Manna P K, Basu S K
Institute of Pharmaceutical Technology, Annamalai University, Annamalainagar, India.
Drug Dev Ind Pharm. 1999 Mar;25(3):391-5. doi: 10.1081/ddc-100102188.
Erythromycin maltobionate, a new water-soluble derivative of erythromycin, was prepared, and its physiochemical 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 micrograms/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.
制备了红霉素麦芽酚酯，一种红霉素的新型水溶性衍生物，并对其理化和生物学性质进行了评估。该衍生物在有机溶剂中有相当大的溶解度。其在不同有机溶剂 - 水体系中的分配系数数据表明它可能在体内各种组织中分布良好。该衍生物的体外抗菌效价为589微克/毫克，其抗菌谱与母体抗生素相当。新衍生物在小鼠腹腔内的LD50值为244.7毫克/千克。本次研究以及之前的药代动力学和蛋白结合研究结果表明，新型衍生物红霉素麦芽酚酯具有临床应用的潜力。
