美沙拉嗪结肠靶向制剂研究进展  

Progress of colon targeted mesalamine formulations

作　　者：赵亚绘 张赫然[2] 王彦竹[2] 宋丽明[2] 王杏林[2] 田沛[1,2] 

机构地区：[1]天津医科大学,天津300070 [2]天津药物研究院有限公司释药技术与药代动力学国家重点实验室,天津300193

出　　处：《中国新药杂志》2015年第12期1387-1392,共6页Chinese Journal of New Drugs

基　　金：国家"重大新药创制"科技重大专项(2014ZX09507005-001)

摘　　要：美沙拉嗪是近30年来活动期轻中度溃疡性结肠炎的首选用药,具很好的诱导缓解和维持缓解功效。美沙拉嗪只有以原型形式到达结肠病变部位才能发挥治疗效果,而常规制剂口服后迅速被胃肠吸收经肝脏代谢,易产生腹痛、腹泻、肾毒性等不良反应,仅少量到达结肠,已上市结肠靶向美沙拉嗪则极易在小肠过早释药,结肠定位效果较差,因此新型精确美沙拉嗪结肠靶向制剂的研究至关重要。本文主要综述了近年来美沙拉嗪结肠靶向制剂的研究进展,以期为无毒、生物相容、生物可降解、精准结肠靶向的高剂量美沙拉嗪制剂的开发提供参考依据。As the first-line treatment therapy for active mild to moderate ulcerative colitis in the last thirty years, mesalamine is efficacious in inducing and maintaining remission of ulcerative colitis patients. Only in the prototype form can mesalamine play a therapeutic role on the inflamed colonic mucosa, while conventional me- salamine formulations are rapidly absorbed by gastrointestinal tract and metabolized by liver following oral adminis- tration which remain little at the colon inflamed target site and lead to abdominal pain, diarrhea, nephrotoxicity and other adverse reactions, furthermore, most of the marketed colon targeted mesalamine preparations are apt to release in the small intestine, therefore it is essential to develop novel formulation approaches enabling accurate site-specif- ic delivery of mesalamine to the colon. This article focuses exclusively on the latest progress of colon targeted me- salamine formulations, to provide a reference for the development of non-toxic, biocompatible, biodegradable, high-dose and precise colon-specific mesalazine formulations.

关 键 词：美沙拉嗪 溃疡性结肠炎 结肠靶向 生物相容 生物降解 

分 类 号：R975[医药卫生—药品]