The aim of the current study is to develop a multiparticulate, high loading, colon targeted drug delivery system for mesalazine (5-ASA) suitable for once daily dosing by incorporating pH responsive polymers (Eudragit S and/or Eudragit L) into matrix based tablets composed of hydrophilic-hydrophobic polymers. The compatibility of the drug with formulation components was established by differential scanning calorimetry (DSC) and Fourier transform infra-red (FTIR) spectroscopy. Matrix tablets were prepared by wet granulation technique and were characterized for physical parameters, in-vitro drug release, release kinetics, and stability on storage. A 16-hr drug release profile with no or negligible release in the initial phase (4hr) followed by controlled release for 12hr was proposed as an ideal, targeted profile and was deduced from 5-ASA release profile of the once daily marketed product. In-vitro release studies indicated that the presence of pH-sensitive polymers in retarded the initial release (≈15% release in 4 hr) followed with controlled release for the next 12hr in simulated GI fluid pH. Such a matrix design could have potential application as colon-specific drug delivery systems with pH and time-dependent drug release profile.
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