Development and characterization of bilayer tablet containing leflunomide and co-enzyme Q-10

Disease modifying anti-rheumatic drugs are the first line treatment for rheumatoid arthritis. The combination approach of the synthetic DMRDA has evolved recently. Leflunomide and co-enzyme Q10 were effective individually on the management of rheumatoid arthritis and hence they were chosen to form the bilayer tablet containing sustained release layer and immediate release layer. Both the active ingredients were estimated and validated by simultaneous UV spectrophotometric technique. It was discovered that the suggested approach was clear-cut, accurate, reliable, and sturdy. For the development of sustained release layer, co-processed excipient containing mannitol and HPMC K4M was developed and evaluated. Immediate released layer containing co-enzyme Q10 was evaluated by using different super disintegrants at different concentration. Finally, SR layer containing leflunomide, and IR layer containing co-enzyme Q10, was selected based on dissolution study and disintegration time respectively. From the DSC graph and FT-IR, it was clear that co-process excipients, leflunomide, and co-enzyme Q10 do not interact chemically. From the above selected batches, bilayer tablet was formulated by direct compression method and evaluated for pre-compression and post compression parameters. The composed batch was in compliance with the weight variation, hardness, friability, and disintegration time, which indicated good physical qualities. From the results, drug release of IR layer was found to be 98.13 % in 3 h and that of the SR layer was 85.62 % at the end of 8 h followed Korsymeyer-Peppas model, indicated the utility of coprocessed excipient containing mannitol and HPMCK4M for its sustained release characteristic at industrial level. Combination of DMARD and co-enzyme Q 10 will be the promising and eco friendly formulation for rheumatoid arthritis. [Display omitted] •Bilayer tablets were formulated by combining antiarthritic DMARDS, leflunomide with co-enzyme Q-10, as a supplement.•Simultaneous equation method by UV spectrophotometer was performed for estimation of leflunomide and co-enzyme Q10.•Both the active ingredients were incorporated as Bilayer tablet and the dissolution study were performed.