Pharmacokinetic Comparison of Capsule and Tablet Formulations of Opicapone in Healthy Japanese Subjects: Phase 1 Study.

Opicapone, a peripheral, long-acting catechol-O-methyltransferase inhibitor has been shown to improve wearing-off phenomenon in randomized, double-blind studies. This study compared the pharmacokinetic characteristics of opicapone small-tablet and size 1 capsule formulations after single oral administration to healthy Japanese subjects. In this open-label, randomized, 2-way and 2-period crossover phase 1 study, 48 healthy male subjects (aged 20 to 45 years; body mass index, 18.

Effect of Opicapone Tablets on Levodopa and 3-O-Methyldopa Pharmacokinetics in Healthy Japanese Subjects: Phase 1 Study.

This study evaluated the effect of a small-tablet formulation of opicapone for use in clinical trials in Japan on the pharmacokinetics of levodopa (l-dopa) and 3-O-methyldopa (3-OMD). In an open-label, 3-period, single-sequence crossover phase 1 study in 80 healthy Japanese males (aged 20-45 years; body mass index, 18.5 to <30.

Scale-up of in vitro permeation assay data to human intestinal permeability using pore theory.

The aim of this study is to establish a theoretical method for the prediction of human intestinal permeability from in vitro permeation assay. Pore radius and porosity/length and ion selectivity of the paracellular pathway were calculated using the Renkin function using permeabilities of mannitol and urea and potential difference study to evaluate paracellular permeability in Caco-2 cell monolayer; they were calculated to be 5.91 Å, 7.