Objective: 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 un...Objective: 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.Methods: The intestinal absorption behavior of active ingredients in Shenkang extract(SKE) and rhubarb anthraquinone ingredients(RAI) were investigated by in situ single-pass intestinal perfusion model. And the bidirectional transport characteristics of these active ingredients were assessed by in vitro Caco-2 cell monolayer model.Results: In situ experiment on Sprague-Dawley rats, the effective permeability coefficient values of aloeemodin, 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. In vitro 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(ER) values in SKE and RAI were all similar.Conclusion: 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.展开更多
目的:研究不同电荷自乳化递药系统对细梗香草皂苷B(CAPB)小肠吸收的影响。方法:分别制备CAPB的正电荷自乳化递药系统(PO-SEDDS)与负电荷自乳化递药系统(NE-SEDDS),评价其乳粒粒径、Zeta电位和自乳化时间,采用大鼠在体单向肠灌流模型考察...目的:研究不同电荷自乳化递药系统对细梗香草皂苷B(CAPB)小肠吸收的影响。方法:分别制备CAPB的正电荷自乳化递药系统(PO-SEDDS)与负电荷自乳化递药系统(NE-SEDDS),评价其乳粒粒径、Zeta电位和自乳化时间,采用大鼠在体单向肠灌流模型考察CAPB以及两种自乳化递药系统的有效肠渗透速率Peff。结果:CAPB-PO-SEDDS与CAPB-NE-SEDDS的乳粒粒径、Zeta电位和自乳化时间分别为在57.14±6.11 nm vs 56.80±4.72 nm,16.77±4.59 m V vs-3.52±0.31 m V,23±12.1 s vs 27±10.6 s,CAPB在p H=6.55的肠灌流液中能保持稳定,CAPB-PO-SEDDS的Peff为3.73±0.62×105 cm/s,显著高于CAPB-NE-SEDDS(Peff=2.72±0.42×105 cm/s)以及CAPB溶液(Peff=1.08±0.72×105 cm/s)。结论:正电荷自乳化递药系统与负电荷自乳化递药系统以及药物溶液相比,即能保持自乳化性能,又能明显促进CAPB的小肠吸收。展开更多
基金supported by the National Natural Science Foundation of China (No. 81673397)the Natural Science Basic Research Plan in Shaanxi Province of China (No. 2020JM-023)。
文摘Objective: 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.Methods: The intestinal absorption behavior of active ingredients in Shenkang extract(SKE) and rhubarb anthraquinone ingredients(RAI) were investigated by in situ single-pass intestinal perfusion model. And the bidirectional transport characteristics of these active ingredients were assessed by in vitro Caco-2 cell monolayer model.Results: In situ experiment on Sprague-Dawley rats, the effective permeability coefficient values of aloeemodin, 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. In vitro 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(ER) values in SKE and RAI were all similar.Conclusion: 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.
文摘目的:研究不同电荷自乳化递药系统对细梗香草皂苷B(CAPB)小肠吸收的影响。方法:分别制备CAPB的正电荷自乳化递药系统(PO-SEDDS)与负电荷自乳化递药系统(NE-SEDDS),评价其乳粒粒径、Zeta电位和自乳化时间,采用大鼠在体单向肠灌流模型考察CAPB以及两种自乳化递药系统的有效肠渗透速率Peff。结果:CAPB-PO-SEDDS与CAPB-NE-SEDDS的乳粒粒径、Zeta电位和自乳化时间分别为在57.14±6.11 nm vs 56.80±4.72 nm,16.77±4.59 m V vs-3.52±0.31 m V,23±12.1 s vs 27±10.6 s,CAPB在p H=6.55的肠灌流液中能保持稳定,CAPB-PO-SEDDS的Peff为3.73±0.62×105 cm/s,显著高于CAPB-NE-SEDDS(Peff=2.72±0.42×105 cm/s)以及CAPB溶液(Peff=1.08±0.72×105 cm/s)。结论:正电荷自乳化递药系统与负电荷自乳化递药系统以及药物溶液相比,即能保持自乳化性能,又能明显促进CAPB的小肠吸收。
