scholarly journals Significance and Regional Dependency of Peptide Transporter (PEPT) 1 in the Intestinal Permeability of Glycylsarcosine: In Situ Single-Pass Perfusion Studies in Wild-Type andPept1Knockout Mice

2010 ◽  
Vol 38 (10) ◽  
pp. 1740-1746 ◽  
Author(s):  
Dilara Jappar ◽  
Shu-Pei Wu ◽  
Yongjun Hu ◽  
David E. Smith
Keyword(s):  
Intestinal Permeability ◽  
Peptide Transporter ◽  
Wild Type ◽  
Single Pass ◽  
Pass Perfusion ◽  
Perfusion Studies

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.

scholarly journals In vitro and in situ effects of atorvastatin and ezetimibe on P-glycoprotein expression and function

2016 ◽  
Vol 11 (4) ◽  
pp. 911
Author(s):  
Mehran Mesgari Abbasi ◽  
Hadi Valizadeh ◽  
Hamed Hamishehkar ◽  
Maryam Bannazadeh Amirkhiz ◽  
Parvin Zakeri-Milani
Keyword(s):  
Intestinal Permeability ◽  
High Performance ◽  
Video Clip ◽  
Permeability Model ◽  
Active Efflux ◽  
Single Pass ◽  
P Glycoprotein ◽  
And Function

<p class="Abstract">P-glycoprotein (P-gp) is a membrane transporter responsible for the active efflux from the cell. Inhibition of the activity may lead to clinically significant drug-drug interactions. This study was performed to investigate the effects of atorvastatin and ezetimibe on the function and expression of P-gp. The <em>in vitro</em> rhodamine-123 (Rho123) efflux assay and Western blot in Caco-2 cells, and the <em>in situ</em> rat single-pass intestinal permeability model followed by high performance liquid chromatography were developed. Rho123 intracellular accumulation in 100 µM of atorvastatin- and ezetimibe-treated cells was significantly higher than that in control cells (p&lt;0.05). P-gp expression was decreased by 100 µM atorvastatin and ezetimibe. Intestinal effective permeability of digoxin in the presence of atorvastatin (3 and 100 µM), ezetimibe (10 and 100 µM) was significantly increased (p&lt;0.05). Both drugs  inhibited P-gp activity in vitro and<em> in situ</em>. Atorvastatin and ezetimibe down-regulated the expression of P-gp <em>in vitro</em>. </p><p class="Abstract"><strong>Video Clip of Methodology</strong>:</p><p class="Abstract"><a href="https://youtube.com/v/BQuz1ER3_NQ">Single-pass intestinal permeability</a>: 17 min 26 sec</p><p> </p>

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

In vivo absorption of water and electrolytes in mouse intestine. Application to villin −/− mice

2002 ◽  
Vol 282 (4) ◽  
pp. G634-G639 ◽  
Author(s):  
Rafika Athman ◽  
Annick Tsocas ◽  
Olivier Presset ◽  
Sylvie Robine ◽  
Claude Rozé ◽  
...  
Keyword(s):  
Wild Type ◽  
Single Pass ◽  
Perfusion Method ◽  
Mixed Genetic Background ◽  
Pass Perfusion ◽  
Mouse Small Intestine ◽  
In Vivo Absorption ◽  
Measured Absorption ◽  
Mouse Intestine

This study was done to establish and validate a single-pass perfusion method for measuring the absorption of water and electrolytes by the mouse small intestine. The method was then used to study intestinal absorption in mice whose villin gene had been invalidated ( v−/−). The single-pass perfusion of the jejunum measures the absorption of water, Cl−, Na+, K+, HCO[Formula: see text], and glucose in anesthetized wild-type and v−/− mice in vivo. We measured absorption under basal and stimulated conditions (carbachol, vasoactive intestinal polypeptide, intralumen PGE2). Basal absorption and stimulated secretions were similar to those previously obtained in rats. There was no difference between wild-type and v−/− mice in animals with mixed genetic background or in pure C57BL6 mice. We conclude that this in vivo perfusion method is suitable for studying the absorption/secretion of electrolytes in the mouse intestine and that a lack of villin does not significantly alter basal and secretagogue-stimulated electrolyte movements across the epithelium of the mouse jejunum in vivo.

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