缓释美沙拉嗪（5-氨基水杨酸）：在回肠造口术患者中的包衣溶解及排泄情况
Delayed-release mesalazine (5-aminosalicylic acid): coat dissolution and excretion in ileostomy subjects.
作者信息
Riley S A, Tavares I A, Bennett A, Mani V
机构信息
University Department of Medicine, Hope Hospital, Salford.
出版信息
Br J Clin Pharmacol. 1988 Aug;26(2):173-7. doi: 10.1111/j.1365-2125.1988.tb03383.x.
Abstract
- Delayed-release mesalazine has been formulated to deliver 5-aminosalicylic acid to the colon. We have therefore studied the ileostomy excretion and coat dissolution of this preparation. 2. Following ingestion of a single tablet 88% (range 69-114%) of the 400 mg dose appeared unchanged in the ileosomy effluent over the subsequent 12 h. 3. Ileostomy effluent pH appeared to be a major determinant of 5-aminosalicylic acid release. 4. In vitro studies revealed rapid coat dissolution above pH 7.0, slow dissolution between pH 6.0 and 7.0 and non-dissolution at pH 2.0 and 4.0.
摘要
- 缓释美沙拉嗪制剂旨在将5-氨基水杨酸输送至结肠。因此，我们对该制剂的回肠造口排泄物及包衣溶解情况进行了研究。2. 服用单片制剂后，在随后12小时内，回肠造口流出物中400毫克剂量的88%（范围为69%-114%）未发生变化。3. 回肠造口流出物的pH值似乎是5-氨基水杨酸释放的主要决定因素。4. 体外研究显示，在pH值高于7.0时包衣迅速溶解，在pH值介于6.0和7.0之间时溶解缓慢，而在pH值为2.0和4.0时不溶解。
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