Caco-2 monolayers in experimental and theoretical predictions of drug transport

P Artursson, K Palm, K Luthman - Advanced drug delivery reviews, 2001 - Elsevier
This review examines the use of Caco-2 monolayers in the prediction of intestinal drug
absorption. First, the different routes of drug transport in Caco-2 monolayers are compared …

Pharmacokinetic interactions with rifampicin: clinical relevance

M Niemi, JT Backman, MF Fromm, PJ Neuvonen… - Clinical …, 2003 - Springer
The antituberculosis drug rifampicin (rifampin) induces a number of drug-metabolising
enzymes, having the greatest effects on the expression of cytochrome P450 (CYP) 3A4 in …

Polymorphisms in Human MDR1 (P‐glycoprotein): Recent Advances and Clinical Relevance

C Marzolini, E Paus, T Buclin… - Clinical Pharmacology & …, 2004 - Wiley Online Library
Drug transporters are increasingly recognized to be important to drug disposition and
response. P‐glycoprotein, the encoded product of the human MDR1 (ABCB1) gene, is of …

Property-based design: optimization of drug absorption and pharmacokinetics

H Van De Waterbeemd, DA Smith… - Journal of medicinal …, 2001 - ACS Publications
Drugs may be administered via different routes, the oral route generally being the preferred
for reasons of ease and compliance by the patient. Absorption via these routes will take …

High-Throughput Permeability pH Profile and High-Throughput Alkane/Water log P with Artificial Membranes

F Wohnsland, B Faller - Journal of medicinal chemistry, 2001 - ACS Publications
This study reports on a novel, high-throughput assay, designed to predict passive,
transcellular permeability in early drug discovery. The assay is carried out in 96-well …

The ABCs of drug transport in intestine and liver: efflux proteins limiting drug absorption and bioavailability

LMS Chan, S Lowes, BH Hirst - European journal of pharmaceutical …, 2004 - Elsevier
Many orally administered drugs must overcome several barriers before reaching their target
site. The first major obstacle to cross is the intestinal epithelium. Although lipophilic …

Human intestinal permeability

H Lennernaäs - Journal of pharmaceutical sciences, 1998 - Elsevier
Abstract□ This review focuses on permeability measurements in humans, briefly discussing
different perfusion techniques, the relevance of human P eff values, and various aspects of …

Estimation of permeability by passive diffusion through Caco-2 cell monolayers using the drugs' lipophilicity and molecular weight

G Camenisch, J Alsenz, H van de Waterbeemd… - European journal of …, 1998 - Elsevier
A recently developed, new theoretical absorption model for passive diffusion through
biological membranes describing the dependency of membrane permeability on lipophilicity …

Impact of excipients on the absorption of P-glycoprotein substrates in vitro and in vivo

G Cornaire, J Woodley, P Hermann, A Cloarec… - International journal of …, 2004 - Elsevier
The efflux transporter, P-glycoprotein (P-gp), located in the apical membranes of intestinal
absorptive cells, can reduce the bioavailability of a wide range of orally administered drugs …

Is the role of the small intestine in first-pass metabolism overemphasized?

JH Lin, M Chiba, TA Baillie - Pharmacological reviews, 1999 - ASPET
The primary function of the small intestine is to absorb nutrients and water. This is achieved
by mixing food with digestive enzymes to increase the contact of foodstuffs with the …