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抗酸剂对吲哚美辛生物利用度的影响。

The effect of an antacid on the bioavailability of indomethacin.

作者信息

Galeazzi R L

出版信息

Eur J Clin Pharmacol. 1977 Aug 17;12(1):65-8. doi: 10.1007/BF00561407.

Abstract

The biovailability of indomethacin from two indomethacin-antacid (aluminum hydroxide magnesium carbonate and magnesium hydroxide) combinations was compared with the bioavailability of oral indomethacin. Relative bioavailability was estimated by three methods: comparison of plasma concentrations at various times, comparison of areas under plasma concentration time curves, and comparison of the amount of drug excreted unchanged in the urine. A double blind three-way crossover study was conducted in twelve healthy volunteers. The combination with the slightly smaller amount of antacid (preparation A) showed significantly decreased bioavailability by all three methods in comparison with indomethacin alone (preparation C). The combination with the larger amount of antacid (preparation B) was also less bioavailable than preparation C. This effect was significantly only for the comparison of areas under curves and not for plasma levels, although the mean plasma levels produced by preparation B at all times were lower than those for preparation C. These findings suggest that aluminum hydroxide magnesium carbonate and magnesium hydroxide decrease the bioavailability of indomethacin.

摘要

将两种消炎痛-抗酸剂(氢氧化铝碳酸镁和氢氧化镁)组合制剂中消炎痛的生物利用度与口服消炎痛的生物利用度进行了比较。通过三种方法估算相对生物利用度:不同时间血浆浓度的比较、血浆浓度-时间曲线下面积的比较以及尿液中未变化排泄的药物量的比较。在12名健康志愿者中进行了一项双盲三交叉研究。与单独使用消炎痛(制剂C)相比,抗酸剂用量略少的组合(制剂A)通过所有三种方法显示生物利用度显著降低。抗酸剂用量较大的组合(制剂B)的生物利用度也低于制剂C。这种效应仅在曲线下面积比较时显著,而在血浆水平比较时不显著,尽管制剂B在所有时间产生的平均血浆水平均低于制剂C。这些发现表明,氢氧化铝碳酸镁和氢氧化镁会降低消炎痛的生物利用度。

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