Hardy J G, Healey J N, Reynolds J R
Department of Medical Physics, Queen's Medical Centre, Nottingham.
Aliment Pharmacol Ther. 1987 Aug;1(4):273-80. doi: 10.1111/j.1365-2036.1987.tb00627.x.
Gastrointestinal transit of an enteric coated delayed release 5-aminosalicylic acid tablet radiolabelled with 111indium has been monitored in a total of 13 patients with Crohn's disease and ulcerative colitis. More than 70% of the tablets disintegrated in the small intestine, on average 3.2 hours after emptying from the stomach. Dispersed preparation was detected in the proximal colon of all the patients, except one with an ileostomy. Mean peak plasma concentrations of 5-aminosalicylic acid and its metabolite acetyl-5-aminosalicylic acid occurred 3-4 hours after gastric emptying. The tablets provide a reliable means of drug delivery to the ileum and proximal colon.
用111铟标记的肠溶包衣缓释5-氨基水杨酸片在13例克罗恩病和溃疡性结肠炎患者中进行了胃肠道转运监测。超过70%的片剂在小肠崩解,平均在胃排空后3.2小时。除1例回肠造口术患者外,所有患者的近端结肠均检测到分散制剂。5-氨基水杨酸及其代谢物乙酰-5-氨基水杨酸的平均血浆峰值浓度在胃排空后3-4小时出现。该片剂为药物输送至回肠和近端结肠提供了一种可靠的方法。