Format

Send to

Choose Destination
J Pharm Pharmacol. 2019 Apr;71(4):557-580. doi: 10.1111/jphp.12999. Epub 2018 Sep 11.

The impact of food intake on the luminal environment and performance of oral drug products with a view to in vitro and in silico simulations: a PEARRL review.

Author information

1
Department of Pharmacy, National and Kapodistrian University of Athens, Athens, Greece.
2
Drug Product Design, Pfizer PGRD, Sandwich, Kent, UK.
3
Institute of Pharmaceutical Technology, Goethe University, Frankfurt/Main, Germany.

Abstract

OBJECTIVES:

Using the type of meal and dosing conditions suggested by regulatory agencies as a basis, this review has two specific objectives: first, to summarize our understanding on the impact of food intake on luminal environment and drug product performance and second, to summarize the usefulness and limitations of available in vitro and in silico methodologies for the evaluation of drug product performance after food intake.

KEY FINDINGS:

Characterization of the luminal environment and studies evaluating product performance in the lumen, under conditions suggested by regulatory agencies for simulating the fed state, are limited. Various in vitro methodologies have been proposed for evaluating drug product performance in the fed state, but systematic validation is lacking. Physiologically based pharmacokinetic (PBPK) modelling approaches require the use of in vitro biorelevant data and, to date, have been used primarily for investigating the mechanisms via which an already observed food effect is mediated.

SUMMARY:

Better understanding of the impact of changes induced by the meal administration conditions suggested by regulatory agencies on the luminal fate of the drug product is needed. Relevant information will be useful for optimizing the in vitro test methods and increasing the usefulness of PBPK modelling methodologies.

KEYWORDS:

fed state; in silico modelling; in vitro simulation; luminal environment; oral drug absorption

PMID:
30203429
DOI:
10.1111/jphp.12999
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Wiley
Loading ...
Support Center