Formulation and Evaluation of Gastro-retentive Drug Delivery Systems of Cinnarizine

Abstract

Background and Aim Cinnarizine is an antihistamine and calcium channel blocker used for the treatment of vertigo and vomiting. It has poor bioavailability and a half-life of 3.4 hours. Cinnarizine has low solubility and low dissolution rate in the gastrointestinal tract which causes the main problem for systemic circulation after oral administration. Hence this study aimed to achieve 24-hour drug release and floating cinnarizine effervescent floating tablets formulated using synthetic and natural polymers.Methods Gastro retentive floating sustained-release tablets of Cinnarizine an H-1 anti-histaminic drug were prepared by direct compression. The tablets were prepared to enhance bioavailability and observe the effects of synthetic polymers such as sodium CMC HPMC K5M polyox and natural polymers such as guar gum and xanthan gum. Pre- and post-formulation parameters were also evaluated.Results A better release profile was observed for drugs in the gastro-retentive drug delivery system because of its specific absorption. The prepared tablets started floating within three minutes and continued to float for gt 24 h. All the results were within the limits.Conclusion The present study aids in overcoming the dosing frequency by providing sustained release.