Incompatibility of Bisoprolol Fumarate with Some Super-disintegrating Agents

Aims: Bisoprolol fumarate, a selective β1adrenoreceptor blocker, is usually formulated as immediate release tablet dosage form. While developing the immediate release tablet formula in laboratory, the assay and dissolution results were found below acceptance limit in some formulation. The formulations differed only in disintegrating agents. Therefore a chemical interaction was suspected with some of the disintegrants with the drug used in the formulas. The aims of this study were to find out the interaction with the specific excipient.
Study Design: Consequently, a pilot study of binary mixture of Bisoprolol-excipients (conventionally used in solid dosage form, e.g. binder, diluents, disintegrating agents, glidants, dissolution enhancer etc.) was carried out in laboratory using different analytical methods such as dissolution tester, UV, HPLC, DSC etc. Also formulated tablets were studied.
Place: Study was carried in drug testing and analytical research laboratory in Center for Advanced Research in Sciences, University of Dhaka.
Results: From the study, bisoprolol fumarate was found quite incompatible with ‘sodium starch glycolate’(SSG) and ‘croscarmellose sodium’(CCS) both of which are used as disintegrating agents in conventional solid dosage forms. But other disintegrating agents such as kollidon CL (KCL) has shown no interaction towards bisoprolol fumarate.
Conclusion: Thus from this study we reached a valuable conclusion that bisoprolol fumarate is quite incompatible with two disintegrating agents namely sodium starch glycolate and croscarmellose sodium. With sodium starch glycolate, the drug was found to be degraded by around 19% whereas with croscarmellose sodium degradation was estimated around 13% in freshly prepared tablets. On the other hand, kollidon CL is compatible with this drug in its solid dosage formulation.