Abstract

The objective of this investigation was to develop an oral sustained release formulation of linezolid that would maximize the duration of active drug concentration in the extracellular fluid, thus assuring the therapeutic efficacy. This rationale was based on the observation that the an efficacy of linezolid depends mainly on the length of time that bacteria are exposed to antibiotic concentrations above the minimum inhibitory concentration (T>MIC). linezolid sustained release tablets were prepared by wet granulation method. A full factorial design for two-factor three levels was employed systematically to optimize drug release profile at 1, 4, 8 and 16 h. Film-coated sustained release matrix tablet exhibited fickian diffusion drug release kinetics approaching Higuchi model. The significance of the results was analyzed using analysis of non-variance (ANOVA) and P MIC for at least 24 hours.

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