Human intestinal permeability

Journal of Pharmaceutical Sciences
Hans Lennernäs

Abstract

This review focuses on permeability measurements in humans, briefly discussing different perfusion techniques, the relevance of human Peff values, and various aspects of in vivo transport mechanisms. In addition, human Peff values are compared with corresponding data from three preclinical transport models. The regional human jejunal perfusion technique has been validated in several important ways. One of the most important findings is that there is a good correlation between the measured human effective permeability values and the extent of absorption of drugs in humans determined by pharmacokinetic studies. Estimations of the absorption half-lives from the measured Peff agree very well with the time to maximal amount of the dose absorbed achieved after an oral dose in humans. We have also shown that it is possible to determine the Peff for carrier-mediated transported compounds and to classify them according to the proposed biopharmaceutical classification system (BCS). Furthermore, human in vivo permeabilities can be predicted using preclinical permeability models, such as in situ perfusion of rat jejunum, the Caco-2 model, and excised intestinal segments in the Ussing chamber. The permeability of passively transported compo...Continue Reading

References

Jan 1, 1976·Clinical Pharmacokinetics·G Johnsson, C G Regàrdh
Aug 1, 1978·The American Journal of Digestive Diseases·R ModiglianiJ J Bernier
Oct 1, 1992·Pharmaceutical Research·H LennernäsL K Paalzow
Apr 1, 1990·Gastroenterology·L KnutsonR Hällgren
Nov 1, 1990·The Journal of Clinical Investigation·M D LevittD G Levitt
May 10, 1990·The New England Journal of Medicine·O AhrenstedtR Hällgren
Feb 1, 1989·The Journal of Membrane Biology·D W Deamer, J W Nichols
Jan 1, 1989·British Journal of Clinical Pharmacology·L BorgströmJ Paulson
Mar 1, 1988·The American Journal of Physiology·S E AndersonP M Cala
Jan 1, 1987·The Journal of Membrane Biology·J L Madara, J R Pappenheimer
Jan 1, 1986·Digestive Diseases·I BjarnasonA J Levi
Aug 1, 1971·The Journal of Clinical Investigation·H S MekjianA F Hofmann
Dec 1, 1984·The Journal of Clinical Investigation·M D LevittD G Levitt
Jun 1, 1984·Canadian Journal of Physiology and Pharmacology·A B Thomson
Dec 1, 1980·Journal of Pharmaceutical Sciences·G L AmidonE N Lightfoot
Oct 1, 1995·Gastroenterology·R M SchwartzM D Levitt
Jul 13, 1995·Nature·J M Diamond
Mar 1, 1995·Pharmaceutical Research·H LennernäsR Hällgren
May 1, 1995·Gastroenterology·I BjarnasonD Hollander
Jun 1, 1995·The Journal of Clinical Investigation·M R Uhing, R E Kimura
Jan 1, 1994·European Journal of Clinical Pharmacology·T GramattéU Klotz
Aug 1, 1994·The American Journal of Physiology·M B LandeM L Zeidel
Jan 1, 1993·European Journal of Clinical Pharmacology·G M PacificiL Giuliani
Apr 1, 1994·Digestive Diseases and Sciences·P KrugliakT Y Ma

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Citations

Apr 4, 2006·Journal of Molecular Modeling·Govindan Subramanian, Douglas B Kitchen
Dec 6, 2006·Investigational New Drugs·Amit KokateBhaskara Jasti
Jan 15, 2005·Pharmaceutical Research·Jennifer M Carrozzino, Morteza G Khaledi
Feb 23, 2008·Pharmaceutical Research·Mark LakeramBen Forbes
Mar 5, 2004·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Marival BermejoVirginia Merino
Mar 22, 2005·International Journal of Pharmaceutics·Kouki ObataYosinori Aso
Jul 20, 2002·European Journal of Medicinal Chemistry·Michael H AbrahamIan Cooper
Apr 25, 2003·International Journal of Pharmaceutics·Kiyohiko SuganoYoshinori Aso
Mar 7, 2001·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·T OsterbergP Lundahl
Mar 30, 2002·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·H LennernäsG L Amidon
Jan 7, 2004·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Pascale AnderleWolfgang Sadée
Feb 19, 2000·Current Opinion in Biotechnology·J F Blake
Mar 29, 2001·Journal of Pharmacological and Toxicological Methods·P V BalimaneR A Morrison
Oct 26, 2001·Drug Discovery Today·Robert A. ColemanAnthony M. Brown
Dec 4, 2003·Drug Discovery Today·Kuresh A YoudimN Joan Abbott
May 14, 1999·Pharmaceutical Science & Technology Today·A L Daugherty, R J Mrsny
Apr 25, 2012·Molecular Pharmaceutics·Arik DahanGordon L Amidon
Jul 31, 2010·Nature Reviews. Drug Discovery·Kiyohiko SuganoFrank Senner
Jun 27, 2013·BMC Pharmacology & Toxicology·David G Levitt
May 2, 2012·The AAPS Journal·J-M Cardot, B M Davit
Aug 19, 2007·Expert Opinion on Drug Metabolism & Toxicology·Aristides DokoumetzidisNikoletta Fotaki
Sep 12, 2008·Clinical Pharmacokinetics·Jennifer B DressmanEkarat Jantratid
Jun 30, 2005·BioDrugs : Clinical Immunotherapeutics, Biopharmaceuticals and Gene Therapy·Josias H HammanAwie F Kotzé
Aug 28, 2012·Indian Journal of Pharmaceutical Sciences·B BoonyapiwatG B Steventon
Apr 8, 2006·Biomedical Papers of the Medical Faculty of the University Palacký, Olomouc, Czechoslovakia·Martin KunesJirí Bajgar
Dec 19, 2013·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Sara CarlertBertil Abrahamsson
Jul 9, 2013·Journal of Pharmacological and Toxicological Methods·Zhiqiang LuoLi Wei

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