PREPARATION AND EVALUATION OF ERYTHROMYCIN FUMARATE - A NEW DERIVATIVE OF ERYTHROMYCIN

Erythromycin fumarate, a new water-soluble derivative of erythromycin, was prepared and its physicochemical and biological properties were e valuated. The derivative also has consider-able solubility in organic solvents. Its partition coefficient data in different organic solvent- water systems may indicate that it is well-distributed in various tiss ues in vivo. Antimicrobial potency in vitro of the derivative, 725 mu g/mg, is much higher than that of the existing derivatives and its ant imicrobial spectrum is comparable to that of the parent antibiotic. Th e LD50 value of the new derivative in mice intraperitoneally is 402.7 mg/kg. Results of this and the previous investigation on pharmacokinet ics and protein binding indicate that erythromycin fumarate has high p otential for possible clinical application and further investigation m ay be undertaken.