Abstract:
Metoprolol tartrate is β1-selective adrenergic blocking agent and widely used in
the treatment of hypertension and angina-pectoris. The present investigation was
undertaken with an objective to increase the bioavailability of the drug by
avoiding hepatic first pass metabolism giving quick onset of action. The
sublingual tablets of Metoprolol tartrate were prepared in various batches (trial
batches) and evaluated for various parameters such as hardness, friability, drug
content, in vitro disintegrating time and in vitro dissolution study. The tablets
containing 3.5mgsodium starch glycolate and 3.5 mg crospovidone showed the
least disintegrating time and highest drug release. The formulation was further
optimized using 32 factorial design taking X1 and X2 as independent variables
(concentration of sodium starch glycolate and crospovidone) and disintegrating
time and %drug release as dependent variables. The batch B9 was selected as
optimized batch which showed least disintegrating time 35 seconds, cumulative
percentage drug release at 25min 96.75±0.19 %. The two extra check point
batches were prepared and evaluated. The closeness of predicted and actual
values validated the design. Thus, the sublingual tablets of Metoprolol tartrate
were successfully formulated to give quick onset of action.