【摘要】 <正> 乙基西索米星为一新的半合成氨基糖苷抗生素类,对需氧革蓝氏阴性杆菌具有良好抗菌作用,尤其是某些庆大霉素、妥布拉霉素耐药菌株对其仍可呈现敏感;对产酶金葡菌亦具有高度抗菌活性。乙基西索米星的另一突出优点是它在氨基糖苷抗生素类中是耳、肾毒性发生率最低者。1976年国外由西索米星半合成本品,1980～1981年较大规模进行了临床应用,治疗敏感革蓝氏阴性杆菌感染安全而有效,国内目前正在研制中。本文报告乙基西索米星首次在国内应用于健康志愿者的药物代谢动力学研究,以及据此而拟定的给药方案,旨在为今后此药临床安全有效应用提供可靠的科学依据。更多还原

【Abstract】 Clinical pharmacological study was carried out in normal volunteers. 10 healthy volunteers were given a single dose of 2mg/kg of netromycin(ethylsisomicin) by IM injection and IV infusion. Serum and urine samples were obtained at regular interval and the drug concentrations were assayed.The mean peak serum concentrations of netromycin were 7.63±1.31 and 14.08±2.87μg/ ml, the t~1/2α being 0.83h and 0.35h after IM injection and Ⅳ infusion respectively. The elimination half lives were around 2h after both routes of administration. The observed and expected values of serum concentrations after IM injection and Ⅳ infusion were very similar,the correlation coefficient being 0.9644 and 0.9756 respectively. The bioavailability of netromycin after IM injection was 95.92%.Netromycin was rapidly excreted in urine, the urinary recovery rate within 24 hours after the administration being around 85%.Based on the above data and the antibacterial activity of netromycin, we suggest a therapeutic regimen to be d in the treament of various infections.更多还原