Once Daily, High-dose Mesalazine Controlled-release Tablet for Colonic Delivery: Optimization of Formulation Variables Using Box-Behnken Design

Overview

Journal AAPS PharmSciTech

Publisher Springer

Specialty Pharmacology

Date 2011 Nov 1

PMID 22038474

Citations 5

Authors

Ahmed Abd Elbary

Ahmed A Aboelwafa

Ibrahim M Al Sharabi

Affiliations

Soon will be listed here.

Abstract

The aim of this work was to statistically optimize a novel high-dose, mesalazine colonic delivery matrix system, potentially suitable for once daily administration, using simple wet granulation method. A hydrophobic-hydrophilic polymeric blend was used to manipulate drug release. A three-factor, three-level Box-Behnken design was used to construct polynomial models correlating the dependent and independent variables. Independent formulation variables were the percentages of the hydrophilic polymer Carbopol® 940, hydrophobic polymer Eudragit® RS, and the superdisintegrant croscarmellose sodium. The cumulative percentages of drug released at 6, 10, and 14 h were selected as dependent variables and restricted to 7.5-22.5% (Y(1)), 42.5-57.5 % (Y(2)), and 72.5-87.5% (Y(3)), respectively. A second-order polynomial equation fitted to the data was used to optimize the independent formulation variables. Based on Box-Behnken experimental design, different mesalazine release profiles were obtained. The optimized formulation containing 5.72% Carbopol®, 9.77% Eudragit® RS, and 1.45% croscarmellose sodium was prepared according to the software determined levels. It provided a release profile which was very close to the targeted release profile, where the calculated values of f(1) and f(2) were 8.47 and 67.70, respectively, and followed zero-order release kinetics.

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