Development, Optimization And Comparative Pharmacokinetics Evaluation Of Glibenclamide Buoyant Tablet Formulation

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Osman, Bashier Ibrahim
Nur, Abubakr O.
Osman, Zuheir A.
Alkarib,Suad Y.
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University of Khartoum
This study address utilization of medium viscosity grade hydroxypropyl methylcellulose (HPMC, 4000cps), polyvinyl pyrollidone, stearyl alcohol, magnesium stearate and varying compression load to develop and optimize glibenclamide gastric floating tablets capable to float and sustain the release of loaded drug over a prolonged time duration in simulated gastric fluid through consecutive application of Box-Wilson and composite index designs. Time for floating onset, initial drug release and time for 50% drug release were found to be influenced by tablet hardness in linear fashion and by stearyl alcohol content in quadratic manner (p< 0.05 at CI95% for all influences) whereas floating duration confirmed to be affected by content of magnesium stearate and the joined influence of Mg stearate-sterayl alcohol content levels (p= 0.018 and 0.041 at CI95%, respectively). Glibenclamide floating tablet comprises of 46.7% w/w HPMC as matrixing agent, 16.7% stearyl alcohol as buoyancy enhancer, 2% magnesium stearate as lubricant, stated content of polyvinyl pyrollidone and compressed to 50N hardness was considered as best ranked formulation that fulfill preset constraints for floating onset (immediate floating), floating duration (6hrs), drug release in the first hour (28%), drug release within 6 hours (84%) and time for 50% drug release (3.2hr). Compared to an immediate release non floating glibenclamide tablets, in vivo investigation in 16 healthy human subjects revealed that glibenclamide plasma concentrations from floating tablet were maintained with less fluctuations over 24 hrs. Moreover, significant increase in Tmax, AUC0-∞, t½ aand MRT of glibenclamide was measured with the optimized WORLD JOURNAL OF PHARMACY AND PHARMACEUTICAL SCIENCES SJIF Impact Factor 5..210 Volume 4,, Issue 08,, 238-259 Research Article ISSN 2278 – 4357 Article Received on 14 June 2015, Revised on 05 July 2015, Accepted on 25 July 2015 *Correspondence for Author Suad Y. Alkarib Department of Pharmaceutics, College of Pharmacy, Karary University, Sudan. Vol 4, Issue 08, 2015. 239 Alkarib et al. World Journal of Pharmacy and Pharmaceutical Sciences floating tablet formulation (p<0.004 at CI90% for these parameters), indicating persistence in duration of glibenclamide plasma concentration from floating tablet formulation. .
Glibenclamide, Floating tablets, In vitro investigation, In vivo evaluation, Comparative pharmacokinetics