Christensen L A, Slot O, Sanchez G, Boserup J, Rasmussen S N, Bondesen S, Hansen S H, Hvidberg E F
Br J Clin Pharmacol. 1987 Mar;23(3):365-9. doi: 10.1111/j.1365-2125.1987.tb03061.x.
The influence of intestinal transit time on the release of 5-aminosalicylic acid (5-ASA) from a peroral, slow-release preparation (Pentasa) was studied at steady state in seven healthy volunteers. Daily dose was 1500 mg Pentasa, normal transit time (NTT) was 24 h (16-26 h) and accelerated transit time (ATT), caused by a laxative, was 5 h (4-9 h). Median total recovery (24 h, 5-ASA + acetyl-5-ASA) was 87% (61-129%) (NTT) and 81% (56-100%) (ATT), respectively, (P greater than 0.10). The total faecal excretion of 5-ASA (per cent of dose) increased from 16%, (9-21%) (NTT) to 29%, (16-38%) (ATT) (P less than 0.02). Free 5-ASA rose from 12% (4-19%) to 17% (10-25%), the retained part (in granules) from 4% (2-5%) to 12% (4-24%). Urinary excretion decreased correspondingly from 32% (19-59%) to 21% (11-38%), predominantly as Ac-5-ASA (P less than 0.05). Mean plasma Ac-5-ASA concentration decreased from 1.42 micrograms ml-1 to 0.86 microgram ml-1 (P less than 0.05). An almost complete release of 5-ASA from Pentasa takes place during NTT. At ATT conditions about 88% is released, indicating Pentasa to be an acceptable source of 5-ASA in diarrhoeal states.
在7名健康志愿者中，在稳态条件下研究了肠道转运时间对口服缓释制剂（颇得斯安）中5-氨基水杨酸（5-ASA）释放的影响。每日剂量为1500mg颇得斯安，正常转运时间（NTT）为24小时（16 - 26小时），由泻药引起的加速转运时间（ATT）为5小时（4 - 9小时）。5-ASA总量（24小时，5-ASA + 乙酰-5-ASA）的回收率中位数分别为87%（61 - 129%）（NTT）和81%（56 - 100%）（ATT），（P大于0.10）。5-ASA的粪便总排泄量（占剂量的百分比）从16%（9 - 21%）（NTT）增加到29%（16 - 38%）（ATT）（P小于0.02）。游离5-ASA从12%（4 - 19%）升至17%（10 - 25%），保留部分（在颗粒中）从4%（2 - 5%）升至12%（4 - 24%）。尿液排泄相应地从32%（19 - 59%）降至21%（11 - 38%），主要是乙酰-5-ASA（P小于0.05）。血浆中乙酰-5-ASA的平均浓度从1.42μg/ml降至0.86μg/ml（P小于0.05）。在正常转运时间内，颇得斯安中的5-ASA几乎完全释放。在加速转运时间条件下，约88%的药物释放，表明颇得斯安在腹泻状态下是5-ASA的可接受来源。
