Ofori-Kwakye Kwabena, Fell John T, Sharma Harbans L, Smith Anne-Marie
School of Pharmacy and Pharmaceutical Sciences, University of Manchester, Manchester M13 9PL, UK.
Int J Pharm. 2004 Feb 11;270(1-2):307-13. doi: 10.1016/j.ijpharm.2003.11.009.
The gastrointestinal transit and in vivo drug release behaviour of a film-coated tablet formulation was investigated in five healthy human subjects using the technique of gamma scintigraphy. The film coating system consisted of a mixture of pectin, chitosan and HPMC in a ratio of 6:1:0.37 applied to 750 mg cores at a coat weight gain of 9%. The estimated mean values of the gastric emptying time (62+/-17 min), small intestinal transit time (219+/-53 min), ileocaecal junction lag time (79+/-30 min) and the colon arrival time (345+/-33 min), were similar to published values for the transit of similar sized tablets in humans. The amount of radioactive tracer released from the labelled tablets was minimal when the tablets were in the stomach and the small intestine. There was increased release of radioactivity when the tablets were in the colon due to increased degradation of the film coatings by pectinolytic enzymes resident in the colon. The pectin/chitosan/HPMC film coating system thus acts as a colonic delivery system.
采用γ闪烁扫描技术，在5名健康人体受试者中研究了薄膜包衣片剂制剂的胃肠道转运及体内药物释放行为。薄膜包衣系统由果胶、壳聚糖和羟丙基甲基纤维素按6:1:0.37的比例混合而成，以9%的包衣增重施加于750mg片芯上。胃排空时间（62±17分钟）、小肠转运时间（219±53分钟）、回盲部连接滞后时间（79±30分钟）和结肠到达时间（345±33分钟）的估计平均值与已发表的类似大小片剂在人体中转运的数值相似。当片剂位于胃和小肠中时，从标记片剂中释放的放射性示踪剂数量极少。当片剂位于结肠中时，由于结肠中存在的果胶分解酶使薄膜包衣降解增加，放射性释放增加。因此，果胶/壳聚糖/羟丙基甲基纤维素薄膜包衣系统可作为一种结肠给药系统。
