DEVELOPMENT AND CHARACTERIZATION OF DIACEREIN AND CHLORZOXAZONE PULSATILE RELEASE TABLET DOSAGE FORM

Richa Dayaramani, Sandeep V. Nathwani*

The aim of this study was to develop and characterize press coated tablet of Diacerein and Chlorzoxazone. The drug delivery system is based on the concept of chronotherapeutics where the drug is released rapidly after a well defined lag-time. A pulsatile-release profile is characterized by a time period of no release (lag time) followed by a rapid and complete drug release. Diacerein (DMARD) and Chlorzoxazone (NSAID) combination has been used for obtaining synergistic effect in the management of arthritis. Drug polymer compatibility studies were carried out by FT-IR. Core tablet was prepared by direct compression using super disintegrant sodium starch glycolate. The core tablet was compression coated with different quantities of coating material containing different polymers. A 3² Full factorial design was used for optimization of the barrier layer. Total coat weight (X₁₎ and % HPMC K4M (X₂) were selected as independent variables. The lag time for Diacerein (Y₁), CPR at 1st hr after lag time for Diacerein (Y₂), time for 90% drug release for Diacerein (Y₃), the lag time for Chlorzoxazone (Y₄), CPR at 1^st hr after lag time for Chlorzoxazone (Y₅) and time for 90% drug release for Chlorzoxazone (Y₆) were selected as dependent variables. Tablets were evaluated for various evaluation parameters. Comparative dissolution profiles of all the batches indicated drug release from tablet was inversely proportional to the coat weight. From the release profile it was deduced that delay lag time was observed for the press-coated tablet containing a higher amount of HPMC K4M in the outer shell. The press coated tablets coated with HPMC K4M:HPMC K100 in 64.39:35.61 ratios with 200 mg coat weight are most likely to provide the desired delivery of Diacerein and Chlorzoxazone.