Leopold C S
Institut für Pharmazeutische Technologie, Heinrich-Heine-Universität Düsseldorf.
Med Klin (Munich). 1999 Feb 15;94 Suppl 1:6-11. doi: 10.1007/BF03042026.
Drug delivery to the intestine has become attractive to researchers with the main interest in the delivery of peptide drugs to the large intestine and the treatment of colonic diseases. There are currently 4 strategies that are pursued to reach colon specificity: 1. by relying on the pH difference between the small and the large intestine; 2. by exploiting the enzymatic activity of the colonic microflora; 3. by relying on the relatively constant small intestinal transit time and 4. by taking advantage of the increase of the luminal pressure in the colon due to strong peristaltic waves. Drug delivery to the small intestine may be achieved by pH-controlled and time-controlled drug release mechanisms. Diffusion-controlled systems allow drug delivery over the entire gastrointestinal tract.
药物递送至肠道已引起研究人员的关注,其主要兴趣在于将肽类药物递送至大肠以及治疗结肠疾病。目前有4种实现结肠特异性的策略:1. 依靠小肠和大肠之间的pH差异;2. 利用结肠微生物群的酶活性;3. 依靠相对恒定的小肠转运时间;4. 利用强烈蠕动波导致的结肠腔内压力增加。通过pH控制和时间控制的药物释放机制可实现药物递送至小肠。扩散控制型系统可使药物在整个胃肠道中释放。