Der Pharmacia Lettre
Abstract
Author(s): Shreeraj H. Shaha, Jayvadan K. Patelb and Nirav V. Patel
The purpose of the present study was to develop an optimized gastric floating drug delivery
system (GFDDS) containing gatifloxacin as a model drug using Box-Behnken design. 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 conc. of
compritol ATO 888 (X1), conc. of poloxamer 188 (X2) and conc. of chitosan (X3). Batches were
prepared by wet granulation method and evaluated for Floating lag time (FLT), Total floating
time (TFT) and time required to release 50% of the drug (t50) as dependent variables. Compritol
ATO 888 containing tablets were found to be significant for floating properties. Poloxamer 188
had a negative effect on floating properties but was found helpful in controlling the release rate
of the drug. No significant effect of chitosan on floating properties was observed but it was
important for gel formation. The quadratic mathematical model developed could be used to
predict formulations with desired release and floating properties. The transformed values of the
independent variables and dependent variables were subjected to multiple regressions to
establish a full-model second-order polynomial equation. Contour plots as well as response
surface plots were constructed to show the effects of X1, X2 and X3 on the FLT, TFT and t50. A
model was validated for accurate prediction of the FLT, TFT and t50 by performing checkpoint
analysis. The computer optimization process, contour plots and response surface plots predicted
at the conc. of independent variables X1, X2, and X3 (25.25 %, 13.62% and 15% respectively), for
maximized response of TFT. The Box-Behnken design demonstrated the role of the derived
equation and contour plots with response surface plots in predicting the values of dependent
variables for the preparation and optimization of gatifloxacin gastric floating matrix tablet.
