A comparative in vitro drug release prospective with two different polymers for the development of floating single unit dosage form of imatinib mesylate for chronic myelogenous leukemia
Keywords:
Imatinib mesylate, gastroretention, floating tablets, in vitro buoyancyAbstract
Aim: The purpose of this investigation was to prepare a gastroretentive drug delivery system of Imatinib mesylate.
Materials and Method: Floating tablets of imatinib mesylate were prepared employing HPMC K4M and HPMC K15M by effervescent technique; these grades of HPMC were evaluated for their gel forming properties. Sodium bicarbonate was incorporated as a gas-generating agent. The floating tablets were evaluated for uniformity of weight, hardness, friability, drug content, in vitro buoyancy and dissolution studies.
Results: The prepared tablets exhibited satisfactory physico-chemical characteristics. All the prepared batches showed good in vitro buoyancy. The tablet swelled radially and axially during in vitro buoyancy studies. It was observed that the tablet remained buoyant for >12 hours. The tablets with HPMC K4M were found to float for longer duration as compared with formulations containing HPMC K15M. The drug release from the tablets was sufficiently sustained and non-Fickian transport of the drug from tablets was confirmed. From the radiographic pictures obtained at different time intervals, it has been proved that that the tablet was floating during the observed time intervals up to 6h against all peristaltic movements.
Conclusion: Gastric retention of Imatinib mesylate unit dosage form was achived by floatation. HPMC K4 gave better release up to 98.4% in 12 hrs. All the gastroretentive floating tablets showed good floatation during the period of drug release, and the drug release was found to follow non-fickian diffusion type.
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