Abstract

FORMULATION DEVELOPMENT OF TELMISARTAN AND METOPROLOL(FDC) FOR TIMED RELEASE DOSAGE FORM

Gokul B.*, Anandh R., Gokul H., Gurusabariysh G., Harichitharthan M., Kannan M., Kumaravelrajan R.

ABSTRACT

This study focuses on the formulation and evaluation of timed-release pellets of Metoprolol succinate and Telmisartan using the extrusion-spheronization technique, optimized through a 2-level factorial design with four experiments. The primary objective was to achieve sustained release of Metoprolol succinate up to 4 hours while ensuring rapid release of Telmisartan within 30 minutes, thereby enhancing therapeutic efficacy in cardiovascular therapy. Hydroxypropyl Methylcellulose (HPMC K100M) and Microcrystalline Cellulose (MCC) were employed as key excipients to modulate drug release kinetics. The formulated pellets exhibited good sphericity, low friability, and high density. The study demonstrated that a higher proportion of MCC resulted in increased cumulative drug release, whereas an increased HPMC concentration led to a more controlled and sustained release profile. Among the tested formulations, Formulation 1 exhibited the highest drug release (85.43%) due to the absence of HPMC, while Formulation 4 showed the lowest release(69.08%). Additionally, Telmisartan exhibited rapid release in all formulations, with approximately 85% released within 30 minutes. The findings highlight the influence of polymer composition on drug release kinetics and establish the potential of extrusion-spheronization in developing optimized timed-release formulations for improved cardiovascular therapy.

Keywords: Telmisartan, Metoprolol, pellets, Anti hypertension. Running title: Metoprolol TR Spansules.