Nwokolo C U, Gavey C J, Smith J T, Pounder R E
Academic Department of Medicine, Royal Free Hospital School of Medicine, London, UK.
Aliment Pharmacol Ther. 1989 Feb;3(1):29-39. doi: 10.1111/j.1365-2036.1989.tb00188.x.
Two studies measured plasma concentrations of bismuth during dosing with tripotassium dicitrato bismuthate (De-Noltab). The first study compared 24 h plasma bismuth concentration and urinary bismuth excretion in six patients who had already received 29-131 days (median 47 days) of treatment with De-Noltab 2 b.d., and six healthy subjects who only received De-Noltab 2 b.d. on the day of study. There was a prompt rise in plasma bismuth concentration after each dose of De-Noltabs. The median 24 h integrated plasma bismuth concentration was similar in both groups, but the median 24 h urinary bismuth excretion was 5.4-fold higher in the patients. The second study compared the plasma bismuth concentrations after the first and third doses of De-Noltab 2 b.d. in 16 healthy subjects. The median peak bismuth concentration occurred 30 min (range 15-105 min) post-dosing. The peak plasma bismuth concentration was greater than 50 ng/ml in 14 of the 16 subjects, and greater than 100 ng/ml in nine of the subjects. There was no significant difference in the median integrated 10-h plasma bismuth concentration after the first or third dose of De-Noltabs. The results of these studies confirm that bismuth is absorbed and sequestrated during dosing with De-Noltabs. Bismuth is absorbed rapidly after oral dosing with De-Noltabs, to produce peak plasma bismuth concentrations hitherto considered to be in the range associated with bismuth neurotoxicity.
两项研究测量了服用枸橼酸铋钾(得乐)期间的铋血浆浓度。第一项研究比较了6例已接受得乐2次/日治疗29 - 131天(中位数47天)的患者与6例仅在研究当天接受得乐2次/日治疗的健康受试者的24小时血浆铋浓度和尿铋排泄情况。每次服用得乐后,血浆铋浓度迅速升高。两组的24小时血浆铋浓度中位数相似,但患者组的24小时尿铋排泄中位数高出5.4倍。第二项研究比较了16例健康受试者在得乐2次/日服用第一剂和第三剂后的血浆铋浓度。铋浓度峰值中位数出现在给药后30分钟(范围15 - 105分钟)。16名受试者中有14名的血浆铋浓度峰值大于50 ng/ml,9名受试者大于100 ng/ml。得乐服用第一剂或第三剂后,10小时血浆铋浓度积分中位数无显著差异。这些研究结果证实,服用得乐期间铋被吸收并蓄积。口服得乐后铋吸收迅速,可产生迄今认为与铋神经毒性相关范围内的血浆铋浓度峰值。