Formulation Approach to Improve the Gastric Residence Time of Bisoprolol Fumarate by Gastro-Retentive Tablets

Abstract

Purpose: Gastric retentive drug delivery devices can be used for controlled drug delivery systems containing drugs, which are degraded in the colon. The main objective of the present study is to design and formulate gastric retentive controlled release dosage form of bisoprolol fumarate in order to improve the gastric residence time, which in turn increases its bioavailability. Approach: Floating dosage form of bisoprolol fumarate was prepared by direct compression method using different concentration and grades of hydroxypropyl methylcellulose and sodium bicarbonate. Prepared powder mixtures and tablets were subjected to various pre-compression and post-compression evaluations respectively. Findings: Powder mixture showed good flow properties for uniform die filling. The SEM analysis showed minimum number of pores and erosion on the surface of the tablet. The optimized formulation F8 gave floating lag time less than 3 min with a floating time of 12 h, and an in vitro release profile very near to the desired release. The prepared dosage form reported to follow the zero order release and non-Fickian mechanism. Best formulations were subjected to accelerated stability studies. The assay results showed that the drug was stable for 3 months without any change in the drug content. Conclusion: Finally it can be concluded that the gastric retentive time of bisoprolol can be increased by formulating it in a floating dosage form.