Preparation, in vitro and in vivo evaluation of Floating-bioadhesive tablets of Baclofen using natural gums

The content of the investigation was to prepare and evaluate the floating-bioadhesive tablets of baclofen (BC) to sustain the drug release. BC is a skeletal muscle relaxant and is used to treat muscle symptoms and also acts as antispastic agent. BC have biological half-life of 1.5 to 4 h and also shows pH dependent solubility. Hence, it is considered as a potential candidate for development of floating-bioadhesive drug delivery system. The BC tablets were prepared by wet granulation method using guar gum and xanthan gum as gel forming agents and sodium bicarbonate as gas generating agent. The prepared tablets were evaluated for physical parameters, in vitro buoyancy and in vitro dissolution studies. Further, in vivo radio graphic studies of optimized formulation were performed in healthy human volunteers in fasting condition. In vitro release studies revealed that guar gum and xanthan gum containing (F9) tablets of baclofen showed 97.89±1.04% of drug release at 8 h time period. DSC studies revealed that no interaction between drug and other excipients. In vivo radio graphic studies revealed that the tablets showed mean gastric residence time of 4 ± 0.8 h in the stomach. Therefore, the results conclusively demonstrate the sustained effect of baclofen was achieved by the combination of floating and bioadhesive mechanism.