Haderslev K V, Sonne J, Poulsen H E, Loft S
Department of Gastroenterology and Internal Medicine F, Gentofte University Hospital, Denmark.
Br J Clin Pharmacol. 1998 Nov;46(5):513-6. doi: 10.1046/j.1365-2125.1998.00808.x.
The capacity for sulphation of phenols appears to be impaired in the colonic mucosa of patients with ulcerative colitis. The aim of the present study was to investigate the systemic capacity for sulphation of phenols in patients with ulcerative colitis assessed by the metabolic clearances of paracetamol to the sulphate, glucuronide and glutathione derived metabolites.
Ten patients with ulcerative colitis and 10 control subjects received a single oral dose of paracetamol (1 g). Venous blood samples were collected frequently for pharmacokinetic determinations (one compartment model). Urine was collected for 24 h. Plasma samples were analysed for parent drug and urine samples for parent drug and metabolites by h.p.l.c. Partial metabolic clearances were calculated as the fractional urinary recovery of each conjugate multiplied by the apparent oral clearance of paracetamol.
The apparent oral clearance of paracetamol and the partial clearances of its metabolites were not significantly different between the two study groups. Median value and the corresponding 25th and 75th percentiles for the clearance of the sulphate metabolites were 93.6 (82.5-138.8) ml kg(-1)h(-1) and 77.4 (75.5-99.1), patients with ulcerative colitis and control subjects, respectively.
These results do not indicate a general impairment of the systemic capacity for sulphation of paracetamol in patients with ulcerative colitis.
溃疡性结肠炎患者结肠黏膜中酚类硫酸化能力似乎受损。本研究的目的是通过对乙酰氨基酚向硫酸盐、葡萄糖醛酸和谷胱甘肽衍生代谢物的代谢清除率来评估溃疡性结肠炎患者酚类的全身硫酸化能力。
10例溃疡性结肠炎患者和10例对照受试者口服单剂量对乙酰氨基酚（1g）。频繁采集静脉血样用于药代动力学测定（一室模型）。收集24小时尿液。通过高效液相色谱法分析血浆样本中的母体药物以及尿液样本中的母体药物和代谢物。部分代谢清除率计算为每种结合物的尿回收率分数乘以对乙酰氨基酚的表观口服清除率。
两个研究组之间对乙酰氨基酚的表观口服清除率及其代谢物的部分清除率无显著差异。溃疡性结肠炎患者和对照受试者硫酸盐代谢物清除率的中位数及相应的第25和第75百分位数分别为93.6（82.5 - 138.8）ml·kg⁻¹·h⁻¹和77.4（75.5 - 99.1）。
这些结果并未表明溃疡性结肠炎患者对乙酰氨基酚全身硫酸化能力普遍受损。
