FORMULATION & OPTIMIZATION OF IMMEDIATE RELEASE TABLET OF RUPATADINE FUMARATE

Abstract

The anti-allergic drug rupatadine may be slowly or incompletely dissolved in gastro intestinal tract. The rate of dissolution and bioavailability of the drug may be increased by using superdisintegrants in its immediate release tablets. In the present study the selection of proper superdisintegrants among sodium CMC, crospovidone and alginic acid was carried out to develop immediate release tablets of nateglinide. The FT-IR studies were carried out for compatibility testing between drug and excipients used in tablets. A 32 full factorial design was used to investigate the joint influence of 2 independent variables: amount of selected superdisintegrants, crospovidone and hardness of the tablets. The results of multiple linear regression analysis revealed that the dependent variables; disintegration time and drug release at 0.5h values are strongly dependent on the selected independent variables. The sign of coefficient of polynomial equation signified that an increase in disintegration time on decreasing the hardness of the tablets. An increase in the value of drug release at time 30 min observed on increasing the concentration of crospovidone. A checkpoint batch was also prepared to prove the validity of the evolved mathematical model. The systematic formulation approach helped in understanding the effect of formulation processing variables. Stability studies of factorial batches indicated that no significant change in appearance of the tablets, disintegration time, and percentage drug release were observed.