Abstract

FORMULATION AND EVALUATION OF BILAYER TABLET OF TELMISARTAN & METOPROLOL SUCCINATE

Ram Pentewar, Seema Balurkar*, R.V. Sugave, Ravi Rajurkar and S. Zingade

ABSTRACT

The main objective of this combination therapy is to develop a stable formulation of antihypertensive drugs of angiotensin II receptor antagonist (ARB) as an immediate release and β1-Selective Adrenergic Receptor Blocker (β1-SARB) as sustain release bilayer tablet and evaluate their precompression and post-compression parameters. A bilayer tablet comprises first layer formulated for instant release of the angiotensin II receptor antagonist (ARB) from a dissolving tablet matrix and a second layer formulated for sustain release β1-Selective Adrenergic Receptor Blocker from a bilayer tablet. The formulation of the developed work was initiated with direct compression method for telmisartan layer and metoprolol succinate layer. In the formulation of immediate release Micro crystalline cellulose and Croscarmellose sodium (CCS) were used as super disintegrants and was directly compressed. Mannitol was used as diluents. Magnesium stearate used as lubricant. The compressed bilayer tablets were evaluated for weight variation, thickness, hardness, friability, drug content, and in-vitro drug release using USP dissolution apparatus type 2 (paddle). The optimized formulation F-2 had 91.25% of drug release for ARB layer and 99.38% drug release for β1-SARB layer. The IR spectrum and DSC studies revealed that there is no disturbance in the principal peaks of pure drugs Metoprolol succinate and Telmisartan. This further confirms the integrity of pure drugs and no incompatibility of them with excipients. The stability studies were carried out for the optimized batch for one months and it showed acceptable results. The present studies concluded that bilayer tablet of Telmisartan and Metoprolol Succinate is novel approach to prevent hypertension.

Keywords: Bilayer Tablet, telmisartan, metoprolol succinate, direct compression method.