scholarly journals Intestinal absorption of forsythoside A in in situ single-pass intestinal perfusion and in vitro Caco-2 cell models

2012 ◽  
Vol 33 (8) ◽  
pp. 1069-1079 ◽  
Author(s):  
Wei Zhou ◽  
Liu-qing Di ◽  
Juan Wang ◽  
Jin-jun Shan ◽  
Shi-jia Liu ◽  
...  
Keyword(s):  
Intestinal Absorption ◽  
Intestinal Perfusion ◽  
Cell Models ◽  
Single Pass

Intestinal absorption mechanisms of araloside A in situ single-pass intestinal perfusion and in vitro Caco-2 cell model

2018 ◽  
Vol 106 ◽  
pp. 1563-1569 ◽  
Author(s):  
Hui Yang ◽  
Bingtao Zhai ◽  
Yu Fan ◽  
Jing Wang ◽  
Jing Sun ◽  
...  
Keyword(s):  
Intestinal Absorption ◽  
Cell Model ◽  
Intestinal Perfusion ◽  
Single Pass

Intestinal transport of HDND-7, a novel hesperetin derivative, in in vitro MDCK cell and in situ single-pass intestinal perfusion models

Xenobiotica ◽  
2016 ◽  
Vol 47 (8) ◽  
pp. 719-730 ◽  
Author(s):  
Ruonan Chen ◽  
Lan Li ◽  
Chenlin Shen ◽  
Cheng Huang ◽  
Taotao Ma ◽  
...  
Keyword(s):  
Mdck Cell ◽  
Intestinal Transport ◽  
Intestinal Perfusion ◽  
Single Pass

Absorption Properties of Luteolin and Apigenin in Genkwa Flos Using In Situ Single-Pass Intestinal Perfusion System in the Rat

2017 ◽  
Vol 45 (08) ◽  
pp. 1745-1759 ◽  
Author(s):  
Xin He ◽  
Zi-Jing Song ◽  
Cui-Ping Jiang ◽  
Chun-Feng Zhang
Keyword(s):  
Small Intestine ◽  
Intestinal Absorption ◽  
Rat Model ◽  
Clinical Effectiveness ◽  
Intestinal Perfusion ◽  
Flower Bud ◽  
Transport Pathway ◽  
Absorption Enhancers ◽  
Single Pass

The flower bud of Daphne genkwa (Genkwa Flos) is a commonly used herbal medicine in Asian countries. Luteolin and apigenin are two recognized active flavonoids in Genkwa Flos. The aim of this study was to investigate the intestinal absorption mechanisms of Genkwa Flos flavonoids using in situ single-pass intestinal perfusion rat model. Using HPLC, we determined its major effective flavonoids luteolin, apigenin, as well as, hydroxygenkwanin and genkwanin in biological samples. The intestinal absorption mechanisms of the total flavonoids in Genkwa Flos (TFG) were investigated using in situ single-pass intestinal perfusion rat model. Comparing the TFG absorption rate in different intestinal segments, data showed that the small intestine absorption was significantly higher than that of the colon ([Formula: see text]). Compared with duodenum and ileum, the jejunum was the best small intestinal site for TFG absorption. The high TFG concentration (61.48[Formula: see text][Formula: see text]g/ml) yielded the highest permeability ([Formula: see text]). Subsequently, three membrane protein inhibitors (verapamil, pantoprazole and probenecid) were used to explore the TFG absorption pathways. Data showed probenecid, a multidrug resistance protein (or MRP) inhibitor, effectively enhanced the TFG absorption ([Formula: see text]). Furthermore, by comparing commonly used natural absorption enhancers on TFG, it was observed that camphor was the most effective. In Situ single-pass intestinal perfusion experiment shows that TFG absorption is much higher in the small intestine than in the colon, and the TFG is absorbed mainly via an active transport pathway with MRP-mediated efflux mechanism. Camphor obviously enhanced the TFG absorption, and this could be an effective TFG formulation preparation method to increase clinical effectiveness after Genkwa Flos administration. Our study elucidated the TFG absorption mechanisms, and provided new information for its formulation preparation.

scholarly journals Intestinal Absorption Mechanisms of Five Flavonoids from Malus hupehensis (Pamp.) Rehd. Extracts in Situ Single-Pass Intestinal Perfusion and in Vitro Caco-2 Cell Model

2020 ◽  
Author(s):  
Hui Yang ◽  
Zhishu Tang ◽  
Jiangxue Cheng ◽  
Jing Wang ◽  
Junbo Zou ◽  
...  
Keyword(s):  
Cell Model ◽  
Paracellular Pathway ◽  
Intestinal Perfusion ◽  
Cancer Resistance ◽  
Absorption Mechanism ◽  
Single Pass ◽  
Malus Hupehensis ◽  
Intestinal Segments

Abstract Background: Previous studies have shown that Malus hupehensis (Pamp.) Rehd. extracts have anti-oxidant, anti-aging and other effects, its bioavailability is low, however its absorption mechanism is still unclear. To investigate the absorption properties of hyperin, quercitrin, phloridzin, quercetin, and phloretin in total flavonoids of Malus hupehensis (Pamp.) Rehd. Extracts. Methods: In situ single-pass intestinal perfusion model and in vitro Caco-2 cell model were used in this study. The effects of concentration of the extract, administration time, temperature, different intestinal segments, paracellular pathway were analyzed, and the effect of efflux inhibitors, such as the P-gp inhibitor verapamil, the multidrug resistance protein2 (MRP2) inhibitor indomethacin, the breast cancer resistance protein (BCRP) inhibitor reserpine, on the transport were evaluated. As well as EDTA, a tight junction regulator, was studied.Results: The results indicated that the jejunum was the optimal absorption intestine segment of quercitrin, phloridzin, and phloretin. And the greatest absorption intestine segment of quercetin was ileum. Furthermore, it was found that the absorption mechanisms of phloridzin in extract was involved in passive diffusion and the mediation of P-gp and MRP2 should not be neglected. The absorption mechanisms of quercetin and phloretin from extract involved active transport and were accompanied by the participation of efflux transporters, such as P-gp, MRP2 and BCRP. And also the paracellular pathway was involved in hyperin and quercitrin. Conclusion: The absorption mechanisms of five flavonoids from Malus hupehensis (Pamp.) Rehd. extract are related to the concentration of the drugs, intestinal segments, and efflux protein.

scholarly journals Preparation of Puerarin Chitosan Oral Nanoparticles by Ionic Gelation Method and Its Related Kinetics

Pharmaceutics ◽  
2020 ◽  
Vol 12 (3) ◽  
pp. 216 ◽  
Author(s):  
Jie Yan ◽  
Zhi-Yu Guan ◽  
Wei-Feng Zhu ◽  
Ling-Yun Zhong ◽  
Zhuo-Qi Qiu ◽  
...  
Keyword(s):  
In Vitro Release ◽  
Intestinal Perfusion ◽  
Pharmacokinetic Studies ◽  
Ultrasonic Power ◽  
Ionic Gelation ◽  
Single Pass ◽  
Perfusion Model ◽  
Vitro Release

In this paper, as an active ingredient, puerarin chitosan nanoparticles (Pur-CS/TPP-NPs) are prepared by an ionic gelation method. The chitosan (CS) concentration, pH of the CS solution, sodium tripolyphosphate (TPP) concentration, stirring speed, stirring time, ultrasonic power, and dosage are used as single factors for investigation, and the encapsulation efficiency, drug loading capacity, particle size, and polydispersity index (PDI) are used as indicators for investigation. The optimal prescription is determined using the Box–Behnken effect surface design method. The characterization of the best formulation, which is determined via an in vitro release assay and liquid chromatography/tandem mass spectrometry (LC-MS/MS) analysis methods, is used here for pharmacokinetic studies. An in situ single-pass intestinal perfusion model is used to investigate drug absorption in the intestine. After characterization, the morphologies of the nanoparticles are intact. It can be seen from the in vitro release experiments that the equation fitted by the nanoparticles is the Higuchi model, the nanoparticle release process is very stable and without sudden release, indicating that the nanoparticles are well-released in vitro. The pharmacokinetic results and the in situ single-pass intestinal perfusion model study show that the bioavailability and absorption of Pur-CS/TPP-NPs were significantly higher than Pur. Thus, all the results show that the prepared nanoparticles can significantly improve the bioavailability of Pur, and we hope to lay the foundation for the development of new products of Pur.

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