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Human in Vivo Regional Intestinal Permeability: Importance for Pharmaceutical Drug Development
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacy.
2014 (English)In: Molecular Pharmaceutics, ISSN 1543-8384, Vol. 11, no 1, 12-23 p.Article, review/survey (Refereed) Published
Abstract [en]

Both the development and regulation of pharmaceutical dosage forms have undergone significant improvements and development over the past 25 years, due primarily to the extensive application of the biopharmaceutical classification system (BCS). The Biopharmaceutics Drug Disposition Classification System, which was published in 2005, has also been a useful resource for predicting the influence of transporters in several pharmacokinetic processes. However, there remains a need for the pharmaceutical industry to develop reliable in vitro/in vivo correlations and in silica methods for predicting the rate and extent of complex gastrointestinal (GI) absorption, the bioavailability, and the plasma concentration time curves for orally administered drug products. Accordingly, a more rational approach is required, one in which high quality in vitro or in silico characterizations of active pharmaceutical ingredients and formulations are integrated into physiologically based in silica biopharmaceutics models to capture the full complexity of GI drug absorption. The need for better understanding of the in vivo GI process has recently become evident after an unsuccessful attempt to predict the GI absorption of BCS class II and IV drugs. Reliable data on the in vivo permeability of the human intestine (P-eff) from various intestinal regions is recognized as one of the key biopharmaceutical requirements when developing in silico GI biopharmaceutics Models with improved predictive accuracy. The P-eff values for human jejunum and ileum, based on historical open, single-pass, perfusion studies are presented in this review. The main objective of this review is to summarize and discuss the relevance and current status of these human in vivo regional intestinal permeability values.

Place, publisher, year, edition, pages
2014. Vol. 11, no 1, 12-23 p.
Keyword [en]
human intestinal permeability, drug absorption, bioavailability, Biopharmaceutics Classification System, Biopharmaceutics Drug Disposition Classification System, intestinal transporters, pharmacokinetics, intestinal perfusion
National Category
Medical and Health Sciences
URN: urn:nbn:se:uu:diva-218523DOI: 10.1021/mp4003392ISI: 000329529700002OAI: oai:DiVA.org:uu-218523DiVA: diva2:696410
Available from: 2014-02-13 Created: 2014-02-12 Last updated: 2014-02-13Bibliographically approved

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Lennernäs, Hans
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