Development and optimization of novel fast disintegrating tablet formulation using beta cyclodextrin as a diluent

Purpose. The objective of this dissertation was to investigate novel application of beta cyclodextrin, as a diluent, to develop and optimize novel fast disintegrating tablet formulation of granisetron hydrochloride and piroxicam.; Methods. Granisetron hydrochloride was used to develop and optimize novel fast disintegrating tablet formulation using beta cyclodextrin as a diluent. Compatibility of selected tablet excipients was determined using thermal and non-thermal methods. Experiments were performed according to Face centered central composite design to evaluate effects of formulation parameters like concentration of diluent, concentration of disintegrating agent and concentration of direct compression aid agent, and their interactions on disintegration time and hardness of the fast disintegrating tablet formulation. Effects of disintegration promoting agent and different lubricants on the optimized formulation were evaluated by full factorial design.; Model poorly soluble compound, piroxicam, was used to study influence of complexation of drug with beta cyclodextrin on the dissolution and tabletting properties of the optimized fast disintegrating tablet formulation. Piroxicam-beta cyclodextrin complexes were prepared by different methods. These complexes were further used to prepare fast disintegrating tablets. Tablets prepared using physical mixture of piroxicam with beta cyclodextrin were used for comparison purpose.; Stability of the optimized novel formulation was evaluated at different temperature and humidity conditions.; Results. All the selected excipients were found compatible with granisetron hydrochloride. Response surface plots revealed that concentration of beta cyclodextrin was the most important formulation parameter in optimizing fast disintegrating tablet formulation. At low concentration of beta cyclodextrin (below 30%), tablets disintegrated predominantly by dissolution mechanism, while at high concentration, tablet disintegration was due to swelling of the disintegrating agent because of the water uptake and disintegration as result of force generated inside the tablet. Concentration of lubricant significantly affected the disintegration time and tablet hardness. Lubricant was important for the preparation of intact tablets.; Tablets prepared using spray dried and freeze dried inclusion complexes strongly affected disintegration time and hardness of the optimized fast disintegrating tablets. Fast disintegrating tablets were fairly stable at lower humidities and temperatures till 37°C.; Conclusion. Novel application of beta cyclodextrin, as a diluent, enabled development and optimization of novel fast disintegrating tablet formulations of granisetron hydrochloride and piroxicam.