Berg M J, Rose J Q, Wurster D E, Rahman S, Fincham R W, Schottelius D D
Ther Drug Monit. 1987;9(1):41-7. doi: 10.1097/00007691-198703000-00008.
The effects of two different oral charcoal suspensions on the elimination of a 200 mg/70 kg, 1 h intravenous (i.v.) infusion of phenobarbital and the tolerances of the two regimens were determined in a randomized crossover study in six healthy male volunteers. Phenobarbital was given i.v. alone or together with 105 g of oral activated charcoal suspension or with 105 g of a commercially available sorbitol-charcoal suspension over a 36-h period. A 13-34% decrease in the area under the serum concentration time curve (AUC) for 0-60 h occurred with the administration of the activated charcoal, and a 19-52% decrease occurred with the commercial sorbitol-charcoal regimen. The mean apparent systemic clearance of total phenobarbital increased from 0.089 +/- 0.019 ml/min/kg to 0.141 +/- 0.029 and 0.146 +/- 0.036 ml/min/kg with the charcoal and sorbitol-charcoal treatments, respectively. No significant change in the fraction of phenobarbital bound to protein was detected. The charcoal regimen caused constipation in one subject. All subjects taking the sorbitol-charcoal preparation experienced diarrhea; there were no changes in electrolytes with either charcoal suspension. All subjects preferred the sorbitol-charcoal preparation.
在一项针对6名健康男性志愿者的随机交叉研究中,测定了两种不同口服活性炭混悬液对消除静脉注射(i.v.)200 mg/70 kg苯巴比妥1小时后的影响以及两种给药方案的耐受性。在36小时内,单独静脉注射苯巴比妥,或与105 g口服活性炭混悬液或与105 g市售山梨醇 - 活性炭混悬液一起给药。给予活性炭后,0 - 60小时血清浓度 - 时间曲线下面积(AUC)降低了13 - 34%,而市售山梨醇 - 活性炭给药方案使AUC降低了19 - 52%。总苯巴比妥的平均表观全身清除率在活性炭治疗时从0.089±0.019 ml/min/kg增加到0.141±0.029 ml/min/kg,在山梨醇 - 活性炭治疗时增加到0.146±0.036 ml/min/kg。未检测到与蛋白质结合的苯巴比妥比例有显著变化。活性炭给药方案导致一名受试者便秘。所有服用山梨醇 - 活性炭制剂的受试者均出现腹泻;两种活性炭混悬液均未引起电解质变化。所有受试者都更喜欢山梨醇 - 活性炭制剂。