Campieri M, Lanfranchi G A, Boschi S, Brignola C, Bazzocchi G, Gionchetti P, Minguzzi M R, Belluzzi A, Labò G
Gut. 1985 Apr;26(4):400-5. doi: 10.1136/gut.26.4.400.
5-aminosalicylic acid (5-ASA) is a new treatment for patients suffering from ulcerative colitis but only limited information is available about its rectal absorption. We therefore studied seven patients with ulcerative colitis in remission, and five with active disease to determine acetylated and free 5-ASA plasma concentrations and urinary acetyl 5-ASA after the administration of three different types of enemas: (2 g 5-ASA/100 ml, 4 g/100 ml, and 200 ml). In patients in remission urinary acetyl 5-ASA excretion was dose and volume dependent (p less than 0.01; p less than 0.05) but this correlation was absent in active disease. Because aminosalicylates are usually eliminated through the kidney, these low values (10% in active disease and 19% in those in remission) suggest that the beneficial action may be local. Urinary recovery was significantly lower in patients with active disease (p less than 0.01; p less than 0.02). No accumulation of 5-ASA was found in plasma after repeated daily administration.
5-氨基水杨酸(5-ASA)是治疗溃疡性结肠炎患者的一种新疗法,但关于其直肠吸收的信息有限。因此,我们研究了7例缓解期溃疡性结肠炎患者和5例活动期患者,在给予三种不同类型的灌肠剂(2g 5-ASA/100ml、4g/100ml和200ml)后,测定乙酰化和游离5-ASA的血浆浓度以及尿乙酰5-ASA。在缓解期患者中,尿乙酰5-ASA排泄量与剂量和体积有关(p<0.01;p<0.05),但在活动期疾病中这种相关性不存在。由于氨基水杨酸盐通常通过肾脏排泄,这些低值(活动期疾病患者为10%,缓解期患者为19%)表明其有益作用可能是局部性的。活动期疾病患者的尿回收率显著较低(p<0.01;p<0.02)。每日重复给药后,血浆中未发现5-ASA蓄积。