Synthesis And Preformulation Studies Of A Prodrug Of Lomefloxacin
A prodrug of lomefloxacin was synthesized by reacting the free base with aqueous formaldehyde solution in a 1:1 mixture of methylene chloride and methanol. The colourless, crystalline N-hydroxy methyl derivative, m.p. 220o showed a two-fold increase in solubility and a three fold increase in the dissolution rate over the parent drug. The degradation kinetics, pH-rate profile, antimicrobial activity, LD50 and physical characteristics such as particle size distribution, angle of repose of the prodrug were studied. The prodrug showed increased solubility and dissolution and gets easily converted to parent drug.