Sawae Y, Okada K, Umemura K
Jpn J Antibiot. 1982 Mar;35(3):770-8.
The pharmacokinetic behavior of dibekacin was studied in 8 elderly subjects. These subjects had not apparent renal failure, although they were diagnosed as having various diseases such as arteriosclerosis, essential hypertension, etc. Dibekacin, 50 mg/subject, was infused intravenously for 1 hour. Serum and urine concentrations of dibekacin were measured by the bioassay and radioimmunoassay methods. The peak serum concentration of dibekacin ranged from 3.55 to 5.35 micrograms/ml when measured by bioassay, and from 3.19 to 8.9 micrograms/ml by radioimmunoassay. The biological half-life of dibekacin ranged from 2.13 to 3.45 hours, and from 1.57 to 3.55 hours, with these 2 methods. The area under the curve (AUC) ranged from 14.8 to 25.6 micrograms/ml-hr and from 11.3 to 18.0 microgram/ml . hr, respectively. Creatinine clearance showed a positive correlation with the elimination rate constant and a negative correlation with the distribution volume of dibekacin. These relationships were more pronounced when determined by radioimmunoassay. These data suggest that the peak serum concentration of dibekacin decreases with creatinine clearance. The serum and urine concentrations of dibekacin measured by the radioimmunoassay method correlated well with those measured by the bioassay method. Therefore, it was concluded that the radioimmunoassay method is a useful technique for monitoring the serum concentration of dibekacin.
对8名老年受试者的地贝卡星药代动力学行为进行了研究。这些受试者虽被诊断患有动脉硬化、原发性高血压等多种疾病,但并无明显肾功能衰竭。给每位受试者静脉输注50毫克地贝卡星,持续1小时。采用生物测定法和放射免疫测定法测量地贝卡星的血清和尿液浓度。通过生物测定法测得地贝卡星的血清峰值浓度为3.55至5.35微克/毫升,通过放射免疫测定法测得为3.19至8.9微克/毫升。采用这两种方法测得地贝卡星的生物半衰期分别为2.13至3.45小时和1.57至3.55小时。曲线下面积(AUC)分别为14.8至25.6微克/毫升·小时和11.3至18.0微克/毫升·小时。肌酐清除率与消除速率常数呈正相关,与地贝卡星的分布容积呈负相关。采用放射免疫测定法时,这些关系更为明显。这些数据表明,地贝卡星的血清峰值浓度随肌酐清除率降低。采用放射免疫测定法测得的地贝卡星血清和尿液浓度与采用生物测定法测得的结果相关性良好。因此,得出结论:放射免疫测定法是监测地贝卡星血清浓度的一种有用技术。