Controlled Release Imatinib Mesylate Tablet Formulation: Using Hydrophilic Matrix System

Abstract

Background: Imatinib mesylat as an oral anticancer agent need a controlled released formulation to get steady and stable plasma concentration. The aim of the present study was to develop controlled release matrix tablet formulations of Imatinib using hydroxy propyl methyl Cellulose as a hydrophilic release retardant polymer and to study the effects of different formulation features like polymer viscosity grade, ratio of the polymer,  compression force, and release medium on the in vitro release properties. Methods: The in vitro release studies were performed using US Pharmacopoeia type I apparatus. The release kinetics was analyzed by Korsmeyer–Peppas model and were also analyzed using statistical method and f2 metric values. The release profiles look like Higuchi’s square root kinetics model irrespective of the viscosity grade and polymer proportion. Results:  The results showed that the release rate of the drug is greatly affected by the drug/polymer ratio and viscosity grade. Also, the effect of release medium and compression force was showed to be significant on the release profiles. The release mechanism was found to be anomalous non-Fickian diffusion in all formulations. Conclusions:  The formulations were found to be reproducible and stable. Controlled release formulations were developed with different release rates and profiles so that these formulations could be evaluated for more in vivo studies.

Keywords: Imatinib, Controlled release, HPMC, Dissolution