Functional coating of linezolid microcapsules for taste-masking and associated formulation for oral administration

Abstract

The present invention provides taste-masked microcapsules of Linezolid or the like (any member of the orally effective oxazolidinone or macrolide antibiotics), suitable for oral administration as a suspension, a fast-disintegrating, effervescent or chewable tablet, and more specifically relates to such oral dosage forms in which the bitter taste of Linezolid contained therein is masked by a combination of microencapsulation by solvent coacervation and subsequent functional membrane coating on said microcapsules. The taste-masked granules thus obtained release less than 5%, most preferably less than 3%, at a pH of 4.0 to 6.0 (pH of the saliva) but rapidly release (as a burst) at pHs of the upper intestinal tract. The taste-masked granules are optionally blended with other pharmaceutically acceptable excipients and filled into unit dose containers or compressed into fast-disintegrating/effervescent/chewable tablets. The contents of the Linezolid unit dose containers are suspended in an aqueous medium prior to oral administration to pediatric and geriatric patients, who are unwilling and/or find it difficult to swallow Linezolid tablets. In contrast, fast-disintegrating tablets on administration without water rapidly disperse into taste masked granules in the mouth.