Cabana B E, Taggart J G
Antimicrob Agents Chemother. 1973 Apr;3(4):478-83. doi: 10.1128/AAC.3.4.478.
Comparative studies in beagle dogs suggested that the pharmacokinetic profiles of BB-K8 and kanamycin are similar. After intravenous (iv) administration to dogs, BB-K8 and kanamycin were rapidly distributed in plasma and tissue fluids; their "apparent" volumes of distribution comprised approximately 23% of the total body volume. Like kanamycin, BB-K8 had a plasma half-life of about 0.8 h which paralleled the urinary excretion rate. Approximately 92% of the dose was excreted as unchanged drug within 6 h of dosing, and clearance appeared to be primarily by glomerular filtration. After intramuscular (im) administration to dogs, BB-K8 and kanamycin were totally and rapidly absorbed; peak concentrations in the plasma occurred 0.5 to 1.0 h after dosing. The kinetic parameters governing the distribution and elimination of BB-K8 and kanamycin after an im dose were similar to those obtained for iv dosing and indicate desirable dose-independent kinetics. A human pharmacokinetic study indicated that the kinetic profiles of BB-K8 and kanamycin are similar in man after im dosing. Like kanamycin, BB-K8 is rapidly absorbed, yielding peak serum concentrations of about 20 mug/ml at 1 h after a 500-mg im dose. The plasma half-life of these two drugs was approximately 2.3 h. Clearance in man was primarily by glomerular filtration, and the urinary excretion of BB-K8 and kanamycin accounted for 83% of the dose.
对比格犬的比较研究表明，BB-K8和卡那霉素的药代动力学特征相似。给犬静脉注射后，BB-K8和卡那霉素迅速分布于血浆和组织液中；它们的“表观”分布容积约占总体积的23%。与卡那霉素一样，BB-K8的血浆半衰期约为0.8小时，这与尿排泄率平行。给药后6小时内，约92%的剂量以原形药物排出，清除似乎主要通过肾小球滤过。给犬肌肉注射后，BB-K8和卡那霉素完全且迅速吸收；给药后0.5至1.0小时血浆中出现峰值浓度。肌肉注射剂量后，控制BB-K8和卡那霉素分布和消除的动力学参数与静脉注射给药时获得的参数相似，表明具有理想的非剂量依赖性动力学。一项人体药代动力学研究表明，肌肉注射给药后，BB-K8和卡那霉素在人体中的动力学特征相似。与卡那霉素一样，BB-K8迅速吸收，500毫克肌肉注射剂量后1小时血清峰值浓度约为20微克/毫升。这两种药物的血浆半衰期约为2.3小时。人体清除主要通过肾小球滤过，BB-K8和卡那霉素的尿排泄占剂量的83%。
