Prediction of oral absorption of griseofulvin, a BCS class II drug, based on GITA model: Utilization of a more suitable medium for in-vitro dissolution study

Yoshitsugu Fujioka, Keitaro Kadono, Yasuko Fujie, Yukiko Metsugi, Ken ichi Ogawara, Kazutaka Higaki, Toshikiro Kimura

Research output: Contribution to journalArticle

16 Citations (Scopus)

Abstract

The in-vivo absorbability of drugs categorized into the biopharmaceutics classification system (BCS) class II is very difficult to be predicted because of the large variability in the absorption and/or dissolution kinetics and the lack of an adequate in-vitro system for evaluating the dissolution behavior. We tried to predict the in-vivo absorption kinetics of griseofulvin, categorized into BCS class II, orally administrated as powders into rats, based on Gastrointestinal-Transit-Absorption model (GITA model), consisting of the absorption, dissolution and GI-transit processes. Using the dissolution rate constants (kdis) of griseofulvin obtained with JP 1st solution, JP 2nd solution, FaSSIF, FeSSIF and modified SIBLM as a medium, simulation lines were not able to describe the observed mean plasma profile at all. On the other hand, a calculated line provided by employing kdis obtained with MREVID 2 (medium reflecting in-vivo dissolution 2), a new medium, was in better agreement with the observed mean plasma profile than existing media, indicating that the utilization of adequate kdis value made it possible to predict the in-vivo absorption kinetics of drugs classified into BCS class II based on GITA model and that MREVID 2 could be a useful medium for describing the in-vivo dissolution kinetics.

Original languageEnglish
Pages (from-to)222-228
Number of pages7
JournalJournal of Controlled Release
Volume119
Issue number2
DOIs
Publication statusPublished - Jun 1 2007

Keywords

  • Biopharmaceutics classification system class II
  • In-vitro dissolution study
  • Oral absorption
  • Powder
  • Prediction

ASJC Scopus subject areas

  • Pharmaceutical Science

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