Journal ArticleDOI
Determination of Absorption Characteristics of AG337, a Novel Thymidylate Synthase Inhibitor, Using a Perfused Rat Intestinal Model
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In this paper, the authors determined the intestinal absorption characteristics of AG337, a mechanism-based inhibitor of thymidylate synthase, using a perfused rat intestinal model.About:
This article is published in Journal of Pharmaceutical Sciences.The article was published on 1998-07-01. It has received 32 citations till now. The article focuses on the topics: Intestinal absorption & Hypoxanthine.read more
Citations
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Journal ArticleDOI
Metabolism of Flavonoids via Enteric Recycling: Role of Intestinal Disposition
Jun Chen,Huimin Lin,Ming Hu +2 more
TL;DR: In conclusion, intestinal disposition may be more important than hepatic disposition in the first-pass metabolism of flavonoids such as apigenin and enteric recycling may be used to explain why flavonoid have poor systemic bioavailabilities.
Journal ArticleDOI
Strategies for Absorption Screening in Drug Discovery and Development
Hilde Bohets,Pieter Annaert,Geert Mannens,Ludy van Beijsterveldt,Katelijne Anciaux,Peter Verboven,Willem Meuldermans,K. Lavrijsen +7 more
TL;DR: The everted sac and Ussing chamber techniques are more advanced models in the sense that they can provide additional information with respect to intestinal metabolism and the role of the liver in affecting bioavailability can be evaluated by portal vein sampling experiments in dogs.
Journal ArticleDOI
Nucleobase transporters (review).
H. P. de Koning,George Diallinas +1 more
TL;DR: It is shown that nucleobase transporters and similar sequences of unknown function present in databases constitute three basic families, which will be designated NAT, PRT and PUP, which includes members from archea, eubacteria, fungi, plants and metazoa, and the last one is only found in plants.
Journal ArticleDOI
Poor oral bioavailability of a promising anticancer agent andrographolide is due to extensive metabolism and efflux by P-glycoprotein.
Ling Ye,Tao Wang,Lan Tang,Wei Liu,Zhen Yang,Juan Zhou,Zhijie Zheng,Zheng Cai,Ming Hu,Ming Hu,Zhongqiu Liu +10 more
TL;DR: AP has poor oral bioavailability because of its rapid biotransformation and efflux by P-gp, and how intestinal disposition affects its bioavailability is determined.
Journal ArticleDOI
Disposition of flavonoids via enteric recycling: enzyme-transporter coupling affects metabolism of biochanin A and formononetin and excretion of their phase II conjugates.
TL;DR: Efficiency of enzyme-transporter coupling controls the amounts of metabolites excreted by the intestine and liver and determines the relative contribution of enteric and enterohepatic recycling to the in vivo disposition of isoflavones.
References
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Book ChapterDOI
Permeation of Nucleosides, Nucleic Acid Bases, and Nucleotides in Animal Cells
TL;DR: The chapter discusses the importance of the mechanism of permeation of nucleosides, nucleobases, and nucleotides through the cell membranes of eukaryotes and discusses the carrier model for facilitated diffusion and tests for its applicability to nucleoside and base transport.
Journal ArticleDOI
Intestinal transport of dipeptides in man: relative importance of hydrolysis and intact absorption
TL;DR: It is suggested that dipeptide disappearance in the gut lumen is principally accomplished by intact absorption and not by hydrolysis and there is no appreciable hydrolytic activity against glycylglycine by the membrane-bound enzymes and only a small fraction of glycylleucine is hydrolyzed by these enzymes.
Journal ArticleDOI
Estimating Human Oral Fraction Dose Absorbed: A Correlation Using Rat Intestinal Membrane Permeability for Passive and Carrier-Mediated Compounds
TL;DR: The correlation between fraction dose absorbed in humans and Pw* determined from steady-state perfused rat intestinal segments gives an excellent correlation, indicating that Pw*, is one of the key variables controlling oral drug absorption and that the correlation may be useful for estimating oral drugabsorption in humans regardless of the mechanism of absorption.
Journal ArticleDOI
Active and Passive Bile Acid Absorption in Man. PERFUSION STUDIES OF THE ILEUM AND JEJUNUM
Einar Krag,Sidney F. Phillips +1 more
TL;DR: These results, which are comparable with those from animal experiments, provide a basis for estimation of intestinal reabsorption of bile acids in intact man.
Journal ArticleDOI
Transepithelial glycylsarcosine transport in intestinal Caco-2 cells mediated by expression of H(+)-coupled carriers at both apical and basal membranes.
TL;DR: Direct evidence is provided for dipeptide-stimulated H(+)-influx, across both apical and basolateral membranes, in this intact epithelial cell system, which is consistent with the expression of H( +)-coupled dipeptic transporters at both membrane faces of the human intestinal epithelial Caco-2 cell line.
Related Papers (5)
Metabolism of Flavonoids via Enteric Recycling: Role of Intestinal Disposition
Jun Chen,Huimin Lin,Ming Hu +2 more
Metabolism of Flavonoids via Enteric Recycling: Mechanistic Studies of Disposition of Apigenin in the Caco-2 Cell Culture Model
Ming Hu,June Chen,Huimin Lin +2 more