咪唑硫嘌呤药物动力学后静脉注射、口服、延迟释放口服和直肠泡沫管理。
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范Os EC,寻BJ, Sandborn WJ,梅斯,屈里曼WJ, Mahoney DW, Zinsmeister AR,利普斯基JJ
咪唑硫嘌呤药物动力学后静脉注射、口服、延迟释放口服和直肠泡沫管理。
肠道。1996年7月,39 (1):63 - 8。doi: 10.1136 / gut.39.1.63。
- PubMed ID
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8881811 (在PubMed]
- 文摘
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背景:6 -巯基嘌呤及其前体药物用药是耐火炎症性肠病的有效药物。然而,使用这些药物是有限的对其毒性的担忧。结肠的用药可能会减少其系统性的生物利用度和毒性限制。目的:确定的生物利用度6 -巯基嘌呤后通过三个结肠交付配方用药管理。方法:24个健康人体每个收到50毫克的咪唑硫嘌呤四交付配方(每n = 6):口服;延迟发布口头;疏水性泡沫直肠;和亲水性直肠泡沫。所有科目也收到了50毫克剂量的另一项研究期间静脉用药。等离子体浓度的6 -巯基嘌呤高压液相色谱法测定。 RESULTS: The bioavailabilities of 6-mercaptopurine after colonic azathioprine administration via delayed release oral, hydrophobic rectal foam, and hydrophilic rectal foam (7%, 5%, 1%; respectively) were significantly lower than the bioavailability of 6-mercaptopurine after oral azathioprine administration (47%) by Wilcoxon rank sum pairwise comparison. CONCLUSIONS: Azathioprine delivered to the colon by delayed release oral and rectal foam formulations considerably reduced systemic 6-mercaptopurine bioavailability. The therapeutic potential of these colonic delivery methods, which can potentially limit toxicity by local delivery of high doses of azathioprine, should be investigated in patients with inflammatory bowel disease.
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- 药物