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口服含八硫酸蔗糖铋、碱式水杨酸铋和枸橼酸铋钾制剂后,Sprague-Dawley大鼠对铋的吸收比较

Comparative absorption of bismuth in Sprague-Dawley rats following oral administration of preparations containing bismuth sucrose octasulfate, bismuth subsalicylate, and bismuth subcitrate.

作者信息

Rao N, Brown P W, Yerino P, Chang J, Hwang K K

机构信息

Department of Clinical Pharmacokinetics, Hoechst Marion Roussel, Kansas City, MO 64137, USA.

出版信息

Biopharm Drug Dispos. 1997 Jan;18(1):1-8. doi: 10.1002/(sici)1099-081x(199701)18:1<1::aid-bdd996>3.0.co;2-0.

DOI:10.1002/(sici)1099-081x(199701)18:1<1::aid-bdd996>3.0.co;2-0
PMID:9008264
Abstract

The absorption of bismuth from De-Nol (bismuth subcitrate, DN), Pepto-Bismol (bismuth subsalicylate, PB) and bismuth sucrose octasulfate (BISOS) was examined in male Sprague-Dawley rats after a single oral dose of each compound (60mg bismuth). Bismuth was analysed in blood, urine, kidney, brain, liver, and lung using graphite furnace atomic absorption spectrophotometry. Bismuth Cmax averaged 18.4 +/- 11.6 ng mL(-1) for BISOS, 292 +/- 130 ng mL(-1) for DN, and 21.5 +/- 9.63 ng mL(-1 ) for PB. Cmax was significantly lower for BISOS compared to DN (p<0.05) but not significantly different for BISOS compared to PB (p > 0.05). Bismuth AUC was 1356 +/- 474 ng h(-1) mL (-1) for BISOS, 2129 +/- 452 ng h(-l) mL(-1) for DN, and 1824 +/- 919 ng h(-1) for PB, which indicated a lower extent of absorption from BISOS compared to DN. Kidney, liver, and lung levels of bismuth were also significantly lower for BISOS compared to DN (p < 0.05). Bismuth urinary excretion was significantly lower for BISOS (0.04 +/- 0.02%) compared to DN (0.27 +/- 0.15%) but not significantly different compared to PB (0.07 +/- 0.03%). These data suggest that the absorption of bismuth following oral administration of bismuth sucrose octasulfate is significantly lower than that from De-Nol and similar to that from Pepto-Bismo.

摘要

在雄性斯普拉格 - 道利大鼠单次口服给予每种化合物(60mg铋)后,检测了来自得乐(枸橼酸铋,DN)、必奇(碱式水杨酸铋,PB)和蔗糖八硫酸铋(BISOS)的铋吸收情况。使用石墨炉原子吸收分光光度法分析血液、尿液、肾脏、大脑、肝脏和肺中的铋。BISOS的铋Cmax平均为18.4±11.6 ng mL⁻¹,DN为292±130 ng mL⁻¹,PB为21.5±9.63 ng mL⁻¹。与DN相比,BISOS的Cmax显著更低(p<0.05),但与PB相比无显著差异(p>0.05)。BISOS的铋AUC为1356±474 ng h⁻¹ mL⁻¹,DN为2129±452 ng h⁻¹ mL⁻¹,PB为1824±919 ng h⁻¹,这表明与DN相比,BISOS的吸收程度更低。与DN相比,BISOS在肾脏、肝脏和肺中的铋水平也显著更低(p<0.05)。与DN(0.27±0.15%)相比,BISOS的铋尿排泄显著更低(0.04±0.02%),但与PB(0.07±0.03%)相比无显著差异。这些数据表明,口服蔗糖八硫酸铋后铋的吸收显著低于得乐,与必奇相似。

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