Watson W A, Jenkins T C, Velasquez N, Schentag J J
J Toxicol Clin Toxicol. 1987;25(3):171-84. doi: 10.3109/15563658708992622.
Factors which determine the ability of activated charcoal to increase systemic drug clearance include adsorption characteristics, the extent of back diffusion, and biliary excretion into the gut. Orally absorbed drugs diffuse back into the gut, but it is not known whether non-absorbed agents also diffuse back. Tobramycin was studied with a highly activated charcoal to determine whether this occurs. Five volunteers received a single IV dose of tobramycin on two occasions. Using a randomized, crossover design, subjects received 10 g of activated charcoal (as SuperCharR suspension) 2 hr prior, and at 0, 2, 6, and 8 hr after tobramycin administration during one of the study days. In vitro, tobramycin adsorbed to charcoal at pH 5.6, but not at pH 2.6. A 20:1 charcoal:tobramycin ratio resulted in 34.9% of tobramycin adsorbed to activated charcoal. Blood (0-12 hr) and urine (0-24 hr) were collected and tobramycin concentrations determined. Urinary tobramycin recovery, renal and total drug clearance, half-life, and volume of distribution were calculated. There were no differences in these parameters between the two groups. We conclude that activated charcoal has no effect on tobramycin distribution or elimination in normal volunteers, and that back diffusion does not occur with this drug.
决定活性炭增加全身药物清除率能力的因素包括吸附特性、反向扩散程度以及胆汁排泄至肠道的情况。经口服吸收的药物会反向扩散至肠道,但尚不清楚未被吸收的药物是否也会发生反向扩散。本研究使用高活性的活性炭对妥布霉素进行研究,以确定是否会发生这种情况。五名志愿者分两次接受了单次静脉注射妥布霉素。采用随机交叉设计,在其中一个研究日,受试者在给予妥布霉素前2小时以及给药后0、2、6和8小时接受10克活性炭(作为SuperCharR悬浮液)。在体外,妥布霉素在pH 5.6时吸附于活性炭,但在pH 2.6时不会。20:1的活性炭与妥布霉素比例导致34.9%的妥布霉素吸附于活性炭。收集血液(0至12小时)和尿液(0至24小时)并测定妥布霉素浓度。计算尿中妥布霉素回收率、肾脏和总药物清除率、半衰期以及分布容积。两组之间这些参数没有差异。我们得出结论,活性炭对正常志愿者体内妥布霉素的分布或消除没有影响,且该药物不会发生反向扩散。