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Effects of an Al3+- and Mg2+-containing antacid, ferrous sulfate, and calcium carbonate on the absorption of nemonoxacin (TG-873870) in healthy Chinese volunteers

文献类型：期刊论文

作者Zhang, Yi-fan1; Dai, Xiao-jian1; Wang, Ting3; Chen, Xiao-yan1; Liang, Li3; Qiao, Hua3; Tsai, Cheng-yuan2; Chang, Li-wen2; Huang, Ping-ting2; Hsu, Chiung-yuan2
刊名ACTA PHARMACOLOGICA SINICA
出版日期2014-12
卷号35期号:12页码:1586-1592
ISSN号1671-4083
关键词nemonoxacin nonfluorinated quinolone drug-drug interaction antacid ferrous sulfate calcium carbonate drug absorption clinical pharmacokinetics
DOI10.1038/aps.2014.95
文献子类Article
英文摘要Aim: To evaluate the effects of an Al3+-and Mg2+-containing antacid, ferrous sulfate, and calcium carbonate on the absorption of nemonoxacin in healthy humans. Methods: Two single-dose, open-label, randomized, crossover studies were conducted in 24 healthy male Chinese volunteers (12 per study). In Study 1, the subjects orally received nemonoxacin (500 mg) alone, or an antacid (containing 318 mg of Al3+ and 496 mg of Mg2+) plus nemonoxacin administered 2 h before, concomitantly or 4 h after the antacid. In Study 2, the subjects orally received nemonoxacin (500 mg) alone, or nemonoxacin concomitantly with ferrous sulfate (containing 60 mg of Fe2+) or calcium carbonate (containing 600 mg of Ca2+). Results: Concomitant administration of nemonoxacin with the antacid significantly decreased the area under the concentration-time curve from time 0 to infinity (AUC(0-infinity)) for nemonoxacin by 80.5%, the maximum concentration (C-max) by 77.8%, and urine recovery (Ae) by 76.3%. Administration of nemonoxacin 4 h after the antacid decreased the AUC(0-infinity) for nemonoxacin by 58.0%, C-max by 52.7%, and Ae by 57.7%. Administration of nemonoxacin 2 h before the antacid did not affect the absorption of nemonoxacin. Administration of nemonoxacin concomitantly with ferrous sulfate markedly decreased AUC(0-infinity) by 63.7%, C-max by 57.0%, and Ae by 59.7%, while concomitant administration of nemonoxacin with calcium carbonate mildly decreased AUC(0-infinity) by 17.8%, C-max by 14.3%, and Ae by 18.4%. Conclusion: Metal ions, Al3+, Mg2+, and Fe2+ markedly decreased the absorption of nemonoxacin in healthy Chinese males, whereas Ca2+ had much weaker effects. To avoid the effects of Al3+ and Mg2+-containing drugs, nemonoxacin should be administered >= 2 h before them.
WOS关键词NON-FLUORINATED QUINOLONE ; CIPROFLOXACIN ; GATIFLOXACIN ; PHARMACOKINETICS ; BIOAVAILABILITY ; ALUMINUM ; SAFETY ; SLEEP
WOS研究方向Chemistry ; Pharmacology & Pharmacy
语种英语
出版者ACTA PHARMACOLOGICA SINICA
WOS记录号WOS:000345912300013
源URL[http://119.78.100.183/handle/2S10ELR8/276815]  
专题上海药物代谢研究中心
通讯作者Zhong, Da-fang
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China;
2.TaiGen Biotechnol Co Ltd, Taipei 11470, Taiwan
3.Lanzhou Univ, Affiliated Hosp 1, Lanzhou 730000, Peoples R China;
推荐引用方式
GB/T 7714		 Zhang, Yi-fan,Dai, Xiao-jian,Wang, Ting,et al. Effects of an Al3+- and Mg2+-containing antacid, ferrous sulfate, and calcium carbonate on the absorption of nemonoxacin (TG-873870) in healthy Chinese volunteers[J]. ACTA PHARMACOLOGICA SINICA,2014,35(12):1586-1592.
APA Zhang, Yi-fan.,Dai, Xiao-jian.,Wang, Ting.,Chen, Xiao-yan.,Liang, Li.,...&Zhong, Da-fang.(2014).Effects of an Al3+- and Mg2+-containing antacid, ferrous sulfate, and calcium carbonate on the absorption of nemonoxacin (TG-873870) in healthy Chinese volunteers.ACTA PHARMACOLOGICA SINICA,35(12),1586-1592.
MLA Zhang, Yi-fan,et al."Effects of an Al3+- and Mg2+-containing antacid, ferrous sulfate, and calcium carbonate on the absorption of nemonoxacin (TG-873870) in healthy Chinese volunteers".ACTA PHARMACOLOGICA SINICA 35.12(2014):1586-1592.

入库方式： OAI收割

来源：上海药物研究所

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