COMPARATIVE STUDY OF MUCOADHESIVE POLYMERS CARBOPOL 974P AND SODIUM CARBOXYMETHYL CELLULOSE FOR SINGLE UNIT DOSAGE OF IMATINIB MESYLATE

The aim of this study was to design and develop controlled release Imatinib mesylate (IM) oral dosage form by fabricating gastroretentive mucoadhessive tablet which can retain the drug in the stomach for prolonged duration and to achieve therapeutic levels over an extended period of time for the treatment of myelogenous leukemia (CML) and gastro intestinal stromal tumor (GIST). Single unit formulations containing carbopol 974P or sodium carboxy methyl cellulose (MC) which helps the drug in adhering to the gastric mucosa for an extended period of time were formulated and evaluated. Gastroretentive tablets of IM were prepared by direct compression. The results obtained showed no physicochemical incompatibility between the drug and other excipients used in the formulations. The prepared tablets were evaluated by different parameters such as thickness, weight variation, hardness, content uniformity, swelling index and mucoadhesive strength. Indigenously fabricated assembly was used to measure the bioadhesive strength of the mucoadhesive tablets, and goat gastric mucosa was used as a model tissue. Bioadhesive strength increased with increasing the amounts of carbopol 974P and sodium CMC in the formulations. The physicochemical compatibility of the drug with other excipients used in the formulations was studied by FTIR analysis. The tablets were also evaluated for in vitro drug release in 0.1N HCl for 12 h in USP Type II dissolution apparatus. In order to determine the mode of release, the data was fitted into various kinetic models and the optimised formulation followed Korsmeyer peppas model and the ‘n’ value was greater than one indicated super case II mechanism of drug release. The radiographic pictures of the rabbits confirm the in vivo mucoadhesion in the stomach for 6 h.