McGirr Matthew E A, McAllister S Mark, Peters Erin E, Vickers Ann W, Parr Alan F, Basit Abdul W
Department of Pharmaceutics, The School of Pharmacy, University of London, 29/39 Brunswick Square, London, WC1N 1AX, UK.
Eur J Pharm Sci. 2009 Mar 2;36(4-5):386-91. doi: 10.1016/j.ejps.2008.11.007. Epub 2008 Nov 21.
The aims of this study were two-fold; first to report on the use of the novel InteliSite Companion device to deliver material to the colon, and second to use this new technology to assess the potential of mucoadhesive polymers to be retained in the large intestine. In this three-way crossover study in beagle dogs, two mucoadhesive polymers and a non-mucoadhesive polymer were remotely delivered in powder form to the colon. The retention of 150mg doses of the radiolabelled mucoadhesive polymers Carbopol 980 and polycarbophil AA-1, and the retention of ethylcellulose (control) in the colon of three canines was examined using gamma scintigraphy. The InteliSite Companion device had a mean gastric emptying time of 1.0+/-0.8h and a mean caecal arrival time of 2.3+/-1.0h. The device was remotely activated to expel the polymers at the caecum. Although incomplete release was noted with all polymers, Carbopol 980 was found to have increased retention in the proximal colon of all three dogs. The mean retention time within the proximal colon for Carbopol 980 (15.3+/-1.4h) was significantly higher than that of polycarbophil AA-1 (10.0+/-5.7h) and the control (7.1+/-1.4h) (p<0.05). The increased colon retention time demonstrated by Carbopol 980 may be suggestive of a mucoadhesive effect.
其一，报告新型InteliSite Companion装置用于向结肠输送物质的情况；其二，利用这项新技术评估黏膜黏附聚合物在大肠中留存的可能性。在这项针对比格犬的三交叉研究中，两种黏膜黏附聚合物和一种非黏膜黏附聚合物以粉末形式被远程输送至结肠。使用γ闪烁扫描法检测了三只犬结肠中150mg放射性标记的黏膜黏附聚合物卡波姆980和聚卡波非AA - 1的留存情况，以及乙基纤维素（对照）的留存情况。InteliSite Companion装置的平均胃排空时间为1.0±0.8小时，平均盲肠到达时间为2.3±1.0小时。该装置在盲肠处被远程激活以排出聚合物。尽管所有聚合物均出现不完全释放的情况，但发现卡波姆980在所有三只犬的近端结肠中的留存有所增加。卡波姆980在近端结肠中的平均留存时间（15.3±1.4小时）显著高于聚卡波非AA - 1（10.0±5.7小时）和对照（7.1±1.4小时）（p<0.05）。卡波姆980显示出的结肠留存时间增加可能提示存在黏膜黏附效应。
