Erythromycin maltobionate, a new water-soluble derivative of erythromycin,
was prepared, and its physicochemical and biological properties were evalua
ted. The derivative has considerable solubility in organic solvents. Its pa
rtition coefficient data in different organic solvent-water systems indicat
e it is possibly well distributed in various tissues in vivo. Antimicrobial
potency in vitro of the derivative is 589 mu g/mg, and its antimicrobial s
pectrum is comparable to that of the parent antibiotic. The LD50 value of t
he new derivative in mice intraperitoneally is 244.7 mg/kg. Results of this
and the previous investigation of pharmacokinetics and protein binding ind
icate that the new derivative erythromycin maltobionate has a potential for
possible clinical application.