Manna P K, Basu S K
Institute of Pharmaceutical Technology, Annamalai University, India.
Drug Dev Ind Pharm. 1998 Sep;24(9):879-82. doi: 10.3109/03639049809088535.
Erythromycin fumarate, a new water-soluble derivative of erythromycin, was prepared and its physicochemical and biological properties were evaluated. The derivative also has considerable solubility in organic solvents. Its partition coefficient data in different organic solvent-water systems may indicate that it is well-distributed in various tissues in vivo. Antimicrobial potency in vitro of the derivative, 725 micrograms/mg, is much higher than that of the existing derivatives and its antimicrobial spectrum is comparable to that of the parent antibiotic. The LD50 value of the new derivative in mice intraperitoneally is 402.7 mg/kg. Results of this and the previous investigation on pharmacokinetics and protein binding indicate that erythromycin fumarate has high potential for possible clinical application and further investigation may be undertaken.
富马酸红霉素是红霉素的一种新型水溶性衍生物，已制备出来并对其理化性质和生物学性质进行了评估。该衍生物在有机溶剂中也有相当的溶解度。其在不同有机溶剂 - 水体系中的分配系数数据可能表明它在体内各种组织中分布良好。该衍生物的体外抗菌效力为725微克/毫克，远高于现有衍生物，其抗菌谱与母体抗生素相当。新衍生物对小鼠腹腔注射的半数致死量值为402.7毫克/千克。本次及之前关于药代动力学和蛋白结合的研究结果表明，富马酸红霉素具有很高的临床应用潜力，可进一步开展研究。
