Design and Evaluation of Controlled Onset Extended-Release System for Chronotherapeutic Delivery of Aceclofenac

Abstract

The purpose of this research is to design and test Aceclofenac-containing capsule dosage type, which may be intended for the treatment of early morning stiffness and symptomatic pain relief in patients with rheumatoid arthritis. Immediate release tablets were prepared by wet granulation method using crospovidone, SSG, Lycoat, and Ludiflash. Enteric coated Microspheres were prepared using Eudragit L100 and Eudragit R100 by oil-in-oil solvent evaporation method. Both IR tablets and microspheres of aceclofenac have been tested for pre-compression, post-compression and findings find to be appropriate in our trials. Chemical reactions between the drug and the polymeric substance have been tested using FTIR. There was no disparity between the IR patterns of Aceclofenac, the physical mixture of Aceclofenac and polymers. Based on the results obtained IR tablet (AI12) containing Crospovidone as super disintegrant was considered as the optimum powder blend for fabrication of capsule system. Among the enteric coated microspheres AC9 was considered as optimized formulation for colonic drug delivery. As our aim of work is to maintain a chronotherapeutic drug delivery, now we combine the optimized IR tablets and optimized enteric coated microspheres in a single capsule. Based on the drug release studies, it shows drug released up to 20hrs and follows zero order release kinetics with non-ficikian diffusion mechanism.