In vitro methods to assess drug precipitation in the fasted small intestine – a PEARRL review
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Autor:innen
O'Dwyer, Patrick J.
Litou, Chara
Box, Karl, J.
Dressman, Jennifer
Kostewicz, Edmund, S.
Reppas, Christos
Autor:in (Körperschaft)
Publikationsdatum
06/2018
Typ der Arbeit
Studiengang
Sammlung
Typ
01A - Beitrag in wissenschaftlicher Zeitschrift
Herausgeber:innen
Herausgeber:in (Körperschaft)
Betreuer:in
Übergeordnetes Werk
Journal of Pharmacy and Pharmacology
Themenheft
DOI der Originalpublikation
Reihe / Serie
Reihennummer
Jahrgang / Band
71
Ausgabe / Nummer
Seiten / Dauer
Patentnummer
Verlag / Herausgebende Institution
Wiley
Verlagsort / Veranstaltungsort
Auflage
Version
Programmiersprache
Abtretungsempfänger:in
Praxispartner:in/Auftraggeber:in
Zusammenfassung
Objectives
Drug precipitation in vivo poses a significant challenge for the pharmaceutical industry. During the drug development process, the impact of drug supersaturation or precipitation on the in vivo behaviour of drug products is evaluated with in vitro techniques. This review focuses on the small and full scale in vitro methods to assess drug precipitation in the fasted small intestine.
Key findings
Many methods have been developed in an attempt to evaluate drug precipitation in the fasted state, with varying degrees of complexity and scale. In early stages of drug development, when drug quantities are typically limited, small‐scale tests facilitate an early evaluation of the potential precipitation risk in vivo and allow rapid screening of prototype formulations. At later stages of formulation development, full‐scale methods are necessary to predict the behaviour of formulations at clinically relevant doses. Multicompartment models allow the evaluation of drug precipitation after transfer from stomach to the upper small intestine. Optimisation of available biopharmaceutics tools for evaluating precipitation in the fasted small intestine is crucial for accelerating the development of novel breakthrough medicines and reducing the development costs.
Summary
Despite the progress from compendial quality control dissolution methods, further work is required to validate the usefulness of proposed setups and to increase their biorelevance, particularly in simulating the absorption of drug along the intestinal lumen. Coupling results from in vitro testing with physiologically based pharmacokinetic modelling holds significant promise and requires further evaluation.
Schlagwörter
biorelevant, in vitro techniques, oral drug absorption, pecipitation, supersaturation
Fachgebiet (DDC)
Veranstaltung
Startdatum der Ausstellung
Enddatum der Ausstellung
Startdatum der Konferenz
Enddatum der Konferenz
Datum der letzten Prüfung
ISBN
ISSN
0022-3573
2042-7158
2042-7158
Sprache
Englisch
Während FHNW Zugehörigkeit erstellt
Ja
Publikationsstatus
Veröffentlicht
Begutachtung
Peer-Review der ganzen Publikation
Open Access-Status
Lizenz
Zitation
O’DWYER, Patrick J., Chara LITOU, Karl, J. BOX, Jennifer DRESSMAN, Edmund, S. KOSTEWICZ, Martin KUENTZ und Christos REPPAS, 2018. In vitro methods to assess drug precipitation in the fasted small intestine – a PEARRL review. Journal of Pharmacy and Pharmacology. Juni 2018. Bd. 71. DOI 10.1111/jphp.12951. Verfügbar unter: http://hdl.handle.net/11654/27327