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

作　　者：Yi-fan ZHANG Xiao-jian DAI Ting WANG Xiao-yan CHEN Li LIANG Hua QIAO Cheng-yuan TSAI Li-wen CHANG Ping-ting HUANG Chiung-yuan HSU Yu-ting CHANG Chen-en TSAI Da-fang ZHONG 

机构地区：[1]Shanghai Institute of Mateda Medica, Chinese Academy of Sciences, Shanghai 201203, China [2]The First Hospital Affiliated to Lanzhou University, Lanzhou 730000, China [3]TaiGen Biotechnology Co Ltd, Taipei 11470, Taiwan, China

出　　处：《Acta Pharmacologica Sinica》2014年第12期1586-1592,共7页中国药理学报（英文版）

摘　　要：Aim： To evaluate the effects of an AI3＋- 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 80o5%, 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.Aim： To evaluate the effects of an AI3＋- 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 80o5%, 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.

关 键 词：nemonoxacin nonfluorinated quinolone drug-drug interaction ANTACID ferrous sulfate calcium carbonate drug absorption clinical pharmacokinetics 

分 类 号：TQ138.11[化学工程—无机化工] TQ132.32