, Yang Xiaoying, Wang Jie, Han Chengkun, Hua Ruochen, Lu Wen
Health Science Center, School of Pharmacy, Xi'an Jiaotong University, Xi'an 710061, China.
Shaanxi Regional Center, National Anti-Drug Laboratory, Xi'an 710000, China.
Chin Herb Med. 2022 Dec 5;15(1):117-122. doi: 10.1016/j.chmed.2022.09.004. eCollection 2023 Jan.
The intestinal absorption characteristics of active ingredients are very important for oral administration of traditional Chinese medicine (TCM) to achieve the desired therapeutic effect. However, a deeper understanding about active ingredients absorption characteristics is still lack. The aim of this study was to investigate the absorption properties and mechanism of rhubarb active ingredients in TCM preparation and pure form.
The intestinal absorption behavior of active ingredients in Shenkang extract (SKE) and rhubarb anthraquinone ingredients (RAI) were investigated by single-pass intestinal perfusion model. And the bidirectional transport characteristics of these active ingredients were assessed by Caco-2 cell monolayer model.
experiment on Sprague-Dawley rats, the effective permeability coefficient values of aloe-emodin, emodin and chrysophanol in RAI were higher than those in SKE, and the value of rhein in RAI was lower than that in SKE. But the easily absorbed segments of intestine were consistent for all ingredients, whether in SKE or in RAI. experiment, the apparent permeability coefficient values of rhein, emodin and chrysophanol in RAI were higher than those in SKE, and this value of aloe-emodin in RAI was lower than that in SKE. But their efflux ratio () values in SKE and RAI were all similar.
Four rhubarb anthraquinone ingredients in SKE and RAI have similar absorption mechanism and different absorption behavior, and the microenvironment of the study models influenced their absorption behavior. The results may provide an aid for understanding of the absorption characteristics of the TCM active ingredients in complex environments and the complementarities of different research models.
活性成分的肠道吸收特性对于口服中药达到预期治疗效果非常重要。然而，对活性成分吸收特性仍缺乏更深入的了解。本研究旨在探讨中药制剂及纯品形式下大黄活性成分的吸收特性及机制。
采用单通道肠道灌注模型研究肾康提取物（SKE）和大黄蒽醌成分（RAI）中活性成分的肠道吸收行为。并通过Caco-2细胞单层模型评估这些活性成分的双向转运特性。
在Sprague-Dawley大鼠实验中，RAI中芦荟大黄素、大黄素和大黄酚的有效渗透系数值高于SKE中的，而RAI中大黄酸的值低于SKE中的。但所有成分在SKE和RAI中，肠道易吸收段是一致的。在实验中，RAI中大黄酸、大黄素和大黄酚的表观渗透系数值高于SKE中的，而RAI中芦荟大黄素的该值低于SKE中的。但它们在SKE和RAI中的外排率（）值都相似。
SKE和RAI中的四种大黄蒽醌成分具有相似的吸收机制和不同的吸收行为，研究模型的微环境影响了它们的吸收行为。该结果可能有助于理解复杂环境中中药活性成分的吸收特性以及不同研究模型的互补性。
