Development and execution of a novel strategic statistical tool to determine in-vitro in-vivo correlation for sustained release capsules of metoprolol tartrate in humans

Abstract

The aim of this present study was to develop and formulate sustained release coated metoprolol tartrate matrix granules and to design an in-vitro in-vivo correlation (IVIVC) tool based on bioavailability data available from human volunteers. USP apparatus II, paddle type was used for generation of in-vitro drug release data for each formulation. The similarity factor (f2) was determined using dissolution data parameters of the formulations. Twenty-four healthy male volunteers participated in the two-way crossover bioequivalent study where the volunteers were treated in a completely randomized fashion. The percent drug dissolved in the dissolution test and percent absorbed data shows a ‘level A’ IVIVC was achieved with a good linear regression relation. Different release rate formulation including Fast, Moderate and Slow release formulations exhibited an excellent covenant between the three dosage forms. Key words: Sustained-release capsules, metoprolol tartrate, bioavailability, in-vitro in-vivo correlation (IVIVC), humans.