5-氨基水杨酸在人体内的N-乙酰化作用是可逆的吗？
Is N-acetylation of 5-aminosalicylic acid reversible in man?
作者信息
Meese C O, Fischer C, Klotz U
出版信息
Br J Clin Pharmacol. 1984 Oct;18(4):612-5. doi: 10.1111/j.1365-2125.1984.tb02513.x.
Abstract
In two healthy male subjects the disposition of deuterated N-(2H3) acetyl-5-aminosalicylic acid (d3-ac-5-AS) was investigated after a single rectal dose of 500 mg d3-ac-5-AS. Urine and plasma were analysed by h.p.l.c. and gas chromatography mass-spectrometry. Peak concentrations of around 0.5 microgram/ml occurred within 6 h and plasma concentrations declined thereafter with a half-life (t1/2) of about 6 h which was confirmed by urinary excretion data. Renal clearance of d3-ac-5-AS ranged between 200 and 300 ml/min and only 4.4-11.2% of the dose could be recovered in the 48 h urine. Since no undeuterated ac-5-AS could be detected in any of the plasma and urine samples an irreversible acetylation of 5-AS is assumed in man.
摘要
在两名健康男性受试者中，单次直肠给予500毫克氘代N-(2H3)乙酰基-5-氨基水杨酸（d3-ac-5-AS）后，对其处置情况进行了研究。通过高效液相色谱法和气相色谱 - 质谱法分析尿液和血浆。给药后6小时内出现了约0.5微克/毫升的峰值浓度，此后血浆浓度下降，半衰期（t1/2）约为6小时，这一点通过尿排泄数据得到证实。d3-ac-5-AS的肾清除率在200至300毫升/分钟之间，在48小时尿液中仅能回收4.4 - 11.2%的给药剂量。由于在任何血浆和尿液样本中均未检测到未氘代的ac-5-AS，因此推测在人体中5-AS发生了不可逆的乙酰化。
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