Formulation and Evaluation of Sublingual Tablets of Rabeprazole Sodium using Bioadhesive Polymers

Abstract

Oromucosal delivery of drugs promotes rapid absorption and high bioavailability, with faster onset of pharmaco-logical effect. However, many oromucosal delivery systems are compromised by the possibility of the patient swallowing the active substance before it has been released and absorbed locally into the systemic circulation. The present work introduces a new tablet system for sublingual administration in which the tablet is based on interactive mixtures of components, consisting of carrier particles partially covered by fine dry particles of the drug, in this case rabeprazole sodium. In the interests of increasing retention of the drug at the site of absorption in the oral cavity, a bioadhesive component was also added to the carrier particles. With this approach, it is possible to obtain rapid dissolution in combination with bioadhesive retention of the drug in the oral cavity. Rabeprazole sodium is an anti-ulcer drug having oral bioavailability 52% due to hepatic first pass metabolism. This work aims to avoid degradation of drug in acidic environment of stomach. In this study, rabeprazole sodium sublingual tablets were prepared by direct compression method using different bioadhesive polymers such as HPMC K4M and chitosan and sodium starch glycolate as a superdisintegrant. The effect of different concentration of polymers and super-disintegrating agents was measured by applying Box-Behnken design. The prepared tablets were evaluated for thickness, weight variation, hardness, friability, disin-tegration time, wetting time, bioadhesive strength, surface pH, drug content and in vitro drug release. FT-IR spectroscopy study revealed that there was no possible interaction between drug and polymers. Our results show that optimized formulation showed bioadhesive strength 12.34 ± 0.695 gm along with disintegration time 48.45 ± 0.230 seconds and in vitro drug release 95.98% in              10 min.