DESIGN, DEVELOPMENT & CHARACTERIZATION OF FAST DISSOLVING TABLET OF CARVEDILOL

Abstract

Fast dissolving tablets are developed as an alternative to tablet, capsule and syrup for the paediatric and geriatric patient suffering from disease who feels difficulty in swallowing the oral solid dosage form. Carvedilol is practically insoluble in water, slightly soluble in an alcohol, practically insoluble in dilute acids. Carvedilol is a non-cardioselective beta blocker. It has vasodilating properties, which are attributed mainly to its blocking activity at alpha1 receptors; at higher doses calcium-channel blocking activity may contribute. Carvedilol competitively blocks receptors. The elimination half-life is about 6 to 10 hours. The main objective of this research work was to formulate and evaluate fast dissolving tablet of carvedilol using excipients like Croscarmellose sodium, Crospovidone, Microcrystalline Cellulose,   magnesium stearate, PVP etc.  Formulation of fast dissolving tablets of Carvedilol by direct compression method using different types of polymer in different percentages. The tablets with drug were also evaluated for uniformity of drug content, in-vitro drug release and stability studies. The drug content in the fast dissolving tablets was found to be uniform and with low correlation of variation. The tablets prepared with solid dispersion in combination with super disintegrate showed better release profile as compared to only incorporation of super disintegrates.  The tablets prepared by effervescent and pore forming technology provides satisfactory drug release. The release of drug followed first order kinetics and mechanism of drug release was found to be diffusion controlled.

The stability data at different temperature and humidity showed no significant degradation of Carvedilol and shelf life found to be more than 520 days. Fast dissolving tablets prepared by the Ac – Di – Sol in 4% concentration are promising for rapid release of Carvedilol.  Incorporation of solid dispersion (PEG 4000 : CARVEDILOL) (4:1)  into Ac – Di – Sol in 2 % concentration enhanced the release rate of Carvedilol and thus therapeutic levels of the drug could be achieved through fast dissolving tablets. Tablets prepared by effervescent and pore forming technologies are also very promising for stable and rapid release of Carvedilol.

Keywords: Carvedilol, FDDS, solid dispersion, tablets, Sodium, Crospovidone, Microcrystalline Cellulose,   magnesium stearate, PVP.