Studies of Erythromycin Maltobionate, a New Derivative of Erythromycin

Abstract

Erythromycin maltobionate, a new water-soluble derivative of erythromycin, was prepared, and its physicochemical and biological properties were evaluated. The derivative has considerable solubility in organic solvents. Its partition coefficient data in different organic solvent-water systems indicate it is possibly well distributed in various tissues in vivo. Antimicrobial potency in vitro of the derivative is 589 μg/mg, and its antimicrobial spectrum is comparable to that of the parent antibiotic. The LD₅₀ value of the new derivative in mice intraperitoneally is 244.7 mg/kg. Results of this and the previous investigation of pharmacokinetics and protein binding indicate that the new derivative erythromycin maltobionate has a potential for possible clinical application.