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[部位特异性给药系统。I. 结肠靶向给药]

[Site-specific drug delivery systems. I. Colon targeted delivery].

作者信息

Szente Virág, Zelkó Romána

机构信息

Semmelweis Egyetem, Egyetemi Gyógyszertár Gyógyszerügyi Szervezési Intézet, Budapest.

出版信息

Acta Pharm Hung. 2007;77(3):185-9.

Abstract

Colon specific drug delivery has gained increased importance not just for the delivery of the drugs for the treatment of local diseases associated with the colon like Chron's disease, ulcerative colitis, irritable bowel syndrome, cancer or infections, but also for the potential it holds for the systemic delivery of proteins (e.g. insulin) and therapeutic peptides. These systems enable the protection of healthy tissues from the side effects of drugs and the drug intake of targeted cells, as well. The formulation of colon specific drug delivery systems is of great impact in the case of diseases having circadian rhythm (midnight gerd). Such circadian rhythm release drug delivery systems are designed to provide a plasma concentration--time profile, which varies according to physiological need at different times during the dosing period, i.e., mimicking the circadian rhythm and severity/manifestation of gastric acid secretion (and/or midnight gerd). In general four primary approaches have been proposed for colon targeted delivery namely pH-dependent systems, time dependent systems, colonic microflora activated systems and prodrugs.

摘要

结肠特异性药物递送不仅对于递送用于治疗与结肠相关的局部疾病(如克罗恩病、溃疡性结肠炎、肠易激综合征、癌症或感染)的药物变得越来越重要,而且对于其在蛋白质(如胰岛素)和治疗性肽的全身递送方面的潜力也很重要。这些系统能够保护健康组织免受药物副作用的影响,同时也能使靶向细胞摄取药物。对于具有昼夜节律的疾病(午夜胃食管反流病),结肠特异性药物递送系统的制剂具有重大影响。这种昼夜节律释放药物递送系统旨在提供一种血浆浓度-时间曲线,该曲线根据给药期间不同时间的生理需求而变化,即模拟昼夜节律以及胃酸分泌(和/或午夜胃食管反流病)的严重程度/表现。一般来说,已经提出了四种用于结肠靶向递送的主要方法,即pH依赖性系统、时间依赖性系统、结肠微生物群激活系统和前体药物。

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