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Please use this identifier to cite or link to this item: http://hdl.handle.net/10481/26298

Title: 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
Other Titles: Estudio in vitro de dos polímeros utilizados en sistemas flotantes de mesilato para leucemia mielógena crónica
Authors: Vinod, Kombath R.
Santosh, Vasa
Sandhya, Subhadra
Otilia, Banji J.
David, Banji
Padmasri, Anugu
Issue Date: 2012
Abstract: 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.
Objetivo. El propósito de este trabajo ha sido elaborar un sistema de liberación gástrica de mesilato de imatinib. Material y Método. Se han elaborado comprimidos flotantes de mesilato de imatinib empleando HPMC K4M y HPMC K15M junto con excipientes efervescentes. Los excipientes celulósicos fueron seleccionados según su capacidad de formación de estructuras de gel y controladores de cesión. El bicarbonato de sodio se incorporó como agente efervescente. Se evaluaron la capacidad flotante de los comprimidos, uniformidad de peso, dureza, friabilidad, riqueza y velocidad de disolución. Resultados. Las formulaciones seleccionadas demostraron tener buenas propiedades físico-químicas incluyendo buena capacidad de flotación con un aumento de tamaño por captación de agua durante su disolución. Los comprimidos pueden flotar durante más de 12 horas. Los comprimidos con HPMC K4M tienen mayor capacidad de flotación que los obtenidos con HPMC K15M. Se puede controlar satisfactoriamente la cesión del fármaco. En un ensayo in vivo se ha demostrado que los comprimidos pueden estar 6 horas en el estómago. Conclusión: La retención gástrica de la unidad de mesilato de imatinib se hace utilizando sistemas flotantes. HPMC K4 dio una mejor liberación, hasta el 98,4% en 12 horas. Todos los comprimidos flotantes gastroretentivo mostraron una buena flotación durante el período de liberación del fármaco.
Publisher: Universidad de Granada, Facultad de Farmacia
Keywords: Imatinib mesylate
Mesilato de imatinib
Gastroretention
Gastroretención
Floating tablets
Comprimidos flotantes
In vitro buoyancy
Flotabilidad in vitro
URI: http://hdl.handle.net/10481/26298
ISSN: 0004-2927
Rights : Creative Commons Attribution-NonCommercial-NoDerivs 3.0 License
Citation: Vinod, K.R.; et al. 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. Ars Pharm. 2012; 53(4): 01-07. [http://hdl.handle.net/10481/26298]
Appears in Collections:APh, vol. 53(4)

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