PREPARATION AND CHARACTERIZATION OF CINNARIZINE FLOATING OIL ENTRAPPED CALCIUM ALGINATE BEADS

摘要

Gastroretentive delivery systems can be retained in the stomach and assist in improving absorption and consequently the bioavailability of drug that has a narrow absorption window in a particular region of gastrointestinal tract. A floatable multiparticulate system with potential for intragastric sustained delivery is one of the approaches to get the gastroretention. Cinnarizine(CNZ), an antihistaminic drug used in vertigo caused by meniere’s disease was taken as a model drug for floating beads prepared by non effervescent method. Floating CNZ olive oil-entrapped emulsion gel beads were prepared by the emulsion–gelation method. Different concentrations of sodium alginate (1%, 2%, and 3% w/v), oil (5%, 10%, and 15% v/v), and calcium chloride (0.02, 0.1, and 0.5M) were used and their influence on beads uniformity, buoyancy, and in vitro drug release was studied. The results indicated that retardation of drug release was achieved by the oil hydrophobic diffusion barrier, especially in the presence of the compact network of alginate beads. The selected formula of calcium alginate beads using 3% w/v sodium alginate, 15% v/v oil and 0.1 M calcium chloride, showed a higher similarity factor (f₂ =70.1) of CNZ release in comparison to release from standard gastroretentive sustained release floating cinnarizine tablet with good floating over duration of more than 12 hours.