Development of atenolol gastro retentive floating drug Delivery systems: in vitro and vivo evaluation

Abstract

The objective of the present study was to develop sustained-release Atenolol tablets using floating technique to prolong the gastric residence time and compared their pharmacokinetic behavior with conventional tablets. Floating tablets were prepared using guar gum (GG) as hydrophilic gel material at different concentrations and sodium bicarbonate as gas-generating agent. The tablets were prepared by wet granulation method, then optimizing floating tablets formulation (containing 40% (w/w) of GG was able to float more than 12 h). The selected formulation was evaluated for uniformity of weight, hardness, friability, drug content and in vitro study which showed the desired sustained release The pharmacokinetic parameters of optimized formulation and conventional tablets in dogs were compared. The area under the curve of plasma concentration–time (AUC) and the average peak concentration (Cmax) of floating tablets were higher than the conventional tablets and (Tmax) was prolonged. The results proved that, the floating sustained-release design is a feasible approach for improving bioavailability of atenolol.