Lentzen H, Kölle E U, Daschner F
Arzneimittelforschung. 1981;31(11):1967-71.
In a comparative study absorption and elimination characteristics of p.o. administered paromomycin and neomycin were investigated in healthy volunteers and patients with liver cirrhosis and/or portocaval shunt. Serum and urine concentrations were determined by means of the diffusion test. 1. In a cross-over study 6 volunteers were each administered single p.o. doses of 14.28 g paromomycin sulfate (= 10 g free base = 1.6 X 10(-2) mol) and 16 g neomycin sulfate (= 10.65 g free base = 1.7 X 10(-2) mol). Following these virtually equimolar doses AUC values of neomycin were 2.5 times as high as those of paromomycin (p less than 0.01). Paromomycin serum level time courses could be described by an open one-compartment model with a mean half-life of 2.6 h (harmon. mean). Mean computed maximum levels of 3.6 microgram/ml appeared on an average of 1.9 h after administration. After 32 h the mean recovery in urine was 0.2%. 5 volunteers showed a similar behavior with a mean excretion of 0.1%, whereas one person excreted 0.8% in urine. The time course of neomycin was evaluated according to an open two-compartment model with a distribution half-life of 1.5 h and a terminal half-life of 9 h (harmon. means). Mean computed maximum levels of 5.1 microgram/ml appeared on an average of 2.6 h after administration. The mean lag time was 1.3 h. 32 h after administration 0.3% of the dose were detected in urine. 2. Patients with cirrhosis and/or portocaval shunt were treated with 8 capsules/d of either 357.1 mg paromomycin sulfate or 250 mg neomycinsulfate each over a period of 7 days. Despite the lower dose of neomycin comparable serum levels of both aminoglycosides were observed. This result can be explained by a lower elimination rate and a higher extent of accumulation of neomycin. Mean amounts excreted in the urine of the 7th day were 0.1% for paromycin and 0.2% for neomycin.
在一项比较研究中，对健康志愿者以及肝硬化和/或门腔分流患者口服巴龙霉素和新霉素后的吸收和消除特性进行了研究。血清和尿液浓度通过扩散试验测定。1. 在一项交叉研究中，给6名志愿者每人单次口服14.28克硫酸巴龙霉素（=10克游离碱 = 1.6×10⁻²摩尔）和16克硫酸新霉素（=10.65克游离碱 = 1.7×10⁻²摩尔）。给予这些几乎等摩尔剂量后，新霉素的AUC值是巴龙霉素的2.5倍（p<0.01）。巴龙霉素血清水平的时间过程可用开放的一室模型描述，平均半衰期为2.6小时（调和均值）。给药后平均1.9小时出现计算得出的平均最大水平3.6微克/毫升。32小时后尿液中的平均回收率为0.2%。5名志愿者表现出类似行为，平均排泄率为0.1%，而一人尿液排泄率为0.8%。新霉素的时间过程根据开放的二室模型评估，分布半衰期为1.5小时，终末半衰期为9小时（调和均值）。给药后平均2.6小时出现计算得出的平均最大水平5.1微克/毫升。平均滞后时间为1.3小时。给药32小时后，在尿液中检测到0.3%的剂量。2. 对肝硬化和/或门腔分流患者，分别给予每天8粒胶囊，每粒含357.1毫克硫酸巴龙霉素或250毫克硫酸新霉素，持续7天。尽管新霉素剂量较低，但观察到两种氨基糖苷类药物的血清水平相当。这一结果可通过新霉素较低的消除率和较高的蓄积程度来解释。第7天尿液中排出的平均量，巴龙霉素为0.1%，新霉素为0.2%。
