Journal article Open Access
Akshay Kumar Soni*1, Dr. Surendra Lalwani1, Anshul Jain2, Monika Chauhan2
The purpose of the present study was to develop gastro-retentive floating tablet of Atenolol. It is a beta-adrenoreceptor antagonist (beta-blocker) used in the treatment of hypertension and angina pectoris. It is incompletely absorbed from the gastrointestinal tract and has an oral bioavailability of only 50% while remaining drug is excreted unchanged in feces. This is because of poor absorption in lower gastrointestinal tract. Therefore, the formulation of Atenolol as a gastro-retentive floating drug delivery system (GFDDS) was thought to be beneficial, with a view to improve its oral bioavailability and therapeutic efficacy. The floating tablets of Atenolol (F1-F9) were prepared by direct compression technique using HPMC of different viscosity grades (K4M and K15M) as the polymers and sodium bicarbonate and citric acid as a gas generating agent, to reduce floating lag time. The blends were evaluated to bulk density, tapped density, compressibility index, Hausner’s ratio and angle of repose. The tablets were evaluated to thickness, hardness, diameter, weight variation, and drug content uniformity, friability, floating lag time, effect of hardness on buoyancy lag time and in-vitro swelling studies, in-vitro drug release studies. In-vitro drug release study was performed using USP dissolution test apparatus-II at 50 rpm using 900 ml of hydrochloric acid buffer pH 1.2 maintained at 37±0.5ºC as the dissolution medium. Among the various floating tablet formulations studied, formulation F6 containing drug polymer ratio (1:3) prepared with HPMC K4M & K15M showed promising results releasing 92.63% of the drug in 12 hours with a floating lag time of 30 seconds and floating time of more than 24 hours has been considered as an ideal formulation. FTIR studies indicate that there is no interaction between drug and excipients. Stability study of F6 formulation was performed and that showed no major change in physicochemical parameters, floating properties and drug release profile.