Roberts J R, Gracely E J, Schoffstall J M
Department of Emergency Medicine, Mercy Catholic Medical Center, Philadelphia, PA, USA.
Acad Emerg Med. 1997 Mar;4(3):167-74. doi: 10.1111/j.1553-2712.1997.tb03735.x.
To compare the abilities of low-surface-area (LSA) vs 2 types of high-surface-area (HSA) activated charcoal given orally to adsorb acetaminophen in the gastrointestinal (GI) tract, as demonstrated by the impact of these agents on the serum levels and area under the curve (AUC) in a simulated human overdose model.
The main arm of the study was a prospective double-blind crossover trial in which 6 volunteers, serving as their own controls, ingested acetaminophen (50 mg/kg), followed randomly in 10 minutes by either powdered LSA charcoal (950 m2/g) or powdered HSA charcoal (2,000 m2/g) in a charcoal:drug ratio of 8:1. In a second arm of the study, 3 subjects additionally ingested an equal dose of a granular preparation of the HSA charcoal. Serial serum acetaminophen levels were analyzed at various intervals (30, 60, 90, 120, 180, 240, and 300 minutes postingestion), and a 5-hour AUC was calculated. The subjects also rated the charcoal preparations for palatability.
Serum acetaminophen levels were lower at all measured times in the groups receiving both forms of the HSA charcoal vs the LSA product. With the powdered HSA charcoal, comparison serum levels were significantly lower at 120 minutes postingestion and all times thereafter (p < 0.05), reaching high significance at 4 and 5 hours (p < 0.001). The subjects receiving the granular HSA charcoal also had consistently lower serum acetaminophen levels than did those receiving the LSA product, and the difference in mean serum levels was significant at the 4- and 5-hour sample (p = 0.012). Compared with the LSA charcoal, at the 4-hour postingestion sample, serum acetaminophen levels were reduced by 44% to 85% by the powdered HSA charcoal. The total AUC for the 5-hour study period was also significantly reduced by the powdered HSA product (p = 0.005) and the granular HSA product (p = 0.043). All the subjects rated the powdered HSA charcoal to be more palatable and easier to drink than the powdered LSA charcoal.
The surface area of oral activated charcoal is a major determining factor in its ability to limit acetaminophen absorption and to fulfill its adsorptive role in GI decontamination. In a human acetaminophen overdose model, 2 types of HSA charcoal, when compared with equal doses of LSA charcoal, significantly reduced serum levels and total acetaminophen absorption as measured by the AUC.
在模拟人体过量服药模型中，通过观察低比表面积（LSA）活性炭与两种高比表面积（HSA）活性炭对血清水平及曲线下面积（AUC）的影响，比较口服这两种活性炭在胃肠道吸附对乙酰氨基酚的能力。
该研究的主要部分是一项前瞻性双盲交叉试验，6名志愿者作为自身对照，先服用对乙酰氨基酚（50mg/kg），10分钟后随机服用活性炭与药物比例为8:1的粉末状LSA活性炭（950m²/g）或粉末状HSA活性炭（2000m²/g）。在研究的第二部分，3名受试者额外服用了等量的颗粒状HSA活性炭。在不同时间间隔（服药后30、60、90、120、180、240和300分钟）分析血清对乙酰氨基酚水平，并计算5小时的AUC。受试者还对活性炭制剂的口感进行评分。
与LSA产品相比，接受两种形式HSA活性炭的组在所有测量时间的血清对乙酰氨基酚水平均较低。对于粉末状HSA活性炭，服药后120分钟及之后的比较血清水平显著降低（p<0.05），在4小时和5小时时差异极显著（p<0.001）。接受颗粒状HSA活性炭的受试者血清对乙酰氨基酚水平也始终低于接受LSA产品的受试者，在4小时和5小时样本中平均血清水平差异显著（p = 0.012）。与LSA活性炭相比，在服药后4小时样本中，粉末状HSA活性炭使血清对乙酰氨基酚水平降低了44%至85%。粉末状HSA产品（p = 0.005）和颗粒状HSA产品（p = 0.043）也使5小时研究期的总AUC显著降低。所有受试者都认为粉末状HSA活性炭比粉末状LSA活性炭口感更好，更易饮用。
口服活性炭的比表面积是其限制对乙酰氨基酚吸收及在胃肠道净化中发挥吸附作用能力的主要决定因素。在人体对乙酰氨基酚过量服药模型中，与等量LSA活性炭相比，两种类型的HSA活性炭显著降低了血清水平及通过AUC测量的对乙酰氨基酚总吸收量。
