scholarly journals Intestinal absorption, metabolism, and excretion of (–)-epicatechin in healthy humans assessed by using an intestinal perfusion technique

2013 ◽  
Vol 98 (4) ◽  
pp. 924-933 ◽  
Author(s):  
Lucas Actis-Goretta ◽  
Antoine Lévèques ◽  
Maarit Rein ◽  
Alexander Teml ◽  
Christian Schäfer ◽  
...  
Keyword(s):  
Intestinal Absorption ◽  
Intestinal Perfusion ◽  
Perfusion Technique ◽  
Healthy Humans

scholarly journals Reply to “Comment on López-Yerena et al. ‘Absorption and Intestinal Metabolic Profile of Oleocanthal in Rats’ Pharmaceutics 2020, 12, 134”

Pharmaceutics ◽  
2020 ◽  
Vol 12 (12) ◽  
pp. 1221
Author(s):  
Anallely López-Yerena ◽  
Anna Vallverdú-Queralt ◽  
Raf Mols ◽  
Patrick Augustijns ◽  
Rosa M. Lamuela-Raventós ◽  
...  
Keyword(s):  
Intestinal Absorption ◽  
Metabolic Profile ◽  
Scientific Community ◽  
Intestinal Perfusion ◽  
Perfusion Technique ◽  
Specific Data ◽  
Single Pass ◽  
Published Paper

Recently, in February 2020, we published a study exploring the intestinal absorption and metabolism of oleocanthal (OLC) in rats. A single-pass intestinal perfusion technique (SPIP) was used, involving simultaneous sampling from the luminal perfusate and mesenteric blood. Later, comments on our published paper were released, requesting clarification of specific data. In this detailed reply, we hope to have addressed and clarified all the concerns of A. Kaddoumi and K. El Sayed and that the scientific community will benefit from both the study and the comments it has generated.

Intestinal Absorption of Cystine and Cysteine in Normal Human Subjects and Patients with Cystinuria

1974 ◽  
Vol 47 (4) ◽  
pp. 393-397 ◽  
Author(s):  
D. B. A. Silk ◽  
D. Perrett ◽  
A. D. Stephens ◽  
M. L. Clark ◽  
E. F. Scowen
Keyword(s):  
Intestinal Absorption ◽  
Human Subjects ◽  
Transport Processes ◽  
Intestinal Perfusion ◽  
Perfusion Technique ◽  
Normal Human

1. An intestinal perfusion technique has been used to study absorption in vivo of l-cystine and l-cysteine in six normal human subjects and three patients with homozygous cystinuria. 2. No significant absorption of l-cystine was detected during perfusion of the cystinuric patients, whereas l-cysteine absorption was normal. These results imply that l-cystine and l-cysteine are normally absorbed by different transport processes. 3. No significant reduction of l-cystine to l-cysteine occurred in the gut lumen during the perfusion experiments. No more oxidation of l-cysteine to l-cystine occurred in the gut lumen during the perfusion experiments than in the test solutions which were simultaneously incubated in vitro.

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.

The Intestinal Absorption of a Prodrug of the mGlu2/3 Receptor Agonist LY354740 is Mediated by PEPT1: In Situ Rat Intestinal Perfusion Studies

2010 ◽  
Vol 99 (3) ◽  
pp. 1574-1581 ◽  
Author(s):  
André H. Eriksson ◽  
Manthena V.S. Varma ◽  
Everett J. Perkins ◽  
Cheryl L. Zimmerman
Keyword(s):  
Intestinal Absorption ◽  
Receptor Agonist ◽  
Intestinal Perfusion ◽  
Perfusion Studies

scholarly journals INFLUENCE OF P-GLYCOPROTEIN AND CYTOCHROME ISOENZYME-P3A4 ON BIOAVAILABILITY OF ANTICANCER DRUGS WITH CURCUMIN BY IN SITU INTESTINAL PERFUSION IN MALE WISTAR RATS

2019 ◽  
pp. 184-187
Author(s):  
MANOJ KANNA NALLA ◽  
SHANKARAIAH PULIGILLA
Keyword(s):  
Venous Blood ◽  
Hepatic Metabolism ◽  
Intestinal Perfusion ◽  
Hepatic Veins ◽  
Perfusion Technique ◽  
Flow Rates ◽  
P Glycoprotein ◽  
Drug Concentrations ◽  
In Situ Intestinal Perfusion

Objectives: An orally administered anticancer drug has been poor drug absorption; drug resistance and metabolism, which alters the bioavailability of drugs. An in situ intestine perfusion technique is developing under the different perfusion rates in the presence of drug inducers and inhibitors of cytochrome isoenzyme-P (CYP)-3A4 and P-glycoprotein (P-gp) for drug concentrations. Materials and Methods: The modified in situ intestinal perfusion technique was developed and followed to obtain the portal and hepatic venous blood samples paralleled at different perfusion time and flow rates of 0.05, 0.1, 0.5, and 1.0 mL/min using the imatinib (1 mg/mL) drug alone and in the presence of drug inducer and drug inhibitor for the period of 3 h. The imatinib drug concentrations were assayed using high-pressure liquid chromatography. Results: The results reveal that the mean imatinib drug concentrations in portal vein were higher than hepatic vein at various perfusion flow rates and time intervals were observed. The area under curve and plasma drug concentrations maximum of imatinib alone absorptions were significantly different between portal and hepatic veins (p<0.05) at the flow rates of 0.5 and 1.0 mL/min and also in the presence of drug inducer and inhibitors that indicating for the considerable hepatic involvement in the presystemic extraction or metabolism of drugs. Conclusions: The in situ perfusions approach could provide the useful tool for improving the basic understanding of absorption kinetics and hepatic metabolism of drugs in the presence of drug inducers and drug inhibitors (CYP3A4 and P-gp) under the development and facilitating the clinical applications.

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