文摘

慢性炎症性肠病的主要积极抗炎一半是5-aminosalicylic酸(5-ASA)。作为保护5-ASA正迅速在上消化道吸收一些缓释制剂开发允许通过5-ASA降低小肠和结肠。调查腔的动力学和程度的释放5-ASA管腔内的浓度和加载的复合在一起的主要代谢物acetyl-5-aminosalicylic酸(ac-5-ASA)进行了研究,超过15小时后给缓释制剂Salofalk 500毫克的剂量口服一起测试。等离子体浓度和尿排泄也测量。六个健康志愿者11管腔oroileal吞噬,使得标记灌注,渴望从十二指肠腔的内容,mid-jejunum,回肠,肠道蠕动的记录。清空5-ASA进入十二指肠排空后开始吃饭,一起interdigestive第III期的能动性。意味着5-ASA腔的浓度和ac-5-ASA不断增加十二指肠(既:15到30微克/毫升),回肠(60至110微克/毫升和80 - 150微克/毫升)超过三小时,减少在接下来的三个小时。在10小时后吃,30%的总剂量在溶液中通过回肠和另一个10%是随着尿液排出。因此约60%达到结肠未释放的平板电脑和另一个30%的解决方案。5-ASA和ac-5-ASA解决方案的比例是1:1的十二指肠和1:1.5 1:2越远端小肠。 The data suggest that the large quantities of intraluminal ac-5-ASA are generated in the intestinal mucosa and reach the lumen by back diffusion. The results show that most of the 5-ASA from this slow release preparation is delivered into the colon, which explains its effectiveness in ulcerative colitis. The considerable luminal concentrations already present in the distal ileum might justify therapeutic trials in Crohn's disease.