Prediction of Human Intestinal Absorption of the Prodrug Temocapril by In Situ Single-Pass Perfusion Using Rat Intestine with Modified Hydrolase Activity

2011 ◽  
Vol 39 (7) ◽  
pp. 1263-1269 ◽  
Author(s):  
Takaaki Nozawa ◽  
Teruko Imai
Keyword(s):  
Intestinal Absorption ◽  
Hydrolase Activity ◽  
Rat Intestine ◽  
Single Pass ◽  
Human Intestinal Absorption ◽  
Pass Perfusion

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.

Assessment of Ferrous Glycinate Liposome Absorption Using in Situ Single-Pass Perfusion Model

2017 ◽  
Vol 13 (9) ◽  
Author(s):  
Baomiao Ding ◽  
Xiangzhou Yi ◽  
Li Li ◽  
Hualin Yang
Keyword(s):  
Particle Size ◽  
Phytic Acid ◽  
Intestinal Permeability ◽  
Iron Absorption ◽  
Inhibitory Effects ◽  
Single Pass ◽  
Pass Perfusion ◽  
Absorption Pathways ◽  
Main Factor

AbstractLiposomes could be employed to improve the absorption of iron. The purpose of this study was to estimate the intestinal permeability of ferrous glycinate liposomes and to assess the effects of phytic acid, zinc and particle size on iron absorption usingin situsingle-pass perfusion in rats. The results showed that the absorption of ferrous glycinate liposomes was obviously higher than that of ferrous glycinate. The inhibitory effects of phytic acid and zinc on iron absorption were reduced by incorporating ferrous glycinate into liposomes. The particle size of ferrous glycinate liposomes was also a main factor for affecting iron absorption, and the intestinal permeability of the liposomes decreased with its particle size increasing. The results suggested that liposomes could be a potent delivery system to decrease the inhibitory effects of phytic acid and zinc and to enhance iron absorption. Furthermore, liposomes could alter the absorption pathways of ferrous glycinate.

scholarly journals Regional Absorption of Fimasartan in the Gastrointestinal Tract by an Improved in situ Absorption Method in Rats

Pharmaceutics ◽  
2018 ◽  
Vol 10 (4) ◽  
pp. 174 ◽  
Author(s):  
Tae Hwan Kim ◽  
Soo Heui Paik ◽  
Yong Ha Chi ◽  
Jürgen B. Bulitta ◽  
Da Young Lee ◽  
...  
Keyword(s):  
Small Intestine ◽  
Large Intestine ◽  
Great Promise ◽  
Absorption Method ◽  
Single Pass ◽  
Pass Perfusion ◽  
Starting Point ◽  
Fraction Absorbed ◽  
In Situ Absorption

The aim of the present study was to assess the regional absorption of fimasartan by an improved in situ absorption method in comparison with the conventional in situ single-pass perfusion method in rats. After each gastrointestinal segment of interest was identified, fimasartan was injected into the starting point of each segment and the unabsorbed fimasartan was discharged from the end point of the segment. Blood samples were collected from the jugular vein to evaluate the systemic absorption of the drug. The relative fraction absorbed (Fabs,relative) values in the specific gastrointestinal region calculated based on the area under the curve (AUC) values obtained after the injection of fimasartan into the gastrointestinal segment were 8.2% ± 3.2%, 23.0% ± 12.1%, 49.7% ± 11.5%, and 19.1% ± 11.9% for the stomach, duodenum, small intestine, and large intestine, respectively, which were comparable with those determined by the conventional in situ single-pass perfusion. By applying the fraction of the dose available at each gastrointestinal segment following the oral administration, the actual fraction absorbed (F’abs) values at each gastrointestinal segment were estimated at 10.9% for the stomach, 27.1% for the duodenum, 40.7% for the small intestine, and 5.4% for the large intestine, which added up to the gastrointestinal bioavailability (FX·FG) of 84.1%. The present method holds great promise to assess the regional absorption of a drug and aid to design new drug formulations.

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

scholarly journals Solvent drag in jejunal absorption of salicylic acid and antipyrine obtained by in situ single-pass perfusion method in rat.

1984 ◽  
Vol 7 (4) ◽  
pp. 246-253 ◽  
Author(s):  
TOYOTO HIRASAWA ◽  
TOSHIKO MURAOKA ◽  
AKIRA KARINO ◽  
MASAHIRO HAYASHI ◽  
SHOJI AWAZU
Keyword(s):  
Salicylic Acid ◽  
Solvent Drag ◽  
Jejunal Absorption ◽  
Single Pass ◽  
Perfusion Method ◽  
Pass Perfusion
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