Microparticulation of Levofloxacin HCl by Crystallo-co-agglomeration Technique

Abstract

Particle engineering techniques have gained a unique place in the present pharma industry to improve physicochemical properties of the drugs. The aim of this research work was to formulate and evaluate directly compressible agglomerates of Levofloxacin HCl with a view to improve their micromeritic properties and thereby to reduce the cost of production. Fluoroquinolone anti-infective, is used to treat bacterial conjunctivitis, sinusitis, chronic bronchitis, community- acquired pneumonia and pneumonia caused by penicillin resistant strains of Streptococcus pneumonia. Some of the fluoroquinolone high dose’s exhibit poor compressibility and flow properties, hence may not be suitable candidate for direct compression process, but by applying the crystallo-co-agglomeration (CCA) technique, the attempt may be made to change the properties of these molecules to make them suitable candidates for direct compression. This investigation was aimed to utilize CCA process to develop spherical agglomerates of levofloxacin HCl in selected polymers in different ratio. The developed spherical agglomerates of levofloxacin HCl may exhibit improved micrometric and dissolution properties hence may be suitable for direct compression process. Results indicated that micromeritic, mechanical and compressional properties of the agglomerates were greatly influenced by nature and type of polymer incorporated. The mean release time, mean dissolution time, dissolution efficiency, Q30 and Q90 of the tablets prepared from agglomerates showed remarkable increase in CCA compared to tablets prepared by wet granulation. Observations also revealed that by varying the type and concentration of polymer, desired release rate can be obtained.