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Early pharmaceutica...
Early pharmaceutical profiling to predict oral drug absorption : Current status and unmet needs
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- Bergström, Christel A. S. (author)
- Uppsala universitet,Institutionen för farmaci
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Holm, Rene (author)
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Jorgensen, Soren Astrup (author)
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- Andersson, Sara B. E. (author)
- Uppsala universitet,Institutionen för farmaci
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- Artursson, Per (author)
- Uppsala universitet,Institutionen för farmaci
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Beato, Stefania (author)
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Borde, Anders (author)
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Box, Karl (author)
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Brewster, Marcus (author)
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Dressman, Jennifer (author)
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Feng, Kung-I. (author)
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Halbert, Gavin (author)
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Kostewicz, Edmund (author)
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McAllister, Mark (author)
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Muenster, Uwe (author)
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Thinnes, Julian (author)
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Taylor, Robert (author)
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Mullertz, Anette (author)
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(creator_code:org_t)
- Elsevier BV, 2014
- 2014
- English.
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In: European Journal of Pharmaceutical Sciences. - : Elsevier BV. - 0928-0987 .- 1879-0720. ; 57, s. 173-199
- Related links:
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Subject headings
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- Preformulation measurements are used to estimate the fraction absorbed in vivo for orally administered compounds and thereby allow an early evaluation of the need for enabling formulations. As part of the Oral Biopharmaceutical Tools (OrBiTo) project, this review provides a summary of the pharmaceutical profiling methods available, with focus on in silica and in vitro models typically used to forecast active pharmaceutical ingredient's (APIs) in vivo performance after oral administration. An overview of the composition of human, animal and simulated gastrointestinal (GI) fluids is provided and state-of-the art methodologies to study API properties impacting on oral absorption are reviewed. Assays performed during early development, i.e. physicochemical characterization, dissolution profiles under physiological conditions, permeability assays and the impact of excipients on these properties are discussed in detail and future demands on pharmaceutical profiling are identified. It is expected that innovative computational and experimental methods that better describe molecular processes involved in vivo during dissolution and absorption of APIs will be developed in the OrBiTo. These methods will provide early insights into successful pathways (medicinal chemistry or formulation strategy) and are anticipated to increase the number of new APIs with good oral absorption being discovered. (C) 2013 Elsevier B.V. All rights reserved.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Farmaceutiska vetenskaper (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Pharmaceutical Sciences (hsv//eng)
Keyword
- Preformulation
- Physicochemical properties
- Pharmaceutical profiling
- Biorelevant media
- Intestinal fluid
- Absorption
Publication and Content Type
- ref (subject category)
- art (subject category)
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- By the author/editor
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Bergström, Chris ...
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Holm, Rene
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Jorgensen, Soren ...
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Andersson, Sara ...
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Artursson, Per
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Beato, Stefania
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show more...
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Borde, Anders
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Box, Karl
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Brewster, Marcus
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Dressman, Jennif ...
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Feng, Kung-I.
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Halbert, Gavin
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Kostewicz, Edmun ...
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McAllister, Mark
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Muenster, Uwe
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Thinnes, Julian
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Taylor, Robert
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Mullertz, Anette
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show less...
- About the subject
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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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and Basic Medicine
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and Pharmaceutical S ...
- Articles in the publication
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European Journal ...
- By the university
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Uppsala University