结肠菌群激活性结肠定位给药系统设计的生物药剂学思考

Biopharmaceutical Considerations in the Design of Colon-Specific Drug Delivery Systems Activated by Colonic Microflora

由于结肠菌群的存在与胃肠通过时间、pH以及疾病状况无关,因此,结肠菌群依赖性非淀粉多糖发酵是实现结肠定位给药的一种普遍触发机制。现已就这种给药系统设计出了结肠定位骨架片和结肠定位薄膜包衣两种释药平台。本文分析评价了这两种释药平台的体内崩解特性,并试图阐明哪种释药平台更适于结肠定位给药。此外,还简要介绍了与结肠释药有关的结肠生理参数。

The fermentation of nonstarch polysaccharides by colonic microflora is popular as a triggering mechanism to achieve a colon-specific drug delivery in that the existence of colonic microflora is independent of gastrointestinal transit time, pH, and disease conditions. Such delivery systems have been designed in two platforms： matrix tablets and film-coating. The objective of this article is to analyze and evaluate the in vivo disintegration characteristics of these systems from published reports and attempt to elucidate which strategy would be preferable in achieving colon-specific drug delivery. A brief description of physiological parameters of the colon relevant to colonic drug release is also presented.