Abstract
Sustained-release (SR) dosage forms consisting of pellets coated with different pH-sensitive film layers, previously optimized in vitro with regard to pH independence of their durg release characteristics, were evaluated in vivo after single administration to Beagle dogs. In vivo performances were compared to those of a nonoptimized SR matrix tablet and a reference instant release (IR) capsule, in terms of the observed plasma pharmacokinetic profiles for the parent drug (ucb 11056) and its primary metabolite (ucb 26201), the bioavailability results, and the drug tolerance data. All SR dosage forms were seen to be effective in prolonging the relatively short biological half-life of the compound and in reducing the incidence of concentration-related side-effects, e.g., emesis, and of behavioral symptoms, e.g., restlessness, discomfort, and indisposition. The film-coated SR pellets offer a number of advantages over the monolithic SR matrix system in terms of a drug delivery pattern less dependent on pH changes in the gastrointestinal (GI) tract, a higher flexibility for adjusting and controlling the pharmacokinetic profiles, and a consequently more efficient approach for keeping all concentration-related side-effects under control.
Published Version
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call