DESIGN AND CHARACTERIZATION OF FLOATING CONTROLLED RELEASE TABLETS OF IMATINIB MESYLATE FOR SITE SPECIFIC DRUG DELIVERY

Abstract

Imatinib Mesylate is an anti cancer agent which is used to treat chronic myelogenous leukemia (CML), gastrointestinal stromal tumors (GISTs) and a number of other malignancies. In the present research work an attempt has been made for the formulation of floating tablet containing Imatinib Mesylate as a drug candidate which would remain in stomach or upper part of GIT for prolonged period of time thereby maximizing the drug release at the desired site within the stipulated time. In the present study Imatinib Mesylate floating tablets were prepared by wet granulation method. The floating tablets were subjected to preformulation studies, in- vitro drug release, kinetic studies and stability studies. FTIR studies shown there was no interaction between drug and polymers. The percentage of Imatinib Mesylate content from the tablets was determined by UV-Spectroscopy and ranged from 98.32±2.3 to 99.46±1.4. The in-vitro percentage release of Imatinib Mesylate from the optimized tablets at the end of 12 hours was 98.90±1.2. The kinetic studies revealed that the drug was released by zero-order kinetics. The optimized formulation was subjected to stability studies and shown there were no significant changes in drug content, physicochemical parameters and release pattern. From this study, it is concluded that, the formulations retained for longer period of time in the stomach and provides controlled release of the drug. Hence, it will be increasing the bioavailability of the drug and patient compliance.