Christensen L A, Fallingborg J, Jacobsen B A, Abildgaard K, Rasmussen H H, Rasmussen S N, Hansen S H
Department of Medical Gastroenterology, Aalborg Hospital, Denmark.
Dig Dis Sci. 1993 Oct;38(10):1831-6. doi: 10.1007/BF01296106.
The bioavailability of a controlled release 5-aminosalicyclic acid preparation (Pentasa) was investigated in nine healthy children after a medication period of six days (1000 mg/day) and compared with sulfasalazine (Salazopyrin) (2000 mg/day). The local bioavailability in the distal gut lumen, reflected by the 5-aminosalicylic acid concentration in the fecal water, showed comparable values after Pentasa (4.44 mmol/liter) and Salazopyrin (6.25 mmol/liter). The concentration of N-acetyl-5-ASA was significantly higher after Pentasa, reflecting the more proximal release of 5-aminosalicyclic acid compared with Salazopyrin. No relation was found between the 5-aminosalicylic acid fecal water concentration water concentration and the 5-aminosalicylic acid dose per kilogram of body weight. The urinary excretion of 5-aminosalicylic acid and N-acetyl-5-aminosalicylic acid was higher after Pentasa than after Salazopyrin (32% vs 25%). Dose interval plasma concentration curves showed low values after both preparations. Based on the concept that the fecal water concentration is decisive for the efficacy of 5-aminosalicylic acid in distal inflammatory bowel disease, Pentasa treatment offers a relevant alternative in cases of Salazopyrin intolerance or allergy in children. The higher systemic bioavailability from Pentasa warrants monitoring of the renal function.
在9名健康儿童服用控释5-氨基水杨酸制剂（颇得斯安）6天（1000毫克/天）后，对其生物利用度进行了研究，并与柳氮磺胺吡啶（2克/天）进行了比较。以粪便水中5-氨基水杨酸浓度反映的远端肠腔局部生物利用度，在服用颇得斯安（4.44毫摩尔/升）和柳氮磺胺吡啶（6.25毫摩尔/升）后显示出相当的值。服用颇得斯安后，N-乙酰-5-ASA的浓度显著更高，这反映出与柳氮磺胺吡啶相比，5-氨基水杨酸的释放位置更靠近近端。未发现粪便水5-氨基水杨酸浓度与每千克体重5-氨基水杨酸剂量之间存在关联。服用颇得斯安后，5-氨基水杨酸和N-乙酰-5-氨基水杨酸的尿排泄量高于柳氮磺胺吡啶（32%对25%）。两种制剂的给药间隔血药浓度曲线均显示值较低。基于粪便水浓度对远端炎症性肠病中5-氨基水杨酸疗效起决定性作用这一概念，在儿童对柳氮磺胺吡啶不耐受或过敏的情况下，颇得斯安治疗提供了一种相关的替代方案。颇得斯安较高的全身生物利用度需要监测肾功能。
