Clarithromycin has a short elimination half-life, a narrow absorption window and is mainly absorbed in proximal areas of GIT. The purpose of this study was to develop a gastro retentive controlled release drug delivery system with swelling, floating, and mucoadhesive properties. Ten tablet formulations were designed using hydroxypropylmethylcellulose (HPMC K100M) and xanthan gum as release-retarding polymer(s) and sodium bicarbonate (NaHCO3), Sodium carbonate (NaCO3) and calcium carbonate (CaCO3) as a gas former. Swelling ability, floating behaviour, adhesion period and drug release studies were conducted in 0.1 N HCl (pH 1.2) at 37 ± 0.5º C. The tablets were subjected to various physiochemical tests, weight variation, content uniformity, thickness, hardness, floating lag time, adhesion period, total floating time etc. The study data revealed acceptable values of physicochemical properties. Drug release profiles of all formulation followed first order kinetic and diffusion mechanism. Statistical analyses of data revealed that tablets containing HPMC K100M (20% w/w), xanthan gum (5% w/w) and NaHCO3 (12%, w/w) in F8 or CaCO3 (12%, w/w) in F9 were promising systems exhibiting excellent floating properties, extended adhesion periods and sustained drug release characteristics. Both formulations were stored at 40º C/75% RH for 3 months according to ICH guidelines. Formula F10 showed better physical stability and longer release profile, so F10 was selected for the further in vivo study. Abdominal X-ray imaging of formula F10, loaded with barium sulfate, in New Zealand albino rabbit revealed a mean gastric retention period of 9.2 ± 0.51 h.
Loading....