Formulation and evaluation of Tadalafil oral disintegrating tablets with enhanced dissolution rate by complexation

http://dx.doi.org/10.21276/IJRDPL.22780238.2017.6(3).2631-2640 ABSTRACT: Aim: In the present study was to enhance the solubility of Tadalafil (TDF) by forming inclusion complexes with β-cyclodextrin (βCD) and further to enhance its dissolution rate by formulating orally disintegrating tablet (ODT) by direct compression technique. Objectives: To perform the phase solubility studies, for to determine the ratio of drug: carrier ratio in the formation of complexes. Physico-chemical characterization of complexes by DSC and X-ray diffraction studies. To check the superiority of selected superdisintegrants [sodium starch glycolate (SSG), croscarmellose sodium (CCS), crospovidone (CPV)] in enhancing the dissolution rate of TDF. To fasten the onset of action and thereby increasing TDF’s bioavailability in comparison to its conventional tablets. Methods: Standard calibration curve of TDF in pH 6.8 phosphate buffer was constructed by spectrophotometric method, drug-excipient compatibility was checked by FT-IR studies. All the Formulations were evaluated for pre& post-compression studies. Accelerated stability studies up to 3 months were conducted for the optimized formulation, as per ICH guidelines. Results and Discussions: polymers used in the study are compatible with TDF. Pre& postcompression parameters were within the acceptable limits for all formulations. In vitro dissolution kinetic studies indicate the release of TDF from ODT increases with the increased concentration of superdisintegrants. The order of superdisintegrants in enhancing the dissolution rate of TDF is CPV>SSG>CCS. Formulation F6, had the highest dissolution efficiency at 5 min (DE5=39.55 %); first order dissolution rate constant (K1 =0.1052 min-1) with a regression coefficient (r2=0. 9844) and lesser time for 50% of drug release (t50=4 min), was considered as the optimal ODT. It passed the test for stability as per ICH guidelines. Conclusion: The optimized TDF ODT with its 1:4 βCD complex was formulated by the direct compression technique, with 6% w/w CPV as superdisintegrant, which will fasten the onset of action and enhances the bioavailability of TDF in comparison to its conventional tablets.