DEVELOPMENT AND OPTIMIZATION OF EFFERVESCENT TABLETS OF PROMETHAZINE

摘要

The objective of present study was to develop effervescent tablets of promethazine (PMZ) for the treatment of emesis. Effervescent tablets were prepared by direct compression method and were optimized using 32 full factorial design. Amount to sodium starch glycolate(X1) and amount of sodium bicarbonate (X2) were selected as independent variables, whereas disintegration time (Y1), amount of carbon dioxide (Y2) and drug release in 5 minutes (Y3) were selected as dependent variables. All the batches were also evaluated for general post compression evaluation of tablet such as- weight variation, thickness, friability and hardness. From the results of design batches, best batch was selected and evaluated for in vivo pharmacokinetic study in a rabbit model. The disintegration time ranged from 58.67±0.27sec to 228.67± 0.67sec while amount of carbon dioxide ranged from 0.1±0.082 gm to 0.29±0.061gm in all the design batches. From the results of design batches, batch F9 was selected as optimized batch due to higher amount of carbon dioxide released and faster drug release as compared to other batches. Batch B4 was showing higher AUC and C_max while lower t_max as compared to drug suspension while performing in vivo study of optimized batch in a rabbit model. The study concluded that the combination of sodium starch glycolate and sodium bicarbonate approach for development of effervescent tablet aids to achieve faster disintegration and faster drug release property for PMZ.