Excellent Absorption Enhancing Characteristics of NO Donors for Improving the Intestinal Absorption of Poorly Absorbable Compound Compared with Conventional Absorption Enhancers

2006 ◽  
Vol 21 (3) ◽  
pp. 222-229 ◽  
Author(s):  
Gihan Fetih ◽  
Fawsia Habib ◽  
Hidemasa Katsumi ◽  
Naoki Okada ◽  
Takuya Fujita ◽  
...  
Keyword(s):  
Intestinal Absorption ◽  
Absorption Enhancers ◽  
No Donors

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 Mechanistic Studies on the Absorption-Enhancing Effects of Gemini Surfactant on the Intestinal Absorption of Poorly Absorbed Hydrophilic Drugs in Rats

Pharmaceutics ◽  
2019 ◽  
Vol 11 (4) ◽  
pp. 170 ◽  
Author(s):  
Tammam Alama ◽  
Kosuke Kusamori ◽  
Masaki Morishita ◽  
Hidemasa Katsumi ◽  
Toshiyasu Sakane ◽  
...  
Keyword(s):  
Intestinal Absorption ◽  
Gemini Surfactant ◽  
Closed Loop ◽  
Intestinal Cell ◽  
Mechanistic Studies ◽  
High Potency ◽  
Absorption Enhancers ◽  
Hydrophilic Drugs ◽  
Loop Method

Generally, the use of absorption enhancers might be the most effective approaches to ameliorate the enteric absorption of poorly absorbed substances. Among numerous absorption enhancers, we already reported that a gemini surfactant, sodium dilauramidoglutamide lysine (SLG-30) with two hydrophobic and two hydrophilic moieties, is a novel and promising adjuvant with a high potency in improving the absorption safely. Here, we examined and elucidated the absorption-improving mechanisms of SLG-30 in the enteric absorption of substances. SLG-30 increased the intestinal absorption of 5(6)-carboxyfluorescein (CF) to a greater level than the typical absorption enhancers, including sodium glycocholate and sodium laurate, as evaluated by an in situ closed-loop method. Furthermore, SLG-30 significantly lowered the fluorescence anisotropy of dansyl chloride (DNS-Cl), suggesting that it might increase the fluidity of protein sections in the intestinal cell membranes. Moreover, SLG-30 significantly lowered the transepithelial-electrical resistance (TEER) values of Caco-2 cells, suggesting that it might open the tight junctions (TJs) between the enteric epithelial cells. Additionally, the levels of claudin-1 and claudin-4 expression decreased in the presence of SLG-30. These outcomes propose that SLG-30 might improve the enteric transport of poorly absorbed substances through both transcellular and paracellular routes.

scholarly journals Improvement of intestinal absorption of azetirelin, a new TRH analogue, by absorption enhancers.

1994 ◽  
Vol 9 (3) ◽  
pp. 193-197
Author(s):  
Isao Sasaki ◽  
Takashi Tamura ◽  
Takuya Fujita ◽  
Akira Yamamoto ◽  
Shozo Muranishi
Keyword(s):  
Intestinal Absorption ◽  
Absorption Enhancers

Modulation of Ganciclovir Intestinal Absorption in Presence of Absorption Enhancers

2007 ◽  
Vol 96 (10) ◽  
pp. 2710-2722 ◽  
Author(s):  
Pranav Shah ◽  
Viral Jogani ◽  
Pushpa Mishra ◽  
Anil Kumar Mishra ◽  
Tamishraha Bagchi ◽  
...  
Keyword(s):  
Intestinal Absorption ◽  
Absorption Enhancers
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