抗酸剂对喹诺酮类药物洛美沙星吸收的影响。
Effect of antacid on absorption of the quinolone lomefloxacin.
作者信息
Shimada J, Shiba K, Oguma T, Miwa H, Yoshimura Y, Nishikawa T, Okabayashi Y, Kitagawa T, Yamamoto S
机构信息
St. Marianna University School of Medicine, Institute of Medical Science, Kanagawa, Japan.
出版信息
Antimicrob Agents Chemother. 1992 Jun;36(6):1219-24. doi: 10.1128/AAC.36.6.1219.
The effect of antacid on the absorption of lomefloxacin (LFLX) in humans was studied. When LFLX was orally administered concomitantly with aluminum- and magnesium-containing antacids under fasting conditions, its level in plasma decreased by one-half and its area under the concentration-time curve was reduced by 40% compared with the levels observed after treatment with LFLX alone. The urinary recovery value also decreased by 40%. No such effects were noted after coadministration of LFLX and a nonmetallic antacid. This study confirmed the existence of chelate complexes of LFLX with Al3+ and Mg2+ and examined the chelating strength. The stability constants of LFLX with Al3+ and Mg2+ were measured and compared with those of ofloxacin and norfloxacin; little difference was observed among them. LFLX was found to bind more strongly with Al3+ than with Mg2+. Further, the existence of chelate formation was proven by 13C-nuclear magnetic resonance spectroscopy. The decrease in the LFLX level in plasma in humans could be explained by a reduced absorption of the Al(3+)- and Mg(2+)-LFLX chelate complexes.
研究了抗酸剂对洛美沙星（LFLX）在人体中吸收的影响。在禁食条件下，当LFLX与含铝和镁的抗酸剂同时口服时，与单独使用LFLX治疗后观察到的水平相比，其血浆水平降低了一半，浓度-时间曲线下面积减少了40%。尿回收率也降低了40%。LFLX与非金属抗酸剂合用时未观察到此类影响。本研究证实了LFLX与Al3+和Mg2+螯合物的存在，并检测了螯合强度。测量了LFLX与Al3+和Mg2+的稳定常数，并与氧氟沙星和诺氟沙星的稳定常数进行比较；它们之间观察到的差异很小。发现LFLX与Al3+的结合比与Mg2+的结合更强。此外，通过13C-核磁共振光谱证实了螯合物的形成。人体血浆中LFLX水平的降低可以用Al(3+)-和Mg(2+)-LFLX螯合物吸收减少来解释。
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