Bartlett A, Costa A, Martínez L, Roser R, Sagarra R, Sánchez J
Department of Clinical Research, Laboratorios Dr. Esteve, Barcelona, Spain.
J Clin Pharmacol. 1992 Dec;32(12):1115-9.
Droxicam is a nonsteroidal anti-inflammatory drug that is a pro-drug of piroxicam. The influence of concomitant administration of antacid or ranitidine on droxicam pharmacokinetics has been investigated. On three separate phases, 15 healthy volunteers received a single oral 20-mg dose of droxicam either alone, with antacid (400 mg aluminum hydroxide + 400 mg magnesium hydroxide, three times/day), or with ranitidine (300 mg, two times/day) for 6 days. Piroxicam, the active substance from droxicam, was quantified by high-performance liquid chromatography. The pharmacokinetic parameters for droxicam given alone were: maximum peak plasma concentration (Cmax) = 1.53 +/- .21 micrograms/mL (mean +/- SD), time to peak concentration (Tmax) = 7.5 +/- 2.1 hr, t1/2a = 1.38 +/- .82 hour, t1/2el = 53.3 +/- 11.9 hr, Cl/F = 2.98 +/- .71 mL/min, volume of distribution (Vd/F) = 13.2 +/- 1.8 L and area under the curve (AUC) = 117.6 +/- 26.8 micrograms/hour/mL. The subject effect was significant for all the pharmacokinetic parameters except for the absorption half-life (P < .05). Concomitant antacid or ranitidine administration had no significant effect on any of the droxicam pharmacokinetic parameters. The results of this study suggest that antacid or ranitidine do not significantly alter the oral absorption or pharmacokinetic disposition of single-dose droxicam.
屈昔康是一种非甾体抗炎药，是吡罗昔康的前体药物。已研究了抗酸剂或雷尼替丁联合给药对屈昔康药代动力学的影响。在三个不同阶段，15名健康志愿者分别单独、与抗酸剂（400mg氢氧化铝+400mg氢氧化镁，每日三次）或与雷尼替丁（300mg，每日两次）联合口服20mg屈昔康，持续6天。通过高效液相色谱法定量测定屈昔康的活性物质吡罗昔康。单独给予屈昔康的药代动力学参数为：最大血浆峰浓度（Cmax）=1.53±0.21μg/mL（平均值±标准差），达峰浓度时间（Tmax）=7.5±2.1小时，吸收半衰期（t1/2a）=1.38±0.82小时，消除半衰期（t1/2el）=53.3±11.9小时，清除率（Cl/F）=2.98±0.71mL/分钟，分布容积（Vd/F）=13.2±1.8L，曲线下面积（AUC）=117.6±26.8μg/小时/mL。除吸收半衰期外，所有药代动力学参数的个体效应均显著（P<0.05）。联合给予抗酸剂或雷尼替丁对屈昔康的任何药代动力学参数均无显著影响。本研究结果表明，抗酸剂或雷尼替丁不会显著改变单剂量屈昔康的口服吸收或药代动力学特征。
