Formulation predictive dissolution (fPD) testing to advance oral drug product development: an introduction to the US FDA funded ‘21st Century BA/BE’ project

Over the past decade, formulation predictive dissolution (fPD) testing has gained increasing attention. Another mindset is pushed forward where scientists in our field are more confident to explore the in vivo behavior of an oral drug product by performing predictive in vitro dissolution studies. Si...

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Main Authors: Hens, Bart, Sinko, Patrick, Job, Nicholas, Dean, Meagan, Al-Gousous, Jozef, Salehi, Niloufar, Ziff, Robert M., Tsume, Yasuhiro, Bermejo, Marival, Paixao, Paulo, Brasseur, James G., Yu, Alex, Talattof, Arjang, Benninghoff, Gail, Langguth, Peter, Lennernas, Hans, Hasler, William L., Marciani, Luca, Dickens, Joseph, Shedden, Kerby, Sun, Duxin, Amidon, Gregory E., Amidon, Gordon L.
Format: Article
Published: Elsevier 2018
Subjects:
Online Access:https://eprints.nottingham.ac.uk/52793/
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author Hens, Bart
Sinko, Patrick
Job, Nicholas
Dean, Meagan
Al-Gousous, Jozef
Salehi, Niloufar
Ziff, Robert M.
Tsume, Yasuhiro
Bermejo, Marival
Paixao, Paulo
Brasseur, James G.
Yu, Alex
Talattof, Arjang
Benninghoff, Gail
Langguth, Peter
Lennernas, Hans
Hasler, William L.
Marciani, Luca
Dickens, Joseph
Shedden, Kerby
Sun, Duxin
Amidon, Gregory E.
Amidon, Gordon L.
author_facet Hens, Bart
Sinko, Patrick
Job, Nicholas
Dean, Meagan
Al-Gousous, Jozef
Salehi, Niloufar
Ziff, Robert M.
Tsume, Yasuhiro
Bermejo, Marival
Paixao, Paulo
Brasseur, James G.
Yu, Alex
Talattof, Arjang
Benninghoff, Gail
Langguth, Peter
Lennernas, Hans
Hasler, William L.
Marciani, Luca
Dickens, Joseph
Shedden, Kerby
Sun, Duxin
Amidon, Gregory E.
Amidon, Gordon L.
author_sort Hens, Bart
building Nottingham Research Data Repository
collection Online Access
description Over the past decade, formulation predictive dissolution (fPD) testing has gained increasing attention. Another mindset is pushed forward where scientists in our field are more confident to explore the in vivo behavior of an oral drug product by performing predictive in vitro dissolution studies. Similarly, there is an increasing interest in the application of modern computational fluid dynamics (CFD) frameworks and high-performance computing platforms to study the local processes underlying absorption within the gastrointestinal (GI) tract. In that way, CFD and computing platforms both can inform future PBPK-based in silico frameworks and determine the GI-motility-driven hydrodynamic impacts that should be incorporated into in vitro dissolution methods for in vivo relevance. Current compendial dissolution methods are not always reliable to predict the in vivo behavior, especially not for biopharmaceutics classification system (BCS) class 2/4 compounds suffering from a low aqueous solubility. Developing a predictive dissolution test will be more reliable, cost-effective and less time-consuming as long as the predictive power of the test is sufficiently strong. There is a need to develop a biorelevant, predictive dissolution method that can be applied by pharmaceutical drug companies to facilitate marketing access for generic and novel drug products. In 2014, Prof. Gordon L. Amidon and his team initiated a far-ranging research program designed to integrate (1) in vivo studies in humans in order to further improve the understanding of the intraluminal processing of oral dosage forms and dissolved drug along the gastrointestinal (GI) tract, (2) advancement of in vitro methodologies that incorporates higher levels of in vivo relevance and (3) computational experiments to study the local processes underlying dissolution, transport and absorption within the intestines performed with a new unique CFD based framework. Of particular importance is revealing the physiological variables determining the variability in in vivo dissolution and GI absorption from person to person in order to address (potential) in vivo BE failures. This paper provides an introduction to this multidisciplinary project, informs the reader about current achievements and outlines future directions.
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spelling nottingham-527932020-05-04T19:49:06Z https://eprints.nottingham.ac.uk/52793/ Formulation predictive dissolution (fPD) testing to advance oral drug product development: an introduction to the US FDA funded ‘21st Century BA/BE’ project Hens, Bart Sinko, Patrick Job, Nicholas Dean, Meagan Al-Gousous, Jozef Salehi, Niloufar Ziff, Robert M. Tsume, Yasuhiro Bermejo, Marival Paixao, Paulo Brasseur, James G. Yu, Alex Talattof, Arjang Benninghoff, Gail Langguth, Peter Lennernas, Hans Hasler, William L. Marciani, Luca Dickens, Joseph Shedden, Kerby Sun, Duxin Amidon, Gregory E. Amidon, Gordon L. Over the past decade, formulation predictive dissolution (fPD) testing has gained increasing attention. Another mindset is pushed forward where scientists in our field are more confident to explore the in vivo behavior of an oral drug product by performing predictive in vitro dissolution studies. Similarly, there is an increasing interest in the application of modern computational fluid dynamics (CFD) frameworks and high-performance computing platforms to study the local processes underlying absorption within the gastrointestinal (GI) tract. In that way, CFD and computing platforms both can inform future PBPK-based in silico frameworks and determine the GI-motility-driven hydrodynamic impacts that should be incorporated into in vitro dissolution methods for in vivo relevance. Current compendial dissolution methods are not always reliable to predict the in vivo behavior, especially not for biopharmaceutics classification system (BCS) class 2/4 compounds suffering from a low aqueous solubility. Developing a predictive dissolution test will be more reliable, cost-effective and less time-consuming as long as the predictive power of the test is sufficiently strong. There is a need to develop a biorelevant, predictive dissolution method that can be applied by pharmaceutical drug companies to facilitate marketing access for generic and novel drug products. In 2014, Prof. Gordon L. Amidon and his team initiated a far-ranging research program designed to integrate (1) in vivo studies in humans in order to further improve the understanding of the intraluminal processing of oral dosage forms and dissolved drug along the gastrointestinal (GI) tract, (2) advancement of in vitro methodologies that incorporates higher levels of in vivo relevance and (3) computational experiments to study the local processes underlying dissolution, transport and absorption within the intestines performed with a new unique CFD based framework. Of particular importance is revealing the physiological variables determining the variability in in vivo dissolution and GI absorption from person to person in order to address (potential) in vivo BE failures. This paper provides an introduction to this multidisciplinary project, informs the reader about current achievements and outlines future directions. Elsevier 2018-09-05 Article PeerReviewed Hens, Bart, Sinko, Patrick, Job, Nicholas, Dean, Meagan, Al-Gousous, Jozef, Salehi, Niloufar, Ziff, Robert M., Tsume, Yasuhiro, Bermejo, Marival, Paixao, Paulo, Brasseur, James G., Yu, Alex, Talattof, Arjang, Benninghoff, Gail, Langguth, Peter, Lennernas, Hans, Hasler, William L., Marciani, Luca, Dickens, Joseph, Shedden, Kerby, Sun, Duxin, Amidon, Gregory E. and Amidon, Gordon L. (2018) Formulation predictive dissolution (fPD) testing to advance oral drug product development: an introduction to the US FDA funded ‘21st Century BA/BE’ project. International Journal of Pharmaceutics, 548 (1). pp. 120-127. ISSN 0378-5173 In vivo dissolution ; Bioequivalence ; Bioavailability ; Oral absorption ; MRI ; Manometry ; Computational fluid dynamics https://www.sciencedirect.com/science/article/pii/S0378517318304496 doi:10.1016/j.ijpharm.2018.06.050 doi:10.1016/j.ijpharm.2018.06.050
spellingShingle In vivo dissolution ; Bioequivalence ; Bioavailability ; Oral absorption ; MRI ; Manometry ; Computational fluid dynamics
Hens, Bart
Sinko, Patrick
Job, Nicholas
Dean, Meagan
Al-Gousous, Jozef
Salehi, Niloufar
Ziff, Robert M.
Tsume, Yasuhiro
Bermejo, Marival
Paixao, Paulo
Brasseur, James G.
Yu, Alex
Talattof, Arjang
Benninghoff, Gail
Langguth, Peter
Lennernas, Hans
Hasler, William L.
Marciani, Luca
Dickens, Joseph
Shedden, Kerby
Sun, Duxin
Amidon, Gregory E.
Amidon, Gordon L.
Formulation predictive dissolution (fPD) testing to advance oral drug product development: an introduction to the US FDA funded ‘21st Century BA/BE’ project
title Formulation predictive dissolution (fPD) testing to advance oral drug product development: an introduction to the US FDA funded ‘21st Century BA/BE’ project
title_full Formulation predictive dissolution (fPD) testing to advance oral drug product development: an introduction to the US FDA funded ‘21st Century BA/BE’ project
title_fullStr Formulation predictive dissolution (fPD) testing to advance oral drug product development: an introduction to the US FDA funded ‘21st Century BA/BE’ project
title_full_unstemmed Formulation predictive dissolution (fPD) testing to advance oral drug product development: an introduction to the US FDA funded ‘21st Century BA/BE’ project
title_short Formulation predictive dissolution (fPD) testing to advance oral drug product development: an introduction to the US FDA funded ‘21st Century BA/BE’ project
title_sort formulation predictive dissolution (fpd) testing to advance oral drug product development: an introduction to the us fda funded ‘21st century ba/be’ project
topic In vivo dissolution ; Bioequivalence ; Bioavailability ; Oral absorption ; MRI ; Manometry ; Computational fluid dynamics
url https://eprints.nottingham.ac.uk/52793/
https://eprints.nottingham.ac.uk/52793/
https://eprints.nottingham.ac.uk/52793/