چکیده (انگلیسی):

The purpose of this research was to develop the hydrodynamically balanced delivery system of
Clarithromycin (CLA) which, after oral administration should have the ability to prolong gastric
residence time with the desired in vitro release profile for the localized action in the stomach, in the
treatment of Helicobacter pylori (H.pylori) mediated peptic ulcer. By applying wet granulation technique
floating tablets of Clarithromycin were prepared. The proportion of sodium bicarbonate was varied to
get the least possible lag time, also the polymer part varied to get the desired release. In vivo
radiographic studies were performed with Barium sulphate loaded formulation to justify the increased
gastric residence time of the dosage form in the stomach, based on the floating principle. The formulation
developed using 66.2% Clarithromycin, 12% HPMC K4M polymer, 8% sodium bicarbonate gave
floating lag time less than 3 min with a floating time of 12 h, and an in vitro release profile very near to
the desired release. X-ray studies showed the enhanced gastric residence time of the tablet to 220±
30 min. The mechanism of release of Clarithromycin from the floating tablets is anomalous diffusion
transport and follows zero order kinetics. In vivo radiographic studies suggest that the tablet has
increased gastric residence time for the effective localized action of the antibiotic (Clarithromycin) in the
treatment of H.pylori mediated peptic ulcer.