Title:Enhanced Bioavailability of Cinnarizine Using Solid Dispersion: In Vitro and In Vivo Evaluation
VOLUME: 9 ISSUE: 4
Author(s):Muzeyyeu Demirel, Gulary Buyukkoroglu, Basar Sırmagul, Bahar S. Kalava, N. Ozturk and Yesemin Yazan
Affiliation:Anadolu University, Faculty of Pharmacy, Department of Pharmaceutical Technology, Eskişehir, Turkey.
Keywords:Cinnarizine, in vitro-in vivo evaluations, solid dispersion.
Abstract:The aim of this study was to modify the release and thus enhance the bioavailability of a
calcium antagonist cinnarizine whose aqueouse solubility is low and half-life is short. For this
purpose, solid dispersion system was chosen as the delivery system since it is a simple method at
laboratory conditions and it is belived to increase the dissolution of the active agents. Eight
formulations of solid dispersions were prepared using four different methods and two different vehicles, to investigate the
effects of the preparation method and the vehicle used on the release of the active ingredient, cinnarizine. For the
characterization of cinnarizine solid dispersions, cinnarizine amount, practical yield %, thermal, particle size distribution
and X-ray diffraction analysis were performed. In vitro dissolution from hard cellulose capsules containing cinnarizine
solid dispersions was compared to pure cinnarizine. Aqueous dispersions of pure cinnarizine and the formulation selected
depending on the results of the in vitro analyses were applied to rabbits orally. As a conclusion of the in vitro-in vivo
evaluations of solid dispersions planned to be developed for increasing cinnarizine absorption potential, it was determined
that the dissolution could be modified and the bioavailability could be enhanced.
