On the usefulness of compendial setups and tiny-TIM system in evaluating the in vivo performance of oral drug products with various release profiles in the fasted state: Case example sodium salt of A6197.


Journal

European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V
ISSN: 1873-3441
Titre abrégé: Eur J Pharm Biopharm
Pays: Netherlands
ID NLM: 9109778

Informations de publication

Date de publication:
Apr 2020
Historique:
received: 05 09 2019
revised: 13 01 2020
accepted: 05 02 2020
pubmed: 15 2 2020
medline: 1 12 2020
entrez: 15 2 2020
Statut: ppublish

Résumé

We evaluated the usefulness of quality control dissolution data collected with compendial Apparatus I and II, biorelevant dissolution data collected with compendial apparatus IV, and bioaccessibility data collected with the non-compendial tiny-TIM system in screening modified release formulations during the development of BCS Class I compounds using a Boehringer Ingelheim model experimental compound, A6197. Four products were investigated: an immediate release tablet, an extended release tablet, modified release mini-tablets, and extended release pellets. Data with modified release products collected with the compendial apparatus were evaluated vs. the average intraluminal dissolution estimated after deconvoluting clinical data collected in healthy adults. Data collected with the tiny-TIM system were evaluated vs. the average AUC and C

Identifiants

pubmed: 32057905
pii: S0939-6411(20)30036-9
doi: 10.1016/j.ejpb.2020.02.003
pii:
doi:

Substances chimiques

Delayed-Action Preparations 0
Pharmaceutical Preparations 0
Tablets 0
Sodium 9NEZ333N27

Types de publication

Comparative Study Journal Article Randomized Controlled Trial

Langues

eng

Sous-ensembles de citation

IM

Pagination

154-162

Informations de copyright

Copyright © 2020 Elsevier B.V. All rights reserved.

Auteurs

Ronald Schilderink (R)

Triskelion B.V., Zeist, the Netherlands.

Marianella Protopappa (M)

Department of Pharmacy, School of Health Science, National and Kapodistrian University of Athens, Athens, Greece.

Jeannine Fleth-James (J)

Boehringer Ingelheim Pharma GmbH & Co. KG, Ingelheim am Rhein, Germany.

Maria Vertzoni (M)

Department of Pharmacy, School of Health Science, National and Kapodistrian University of Athens, Athens, Greece.

Kerstin Schaefer (K)

Boehringer Ingelheim Pharma GmbH & Co. KG, Ingelheim am Rhein, Germany.

Robert Havenaar (R)

Triskelion B.V., Zeist, the Netherlands.

Ivonne Kulla (I)

Boehringer Ingelheim Pharma GmbH & Co. KG, Ingelheim am Rhein, Germany.

Markus Metzger (M)

Boehringer Ingelheim Pharma GmbH & Co. KG, Ingelheim am Rhein, Germany.

Christos Reppas (C)

Department of Pharmacy, School of Health Science, National and Kapodistrian University of Athens, Athens, Greece. Electronic address: reppas@pharm.uoa.gr.

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Classifications MeSH