Das K M, Eastwood M A, McManus J P, Sircus W
Gut. 1973 Aug;14(8):631-41. doi: 10.1136/gut.14.8.631.
The metabolism of salicylazosulphapyridine was studied in 16 patients with ulcerative colitis admitted to hospital. The acetylator phenotype was determined on admission. The mean serum concentration (mug/ml) (at steady state eight +/- two days in patients responding to treatment) of SASP, total SP, and 5-ASA were 18.7 +/- 12.8; 53.7 +/- 23.1; and 1 +/- 0.9 for slow acetylators and 17.6 +/- 7.1; 31 +/- 9.0 and 1 +/- 0.9 for fast acetylators respectively. Twenty-four hour urinary excretion of SASP, total SP, and 5-ASA were 4.6% +/- 3.1; 52% +/- 9.6 and 22.3 +/- 6.7% of the administered dose respectively. Serum total SP concentration of 20 to 50 mug/ml appeared to coincide with clinical improvement in the absence of any side effects related to salicylazosulphapyridine. No such relationship could be shown with serum SASP, individual metabolites, or 5-aminosalicyclic acid.
对16例入院的溃疡性结肠炎患者的柳氮磺胺吡啶代谢情况进行了研究。入院时测定乙酰化表型。慢乙酰化者的柳氮磺胺吡啶（SASP）、总磺胺吡啶（SP）和5-氨基水杨酸（5-ASA）的平均血清浓度（μg/ml）（在对治疗有反应的患者中，稳态时为8±2天）分别为18.7±12.8；53.7±23.1；和1±0.9，快乙酰化者分别为17.6±7.1；31±9.0和1±0.9。SASP、总SP和5-ASA的24小时尿排泄量分别为给药剂量的4.6%±3.1；52%±9.6和22.3±6.7%。血清总SP浓度在20至50μg/ml时，在无任何与柳氮磺胺吡啶相关的副作用的情况下，似乎与临床改善相符。血清SASP、单个代谢物或5-氨基水杨酸之间未显示出这种关系。
