Development and Characterization of An Enteric Coated Extended-Release Formulation of Beta-Blocker

Abstract

The objective behind this research work was to design and formulate a patient compliant extended release compressed tablet of a beta-blocker which reduced dose from three to four times a day to once daily. This tablet comprising different concentration of excipients required to extend release like polymers include HPMC, with different grades also and achieving concentration of drug at desired site of action I.e., at jejunum by using enteric coating polymer i.e., Eudragit of grade having desired pH dependent degradation profile. Beta blockers are widely used in cardiovascular disorders like congestive heart failure, hypertension, angina pectoris etc. To obtain desired flow properties, wet granulation process is used to formulate the tablet blend by using rapid mixer granulator. PVP K90 was used as binder and was dissolved in isopropyl alcohol. Trials were taken with HPMC K100M and K4M in combination, and it was observed that, combination of HPMC K100M and HPMC K4M showed best release profile. The coating of Eudragit L100 dissolved in IPA and Acetone showed release in jejunum which is the site of action for API. Talc was added after homogenization, to the coating solution to avoid caking. During the process of coating with Neo Cota coater, gun blockage was observed as a major problem for which spray rpm and atomization were monitored throughout the process. The hardness of the tablet was also affecting the dissolution of the formulation. It was concluded that, as the concentration of HPMC increased, the dissolution of the tablet also led to slow release.