Formulation Development and In Vitro Characterization of Zolmitriptan Controlled Release Drug Delivery Systems

Abstract

Background: Zolmitriptan is an artificial tryptamine, employed for the acute cure of migraine attack with or exclusive of aura and cluster headaches. Objective: It is an attempt to develop the extended release (ER) of Zolmitriptan matrix (ZMT) tablets to treat migraine safely and effectively. Methods: All formulations were prepared with natural polymers or gums like guar gum, xanthan gum, karaya gum through direct compression method using 6mm punch. Results: Powder blend of all formulations (F1 - F12) using different ratios of the above mentioned gums (5%, 10%, 15% and 20%) were characterized with pre-compression parameters (angle of repose, bulk density, tapped density, compressibility index, hausner ratio, compatibility studies) and post-compression parameters (weight variation, thickness, friability, hardness, assay, in vitro dissolution studies). F1 - F4 formulations were prepared with gum karaya and compared with remaining gums; gum karaya shows more retardance capacity. F9 - F12 (with guar gum) formulations were unable to produce the desired release, whereas F5 - F8 formulations containing with xanthan gum exhibited more retarding effect with increasing concentration of polymer. Conclusion: All prepared formulations (F1 - F12) were characterized and F3 formulation was optimized (97.3% drug released in 8 hours). All prepared formulations (F1 - F12) showed good flow properties and release patterns. Hence, formulations of ZMT matrix tablets have a promising delivery system which will enhance bio-availability and achieve greater therapeutic efficacy.