Box-Behnken experimental design in the development of pectin-compritol ATO 888 compression coated colon targeted drug delivery of mesalamine

The aim of this study was to investigate the combined influence of 3 independent variables in the compression coated tablet of mesalamine for ulcerative colitis. A 3-factor, 3-level Box-Behnken design was used to derive a second order polynomial equation and construct contour plots to predict responses. The independent variables selected were: percentage of polymers (pectin and compritol ATO 888) in compression coating (X₁), coating mass (X₂) and coating force (X₃). Fifteen batches were prepared and evaluated for percent of drug released in 5 h (Y₅), time required for 50 % mesalamine to dissolve (t₅₀) with rat cecal (RC) content and without rat cecal content (t₅₀), percent of drug released in 24 h in the presence of rat cecal content (Y₂₄ with RC). Transformed values of independent and dependent variables were subjected to multiple regressions to establish a full-model second-order polynomial equation. F was calculated to confirm the omission of insignificant terms from the full-model equation. The computer optimization process and contour plots predicted the levels of independent variables X₁, X₂, and X₃ (0, 0.2 and -0.15, respectively) for colon targeting and total percent of drug released up to 24 h.