Abstract

DESIGN AND EVALUATION OF ALBENDAZOLE FLOATING TABLETS FOR ENHANCED GASTRO-RETENTIVE AND SUSTAINED RELEASE EFFECTS

Romanus Chijioke Omeh*, Cyprain Uzochukwu, Mercy Ebere Ugwueze, Raymond Ogbonna Offiah, Agatha Adaora Ugwu, Ibeabuchi Jude Ali and Amala Chukwunwike Ofor

ABSTRACT

Many therapeutically important drugs experience quick passage through the stomach either due to the nature of the drug or the presence of some pathological conditions. Rapid transit through the stomach limits the effectiveness of drugs in treating local stomach lesions/diseases and prevents optimum concentration of such drugs in the gastric fluid. Floating pharmaceutical formulations prolong gastric residence time of dosage forms thereby promoting local release and actions. The aim of this work was to utilized floating tablet formulations to enhance gastro-retention and sustained release of orally administered albendazole. Tablets formulated with hydroxypropylmethylcellulose, microcrystalinecellulose and sodium bicarbonate in varying proportions were prepared by the direct compression method. The tablets were evaluated for floating lag time, buoyancy, swelling indices and other pharmaceutical properties including friability, hardness, disintegration time and drug release profiles. Most of the parameters were affected by the concentrations of the hydroxypropylmethylcellulos and sodium bicarbonate. The floating lag times of all the formulations were below 6 min while the total floating times (buoyancy) ranged from 7 – over 12 h. The cumulative percentage drug release from various formulations determined at 12 h points in the simulated gastric fluid (SGF) ranged from 25.47 ± 2 – 43.64 ± 2 while releases in the simulated intestinal fluid (SIF) were in the range of 36.75 ± 3.5 - 88.53 ± 0.80%. It was concluded that an optimized albendazole tablet formulation containing hydroxpropylmethylcellulose and sodiumbicarbonate has the potential to float on top of the gastric fluid thereby delaying passage through the stomach and facilitating both local and sustained release of the drug.

Keywords: Floating tablet, sustained release, hydroxypropylmethylcellulose, gastro-retentive, albendazole, antihelminthics.