The objective of the study was to formulate and evaluate once daily, multiparticulate gastroretentive dosage form of baclofen for achieving sustained drug release, reducing side effects and frequency of administration leading to improved patient compliance. Gastroretention was achieved by designing multilayered effervescent pellets using extrusion spheronization technique. The pellet core contained balclofen, an antispastic drug used in the treatment of multiple sclerosis, as a central composite of multilayered particulate system. Sustained release and gastroretention was achieved by means of multiple coating of polymers viz. retardant coat of ethyl cellulose, effervescent layer of sodium bicarbonate and final gas entrapping layer of Eudragit®RLPO. The optimized formulation was characterized for its micromeritic properties, floating lag time, total floating time, in-vitro drug release and in-vivo floating behavior in rabbit by roentgenography. Promising results were obtained as the formulation showed sustained drug release upto 24 h during in-vitro evaluation. Radiological evidences also suggested that the gastroretention period of the floating barium sulfate-loaded pellets was not less than 10 h.
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