O'Neill P J, Yorgey K A, Renzi N L, Williams R L, Benet L Z
J Clin Pharmacol. 1982 Oct;22(10):470-6. doi: 10.1002/j.1552-4604.1982.tb02637.x.
Five healthy male human subjects were administered 200 mg oral solution doses of zomepirac-14C sodium. Plasma and urine samples were analyzed for zomepirac, hydroxyzomepirac, and zomepirac glucuronide. Zomepirac was the major circulating compound, with zomepirac glucuronide and hydroxyzomepirac accounting for the remainder of the radioactivity. Elimination half-lives for zomepirac, zomepirac glucuronide, and hydroxyzomepirac were 7.6, 8.2, and 7.8 hours, respectively. The dose was completely recovered in the urine (95 per cent in 72 hours). Zomepirac glucuronide constituted up to 90 per cent of the urinary radioactivity, with zomepirac and hydroxyzomepirac about 5 per cent each. The urinary zomepirac was probably present as a result of hydrolysis of zomepirac glucuronide. The plasma clearance of zomepirac was 189 +/- 23 ml/min. The metabolites were cleared by the kidney at rates of 343 +/- 88 ml/min (zomepirac glucuronide) and 339 +/- 88 ml/min (hydroxyzomepirac). Thus, metabolic clearance appears to be the sole mode of zomepirac elimination. The metabolites are then rapidly cleared by the kidneys.
对五名健康男性受试者口服给予200mg的唑美匹拉克-14C钠溶液剂。分析血浆和尿液样本中的唑美匹拉克、羟基唑美匹拉克和唑美匹拉克葡糖醛酸化物。唑美匹拉克是主要的循环化合物，唑美匹拉克葡糖醛酸化物和羟基唑美匹拉克占其余的放射性。唑美匹拉克、唑美匹拉克葡糖醛酸化物和羟基唑美匹拉克的消除半衰期分别为7.6、8.2和7.8小时。给药剂量在尿液中完全回收（72小时内回收95%）。唑美匹拉克葡糖醛酸化物占尿液放射性的比例高达90%，唑美匹拉克和羟基唑美匹拉克各约占5%。尿液中的唑美匹拉克可能是由于唑美匹拉克葡糖醛酸化物水解所致。唑美匹拉克的血浆清除率为189±23ml/min。代谢物经肾脏清除的速率分别为343±88ml/min（唑美匹拉克葡糖醛酸化物）和339±88ml/min（羟基唑美匹拉克）。因此，代谢清除似乎是唑美匹拉克消除的唯一方式。然后代谢物迅速经肾脏清除。
