Effects of an Al3+- and Mg2+-containing antacid, ferrous sulfate, and calcium carbonate on the absorption of nemonoxacin (TG-873870) in healthy Chinese volunteers
Effects of an Al3+- and Mg2+-containing antacid, ferrous sulfate, and calcium carbonate on the absorption of nemonoxacin (TG-873870) in healthy Chinese volunteers
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含 Al3 和 Mg2 的抗酸剂、硫酸亚铁和碳酸钙对中国健康志愿者吸收奈诺沙星 (TG-873870) 的影响
DOI：
10.1038/aps.2014.95
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发表时间：
2014
影响因子：
1.5
通讯作者：
D. Zhong
中科院分区：
文献类型：
--
作者：
Yifan Zhang;Xiao;Ting Wang;Xiaoyan Chen;Li Liang;Hua Qiao;Cheng;Li;Ping;Chiung;Yu;Chen;D. Zhong
目的：评价含Al~(3+)和Mg~(2+)的抗酸剂、硫酸亚铁和碳酸钙对尼莫沙星在健康人体内吸收的影响。方法：24名中国健康男性志愿者，每组12人，采用单剂量、开放标签、随机、交叉试验。在研究1中，受试者单独口服尼莫沙星(500 Mg)，或在服用抗酸剂前2小时、同时或之后4小时口服尼莫沙星(含318毫克铝和496毫克镁)。结果：尼莫沙星与碳酸钙合用后，尼莫沙星的血药浓度-时间曲线下面积(AUC0-∞)下降80.5%，最大血药浓度(Cmax)下降77.8%，尿回收率(Ae)下降76.3%。给药后4h给药，尼莫沙星的AUC0-∞降低58.0%，Cmax降低52.7%，Ae降低57.7%。在抗酸剂前2 h给药不影响尼莫沙星的吸收。结论：金属离子、Al~(3+)、Mg~(2+)、Fe~(2+)均能显著降低中国健康男性对尼莫沙星的吸收。结论：金属离子、Al~(3+)、Mg~(2+)、Fe~(2+)均可使健康男性体内的AUC_0-∞下降17.8%，C_(Max)下降14.3%，Ae下降18.4%。结论：金属离子、Al~(3+)、Mg~(2+)、Fe~(2+)均能显著降低中国健康男性体内的吸收。为避免含Al~(3+)、Mg~(2+)药物的影响，应在服药前2 h≥给予尼莫沙星。
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 (AUC0–∞) for nemonoxacin by 80.5%, the maximum concentration (Cmax) by 77.8%, and urine recovery (Ae) by 76.3%. Administration of nemonoxacin 4 h after the antacid decreased the AUC0–∞ for nemonoxacin by 58.0%, Cmax 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 AUC0–∞ by 63.7%, Cmax by 57.0%, and Ae by 59.7%, while concomitant administration of nemonoxacin with calcium carbonate mildly decreased AUC0–∞ by 17.8%, Cmax 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.
抗酸剂与新喹诺酮类药物的相互作用：基于环丙沙星、加替沙星、诺氟沙星和金属阳离子临床数据的药代动力学模型的剂量方案建议。
DOI：
--
发表时间：
2007
期刊：
International Journal of Clinical Pharmacology and Therapeutics 45
影响因子：
--
作者：
K.Miyata;H.Ohtani;M.Tsujimoto;Y.Sawada
通讯作者：
Y.Sawada