Early pharmaceutical profiling to predict oral drug absorption: current status and unmet needs

Research output: Contribution to journalJournal articleResearchpeer-review

Standard

Early pharmaceutical profiling to predict oral drug absorption : current status and unmet needs. / Bergström, Christel A S; Holm, René; Jørgensen, Søren Astrup; Andersson, Sara B E; Artursson, Per; Beato, Stefania; Borde, Anders; Box, Karl; Brewster, Marcus; Dressman, Jennifer; Feng, Kung-I; Halbert, Gavin; Kostewicz, Edmund; McAllister, Mark; Muenster, Uwe; Thinnes, Julian; Taylor, Robert; Mullertz, Anette.

In: European Journal of Pharmaceutical Sciences, Vol. 57, 16.06.2014, p. 173-99.

Research output: Contribution to journalJournal articleResearchpeer-review

Harvard

Bergström, CAS, Holm, R, Jørgensen, SA, Andersson, SBE, Artursson, P, Beato, S, Borde, A, Box, K, Brewster, M, Dressman, J, Feng, K-I, Halbert, G, Kostewicz, E, McAllister, M, Muenster, U, Thinnes, J, Taylor, R & Mullertz, A 2014, 'Early pharmaceutical profiling to predict oral drug absorption: current status and unmet needs', European Journal of Pharmaceutical Sciences, vol. 57, pp. 173-99. https://doi.org/10.1016/j.ejps.2013.10.015

APA

Bergström, C. A. S., Holm, R., Jørgensen, S. A., Andersson, S. B. E., Artursson, P., Beato, S., ... Mullertz, A. (2014). Early pharmaceutical profiling to predict oral drug absorption: current status and unmet needs. European Journal of Pharmaceutical Sciences, 57, 173-99. https://doi.org/10.1016/j.ejps.2013.10.015

Vancouver

Bergström CAS, Holm R, Jørgensen SA, Andersson SBE, Artursson P, Beato S et al. Early pharmaceutical profiling to predict oral drug absorption: current status and unmet needs. European Journal of Pharmaceutical Sciences. 2014 Jun 16;57:173-99. https://doi.org/10.1016/j.ejps.2013.10.015

Author

Bergström, Christel A S ; Holm, René ; Jørgensen, Søren Astrup ; Andersson, Sara B E ; Artursson, Per ; Beato, Stefania ; Borde, Anders ; Box, Karl ; Brewster, Marcus ; Dressman, Jennifer ; Feng, Kung-I ; Halbert, Gavin ; Kostewicz, Edmund ; McAllister, Mark ; Muenster, Uwe ; Thinnes, Julian ; Taylor, Robert ; Mullertz, Anette. / Early pharmaceutical profiling to predict oral drug absorption : current status and unmet needs. In: European Journal of Pharmaceutical Sciences. 2014 ; Vol. 57. pp. 173-99.

Bibtex

@article{111aa6ef9a2b49b888c07a4f44eb763b,
title = "Early pharmaceutical profiling to predict oral drug absorption: current status and unmet needs",
abstract = "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 silico 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.",
author = "Bergstr{\"o}m, {Christel A S} and Ren{\'e} Holm and J{\o}rgensen, {S{\o}ren Astrup} and Andersson, {Sara B E} and Per Artursson and Stefania Beato and Anders Borde and Karl Box and Marcus Brewster and Jennifer Dressman and Kung-I Feng and Gavin Halbert and Edmund Kostewicz and Mark McAllister and Uwe Muenster and Julian Thinnes and Robert Taylor and Anette Mullertz",
note = "Copyright {\circledC} 2013 Elsevier B.V. All rights reserved.",
year = "2014",
month = "6",
day = "16",
doi = "10.1016/j.ejps.2013.10.015",
language = "English",
volume = "57",
pages = "173--99",
journal = "European Journal of Pharmaceutical Sciences",
issn = "0928-0987",
publisher = "Elsevier",

}

RIS

TY - JOUR

T1 - Early pharmaceutical profiling to predict oral drug absorption

T2 - current status and unmet needs

AU - Bergström, Christel A S

AU - Holm, René

AU - Jørgensen, Søren Astrup

AU - Andersson, Sara B E

AU - Artursson, Per

AU - Beato, Stefania

AU - Borde, Anders

AU - Box, Karl

AU - Brewster, Marcus

AU - Dressman, Jennifer

AU - Feng, Kung-I

AU - Halbert, Gavin

AU - Kostewicz, Edmund

AU - McAllister, Mark

AU - Muenster, Uwe

AU - Thinnes, Julian

AU - Taylor, Robert

AU - Mullertz, Anette

N1 - Copyright © 2013 Elsevier B.V. All rights reserved.

PY - 2014/6/16

Y1 - 2014/6/16

N2 - 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 silico 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.

AB - 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 silico 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.

U2 - 10.1016/j.ejps.2013.10.015

DO - 10.1016/j.ejps.2013.10.015

M3 - Journal article

C2 - 24215735

VL - 57

SP - 173

EP - 199

JO - European Journal of Pharmaceutical Sciences

JF - European Journal of Pharmaceutical Sciences

SN - 0928-0987

ER -

ID: 117195749