Busch U, Heinzel G, Narjes H
Department of Pharmacokinetics, Karl Thomae GmbH, Biberach, Germany.
Eur J Clin Pharmacol. 1995;48(3-4):269-72. doi: 10.1007/BF00198310.
The influence of multiple oral doses of cholestyramine on the single dose pharmacokinetics of meloxicam has been studied in 12 healthy male volunteers. Each subject received on two occasions a single IV injection of meloxicam 30 mg. The cholestyramine group received the material suspended in water 3 times a day. Compared to controls, cholestyramine accelerated the elimination of meloxicam. The mean terminal phase elimination half-life was reduced from 19.5 h to 12.7 h due to an increase in clearance of the drug (0.426 vs 0.636 l.h-1). Also, as a consequence of increased clearance in the presence of cholestyramine, the mean residence time of the drug in the body was significantly decreased (39%) P < 0.01. However, the volume of distribution for meloxicam was largely unaffected by cholestyramine which suggests that meloxicam undergoes gut recirculation. These changes are of the same magnitude as those previously reported for the structurally related piroxicam and are much smaller than those observed for tenoxicam.
在12名健康男性志愿者中研究了多次口服考来烯胺对美洛昔康单剂量药代动力学的影响。每位受试者分两次接受30毫克美洛昔康的单次静脉注射。考来烯胺组每天3次接受混悬于水中的该物质。与对照组相比,考来烯胺加速了美洛昔康的消除。由于药物清除率增加(0.426对0.636升·小时⁻¹),平均终末相消除半衰期从19.5小时缩短至12.7小时。此外,由于考来烯胺存在时清除率增加,药物在体内的平均驻留时间显著缩短(39%),P<0.01。然而,美洛昔康的分布容积在很大程度上不受考来烯胺影响,这表明美洛昔康会发生肠肝循环。这些变化与先前报道的结构相关药物吡罗昔康的变化幅度相同,且远小于替诺昔康所观察到的变化。