Truelove S C
Gastroenterology Unit Radcliffe Infirmary, Oxford, U.K.
Scand J Gastroenterol Suppl. 1988;148:3-6. doi: 10.3109/00365528809101538.
Sulphasalazine was first produced nearly 50 years ago through the inspiration of a Swedish doctor, Dr Nanna Svartz. Later, in controlled trials, this compound was shown to reduce substantially the frequency of recurrent attacks of ulcerative colitis when used as long-term maintenance therapy. Studies into the metabolism of sulphasalazine have shown that, when taken orally, most of the ingested dose reaches the colon intact, and within the colonic lumen, bacteria split sulphasalazine into two breakdown products, sulphapyridine and 5-ASA. 5-ASA was shown to be the active therapeutic moiety while sulphapyridine served simply as a carrier. Olsalazine was developed to retain the property of sulphasalazine of reaching the colon intact, but also to liberate two molecules of 5-ASA with no residual carrier.
柳氮磺胺吡啶是近50年前在瑞典医生南娜·斯瓦尔茨博士的启发下首次生产出来的。后来，在对照试验中，这种化合物被证明在用作长期维持治疗时，能大幅降低溃疡性结肠炎复发的频率。对柳氮磺胺吡啶代谢的研究表明，口服时，大部分摄入剂量完整地到达结肠，在结肠腔内，细菌将柳氮磺胺吡啶分解为两种分解产物，磺胺吡啶和5-氨基水杨酸。5-氨基水杨酸被证明是活性治疗部分，而磺胺吡啶仅作为载体。奥沙拉嗪的研发目的是保留柳氮磺胺吡啶完整到达结肠的特性，同时释放出两分子5-氨基水杨酸且无残留载体。
