Kärkkäinen S, Neuvonen P J
Int J Clin Pharmacol Ther Toxicol. 1984 Aug;22(8):441-6.
The effects of orally given activated charcoal, sodium bicarbonate and ammonium chloride on the pharmacokinetics of sotalol were studied in 7 volunteers in a randomized, cross-over study. Serum and urine concentrations of sotalol were determined by HPLC up to 72 h. Activated charcoal, 50 g, given within 5 min of sotalol hydrochloride (160 mg), reduced its absorption by 99%. When given in repeated doses from 6 h on, 50 g followed by 12.5 g at 6 h intervals, charcoal shortened the half-life after sotalol in serum from 9.4 +/- 0.4 h to 7.6 +/- 0.3 h and in urine from 9.4 +/- 0.4 h to 7.3 +/- 0.3 h (p less than 0.01). The excretion of unchanged sotalol into urine was 65% of the dose during the control phase but neither acidification nor alkalinization of urine for 3 days did increase its urinary excretion. Thus, activated charcoal seems to be effective in prevention of the absorption of sotalol when ingested without delay. Given in repeated oral doses charcoal moderately increases the rate of sotalol elimination, probably by interrupting its enterohepatic or enteroenteric circulation.
在一项随机交叉研究中,对7名志愿者研究了口服活性炭、碳酸氢钠和氯化铵对索他洛尔药代动力学的影响。采用高效液相色谱法测定索他洛尔血清和尿液浓度,测定时间长达72小时。在盐酸索他洛尔(160毫克)给药后5分钟内给予50克活性炭,可使其吸收减少99%。从6小时起重复给药,每次50克,随后每隔6小时给予12.5克,活性炭可使索他洛尔在血清中的半衰期从9.4±0.4小时缩短至7.6±0.3小时,在尿液中的半衰期从9.4±0.4小时缩短至7.3±0.3小时(p<0.01)。在对照期,未变化的索他洛尔经尿液排泄量为给药剂量的65%,但连续3天尿液酸化或碱化均未增加其经尿液排泄量。因此,活性炭似乎能有效防止索他洛尔摄入后立即被吸收。重复口服活性炭可适度提高索他洛尔的消除速率,可能是通过中断其肠肝循环或肠肠循环实现的。