Enhancement of the in-vitro controlled-release of nimesulide from alginate-based matrix devices

Abstract

ABSTRACT: The goal of this paper is to develop an alginate-based matrix device to control the release rate of a very poorly soluble drug such as nimesulide for 12h. The molecular weight and degree of substitution of the polymer were determined by capillary viscometry and conductimetry, respectively. The compaction behavior was determined using the Heckel and Leuenberger analyses. The intrinsic dissolution was conducted on an Apparatus II dissolutor using a pH 6.8 phosphate buffer. Matrixes containing 100 mg of nimesulide and different levels of sodium alginate and electrolytes or surfactants were made on a single punch tablet machine. Matrixes containing benzalconium chloride at levels >300mg improved the solubility and the release profile of nimesulide. Conversely, sorbitan laurate, sodium lauryl sulfate and electrolytes such as sodium chloride failed to improve the release rate of nimesulide from the hydrophilic matrix. The release characteristics of nimesulide from these matrixes were best described by the Korschmeyer-Peppas model. The alginate-based system containing benzalconium chloride has a potential to improve and control the release characteristics of nimesulide within 12h.