Kinget R, Kalala W, Vervoort L, van den Mooter G
Laboratorium voor Farmacotechnologie en Biofarmacie, Katholieke Universiteit Leuven, Belgium.
J Drug Target. 1998;6(2):129-49. doi: 10.3109/10611869808997888.
Specific targeting of drugs to the colon is recognized to have several therapeutic advantages. Drugs which are destroyed by the stomach acid and/or metabolized by pancreatic enzymes are slightly affected in the colon, and sustained colonic release of drugs can be useful in the treatment of nocturnal asthma, angina and arthritis. Treatment of colonic diseases such as ulcerative colitis, colorectal cancer and Crohn's disease is more effective with direct delivery of drugs to the affected area. Likewise, colonic delivery of vermicides and colonic diagnostic agents require smaller doses. This article is aimed at providing insight into the design considerations and evaluation of colonic drug delivery systems. For this purpose, the anatomy and physiology of the lower gastrointestinal tract are surveyed. Furthermore, the biopharmaceutical aspects are considered in relation to drug absorption in the colon and hence various approaches to colon-specific drug delivery are discussed.
将药物特异性靶向输送至结肠具有多种治疗优势，这已得到公认。那些会被胃酸破坏和/或被胰酶代谢的药物在结肠中受到的影响较小，药物在结肠中的持续释放可用于治疗夜间哮喘、心绞痛和关节炎。将药物直接输送到受影响区域，对溃疡性结肠炎、结直肠癌和克罗恩病等结肠疾病的治疗更为有效。同样，结肠给药驱虫剂和结肠诊断剂所需剂量更小。本文旨在深入探讨结肠给药系统的设计考量和评估方法。为此，对下消化道的解剖学和生理学进行了综述。此外，还结合结肠中的药物吸收对生物药剂学方面进行了考量，进而讨论了各种结肠特异性给药方法。
