Application of the correlation of in vitro dissolution behavior and in vivo plasma concentration profile (IVIVC) for soft-gel capsules - A pointless pursuit?

Hidekatsu Nishimura, Chiaki Hayashi, Tetsuya Aiba, Ichiro Okamoto, Yuji Miyamoto, Susumu Nakade, Kazuhisa Takeda, Yuji Kurosaki

Research output: Contribution to journalArticle

14 Citations (Scopus)

Abstract

Plasma concentration profiles of arundic acid ((R)-(-)-2-propyloctanoic acid), an oil-like medicine, administered as soft-gel capsules in human clinical tests were predicted from the dissolution test data of the soft-gel capsules with different storage terms (short- and long-term stored drugs) by applying the in vitro-in vivo correlation (IVIVC). We established two linear-regression IVIVCs, which were characterized by either the in vitro dissolution behaviors against the pH 8.0 dissolution medium or the pH 6.8 dissolution medium containing 2% sodium dodecyl sulfate (SDS), in this study. Also, the prediction accuracies for the in vivo plasma profiles in humans for these two IVIVCs were compared. Regarding dissolution from the long-term stored capsule in pH 8.0 dissolution medium without surfactant, the prediction accuracies of the in vivo plasma profiles in humans were not satisfactory for the obtained IVIVC. The use of pH 6.8 dissolution medium containing 2% SDS, according to the Japanese guideline, improved the dissolution of the long-term stored capsule. Furthermore, the prediction accuracies for the in vivo plasma profiles in humans for these two IVIVCs were compared. The IVIVC established by the in vitro dissolution data obtained with the dissolution medium containing surfactant more effectively predicted the plasma drug concentration profiles following oral administrations of the soft-gel capsules under both storage conditions.

Original languageEnglish
Pages (from-to)2221-2225
Number of pages5
JournalBiological and Pharmaceutical Bulletin
Volume30
Issue number11
DOIs
Publication statusPublished - Nov 2007

Keywords

  • IVIVC
  • Prediction accuracy
  • Soft-gel capsule
  • Storage condition
  • in vitro-in vivo correlation

ASJC Scopus subject areas

  • Pharmacology
  • Pharmaceutical Science

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