ArticlePharmaceutical research1999
Transport of pregabalin in rat intestine and Caco-2 monolayers.
Article in Pharmaceutical research, 1999. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
13 citing papers in PubMed, 35 citations in OpenAlex.
- Informing the risk assessment related to lactation and drug exposure: A physiologically based pharmacokinetic lactation model for pregabalin.CPT: pharmacometrics & systems pharmacology · 2024Article
- Solubility-Permeability Interplay in Facilitating the Prediction of Drug Disposition Routes, Extent of Absorption, Food Effects, Brain Penetration and Drug Induced Liver Injury Potential.Journal of pharmaceutical sciences · 2023Review
- Evaluation of an Ussing Chamber System Equipped with Rat Intestinal Tissues to Predict Intestinal Absorption and Metabolism in Humans.European journal of drug metabolism and pharmacokinetics · 2022Article
- Drug Screening, Oral Bioavailability and Regulatory Aspects: A Need for Human Organoids.Pharmaceutics · 2021Review
- Organoids to Study Intestinal Nutrient Transport, Drug Uptake and Metabolism - Update to the Human Model and Expansion of Applications.Frontiers in bioengineering and biotechnology · 2020Article
- Predictive Performance of Physiologically Based Pharmacokinetic and Population Pharmacokinetic Modeling of Renally Cleared Drugs in Children.CPT: pharmacometrics & systems pharmacology · 2016Article
- In vivo and in vitro evaluations of intestinal gabapentin absorption: effect of dose and inhibitors on carrier-mediated transport.Pharmaceutical research · 2015Article
- Drug discovery and regulatory considerations for improving in silico and in vitro predictions that use Caco-2 as a surrogate for human intestinal permeability measurements.The AAPS journal · 2013Article
- Pregabalin for the management of partial epilepsy.Neuropsychiatric disease and treatment · 2008Article
- In vivo effects of glycyl-glutamate and glycyl-sarcosine on gabapentin oral absorption in rat.Pharmaceutical research · 2007Article
- PEPT1 enhances the uptake of gabapentin via trans-stimulation of b0,+ exchange.Pharmaceutical research · 2007Article
- Mucosal uptake of gabapentin (neurontin) vs. pregabalin in the small intestine.Pharmaceutical research · 2001Article
- Drug, meal and formulation interactions influencing drug absorption after oral administration. Clinical implications.Clinical pharmacokinetics · 1999Review
Corrections and comments
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
Abstract
purposeThe purpose of this study was to determine if the intestinal transport of pregabalin (isobutyl gamma-aminobutyric acid, isobutyl GABA), a new anticonvulsant drug, was mediated by amino acid carriers with affinity for large neutral amino acids (LNAA).
methodsPregabalin transport was studied in rat intestine and Caco-2 monolayers. An in vitro Ussing/diffusion chamber model and an in situ single-pass perfusion model were used to study rat intestinal transport. An in vitro diffusion chamber model was used to evaluate Caco-2 transport.
resultsIn rat ileum, pregabalin transport was saturable and inhibited by substrates of intestinal LNAA carriers including neurontin (gabapentin), phenylalanine, and proline. Weak substrates of intestinal LNAA carriers (beta-alanine, gamma-aminobutyric acid, and methyl aminoisobutyric acid) did not significantly change pregabalin transport. In Caco-2 monolayers that showed a high capacity for phenylalanine transport, pregabalin transport was concentration- and direction-independent and equivalent in magnitude to the paracellular marker, mannitol. The in vitro and in situ rat ileal permeabilities of the LNAA carrier-mediated compounds neurontin, pregabalin, and phenylalanine correlated well with the corresponding in vivo human oral absorption.
conclusionsThe transport of pregabalin was mediated by LNAA carriers in rat ileum but not in Caco-2 monolayers. Caco-2 was not an appropriate model for evaluating the in vivo human oral absorption of pregabalin and neurontin.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.