Formulation and characterization of floating tablets for site specific sustainedrelease of metoprolol succinate

摘要

The present study was undertaken to formulate a floating matrix for site specific sustained release of Metoprolol Succinate in stomach with the aid of polymers HPMC K4M, Carbopol 934P and natural polysaccharide Xanthine gum as release modifiers. Metoprolol Succinate, β1-selective adrenergic receptor- blocking agent used in the management of hypertension, angina pectoris, cardiac arrhythmias, myocardial infarction, heart failure, hyperthyroidism and in the prophylactic treatment of migraine. The short half-life of Metoprolol Succinate, need of multiple administrations during therapy and hence, absorption window in the small intestine, warrants the gastric retarded sustained release formulation. Ten formulations of Metoprolol Succinate floating tablets had been done by employing various combinations and concentration of release modifying polymers. The tablets were evaluated for uniformity in weight, hardness, friability, content uniformity, Swelling index and in vitro release study. It was found that the Metoprolol Succinate floating tablets optimized formulation F3 had good floating characters and sustained the release of the drug for about 53.13±1.26% over 12 hrs. The release of drug from the formulations follows zero order, non-fickian mechanism except F3 where it follows supercase II model. The optimized formulation subjected for short term stability studies.