Busch U, Heinzel G, Narjes H, Nehmiz G
Department of Pharmacokinetics, Karl Thomae GmbH, Biberach/Riss, Germany.
J Clin Pharmacol. 1996 Jan;36(1):79-84. doi: 10.1002/j.1552-4604.1996.tb04155.x.
Meloxicam is a new enol carboxamide nonsteroidal antiinflammatory drug (NSAID). Preclinical studies have indicated that it possesses a high antiinflammatory potency and a low ulcerogenic potency. This open, randomized, crossover study was conducted to examine the effects of aspirin, the antacid Maalox (Rhone-Poulenc Rorer, Cologne, Germany), and cimetidine on the pharmacokinetics and bioavailability of a single oral dose of meloxicam 30 mg in healthy male volunteers. Plasma concentrations of meloxicam were determined and subjected to noncompartmental pharmacokinetic analysis. Meloxicam was well tolerated, and concomitant treatment with cimetidine or Maalox had little or no effect on the plasma concentration-time curves, maximum plasma concentration (Cmax), or the area under the plasma concentration-time curve (AUC0-infinity) of meloxicam. Concurrent treatment with aspirin increased plasma concentrations of meloxicam, increasing Cmax by approximately 25% and AUC0-infinity by 10%. These differences were not considered to be clinically relevant, and no adjustments of meloxicam dose should be required with coadministration of aspirin, Maalox, or cimetidine.
美洛昔康是一种新型的烯醇羧酰胺类非甾体抗炎药（NSAID）。临床前研究表明，它具有高抗炎效力和低致溃疡效力。本开放性、随机、交叉研究旨在考察阿司匹林、抗酸剂马洛昔（Rhone-Poulenc Rorer公司，德国科隆）和西咪替丁对健康男性志愿者单次口服30mg美洛昔康的药代动力学和生物利用度的影响。测定了美洛昔康的血浆浓度，并进行非房室药代动力学分析。美洛昔康耐受性良好，与西咪替丁或马洛昔同时治疗对美洛昔康的血浆浓度-时间曲线、最大血浆浓度（Cmax）或血浆浓度-时间曲线下面积（AUC0-∞）几乎没有影响。与阿司匹林同时治疗可提高美洛昔康的血浆浓度，使Cmax增加约25%，AUC0-∞增加10%。这些差异被认为无临床相关性，与阿司匹林、马洛昔或西咪替丁合用时无需调整美洛昔康剂量。
